Flunitrazepam chemical structure
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Flunitrazepam

Flunitrazepam (formerly marketed under the trade name Rohypnol in the United States) is a drug which is a benzodiazepine derivative. It has powerful sedative, anxiolytic, and skeletal muscle relaxant properties. more...

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History

Flunitrazepam was first synthesized in the early 1970s by Roche and was used in hospitals when deep sedation was needed. It first entered the commercial market in Europe in 1975, and in the 1980s it began to be available in other countries.

It originally came in 1mg, 2mg, and 5mg sizes, but due to its potency and potential for abuse, the higher doses were taken off the market and it is now only available in 1mg.

Pharmacology

Like other benzodiazepines, flunitrazepam's pharmacological effects include sedation, muscle relaxation, reduction in anxiety, and prevention of convulsions. However, flunitrazepam's sedative effects are approximately 7 to 10 times more potent than diazepam. The effects of flunitrazepam appear approximately 15 to 20 minutes after oral administration, and last for approximately four to six hours. Some residual effects can persist up to 12 hours or more after administration.

Medical Uses

Flunitrazepam has not been approved by the Food and Drug Administration for medical use in the United States.

Illegal Uses

Use as a date rape drug

Flunitrazepam is known to induce anterograde amnesia in sufficient doses; individuals are unable to remember certain events that they experienced while under the influence of the drug. This effect is particularly dangerous when flunitrazepam is used to aid in the commission of sexual assault; victims may not be able to clearly recall the assault, the assailant, or the events surrounding the assault.

It is difficult to estimate just how many flunitrazepam-facilitated rapes have occurred in the United States. Very often, biological samples are taken from the victim at a time when the effects of the drug have already passed and only residual amounts remain in the body fluids. These residual amounts are difficult, and sometimes impossible, to detect using standard screening assays available in the United States. If flunitrazepam exposure is to be detected at all, urine samples need to be collected within 72 hours and subjected to sensitive analytical tests. The problem is compounded by the onset of amnesia after ingestion of the drug, which causes the victim to be uncertain about the facts surrounding the rape. This uncertainty may lead to critical delays or even reluctance to report the rape and provide appropriate biological samples for testing. If a person suspects that he or she is the victim of a flunitrazepam-facilitated rape, he or she should get laboratory testing for flunitrazepam as soon as possible.

It must be noted that an inability to remember events, including sexual encounters, is not conclusive evidence of having consumed a drugged drink: Drunkenness itself causes blackouts, sleepiness, and a reduction in inhibitions. Only a timely screening for flunitrazepam can demonstrate its use.

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Comparison of zolpidem , triazolam , and flunitrazepam effects on arterial blood gases and control of breathing in patients with severe chronic obstructive
From CHEST, 3/1/90 by D. Murchiano

Patients with severe COPD commonly suffer from insomnia. However, hypnotic drugs are generally contraindicated in these patients because of their depressant effect on the respiratory centers. New hypnotic drugs with short half-lives are now available. The aim of this study was, therefore, to compare the effects of 2 benzodiazepine hypnotics, T, 0.25 mg (half-life, 2.7 hr) and F, 1 mg (half-life, 19 h), and also of a new drug, Z, 10 mg (half-life), 2.4 h), an imidazopyridine compound, in hypercapnic COPD patients. Nine COPD patients (mean [PaO.sub.2] 60 [+ or -] 5 and mean [PaCO.sub.2] 48 [+ or -] 7 mm Hg) gave their oral informed consent and were studied in stable state. In all the patients, the following measurements were performed: [PaO.sub.2] and [PaCO.sub.2] minute ventilation (Ve), and mouth occlusion pressure ([P.sub.0.1]). Rebreathing [CO.sub.2] tests with Read's method were also performed, and the slopes of the changes in Ve and in [P.sub.0.1] while increasing [PaCO.sub.2] ([delta] Ve/[delta][PaCO.sub.2] and [delta] [P.sub.0.1]/[delta][PaCO.sub.2]) were calculated. The measurements were performed in a randomized double-blind fashion, each patient receiving 1 of each drug (Z, T, or F) on 3 different days. Each measurement in a given patient was separated by a 1-week interval, a control measurement being performed before each drug administration. Measurements were performed 2 hours after each drug administration, since maximum plasmatic level has been shown to be achieved at that time for the 3.drugs. No difference in [PaO.sub.2], [PaCO.sub.2], Ve, [P.sub.0.1], [delta]Ve/[delta][PaCO.sub.2], and [delta][P.sub.0.1]/[delta] [PaCO.sub.2] was noted between control measurements and 2 hours after administration of T and Z. Two hours after administration of F, a significant difference was noted in [PaCO.sub.2] (50 [+ or -] 6 during control vs 54.5 [+ or -] 7 mm Hg 2 h after F, p < 0.01) and [delta]Ve/[delta][PaCO.sub.2] (0.42 [+ or -] 0.23 during control vs 0.29 [+ or -] 0.21 1. [min.sup.-1] mm Hg 2 h after F, p < 0.01). [PaO.sub.2] also decreased from 60.5 [+ or -] 7 to 57.5 [+ or -] 8 mm Hg 2 hours after F, but this decrease did not reach significance. This study demonstrates that, given at single equivalent doses, hypnotic drugs (T and Z) with short half-lives have no significant effect on arterial blood gases and control of breathing in severe COPD patients, compared with a long-half-life hypnotic (F). Long-term administration of T or Z should, therefore, be evaluated in severe COPD patients, since sleep disturbances are a major problem in these patients.

COPYRIGHT 1990 American College of Chest Physicians
COPYRIGHT 2004 Gale Group

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