Progesterone

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

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

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

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

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

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.