Bromazepam

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Bromazepam (marketed under several brand names, including Lectopam , Lexotan , Lexilium , Lexaurin Brazepam , Bromaze , Somalium and Lexotanil ) are benzodiazepines medicine derivative, patented by Roche in 1963 and developed clinically in the 1970s. It is primarily an anti-anxiety agent with side effects similar to diazepam (Valium). Besides being used to treat anxiety or panic states, bromazepam can be used as premedan before small surgery. Bromazepam usually comes in doses of 3 mg and 6 mg tablets. Bromazepam is contraindicated and should be used with caution in pregnant women, elderly, patients with a history of alcohol or substance abuse disorder and other children. The prolonged use of bromazepam causes tolerance and may cause physical and psychological dependence on drugs, and as a result, it is a drug controlled by international law.

Video Bromazepam

Indication

• Short-term treatment of severe anxiety.

Maps Bromazepam

Side effects

Bromazepam has side effects similar to other benzodiazepines. The most commonly reported side effects are drowsiness, sedation, ataxia, memory impairment, and dizziness. Impaired memory function is common with bromazepam and includes reduced working memory and reduced ability to process environmental information. A healthy 1975 experiment, male students explored the effects of four different drugs on learning capacity observing that taking bromazepam alone at 6 mg 3 times daily for 2 weeks of significantly impaired learning capacity. In combination with alcohol, impairment in learning capacity becomes more pronounced. Various studies reported memory impairment, processing of visual information and sensory data and psychomotor performance disorders; cognitive impairment including attention capacity and impaired co-ordination skills; disruption of reactive performance and attention, which may interfere with driving skills; drowsiness and decreased libido. The deficiency after taking bromazepam, however, is less clear than other benzodiazepines such as lorazepam.

Occasionally, benzodiazepines can cause extreme changes in memory such as anterograde amnesia and amnesia automatism, which may have medical-legal consequences. Such reactions occur usually only at higher end doses of the specified spectrum.

Very rarely, dystonia can develop.

Up to 30% long-term treatment develops a dependency form, ie these patients can not stop treatment without experiencing withdrawal symptoms of physical and/or psychological benzodiazepines.

Leukopenia and colostatic-type liver damage with or without jaundice (jaundice) have also been seen; Roche's original manufacturer recommends routine laboratory checks to be done on a regular basis.

Outpatients should be warned that bromazepam may damage the ability to move the vehicle and operate the machine. The damage is exacerbated by alcohol consumption, as both act as depressants of the central nervous system. During therapy, tolerance to the effects of sedatives usually develops.

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Tolerance, Dependency, and Withdrawal

Bromazepam shares with other benzodiazepines the risks of abuse, abuse, psychological dependence or physical dependence. Withdrawal studies show both psychological dependence and physical dependence on bromazepam including rebound anxiety characterized after 4 weeks of chronic use. Those whose doses were gradually reduced did not withdraw.

Patients treated with bromazepam for generalized anxiety disorders were found to experience withdrawal symptoms such as worsening anxiety, as well as the development of physical withdrawal symptoms when abruptly withdrawn bromazepam. Sudden or over rapid withdrawal of bromazepam after chronic use even at prescribed doses of therapy may lead to severe withdrawal syndrome including epileptic status and conditions that resemble delerium tremens.

Animal studies have shown that administration of diazepam or chronic bromazepam causes a decrease in spontaneous locomotor activity, decreased noradrenaline and dopamine and serotonin turnover, increased tyrosine hydroxylase activity and elevated catecholamine levels. During withdrawal of bromazepam or diazepam decreased tryptophan, serotonin levels occur as part of the benzodiazepine withdrawal syndrome. Changes in the level of these chemicals in the brain can cause headaches, anxiety, tension, depression, insomnia, anxiety, confusion, irritability, sweating, dysphoria, dizziness, derealization, depersonalization, numbness/tingling of extremities, hypersensitivity to light, sound, and odor, perceptual distortion, nausea, vomiting, diarrhea, loss of appetite, hallucinations, delirium, seizures, tremors, abdominal cramps, myalgia, agitation, palpitations, tachycardia, panic attacks, short-term memory loss, and hyperthermia.

