International generic name

Clonidine

Drug form and composition

Solution for injection. One ampoule of 1 ml, contains 0.15 mg Clonidine hydrochloride (0.15 mg per ml). Tablets. One tablet contains 0,15 mg Clonidine hydrochloride.

Indications

In the treatment of the different forms and stages of the arterial hypertension, including cases resistant to other antihypertensive treatment.

Dosage and administration

Solution for injection: Chlophazolin may be administered subcutaneously, intramuscularly and intravenously. The treatment of the hypertensive crisis may start with subcutaneous or intramuscular injection in dose 1-2 ampoules (0.150-0.300 mg), which is determined depending on the blood pressure level. The preparation may be administered intravenously also, while the ampoule is diluted in 10 ml saline and is injected slowly intravenously with patient in prone position. The hypotensive effect becomes apparent more than 10 minutes after injection, reaches the maximum 30-60 minutes later and lasts 3 - 7 hours. If necessary, up to 5 ampoules (0.750 mg) per 24 hours may be injected intravenously. Tablets: the usual initial dose is 0.075 mg (½ tablet), 2-3 times daily. If necessary the dose may be gradually enhanced up to 0.15 - 0.30 mg (1-2 tablet) 2-3 times daily. The optimal dosage is determined individually.

Contraindications

Hypersensitivity to clonidine; recent myocardial infarction; significant bradycardia; hepatal and renal function disorders; AV-block II or III degree; cerebrovascular diseases; depressive syndrome; Reynaud’s syndrome.

Special warnings and precautions

In patients with preexisting heart diseases rhythm disorders may appear, which are resolved with reducing the dosage. The treatment should not be interrupted abruptly in order to prevent a relapse of quick elevation of the blood pressure. If severe renal failure exists the preparation should be used under doctor’s control with monitoring of the creatine clearance. In pregnant women the preparation is indicated only in case of the expected benefit exceed the adverse effects. In drivers and machinery operating persons the preparation should be administered carefully, as it may provoke dizziness and orthostatic reactions. During the treatment alcohol should be avoided.

Drug interactions

The action of the preparation is potentiated in concomitant administration of diuretics and vasodilators. Chlophazolin increases the depressive effect of alcohol, barbiturates, and sedative agents. In concomitant treatment with nonsteroid antiinflammatory drugs and tricycled antidepressants the antihypertensive activity of the preparation is reduced. Concomitant administration with cardiac glycosides may cause bradycardia and occasionally rhythm disorders (AV - block).

Adverse reactions

In the beginning of the treatment a slight sedative effect, fatigue; mouth drying dizziness, orthostatic collapse, nausea, and vomiting may be seen. Rarely hypersensitivity reactions, gynecomastia, and paraauricular gland inflammation may appear. In case of abrupt interruption of the treatment a sudden elevation of the blood pressure is possible - rebound effect.

Pharmacological mechanisms

Chlophazolin reduces the blood pressure by the influence of the sympathetic nervous system. It enhances sensitivity of the bar receptor reflexes with resulting elevation of the parasympathetic tone and reduction of the sympathetic tone. As a result of the former the blood pressure, the heart rate and the peripheral resistance are reduced. The preparation reduces the venous reflux and elevates renin level, while the renal perfusion and glomerular filtration are improved. It possesses slight sedative effect. Chlophazolin does not stimulate stomach secretion.

Supplied

50 ampoules of 1 ml (0.15 mg ). 50 tablets of 0.15 mg.

Expiry

Solution for injection and tablets - 3 years.