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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.
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