Phenobarbital
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Category：Chemical Additives Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
Phenobarbital is a kind of long-acting barbital drugs, in which the pivot inhibition effect varies with the dose. It has sedative, hypnotic and anticonvulsant effects. It can also resist epilepsy, and has good effects on large and limited seizures and status epilepticus; The curative effect on small seizures is poor。
However, it is often ineffective for psychomotor attacks, and may aggravate the attacks when treated with this medicine alone. This product also has the effect of enhancing antipyretic and analgesic drugs, and can induce the activity of hepatic microsomal glucuronic acid transferase, promote the combination of bilirubin and glucuronic acid, reduce the concentration of plasma bilirubin, and treat neonatal hyperbilirubinemia (cerebral nuclear jaundice).
| Category | Details |
|---|---|
| Chemical Formula | C₁₂H₁₈N₂O₃ (Barbiturate derivative) |
| Therapeutic Class | Anticonvulsant – Voltage-gated sodium channel blocker |
| Primary Indications | – Partial seizures: Adjunctive therapy – Generalized tonic-clonic seizures: Secondary prevention – Essential tremor: First-line treatment – Myoclonus: Symptomatic control |
| Pharmacodynamics | – Metabolites: Active phenobarbital (80% conversion) – Mechanism: Enhances GABA-ergic inhibition – Onset: 1-2 weeks (therapeutic effect) |
| Pharmacokinetics | – Bioavailability: ~100% (oral) – Half-life: 12-16 hours – Protein binding: 20-30% – Excretion: Renal (metabolites) |
| Dosage Forms | – Tablets: 50mg, 250mg – Capsules: 250mg – Oral suspension: 250mg/5mL |
| Standard Regimen | – Adults: 125-250mg BID (max 2.5g/day) – Elderly: Reduce by 50% – Pediatrics: 25mg/kg/day divided TID |
| Adverse Effects | – Common: Sedation, ataxia, nystagmus – Severe: Stevens-Johnson syndrome (rare) – Chronic: Osteomalacia (long-term use) |
| Drug Interactions | – Enhanced effects: Alcohol, CNS depressants – Reduced efficacy: Carbamazepine, phenytoin (enzyme induction) – Monitoring required: Warfarin, oral contraceptives |
| Regulatory Status | – FDA: Pregnancy Category D – EMA: Requires risk-benefit assessment – Generic availability: Multiple manufacturers (low-cost options) |
| Market Position | – Declining use: Replaced by newer AEDs – Niche applications: Essential tremor, refractory epilepsy – Cost advantage: Affordable in resource-limited settings |
Note: Requires therapeutic drug monitoring due to variable metabolism. Contraindicated in porphyria and severe hepatic impairment.
,Disclaimer: The above content is for reference and communication only among industry insiders, and does not guarantee its accuracy or completeness. According to relevant laws and regulations and the regulations of this website, units or individuals who purchase related items should obtain valid qualifications and qualification conditions.
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