About Drugs

News About Drugs

2007-01-27T10:23:00.000-08:00

Good news for About Drugs

Droperidol

2006-09-23T17:15:00.000-07:00

Droperidol (droe-PER-i-dole)is used to reduce the amount of nausea and vomiting you may have after surgery or other procedures.
This medicine is available only with your doctor's prescription, in the following dosage form(s):
Parenteral Injection (U.S. and Canada)

Before Receiving This MedicineIn deciding to use a medicine, the risks of using the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For droperidol, the following should be considered:
Allergies-Tell your doctor if you have ever had any unusual or allergic reaction to droperidol, haloperidol, or similar medicines. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes.
Pregnancy-Droperidol has been used in some pregnant patients. There was no increase in premature births or birth defects when droperidol was used. Droperidol has been used in patients undergoing cesarean section. Newborn babies whose mothers received droperidol did not have an increase in breathing problems.
Breast-feeding-Droperidol passes into breast milk. Breast-feeding is not recommended while you are receiving droperidol.
Children-Droperidol has not been studied in children up to 2 years of age. There is no specific information comparing the use of droperidol in children with use in other age groups. However, based on experience with similar drugs, children may be more likely than older patients to experience side effects after receiving droperidol, such as muscle spasms in the tongue, face, neck, and back, and inability to move the eyes.
Older adults-Older patients may be more likely than younger adult patients to experience dizziness and excessive sleepiness from droperidol. Older patients may also have problems with unusual heartbeats from droperidol
Other medicines-Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking droperidol, it is especially important that your doctor and pharmacist know if you are taking any of the following:
Benzodiazepines (e.g., Valium, Xanax) or Diuretics (e.g., Hydrochlorothiazide, Lasix) or General anesthetics or Intravenous opiates (e.g., Demerol, Morphine)-Droperidol used with these medicines may cause serious heart problems Other medical problems-The presence of other medical problems may affect the use of droperidol. Make sure you tell your doctor if you have any other medical problems, especially:
Age over 65 or Alcoholism or Congestive heart failure or Enlargement of the heart or Hypokalemia (too little potassium in the blood) or Hypomagnesemia (too little magnesium in the blood) or Irregular heartbeat Slow heartbeat-Droperidol may increase the risk of irregular heartbeats Epilepsy-The risk of seizures may be increased Heart disease or Mental depression or Parkinsonism-Droperidol may worsen these conditions Hypovolemia-The risk of dizziness may be increased Liver disease-The risk of side effects may be increased Pheochromocytoma-High blood pressure and rapid heart rate may occur

Proper Use of This MedicineDosing-The dose of droperidol will be different for different patients. Your health care professional will decide on the right amount for you, depending on:
Your age; Your general physical condition; The reason you are receiving droperidol; and Other medicines you are taking or will receive before or after droperidol is given.

Precautions After Receiving This MedicineFor patients going home within a few hours after surgery:
Droperidol and other medicines that may be given during surgery may cause some people to feel drowsy, tired, or weak for up to a few days afterwards. Therefore, for at least 24 hours (or longer if necessary) after receiving this medicine, do not drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert. Unless otherwise directed by your medical doctor, do not drink alcoholic beverages or take other central nervous system (CNS) depressants (medicines that slow down the nervous system, possibly causing drowsiness) for about 24 hours after you have received this medicine. To do so may add to the effects of droperidol. Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies, or colds; sedatives, tranquilizers, or sleeping medicine; prescription pain medicine or narcotics; barbiturates; medicine for seizures; and muscle relaxants.

Side Effects of This MedicineAlong with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
Less common
Anxiety; high blood pressure; restlessness
Rare
Fainting; fever; fixed upward position of the eyeballs; irregular or slow heart rate; spasm of the muscles of the tongue, face, neck, and back; sudden death
Side effects are possible for one or two days after you receive droperidol. During this period of time, check with your doctor if you notice any of the side effects listed above.
Symptoms of overdose
Dizziness; fixed upward position of the eyeballs; restlessness; slowed breathing; spasm of the muscles of the tongue, face, neck, and back
Other side effects may occur that usually do not need medical attention. However, check with your doctor if any of the following side effects continue or are bothersome:
More common
Drowsiness; lightheadedness; rapid heart rate
Other side effects not listed above may also occur in some patients. If you notice any other effects, check with your doctor.

Additional InformationOnce a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, droperidol is used
In certain patients with severe agitation and combativeness To produce sleepiness or drowsiness before surgery or certain procedures
For patients receiving this medicine for severe agitation and combativeness, the dose administered will depend on the degree of agitation and the size of the patient.

New Study Shows How Worms Can Help Screen For New Drugs

2006-07-30T12:17:00.000-07:00

The humble nematode worm could prove invaluable in screening new compounds for active drugs, new research published today suggests.

Soil-dwelling nematodes have a programmed avoidance response to harmful chemicals, which they detect through nerves exposed to their environment. Scientists led by the Wellcome Trust Sanger Institute have genetically modified the worm C. elegans to make human proteins called receptors in these nerves: the modified worms detect and avoid human signalling molecules and drug candidates.

The exciting results, reported today, 20 July 2006, in the open-access journal BMC Biology, promise a simple assay that can be used to screen thousands of compounds for activity against human proteins - a foundation of drug development.

“The worm is a great tool to understand biology,” said Dr Michelle Teng of the Wellcome Trust Sanger Institute, a lead author on the report. “Because we understand it so well - it has a simple well studied nervous system - the role for each nerve has been mapped in detail. We also have a good understanding of the signalling mechanisms in nerves that drive the responses.

“We showed that the biochemical response of the receptors emulated that seen in humans. It is just that, in the worm, the effects of that response are to make them crawl away from the chemical stimulus. This simple response could be used to test many unknown drug candidates.”

Medicines often interact with receptors, which are “sensors” at the surface of cells. The team introduced the somatostatin receptor (Sstr2) and the chemokine receptor 5 (CCR5) in the nerves that respond to environmental cues. Somatostatin is a hormone that mediates a wide range of activities in humans and chemokines play an important role in the immune system. The CCR5 receptor used is also the gateway that HIV/AIDS virus uses to enter cells. Both receptors belong to a receptor family called GPCRs, which represent up to 50% of current drug targets.

The response was specific. In tests, worms responded by avoiding somatostatin or chemokine placed in their paths only when the appropriate receptor was made in the appropriate nerves.

“We have shown that we can hijack the cellular machinery of the worm so that the human receptor proteins drive the avoidance response,” explained Dr John McCafferty, Principal Investigator at the Wellcome Trust Sanger Institute and senior author. “We chose two receptors with widely differing functions in humans. The responses were specific to the compounds we added and could be inhibited in the same way a response in humans could be inhibited.”

The worms could also be desensitized by pre-exposure to somatostatin or chemokine: desensitization is an important part of normal human response, because it ensures that our receptors can recover for a fresh round of stimulus. This is the first time that activation has been programmed in these nerves and the team have shown that the human receptors integrate into the worm signalling machinery.

“Systems exist already to study the response of cells in test-tubes to added compounds,” continued Dr McCafferty. “However, because these are soil-dwelling worms which feed on bacteria, we could test crude samples for drug candidates. Together, these results make us very optimistic that these models will be widely applicable and that development of a high-throughput system is feasible.”

The team used a rapid sorting system to isolate the genetically modified worms. Although, for this study, worm responses were scored under the microscope, automation could be integrated to achieve a higher rate of testing.

The worm model can also help to define which regions of a novel compound are important for its biological effect, which can be crucial for producing effective drugs. The team were able to use the worm assay to identify four important building blocks within the somatostatin molecule which are known to be necessary for its effect.

"These results show the power of simple organisms such as the worm to help us not only in our understanding of biology but also in the search for new ways to improve healthcare," said Professor Ronald Plasterk, Professor of Developmental Genetics at the University of Utrecht and Director of the Hubrecht Laboratory, in the Netherlands. "It is a nice irony of history that the worm was chosen for biomedical research by Sydney Brenner forty years ago in Cambridge, only a few miles from the Sanger Institute. Then twenty years ago John Sulston started to make a gene map of the animal, and eventually read its sequence as the first of all animal genomes.

“And now a new generation of researchers again in the Cambridge area uses it to test candidate drugs that are immediately relevant to human health."

Publication details
Teng MS et al. (2006) Expression of mammalian GPCRs in C. elegans generates novel behavioural responses to human ligands. BMC Biology 4:22 doi:10.1186/1741-7007-4-22

