PAXIPAM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PAXIPAM (PAXIPAM).
PAXIPAM (flurazepam) is a benzodiazepine that enhances GABA-A receptor activity by binding to the benzodiazepine site, increasing chloride ion conductance and producing CNS depression.
| Metabolism | Hepatic via CYP450 (primarily CYP2C19 and CYP3A4) to active metabolites (N-desalkylflurazepam). |
| Excretion | Renal excretion of unchanged drug and glucuronide metabolites accounts for 60-70%; fecal excretion accounts for 20-30%. |
| Half-life | Terminal elimination half-life is 30-40 hours in healthy adults; prolonged in elderly and hepatic impairment. |
| Protein binding | 92-98% bound to albumin. |
| Volume of Distribution | 0.5-1.0 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 80-100%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: 1-5 minutes. |
| Duration of Action | Oral: 6-8 hours; intravenous: 2-4 hours; clinical notes: Duration may be extended with repeated dosing due to accumulation. |
5-10 mg orally every 8-12 hours as needed; maximum 40 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-89 mL/min: no adjustment; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: contraindicated. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: contraindicated. |
| Pediatric use | Children 6-12 years: 0.5-1 mg/kg/day divided every 6-8 hours, not to exceed 20 mg/day; Children <6 years: not recommended. |
| Geriatric use | Initiate at 2.5 mg every 12 hours; titrate cautiously due to increased sensitivity and risk of falls. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PAXIPAM (PAXIPAM).
| Breastfeeding | Halazepam is excreted into breast milk; M/P ratio not established. Potential for infant sedation and withdrawal; avoid breastfeeding or monitor infant for drowsiness and feeding difficulties. |
| Teratogenic Risk | Paxipam (halazepam) is a benzodiazepine. First trimester: Increased risk of congenital malformations including oral cleft. Second trimester: Risk persists but lower; possible adverse neurodevelopmental effects. Third trimester: Risk of neonatal withdrawal, floppy infant syndrome, and respiratory depression. |
■ FDA Black Box Warning
Concomitant use with opioids may result in profound sedation, respiratory depression, coma, and death. Reserve for patients without adequate alternative treatment options.
| Serious Effects |
Hypersensitivity to benzodiazepines; severe respiratory insufficiency; sleep apnea; severe hepatic impairment; narrow-angle glaucoma; pregnancy (avoid due to teratogenicity); lactation.
| Precautions | Risk of dependence and withdrawal; CNS depressant effects; impaired psychomotor function; anterograde amnesia; worsening of depression; respiratory depression in COPD/sleep apnea; elderly fall risk. |
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| Fetal Monitoring |
| Monitor maternal vital signs and sedation level. Fetal monitoring: ultrasound for congenital anomalies if exposed in first trimester; neonatal monitoring for respiratory depression, hypotonia, and withdrawal symptoms after delivery. |
| Fertility Effects | No specific data on halazepam; benzodiazepines may cause menstrual irregularities and reduced libido; impact on fertility not established. |