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Pronunciation
(me proe BA mate)
Generic Available (U.S.)
Yes
Index Terms
Controlled Substance
C-IV
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Management of anxiety disorders
Use: Dental
Treatment of muscle spasm associated with acute temporomandibular joint (TMJ) pain; management of dental anxiety disorders
Use: Unlabeled/Investigational
Demonstrated value for muscle contraction, headache, premenstrual tension, external sphincter spasticity, muscle rigidity, opisthotonos-associated with tetanus; treatment of muscle spasm associated with acute temporomandibular joint (TMJ) pain
Pregnancy Risk Factor
D
Lactation
Enters breast milk/not recommended
Breast-Feeding Considerations
Breast milk concentrations are higher than plasma; effects are unknown.
Contraindications
Hypersensitivity to meprobamate, related compounds (including carisoprodol), or any component of the formulation; acute intermittent porphyria
Warnings/Precautions
Concerns related to adverse effects:
• Allergic reactions: May occur in patients with history of dermatological condition (usually by fourth dose).
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Depression: Use with caution in patients with depression or suicidal tendencies.
• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Renal impairment: Use with caution in patients with renal impairment.
• Seizure disorder: Use with caution in patients with a history of seizure disorder.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Elderly: Use with caution in the elderly; may cause confusion, cognitive impairment, excessive sedation, or addiction with prolonged use (Beers Criteria).
Other warnings/precautions:
• Abrupt discontinuation: May precipitate withdrawal.
Adverse Reactions
Frequency not defined.
Cardiovascular: Arrhythmia EEG abnormalities, hypotensive crisis, peripheral edema, palpitation, syncope, tachycardia
Central nervous system: Ataxia, chills, dizziness, drowsiness, euphoria, fever, headache, overstimulation, paradoxical excitement, slurred speech, vertigo
Dermatologic: Angioneurotic edema, bruising, dermatitis, erythema multiforme, petechiae, purpura, rash, Stevens-Johnson syndrome
Gastrointestinal: Diarrhea, nausea, proctitis, stomatitis, vomiting
Hematologic: Agranulocytosis, aplastic anemia, eosinophilia, leukopenia, porphyria exacerbation, thrombocytopenic purpura
Neuromuscular & skeletal: Paresthesia, weakness
Ocular: Impairment of accommodation
Renal: Anuria, oliguria
Respiratory: Bronchospasm
Miscellaneous: Anaphylaxis, hypersensitivity
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Yohimbine: May diminish the therapeutic effect of Antianxiety Agents. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
Mechanism of Action
Affects the thalamus and limbic system; also appears to inhibit multineuronal spinal reflexes
Pharmacodynamics/Kinetics
Onset of action: Sedation: ~1 hour
Distribution: Crosses placenta; enters breast milk
Metabolism: Hepatic
Half-life elimination: 10 hours
Excretion: Urine (8% to 20% as unchanged drug); feces (10% as metabolites)
Dosage
Oral:
Anxiety:
Children 6-12 years: 200-600 mg/day in 2-3 divided doses
Adults: 1200-1600 mg/day in 3-4 divided doses, up to 2400 mg/day
Muscle spasm (TMJ) pain (unlabeled use): Adults: 1200-1600 mg/day in 3-4 divided doses, up to 2400 mg/day
Dosing interval in renal impairment:
Clcr 10-50 mL/minute: Administer every 9-12 hours
Clcr <10 mL/minute: Administer every 12-18 hours
Hemodialysis: Moderately dialyzable (20% to 50%)
Dosing adjustment in hepatic impairment: Probably necessary in patients with liver disease
Dental Usual Dosing
Muscle spasm (TMJ) pain or anxiety: Adults: Oral: 400 mg 3-4 times/day, up to 2400 mg/day
Monitoring Parameters
Mental status
Reference Range
Therapeutic: 6-12 mcg/mL (SI: 28-55 μmol/L); Toxic: >60 mcg/mL (SI: >275 μmol/L)
Patient Education
Drug may cause physical and/or psychological dependence. Do not use alcohol or other prescription or OTC medications (especially pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration unless instructed to restrict fluid intake. You may experience drowsiness, lightheadedness, impaired coordination, dizziness, blurred vision, nausea, vomiting, dry mouth, or diarrhea. Report persistent CNS effects, skin rash or irritation, changes in urinary pattern, wheezing or respiratory difficulty, or worsening of condition.
Geriatric Considerations
Meprobamate is not considered a drug of choice in the elderly because of its potential to cause physical and psychological dependence. Interpretive guidelines from the Centers for Medicare and Medicaid Services (CMS) strongly discourage the use of meprobamate in residents of long-term care facilities.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria severity: High).
Additional Information
Withdrawal should be gradual over 1-2 weeks. Benzodiazepine and buspirone are better choices for treatment of anxiety disorders.
Anesthesia and Critical Care Concerns/Other Considerations
Withdrawal should be gradual over 1-2 weeks. Benzodiazepines and buspirone are better choices for treatment of anxiety disorders.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Nursing: Physical Assessment/Monitoring
Assess for history of addiction; long-term use can result in dependence, abuse, or tolerance; periodically evaluate need for continued use. Monitor for CNS depression. Taper dosage slowly when discontinuing.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral: 200 mg, 400 mg
Pricing: U.S. (www.drugstore.com)
Tablets (Meprobamate)
200 mg (30): $47.99
400 mg (100): $157.99
References
Hassan E, “Treatment of Meprobamate Overdose With Repeated Oral Doses of Activated Charcoal,” Ann Emerg Med, 1986, 15(1):73-6.
Jacobsen D, Wiik-Larsen E, Saltvedt E, et al, “Meprobamate Kinetics During and After Terminated Hemoperfusion in Acute Intoxications,” J Toxicol Clin Toxicol, 1987, 25(4):317-31.
Volturo GA, “Meprobamate and Bezoar Formation,” Ann Emerg Med, 1987, 16(4):472-3.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
Content last modified May 2011
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