Anxiety pain from apprehension & depression, acute & chronic stress of life, skeletal muscle spasm & strychnine poisoning. For surgical measures, Diazepam is a useful premedication (I.M. route recommended).
Benzodiazepine; Anxiolytic
Diazepam attaches to the specific site on the GABA receptor and potentiates the effect of GABA, which acts by opening chloride ion channels into cells. Diazepam is absorbed rapidly and completely after oral administration. Peak Plasma concentration reaches within 15-90 minutes. Mean plasma half-life is 30 hours. Plasma protein binding is 98-99%. Diazepam is metabolized in the liver with only traces of the unchanged drug excreted in urine. A very small proportion of the metabolites is excreted through the bile into the intestine and eliminated with the feces. After rectal administration in suppository form diazepam is significantly absorbed and peak concentration reaches within 1.5-2 hours.
Diazepam 15 to 30 mg daily in divided doses.
Concomitant intake with alcohol is not recommended. Sedation may be increased due to concomitant use of neuroleptics (antipsychotics), hypnotics, sedative antihistamines and CNS depressants e.g., general anesthetics, narcotic analgesics or antidepressants. Diazepam clearance is increased by concomitant administration of phonobarbitone and is decreased by administration of cimetidine. Omeprazole and isoniazide inhibit diazepam metabolism.
Diazepam is contraindicated in patients with known history of hypersensitivity to it. Porphyria or a family history of porphyria contraindicates the use of Diazepam.
Infrequent & mild. Drowsiness, headedness, ataxia, vertigo, dry mouth, inattentiveness, hypotension, gastro-intestinal & visual disturbances.
Pregnancy category D . Breastfeeding is not recommended during treatment
Sedation, muscle weakness, profound sleep or paradoxical excitation. In more severe cases symptoms may include ataxia, hypotonia, hypotension, respiratory depression and rarely coma and death.
Store in a cool (below 25˚C temperature) and dry place protected from light.
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