meprobamate (Equanil, Miltown)
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Introduction
Tradenames: Equanil, Miltown. DEA-controlled substance: class 4.
Indications
treatment of anxiety disorders
Contraindications
- CNS depression
- narrow-angle glaucoma
- severe, uncontrolled pain
Dosage
Tabs: 200, 400, 600 mg.
Dosage adjustment in renal failure
Table
| creatinine clearance | dosage |
|---|---|
| 10-50 mL/min | every 9-12 hours |
| < 10 mL/min | every 12-18 hours |
Dosage adjustment probably necessary with hepatic insufficiency[2]
Pharmacokinetics
- well absorbed from GI tract
- peak concentrations of 5-30 ug/mL reached 1-3 hours after oral dose of 400 mg
- uniformly distributed throughout the body
- crosses placenta
- plasma protein binding 20%
- elimination 1/2life of 6-16 hours, generally 10-11 hours
- rapidly metabolized in liver
- metabolites excreted in urine
- 10-12% excreted unchanged in urine within 24 hours
elimination via liver
1/2life = 11.3 hours
protein binding = <5 %
elimination by hemodialysis = +
elimination by peritoneal dialysis = +
Adverse effects
- common (> 10%)
- drowsiness, clumsiness, ataxia
- less common (1-10%)
- uncommon (< 1%)
- other
- physical & psychologic dependence may occur taper over 1-3 weeks
* allergic reaction may occur in patients with history of dermatitis, generally by 4th dose
- plasma levels of 30-100 ug/mL associated with mild overdose, stupor or light coma
- plasma levels of 100-200 ug/mL associated with deep coma & potential fatality
- fatality associated with plasma levels > 200 ug/L
Drug interactions
alcohol & other CNS depressants