Pharmacology benzodiazepines

Benzodiazepines. Figure 3 Dissection of benzodiazepine pharmacology. The functional roles of GABAa receptor subtypes, mediating particular actions of diazepam, are indicated. A sign indicates that the respective response is mediated by the respective receptor subtype, a sign indicates that the respective response is apparently not mediated by the respective receptor subtype. ND = not determined. 

The subunits yi and ya characterize a small population of receptors that contain various types of a- and P-subunits. Due to their reduced affinity for the classical benzodiazepines, these receptors do not appear to contribute to any great extent to benzodiazepine pharmacology in vivo. 

Mohler H (2002) Pathophysiological aspects of diversity in neuronal inhibition a new benzodiazepine pharmacology. Dialogues Clin Neurosci 4 261-269 (this reference served as major source for the present article)... 

Mohler H, Fritschy JM, Rudolph U A new benzodiazepine pharmacology. J Pharmacol Exp Ther 2002 300 2. [PMID 11752090]... 

Triazolam, USP. Triazolam. 8-chloro-6-(o-chlorophc-nyl)-l-methyl-4Ay-j-triaz.olol4.3-a f l,4 benzxxliazcpinc (Hal-cion). has all of the characteristic benzodiazepine pharmacological actions. It is marketed as a sedative-hypnotic drug said to impair little, if any. daytime function. It is rapidly metabolized to the I-methyl alcohol, which is then conjugated and excreted. 

Pritchett DB, Sontheimer H, Shivers BD, Ymer S, Kettenmann H, Schofield PR, Seeburg PH (1989) Importance of a novel GABA receptor subunit for benzodiazepine pharmacology. Nature, 338, 582-585. 

Authors are designed row sensitive and selective test-systems for analysis of heavy metals, active chlorine, phenols, nitrates, nitrites, phosphate etc. for analysis of objects of an environment and for control of ions Ee contents in the technological solutions of KH PO, as well as for testing some of pharmacological psychotropic daigs alkaloids (including opiates), cannabis as well as pharmaceutical preparations of phenothiazines, barbiturates and 1,4-benzodiazepines series too. 

The anxiolytic agent buspirone (131) is notable for the fact that it does not interact with the receptor for the benzodiazepines. This difference in biochemical pharmacology is reflected in the fact that buspirone (131) seems to be devoid of some of the characteristic benzodiazepine side effects. The spiran function is apparently not required for anxiolytic activity. Alkylation of 3,3-dimethylglutarimide with dichlorobutane in the presence of strong base yields the intermedi-... 

The benzazepines are not as important pharmacologically as their more famous relatives the benzodiazepines. However, 3-aryl-2-(piperazin-l-yl)-5//-l-benzazepines, e.g. 14, and 17/-3-benzazepin-2-amines 15 possess neuroleptic activity,60 and antihypertensive activity,45 61 respectively. 

Although many factots contribute to drug dependence and misuse, only the pharmacological origins of benzodiazepine dependence will be considered here. The capacity of a benzodiazepine to induce dependence is telated to its... 

Griffiths RR, Wolf B Relative abuse liability of different benzodiazepines in drug abusers. J Clin Psychopharmacol 10 237-243, 1990 Griffiths RR, Weerts EM Benzodiazepine self-administration in humans and laboratory animals—implications for problems of long-term use and abuse. Psycho-pharmacology (Berl) 134 1-37, 1997... 

Pritchett DB, Seeburg PH Gamma-aminobutyric acidA receptor alpha3-subunit creates novel type II benzodiazepine receptor pharmacology. J Neurochem 34 1802-1804, 1990... 

Silberstein SD, McCrory DC Butalbital in the treatment of headache history, pharmacology, and efficacy. Headache 41 953-967, 2001 Smith DE, Wesson DR Benzodiazepine dependency syndromes. J Psychoactive Drugs 15 85-95, 1983... 

Van Sickle BJ, Tietz El Selective enhancement of AMPA receptor-mediated function in hippocampal CAl nemons from chronic benzodiazepine-treated rats. Nemo-pharmacology 43 11—27, 2002... 

Williams H, Oyefeso A, Ghodse AH Benzodiazepine misuse and dependence among opiate addicts in treatment. It J Psychol Med 13 62-64, 1996 Wiseman SM, Spencer-Peet J Prescribing for alcoholics a survey of drugs taken prior to admission to an alcoholism unit. Practitioner 229 88—89, 1985 Wolf B, Grohmann R, Biber D, et al Benzodiazepine abuse and dependence in psychiatric inpatients. Pharmacopsychiatry 22 54—60, 1989 Wood MR, Kim JJ, Han W, et al Benzodiazepines as potent and selective bradykinin B1 antagonists. J Med Chem 46 1803—1806, 2003 Zawertailo LA, Busto UE, Kaplan HL, et al Comparative abuse liability and pharmacological effects of meprobamate, triazolam, and butabarbital. J Clin Psycho-pharmacol 23 269-280, 2003... 

There is, however, a unique risk in the bipolar form that antidepressant treatment may trigger a switch into mania. This may occur either as the natural outcome of recovery from depression or as a pharmacological effect of the drug. Particular antidepressants (the selective serotonin reuptake inhibitors) seem less liable to induce the switch into mania than other antidepressants or electroconvulsive therapy. Treatment for mania consists initially of antipsychotic medication, for instance the widely used haloperidol, often combined with other less specific sedative medication such as the benzodiazepines (lorazepam intramuscularly or diazepam orally). The manic state will usually begin to subside within hours and this improvement develops further over the next 2 weeks. If the patient remains disturbed with manic symptoms, additional treatment with a mood stabilizer may help. 

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