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	1812-30-2
ATC code	N05BA08
PubChem	2441
DrugBank	?
Chemical data
Formula	C14H10BrN3O
Mol. mass	316.2
Pharmacokinetic data
Bioavailability	84%
Metabolism	Hepatic
Half life	10-20 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	D (USA) Image File history File links This is a lossless scalable vector image. ... Image File history File links Size of this preview: 518 × 600 pixelsFull resolution (1000 × 1158 pixel, file size: 171 KB, MIME type: image/png) File history Legend: (cur) = this is the current file, (del) = delete this old version, (rev) = revert to this old version. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article or section does not cite any references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number bromine, Br, 35 Chemical series halogens Group, Period, Block 17, 4, p Appearance gas/liquid: red-brown solid: metallic luster Atomic mass 79. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ present in vertebrates and some other animals. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The kidneys are organs that filter wastes (such as urea) from the blood and excrete them, along with water, as urine. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...
Legal status	Schedule IV(US) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... The Controlled Substances Act (CSA), Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970, is the legal foundation of the United States governments fight against the abuse of drugs and other substances. ...
Routes	Oral

Bromazepam (marketed under brand names Calmepam, Compendium, Creosedin, Durazanil, Lectopam, Lexaurin, Lexilium, Lexomil, Lexotan, Lexotanil, Normoc, Somalium)^[1] is a drug which is a benzodiazepine derivative. It has sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Alprazolam 2mg tablets The benzodiazepines (pronounced , or benzos for short) are a class of psychoactive drugs considered as minor tranquilizers with varying hypnotic, sedative, anxiolytic, anticonvulsant, muscle relaxant and amnesic properties, which are brought on by slowing down the central nervous system. ... A sedative is a substance which depresses the central nervous system (CNS), resulting in calmness, relaxation, reduction of anxiety, sleepiness, slowed breathing, slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes. ... Hypnotic drugs are a class of drugs that induce sleep, used in the treatment of severe insomnia. ... An anxiolytic is a drug prescribed for the treatment of symptoms of anxiety. ... In medicine, a muscle relaxant is a drug that causes skeletal muscle contraction to cease. ...

Pharmacology

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.^[2] It is a 1,4-benzodiazepine, which means that the nitrogens on the seven-sided diazepine ring are in the 1 and 4 positions. Diazepine is a seven-membered heterocyclic compound with two nitrogen atoms (e. ... Benzene is an organic chemical compound with the formula C6H6. ... Pyridine is a chemical compound with the formula C5H5N. It is a liquid with a distinctively putrid odour. ... General Name, Symbol, Number bromine, Br, 35 Chemical series halogens Group, Period, Block 17, 4, p Appearance gas/liquid: red-brown solid: metallic luster Atomic mass 79. ... Alprazolam 2mg tablets The benzodiazepines (pronounced , or benzos for short) are a class of psychoactive drugs considered as minor tranquilizers with varying hypnotic, sedative, anxiolytic, anticonvulsant, muscle relaxant and amnesic properties, which are brought on by slowing down the central nervous system. ...

Bromazepam binds to the GABA receptor GABA_A, causing a conformational change and increasing inhibitory effects of GABA. Other neurotransmitters are not influenced. It does not possess any antidepressant qualities. 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. Gaba may refer to: Gabâ or gabaa (Philippines), the concept of negative karma of the Cebuano people GABA, the gamma-amino-butyric acid neurotransmitter GABA receptor, in biology, receptors with GABA as their endogenous ligand Gaba 1 to 1, an English conversational school in Japan Marianne Gaba, a US model... The GABAA receptor is one of the three ligand-gated ion channels responsible for mediating the effects of Gamma-AminoButyric Acid (GABA), the major inhibitory neurotransmitter in the brain. ...

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.^[3] 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.^[4] Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... Itraconazole (marketed as Sporanox® by Janssen Pharmaceutica) is a triazole antifungal agent that is prescribed to patients with fungal infections. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... Year 1995 (MCMXCV) was a common year starting on Sunday (link will display full 1995 Gregorian calendar). ... Weesp (population: 17,843 in 2004) is a town in the north-western Netherlands, in the province of North Holland. ... Fluvoxamine (brand name as Luvox®, Faverin®, Fevarin® and Dumyrox®) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... Cytochrome P450 2D6 (CYP2D6), a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. ...

The active metabolite of bromazepam is hydroxybromazepam.

Indications

• Short-term treatment of insomnia
• Short-term treatment of anxiety or panic attacks, if a benzodiazepine is required
• Alleviation of the symptoms of alcohol- and opiate-withdrawal, under close clinical supervision

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Availability

Bromazepam is available as a generic in Canada, Germany, The Netherlands, Chile, Italy, France, Macedonia, Bulgaria, Bosnia, Portugal, Poland, Kosovo, Switzerland. It is also available in Greece, Bangladesh, United Arab Emirates, Pakistan, Venezuela and Columbia in the form of Lexotanil, in Australia, Belgium, Brazil, Singapore and Portugal in the form of Lexotan and Somalium, and in Serbia and Macedonia registered as Lexilium.

Dosage

Usually, 3mg to 6mg at bedtime, with additional 1.5mg to 3mg 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 24mg have been given and tolerated for a limited period of time. A 3mg dose of bromazepam is equivalent to a 5mg dose of diazepam. Diazepam (IPA: ), marketed under brand names Valium, Stesolid, Diazemuls, Seduxen, Bosaurin, Diapam, Antenex, Ducene, Apozepam and Pax (South Africa))[1] is a drug which is a benzodiazepine derivative. ...

Side-effects

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. Diazepam (IPA: ), marketed under brand names Valium, Stesolid, Diazemuls, Seduxen, Bosaurin, Diapam, Antenex, Ducene, Apozepam and Pax (South Africa))[1] is a drug which is a benzodiazepine derivative. ...

Up to 30% treated on a long-term basis develop a form of dependence known as 'low-dose-dependence', i.e. these patients do not need increasing doses to experience the feeling of 'well-being' caused by the drug.

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. Hoffmann-La Roche, Ltd. ...

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.

Contraindications

The general contraindications for benzodiazepines apply. Consult the section under Diazepam. Diazepam (IPA: ), marketed under brand names Valium, Stesolid, Diazemuls, Seduxen, Bosaurin, Diapam, Antenex, Ducene, Apozepam and Pax (South Africa))[1] is a drug which is a benzodiazepine derivative. ...

Special Populations

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.^[5] The clinical consequence is that the elderly should be treated with lower doses than younger patients. The volume of distribution (VD) is a pharmacological term used to quantify the distribution of a drug throughout the body after oral or intravenous dosing. ...

Legal Status

Bromazepam is a Schedule IV drug under the Convention on Psychotropic Substances.^[6] The Controlled Substances Act (CSA), Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970, is the legal foundation of the United States governments fight against the abuse of drugs and other substances. ... Convention on Psychotropic Substances Opened for signature February 21, 1971 in Vienna Entered into force August 16, 1976 Conditions for entry into force 40 ratifications Parties 175 The Convention on Psychotropic Substances is a United Nations treaty designed to control psychoactive drugs such as amphetamines, barbiturates, and psychedelics. ...

References

External links

• Inchem - Bromazepam