Brotizolam

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Brotizolam.jpg

[edit] MECHANISM OF ACTION

Brotizolam, 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.

Brotizolam is a short-acting thieno-diazepine hypnotic (average elimination half-life is 4.4 hours). It shortens the time needed to fall asleep, reduces the frequency of awakenings, and prolongs total sleep time.

[edit] INDICATIONS

Short-term treatment of insomnia, such as difficulty in falling asleep and staying asleep.

[edit] DOSAGE

The recommended dose for most adults is 0.25 mg before retiring. In elderly and in patients in whom clearance is decreased, it is recommended that treatment with Brotizolam be initiated at 0.125 mg.

Patients should allow for 7-8 hours sleep after taking the tablet.

Treatment should not exceed several weeks, except in justifiable cases

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Brotizolam or to other benzodiazepines
  • Brotizolam may be used in patients with open angle glaucoma who are receiving appropriate therapy, but is contraindicated in patients with acute narrow angle glaucoma.
  • Pregnancy and breastfeeding
  • Myasthenia gravis (Brotizolam could increase the muscle weakness)
  • Severe respiratory failure or sleep apnea syndrome
  • Severe liver failure

[edit] WARNINGS AND PRECAUTIONS

  • Do not drive or do other dangerous activities after taking Brotizolam until you feel fully awake.
  • Avoid drinking alcohol
  • Respiratory depression may occur in benzodiazepine overdose
  • Use of benzodiazepines can lead to dependence. This risk increases with dose and duration of treatment and in patients with a history of alcohol or drug abuse.
  • Withdrawal symptoms like convulsions, tremor, abdominal and muscle cramps, vomiting, sweating, appetite decrease, weight loss, anxiety and insomnia were seen following abrupt discontinuation. Brotizolam should be discontinued gradually.
  • Paradoxical reactions like restlessness, agitation, irritability, aggressiveness, increased muscle spasticity, insomnia have been reported when using benzodiazepines. Should this occur, the use of the drug should be discontinued.
  • 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.
  • Risk of Fetal Harm: Benzodiazepines can potentially cause fetal harm when administered to pregnant women

[edit] INTERACTIONS

  • Benzodiazepines, including Brotizolam, 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

  • Benzodiazepines can potentially cause fetal harm when administered to pregnant women. If Brotizolam is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Because of experience with other members of the benzodiazepine class, Brotizolam is assumed to be capable of causing an increased risk of congenital abnormalities when administered to a pregnant woman during the first trimester. Because use of these drugs is rarely a matter of urgency, their use during pregnancy, especially in the first trimester is contraindicated
  • Nursing mothers: Benzodiazepines are known to be excreted in human milk. It should be assumed that Brotizolam is as well. Chronic administration of diazepam to nursing mothers has been reported to cause their infants to become lethargic and to lose weight. As a general rule, nursing should not be undertaken by mothers who must use Brotizolam.

[edit] SIDE EFFECTS

Common side effects include: drowsiness, fatigue and ataxia (lack of voluntary coordination of muscle movements), especially in elderly or debilitated patients. These effects may be lessened by a reduction in dosage.


Infrequently reported side effects:

  • Central Nervous System: Sedation and sleepiness, depression, lethargy, apathy, hypoactivity, lightheadedness, disorientation, restlessness, confusion, delirium, headache, slurred speech, dysarthria, syncope, vertigo, tinnitus, dizziness, nervousness, vivid dreams, psychomotor retardation.
  • Gastrointestinal: Constipation, diarrhea, dry mouth, nausea, vomiting, increased salivation.
  • Genitourinary: Incontinence, dysuria, enuresis, changes in libido, urinary retention, menstrual irregularities.
  • Cardiovascular: Bradycardia, tachycardia, hypertension, hypotension, palpitations.
  • Opthalmological: Visual disturbances, diplopia
  • Dermatological: Urticaria, pruritus, skin rash, dermatitis.
  • Other: Hepatic dysfunction (including hepatitis and jaundice), blood dyscrasias including agranulocytosis, anemia, thrombocytopenia, eosinophilia.

See also WARNINGS AND PRECAUTIONS section

[edit] RELATED LINKS

[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)