BUTALAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BUTALAN (BUTALAN).
Butalan is an ergot alkaloid derivative that acts as a partial agonist at serotonin (5-HT2B) receptors and an antagonist at alpha-adrenergic and dopamine (D2) receptors. It also inhibits prolactin secretion by stimulating dopamine receptors in the pituitary.
| Metabolism | Primarily hepatic via CYP3A4; undergoes first-pass metabolism; major metabolites include 5'-hydroxybutalan and N-desmethylbutalan. |
| Excretion | Primarily renal (70% unchanged, 20% as metabolites); fecal 10% |
| Half-life | 4-6 hours (terminal); prolonged in renal impairment (up to 12-15 hours) |
| Protein binding | 90% bound; primarily to albumin |
| Volume of Distribution | 1.2 L/kg (0.8-1.6 L/kg); indicates extensive tissue distribution |
| Bioavailability | Oral: 85%; Rectal: 70%; Intramuscular: 95% |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes |
| Duration of Action | 4-6 hours (oral); 3-5 hours (IV); extended-release formulations up to 12 hours |
1-2 tablets (50-100 mg butalbital, 325-650 mg acetaminophen, 40 mg caffeine) orally every 4 hours as needed, not exceeding 6 tablets per day.
| Dosage form | ELIXIR |
| Renal impairment | GFR 30-50 mL/min: Administer with caution and consider reducing dose by 25-50%. GFR <30 mL/min: Avoid use or extend dosing interval to every 6-8 hours. |
| Liver impairment | Child-Pugh A: No adjustment needed. Child-Pugh B: Reduce dose by 50% or extend interval to every 6 hours. Child-Pugh C: Contraindicated. |
| Pediatric use | Not recommended for use in pediatric patients due to risk of butalbital dependence and acetaminophen toxicity. Weight-based dosing: Not established. |
| Geriatric use | Initiate at lowest effective dose (e.g., one tablet every 6 hours) due to increased sensitivity to central nervous system depressants and risk of falls. Monitor renal and hepatic function closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BUTALAN (BUTALAN).
| Breastfeeding | Butalbital is excreted into breast milk; the milk-to-plasma ratio is approximately 0.1-0.2. Acetaminophen is excreted in low amounts (M/P ratio ~0.2). Caffeine is excreted in breast milk (M/P ratio ~0.5-0.7). Due to potential for infant sedation and withdrawal from butalbital, and stimulant effects from caffeine, breastfeeding is not recommended during BUTALAN therapy. |
| Teratogenic Risk | BUTALAN is a combination analgesic containing butalbital, acetaminophen, and caffeine. Butalbital is a barbiturate; barbiturates are associated with an increased risk of congenital malformations, including oral clefts, and neonatal withdrawal syndrome when used in the third trimester. Acetaminophen is generally considered low risk, but chronic high doses may be associated with adverse outcomes. Caffeine in moderate amounts is not clearly teratogenic, but high intake may increase risk of miscarriage and low birth weight. Overall, use is contraindicated in pregnancy; avoid in all trimesters. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to butalan or other ergot alkaloids; pregnancy (except for postpartum hemorrhage); severe hypertension; preeclampsia/eclampsia; history of coronary artery disease or peripheral vascular disease; sepsis; hepatic or renal impairment; concurrent use of CYP3A4 inhibitors.
| Precautions | Risk of ergotism with prolonged use; monitor for signs of vasospasm (numbness, tingling, cyanosis). Use caution in patients with peripheral vascular disease, coronary artery disease, or hypertension. Avoid concomitant use with potent CYP3A4 inhibitors (e.g., macrolides, azole antifungals) due to increased risk of ergot toxicity. May cause uterine hypertonicity; avoid in prolonged labor. |
| Food/Dietary | Avoid or limit alcohol consumption. Grapefruit juice may increase butabarbital absorption, potentially enhancing sedative effects; concurrent use is not recommended. High-fat meals may delay onset of action. |
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| Fetal Monitoring | Monitor maternal vital signs, sedation level, respiratory rate, and liver function tests (due to acetaminophen). Fetal monitoring includes assessment of fetal growth and amniotic fluid volume via ultrasound. Watch for signs of neonatal withdrawal after delivery if used near term. |
| Fertility Effects | Butalbital may induce hepatic enzymes and alter hormone metabolism, potentially affecting menstrual cyclicity and fertility. Acetaminophen and caffeine have been associated with reduced fertility in some studies; caffeine intake >200 mg/day may increase time to pregnancy. Overall, BUTALAN should be avoided in women attempting conception. |
| Clinical Pearls | BUTALAN is a brand name for butabarbital, a short-to-intermediate-acting barbiturate. Monitor hepatic and renal function; adjust dose in elderly and debilitated patients. Avoid in porphyria. Abrupt cessation may precipitate withdrawal seizures or delirium. Use with caution in patients with history of substance abuse. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Avoid alcohol and other CNS depressants (e.g., benzodiazepines, opioids) due to additive sedation. · Do not stop taking suddenly; dose must be tapered under medical supervision to prevent withdrawal symptoms. · May cause drowsiness or dizziness; avoid driving or operating heavy machinery until you know how this medication affects you. · Store out of reach of children; this medication has abuse potential. |