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mephobarbital (Mebaral)

 

Classes: Sedative/Hypnotics

Dosing and uses of Mebaral (mephobarbital)

 

Adult dosage forms and strengths

tablet

  • 32mg
  • 50mg
  • 100mg

 

Sedation

32-100 mg PO TID/QID; optimum dose is 50 mg PO TID/QId

 

Epilepsy

400-600 mg PO qDay; start with small dose and gradually increase over 4-5 days until optimum dosage determined

 

Other Indications & Uses

Anxiety; grand mal, petit mal seizures

 

Pediatric dosage forms and strengths

tablet

  • 32mg
  • 50mg
  • 100mg

 

Sedation

16-32 mg PO TID/QId

 

Epilepsy

< 5 years old: 16-32 mg PO TID/QId

> 5 years old: 32-64 mg PO TID/QId

 

Mebaral (mephobarbital) adverse (side) effects

Frequency not defined

Common

  • Somnolence

Less Common

  • Bradycardia, hypotension, hypoventilation
  • Agitation, confusion, hyperkinesia, ataxia, CNS depression, nightmares, nervousness
  • Constipation, nausea, vomiting

Rare

  • Fever
  • Headache
  • Rash

 

Warnings

Contraindications

Barbiturate sensitivity, porphyria, liver disease, severe respiratory disease

 

Cautions

Reduce dose in hepatic/renal impairment

Excreted in breast milk

 

Pregnancy and lactation

Pregnancy category: d

Lactation: excreted in breast milk; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Mebaral (mephobarbital)

Half-Life: >30 hr

Onset: 30-60 min

Duration: 10-16 hr

Bioavailability: 50%

Metabolism: N-demethylation, then glucuronate or sulfate conjugation

Metabolites: phenobarbitaL

Excretion: urine

Enzymes induced: CYP1A2, CYP2C9/10, CYP3A4

 

Mechanism of action

Depress cortical & cerebellar function