International generic name

Diazepam

Drug form and composition

Solution for injection. One ampoule of 2 ml contains 10 mg Diazepam (5 mg/ml).

Indications

Diazepam is indicated in acute psychoneurotic condition, accompanied by anxiety, agitation, intensity, irritability, insomnia; in the treatment of the epileptic status and other convulsive conditions. It is used for treatment of the alcohol abstinence. In anesthesiology practice - for the preoperative preparation and in postoperative period. As a premedication in several diagnostic interventions.

Dosage and administration

The solution for injection is applied intramuscularly and intravenously. In adult patients the initial dose is 5-10 mg; the same dose may be repeated if necessary - up to 30 mg maximal dose. In preoperative preparation and in diagnostic interventions the dose is 5-10 mg given before surgery or diagnostic manipulation. In pediatric patients the intravenous application is preferable. The solution should be injected slowly (3-5 minutes). In children aged from 1 month to 5 years the maximal dose is 5 mg, whereas in children older than 5 years the maximal dose is 10 mg. The application may be repeated after 2-4 hours later if necessary.

Contraindications

Diazepam should not be administered in patients with liver or kidney disorders; myasthenia gravis; acute alcohol intoxication; depressive conditions; psychosis; brain diseases; shock; coma; drug abuse or drug dependence; glaucoma; hyperkinesis; hypoalbuminemia; porphyria; chronic obstructive pulmonary disease; apnea; pregnancy in the first and the last trimester; lactation; dysphagia in childhood; hypersensitivity to the benzodiazepines.

Special warnings and precautions

The preparation should be used with particular care in adult patients and patents with respiratory diseases, as the risk of apnea and/or cardiac arrest exists. Diazepam should not be used simultaneously with alcohol. In long-term administration the medicine may lead to drug dependence. In intravenous application the solution should be injected slowly (5 mg per minute), in order to reduce the risk of a venous thrombosis, phlebitis, local irritation or swelling. As the preparation influence the reflex activity, it should be not administered in drivers and machinery operating persons.

Drug interactions

The depressive effect of Diazepam on the central nervous system is potentiated in concomitant use of alcohol, general anesthetics, sedative and hypnotic medicines, neuroleptics, narcotic analgesics, antihystamine preparations, and anticonvulsive drugs. Its action is potentiated by MAO-inhibitors. Simultaneous administration of cimetidin and myorelaxants may delay elimination of the preparation and to enhance its hypnotic effect. Diazepam may enhance the plasma concentrations of the phenytoin if given simultaneously.

Adverse reactions

Somnolence; headache; dizziness; apathy; depressive conditions; ataxia; tremor; hypotension; bradycardia; collapse; constipation; reduced libido. In abrupt discontinuation of the preparation anxiety and aggressive conditions may appear.

Pharmacological mechanisms

Diazepam belongs to the group of the benzodiazepine derivatives and possesses tranquilant, myorelaxing and anticonvulsive actions. It inhibits conduction in the ascending activating system of the reticular formation, limbic system, and hypothalamus. Its mechanism of action includes bounding to the synaptosome membranes in the CNS and facilitating of the GAFA release. Benzodiazepines (including Diazepam) potentiate pre- and postsynaptic inhibition of the GAFA-receptors, potentiate inhibition of the dopaminergic neurons in substantia nigra. Diazepam reduces the fear sensation, and the anxiety. It reduces the psychomotor agitation. Diazepam possesses hypotensive effect and prominent peripheral myorelaxing action.

Supplied

10 and 100 ampoules, 2 ml/10 mg.

Expiry

2 years.