Nitrazepam

Oral
Short-term management of insomnia

Oral
Infantile spasms

May be taken with or without food.

Myasthenia gravis, narrow-angle glaucoma, severe respiratory insufficiency, sleep apnoea syndrome, severe hepatic impairment, porphyria.

May induce anterograde amnesia; caution patients to have uninterrupted sleep of 7-8 hr after ingestion of dose. May impair ability to drive or operate machinery. Depression, especially if suicidal risk may be present. History of drug abuse or acute alcoholism. Hepatic and renal impairment. Respiratory disease. Debilitated patients. Patients who are at risk of falls. Children, elderly. Pregnancy and lactation.

Hypotension, palpitation; agitation, aggressiveness, amnesia, ataxia, confusion, delusions, disorientation, dizziness, fatigue, hallucination, hangover, headache, irritability, nightmares, psychoses, rage, restlessness, sedation; rash; changes in libido; constipation, diarrhoea, excessive salivation, heartburn, nausea, vomiting; granulocytopenia, leukopenia; falling, muscle weakness; blurred or double vision; tinnitus (associated with withdrawal); aspiration, increased bronchial secretion, dyspnoea.

Symptoms: Somnolence, drowsiness, confusion, ataxia, impaired reflexes, coma, dyspnoea, hypotension, respiratory and cardiovascular depression. Management: Supportive. Gastric lavage may be beneficial if performed soon after ingestion. Flumazenil may reverse benzodiazepine-induced CNS depression.

CNS depressant effect increased with alcohol, barbiturates, TCAs, phenothiazines, morphine derivatives. Effects may be antagonised by theophylline. Increased levels/effects with probenecid. Reduced levels/effects with rifampicin. May reduce effects of levodopa.

Increased CNS depression may occur with valerian, kava kava, St John's wort, gotu kola.

May cause false elevations (about 15%) in clozapine plasma levels.

Description: Nitrazepam is a benzodiazepine with a pronounced sleep-inducing activity. It depresses the reticular-activating system in the brainstem by enhancing the inhibitory effect of GABA on brain cells, thus preventing excessive brain activity.
Onset: 30-60 min.
Duration: 6-8 hr.
Pharmacokinetics:
Absorption: Fairly absorbed from the GI tract (oral). Peak plasma levels in 2-3 hr.
Distribution: Crosses the blood-brain barrier and placenta; enters breast milk (trace amounts). Protein-binding: 87%.
Metabolism: Hepatic by nitroreduction followed by acetylation.
Excretion: Urine (as free or conjugated metabolites); 24-30 hr (elimination half-life).

Store at room temperature. Protect from light and moisture.

Hypnotics & Sedatives