indication

For the Short-term treatment of intractable insomnia for patients habituated to barbiturates

pharmacology

Secobarbital, a barbiturate, is used for the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.

mechanism of action

Secobarbital 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.

toxicity

Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.

route of elimination

Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine and, less commonly, in the feces.

drug interactions

Aminophylline: The barbiturate, secobarbital, decreases the effect of aminophylline.

Betamethasone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, betamethasone.

Clomifene: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, clomifene.

Conjugated Estrogens: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, conjugated estrogens.

Cyclosporine: The barbiturate, secobarbital, increases the effect of cyclosporine.

Dexamethasone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, dexamethasone.

Diethylstilbestrol: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, diethylstilbestrol.

Doxycycline: The anticonvulsant , secobarbital, decreases the effect of doxycycline.

Estradiol: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, estradiol.

Ethinyl Estradiol: This product may cause a slight decrease of contraceptive effect

Felodipine: The barbiturate, secobarbital, decreases the effect of felodipine.

Fludrocortisone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, fludrocortisone.

Folic Acid: Folic acid decreases the effect of anticonvulsant, secobarbital.

Gefitinib: The CYP3A4 inducer, secobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.

Griseofulvin: The barbiturate, secobarbital, decreases the effect of griseofulvin.

Hydrocortisone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, hydrocortisone.

Levonorgestrel: Phenobarbital decreases the effect of levonorgestrel

Medroxyprogesterone: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, medroxyprogesterone.

Megestrol: The enzyme inducer, secobarbital, decreases the effect of the hormone agent, megestrol.

Methadone: The barbiturate, secobarbital, decreases the effect of methadone.

Metronidazole: The barbiturate, secobarbital, decreases the effect of metronidazole.

Nifedipine: The barbiturate, secobarbital, decreases the effect of the calcium channel blocker, nifedipine.

Norethindrone: This product may cause a slight decrease of contraceptive effect

Oxtriphylline: The barbiturate, secobarbital, decreases the effect of oxtriphylline.

Prednisolone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, prednisolone.

Prednisone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, prednisone.

Quinidine: The anticonvulsant, secobarbital, decreases the effect of quinidine.

Theophylline: The barbiturate, secobarbital, decreases the effect of theophylline.

Tretinoin: The strong CYP2C8 inducer, Secobarbital, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Secobarbital is initiated, discontinued or dose changed.

Triamcinolone: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, triamcinolone.

Trimipramine: The barbiturate, Secobarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Secobarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.

Triprolidine: The CNS depressants, Triprolidine and Secobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

Verapamil: Secobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Secobarbital is initiated, discontinued or dose changed.

Warfarin: Secobarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if secobarbital is initiated, discontinued or dose changed.