Drug information of Secobarbital

Secobarbital

Drug group:

Mechanism of effect

Depresses CNS activity by binding to barbiturate site at GABA-receptor complex enhancing GABA activity, depressing reticular activity system; higher doses may be gabamimetic.

Pharmacokinetics

Absorption: Well absorbed (90%)

Half-life elimination: 28 hr

Duration: 3-4 hr

Vd: 1.5 L/kg

Onset: 15-30 min (hypnosis)

Excretion: Urine

Protein Bound: 45-60%

Metabolism: hepatic microsomal enzymes, glucuronidationExcretion: mostly urine as metabolites (<5% unchanged)

Enzymes induced: Primarily CYP2C9/10; CYP2C8, CYP2C9

Time to Peak: Serum concentration: Oral: Within 2 to 4 hour

Duration of Action:Hypnosis: Oral: 3 to 4 hours with 100 mg dose

Drug indications

Hypnotic

Pre-procedure Sedation

Dosage

-Hypnotic

Short-term treatment:100 mg PO qHS

Do not administer for more than 2 weeks

-Pre-procedure Sedation

200-300 mg PO 1-2 hours before surgery

Drug contraindications

-Barbiturate hypersensitivity

-Porphyria

-Liver disease

-Severe respiratory disease

-Renal impairment

-Sleep apnea

-Alcoholism

-Drug dependence

-Suicidal tendencies

Side effects

Drowsiness , Abnormality in thinking, agitation, angioedema, anxiety, apnea, ataxia, bradycardia, central nervous system depression, sleep disorder (complex sleep-related behaviors, including cooking, driving, eating, and making phone calls while sleeping), confusion, constipation, dizziness, exfoliative dermatitis, fever, hallucination, headache, hepatotoxicity, hyperexcitability, hyperkinesis, hypotension, hypoventilation, insomnia, megaloblastic anemia, nausea, nervousness, nightmares, pain at injection site, skin rash, syncope, vomiting

Alcohol ,Alizapride ,Azelastine (Nasal),
Beta-Blockers Exceptions: Atenolol; Levobunolol; Metipranolol; Nadolol.

Blonanserin ,Blood Pressure Lowering Agents,

Brexanolone,Brimonidine (Topical),

Bromopride,Bromperidol,Buprenorphine,

Calcium Channel Blockers. Exceptions: Clevidipine. Monitor therapy

Cannabidiol ,Cannabis,Chloramphenicol (Systemic),

Chlormethiazole,Chlorphenesin Carbamate,

CNS Depressants ,CycloSPORINE (Systemic),

Dimethindene (Topical),Doxycycline,Doxylamine,

Dronabinol,Droperidol ,Esketamine ,Estrogen Derivatives ,Felbamate ,Flunitrazepam,Griseofulvin

Hemin,HYDROcodone ,HydrOXYzine ,Kava Kava ,

LamoTRIgine,Lemborexant ,Lofexidine ,Magnesium Sulfate ,Methotrimeprazine,Methoxyflurane,MetyroSINE,

Mianserin,Minocycline (Systemic),Multivitamins/Minerals (with ADEK, Folate, Iron),Nabilone,Opioid Agonists

Orphenadrine,Oxomemazine,OxyCODONE

Paraldehyde,Perampanel ,Piribedil,Pramipexole,

Primidone,Progestins,Propacetamol,Pyridoxine,

Rifamycin Derivatives,ROPINIRole,Rotigotine,

Rufinamide,Selective Serotonin Reuptake Inhibitors,

Sodium Oxybate,Somatostatin acetate,Suvorexant,Tapentadol,Teniposide,

Tetrahydrocannabinol:

Tetrahydrocannabinol and Cannabidiol ,

Thalidomide ,Theophylline Derivatives: Exceptions: Dyphylline. Monitor therapy ,Tricyclic Antidepressants,Trimeprazine ,Ulipristal ,Valproate Products ,Vitamin K Antagonists (eg, warfarin),Zolpidem

Alerts

-Causes CNS depression and impairs mental and physical abilities

-Paradoxical responses: Cay cause hyperactivity and agitation

-Use with caution in patients with depression, hepatic or renal impairment, cardiovascular diseases, or respiratory diseases

-Sleep-related activities: An increased risk for hazardous sleep-related activities such as sleep-driving; cooking and eating food, and making phone calls while asleep have also been noted

- Hypersensitivity reactions

-Abrupt cessation may precipitate withdrawal, including status epilepticus in epileptic patients.

Points of recommendation

-Discontinue treatment in patients who report a sleep-driving episode

-Effects may be potentiated when used with other sedative drugs or ethanol.

-Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric and/or medical illnes

Pregnancy level

D

 

Breast feeding warning

secreted in breast milk; use with caution

Related drugs

Benzobarbital , Butabarbital

Drug forms

Seconal

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