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Brotizolam- sedative-hypnotic thienotriazolodiazepine drug

Brotizolam is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. More

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Description

Brotizolam is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties.

Generic Name

Brotizolam- sedative-hypnotic thienotriazolodiazepine drug

Chemical names

Lendormin; Lendorm; Sintonal; 57801-81-7

Brand names

IUPAC name

4-bromo-7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.0²,?]trideca-2(6),4,7,10,12-pentaene

Pharmacokinetics

Actions

Dosage/Dosage form

250 mcg per day at bedtime, up to 2 weeks.

Therapeutic uses

Treatment of Insomnia.

Adverse effects/Side effects

Drowsiness and lightheadedness, sedation, muscle weakness and ataxia; less frequently vertigo, headache, confusion, depression, slurred speech, changes in libido, tremor, urinary retention, visual disturbances, GI disturbances, amnesia and changes in salivation.

Interaction

  • Enhanced sedation or respiratory and cardiovascular depression with drugs with CNS depressant properties such drugs are antihistamines, antidepressants, antipsychotics, general anaesthitics, other hypnotics or sedatives, opioid analgesics and cisapride.
  • Alcohol.
  • Calcium-channel blockers; diaxozide; clonidine; disulfiram; diuretics; clozapine; moxonidine; nabitone; cimetidine, nitrates; esomeprazole and omeprazole; muscle relaxants; dopaminergics; lofexidine; hydralazine, antifungals; Minoxidil, nitroprusside; angiotensin II receptor antagonist; antiepileptics; βeta-blockers; antibacterials

Contraindications

  • Preexisting CNS depression or coma, respiratory acute pulmonary insufficiency or depression, sleep apnoea; severe hepatic impairment;
  • Pregnancy and lactation.
  • Neonates.

Storage

Keep away from children.

Information

Molecular weight

393.689

Molecular formula

C15H10BrClN4S

CAS number

57801-81-7

Precautions

  • Chronic pulmonary insufficiency; elderly or debilitated patients; impaired liver or kidney function; muscle weakness, drowsiness may affect skilled tasks;
  • Monitor cardio-respiratory function when used for deep sedation; history of alcohol or drug addiction, personality disorders or organic brain changes.
  • Respiratory depression and hypotension with parenteral administration; this route should only be used when facilities for reversing respiratory depression are available. Dependence.