chlordiazepoxide (Librium)
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Introduction
Tradename: Librium. DEA-controlled substance: class 4.
Indications
Contraindications
Caution:
- not drug of choice in the elderly
- abrupt discontinuation may cause withdrawal
- avoid alcohol & other CNS depressants
Dosage
- anxiety, apprehension
- alcohol withdrawal: 25-100 mg IV/IM every 2-4 hours (symptom-triggered)[6]
- maximum: up to 300 mg IM or IV in 6 hour period & no more than 300 mg in 24 hours
Tabs: 5, 10, 25 mg.
Powder for injection: 100 mg
Dosage adjustment in renal failure
- for creatinine clearance < 10 mL/min, use 50% of dose
Pharmacokinetics
- peak effect after oral dose: < 2 hours
- protein binding: 95%
- metabolized by liver
- 1/2life 6-30 hours
- 1/2life prolonged in patients with liver disease
elimination via liver
1/2life = 6-30 hours
protein binding = 95 %
elimination by hemodialysis = -
Adverse effects
- common (> 10%)
- drowsiness, fatigue, impaired coordination, lightheadedness, memory impairment, insomnia, dysarthria, anxiety, decreased libido, depression, headache, dry mouth, decreased salivation, constipation, nausea/vomiting, diarrhea, tachycardia, chest pain, blurred vision, sweating, rash, increased or decreased appetitite
- less common (1-10%)
- uncommon (< 1%)
- menstrual irregularities, blood dyscrasias, reflex slowing, drug dependence & withdrawal
- other
- drug adverse effects of benzodiazepines
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- disulfiram, nefazodone, fluoxetine, fluvoxamine, cimetidine, erythromycin, estrogens & grapefruit juice increase chlordiazepoxide levels
- CNS depressants including tricyclic antidepressants (TCA) increase CNS depressive effects of chlordiazepoxide
- anti-epileptic agents & rifampin increase the metabolism of chlordiazepoxide
- flumazenil (Romazicon) antagonizes the effects of benzodiazepines
- carbamazepine may increase metabolism
- 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
- specimen:
- serum, plasma (EDTA)
- collect at trough concentration
- methods: HPLC, GLC, RIA
- laboratories with Loincs
Mechanism of action
- potentiates inhibitory effects of GABA by increasing neuronal membrane permeability to chloride
More general terms
Component of
- chlordiazepoxide/methscopolamine (Librax refomulated)
- chlordiazepoxide/clidinium (Librax)
- amitriptyline/chlordiazepoxide (Limbitrol)
- Librax
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 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, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 6.0 6.1 6.2 Medical Knowledge Self Assessment Program (MKSAP) 19. American College of Physicians, Philadelphia 2021