Non-steroidal anti-inflammatory drugs

2006-06-29T16:54:00.000-07:00

Non-steroidal anti-inflammatory drugs, usually abbreviated to NSAIDs, are drugs with analgesic, antipyretic and anti-inflammatory effects - they reduce pain, fever and inflammation. The term "non-steroidal" is used to distinguish these drugs from steroids, which (amongst a broad range of other effects) have a similar eicosanoid-depressing, anti-inflammatory action. NSAIDs are sometimes also referred to as non-steroidal anti-inflammatory agents/analgesics (NSAIAs). The most prominent members of this group of drugs are aspirin and ibuprofen. Paracetamol (acetaminophen) has negligible anti-inflammatory activity, and is strictly speaking not an NSAID.
Beginning in 1829, with the isolation of salicylic acid from the folk remedy willow bark, NSAIDs have become an important part of the pharmaceutical treatment of pain (at low doses) and inflammation (at higher doses). Part of the popularity of NSAIDs is that, unlike opioids, they do not produce sedation, respiratory depression, and have a very low addiction rate. NSAIDs, however, are not without their own problems (see below). Certain NSAIDs, including ibuprofen and aspirin, have become accepted as relatively safe and are available over-the-counter without prescription.
Mode of actionMost NSAIDs act as non-selective inhibitors of the enzyme cyclooxygenase, inhibiting both the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes. Cyclooxygenase catalyses the formation of prostaglandins and thromboxane from arachidonic acid (itself derived from the cellular phospholipid bilayer by phospholipase A2). Prostaglandins act (among other things) as messenger molecules in the process of inflammation. This mechanism of action was elucidated by John Vane, who later received a Nobel Prize for his work.
Examples NSAIDs can be broadly classified based on their chemical structure. NSAIDs within a group will tend to have similar characteristics and tolerability. There is little difference in clinical efficacy between the NSAIDs when used at equivalent doses. Rather, differences between compounds tended to be with regards to dosing regimens (related to half-life), route of administration, and tolerability profile. Some more common examples are given below.
Paracetamol (acetaminophen), owing to its inhibitory action on cyclooxygenase, is sometimes grouped together with the NSAIDs. Paracetamol, however, does not have any significant anti-inflammatory properties and is not a true NSAID. Though it has not been clearly elucidated, it is suspected that this lack of anti-inflammatory action may be due to the paracetamol inhibiting cyclooxygenase predominantly in the central nervous system. There is also some speculation that paracetamol acts through the inhibition of the recently discovered COX-3 isoform (see below).
Salicylates * Aspirin* Methyl salicylate* Diflunisal* Banorylate* Faislamine* Amoxiprin
Arylalkanoic acids * Diclofenac* Indomethacin* Sulindac
2-Arylpropionic acids (profens) * Carprofen* Fenoprofen* Flurbiprofen* Ibuprofen* Ketoprofen* Ketorolac* Loxoprofen* Naproxen* Tiaprofenic acid
N-Arylanthranilic acids (fenamic acids) * Mefenamic acid* Meclofenamic acid
Oxicams * Piroxicam* Meloxicam
Coxibs * Celecoxib* Rofecoxib (withdrawn from market)* Valdecoxib (withdrawn from market)* Parecoxib* Etoricoxib
Sulphonanilides * Nimesulide
Uses NSAIDs are usually indicated for the treatment of acute or chronic conditions where pain and inflammation are present. Research continues into their potential for prevention of colorectal cancer, and treatment of other conditions, such as cancer and cardiovascular disease.
NSAIDs are generally indicated for the symptomatic relief of the following conditions: (Rossi, 2006)
* Rheumatoid arthritis* Osteoarthritis* Inflammatory arthropathies (e.g. ankylosing spondylitis, psoriatic arthritis, Reiter's syndrome)* Acute gout* Dysmenorrhoea* Metastatic bone pain* Headache and migraine* Postoperative pain* Mild-to-moderate pain due to inflammation and tissue injury* Pyrexia* Renal colic
Aspirin, the only NSAID able to irreversibly inhibit COX-1, is also indicated for inhibition of platelet aggregation; an indication useful in the management of arterial thrombosis and prevention of adverse cardiovascular events.
In 2001, NSAIDs accounted for 70,000,000 prescriptions and 30 billion over-the-counter doses sold annually in the United States. (Green, 2001). With the aging of the Baby Boomer generation and the associated rise in the incidence of osteoarthritis and other such conditions for which NSAIDs are indicated, the use of NSAIDs may increase further still.
Adverse effects The widespread use of NSAIDs has meant that the adverse effects of these relatively safe drugs have become increasingly prevalent. The two main adverse drug reactions (ADRs), associated with NSAIDs relate to gastrointestinal (GI) effects and renal effects of the agents.
These effects are dose-dependent, and in many cases severe enough to pose the risk of ulcer perforation, upper gastrointestinal bleeding, and death, limiting the use of NSAID therapy. An estimated 10-20% of NSAID patients experience dyspepsia, and NSAID-associated upper gastrointestinal adverse events are estimated to result in 103,000 hospitalizations and 16,500 deaths per year in the United States, and represent 43% of drug-related emergency visits. Many of these events are avoidable; a review of physician visits and prescriptions estimated that unnecessary prescriptions for NSAIDs were written in 42% of visits. (Green, 2001)
Gastrointestinal ADRs The main ADRs associated with use of NSAIDs relate to direct and indirect irritation of the gastrointestinal tract (GIT). NSAIDs cause a dual insult on the GIT - the acidic molecules directly irritate the gastric mucosa; and inhibition of COX-1 reduces the levels of protective prostaglandins.
Common gastrointestinal ADRs include: (Rossi, 2006)
* Nausea* Dyspepsia* Gastric ulceration/bleeding* Diarrhoea
Risk of ulceration increases with duration of therapy, and with higher doses. In attempting to minimise GI ADRs, it is prudent to use the lowest effective dose for the shortest period of time, a practice which studies show is not often followed.
There are also some differences in the propensity of individual agents to cause gastrointestinal ADRs. Indomethacin, ketoprofen and piroxicam appear to have the highest prevalence of gastric ADRs, while ibuprofen (lower doses) and diclofenac appear to have lower rates. (Rossi, 2006)
Certain NSAIDs, such as aspirin, have been marketed in enteric-coated formulations which are claimed to reduce the incidence of gastrointestinal ADRs. Similarly, there is a belief that rectal formulations may reduce gastrointestinal ADRs. However, in consideration of the mechanism of such ADRs and indeed in clinical practice, these formulations have not been shown to have a reduced risk of GI ulceration. (Rossi, 2006)
Commonly, gastrointestinal adverse effects can be reduced through suppressing acid production, by concomitant use of a proton pump inhibitor, e.g. omeprazole; or the prostaglandin analogue misoprostol. Misoprostol is itself associated with a high incidence of gastrointestinal ADRs (diarrhoea). While these techniques may be effective, they prove to be expensive for maintenance therapy.
Renal ADRs NSAIDs are also associated with a relatively high incidence of renal ADRs. The mechanism of these renal ADRs is probably due to changes in renal haemodynamics (bloodflow), ordinarily mediated by prostaglandins, which are affected by NSAIDs. Horses are particularly prone to these adverse affects compared to other domestic animal species.
Common ADRs associated with altered renal function include: (Rossi, 2006)
* Salt and fluid retention* Hypertension
These agents may also cause renal impairment, especially in combination with other nephrotoxic agents. Renal failure is especially a risk if the patient is also concomitantly taking an ACE inhibitor and a diuretic - the so-called "triple whammy" effect. (Thomas, 2000)
In rarer instances NSAIDs may also cause more severe renal conditions: (Rossi, 2006)* Interstitial nephritis* Nephrotic syndrome* Acute renal failure* Acute tubular necrosis
Photosensitivity Photosensitivity is a commonly overlooked adverse effect of many of the NSAIDs. (Moore, 2002) It is somewhat ironic that these anti-inflammatory agents may themselves produce inflammation in combination with exposure to sunlight. The 2-arylpropionic acids have proven to be the most likely to produce photosensitivity reactions, but other NSAIDs have also been implicated including piroxicam, diclofenac and benzydamine.
Benoxaprofen, since withdrawn due to its hepatotoxicity, was the most photoactive NSAID observed. The mechanism of photosensitivity, responsible for the high photoactivity of the 2-arylpropionic acids, is the ready decarboxylation of the carboxylic acid moiety. The specific absorbance characteristics of the different chromophoric 2-aryl substituents, affects the decarboxylation mechanism. Whilst ibuprofen is somewhat of an exception, having weak absorption, it has been reported to be a weak photosensitising agent.
During pregnancy NSAIDs are not recommended during pregnancy, particularly during the third trimester. While NSAIDs as a class are not direct teratogens, they may cause premature closure of the fetal ductus arteriosus and renal ADRs in the fetus. Additionally, they are linked with premature birth (Ostensen & Skomsvoll, 2004). Aspirin, however, is used together with heparin in pregnant women with antiphospholipid antibodies (Cervera & Balasch, 2004).
In contrast, paracetamol (acetaminophen) is regarded as being safe and well-tolerated during pregnancy (Graham et al., 2005). Doses should be taken as prescribed, due to risk of hepatotoxicity with overdoses (Wilkes et al, 2005).
Other ADRsCommon ADRs, other than listed above, include: raised liver enzymes, headache, dizziness (Rossi, 2006).
Uncommon ADRs include: heart failure, hyperkalaemia, confusion, bronchospasm, rash (Rossi, 2006).
Newer NSAIDs: selective COX inhibitors COX-2 inhibitors The discovery of COX-2 in 1991 by Daniel L. Simmons at Brigham Young University raised the hope of developing an effective NSAID without the gastric problems characteristic of these agents. It was thought that selective inhibition of COX-2 would result in anti-inflammatory action without disrupting gastroprotective prostaglandins.
COX-1 is a constitutively expressed enzyme with a "house-keeping" role in regulating many normal physiological processes. One of these is in the stomach lining, where prostaglandins serve a protective role, preventing the stomach mucosa from being eroded by its own acid. When non-selective COX-1/COX-2 inhibitors (such as aspirin, ibuprofen, and naproxen) lower stomach prostaglandin levels, these protective effects are lost and ulcers of the stomach or duodenum and potentially internal bleeding can result. COX-2 is an enzyme facultatively expressed in inflammation, and it is inhibition of COX-2 that produces the desirable effects of NSAIDs.
The relatively selective COX-2 inhibiting oxicam, meloxicam, was the first step towards developing a true COX-2 selective inhibitor. Coxibs, the newest class of NSAIDs, can be considered as true COX-2 selective inhibitors, and include celecoxib, rofecoxib, valdecoxib, parecoxib and etoricoxib.
Controversies with COX-2 inhibitors While it was hoped that this COX-2 selectivity would reduce gastrointestinal adverse drug reactions (ADRs), there is little conclusive evidence that this is true. The original study touted by Searle (now part of Pfizer), showing a reduced rate of ADRs for celecoxib, was later revealed to be based on preliminary data - the final data showed no significant difference in ADRs when compared with diclofenac.
Rofecoxib however, which has since been withdrawn, had been shown to produce significantly fewer gastrointestinal ADRs compared to naproxen. (Bombardier et al, 2000). This study, the VIGOR trial, raised the issue of the cardiovascular safety of the coxibs - a statistically insignificant increase in the incidence of myocardial infarctions was observed in patients on rofecoxib. Further data, from the APPROVe trial, showed a relative risk of cardiovascular events of 1.97 versus placebo - a result which resulted in the worldwide withdrawal of rofecoxib in October 2004.
COX-3 inhibitors Simmons also co-discovered COX-3 in 2002 and analyzed this new isozyme's relation to paracetamol (acetaminophen), arguably the most widely used analgesic drug in the world. (Chandrasekharan et al, 2002). The authors postulated that inhibition of COX-3 could represent a primary central mechanism by which these drugs decrease pain and possibly fever.
The clinical ramifications and knowledge of COX isozymes are rapidly expanding and may offer significant hope for future treatments of pain, inflammation, and fever.

