temazepam (Restoril)
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Introduction
Tradename: Restoril. DEA-controlled substance: class 4.
Indications
short-term management of transient insomnia
Contraindications
Dosage
Tabs: 7.5, 15 & 30 mg.
Pharmacokinetics
- protein binding is 96%
- time to peak effect within 2-3 hours
- extensively metabolized in the liver primarily by conjugation
- metabolites are pharmacologically inactive[2]
- excreted mainly in the urine as inactive metabolites
- elimination 1/2life is 9-12 hours
elimination via kidney
1/2life = 8-25 hours
protein binding = 98 %
elimination by hemodialysis = -
Adverse effects
- common (> 10%)
- drowsiness, fatigue, impaired coordination, lightheadedness, memory impairment, insomnia, dysarthria, anxiety, decreased libido, depression, headache, dry mouth, constipation, diarrhea, decreased salivation, nausea/vomiting, tachycardia, chest pain, blurred vision, sweating, rash, increased or decreased appetite
- less common (1-10%)
- uncommon (< 1%)
- menstrual irregularities, blood dyscrasias, reflex slowing, drug dependence
- drug adverse effects of benzodiazepines
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- disulfiram, nefazodone, fluoxetine, flovoxamine, cimetidine, ranitidine, erythromycin, grapefruit juice decrease metabolism of benzodiazepines
- CNS depressants, EtOH: in combination increase CNS depression
- antiepileptic agents, rifampin: increase metabolism of benzodiazepines
- flumazenil (Romazicon): is a benzodiazepine antagonist
- probenecid may inhibit glucuronide conjugation
- drug interaction(s) of methadone in combination with benzodiazepines
- drug interaction(s) of benzodiazepines with antidepressants
- drug interaction(s) of benzodiazepines with thiazide diuretics
- drug interaction(s) of antipsycotics with benzodiazepines
- drug interaction(s) of antidepressants with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of alcoholic beverage with benzodiazepines
- drug interaction(s) of benzodiazepine with opiates
Laboratory
Mechanism of action
- produces CNS depression at the subcortical level & at higher doses, the cortical level as well
- potentiates inhibitory effects of GABA by increasing neuronal membrane permeability to chloride
More general terms
References
- ↑ 1.0 1.1 The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 2.0 2.1 2.2 Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 7
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995