QuickView for Amobarbital (compound)

Summary
General Info

PubChem

PubChem Compound 2163

Name:	Amobarbital
PubChem Compound ID:	2163
Description:	A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565)
Molecular formula:	C₁₁H₁₇N₂O₃^-
Molecular weight:	225.264 g/mol

DrugBank

Identification

Name:	Amobarbital
Name (isomeric):	DB01351
Drug Type:	small molecule
Description:	A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565)
Brand:	Isomytal
Category:	GABA Modulators, Hypnotics and Sedatives
CAS number:	57-43-2

Pharmacology

Mechanism of Action:	Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decre... show more » Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Amobarbital also appears to bind neuronal nicotinic acetylcholine receptors. show less «

Mechanism of Action:

Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decre...
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Interactions

Drug interaction:

Clomifene	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, clomifene.
Estradiol	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, estradiol.
Doxycycline	The anticonvulsant, amobarbital, decreases the effect of doxycycline.
Ethinyl Estradiol	This product may cause a slight decrease of contraceptive effect
Aminophylline	The barbiturate, amobarbital, decreases the effect of aminophylline.

Clomifene	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, clomifene.
Estradiol	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, estradiol.
Doxycycline	The anticonvulsant, amobarbital, decreases the effect of doxycycline.
Ethinyl Estradiol	This product may cause a slight decrease of contraceptive effect
Aminophylline	The barbiturate, amobarbital, decreases the effect of aminophylline.
Medroxyprogesterone	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
Prednisolone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisolone.
Methadone	The barbiturate, amobarbital, decreases the effect of methadone.
Quinidine	The anticonvulsant, amobarbital, decreases the effect of quinidine.
Gefitinib	The CYP3A4 inducer, amobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
Prednisone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisone.
Verapamil	Amobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Amobarbital is initiated, discontinued or dose changed.
Folic Acid	Folic acid decreases the effect of anticonvulsant, amobarbital.
Levonorgestrel	Phenobarbital decreases the effect of levonorgestrel
Warfarin	Amobarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if amobarbital is initiated, discontinued or dose changed.
Triamcinolone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Voriconazole	Amobarbital may reduce serum concentrations and efficacy of voriconazole. Concomitant voriconazole and long-acting barbiturates therapy is contraindicated.
Betamethasone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, betamethasone.
Diethylstilbestrol	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
Trimipramine	The barbiturate, Amobarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Amobarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
Oxtriphylline	The barbiturate, amobarbital, decreases the effect of oxtriphylline.
Cyclosporine	The barbiturate, amobarbital, increases the effect of cyclosporine.
Megestrol	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, megestrol.
Griseofulvin	The barbiturate, amobarbital, decreases the effect of griseofulvin.
Metronidazole	The barbiturate, amobarbital, decreases the effect of metronidazole.
Conjugated Estrogens	The enzyme inducer, amobarbital, decreases the effect of the hormone agent, conjugated estrogens.
Felodipine	The barbiturate, amobarbital, decreases the effect of felodipine.
Theophylline	The barbiturate, amobarbital, decreases the effect of theophylline.
Norethindrone	This product may cause a slight decrease of contraceptive effect
Nifedipine	The barbiturate, amobarbital, decreases the effect of the calcium channel blocker, nifedipine.
Triprolidine	The CNS depressants, Triprolidine and Amobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Dexamethasone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Divalproex sodium	Divalproex sodium increases the effect of the barbiturate, amobarbital.
Fludrocortisone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
Hydrocortisone	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, hydrocortisone.

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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

Enzymes

Cytochrome P450 2A6