Nimesulide

2006-05-29T16:25:00.000-07:00

Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties and a specific mode of action.
Nimesulide is a sulphonanilide analogue; it is not related to conventional NSAIDs, which usually present a carboxyl or hydroxyl functional group.
Nimesulide is proved safe and effective in the symptomatic treatment of a wide range of inflammatory and painful conditions, including osteoarthritis, extra-articular disorders, pain and primary dysmenorrhoea. To date, more than 450 million patients treated since the first introduction of nimesulide on the market in Italy in 1985.
The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.
Nimesulide has been developed and licensed out by Helsinn Healthcare SA, Switzerland, which acquired the exclusive world-wide rights for the drug in 1976. Only Helsinn's official partners market the original product, granting the highest quality thanks to first-rate and controlled manufacturing processes under GMP rules.
Nimesulide is currently marketed in around 50 countries world-wide under different brand names, and it is among the most prescribed NSAIDs. It is available as tablets, suppositories and in some countries also as oral drops and oral suspension

Meloxicam

2006-03-04T10:28:00.000-08:00

Meloxicam is non-steroidal anti-inflammatory drug .
GENERIC NAME: meloxicam
BRAND NAME: Mobic
DRUG CLASS AND MECHANISM: Meloxicam is in a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs) and are used to treat pain and/or inflammation. Prostaglandins are chemicals that contribute to inflammation within joints, and it is the inflammation that leads to the common symptoms of pain, tenderness and swelling associated with arthritis. Meloxicam blocks the enzymes that make prostaglandins (cyclooxygenase 1 and 2) and reduces the levels of prostaglandins. As a result, inflammation and its accompanying symptoms are reduced. Meloxicam was approved for use in April 2000.
PREPARATIONS: Meloxicam is available as a yellow, round, biconvex, uncoated tablet containing meloxicam 7.5 mg or as a yellow, oblong, biconvex, uncoated tablet containing meloxicam 15 mg.
STORAGE: Meloxicam should be stored in a dry place at room temperature, 15-30°C (59-86°F).
PRESCRIBED FOR: Meloxicam is used to treat tenderness, swelling and pain caused by the inflammation of osteoarthritis and rheumatoid arthritis.
DOSING: The lowest effective dose should be used for each patient. Meloxicam therapy usually is started at 7.5 mg daily. Some patients require a dose of 15 mg daily, but this dose should be taken only under the direction of a physician. Meloxicam may be taken with or without food.
DRUG INTERACTIONS: In studies where meloxicam was administered with cimetidine (Tagamet), digoxin (Lanoxin), and methotrexate (Rheumatrex), there were no drug interactions. Meloxicam may interfere with a class of drugs called ACE inhibitors, e.g., captopril (Capoten) and ramipril (Altace) or the water pill, furosemide (Lasix), that are used for controlling high blood pressure,. This may lead to an increase in blood pressure, and as a result, the dose of ACE inhibitor or Lasix may need to be changed when starting or stopping meloxicam.
Meloxicam should be avoided by patients with a history of asthma attacks, hives or other allergic reactions to aspirin or other NSAIDs.
If aspirin is taken with meloxicam there may be an increased risk for developing an ulcer.
Persons who have more than 3 alcoholic beverages per day may be at increased risk of developing stomach ulcers when taking meloxicam or other NSAIDs.
Cholestyramine (Questran), colestipol (Colestid) and colesevelam (Welchol) may decrease the effectiveness of meloxicam by preventing its absorption from the intestine.
Lithium (Eskalith or Lithobid) blood levels may increase or decrease after meloxicam therapy starts or stops. Therefore, both the patient taking lithium and the blood level of lithium need to be evaluated when starting or stopping meloxicam.
Meloxicam should be used with caution in combination with blood thinning medications such as warfarin (Coumadin) because of an increased risk of bleeding.
PREGNANCY: There have been no studies of meloxicam therapy in pregnant women. Meloxicam generally should be avoided during the first and second trimester of pregnancy. Since meloxicam may cause a fetal birth defect called ductus arteriosus (early closure of two major blood vessels of the heart and lung) in the third trimester of pregnancy, meloxicam also should be avoided during this last part of pregnancy.
NURSING MOTHERS: There have been no studies in humans to determine if meloxicam is excreted in breast milk.
SIDE EFFECTS: In general, the most common side effects with NSAIDs are related to the gastrointestinal tract (GI) and include nausea, vomiting, abdominal pain, diarrhea and gas. To prevent these common side effects, it is recommended that most NSAIDs be taken with food or milk. NSAIDs may cause ulcers in the stomach and/or small intestine. A few NSAIDs are designed to be less damaging to the stomach and small intestine, and, therefore, they may be taken with or without food. Meloxicam is an example of one of these NSAIDs, but nevertheless, it should be taken cautiously without food.

Novocain

2006-02-09T04:55:00.000-08:00

Procaine hydrochloride is a local anesthetic used primarily in dentistry. It is primarily known as novocaine, Novacaine, or by the trade name Novocain®.
Procaine was first synthesized in 1905, and was the first injectable man-made local anesthetic used. It was created by the German chemist Alfred Einhorn (1857-1917) who gave the chemical the trade name Novocaine, from the Latin 'Novus' (meaning New) plus 'caine' as in "cocaine". It was introduced into medical use by surgeon Heinrich Braun (1862-1934).
Procaine is rarely used today since more effective (and hypoallergenic) alternatives such as lidocaine (xylocaine) exist. Prior to the discovery of procaine, cocaine was the most commonly used local anesthetic. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine; without the euphoric and addictive qualities of cocaine.
Procaine, an ester anesthetic, is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Allergic reactions to procaine are usually not in response to procaine itself, but to PABA. About 1 in 3000 people have an atypical form of pseudocholinesterase, which doesn't hydrolyze ester anesthetics such as procaine, resulting in a prolonged period of high levels of the anesthetic in the blood and increased toxicity.
Procaine is the primary ingredient in the controversial preparation Gerovital H3, which is claimed by its advocates to remedy many effects of aging. The mainstream medical view is that these claims were seriously studied and discredited in the 1960s.
- Wikipedia

Bromhexin

2006-01-03T16:21:00.000-08:00

Bromhexin hydrochloride
Drug form and composition
4 mg/2 ml in one ampoule; 2 mg in 1 ml solution and4 mg in 5 ml syrup.
Indications
All forms of tracheobronchitis; emphysematous bronchitis, bronchiectasis with inflammatory pulmonary diseases. Prior to and after surgical interventions with general anesthesia, particularly in elderly patients.
The drug has pronounced mycolytic and secretolytic activity. It has a soothing effect on cough and a slight emetic action. The mucolytic effect is associated with depolymerization and splitting of mucoproteins and mucopolysaccharide fibres. It has no effect on intestinal peristalsis. It is quickly absorbed in the gastrointestinal tract and excreted with urine.
Dosage and administration
In adult patients is administered 10 ml syrup, 3-4 times daily. In children older than 10 years the dosage is 10 ml, 3 times daily, and in children from 3 to 10 years - 5 ml, 3 times daily. Contraindications
Hypersensitivity to the drug.
Special warnings and precautions
Transitory gastrointestinal disturbances, perspiration. Irritation with cough is likely to occur during inhalation. The adverse effects are transient. In single cases, it can induce short-term elevation of serum transaminase.
Dosage and administration
Orally: adults - 4 ml of the solution, 3 times daily.Children from 5 to 10 years - 2 ml 3-4 times daily; under 5 years - 20 drops, 3 times daily. Ten drops can be given to breast-fed infants, 2-3 times daily.The treatment usually lasts 3-5 weeks (rarely months) for adults, being considerably shorter for children.Parenterally: 1 ampoule 2-3 times daily is prescribed in severe cases, to be injected s. c., i. m. or i. v., but very slowly (for 2-3 min).Inhalation: the solution is diluted with distilled water in a ration of 1: 1 and inhaled: adults, 2 ml 2-3 times daily (with warmed solution); children, 5-10-20 drops, 1-2 times daily, depending on age. The inhalation can be combined with oral intake of the preparation, which can enhance its action.Supplied
Packages with 10, 50 and 100 ampoules of 4 ml/2 ml (0.2 %).Solution 0.2 % in vials of 40 ml.Syrup 0.08% in vials of 125 ml.
Expiry
3 years.

Progesterone

2005-12-14T21:40:00.000-08:00

Progesterone
Drug form and composition
Solution for injection. One ampoule of 1 ml contains 10 mg Progesterone (10 mg/ml).
Indications
Progesteron is applied in the complex therapy of amenorrhoea; dysfunctional uterine bleedings; insufficiency or dysfunction of corpus luteum.
Dosage and administration
The preparation is applied parenterally in a dosage regimen according to the indications and severity of ovarian dysfunction. In secondary amenorrhoea it is applied intramuscularly in a dose of 5-10 mg daily from 6 to 10 days, before the expected menstruation. In uterine bleedings it is applied intramuscularly in a dose of 5-10 mg daily for 6 consecutive days. In insufficiency or dysfunction of corpus luteum it is applied intramuscularly by 10 mg daily. Usually the therapy continues two weeks but may be prolonged , if necessary, up to 11 weeks of pregnancy.
Contraindications
Supersensitivity to the preparation; acute and chronic liver diseases; cancer of breasts and genital system; thrombophlebitis or thromboembolic diseases; unclear bleedings from urinary and genital tract.
Special warnings and precautions
With due attention, after assessment of the ratio benefit/risk to be applied to patients with cardiovascular insufficiency, disturbed renal function, liver diseases, diabetes, asthma, epilepsy, migraine, patients with nervous and psychic diseases, in anamnesis for passed thromboembolic diseases. Progesteron is not recommended to be prescribed during pregnancy and lactation.
Drug interactions
Progesteron reduces the effect of sulfanylurea antidiabetics, uterotonic drugs, anabolic steroids, gonadotropic hormones of the anterior part of the hypophysis. Its effect is reduced by ampicillin, barbiturates, phenytoinum, rifampicin.
Adverse reactions
During administration of the preparation may be observed nausea, vomiting, diarrhoea, fluid retention, headache, allergic skin reactions, reduced libido, depression, irregular uterine bleeding, changes in blood picture.
Pharmacological mechanisms
Progesteron is a natural hormone, synthesized in corpus luteum and placenta. Uterine and vagina are the target organs for progesteron. Its action is expressed in the luteal phase of ovarian cycle and during pregnancy. Progesteron acts on estrogen-stimulated endometrium and transforms it into secretory. This change is necessary to receive the fertilized ovum and the following implantation of embryo in the early stage. Continuing secretion is necessary to maintain pregnancy. The contractile response of myometrium to oxytocin is inhibited. Provokes vagina desquamation. Stimulates development of secretory alveoli in mammary glands. The increase of basal temperature is connected with progesterone secretion. By the way of reverse connection, progesteron inhibits the release of luteinizing hormone.
Supplied
10 or 50 ampoules of 1ml (10 mg).
Expiry
2 years.

