NOLUDAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NOLUDAR (NOLUDAR).
Barbiturate that enhances GABA-A receptor activity by prolonging chloride channel opening, leading to CNS depression.
| Metabolism | Hepatic via CYP2C9 and CYP2C19; undergoes glucuronidation. |
| Excretion | Primarily renal as metabolites; <5% unchanged. Biliary/fecal elimination is negligible. |
| Half-life | 25-35 hours |
| Protein binding | 30%, primarily to albumin |
| Volume of Distribution | 1.5 L/kg, indicating extensive tissue distribution |
| Bioavailability | Oral: 90-95% |
| Onset of Action | Oral: 30-60 minutes |
| Duration of Action | 6-8 hours |
250-500 mg orally at bedtime, with a maximum dose of 1000 mg daily.
| Dosage form | ELIXIR |
| Renal impairment | Contraindicated in patients with GFR <30 mL/min. For GFR 30-50 mL/min, reduce dose by 50%. For GFR >50 mL/min, no adjustment needed. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: contraindicated. |
| Pediatric use | Not recommended in children under 12 years of age. For children 12-18 years, initial dose 250 mg orally at bedtime, adjust based on response and tolerance. |
| Geriatric use | Start at 125 mg orally at bedtime; increase cautiously due to increased risk of sedation and falls. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NOLUDAR (NOLUDAR).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Potential for infant sedation and poor feeding. Discontinue breastfeeding or avoid drug, especially in neonates or preterm infants. |
| Teratogenic Risk | First trimester: Increased risk of congenital malformations, particularly oral clefts and neural tube defects, based on animal studies and limited human data. Second/third trimesters: Risk of neonatal withdrawal syndrome, hypotonia, and respiratory depression. Avoid in pregnant women unless benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to barbiturates","Porphyria","Severe hepatic impairment","Respiratory insufficiency"]
| Precautions | ["Respiratory depression","Dependence and withdrawal risk","Paradoxical reactions (excitation/hyperactivity)","Use with caution in hepatic impairment"] |
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| Fetal Monitoring |
| Monitor maternal vital signs and sedation levels. Fetal ultrasound for structural anomalies if exposed in first trimester. Neonatal observation for withdrawal symptoms, respiratory depression, and hypotonia after delivery. |
| Fertility Effects | May impair fertility in females via disruption of menstrual cycle and ovulation. In males, possible decreased libido and erectile dysfunction. Effects are reversible upon discontinuation. |