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meprobamate (Equanil, Miltown)

Tradenames: Equanil, Miltown. DEA-controlled substance: class 4. Indication: treatment of anxiety disorders. Contraindications: 1) CNS depression 2) narrow-angle glaucoma 3) severe, uncontrolled pain Dosage: 400 mg PO TID/QID. Tabs: 200, 400, 600 mg. Pharmacokinetics: 1) well absorbed from GI tract 2) peak concentrations of 5-30 ug/mL reached 1-3 hours after oral dose of 400 mg 3) uniformly distributed throughout the body 4) crosses placenta 5) plasma protein binding 20% 6) elimination 1/2life of 6-16 hours, generally 10-11 hours 7) rapidly metabolized in liver 8) metabolites excreted in urine 9) 10-12% excreted unchanged in urine within 24 hours Dosage adjustment in renal failure: 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] Adverse effects: 1) common (> 10%) - drowsiness, clumsiness, ataxia 2) less common (1-10%) - blurred vision, skin rashes, wheezing, diarrhea, dizziness, vomiting 3) uncommon (< 1%) - thrombocytopenia, paradoxical excitement, leukopenia, confusion, dyspnea, syncope, slurred speech, headache, euphoria, purpura, peripheral edema, chills, bronchospasm, renal failure, dermatitis*, stomatitis, Stevens-Johnson syndrome 4) 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 Overdose: 1) plasma levels of 30-100 ug/mL associated with mild overdose, stupor or light coma 2) plasma levels of 100-200 ug/mL associated with deep coma & potential fatality 3) fatality associated with plasma levels > 200 ug/L Drug interactions: alcohol & other CNS depressants Laboratory: 1) methods: GLC, HPLC 2) labs with Loincs - meprobamate in specimen - meprobamate in blood - meprobamate in gastric fluid - meprobamate in saliva - meprobamate in serum/plasma - meprobamate in urine

Interactions

drug adverse effects (more general classes)

General

sedative/hypnotic (tranquilizer)

Properties

MISC-INFO: elimination route LIVER 1/2life 11.3 HOURS therapeutic-range 6-12 UG/ML toxic-range >60 UG/ML protein-binding <5% elimination by hemodialysis + peritoneal dialysis + pregnancy-category D

Database Correlations

PUBCHEM cid=4064

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995

Component-of

aspirin/meprobamate