Pilocarpine

2005-12-14T21:33:00.000-08:00

Pilocarpine
rug form and composition
Solution, eye drops. One vial of 10 ml (1%) contains 100 mg of Pilocarpin hydrochloride (10 mg/ml). One vial of 10 ml (2%) contains 200 mg of Pilocarpin hydrochloride (20 mg/ml). Indications
Glaucoma (open angle, closed angle glaucoma, secondary glaucoma); for induction of myosis after surgery and after ophthalmoscopy; before iridectomy.
Dosage and administration
In chronic glaucoma, 1 - 2 drops of Pilocarpin solution (1% or 2%) are applied in the conjunctival sack 2 - 4 times daily, depending on the intraocular pressure. In acute open angle glaucoma, the preparation is used on the conjunctiva in a dose of 1 drop of 1% or 2% solution every 5 to 10 minutes (from 3 to 6 doses) and after that 1 drop every 1 - 3 hours up to the intraocular pressure reduction. For myosis induction the preparation is used on the conjunctiva in a dose of 1 drop 1% or 2% solution.
Contraindications
Hypersensitivity to the drug; iridocyclitis.
Special warnings and precautions
Pilocarpin is used with increased caution in cases of severe heart failure, bronchial asthma, hyperthyroidism, peptic ulcer, disturbed urinary bladder emptying, stenotic changes in the gastrointestinal tract and urinary passages. In pregnancy and lactation, the preparation is used after a strict assessment of the risk/benefit ratio. During the treatment with Pilocarpin there is a possibility of visual disturbances, because of which driving and working with machines should be avoided.
Drug interactions
In chronic interventions should be kept in mind that Pilocarpin potentiates the action of the curare type agents. Atropin and other M-cholinolytics are Pilocarpin antagonists. Combination of the preparation with myotics and adrenomimetics is possible.
Adverse reactions
Myosis; visual disturbances; transitory accommodation spasms, generally disappearing up to the second hour after drug administration; lacrimal secretion increase, conjunctival vasodilation, contact allergy in susceptible patients.
Pharmacological mechanisms
Pilocarpin is a direct parasymatholytic agent and directly acts on the M-cholinoreceptors. When used in the conjunctival sack, myosis and accommodation spasm follow due to stimulation of the cholinoreceptors in m. sphincter pupillae and m. ciliaris. In cases of increased intraocular pressure, lowering of this pressure follows. In the ophthalmology this drug is used widely for the treatment of glaucoma (facilitates of intraocular fluid drainage through the canal of Schlemm) and for improvement of eye trophics. The drug is also used for termination of mydriasis after atropine use. The myosis develops after 15 minutes and lasts for several hours.
Supplied
Vials, containing 10 ml (1%) solution. Vials, containing 10 ml (2%) solution.
Expiry
2 years.

Lidocaine

2005-12-10T22:59:00.000-08:00

Lidocaine
Drug form and composition
Solution for injection. One ampoule of 2 ml (2%) contains 40 mg (20 mg/ml) Lidocaine hydrochloride. One ampoule of 10 ml (0.5%, 1% or 2%) contains 50 mg (5 mg/ml), 100 mg (10 mg/ml), 200 mg (20 mg/ml) Lidocaine hydrochloride respectively.
Indications
Lidocaine hydrochloride is used in different types local anesthesia in surgery, stomatology, urology, cardiology, ophthalmology, otorhinolaryngology, as well as in different invasive diagnostic manipulations. Preventively Lidocain is used in conditions predisposing to cardiac rhythm disorders; in patients with ventricular arrhythmias, particularly those accompanying a myocardial infarction, digitalis intoxication, and cardiac surgery.
Dosage and administration
In patients with cardiac rhythm disorders Lidocain is applied jet intravenously in initial loading dose 1-1.5 mg per kg body weight (mean dose 75-100 mg in adults) injected within 2 minutes. The same dose could be repeated in 10-minutes interval or 50 mg are injected jet intravenously within a minute. The latter dose is repeated 4 times in 5-10-minutes intervals. In order to maintain a therapeutic plasma concentration, the preparation is applied as a continuous infusion with rate 1-4 mg per kg body weight - up to total 24 hours dose 1.5-3 g within 2-3 days. In infiltration anesthesia total solution volume should not exceed 50-100 ml, 0.5% solution, depending on the type of surgery; in conduction and epidural anesthesia - 20-30 ml. Maximal volume should not exceed 500 ml, 0.5% solution or 250 ml, 1% solution.
Contraindications
Hypersensitivity to Lidocain; Adams-Stock’s syndrome; high degree AV - or SA - block.
Special warnings and precautions
Lidocain should not be used in severe heart failure; hepatal function disorders and severe liver diseases, particularly in cases with disturbed liver blood circulation; severe renal diseases and renal function disorders; shock and hypovolemia; incomplete heart block or sinus node bradycardia; WPW-syndrome; in newborns, as a danger of life-threatening side effects exists, including protracted convulsion. Cross-sensitivity reactions with other amide anesthetics were described. Lidocain should not be used in pregnant women, as it and its metabolites pass the placenta, which may lead to newborn's central nervous system depression, bradycardia etc. As the preparation may lead to blood pressure reduction and somnolence, it should be avoided in drivers and machinery-operating persons until the preparation effect disappears.
Drug interactions
In concomitant application of other antiarrhythmic medicines the Lidocain effect is enhanced. In concomitant application of anticonvulsuve preparations and hydantoin a depression of cardiac function is possibly to appear. In combined treatment with β-adrenoreceptor blockers (propranolol, atenolol, etc.) Lidocain plasma concentration is increased and a risk of intoxication exists. In high dosage and particularly in intravenous application of Lidocain together with neuro-muscular blockers the effect of both medicines is potentiated. Adrenalin, applied together with Lidocain, leads to prolongation of the local anesthesia. Adverse reactions
In patients with ventricular dysfunction rarely conduction disorders were seen. Administration of high dose Lidocain leads to the blood pressure decrease, rhythm disorders, heart block or heart arrest, and respiratory insufficiency. In therapeutic plasma concentrations or plasma levels slightly exceeding the therapeutic (1.5 - 6 mg/ml) insomnia, anxiety, dizziness, somnolence, emotional disorders, and visual disorders may appear.
Pharmacological mechanisms
Lidocain is a local anesthetic, belonging to the group of amides, possessing fast analgesic and antiarrhythmic effects. The effects of the preparation are due to a decrease of sensitivity of the pain receptors, retardation of the peripheral nerve conduction, and a prominent membrane-stabilization effect. In the place of application Lidocain inhibits the calcium ion influx, as well as (in lower degree) potassium ion reflux trough the neuron membrane, inhibiting depolarization and permeability of the latter. In the cardiac muscle the preparation exerts a selective antiarrhythmic activity, particularly in ventricular arrhythmias. It slightly depresses myocardial contractility, which make possibly to use the preparation in patients with heart failure. As Lidocain is fast metabolized by the liver microsomes its effect is of short duration. For this reason an intravenous application is recommended.
Supplied
50 ampoules of 10ml (0.5%, 1%, and 2%). 10 or 100 ampoules of 2 ml (40 mg).
Expiry
5 years

Diltiazem

2005-12-06T19:49:00.000-08:00

Diltiazem
Drug form and composition
Tablets. One tablet contains 60 mg Diltiazem hydrochloride.
Indications
Diltiazem is indicated in patients with stable and unstable angina pectoris; vasospastic angina pectoris (Prinzmetal); supraventricular tachyarrhythmias. System hypertension - as a monotherapy or in combination with other antihypertensive medicines.
Dosage and administration
The preparation is used orally in dose 30-60 mg (1/2 - 1 tablet), 3-4 times daily. The dose may be gradually enhanced during the next 1-2 dais until the sufficient effect is achieved. Contraindications
Hypersensitivity to the preparation; acute myocardial infarction; atrioventricular conduction disorders (2-nd and 3-rd degree AV block); bradycardia; sick sinus syndrome; hypotension; severe hepatal diseases; pregnancy and nursing.
Special warnings and precautions
The preparation should be used with care in patients with mild conduction defects (SA-block and 1-st degree AV-block), as well as in interventricular conduction disturbances. In adult patients and patients with severe liver and renal dysfunction the dosage of Diltiazem should be carefully appreciated. The patients in which the preparation causes headache, dizziness, and insomnia should drive and operate machinery with particular care.
Drug interactions
Concomitant use of cimetidin and ranitidin leads to elevation of the plasma concentration of Diltiazem. Diltiazem potentiates the immunosupressive effect of the cyclophosphamide and elevates the serum level of digoxin (by 20 - 45%), ciclosporin A and carbamazepine. In combined treatment with β-adrenoreceptor blocking agents and antiarrhythmic medicines hypotension and heart failure may appear.
Adverse reactions
Headache, dizziness, and weakness; bradycardia and hypotension; itching, and rash. Rarely gastrointestinal disorders may appear - nausea, vomiting, pyrosis, diarrhea or constipation. In high dosage perimaleolar swelling, elevation of the serum level of transaminases, bilirubin and alkal phosphatase may appear.
Pharmacological mechanisms
Diltiazem is a high-specificity synthetic calcium channel blocker. The Diltiazem action is mainly due to reduction of the calcium-dependent contraction of the myocardium and to reduction of the oxygen and phosphate utilization; coronary artery relaxation; suppression of the SA-node activity and AV-node conduction. Diltiazem reduces the oxygen requirements of the cardiac muscle by two mechanisms: direct - influence the energy consuming metabolite processes in the cardiac muscle cells; and indirect - reduces the peripheral resistance, which causes additional reduction of the heart load. All described effects lead to a reduction of the coronary artery resistance; reduction of the intensity of heart muscle perfusion; prevention of the coronary artery spasm; reduction of the blood pressure and the heart rate. The preparation does not cause reflectory tachycardia. The favorable effect of Diltiazem on the atherogenesis process is due to its cytoprotective action on the vascular wall; inhibition of the thrombocytes aggregation and secretion; activation of the intracellular destruction of cholesterol.
Supplied
50 tablets of 60 mg.
Expiry
3 years.

Captopril

2005-12-06T19:46:00.000-08:00

Captopril
Drug form and composition
Tablets. One tablet contains 25 mg Captopril.
Indications
Mild, moderate and severe essential hypertension; renovascular hypertension (as a monotherapy or in combination with diuretics); chronic congestive heart failure.
Dosage and administration
Usual dose in arterial hypertension is 12.5 - 25 mg, 2-3 times daily. If reduction of the blood pressure is insufficient the dose may be enhanced up to 50 mg, 2-3 times daily. In renovascular and renal hypertension the dosage is 12.5 mg, 3 times daily. In cases with renal failure daily dose depends on the creatine clearance, and dosage intervals should be longer. In heart failure the initial dose is 6.25 or 12.5 mg, 3 times daily, which may be enhanced gradually if necessary. The initial dose of Captopril should be consistent with used diuretics. In children Captopril should be used with particular attention and after precise assessment. The advisable dosage is 1-2 mg per kg body weight. Tablets should be taken 1 hour before meal.
Contraindications
Hypersensitivity to Captopril; in patients with neutropenia and thrombopenia; Quinke’s edema; pregnancy and nursing.
Special warnings and precautions
In patients with renovascular hypertension and low sodium serum level the preparation should be used with exceptional attention, because of enhanced hypotensive effect of the medicine, due to high level of renin releasing. In cases with severe renal insufficiency the treatment should be started with low doses Captopril, whereas protein excretion in urine and serum creatine and urea level are monitored. Captopril should be used very carefully in patients with bilateral stenosis of the renal arteries and autoimmune diseases.
Drug interactions
Captopril may reinforce hypoglycemic effect of the insulin and oral antidiabetic medicines. In concomitant treatment with potassium-sparing diuretics the risk of hyperkalemia is enhanced. Enhanced risk of leucopenia exists in concomitant treatment with immunosupressive agents. The orthostatic hypotension is more frequent in combined therapy with neuroleptics. Captopril may elevate serum levels of digoxin and reduces calcium channel blocker activity. Nonsteroid anti-inflammatory drugs reduce its antihypertensive effect. Hypotensive effect of Captopril is enhanced in concomitant treatment with vasodilators, diuretics and β-adrenoreceptor blocking agents.
Adverse reactions
Gastrointestinal disorders (mild and transitory); taste disorders; rashes; headache; dizziness; paresthesias; hypotension. In high dosage of the preparation proteinuria, neutropenia and leucopenia may appear. A comparatively frequent side effect is a dry iritative cough, which resolves after discontinuation of the treatment.
Pharmacological mechanisms
Captopril belongs to ACE-inhibiting agents - blockers of the angiotensin-converting enzyme. Renin-angiotensin system plays an important role in regulation of the blood pressure. Activity of this pressor system is depressed in significant level by the angiotensin-converting enzyme inhibitors, which prevent the transformation of angiotensin I to angiotensin II. In this way ACE - inhibitors prevent formation of the most powerful vasoconstrictive substance in the organism. ACE - inhibitors (in particular Captopril) influence the kallikrein-kinin system also, as the angiotensin I - converting enzyme is identical with kinase II. As the kinins (for example bradikinin) possess powerful vasodilating effect, depressing its degradation leads to vasodilation. Captopril, on the contrary of other vasodilators, does not cause fluid retention and tachycardia. Combined treatment with other antihypertensive medicines is suitable.
Supplied
40 tablets of 25 mg.
Expiry
3 years.

