MEPHOBARBITAL (me-foe-bar'bi-tal)
Mebaral, Methylphenobarbital Classifications: anticonvulsant; barbiturate; sedative-hypnotic; Therapeutic: anticonvulsant; sedative-hypnotic Prototype: Phenobarbital Pregnancy Category: D Controlled Substance: Schedule IV
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Availability
32 mg, 50 mg, 100 mg tablets
Action
Long-acting barbiturate that limits the spread of seizure activity by increasing the threshold for motor cortex stimuli.
Exerts strong sedative effect, but relatively mild hypnotic effect.
Therapeutic Effect
Reduces seizure activity by decreasing excitability in nerve cells. Depresses CNS producing drowiness, hypnosis, and sedation.
Uses
To control grand mal and petit mal epilepsy, alone or in combination with other anticonvulsant agents, and for sedative
effect in management of delirium tremens and other acute agitation and anxiety states.
Contraindications
Hypersensitivity to barbiturates; coma; ethanol intoxication hepatic encephalopathy; porphyria; status epilepticus; pregnancy
(category D).
Cautious Use
Fever, hyperthyroidism, alcoholism; respiratory disorders, COPD, sleep apnea; mental status changes, major depression; suicidal
ideation; liver, kidney, or cardiac dysfunction; lactation.
Route & Dosage
Anticonvulsant Adult: PO 400600 mg/d in divided doses Child: PO ≤5 y, 1632 mg t.i.d. or q.i.d.; ≥5 y, 3264 mg t.i.d. or q.i.d.
Sedative Adult: PO 32100 mg t.i.d. or q.i.d. Child: PO ≤5 y, 1632 mg t.i.d. or q.i.d.; ≥5 y, 3264 mg t.i.d. or q.i.d.
Delirium Tremens Adult: PO 200 mg t.i.d. or q.i.d.
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Administration
Oral
- Change from other anticonvulsant by gradually tapering off the former as mephobarbital doses are increased to maintain seizure
control.
- When prescribed concurrently with phenobarbital, dose should be about one-half the amount of each used alone. When prescribed
concurrently with phenytoin, the dose of phenytoin is usually reduced.
- Reduce discontinued drug dosage gradually over 4 or 5 d to avoid precipitating seizures of status epilepticus.
Adverse Effects (≥1%)
CNS: Drowsiness, dizziness, unsteadiness, hangover, paradoxical excitement.
GI: Nausea, vomiting,
constipation.
Body as a Whole: Hypersensitivity reactions, respiratory
depression.
Interactions
Drug: Alcohol, cns depressants compound
CNS depression; may decrease absorption and increase
metabolism of
oral anticoagulants; increases
metabolism of
corticosteroids,
oral contraceptives,
anticonvulsants,
digitoxin, possibly decreasing their effects;
antidepressants potentiate adverse effects;
griseofulvin decreases absorption of mephobarbitol.
Herbal: Kava, valerian may potentiate sedation.
Pharmacokinetics
Absorption: 50% from GI tract.
Onset: 60 min.
Duration: 1012 h.
Metabolism: In liver to
phenobarbital.
Elimination: In urine. Alkalinization of urine or increase of urinary flow significantly increases the rate of
phenobarbital excretion.
Half-Life: 34 h.
Nursing Implications
Assessment & Drug Effects
- Monitor respiratory status, especially with concurrent CNS therapy with other drugs.
- Be prepared for paradoxical response to barbiturate therapy (i.e., irritability, marked excitement, aggression in children,
depression, confusion) in older adults, debilitated patients, or children.
Patient & Family Education
- Be aware that abrupt cessation after prolonged therapy may result in withdrawal symptoms (tremulousness, weakness, insomnia,
delirium, convulsions).
- Avoid driving and potentially hazardous activities until response to drug has stabilized.
- Do not take alcohol in any amount with a barbiturate.