Butobarbital

Oral
Severe intractable insomnia

Children, young adults, elderly and debilitated patients. Patients with depression or with a history of drug or alcohol abuse or addiction. Insomnia caused by pain. Acute porphyria. Severe hepatic impairment. History of CNS depression or coma, pulmonary insufficiency and sleep apnoea. Pregnancy & lactation.

Renal impairment. Drowsiness may persist till the next day. Tolerance and dependence likely. Must not be withdrawn abruptly as withdrawal syndrome (including mortality) may occur.

Drowsiness, ataxia, paradoxical excitement, confusion, headache and CNS depression; respiratory depression; GI disorders; hepatitis: fever; megaloblastic anaemia.
Potentially Fatal: Erythema multiforme; exfoliative dermatitis.

Uncoordinated movement, dysarthria, hyporeflexia, areflexia, nystagmus or miosis may occur due to CNS and cardiovascular depression. These can lead to hypotension and shock resulting in renal failure and death. The patient may need to be intubated if he is unconscious. If >10 mg/kg has been ingested and the patient is presented within 1 hr of ingestion, administer activated charcoal orally or via nasogastric tube. Repeat doses of charcoal if needed. Charcoal perfusion may be necessary in cases of prolonged coma associated with irregular or absent bowel sounds.

Butobarbital is a potent liver enzyme inducer and may reduce the effect of coumarin for up to 6 wk. Additive CNS depression with alcohol. Reduced effect of tricyclic antidepressants (such as amitriptyline, clomipramine, desipramine, dosulepin, imipramine, melitracen etc), corticosteriods (such as hydrocortisone, dexamethasone etc), coumarins, darifenacin, disopyramide, doxorubicin, metronidazole, theophylline and tolvaptan. It is also likely that the drug level of lidocaine is reduced due to the increased liver enzyme activity. May reduce drug level of memantine. Increased sedation with thalidomide.
Potentially Fatal: Concurrent long-term use with phenmetrazine may result in psychosis. Concurrent use with sodium oxybate is contraindicated due to the additive CNS depressant effect. Butobarbital is a potent inducer of CYP3A4 and is expected to reduce the AUC of gefitinib significantly.

Avoid alcohol.

Description:
Mechanism of Action: Butobarital is a barbiturate and is used as a hypnotic. Although it is no longer recommended due to the risk of dependence, tolerance and adverse effects, its continued use may be necessary in severe intractable insomnia in patients already on it.
Pharmacokinetics:
Distribution: About 26% bound to plasma proteins.
Metabolism: Hepatically mainly via hydroxylation.
Excretion: Small amount excreted unchanged in urine. Half-life: about 40 hr.

Hypnotics & Sedatives