Sedative Hypnotics flunitrazepam

A class of sedative/hypnotic type drug that exert their effects through the benzodiazepine binding site on GABAa receptors. The class consists both of molecules that contain the benzodiazepine moiety, for example diazepam, lorazepam and flunitrazepam, and the newer, non-benzodiazepine compounds such as zolpidem, zopiclone, indiplon and zaleplon. BzRAs are primarily used for the treatment of anxiety, insomnia and to elicit varying levels of sedation. The wide selection of compounds currently available affords the prescribing clinician extensive options in terms of relative efficacies and durations of action. 

Benzodiazepine The family name for a group of drugs with anticonvulsant, muscle relaxant and sedative-hypnotic properties. Examples include chlorodiazepoxide (Librium), diazepam (Valium), flunitrazepam and temazepam. These drugs have largely superseded the barbiturates. 

Nevertheless, the GABAergic properties of benzodiazepines remain their most important clinical application. Over the past 30 years, the most widely used benzodiazepine drug has been diazepam (1.6). It is an anxiolytic, sedative, and muscle relaxant the anxious, depressed person becomes more outgoing and relaxed. There have been many diazepam analogs. Oxazepam (4.177) and lorazepam (4.178) have similar effects. Temazepam (4.179), flunitrazepam (4.180), and flurazepam (4.181) are useful sedative-hypnotics. Clonazepam (4.182) is a clinically useful anticonvulsant. Brotizolam (4.183), a novel benzodiazepine analog, seems to be an effective sedative-hypnotic. Midazolam (4.184) is an imidazolo-benzodiazepine that is water soluble and thus easily injectable. It is a hypnotic sedative with marked amnestic (i.e., memory loss) properties and is used in dentistry, endoscopic procedures, and induction to anesthetics in the elderly and in... 

Flunitrazepam (Rohypnol), also known as roofies, is a benzodiazepine with physiological effects similar to diazepam (Valium), although it is about 10 times more potent. The drug produces sedative-hypnotic effects that include muscle relaxation and amnesia it can also produce physical and psychological dependence. It is illegal and not approved for use in the United States. 

Although some sedative-hypnotics such as the nonbarbiturates glutethimide (Doriden) and methaqualone (Quaalude) were once legally prescribed drugs, these substances were banned from use in the United States because of their potential for addiction and abuse. Some sedative-hypnotics such as flunitrazepam (Rohypnol) are illegal in the United States but are legal in Europe and Latin America. 

Finally, very rapid onset benzodiazepines have been widely reported as a means of "date rape," by using a small tasteless dose of the drug to make the victim incapable of protecting herself (or himself). This produces intoxication but not dependence. The drug most commonly used in this situation has been flunitrazepam (Rohypnol, "roofies," not available in the USA) and more recently GHB. The amnesia-producing effects of the benzodiazepines (see Chapter 22 Sedative-Hypnotic Drugs) make the victim unable to describe the events after she or he has recovered. 

Flunitrazepam is a tranquilizer developed in the 1960s by Hoffmann-LaRoche, Inc., and first marketed under the trade name Rohypnol in Switzerland in 1975. It is a member of a class of drugs called the benzodiazepines, which includes drugs such as Librium , Xanax , and Valium. This family of sedative-hypnotic drugs is used to treat anxiety, convulsions, muscle tension, and sleep disorders. Rohypnol is a very powerful sedative that can last up to 12 hours, with some residual effects lasting as long as 24 hours. Rohypnol is 10 times more potent than the most commonly known benzodiazepine, Valium (Figure 2.1). 

Finally the scaffold behind one of the most famous class of drugs the benzodiazepines, such as diazepam (Vilium), and the other sedatives, hypnotics, and anticonvulsants flunitrazepam, midazolam, lorazepam, etc. 

Lorazepam (la) in 2 or 4 mg doses showed hypnotic activity in insomniacs and good sedation in surgical premedication.41 Flurazepam (2h) is useful in the long term treatment of insomnia42 and shows no rebound effect after withdrawal.43 Flunitrazepam (2 ) has hypnotic activity in man at 2.5 mg, but does not induce physiological sleep.44 Fosazepam (2j) at 60-80 mg decreased sleep onset and awakening in healthy subjects.45 Quazepam (Sch 16134 2k) has been entered in the USAN listing as a sedative, hypnotic.46 Clobazam (9a) at 10—20 mg, but not triflubazam (9b) was useful for limited sleep difficulties in healthy males.47... 

Many benzodiazepines have potent hypnotic activity and are useful in the treatment of insomnia. Examples include flurazepam (Dalmane, A.93), midazolam (Versed, A.94), temazepam (Restoril, A.95), and triazolam (Halcion, A.96) (Figure A.28). Flunitrazepam (Rohypnol, A.97) is a particularly notorious sedative. Often called roofie or the date rape drug, flunitrazepam causes sedation and amnesia. Because of flunitrazepam s tendency to be abused, almost all nations tightly regulate the drug s availability. 

Hypnotics, sedatives, and tranquillisers benperidol, clonazepam, flunitrazepam, flupenthixol, halo-peridol, lorazepam, lormetazepam, triazolam, trifluoperazine. 

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