Atenolol

2005-12-02T11:55:00.000-08:00

Atenolol
Drug form and composition
Film-coated tablets. One tablet contains 50 mg Atenolol.
Indications
Stable and non-stable angina pectoris, which due to coronary artery sclerosis; arterial hypertension of different genesis (including renal hypertension).
Dosage and administration
Usual dosage in patients with angina pectoris and hypertension is 50-100 mg ones daily, as the effect becomes evident 1-2 weeks after initial dose. In patients with renal failure the dose should be corrected depending on the creatine clearance. If the clearance of creatine is 15-35 ml per minute, the dosage of Atenolol should be 50 mg ones daily; if the clearance is lower than 15 ml per minute, the same dose should be given each second day.
Contraindications
Second or third degree heart block; heart failure with decompensated hemodynamics; hypotension in myocardial infarction; cardiogenic shock; sinus node bradicardia (below 45 beats per minute); hypersensitivity to the preparation. Atenolol mustn’t be given to children.
Special warnings and precautions
In case of abrupt interruption of medication with Atenolol is possible to appear “withdrawal syndrome”, manifesting with severely heart disorders. This phenomenon is explained with a sensibilization of the beta-adrenergic receptors and increased norepinephrine releasing. For this reason the treatment with the preparation should be reduced gradually. In patients with bronchial asthma and COPD Atenolol may cause a bronchial obstruction and provoke an asthmatic attack, which due to blocking of the beta-adrenergic bronchial dilation. Atenolol should be administered with caution in patient with diabetes mellitus, as it may mask the tachycardia in case of hypoglycemia. In impending surgery under general anesthesia the treatment should be stopped 48 hours before operation. In pregnancy and lactation Atenolol is used only in cases with favourable risk/benefit ratio.
Drug interactions
In concomitant treatment with clonidin, Atenolol is withdrawn several days prior to clonidin interruption, in order to avoid the clonidin “steal” syndrome. Atenolol intensifies the hypoglycemia, caused by sulphonylurea preparations, depressing the contraregulatory mechanisms; enhances the negative chronotropic and dromotropic effects of the centrally acting antihyprtensive drugs, as reserpin and methyldopa; accentuates antiarrhythmic capabilities of the calcium channel blocking agents (verapamil, diltiazem); potentiates action of the nondepolarizing neuromuscular blocking agents. Concomitant treatment with Atenolol and digitalis glycosides may lead to bradicardia and heart block, which requires an ECG-monitoring. Cimmetidin elevates the plasma level of the Atenolol and increases its effects. Concomitant application of NSAID may reduce the antihypertensive effect of Atenolol, due to suppression of the renal synthesis of prostaglandines as well as fluid and sodium ions retention.
Adverse reactions
Following adverse reactions may be seen: hypotonia; bradicardia; paresthesies; cold limbs; exacerbation of the peripheral circulation disturbances; fatigue; dizziness; headache; nausea and gastrointestinal symptoms; hypersensitivity reactions, particularly skin manifestations. Rarely may appear heart failure aggravation; AV - block; bronchial obstruction; depression; hypoglycemia; thrombocytopenia; hyperlipemia.
Pharmacological mechanisms
Atenolol is a selective antagonist of the β1 - receptors, and has no membrane stabilizing and internal sympathicomimetic action. The basis of its antihypertensive action is depression of the renal renine secretion. Relive of the angina pectoris symptoms is due to reduction of the oxygen requirements of the myocardium. Atenolol reduces the cardiac output and contractility. In therapeutic dose it influences chronotrope, inotrope and dromotrope effects of the cardiac sympathetic stimulation. Its effects are better manifested during exercise and elevated sympathetic tone.
Supplied
30 film-coated tablets Atenolol of 50 mg.
Expiry
2 years.

Codterpin

2005-11-27T15:31:00.000-08:00

Codterpin (Codeine, Terpin hydrate)
Drug form and composition
Tablets. One tablet contains: 10 mg Codeine, 250 mg Terpin hydrate, 250 mg Sodium hydrogen carbonate.
Indications
The preparation is used in acute and chronic bronchitis; pneumonia; bronchiectases; chronic obstructive pulmonary disease; infectious and inflammatory diseases of the upper respiratory tract.
Dosage and administration
Codterpin is administered orally, 1 tablet 3-4 times daily, after nutrition.
Contraindications
Codterpin is contraindicated in hypersensitivity to codein or to some preparation’s constituents; in respiratory insufficiency; in children younger than 6 years; pregnancy and nursing.
Special warnings and precautions
The preparation should be used with particular care in respiratory tract diseases and with strictly observation of the therapeutic dose. Exceptional attention should be given when using the preparation on elderly patients and patients with debility; in cases with severe renal or liver failure; prostatic gland hypertrophy or ureteral sticture. As the medicine may provoke coordination disturbance, it should be used very carefully on driving and machinery operating persons.
Drug interactions
In concomitant administration with alcohol, barbiturates, benzodiazepine, hypnotic and sedative drugs, MAO-inhibitors and tricycled antidepressants Codterpin leads to intensification of its central depressive action on the central nervous system. Concomitant treatment with guanetidin, methyl-dopa and reserpine reduces its antihypertensive effect.
Adverse reactions
Following adverse reactions may be seen: respiratopry tract - depression of the respiration; cardiovascular system - hypotension, tachycardia, premature beats; hematologic - hemolytic anemia, thrombopenia, agranulocytosis; central nervous system - headache, sedation, coordination disorders, fatigue, insomnia, diplopia, neuritis, convulsions; gastrointestinal system - xerostomia, appetite loss, nausea, vomiting, diarrhea, constipation; urinary system - disuria, urine retention. Occasionally rash and photosensitivity are seen. Long-term administration of the preparation leads to drug dependence (codeine-dependence) manifesting with abstinence after medicine interruption.
Pharmacological mechanisms
Codterpin is a combined preparation possessing antitussive and expectorant action. Codeine, as a preparation constituent, depresses the cough reflex, inhibiting directly the cough center in the brainstem. In therapeutic dose it does not depress the respiratory center. The preparation possesses weak sedative and analgesic effects. Terpin hydrate facilitates the elimination of the resilient bronchial secretion, as it is excreted by the lungs and liquefies the secretion. Exerts weak antiseptic effect on the pulmonary parenchyma. Sodium hydrogen carbonate liquefies the respiratory tract secretion and facilitates its elimination.
Supplied
10 or 400 tablets.
Expiry
3 years.

Testosterone

2005-11-26T13:17:00.000-08:00

Testosterone
Drug form and composition
Solution for injection. One ampoule of 1 ml contains 50 mg Testosterone propionate.
Indications
The drug is used in cases of deficiency of androgens; in primary and secondary hypogonadism; late puberty in boys; hormone dependent breast cancer in women, as a hormonal therapy for palliative treatment.
Dosage and administration
In cases of deficiency of androgens and in primary and secondary hypogonadism, the drug is used intramuscularly in a dose of 25 - 50 mg 2 - 3 times weekly. In breast cancer, Testosteron is administered intramuscularly in dose 50 - 100 mg, 3 times weekly. In late puberty in boys, the dose of the drug is 100 mg intramuscularly for a month, generally for a period of 4 to 6 months.
Contraindications
Hypersensitivity to the drug; prostatic carcinoma in men; heart failure and myocardial infarction; renal or hepatic dysfunction; diabetes mellitus; hypercalcemia; hypertrophy of the prostate; pregnancy and lactation.
Special warnings and precautions
The drug should be used with caution in elderly patients, because the prolonged treatment with Testosteron can lead to prostatic hyperplasia or cancer. In patient treated for hypogonadism gynecomastia can develop. In high doses the exogenous testosterone can suppress spermatogenesis because of the inhibition (by the route of the “reciprocal relationship”) of the folliculostimulating hormone.
Drug interactions
Testosterone increases the action of the coumarin anticoagulants, insulin, metformin, sulfanilureic antidiabetic drugs. The effectiveness of the drug is reduced by barbiturates. In severe hypogonadism, Testosteron can be combined with drugs, stimulating the function of the thyroid gland.
Adverse reactions
The most commonly observed are: thrombophlebitis; jaundice of cholestatic type; virilism in women, priapism; retention of water and salts. In high doses and in prolonged treatment courses, there is a risk of development of liver tumors.
Pharmacological mechanisms
Testosterone is a synthetic sex hormone with strong androgenic action. In contrast to the natural hormones, it is absorbed slowly and it is more stable in the organism. During puberty testosterone is responsible for the development of the primary and secondary sex characteristics and the formation of the man type behavior. After puberty its effects are manifested in the spermatogenesis and metabolism. It has a strong anabolic action, facilitates the incorporation of calcium and phosphate in bones, increases the sodium and water retention and augments the skin blood supply. Testosteron inhibits the growth of some types of cancer of the breast, uterus, and ovaries. In women it can lead to virilization.
Supplied
10 or 50 ampoules of 1 ml (50 mg).
Expiry
5 years

