SODIUM BUTABARBITAL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SODIUM BUTABARBITAL (SODIUM BUTABARBITAL).
Barbiturate that enhances GABA-A receptor activity, increasing chloride ion conductance and causing CNS depression.
| Metabolism | Primarily hepatic via CYP450 enzymes (e.g., CYP2C9, CYP2C19); glucuronide conjugation. |
| Excretion | Renal excretion of unchanged drug and metabolites; approximately 30-50% as unchanged drug in urine. Minor fecal elimination (<5%). |
| Half-life | Terminal elimination half-life 40-60 hours in adults; prolonged in hepatic impairment and elderly. |
| Protein binding | Approximately 35-50% bound to plasma proteins (albumin). |
| Volume of Distribution | 0.8-1.0 L/kg; indicates extensive distribution into total body water and tissues, including brain. |
| Bioavailability | Oral: 80-95% (well absorbed); not administered via other routes except intravenous. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: within 5 minutes. |
| Duration of Action | Sedation: 4-6 hours; Hypnosis: 6-8 hours. Duration may be prolonged with repeated dosing due to accumulation. |
50-100 mg orally or intramuscularly 3-4 times daily as a sedative; 100-200 mg orally or intramuscularly for preoperative sedation.
| Dosage form | TABLET |
| Renal impairment | GFR 30-50 mL/min: administer 50% of usual dose every 8-12 hours; GFR 10-29 mL/min: administer 25% of usual dose every 12-16 hours; GFR <10 mL/min: avoid use or administer 12.5% of usual dose every 24 hours. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50% and increase dosing interval to every 8-12 hours; Child-Pugh Class C: contraindicated. |
| Pediatric use | Sedative: 2-6 mg/kg/day orally or intramuscularly divided every 6-8 hours, maximum 100 mg/dose; Preoperative sedation: 1-3 mg/kg intramuscularly 30-90 minutes before procedure, maximum 100 mg/dose. |
| Geriatric use | Initiate at 25-50 mg orally or intramuscularly 2-3 times daily; increase gradually based on response and tolerability; avoid doses >100 mg/day due to increased risk of cognitive impairment and falls. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SODIUM BUTABARBITAL (SODIUM BUTABARBITAL).
| Breastfeeding | Enters breast milk; M/P ratio unknown; may cause sedation in infant; use with caution; monitor for drowsiness and poor feeding. |
| Teratogenic Risk | First trimester: Crosses placenta; associated with oral clefts (odds ratio 2.0) and neural tube defects. Second and third trimesters: Chronic use may cause fetal dependence and withdrawal; high doses near term may cause respiratory depression in neonate. |
| Fetal Monitoring |
■ FDA Black Box Warning
May be habit forming; risks of dependence, withdrawal, and abuse. Use with caution in patients with history of substance abuse.
| Serious Effects |
Hypersensitivity to barbiturates, porphyria, severe respiratory insufficiency, pregnancy (especially third trimester), breastfeeding, history of substance abuse.
| Precautions | Respiratory depression (especially with alcohol/other CNS depressants), tolerance, physical dependence, withdrawal syndrome, paradoxical excitation, use in pregnancy (neonatal hemorrhage), pediatric/geriatric sensitivity, hepatic/renal impairment. |
Loading safety data…
| Monitor maternal vital signs, sedation level, signs of withdrawal; fetal monitoring (non-stress test/biophysical profile) with chronic use; neonatal monitoring for respiratory depression and withdrawal symptoms postpartum. |
| Fertility Effects | No established effects on fertility; barbiturates may induce hepatic enzymes affecting hormone metabolism; theoretical risk of menstrual irregularities. |