QuickView for Butabarbital (compound)

Summary
General Info

PubChem Substance

Name:	secbutabarbital
PubChem Substance ID:	10029
Synonyms:	Nilox; Butatab; Buticaps; Butisol Sodium; Sarisol; Butalan; Secbutabarbital; Butatal; Butabarb; Butabarbital. show more » Nilox; Butatab; Buticaps; Butisol Sodium; Sarisol; Butalan; Secbutabarbital; Butatal; Butabarb; Butabarbital; Medarsed; Sarisol No. 1; Sodium Butabarbital; Unicelles; Butabarbital Sodium; Secbutobarbitone; Butrate; Butabarbitone; Secbubarbital; Secbutobarbital; Butisol show less «

DrugBank

Identification

Name:	secbutabarbital
Name (isomeric):	DB00237
Drug Type:	small molecule
Synonyms:	Sodium Butabarbital; Butabarbital Sodium; Butrate; Secbutobarbitone; Secbubarbital; Secbutabarbital; Butabarbitone; Secbutobarbital
Brand:	Unicelles, Sarisol No. 1, Butatab, Nilox, Butisol, Medarsed, Butatal, Butabarb, Butisol Sodium, Butalan, Sarisol, Buticaps
Category:	Anti-anxiety Agents, Hypnotics and Sedatives, Barbiturates
CAS number:	125-40-6

Pharmacology

Indication:	For short-term treatment of insomnia and anxiety disorders
Pharmacology:	Butabarbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Mechanism of Action:	Butabarbital binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GA... show more » Butabarbital binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission. show less «
Route of elimination:	Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and most metabolic products are excreted in the urine.
Toxicity:	Signs of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Ethinyl Estradiol	This product may cause a slight decrease of contraceptive effect
Nortriptyline	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like nortriptyline. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Gefitinib	The CYP3A4 inducer, butabarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
Triamcinolone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, triamcinolone.
Acenocoumarol	Barbiturates like butabarbital may increase the metabolism of Vitamin K Antagonists like acenocoumarol. onitor for decreased therapeutic effects of oral anticoagulants if a barbiturate is initiated/dose increased (anticoagulant dosage increases of 30% to 60% may be needed based on monitored PT), or increased effects if a barbiturate is discontinued/dose decreased. An increased frequency of PT monitoring should be considered for the period immediately following barbiturate initiation/dosage changes.

Ethinyl Estradiol	This product may cause a slight decrease of contraceptive effect
Nortriptyline	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like nortriptyline. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Gefitinib	The CYP3A4 inducer, butabarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
Triamcinolone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, triamcinolone.
Acenocoumarol	Barbiturates like butabarbital may increase the metabolism of Vitamin K Antagonists like acenocoumarol. onitor for decreased therapeutic effects of oral anticoagulants if a barbiturate is initiated/dose increased (anticoagulant dosage increases of 30% to 60% may be needed based on monitored PT), or increased effects if a barbiturate is discontinued/dose decreased. An increased frequency of PT monitoring should be considered for the period immediately following barbiturate initiation/dosage changes.
Warfarin	Butabarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if butabarbital is initiated, discontinued or dose changed.
Medroxyprogesterone	The enzyme inducer, butabarbital, decreases the effect of the hormone agent, medroxyprogesterone.
Clomifene	The enzyme inducer, butabarbital, decreases the effect of the hormone agent, clomifene.
Lamotrigine	Barbiturates like butabarbital may decrease the serum concentration of lamotrigine. There are separate patient management guidelines for patients age 12 and under and for patients older than 12 years of age. Monitor for decreased serum concentrations/therapeutic effects of lamotrigine if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased.
Aminophylline	The barbiturate, butabarbital, decreases the effect of aminophylline.
Disopyramide	arbiturates may increase the metabolism of Disopyramide. Monitor for decreased therapeutic effects of disopyramide if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased.
Felodipine	The barbiturate, butabarbital, decreases the effect of felodipine.
Griseofulvin	The barbiturate, butabarbital, decreases the effect of griseofulvin.
Protriptyline	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like protriptyline. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Amitriptyline	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like amitriptyline. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Oxtriphylline	The barbiturate, butabarbital, decreases the effect of oxtriphylline.
Prednisone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, prednisone.
Metronidazole	The barbiturate, butabarbital, decreases the effect of metronidazole.
Doxepin	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like doxepin. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Conjugated Estrogens	The enzyme inducer, butabarbital, decreases the effect of the hormone agent, conjugated estrogens.
Quinidine	The anticonvulsant, butabarbital, decreases the effect of quinidine.
Imipramine	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like imipramine. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Prednisolone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, prednisolone.
Amoxapine	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like amoxipine. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Folic Acid	Folic acid decreases the effect of anticonvulsant, butabarbital.
Hydroxyzine	Hydroxyzine may enhance the CNS depressant effect of barbiturates like butabarbital. Consider a decrease in the barbiturate dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination.
Dexamethasone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, dexamethasone.
Droperidol	Droperidol may enhance the CNS depressant effect of CNS Depressants like butabarbital. Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use.
Theophylline	The barbiturate, butabarbital, decreases the effect of theophylline.
Estradiol	The enzyme inducer, butabarbital, decreases the effect of the hormone agent, estradiol.
Cyclosporine	The barbiturate, butabarbital, increases the effect of cyclosporine.
Nifedipine	The barbiturate, butabarbital, decreases the effect of the calcium channel blocker, nifedipine.
Teniposide	Barbiturates like butabarbital may decrease the serum concentration of Teniposide. arbiturates may decrease the serum concentration of Teniposide.
Voriconazole	Butabarbital may reduce serum concentrations and efficacy of voriconazole. Concomitant voriconazole and long-acting barbiturates therapy is contraindicated.
Levonorgestrel	Phenobarbital decreases the effect of levonorgestrel
Verapamil	Butabarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Butabarbital is initiated, discontinued or dose changed.
Hydrocortisone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, hydrocortisone.
Megestrol	The enzyme inducer, butabarbital, decreases the effect of the hormone agent, megestrol.
Doxycycline	The anticonvulsant, butabarbital, decreases the effect of doxycycline.
Clomipramine	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like clomipramine. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Norethindrone	This product may cause a slight decrease of contraceptive effect
Methadone	The barbiturate, butabarbital, decreases the effect of methadone.
Diethylstilbestrol	The enzyme inducer, butabarbital, decreases the effect of the hormone agent, diethylstilbestrol.
Triprolidine	The CNS depressants, Triprolidine and Butabarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Divalproex sodium	Divalproex sodium increases the effect of the barbiturate, butabarbital.
Betamethasone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, betamethasone.
Desipramine	Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like desipramine. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Trimipramine	The barbiturate, Butabarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Butabarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
Fludrocortisone	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, fludrocortisone.

show less «

Targets

Gamma-aminobutyric-acid receptor subunit alpha-1

Gamma-aminobutyric-acid receptor subunit alpha-2

Gamma-aminobutyric-acid receptor subunit alpha-3

Gamma-aminobutyric-acid receptor subunit alpha-4

Gamma-aminobutyric-acid receptor subunit alpha-5

Gamma-aminobutyric-acid receptor subunit alpha-6

Neuronal acetylcholine receptor subunit alpha-4

Neuronal acetylcholine receptor subunit alpha-7

Glutamate receptor 2

Glutamate receptor, ionotropic kainate 2