Flunitrazepam

Severe: Contraindicated.

Flunitrazepam May be taken with or without food.

Myasthenia gravis, sleep apnoea, severe pulmonary insufficiency or chronic obstructive airways disease with incipient respiratory failure. Severe hepatic impairment. Children.

Patient with CV disorders, respiratory disease or respiratory depression, acute narrow-angle glaucoma, seizure disorders; history of alcohol or drug abuse, insomnia, and those with psychological and psychiatric disorders. Debilitated patients. Avoid long-term use. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.

Significant: CNS depression; anterograde amnesia; paradoxical reactions (e.g. hyperactive or aggressive behaviour); hazardous sleep-related activities (e.g. sleep-driving, making phone calls, cooking and eating food while asleep); hypersensitivity reactions, including anaphylaxis and angioedema; tolerance, physical and psychological dependence (high dose and prolonged use); atropine-like reactions; increased risk of seizures (abrupt withdrawal). Rarely, blood dyscrasias.
Gastrointestinal disorders: Gastrointestinal upset, dry mouth.
Nervous system disorders: Headache, dizziness, tiredness, drowsiness, sleepiness, ataxia, confusion, excitation, tremor.
Vascular disorders: Hypotension.

This drug may cause drowsiness or dizziness, if affected, do not drive or operate machinery.

Monitor mental status, heart rate, blood pressure, respiratory function, CBC, liver and kidney function (periodically during long-term use).

Symptoms: Drowsiness, mental confusion and lethargy. Severe cases: Hypotension, hypotonia, ataxia, respiratory depression and coma.

Management: Symptomatic and supportive treatment. Administer activated charcoal to reduce absorption. May give flumazenil to reverse acute benzodiazepine effects.

May enhance CNS depressant effects with barbiturates, antipsychotics, antidepressants, anticonvulsants, antihistamines, sedatives, hypnotics, anaesthetics, skeletal muscle relaxants, and narcotic analgesics. May increase plasma levels with disulfiram and cimetidine. May potentiate the anticholinergic effects of atropine, antihistamines, and antidepressants. May enhance the sedative effect with cisapride.
Potentially Fatal: Increased risk of profound sedation, respiratory depression and coma with opioids.

Additive CNS depressant effect with alcohol.

Description:
Mechanism of Action: Flunitrazepam is an intermediate- to long-acting benzodiazepine. It binds to gamma-aminobutyric acid (GABA)-mediated neuroreceptors in the limbic system, thereby preventing GABAergic transmission which produces hypnotic or sedative effects.
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Bioavailability: 80-90%. Time to peak plasma concentration: 45 minutes.
Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 77-80%.
Metabolism: Extensively metabolised in the liver into 7-aminoflunitrazepam and N-desmethyl-flunitrazepam (active metabolites).
Excretion: Mainly via urine (80%; primarily as 7-aminoflunitrazepam; <2% unchanged or as N-desmethyl-flunitrazepam); faeces (10%). Elimination half-life: 16-35 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3380, Flunitrazepam. https://pubchem.ncbi.nlm.nih.gov/compound/Flunitrazepam. Accessed Nov. 4, 2025.

Store below 30°C.

Hypnotics & Sedatives

N05CD03 - flunitrazepam ; Belongs to the class of benzodiazepine derivatives. Used as hypnotics and sedatives.

Brayfield A, Cadart C (eds). Flunitrazepam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/08/2025.

Flunitrazepam. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 05/08/2025.