Atropine

2005-11-09T12:16:00.000-08:00

Atropine
Drug form and composition
Solution for injection. One ampoule of 1 ml contains 1 mg Atropine sulfate (1 mg/ml).
Indications
Cholelithiasis and nephrolithiasis manifesting with spastic pain; ulcer disease; pylor constriction; cholecystitis; bronchial asthma; acute intoxications with cholinergic agents and digitalis glycosides.
Dosage and administration
Solution for injection - subcutaneous, intramuscular and intravenous application. Dosage for adults is 0.25-1 mg, 1-3 times daily. Maximal single dose is 1 mg, whereas the maximal dose is 3 mg per 24 hours. When Atropine is used as a counter-position in intoxication with phosphoorganic compounds, the daily dose may be enhanced - 1 mg of the medicine is injected in intervals of 15 minutes intramuscularly or intravenously. In children the preparation is injected subcutaneously or intravenously in dose 0.01 mg per kg body weight, each 4-6 hours, if necessary.
Contraindications
Glaucoma; urinary bladder and intestinal atonia; prostate gland hypertrophy; pylor stenosis; tachyarrhythmia and heart failure; reflux-esophagitis; active pulmonary tuberculosis. Pregnancy in the prenatal period and lactation - the preparation passes through the placenta and is excreted in the mother milk, which may lead to intoxication of the fetus and the infant. Special warnings and precautions
Atropine should be used with caution in patients with renal and hepatic insufficiency; hyperthyroidism; cardiac rhythm disorders; and coronary artery disease. During the treatment the patient should not drive and operate machinery.
Drug interactions
Amantadine, chinidine, three- and fourcyclet antidepressants, and neuroleptics all potentiate the anticholinergic action of Atropine. Atropine antagonizes the M-cholinomymetic effect of nivalin, pilocarpine, and neostigmine. In concomitant application of Atropine and H1- blockers, disopyramide, and antiparkinsonic medicines a sedative effect may appear.
Adverse reactions
Due to absorption and systemic action of Atropine following adverse reactions may appear: xerostomia; mydriasis; cycloplegia, intraocular pressure elevation and risk of glaucoma attack in patients with glaucoma; urine retention, particularly in patients with prostate gland hypertrophy; atonic constipation; irritability and confusion in elder patients. Mouth drying and palpitations may appear.
Pharmacological mechanisms
Atropine is an antagonist of the M-choline receptors. It abolishes the parasympathetic influence on the target organs as well as the M-cholinomymetic action of the anticholinesterase agents. Blocking M-cholinoreceptors, Atropine disturbs the neural impulse conduction from postganglionergic cholinergic nerves to effector organs, including exogene and endogene secreting glands, the heart; smooth muscles of the gastrointestinal tract, billiary and urinary pathways. Atropine dilates the pupil and paralyses the accommodation. Atropine is a caunter-poison in intoxication with all agents, acting by M-choline receptor influence, as it penetrates in CNS and eliminates central effects of toxins.
Supplied
10 ampoules of 1 ml (1 mg). 100 ampoules of 1 ml (1 mg).
Expiry
5 years.

Adrenalin

2005-11-06T08:59:00.000-08:00

Adrenalin (Epinephrine)
Drug form and composition
Solution for injection. One ampoule of 1 ml contains 1mg Epinephrine (1 mg/ml).
Indications
Adrenalin is used in cases of anaphylactic shock, cardiac arrest, and resistant ventricular fibrillation.
Dosage and administration
Dosage should be defined according to the severity of the disease state. Adults: In case of anaphylactic shock adrenalin can be injected subcutaneous or intravenously using doses of 0.2 - 0.5 mg, maximally - up to 1 mg. In cardiac arrest adrenalin is used intravenously - doses of 0.5 - 1 mg given every 3 to 5 minutes during resuscitation.
Children: Adrenalin is used intravenously in a dose of 0.01 mg/kg body mass during resuscitation. Contraindications
Adrenalin is contraindicated in: pheochromocytoma, tachyarrhythmias, ventricular fibrillations, and idiopathic hypertrophic subaortic stenosis. Special warnings and precautions
Adrenalin should be used with caution in the elderly, in individuals suffering from hyperthyroidism and severe heart diseases, in pregnant and breast-feeding women. It should be used with increased caution in following conditions: metabolic acidosis, atrial fibrillation, glaucoma, pulmonary hypertension, myocardial infarction, and occlusive vascular diseases.
Drug interactions
Adrenalin attenuates insulin activity. When used concurrently with cyclopropane, halothane, isoprenaline, there is a possibility of occurrence of cardiac rhythm disorders. Thiazide diuretics and phenothiazines induce a decrease in adrenalin activity, and thyroid hormones increase this activity. The application together with imipramine group antidepressants and MAO inhibitors can induce hypertensive crises with rhythm disorders. The combination with beta-blockers may lead to bradicardia, and the combination with -receptore blocking agents may result in fall of blood pressure.
Adverse reactions
The following adverse reactions are possible: palpitations, tremor, pallor, sweating, and difficulties during urination, nausea, vomiting, headache, ventricular arrhythmias, chest pain, hypertension, dispnea, hyperglycemia and hypokalemia.
Pharmacological mechanisms
Adrenalin is an - and -adrenergic receptor agonist representing the effects of the sympathetic influence on the organs. As a -receptor agonist, adrenalin increases the tone of the smooth muscle cells of blood vessels and induces constriction of the vessels in the abdominal cavity, skin and mucosae. Adrenalin induces a sharp, but brief, raise in blood pressure and stimulates the brain respiratory center. As an agonist of the -adrenergic receptors, adrenalin stimulates the contractility and excitability of myocardium, relaxes bronchial muscle cells, and induces glycogenolysis in the muscles and also lipolysis.
Supplied
10 or 100 ampoules of 1 ml (1 mg).
Expiry 2 years.

Ketotifen

2005-11-06T08:53:00.000-08:00

Ketotifen.
Drug form and composition
Tablets. One tablet contains 1 mg Ketotifen equivalent. Syrup. 1 ml syrup contains 0.2 mg Ketotifen equivalent.
Indications
Long-term prevention of all forms of the bronchial asthma, allergic bronchitis, and asthma manifestations in allergic rhinitis. Prevention and treatment of allergic diseases, including: acute and chronic urticaria, atopic dermatitis, allergic rhinitis and conjunctivitis.
Dosage and administration
The tablets and the syrup are taken orally with meal. In adults - 1 mg, 2 times daily, in the morning and in the evening. In case of insufficient effect after 4-week treatment the dose could be increased up to 2 mg, 2 times daily. In children aged 6 months- to 3 years - 0.5 mg (2.5 ml syrup), 2 times daily; in children older than 3 years - 1 mg, 2 times daily (in the morning and in the evening). The treatment with Ketotifen should be discontinued gradually, with graduate reduction of the dose within 2-4 weeks, in order to avoid the risk of asthma symptoms recidivating. It is advisable the treatment to continue 2-3 months.
Contraindications
The preparation should not be used in hypersensitivity and during the first trimester of the pregnancy.
Special warnings and precautions
In patents, sensitive to the sedative effect of the preparation, initial dose should be half of the usual, which could be gradually increased. In order to avoid suprarenal insufficiency, in patients, treated regularly with corticosteroids, Ketotifen should be started after gradually reducing of the corticosteroid dose, or elongation of the interdosage intervals. In case of intercurrent infections Ketotifen should not be discontinued. In pregnant and nursing women Ketotifen is used only after precise consideration of the mother and the fetus risk/benefit ratio. At the beginning of the treatment Ketotifen may cause patient reaction disorders, which requires enhanced attention in drivers and machinery operating persons.
Drug interactions
Concomitant treatment with oral antidiabetic preparations enhances the risk of reversible thrombocytopenia. Ketotifen potentiates the effect of the sedative, hypnotic, and antihistamine medicines, as well as alcohol. The preparation could be combined with antiseptic and antibacterial medicines.
Adverse reactions
During the first several days of the treatment with Ketotifen following adverse effects may appear: somnolence, xerostomia, mild dizziness, and fatigue, which are usually reversible with the treatment. In some patients body weight enhancement is seen, due to appetite increasing. Hypersensitivity is very rare side effect, seen in immunocompromized patients.
Pharmacological mechanisms
Ketotifen is an antihistamine preparation with prolonged preventive effect on the frequency and intensity of the asthma attacks. Its mechanism of action ultimately is associated with reduction of histamine, serotonine and other mast cell mediators release, and simultaneous selective blocking of the H1-receptors. As a result of the latter effects the level of the cell cAMP in enhanced and eosinophilic infiltration is inhibited. Although the preparation influences favorably expectoration, it does not cope the asthmatic attacks, but only prevents their appearance. Supplied
30 tablets of 1 mg. Vials, containing 125 ml syrup.
Expiry
Tablets - 4 years. Syrup - 3 years

Papaverine

2005-11-06T08:49:00.000-08:00

Papaverine
Drug form and composition
Solution for injection. One ampoule of 1 ml (2%) contains 20 mg Papaverine hydrochloride (20 mg/ml).
Indications
The preparation is used as a muscular relaxant in acute peripheral arterial spasms; acute renal, biliary, and gastrointestinal colic; in erection dysfunctions (as a monotherapy or in combination with α-adrenergic blockers, including phentolamine).
Dosage and administration
The solution is applied intravenously or intramuscularly. In adults the dosage is 20-40 mg, 1-2 times daily. If necessary the dose could be repeated every 3 hours - up to 120 mg maximal 24 hours dose. In impotence the preparation could be applied in the cavernous body in single dose 20-40 mg, but no more than 60 mg. In children the preparation is applied intramuscularly or intravenously in dose 1.5 mg per kg body weight, 4 times daily.
Contraindications
Papaverine is contraindicated in hypersensitivity to the preparation; atrioventricular block; acute myocardial infarction; recent stroke; liver function disorders; glaucoma.
Special warnings and precautions
In patients with liver diseases the preparation should be used with care. In patients with Parkinson’s disease, treated with levodopa, a risk of worsening of the disease exists. In pregnancy and nursing women the preparation should be used only after careful assessment of the risk-benefit ratio for the mother and the fetus. The preparation should be used with care in drivers and machinery operating persons, as it possesses some sedative effect.
Drug interactions
Concomitant administration with hypotensive medicines leads to potentiation of their hypotensive effect. The spasmolytic effect of Papaverine on the smooth muscles is abolished by simultaneous application of morphine. The preparation could be combined successfully with other medicines, including phenobarbital, diolan, novphyllin, atropin, etc.
Adverse reactions
During the treatment with Papaverine following adverse reactions may be seen: tachycardia; premature heart contractions; atrioventricular block; xerostomia; constipation; elevation of the liver enzymes serum level; fatigue; dizziness; somnolence; headache.
Pharmacological mechanisms
Papaverine is a synthetic opium alkaloid with prominent spasmolytic and anticholinergic action. It exerts a direct effect on the smooth muscles; reduces the blood vessel tone, particularly of the coronary, intracranial and pulmonary arteries and arterioles. The preparation reduces the tone of the smooth muscles, bronchi, stomach, biliary tract, ureter and uterus also. The mechanism of its action is related to inhibition of the enzyme phosphodiesterase and elevation of the intracellular concentration of cAMP. In higher doses it exerts a weak sedative effect.
Supplied
100 ampoules of 1 ml (20 mg).
Expiry - 2 years.

