BUTISOL SODIUM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BUTISOL SODIUM (BUTISOL SODIUM).
Enhances GABA-A receptor activity, increasing chloride ion conductance and causing central nervous system depression.
| Metabolism | Hepatic metabolism via multiple cytochrome P450 enzymes (mainly CYP2C9 and CYP3A4). |
| Excretion | Primarily hepatic metabolism (80%) with renal excretion of inactive metabolites (<30% unchanged). Less than 1% excreted in feces. |
| Half-life | Terminal elimination half-life: 40-70 hours (mean 60 h) in adults; prolonged in elderly, hepatic impairment, and neonates (up to 100 h). Clinical context: Accumulation occurs with repeated dosing. |
| Protein binding | 26% bound primarily to albumin. Low binding compared to other barbiturates. |
| Volume of Distribution | 0.8-1.0 L/kg. Indicates extensive distribution into tissues; Vd may increase in cirrhosis. |
| Bioavailability | Oral: 78-100% (mean 90%). Bioavailability after IM is complete but variable due to precipitation at injection site. |
| Onset of Action | Oral: 30-60 minutes; IM: 10-20 minutes; IV: 5-10 minutes. |
| Duration of Action | Oral: 4-6 hours with hypnotic doses; IM/IV: 3-6 hours. Duration may extend with higher doses or repeated administration due to long half-life. |
Oral: 50-100 mg 3-4 times daily; maximum 600 mg daily.
| Dosage form | ELIXIR |
| Renal impairment | GFR <10 mL/min: Administer 50% of usual dose. No adjustment for GFR >10 mL/min. |
| Liver impairment | Child-Pugh Class A: No adjustment. Class B: Reduce dose by 50%. Class C: Avoid use. |
| Pediatric use | Preoperative sedation: Oral 2-6 mg/kg 1-2 hours before procedure, maximum 100 mg. Anticonvulsant: Oral 1-3 mg/kg/dose 3-4 times daily. |
| Geriatric use | Initial dose: 25-50 mg 2-3 times daily; titrate cautiously due to increased sensitivity and risk of accumulation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BUTISOL SODIUM (BUTISOL SODIUM).
| Breastfeeding | Butisol (butabarbital) is excreted in breast milk. M/P ratio not established. Use cautiously due to potential sedation and withdrawal in infant. Consider alternative agents. |
| Teratogenic Risk | First trimester: Limited human data; animal studies show increased risk of cleft palate at high doses. Second/third trimester: Chronic use may cause neonatal withdrawal syndrome; respiratory depression if used near term. |
| Fetal Monitoring |
■ FDA Black Box Warning
BUTISOL SODIUM may be habit-forming. Prolonged use can lead to dependence. Abrupt cessation may cause withdrawal symptoms, including seizures and death. Concomitant use with alcohol or other CNS depressants may exacerbate these effects.
| Serious Effects |
Known hypersensitivity to barbiturates. Porphyria. History of addiction to sedatives. Severe respiratory insufficiency. Pregnancy (particularly third trimester).
| Precautions | Risk of dependence and withdrawal. Use with caution in patients with hepatic or renal impairment. May cause respiratory depression, especially in combination with other CNS depressants. Elderly or debilitated patients may be more sensitive. Not recommended during pregnancy, especially third trimester. |
| Food/Dietary | Avoid alcohol and grapefruit juice. Food may delay absorption but does not significantly affect overall bioavailability. CNS depression may be enhanced by large meals. |
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| Monitor for signs of fetal distress, maternal sedation, and respiratory depression. In neonate, monitor for withdrawal symptoms (irritability, tremors, feeding difficulties) and respiratory function. |
| Fertility Effects | Data limited. In animal studies, impaired fertility at high doses. In humans, possible menstrual irregularities and reduced libido; effects reversible upon discontinuation. |
| Clinical Pearls | BUTISOL SODIUM (butabarbital sodium) is a short-acting barbiturate with rapid onset (15-30 minutes) and duration of 4-6 hours. It is primarily used for preoperative sedation and short-term treatment of insomnia. Avoid in patients with porphyria, severe hepatic impairment, or respiratory insufficiency. Tolerance and dependence develop rapidly; limit use to 2 weeks or less. Abrupt discontinuation after prolonged use may precipitate withdrawal seizures. CYP450 enzyme induction reduces efficacy of oral contraceptives, warfarin, and corticosteroids. Monitor for paradoxical excitation in elderly or pediatric patients. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency. · May cause drowsiness or dizziness; avoid driving or operating machinery. · Do not consume alcohol or other CNS depressants. · Do not stop suddenly after long-term use; withdrawal seizures may occur. · Inform your doctor if you have liver disease, breathing problems, or a history of drug abuse. · This medication may reduce the effectiveness of birth control pills; use additional contraception. · Store in a cool, dry place away from light. · Keep out of reach of children. |