LORAZ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LORAZ (LORAZ).
Binds to gamma-aminobutyric acid (GABA) type A receptors at the benzodiazepine binding site, potentiating the effect of GABA, leading to increased chloride ion influx, neuronal hyperpolarization, and inhibition of neurotransmission.
| Metabolism | Primarily hepatic via glucuronidation (UGT2B7, UGT2B15, and UGT1A4); minor oxidation by CYP3A4. |
| Excretion | Renal: ~85% as glucuronide conjugates and ~10% as unchanged drug. Biliary/fecal: ~5%. |
| Half-life | Terminal elimination half-life: 12–15 hours in healthy adults. Extended in elderly (15–20 hours), hepatic impairment (up to 50 hours), and obesity. |
| Protein binding | 85–90% bound to albumin. |
| Volume of Distribution | 0.7–1.2 L/kg; larger Vd in obesity due to lipophilicity. |
| Bioavailability | Oral: 90–95%; Intramuscular: 82–88%; Intravenous: 100%. |
| Onset of Action | Oral: 1–2 hours; Intramuscular: 15–30 minutes; Intravenous: 5–15 minutes. |
| Duration of Action | Oral: 6–8 hours; Intramuscular/Intravenous: 6–8 hours. Prolonged in elderly or hepatic impairment due to reduced clearance. |
| Action Class | Benzodiazepines |
| Brand Substitutes | Zepnap 2mg Tablet, Lorel 2mg Tablet, Texina 2mg Tablet, Larpose 2mg Tablet, Zelor 2mg Tablet, Lzepam 1mg Tablet, Lopam 1mg Tablet, Zepnap 1mg Tablet, Lorel 1mg Tablet, Larpose 1mg Tablet, Calmese 2mg Injection, Zeepam 2mg Injection, Lorawel Injection, Axitan 2mg Injection, Lorazen Injection |
2-6 mg orally or intravenously daily in divided doses; usual range 2-10 mg/day
| Dosage form | TABLET |
| Renal impairment | No specific adjustment required; use caution in severe impairment (CrCl <10 mL/min) due to accumulation of metabolites |
| Liver impairment | Child-Pugh Class A: caution with increased sedation; Child-Pugh B or C: reduce dose by 50% or avoid use |
| Pediatric use | 0.05-0.1 mg/kg/dose orally or intravenously per dose; maximum 2 mg/dose; frequency based on indication |
| Geriatric use | Start with 1-2 mg/day orally in divided doses; titrate slowly; reduce total daily dose by 50% compared to younger adults |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LORAZ (LORAZ).
| Breastfeeding | Lorazepam is excreted into breast milk in low concentrations (M/P ratio ~0.2-0.5). Manufacturer recommends discontinuing breast-feeding or drug due to potential infant sedation and feeding difficulties. Use with caution and monitor infant for drowsiness and weight gain. |
| Teratogenic Risk | FDA Pregnancy Category D. First trimester: Increased risk of oral clefts (odds ratio 2.5). Second/third trimester: Risk of floppy infant syndrome, neonatal withdrawal, and hypotonia. Avoid in third trimester if possible. |
| Fetal Monitoring |
■ FDA Black Box Warning
Concomitant use with opioids may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant use for patients without alternative treatment options.
| Serious Effects |
["Acute narrow-angle glaucoma","Severe respiratory insufficiency","Myasthenia gravis","Known hypersensitivity to benzodiazepines","Concurrent use with opioids (except in specific monitored settings)"]
| Precautions | ["Risk of sedation, respiratory depression, and dependence","May cause drowsiness, impair cognitive and motor function","Avoid abrupt discontinuation to prevent withdrawal symptoms","Use with caution in patients with hepatic impairment","Elderly patients more sensitive to effects"] |
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| Monitor maternal sedation, respiratory rate, and withdrawal symptoms (tachyphylaxis/tolerance). Fetal monitoring: Consider fetal growth ultrasound if used chronically; assess for neonatal withdrawal at birth using Finnegan scoring if used near term. |
| Fertility Effects | No specific human studies. Animal studies show high doses may impair fertility; clinical significance unknown. Evaluate individual case. |