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Contraindications and special precautions

Benzodiazepines require special precautions when used in elderly, pregnant, child, alcohol, or drug dependent individuals and with comorbid psychiatric disorders.

Custom population

• In 1987, a team of scientists led by Ochs reported that the elimination of part-time, peak serum concentrations, and serum-free fractions increased significantly and oral clearance and distribution volume decreased significantly in the subjects of the elderly. The clinical consequence is that the elderly should be treated with a lower dose than the younger patients.
• Bromazepam can affect the driving and the ability to operate the machine.
• Bromazepam is the category of pregnancy D, a classification which means that bromazepam has been shown to cause harm to the fetus. The product information brochure Hoffman LaRoche warns about breastfeeding while taking bromazepam. There is at least one report of sudden infant death syndrome associated with breastfeeding when taking bromazepam.

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Interactions

Cimetidine, fluvoxamine and propranolol cause a clear increase in the elimination of bromazepam half-life which leads to an increase in bromazepam accumulation.

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Pharmacology

Bromazepam is a "classical" benzodiazepine; Other classical benzodiazepines include; diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, flurazepam, and clorazepate. Its molecular structure consists of diazepine connected to a benzene ring and a pyridine ring, a benzene ring having a single nitrogen atom that replaces one of the carbon atoms in the ring structure. It is 1,4-benzodiazepine, which means that the nitrogens on the seven-sided diazepine ring are in positions 1 and 4.

Bromazepam binds to GABA GABA receptor _A , causing conformational changes and increasing GABA inhibitory effect. Bromazepam is a long and lipophilic benzodiazepine and is metabolized by the liver through oxidative pathways. It does not have antidepressant or antipsychotic qualities.

After the administration of bromazepam at night, a very significant reduction in gastric acid secretion occurred during sleep followed by a very significant increase in gastric acid production the following day.

Bromazepam alters the electrical state of the brain leading to increased beta activity and decreased alpha activity in EEG recording.

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Pharmacokinetics

Bromazepam is reportedly metabolized by liver enzymes belonging to the cytochrome P450 family of enzymes. In 2003, the team led by Dr. Oda Manami at Oita Medical University reports that CYP3A4, a member of the Cytochrome P450 family, is not a responsible enzyme because itraconazole, a known CYP3A4 inhibitor, does not affect metabolism. In 1995, J. van Harten at Solvay Duphar B.V. The Department of Clinical Pharmacology at Weesp reports that fluvoxamine, which is a potential inhibitor of CYP1A2, a less potent CYP3A4 inhibitor, and a negligible CYP2D6 inhibitor, inhibits metabolism.

The active metabolite of bromazepam is hydroxybromazepam, which has about the same half-life as bromazepam.

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Overdose

Bromazepam is commonly involved in drug overdose. Severe benzodiazepine overdoses can cause alpha coma type patterns. The toxicity of bromazepam in overdose increases when combined with other CNS depressant drugs such as alcohol or sedative hypnotics. Bromazepam is the most commonly involved benzodiazepine in a deliberate overdose in France. Bromazepam is also responsible for the accidental intoxication of companion animals. A review of benzodiazepine poisoning in cats and dogs from 1991-1994 found that bromazepam is responsible for significantly more poisoning than other benzodiazepines.

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Drug abuse

Bromazepam has a similar risk of misuse such as benzodiazepines such as diazepam. In France car accidents involving psychotropic drugs in combination with alcohol (itself a major contributor) found benzodiazepines, especially diazepam, nordiazepam, and bromazepam, became the most common drug in the bloodstream, almost twice that of the most common cannabis drug. Bromazepam has also been used in serious criminal offenses including robbery, murder, and sexual harassment.

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Legal status

Bromazepam is a drug Schedule IV under the Convention on Psychotropic Substances.

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Synthesis

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See also

• Benzodiazepine
• Benzodiazepine dependency
• Benzodiazepine withdrawal syndrome

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References

External links

• Bromazepam drug information from Lexi-Comp. Includes dosage information and a complete list of international brand names.
• Inchem - Bromazepam
• LEXOTAN product information leaflet from Roche Pharmaceuticals

Source of the article : Wikipedia