HOME WEB NEWS IMAGES CLASSIFIEDS YELLOW PAGESPOLLS - SURVEYS WIKI COUNTRIES PHOTOS US UK INDIA
Cities Stocks Weather Movies Coupons Travel Blogs Health Horoscope Maps ASIA EUROPE Classifieds Yellow Pages
 student athletes, two brothers, cole haan, haan men, view all, all posts | ||
|
nova scotia, added jan, your business employmen, vacancy, news | ||
|
STEELPRODUCTS - steel product | ||
 1
|
| |
| |
| Bromazepam | |
| Systematic (IUPAC) name | |
| 9-bromo-6-pyridin-2-yl- 2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one | |
| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C14H10BrN3O |
| Mol. mass | 316.2 |
| Pharmacokinetic data | |
| Bioavailability | 84% |
| Metabolism | Hepatic |
| Half life | 12-20 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
D (USA) |
| Legal status |
Schedule IV(US) |
| Routes | Oral |
Bromazepam (marketed under brand names Calmepam, Compendium, Creosedin, Durazanil, Lectopam, Lexaurin, Lexilium, Lexomil, Lexotan, Lexotanil, Normoc, Novepam, Somalium, Lexatin)PubChem Substance: Bromazepam National Center of Biotechnology Information. is a drug which is a benzodiazepine derivative. It has mainly anxiolytic and at highr doses also sedative, hypnotic and skeletal muscle relaxant properties (see P.I. information on links).
Contents |
Bromazepam is a "classical" benzodiazepine, other classical benzodiazepines include; diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, flurazepam and clorazepate.Braestrup C; Squires RF. (Apr 1978). "Pharmacological characterization of benzodiazepine receptors in the brain.". Eur J Pharmacol 48 (3): 263-70. PMID 639854. Its molecular structure is composed of a diazepine connected to a benzene ring and a pyridine ring, the benzene ring having a bromine atom attached to it.Bromazepam Eutimia.com - Salud Mental. © 1999-2002. It is a 1,4-benzodiazepine, which means that the nitrogens on the seven-sided diazepine ring are in the 1 and 4 positions.
Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing inhibitory effects of GABA. Other neurotransmitters are not influenced. Bromazepam is intermediate-short acting benzodiazepine and is lipophilic, is metabolised hepatically via oxidative pathways.Oelschläger H. (4). "[Chemical and pharmacologic aspects of benzodiazepines]". Schweiz Rundsch Med Prax. 78 (27-28): 766-72. PMID 2570451. It does not possess any antidepressant qualities.
Bromazepam is reported to be metabolized by a hepatic enzyme belonging to the Cytochrome P450 family of enzymes. In 2003, a team led by Dr. Oda Manami at Oita Medical University reported that CYP3A4 was not the responsible enzyme, seeing as itraconazole, a known inhibitor of CYP3A4, did not effect its metabolism.Oda M, Kotegawa T, Tsutsumi K, Ohtani Y, Kuwatani K, Nakano S. "The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers." European Journal of Clinical Pharmacology. 2003 Nov;59(8-9):615-9. Epub 2003 Sep 27. PMID 14517708 English Fulltext (registration required) Japanese Fulltext (PDF, no registration) In 1995, J. van Harten at Solvay Duphar B.V.\'s Department of Clinical Pharmacology in Weesp reported that fluvoxamine, which is a potent inhibitor of CYP1A2, a less potent CYP3A4 inhibitor, and a negligible inhibitor of CYP2D6, does inhibit its metabolism.van Harten J. "Overview of the pharmacokinetics of fluvoxamine." Clinical Pharmacokinetics. 1995;29 Suppl 1:1-9. PMID 8846617
The active metabolite of bromazepam is hydroxybromazepam, which has half life approximatly equal to bromazepam.
Patients treated with bromazepam for generalised anxiety disorder were found to experience withdrawal symptoms such as a worsening of anxiety, as well as the development of physical withdrawal symptoms when abruptly withdrawn from bromazepam.Chouinard G; Labonte A, Fontaine R, Annable L (1983). "New concepts in benzodiazepine therapy: rebound anxiety and new indications for the more potent benzodiazepines". Prog Neuropsychopharmacol Biol Psychiatry 7 (4-6): 669-73. PMID 6141609.
Bromazepam shares with other benzodiazepines the risk of abuse, misuse, psychological and/or physical dependence. According to many psychiatric experts Bromazepam has a greater abuse potential than other benzodiazepines because of fast resorption and rapid onset of action. Due to its relatively short halflife and duration of action (8 to 12 hours), withdrawal symptoms may be more severe and more frequently encountered than with long acting benzodiazepines.
It is also available as Lexotanil in Bangladesh, Colombia, Greece, Pakistan, United Arab Emirates and Venezuela.
It is available as Lexotan and Somalium in Australia, Brazil, Portugal, Singapore, and the Philippines.
It is available as Lexilium in the Republic of Macedonia and Serbia (also as a generic, produced by ZORKA Pharma). Bromazepam is also available in Canada as Lectopam. Bromazepam is available in Yemen as Novepam and in Cambodia as Lexomil. And it is also available in Spain as Lexatin.
Usually, 3 mg to 6 mg at bedtime, with additional 1.5 mg to 3 mg during the next day if needed. Malnourished patients, patients with compromised cardiovascular, liver or renal function, and elderly patients should receive lower doses. In hospitalized patients with severe agitation and/or anxiety, daily doses of up to 24 mg have been given and tolerated for a limited period of time. A 3 mg dose of bromazepam is equivalent to a 5 mg dose of diazepam.
All common side-effects of benzodiazepines have been noted. Consult the article under Diazepam. Euphoria, leading to a high abuse potential, is quite often reported.
Up to 30% treated on a long-term basis develop a form of dependence, i.e. these patients cannot stop the medication without experiencing physical and/or psychological benzodiazepine withdrawal symptoms.
Leukopenia and liver-damage of the cholostatic type with or without jaundice (icterus) have additionally been seen; the original manufacturer Roche recommends regular laboratory examinations to be performed routinely.
Ambulatory patients should be warned that Bromazepam may impair the ability to drive vehicles and to operate machinery. The impairment is worsened by consumption of alcohol, because both act as central nervous system depressants. During the course of therapy, tolerance to the sedative effect usually develops.
The general contraindications for benzodiazepines apply. Consult the section under Diazepam.
In 1987, a team of scientists lead by Ochs reported that the elimination half-life, peak serum concentration, and serum free fraction are significantly elevated and the oral clearance and volume of distribution significantly lowered in elderly subjects.Ochs HR, Greenblatt DJ, Friedman H, Burstein ES, Locniskar A, Harmatz JS, Shader RI. "Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol." Clinical Pharmacology & Therapeutics. 1987 May;41(5):562-70. PMID 2882883 The clinical consequence is that the elderly should be treated with lower doses than younger patients.
Bromazepam is a Schedule IV drug under the Convention on Psychotropic Substances.List of psychotropic substances under international control (PDF). International Narcotics Control Board.
This article is licensed under the GNU Free Documentation License. It uses material from Wikipedia