FLUNITRAZEPAM

Class

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

FLUNITRAZEPAM commonly prescribed for

(Bold for FDA approved)

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

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

sedation

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

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

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