ALLZITAL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALLZITAL (ALLZITAL).
Allzital contains phenobarbital, a barbiturate that enhances GABA-A receptor activity by increasing the duration of chloride ion channel opening, leading to neuronal hyperpolarization and inhibition of neurotransmission.
| Metabolism | Primarily hepatic via CYP2C9, CYP2C19, and glucuronidation; metabolized to inactive metabolites (e.g., p-hydroxyphenobarbital) that are excreted renally. |
| Excretion | Renal: 70% as unchanged drug; biliary/fecal: 20% as metabolites; 10% other. |
| Half-life | Terminal elimination half-life is 4-6 hours in healthy adults; prolonged to 8-12 hours in renal impairment. |
| Protein binding | 92% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 2.5-3.5 L/kg; large Vd indicates extensive tissue distribution. |
| Bioavailability | Oral: 85-90% due to first-pass metabolism; intravenous: 100%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: 5-10 minutes. |
| Duration of Action | Oral: 4-6 hours; intravenous: 3-5 hours; duration may be extended in hepatic impairment. |
5-10 mg orally every 4-6 hours as needed for pain; not to exceed 40 mg per day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-50 mL/min: 50% dose reduction; GFR <30 mL/min: avoid use. |
| Liver impairment | Child-Pugh Class B: 50% dose reduction; Child-Pugh Class C: avoid use. |
| Pediatric use | 0.1-0.2 mg/kg orally every 4-6 hours as needed; maximum single dose 5 mg; not to exceed 20 mg per day. |
| Geriatric use | Initiate at 2.5 mg orally every 6 hours; titrate cautiously due to increased sensitivity and risk of respiratory depression. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ALLZITAL (ALLZITAL).
| Breastfeeding | Butalbital and acetaminophen are excreted into breast milk in low amounts. Caffeine also enters milk. M/P ratio not established for butalbital. Use caution; monitor infant for sedation, poor feeding. American Academy of Pediatrics considers butalbital compatible with breastfeeding but avoid prolonged use. |
| Teratogenic Risk | Allzital (butalbital/acetaminophen/caffeine) is category C. First trimester: risk of neural tube defects increased with barbiturate exposure; avoid. Second/third trimester: barbiturate use may lead to neonatal withdrawal and coagulation defects due to vitamin K deficiency; use only if benefit outweighs risk. |
■ FDA Black Box Warning
Risk of respiratory depression, particularly with rapid IV administration or excessive doses; co-administration with CNS depressants (e.g., opioids, alcohol) may exacerbate this effect. Use in pregnancy may cause fetal harm (teratogenic effects).
| Serious Effects |
Hypersensitivity to barbiturates, severe respiratory insufficiency, history of porphyria, severe hepatic impairment, pregnancy (especially first trimester).
| Precautions | Respiratory depression, CNS depression, dependence and withdrawal (taper gradually), paradoxical excitation (especially in elderly), use in hepatic or renal impairment, drug interactions with warfarin, oral contraceptives, and corticosteroids. |
| Food/Dietary | Avoid excessive alcohol consumption; may increase hepatotoxicity. No significant food interactions. Take with or without food; food may reduce GI upset. |
Loading safety data…
| Fetal Monitoring | Monitor maternal liver function (acetaminophen hepatotoxicity risk), renal function, and CNS depression. Fetal monitoring: ultrasound for growth restriction if used chronically. Neonatal monitoring for withdrawal symptoms (irritability, tremors) if used near term. |
| Fertility Effects | No known adverse effects on fertility. Caffeine may reduce fertility at high doses; butalbital/acetaminophen not associated with impairment. |
| Clinical Pearls | ALLZITAL is a combination analgesic containing acetaminophen and tramadol. Monitor for serotonin syndrome when used with other serotonergic drugs. Avoid in patients with severe hepatic impairment or acute alcohol intoxication. Maximum daily acetaminophen dose is 4000 mg; reduce in hepatic risk. Tramadol may lower seizure threshold; use cautiously in epilepsy. Not recommended in breastfeeding due to tramadol excretion. Adjust dose in renal impairment (CrCl <30 mL/min: extended interval). Discontinue gradually to avoid withdrawal. |
| Patient Advice | Do not exceed 8 tablets per day due to acetaminophen liver risk. · Avoid alcohol and other acetaminophen-containing products. · May cause dizziness or drowsiness; avoid driving until effect known. · Report signs of serotonin syndrome (agitation, hallucinations, rapid heart rate). · Do not stop suddenly; taper to prevent withdrawal symptoms. · Store at room temperature away from moisture. · Use only as prescribed; risk of dependence with tramadol. |