Products
Flunitrazepam is commercially available in the form of film-coated tablets (Rohypnol). It has been approved in many countries since 1975.
Structure and properties
Flunitrazepam (C16H12FN3O3, Mr = 313.3 g/mol) is a lipophilic, fluorinated and nitrated 1,4-benzodiazepine. It exists as a white to yellowish crystalline powder that is practically insoluble in water.
Effects
Flunitrazepam (ATC N05CD03) has sleep-inducing and sedative as well as antianxiety, muscle relaxant, and anticonvulsant properties. Because of its lipophilicity, it enters the brain well. The effects are due to binding to benzodiazepine receptors and enhancement of GABA-ergic neurotransmission.
Indications
For short-term therapy of sleep disorders. Flunitrazepam is not approved as a sedative in many countries.
Abuse
Flunitrazepam (“roofies”) is abused on the one hand as a centrally acting and depressant narcotic and to enhance the effects of other substances. It also has a bad reputation as a known so-called “date rape drug.” Flunitrazepam was secretly added to alcoholic beverages by the perpetrators in order to anesthetize women and then sexually abuse them. The victims may not have been able to remember the crime the following day because flunitrazepam induces memory loss. Rohypnol tablets contain the color additive indigocarmine (E 132, indigotine) to prevent abuse as a “date rape drug.” The tablets are colored green, solutions blue. The color additive is intended to make it recognizable that a drink has been spiked with the benzodiazepine. However, the odorless and tasteless flunitrazepam is also manufactured illegally without the color additive, and generic drugs with ordinary formulations are also on the market.
Dosage
According to the prescribing information. The usual dose for adults is 0.5 to 1 mg immediately before bedtime. Flunitrazepam should be used only short-term up to a maximum of 2 to 4 weeks. Discontinuation should be gradual.
Contraindications
For complete precautions, see the drug label.
Interactions
Flunitrazepam is metabolized by CYP2C19 and CYP3A4. Alcohol, centrally depressant drugs, narcoanalgesics, muscle relaxants, and CYP inhibitors (e.g., cimetidine) may increase effects and adverse reactions.
Adverse effects
The most common potential adverse effects include drowsiness, headache, dizziness, nightmares, fatigue, and dry mouth. The side effects may also occur the following day due to the long half-life of up to 35 hours. Other possible adverse effects include paradoxical reactions, anterograde amnesia, and depression. Flunitrazepam can be physically and psychologically addictive, cause withdrawal symptoms, and lose its effectiveness over time. Dangerous overdose and drug-drug interactions are possible.