Piroxicam

2005-11-03T22:16:00.000-08:00

Piroxicam
Drug form and composition
Gelatin capsules. One gelatin capsule contains 10 mg or 20 mg of Piroxicam.
Indications
The drug is used in cases of rheumatic diseases like ankylosing spondilitis, osteoarthritis, and rheumatoid arthritis. It is used also in the treatment of the chronic juvenile arthritis. Piroxicam is used in acute gout attacks and in cases of dysmenorrhoea. Dosage and administration
In adults Piroxicam is administered orally in daily dose of 20 mg, given as a single daily dose or divided in two doses of 10 mg each. In acute conditions, the initial daily dose is 40 mg for the first 2 days, followed by a dose of 20 mg daily for a period of 1 - 2 weeks. In case of acute gout attack, the commonly used dose is 40 mg /24 hours for a period of 5 - 7 days. In dysmenorrhoea during the first day the dose is 40 mg and after that the dose is reduced to 20 mg for the next days up to the disappearance of the pain.
Contraindications
Hypersensitivity to Piroxicam or other drugs from the group of oxicams; gastrointestinal hemorrhages or peptic ulcer; severe hepatic diseases; renal dysfunction; pregnancy and breast feeding; children younger than 15 years. Special warnings and precautions
Because of the risk of development of gastrointestinal ulcers, bleedings and perforation the drug should always be taken after nutrition and with enough quantity of liquid. The simultaneous consumption of alcohol should be avoided. The drug is used cautiously in patients with hypersensitivity to foods and drugs. In patients with kidney diseases, prolonged administration of this agent can lead to papillary necrosis, and in patients with liver diseases, a change in transaminase levels is possible. In patients suffering form hematological diseases and in people taking anticoagulants Piroxicam is used with caution and with regular checks of the laboratory indices. Piroxicam can reduce the concentration of the attention and suppress reactions. Because of this the drug is used cautiously and after an assessment of the risk in drivers and in people working with machines.
Drug interactions
Piroxicam has a high affinity to the plasma proteins and due to this fact the concurrent administration with coumarin anticoagulants, sulfonamides, nelidix acid, oral antidiabetic agents, triiodothyronine, cyclophosphamide, and digoxin can lead to an increase in their plasma levels. The concurrent administration with other drugs of the groups of nonsteroidal anti-inflammatory agents, corticosteroids and alcohol increases the risk of development of hypersensitivity and adverse drug reactions by the gastrointestinal tract. Piroxicam reduces the effects of the diuretics and hypotensive drugs and increases the activity of the lithium agents.
Adverse reactions
The most commonly observed adverse reactions associated with Piroxicam administration are: gastrointestinal - burning sensation, nausea, vomiting, diarrhea, peptic ulcers, and hemorrhages, which are usually dose dependent; CNS - somnolence, headache, vertigo; hematological - granulocytopenia, anemia; hypersensitivity reactions - itching, urticaria, photosensitivity. Pharmacological mechanisms
Piroxicam belongs to the group of nonsteroidal anti-inflammatory drugs. It exerts strong anti-inflammatory, analgesic, and antipyretic action. The mechanism of action is explained with the powerful and long lasting, but reversible, inhibition of the prostaglandin synthesis. There are also other effects like the inhibition of platelet aggregation and the influence on the white blood cells. Piroxicam accumulates selectively in the inflamed tissues and penetrates in the synovial fluid.
Supplied
20 gelatin capsules of 10 or 20 mg.
Expiry - 3 years

Indometacin

2005-11-03T21:41:00.000-08:00

Indomethacin

Drug form and composition
Enterosolvent film-coated tablets. One enterosolvent film-coated tablet contains 25 mg Indometacin. Suppositories. One suppository contains 50 mg or 100 mg Indometacin. Ointment. 1g ointment (10%) contains 100 mg Indometacin.
Indications
Rheumatoid arthritis; osteoarthritis; coxarthrosis; Bechterew’s disease; acute gout arthritis; psoriatic arthritis; juvenile arthritis; Reiter’s disease; periarticular diseases - tendinitis, bursitis, etc; dysmenorrhea; some cases of vascular headache.
Dosage and administration
Indometacin, enterosolvent film-coated tablets are used orally in dose 25-50 mg, 2-3 times daily after nutrition. In children older than 14 years recommended dose is 1.5-2.5 mg per kg body weight, divided in three takes. Suppositories are applied rectally in dose 50-100 mg, 1-2 times daily. In children older than 14 years the recommended dose is 1.5-2.5 mg per kg body weight, divided in two takes. Maximal dose in adults should not exceed 200 mg /24 hours and for children older than 14 years - 150 mg /24 hours. Treatment courses longer than 7 days are not recommendable. Indometacin - ointment is indicated in mild clinical manifestations. It is applied as follows: 1-2 cm ointment is spread on the affected region 2-3 times daily.
Contraindications
Hypersensitivity to indometacin, salicylates, and other nonsteroid antiinflammatory drugs; ulcer disease; severe liver and renal diseases; epilepsy and mental diseases; parkinsonysm; proctitis (valid for suppositories); pregnancy and lactation; children younger than 14 years.
Special warnings and precautions
Indometacin should be used with care in patients with renal and liver diseases; ulcer disease in remission (it is obligatory to add H2-blocker or other gastroprotective medicines). Systemic application of Indometacin may cause changes in several laboratory tests, including: elevation of the glucose, bilirubin, transaminases, creatine, and urea serum level; prolongs the bleeding time; reduced the creatine clearance; and reduces osmolality of the urine. Application of the tablets and suppositories in drivers and machine operating persons is not recommendable, as the medicine may provoke side reactions (somnolence, color sensitivity disorders, and diplopia), disturbing the concentration capabilities.
Drug interactions
Indometacin potentiates cumarin anticoagulant activity, activity of the oral antidiabetics, corticosteroids, nifedipin, and verapamil. Concomitant administration with other NSAID and aspirin increases the risk of ulceration. Indometacin reduces the renal clearance of lithium preparation; inhibits the vasodilating effect of nitroglycerin; increases toxicity of the aminoglycoside antibiotics.
Adverse reactions
Nausea; vomiting; epigastral pain; ulcerogenic effect; diarrhea; dizziness; headache; somnolence; visual disorders; leucopenia; hematuria; water and electrolytes retention.
Pharmacological mechanisms
Indometacin is a derivative of indol, possessing prominent anti-inflammatory action, significantly exceeding the antiinflammatory effect of the salicyllates and phenylbutazone. It exerts analgesic, antipyretic, and uricosuric activity also. The mechanism of the analgesic, antipyretic and antiinflammatory effects is related to depression of the prostacycline (PGE1, PGD, and PGI2) synthesis by inhibition of the enzyme cyclooxygenase activity. Indometacin possesses certain ganglion-blocking and antiaggregant effect.
Supplied
30 or 1350 Indometacin Sopharma enterosolvent film-coated tablets of 25 mg. 6 Indometacin suppositories of 50 mg or 100 mg. Tube, containing 40 g Indometacin Sopharma ointment.
Expiry
Enterosolvent film-coated tablets - 5 years. Suppositories - 2 years. Ointment - 3 years.

Paracetamol

2005-11-03T21:21:00.000-08:00

Paracetamol
Drug form and composition
Tablets. One tablet contains 500 mg Paracetamol. Syrup. 5 milliliters syrup contains 120 mg Paracetamol.
Indications
The preparation is indicated in diseases manifesting with pain and fever: headache, toothache, mild and moderate postoperative and injury pain, high temperature, infectious diseases and chills (acute catarrhal inflammations of the upper respiratory tract, flu, small-pox, parotitis, etc.).
Dosage and administration
In adults - 500 mg (1 tablet), 3-4 times daily. In children: aged from 3 months to1 year - 60-120 mg (2.5-5 ml syrup), 3-4 times daily; 1-6 years - 120-240 mg (5-10 ml syrup), 3-4 times daily; children older than 6 years - 250-500 mg, 3-4 times daily. In children younger than 3 months the preparation should be used only on doctor’s prescription. Duration of the treatment in children should not exceed 5 days, whereas in adults it may be continued up to 10 days. Contraindications
Paracetamol should not be used in hypersensitivity to the preparation and in severe liver diseases. Special warnings and precautions
The preparation should be used with care in patients with liver and renal diseases. The treatment with Paracetamol may change the laboratory tests of uric acid and blood glucose analysis. In severe renal failure the interval between two consecutive takings should not be shorter than 8 hours. The treatment with the preparation is not advisable during the first trimester of the pregnancy. In nursing women the preparation should be used with strictly observation of the therapeutic dose and duration of the treatment.
Drug interactions
Concomitant treatment with aminophenazone may lead to an increase of the effects of both medicines. Paracetamol potentiates effects of the anticoagulant medicines. Phenobarbital increases the harming effect of Paracetamol on the liver. Contraceptive preparations and rifampicin reduce the effectivity of Paracetamol. Cimetidin reduces toxicity and potentiates the analgesic effect of the preparation. Paracetamol potentiates the action of the Chloramphenicol. Concomitant usage of alcohol and medicines harming the liver, enhances the risk of severe liver disorders.
Adverse reactions
In rare cases hypersensitivity reactions, predominantly skin allergy (itching and rash), may appear. Long-term treatment with high doses may cause a toxic hepatitis with following initial symptoms: nausea, vomiting, sweating, and discomfort. Occasionally a gastrointestinal discomfort may be seen.
Pharmacological mechanisms
Paracetamol possesses prominent antipyretic and analgesic effects. Its anti-inflammatory activity is weak and has no clinical significance. The mechanism of action is related to depression of the prostaglandin synthesis by inhibition of the specific cell cyclooxygenase, and depression of the thermoregulatory center in the medulla oblongata. Supplied
20 or 400 tablets of 500 mg. Vials, containing 125 ml syrup.
Expiry - Tablets and syrup - 3 years.

