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FLUNITRAZEPAM

ClassFLUNITRAZEPAM commonly prescribed forHow FLUNITRAZEPAM worksHow long until FLUNITRAZEPAM worksNotable Side EffectsLife Threatening Side Effectsweight gainsedationWhat to do about FLUNITRAZEPAM side effectsusual dosage rangeDosage Formslong term usehabit formingRenal ImpairmentHepatic ImpairmentCardiac ImpairmentElderlyChildren and AdolescentsPregnancyBreast Feeding

THERAPEUTICS

Class

  • Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM)
  • Benzodiazepine (hypnotic)

FLUNITRAZEPAM commonly prescribed for

(Bold for FDA approved)

• Short-term treatment of insomnia (severe, disabling)
• Catatonia

How FLUNITRAZEPAM works

• 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

How long until FLUNITRAZEPAM works

• Generally takes effect in less than an hour

SIDE EFFECTS

Notable Side Effects

• 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

Life Threatening Side Effects

• Respiratory depression, especially when taken with CNS depressants in overdose

• Rare hepatic dysfunction, renal dysfunction, blood dyscrasias

weight gain

unusual

unusual

sedation

common

common

What to do about FLUNITRAZEPAM side effects

• 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

DOSING AND USE

usual dosage range

• 0.5–1 mg/day at bedtime

Dosage Forms

• Tablet 0.5 mg, 1 mg, 2 mg, 4 mg

long term use

• Not generally intended for long-term use

• Use is not recommended to exceed 4 weeks

habit forming

• 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

SPECIAL POPULATIONS

Renal Impairment

• Drug should be used with caution

Hepatic Impairment

• Dose should be lowered

• Should not be used in patients with severe hepatic insufficiency, as it may precipitate encephalopathy

Cardiac Impairment

• Benzodiazepines have been used to treat insomnia associated with acute myocardial infarction

Elderly

• 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

Children and Adolescents

• 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

Pregnancy

• 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

Breast Feeding

• 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