Bromazepam

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Bromazepam.jpg

[edit] MECHANISM OF ACTION

Bromazepam, like other Benzodiazepines bind to specific sites on the gamma-aminobutyric acid-A (GABAA) receptors. This enhances the effects of GABA by increasing its affinity for the GABAA receptor.

Activation of the GABAA receptor, which is linked to a chloride channel (Cl-), results in an influx of Cl- into the neurone causing hyperpolarisation, which results in inhibitory effects on the central nervous system.

Benzodiazepines action on GABAA receptors appears to produce their anxiolytic, sedative, muscle relaxant, hypnotic and anticonvulsant actions.

Bromazepam is an intermediate-acting benzodiazepine, its half-life in human plasma reported to be in the range of 11 to 22 hours.

In low doses Bromazepam reduces tension and anxiety. in high doses, sedative and muscle-relaxant properties appear.

[edit] INDICATIONS

Bromazepam is indicated for the short-term, symptomatic relief of tension, anxiety and agitation.

Note that anxiety or tension associated with the normal stress of everyday life usually does not require treatment with benzodizepines

[edit] DOSAGE

The recommended dose for most adults is 1.5-3 mg, two or three times daily.

Severe cases, especially in hospitalised cases: 6‑12mg two or three times daily.

Treatment should begin with low doses, gradually increasing to the optimum level. The duration of treatment should be as short as possible

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Bromazepam or to any drug in the benzodiazepine class
  • Severe liver failure
  • Pregnancy and lactation
  • Myasthenia gravis (Bromazepam could increase the muscle weakness)
  • Severe respiratory failure or sleep apnea syndrome

[edit] WARNINGS AND PRECAUTIONS

  • Do not drive or do other dangerous activities after taking Bromazepam until you feel fully awake.
  • Do not drink alcohol
  • Caution is required in patients with chronic respiratory failure (risk of respiratory depression).
  • Use of benzodiazepines can lead to dependence. This risk increases with dose and duration of treatment.
  • Amnesia: Benzodiazepines may induce anterograde amnesia leading to a partial or complete inability to recall the recent past. Anterograde amnesia may occur using higher therapeutic dosages, the risk increasing at higher dosages.
  • Withdrawal symptoms and rebound effect: headaches, muscle pain, rebound anxiety, insomnia, tension, restlessness, confusion and irritability were seen during discontinuation. In severe cases the following symptoms may occur: derealization, depersonalization, hyperacusis, numbness and tingling of the extremities, hypersensitivity to light, noise and physical contact, hallucinations or epileptic seizures. Bromazepam should be discontinued gradually
  • Paradoxical reactions like restlessness, agitation, irritability, aggressiveness, delusion, rages, nightmares, hallucinations, psychoses, inappropriate behavior and other adverse behavioral effects are known to occur when using benzodiazepines. Should this occur, the use of the drug should be discontinued.
  • Risk of Fetal Harm: Benzodiazepines can potentially cause fetal harm when administered to pregnant women

[edit] INTERACTIONS

Benzodiazepines, including Bromazepam, produce additive CNS depressant effects when co-administered with other medications which themselves produce CNS depression (e.g. barbiturates, alcohol, sedatives, tricyclic antidepressants, antipsychotics, skeletal muscle relaxants, antihistamines or narcotic analgesics and anaesthetics).

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

Bromazepam is well tolerated in therapeutic doses. The following undesirable effects may occur: Drowsiness, tiredness, headache, dizziness, reduced alertness, difficulty with coordination, diplopia and loss of libido.

See also WARNINGS AND PRECAUTIONS section

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://www.roche-australia.com/fmfiles/re7229005/downloads/central-nervous-agents/lexotan-pi.pdf

[edit] REFERENCES

Sedatives / Hypnotics / Anxiolytics
Benzodiazepines Benzodiazepines (Anxiolytics)‎ Alprazolam (Xanax)   Bromazepam (Lexotan, Lexotanil)   Chlordiazepoxide (Librium)   Clobazam (Frisium)   Clorazepate (Tranxene)   Clotiazepam (Rizen, Tienor)   Delorazepam (EN)   Diazepam (Valium)   Etizolam (Depas)   Ketazolam   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Noctamid)   Nordazepam (Nordaz)   Oxazepam (Serepax)   Prazepam (Demetrin, Lysanxia)
Benzodiazepines (Hypnotics) Brotizolam (Lendormin, Bondormin, Dormex, Sintonal, Noctilan)   Clobazam (Frisium)   Estazolam (Esilgan, ProSom)   Etizolam (Depas, Pasaden, Etilaam, Etizest)   Flunitrazepam (Rohypnol)   Flurazepam (Dalmadorm, Dalmane, Felison, Flunox, Valdorm)   Ketazolam (Anseren, Anxon)   Lorazepam (Ativan, Control, Lorans, Tavor, Temesta)   Lormetazepam (Loramet, Minias, Noctamid, Pronoctan, Evamyl)   Midazolam (Dormicum, Hypnovel)   Nitrazepam (Mogadon, Nitrados, Numbon, Radedorm, Alodorm)   Nordazepam (Madar, Nordaz, Stilny, Tranxilium N)   Temazepam (Normison, Restoril, Tenox, Temaze)   Triazolam (Halcion, Hypam, Rilamir)
Non-Benzodiazepine Hypnotics Eszopiclone (Lunesta)   Zolpidem (Ambien, Stilnox, Hypnogen, Sanval, Stilnoct, Zoldem, Zolsana)   Zopiclone (Imovane, Zimovane)
Melatonin agonists Melatonin (Circadin)   Ramelteon (Rozerem)
Orexin agonists Suvorexant (Belsomra)