Analgin

2005-10-30T20:48:00.000-08:00

Analgin (Metamizole sodium)

International generic name - Metamizole sodium
Drug form and composition -
Solution for injection. One ampoule of 2 ml contains 1 g Metamizole sodium (0.5 g/ml). One ampoule of 5 ml contains 2.5 g Metamizole sodium (0.5 g/ml). Tablets. One tablet contains 500 mg Metamizole sodium (100%).
Indications
Analgin tablets are used for the treatment of pains of different origin and variable intensity: toothache, headache, arthralgia, neuralgia, myositis, mild to moderate visceral pain, high fever, not responding to other drugs. Analgin injection is used in cases of acute and severe pain after operations and traumas, pain associated with neoplastic diseases, colicky pain etc.
Dosage and administration
Ampoules: The ampoules can be administered intramuscularly. The single dose in all age groups is 8 to 16 mg/kg body weight. The dose should be given according to the following scheme: 16 to 31 kg body weight - 250 mg Analgin (1/2 ml); 32 to 46 kg body weight - 500 mg Analgin (1 ml); 47 - 62 kg body weight - 500 - 750 mg Analgin (1 - 1.5 ml); and over 63 kg body weight - 750 - 1000 mg Analgin (1.5 - 2 ml). In cases of persistent pain, the dose can be repeated after 6 to 8 hours. Maximum daily dose - 4.0 g Analgin. Analgin should not be used parenterally for a period longer than 3 days. Tablets: The dosage and duration of the treatment must be determined according to the severity of the pain syndrome. The common dose in the adults is 250 to 500 mg (1 to 2 tablets) 2 or 3 times daily. The maximum dose is 3 g/24h. In over 15 year-old children the Analgin dose is 250 mg bid or tid.
Contraindications
Hypersensitivity to metamizole and other pyrazolone derivatives, acute hepatic porphyria, inborn glucose-6-phosphate dehydrogenase deficiency, severe renal or hepatic diseases, blood diseases (such as aplastic anemia, leucopenia and agranulocytosis), pregnancy (the first and the last trimester). Parenteral administration of Analgin is contraindicated in under 1 year-old children. Special warnings and precautions
Analgin is used with increased caution in patients with a history for hypersensitivity to foods and drugs (particularly to analgesic and nonsteroidal antiinflammatory agents) and also in patients suffering from bronchial asthma, Quincke’s edema, chronic pulmonary infections. In patients with hypotension and unstable blood pressure, Analgin should not be used parentarally. If Analgin application is quite necessary, the blood pressure and the heart rate should be monitored. In cases of prolonged Analgin treatment, regular blood count checks are necessary (differential count of the white blood cells). The high Analgin doses can influence unfavourably the active attention. Because of this in these cases driving and working with machines are not advised.
Drug interactions
Analgin potentiates the analgesic and antipyretic action of the nonsteroidal antiinflammatory drugs. The Analgin effects are potentiated by the tricyclic antidepressants, oral contraceptive agents, allopurinol, alcohol. Analgin decreases the activity of the coumarin anticoagulants and plasma levels of cyclosporin. The enzyme inductors (barbiturates, glutethimide, phenylbutazone) attenuate the Analgin effects. Analgin potentiates the effects of the drugs possessing CNS depressant activity. Concurrent administration with chlorpromazine is related with a risk of severe hypothermia. Analgin can be used in combination with buscolysin, atropin, codein.
Adverse reactions
After prolonged administration very rarely can be observed agranulocytosis, leucopenia and thrombocytopenia, proteinuria, interstitial nephritis. In sensitive patients rashes, urticaria, Quincke’s edema, asthmatic attacks, and very rarely anaphylactic shock are possible. Pharmacological mechanisms
Analgin is a medicine of the pyrazolone group, possessing hard analgesic and antipyretic effects and moderate antiinflammatory activity. Blocking of the synthesis of endogenous pyrogens - prostaglandins D and E - is the cause for the antipyretic activity and also for the analgesic action of this drug. The decrease of the prostaglandis production in the periphery (and respective decrease of nerve endings sensitivity) plays a relatively smaller role. In contrast to the other nonnarcotic analgesic drugs, Analgin stimulates the release of β-endorphins, explaining its activity in cases of visceral pain. Analgin has a slight spasmolytic activity on the smooth muscle cells of the biliary and urinary tracts and also on the muscle of the uterus. Supplied
10 or 100 ampoules of 2 ml (1 g). 10 ampoules of 5 ml (2.5 g). 20 or 500 tablets of 500 mg. Expiry
Solution for injection and tablets - 5 years.

Tempalgin

2005-10-30T20:42:00.000-08:00

Tempalgin (Metamizole sodium, Tempidon)
Drug form and composition
Film-coated tablets.
Each film-coated tablet contains: 500 mg Metamizole sodium; 20 mg Tempidon.
Indications Mild to moderate pain of variable origin: headache; migrene; toothache; neuralgia; neuritis; plexitis; lumbalgia; myalgia and myositis; trauma; postsurgery interventions and dental procedures; dysmenorrhoea; burning; premedication in the dental practice.
Dosage and administration In adults, Tempalgin is used orally in dose of 1 - 2 tablets 3 - 4 times daily. In children over 10 years, the drug is administered in dose of 1 tablet 2 - 3 times daily. The treatment course duration should not exceed 5 to 7 days.
Contraindications Hypersensitivity to tempidon, metamizole and other pyrazolone drugs; acute hepatic porphyria and inborn deficiency of glucose-6-phosphate dehydrogenase; aplastic anemia, leucopenia and agranulocytosis; severe kidney and liver diseases; pregnancy; children younger than of 10 years.
Special warnings and precautions The drug is used cautiously in patients suffering from liver or kidney diseases. After more prolonged treatment with Tempalgin regular checks of blood count are necessary. In patients suffering from bronchial asthma, pollinosis, Quincke’s edema, chronic airway infections or showing hypersensitivity to analgesic and nonsteroidal anti-inflammatory agents, as well as to other drugs or foods, there is a risk of allergic reactions and asthmatic attacks. During lactation the drug should be avoided, because both active ingredients are eliminated in the breast milk. Tempidon decreases the attention concentration and slows the reflexes. Because of this it should be used cautiously in car drivers and in people working with machines.
Drug interactions Because of the inhibition of hepatic enzyme systems metabolising drugs, Metamizole effect is potentiated by tricyclic antidepressants (psychophorin, amitriptyline), oral contraceptive agents, and allopurinol. Due to this its biotransformation is slower, and the toxicity is greater. Barbiturates and phenylbutazone are liver enzyme inductors, and they decrease the strength and duration of the metamizole pharmacodynamic effect. Metamizole lowers the plasma cyclosporin levels. Chloramphenicol increases the myelotoxic action of metamizole (additive effect). Alcohol augments the action of both components. Tempidon potentiates the activity of the hypnotic agents, general anesthetics, and narcotic and nonnarcotic analgesics.
Adverse reactions Itching, skin rash, urticaria, Stevens-Johnson’s syndrome, Layell’s syndrome, angioedema, vasomotor disturbances; asthmatic attack, allergic shock; nausea, vomiting, abdominal pain and discomfort, ulcers and bleeding in rare cases. In susceptible patients, agranulocytosis, leucopenia, aplastic anemia, retention of water and electrolytes are possible.
Pharmacological mechanisms The combined product Tempalgin exerts analgesic and antipyretic action and moderate anti-inflammatory activity. The analgesic effect is stronger and longer than that of metamizole, and it influences the psychic pain component. Metamizole exerts its pharmacodynamic effects by inhibition of the prostaglandin synthesis and formation of endogenous pyrogens. The other component, Tempidon, possesses a strong anxiolytic activity and eliminates the state of fear and anxiety. Supplied20 or 300 film-coated tablets.
Expiry4 years

Ibuprofen

2005-10-29T22:17:00.000-07:00

Ibuprofen
Indications:
Temporarily relieves minor aches and pains due to: headache, muscular aches, toothache, minor pain of arthritis, backache, the common cold, menstrual cramps
Temporarily reduces fever
Directions:
Do not take more than directed.
Adults and children 12 years and older:
take 1 tablet every 4 to 6 hours while symptoms persist
if pain or fever does not respond to 1 tablet, 2 tablets may be used
do not exceed 6 tablets in 24 hours, unless directed by a doctor
the smallest effective dose should be used
Children under 12 years: ask a doctor
Read all warnings and directions before use. Keep carton.Store at 20°-25°C (68°-77°F)Avoid high humidity and excessive heat above 40°C (104°F)
If you have questions of a medical nature, please contact your pharmacist, doctor, or health care professional.
Ingredients:
Active Ingredients: Each Tablet Contains: Ibuprofen 200mg (pain reliever/fever reducer)Inactive Ingredients: Colloidal Silicon Dioxide, Corn Starch, Croscarmellose Sodium, Hydroxypropyl Methylcellulose, Iron Oxides, Microcrystalline Cellulose, Stearic Acid, Titanium Dioxide
Warnings:
Allergy alert: Ibuprofen may cause a severe allergic reaction which may include:
hives
asthma (wheezing)
facial swelling
shock
Alcohol warning: if you consume 3 or more alcoholic drinks every day, ask you doctor whether you should take ibuprofen or other pain relievers/fever reducers. Ibuprofen may cause stomach bleeding.
Do not use if you have ever had an allergic reaction to any other pain reliever/fever reducer.
Ask a doctor before use if you have
stomach pain
problems or serious side effects from taking pain relievers or fever reducers
Ask a doctor or pharmacist before use if you are
under a doctor's care for any serious condition
taking any other drug
taking any other product that contains ibuprofen, or any other pain reliever/fever reducer
When using this product take with food or milk if stomach upset occurs.
Stop use and ask a doctor if
an allergic reaction occurs. Seek medical help right away.
pain gets worse or lasts more than 10 days
fever gets worse or lasts more than 3 days
stomach pain or upset gets worse or lasts
redness or swelling is present in the painful area
any new symptoms appear
If pregnant or breast-feeding, ask a health professional before use. It is especially important not to use ibuprofen during the last 3 months of pregnancy unless definitely directed to do so by a doctor because it may cause problems in the unborn child or complications during delivery.
Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center right away.

Aspirin

2005-10-29T22:01:00.000-07:00

Aspirin
Indication
For the temporary relief of minor aches and pains
headaches
reduction of fever
Directions:
Adults: take 4 to 8 tablets every 4 hours, not to exceed 48 tablets in 24 hours or as recommended by a doctor
Children under 12: do not give to children under 12 unless directed by a doctor
Store at controlled room temperature 15°-30° C (59°-86° F)
Ingredients:
Active Ingredients: Aspirin 81mgInactive Ingredients: Black Iron Oxide, Cellulose, Collodial Silicon Dioxide, Croscarmellose Sodium, D&C Yellow 10 Aluminum Lake, FD&C Yellow 6 Aluminum Lake, Hydroxypropyl Methylcellulose, Polydextrose, Polyethylene Glycol, Polyvinyl Acetate Phthalate, Propylene Glycol, Shellac Wax, Sodium Alginate, Sodium Bicarbonate, Starch, Stearic Acid, Talc, Titanium Dioxide, Triacetin, Triethyl Citrate
Warnings:
Children and teenagers should not use this medicine for chicken pox or flu symptoms before a doctor is consulted about Reye Syndrome, a rare but serious illness reported to be associated with aspirin.
Do not take this product
for pain for more than 10 days
for fever for more than 3 days
if you are allergic to aspirin
Ask a doctor before use if you have asthma
stomach problems that persist or recur ulcers
bleeding problems
if you are taking a prescription drug for anticoagulation (thinning of blood), diabetes, gout or arthritis
Stop use and ask a doctor if symptoms do not improve
new symptoms occur
pain or fever persists or gets worse
redness or swelling is present
ringing in the ears or loss of hearing occurs
If pregnant or breast-feeding, ask a health professional before use. It is especially important not to use aspirin during the last 3 months of pregnancy unless specifically directed to do so by a doctor because it may cause problems in the unborn child or complications during delivery.
Keep out of the reach of children. In case of accidental overdose, get medical help or contact a Poison Control Center right away.
Alcohol Warning: If you consume 3 or more alcoholic drinks every day, ask your doctor whether you should take aspirin or other pain relievers/fever reducers. Aspirin may cause stomach bleeding.

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2005-10-29T17:00:00.000-07:00

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