(Bold for FDA approved)
• Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex
• Enhances the inhibitory effects of GABA
• Boosts chloride conductance through GABA-regulated channels
• Inhibitory actions in sleep centers may provide sedative hypnotic effects
• Generally takes effect in less than an hour
• Sedation, fatigue, depression
• Dizziness, ataxia, slurred speech, weakness
• Forgetfulness, confusion
• Hyperexcitability, nervousness
• Rare hallucinations, mania
• Rare hypotension
• Hypersalivation, dry mouth
• Rebound insomnia when withdrawing from long-term treatment
• Respiratory depression, especially when taken with CNS depressants in overdose
• Rare hepatic dysfunction, renal dysfunction, blood dyscrasias
unusual
common
• Wait
• To avoid problems with memory, only take flunitrazepam if planning to have a full night’s sleep
• Lower the dose
• Switch to a shorter-acting sedative hypnotic
• Switch to a non-benzodiazepine hypnotic
• Administer flumazenil if side effects are severe or life-threatening
• 0.5–1 mg/day at bedtime
• Tablet 0.5 mg, 1 mg, 2 mg, 4 mg
• Not generally intended for long-term use
• Use is not recommended to exceed 4 weeks
• Some patients may develop dependence and/or tolerance; risk may be greater with higher doses
• History of drug addiction may increase risk of dependence
• Currently classified as Schedule III by the World Health Organization
• Currently classified as a Schedule IV drug in the USA, but not legally available in the USA
• Drug should be used with caution
• Dose should be lowered
• Should not be used in patients with severe hepatic insufficiency, as it may precipitate encephalopathy
• Benzodiazepines have been used to treat insomnia associated with acute myocardial infarction
• Initial starting dose 0.5 mg at bedtime; maximum generally 1 mg/day at bedtime
• Paradoxical reactions with restlessness and agitation are more likely to occur in the elderly
• Safety and efficacy have not been established
• Not recommended for use in children or adolescents
• Paradoxical reactions with restlessness and agitation are more likely to occur in children
• Positive evidence of risk to human fetus; contraindicated for use in pregnancy
• Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects
• Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy
• Unknown if flunitrazepam is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk
• Recommended either to discontinue drug or bottle feed
• Effects on infant have been observed and include feeding difficulties, sedation, and weight loss
Based on data Published online by Cambridge University Press
Compiled by Dr. Jash Ajmera