Halazepam

Chemical Name 7-Chloro-1 cllhvdro-5-phenvl-1-(2,2 -trifluoroethvl)-2H-1,4-benzodi-azepine-2-one 

Prepares solution of sodium methylate by dissolving 3.9 g of sodium metal in 500 ml of methanol. Add 39.0 g of 7-chloro-1,3-dihydro-5-phenyl-2H-1,4-benzodiazeplne-2-one. Evaporate the reaction mixture to a residue and dissolve the residue in 170 ml of dimethylformamide. Add 30 g of 2,2,2-trifluoroethyl Iodide and stir at room temperature for Vi hour, then heat to 60°C to 70°C for an additional 7 hours. Add 19 g of 2,2,2-trifluoroethyl iodide and resume the heating and stirring at 60°C to 70°C for an additional 16 hours. Filter off the solids and evaporate the filtrate to a residue in vacuo. Triturate the residue with water and extract with ethyl ether. Wash the ethereal extract with water, dry over anhydrous sodium sulfate and evaporate the solvent to a residue. 

Extract the residue with ethyl ether and filter. Concentrate the ethereal extract to a residue. Dissolve the residue in benzene and chromatograph on 300 g of alumina contained In a glass column 1.5 inches in diameter to give the crude product. Elute with benzene. Crystallize this product from acetone-petroleum ether to obtain the product. 

---

The benzodiazepines currently available for clinical use vary substantially in pharmacokinetics, acute euphoriant effects, and frequency of reported dependence. It is likely, therefore, than not all benzodiazepines have the same potential for abuse. Diazepam, lorazepam, and alprazolam may have greater abuse potential than chlordiazepoxide and clorazepate (Wolf et al. 1990). Similarly, oxazepam has been reported to produce low levels of abuse (Eliding 1978). Jaffe et al. (1983) found that in recently detoxified alcoholic patients, halazepam produces minimal euphoria even at a supratherapeutic dosage. The development of partial agonist and mixed agonist/antagonist compounds at the benzodiazepine receptor complex may offer an advantage over approved benzodiazepines for use in alcoholic patients. 

Iwata N, Cowley DS, Radel M, et al Relationship between a GABA alpha g Pro385Ser substitution and benzodiazepine sensitivity. Am] Psychiatry 156 1447—1449,1999 Jacobson AF, Dominguez RA, Goldstein B, et al Comparison of buspirone and diazepam in generalized anxiety disorder. Pharmacotherapy 5 290—296, 1985 Jaffe JH, Ciraulo DA, Nies A, et al Abuse potential of halazepam and diazepam in patients recently treated for acute alcohol withdrawal. Clin Pharmacol Ther 34 623-630, 1983... 

Jaffe JH, Ciraulo DA, Nies A, et al Abuse potential of halazepam and of diazepam in patients recently treated for acute alcohol withdrawal. Clin Pharmacol Ther 34 623-630, 1983... 

Halazepam Paxipam Oral Long 60-160 Anxiety disorders, alcohol withdrawal... 

Halazepam Halazepam, 7-chloro-1 -(2, 2, 2 -trifluoro-1 -ethy 1)-l,3-dihydro-5-pheny 1-2//-l,4-benzodiazepin-2-one (5.1.19), also differs from diazepam in that it has a substituent on the nitrogen atom in the first position of the benzodiazepine system, which in this case is represented by the 2, 2, 2 -trifluoroethyl group. It can be made by any of the diagrams described above [13,14],... 

The pharmacological properties of halazepam are basically the same as those of diazepam, the only difference being that they are shorter lasting. They are primarily used for conditions of anxiety. The most common synonym is paxipam. 

X = 0 Halazepam Anxiolytic Schering-Plough (1981) X = S Quazepam Hypnotic Schering-Plough (1987)... 

Some fluoroamine moities are now present in drugs such as halazepam and quazepam (Figure 8.34) and LGD-2941 (Figure 8.73). Fluoroamines are less basic and cannot be protonated at physiologic pH (cf. Chapter 3). 

Benzodiazepines [P] Decreased metabolism of alprazolam, chlordiazepoxide, diazepam, halazepam, prazepam, and clorazepate but not oxazepam, lorazepam, or temazepam. 

OFFICIAL NAMES Alprazolam (Xanax), chlorazepate (Tranxene) chlordiazepoxide (Librium, Novopoxide), clonazepam (Klonopin), clorazepate (Tranxene), diazepam (Valium, Vivol), estazolam (ProSom), flurazepam (Dalmane, Novoflupam, Somnol), flunitrazepam (Rohypnol), halazepam (Paxipam), lorazepam (Ativan), nitrazepam (Mogadon), oxazepam (Serax), prazepam (Centrax), quazepam (Doral), temazepam (Restoril), triazolam (Halcion)... 

Halazepam see Benzodiazepine Halcion see Benzodiazepine Haldol see Tranquilizers Haloperidol see Tranquilizers Halothane see Inhalants Halotussin DM see Dextromethorphan Hardhay see Herbal drugs Hardware see Inhalants Hash see Marijuana Hash oil see Marijuana Hashish see Marijuana Hashish oil see Marijuana Hat man see Heroin... 

---