Flunitrazepam

Chemical Name 5-(2-fluorophenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one 

Bromoacetyl bromide Potassium nitrate Sodium hydride 

The combined methylene chloride extracts were dried over anhydrous sodium sulfate and the solvent removed to give the crude 2-amino-5-chloro-2 -fluorobenzophenone which upon recrystallization from methanol formed yellow needles melting at 94° to 95°C. 

0 grams of 2-amino-5-chloro-2 -fluorobenzophenone in 300 cc of tetrahydrofuran was hydrogenated at atmospheric pressure in the presence of 10 grams of charcoal (Norite), 

0 grams of potassium acetate and 2.5 cc of a 20% palladous chloride solution (20% by weight of palladium). After an initiation period varying from 10 minutes to an hour, hydrogen uptake was rapid and stopped completely after the absorption of the theoretical amount. 

The differences between the various diazepines with respect to the nature and duration of the effects of they produce are obviously of little relevance to the abuse of these substances. 

Diazepam is the most abused substance of all the benzodiazepines. Not only drug addicts, who use the substance as a bridging aid and to intensify other drug effects, have experience of diazepam, but so also do most medicament-dependent people and alcoholics. The age of first use is lower than in the case of other benzodiazepines, sometimes as early as childhood. Diazepam is therefore also important in the introduction of drugs to people who later exhibit mono- or polytoxicomania. 

The age of first use varies over a wide range, the average being 20-25 years, and, with the exception of a small number of experimental users, most patients abuse this substance over a period of at least 3 years. In a few cases, the duration of dependence exceeds 25 years [1]. 

Flunitrazepan is very well known in the area of general abuse of benzodiazepines. It is mainly taken by polytoxicomanes, who also use heroin, DHC, cocaine etc., usually in doses of up to 20 mg/day. The extent of the abuse of this drug among this group remains at a high level, and no decrease is yet in 

Limitation of the dose of this drug (since 01.04.94) to 1 mg per unit of medication (e.g. tablet) has hardly changed the abuse pattern. Dependents adjust the number of units of medication taken according to the feeling , although the problems of procurement are multiplied accordingly. 

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Timolol maleate a-Bromoacetophenone Nomifensine maleate Bromoacetyl bromide Bromazepam Cephapirin sodium Clonazepam Flunitrazepam 5-Bromoacetyl salicylamide Labetalol HCI m-Bromoanisole Tramadol HCI p-Bromoanisole Cyclofenil Bromobenzene... 

Ferroglycine sulfate Ferrous fumarate Fluoranthene Flora ntyrone Fluoroacetyl chloride Afloqualone p-Fluorobenzaldehyde Sulindac Fluorobenzene Flubendazole o-Fluorobenzoyl chloride Flunitrazepam... 

Narcotan - Halothane Narco26p Flunitrazepam Nardeizine Phenelzine sulfate Nardil - Phenelzine sulfate Narest Valethamate bromide Narigix Nalidixic acid Narsis - Medazepam Nasafarma - Oxymetazoline HCI Nazalide Flunisolide Nasal Yer Naphazoline Nasin Tetrahydrozoline HCI Nasivin - Oxymetazoline HCI Nasky Inositol niacinate Nasmil - Cromolyn sodium Nasophen - Phenylephrine HCI Natacillin - Hetacillln potassium Natacyn - Natamycin Natam - Flurazepam... 

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. 

CijHijClFNO 784-38-3) see Cinolazepam Doxefazepam Ethyl loflazepate Flunitrazepam Flurazepam Flutazolam Midazolam Quazepam... 

C2H2Br20 598-21-0) see Cefapirin Clonazepam Flunitrazepam Haloxazolam Ketazolam Sotalol bromoacetyl chloride... 

CfiHfiClN 106-47-8) see Acetarsol Alprazolam Diazepam Efavirenz Flunitrazepam Flutoprazepam Medazepam Quazepam... 

Bond C, LaForge KS, Tian M, et al Single-nucleotide polymorphism in the human mu opioid receptor gene alters beta-endorphin binding and activity possible implications for opiate addiction. Proc Natl Acad Sci U S A 95 9608-9613, 1998 Borron SW, Monier C, Risede P, et al Flunitrazepam variably alters morphine, bu-prenorphine, and methadone lethality in the rat. Hum Exp Toxicol 21 399-603, 2002... 

Kilicarslan T, Sellers EM Lack of interaction of buprenorphine with flunitrazepam metabolism. Am J Psychiatry 137 1164-1166, 2000 King SA, Strain JJ Benzodiazepines and chronic pain. Pain 41 3-4, 1990a King SA, Strain JJ Benzodiazepine use by chronic pain patients. Clin J Pain 6 143-147, 1990b... 

Note The detection limits for flunitrazepam and its 7-nitrodesmethyl metabolites are 1 to 2 ng/ml plasma or 0.5 ng substance per chromatogram zone. 

The biphasic dissociation of [ H]flunitrazepam binding (Chiu, Dryden and Rosenberg 1982). 

Competition binding studies showing that when using compounds like jS-CCE (ethyl- S-carboline-3-carboxylate), which bind to the benzodiazepine receptor, the displacement curve for [ H]flunitrazepam was shallow in the hippocampus and... 

Chiu, TH, Dryden, DM and Rosenberg, HC (1982) Kinetics of [ H]-labelled flunitrazepam binding to membrane-bound benzodiazepine receptors. Mol. Pharmacol. 21 57-65. 

Effect of Temperature on the Kinetics of [3H]-Flunitrazepam Binding to Rat Brain Homogenates... 

Nitration of benzodiazepines takes place at the electron rich C position, and this was used to prepare flunitrazepam (25), a potent hypnotic agent. 

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. 

Gentil Y, Tavares S, Gorenstein C, Bello C, Mathias L, Gronich G and Singer J (1990). Acute reversal of flunitrazepam effects by Ro 15-1788 and Ro 15-3505 Inverse agonism, tolerance and rebound. Psychopharmacology, 100, 54—59. 

Fig. 20.11. Substrate quality obtained by comparing basolateral-to-apical with apical-to-basolateral transport of substrates in polarized cell monolayers of MDR1-transfected cell lines [86] plotted versus (A) the log of the air/water partition coefficient, or (B) H-bond energy (arbitrary units, EUh cf. text). Units of the air/ water partition coefficient were [M ]. Compound (concentrations in Ref. [86] in brackets) were clozapine (50 nM) (1) cyclosporin A (2 tM) (2) daunorubicin (3) dexamethasone (2 tM) (4) digoxin (2 pM) (5) domperidone (2 pM) (6) etoposide (7) flunitrazepam (500 nM) (8) haloperidol (50 nM) (9) ivermectin (50 nM) (10) loperamide (2 pM) (11) morphine (2 pM) (12) ondansetron...

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