ATIVAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ATIVAN (ATIVAN).

How it works

Benzodiazepine that potentiates GABA-A receptor activity by increasing the frequency of chloride channel opening, leading to neuronal hyperpolarization and inhibition.

What the body does with it

Metabolism	Hepatic via glucuronidation (UGT2B15, UGT2B7); major metabolite is lorazepam glucuronide (inactive).
Excretion	Renal: lorazepam is primarily excreted as inactive glucuronide conjugates; <1% is excreted unchanged. Total: ~95% excreted in urine, ~5% in feces.
Half-life	Terminal elimination half-life is 12–18 hours (mean ~14 h). In elderly, hepatic impairment, or obesity, half-life may be prolonged up to 30 hours.
Protein binding	91% ± 2% bound to albumin. Binding is linear over therapeutic concentrations and not saturable.
Volume of Distribution	1.3 ± 0.2 L/kg. Vd increases with obesity, hepatic cirrhosis, and in elderly patients, indicating extensive tissue distribution.
Bioavailability	Oral: 90% (range 80–100%) with first-pass metabolism negligible; Sublingual: ~90%; Intramuscular: 100% (absolute bioavailability).
Onset of Action	Oral: 1–2 hours; Sublingual: 20–30 minutes; Intramuscular: 15–30 minutes; Intravenous: 1–5 minutes (peak CNS effect at 15–20 min).
Duration of Action	Oral: 6–8 hours (effects may last up to 12 h with high doses). IV: 6–8 hours. IM: 6–8 hours. Clinical duration is sufficient for anxiety and seizure control, but may require repeat dosing for prolonged sedation.

Classification & Brands

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

Dosing & administration

2-3 mg orally divided 2-3 times daily; up to 10 mg/day. IV: 2 mg slow IV push, may repeat in 1-2 hours; max 10 mg/day. IM: 0.05 mg/kg (max 4 mg) 2-4 hours before procedure.

Dosage form	TABLET
Renal impairment	CrCl 10-50 mL/min: reduce dose by 50% or increase interval; CrCl <10 mL/min: avoid or reduce dose by 50-75% with caution.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid or reduce dose by 50-75% with monitoring.
Pediatric use	Children ≥6 months: 0.02-0.05 mg/kg/dose IV/IM (max 2 mg) for status epilepticus; PO: 0.05-0.1 mg/kg/dose (max 2 mg) 2-4 times daily.
Geriatric use	Initiate at 0.5-1 mg orally daily in divided doses; increase slowly; max 2 mg/day. IV/IM: 0.5-1 mg initial; avoid doses >2 mg due to increased sedation risk.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ATIVAN (ATIVAN).

Breastfeeding	Enters breast milk; M/P ratio approximately 0.2–0.5; avoid or use with caution due to infant sedation and feeding difficulties; monitor for drowsiness and weight gain.
Teratogenic Risk	First trimester: Increased risk of oral clefts (odds ratio 1.5–2.0); second and third trimesters: Risk of hypotonia, respiratory depression, and withdrawal symptoms in neonate; avoid in first trimester if possible; use lowest effective dose.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to lorazepam or any benzodiazepine","Acute narrow-angle glaucoma","Severe respiratory insufficiency","Myasthenia gravis","Concurrent use with opioids (absolute unless alternative unavailable)"]

Clinical Precautions

Precautions	["Respiratory depression risk","Dependence and withdrawal syndrome","Abuse potential","Paradoxical reactions (hyperactivity, aggression)","Use with caution in hepatic impairment","Elderly at increased risk for sedation and falls"]
Food/Dietary	No specific food interactions. However, grapefruit juice may increase lorazepam levels (minor interaction). Avoid excessive caffeine as it may reduce sedative effects.

Clinical Tips & Counseling

Drug interactions

Loading safety data…

ATIVAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ATIVAN (ATIVAN).

How it works

Benzodiazepine that potentiates GABA-A receptor activity by increasing the frequency of chloride channel opening, leading to neuronal hyperpolarization and inhibition.

What the body does with it

Metabolism	Hepatic via glucuronidation (UGT2B15, UGT2B7); major metabolite is lorazepam glucuronide (inactive).
Excretion	Renal: lorazepam is primarily excreted as inactive glucuronide conjugates; <1% is excreted unchanged. Total: ~95% excreted in urine, ~5% in feces.
Half-life	Terminal elimination half-life is 12–18 hours (mean ~14 h). In elderly, hepatic impairment, or obesity, half-life may be prolonged up to 30 hours.
Protein binding	91% ± 2% bound to albumin. Binding is linear over therapeutic concentrations and not saturable.
Volume of Distribution	1.3 ± 0.2 L/kg. Vd increases with obesity, hepatic cirrhosis, and in elderly patients, indicating extensive tissue distribution.
Bioavailability	Oral: 90% (range 80–100%) with first-pass metabolism negligible; Sublingual: ~90%; Intramuscular: 100% (absolute bioavailability).
Onset of Action	Oral: 1–2 hours; Sublingual: 20–30 minutes; Intramuscular: 15–30 minutes; Intravenous: 1–5 minutes (peak CNS effect at 15–20 min).
Duration of Action	Oral: 6–8 hours (effects may last up to 12 h with high doses). IV: 6–8 hours. IM: 6–8 hours. Clinical duration is sufficient for anxiety and seizure control, but may require repeat dosing for prolonged sedation.

Classification & Brands

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

Dosing & administration

2-3 mg orally divided 2-3 times daily; up to 10 mg/day. IV: 2 mg slow IV push, may repeat in 1-2 hours; max 10 mg/day. IM: 0.05 mg/kg (max 4 mg) 2-4 hours before procedure.

Dosage form	TABLET
Renal impairment	CrCl 10-50 mL/min: reduce dose by 50% or increase interval; CrCl <10 mL/min: avoid or reduce dose by 50-75% with caution.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid or reduce dose by 50-75% with monitoring.
Pediatric use	Children ≥6 months: 0.02-0.05 mg/kg/dose IV/IM (max 2 mg) for status epilepticus; PO: 0.05-0.1 mg/kg/dose (max 2 mg) 2-4 times daily.
Geriatric use	Initiate at 0.5-1 mg orally daily in divided doses; increase slowly; max 2 mg/day. IV/IM: 0.5-1 mg initial; avoid doses >2 mg due to increased sedation risk.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ATIVAN (ATIVAN).

Breastfeeding	Enters breast milk; M/P ratio approximately 0.2–0.5; avoid or use with caution due to infant sedation and feeding difficulties; monitor for drowsiness and weight gain.
Teratogenic Risk	First trimester: Increased risk of oral clefts (odds ratio 1.5–2.0); second and third trimesters: Risk of hypotonia, respiratory depression, and withdrawal symptoms in neonate; avoid in first trimester if possible; use lowest effective dose.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death.

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions	["Respiratory depression risk","Dependence and withdrawal syndrome","Abuse potential","Paradoxical reactions (hyperactivity, aggression)","Use with caution in hepatic impairment","Elderly at increased risk for sedation and falls"]
Food/Dietary	No specific food interactions. However, grapefruit juice may increase lorazepam levels (minor interaction). Avoid excessive caffeine as it may reduce sedative effects.

Clinical Tips & Counseling

Drug interactions

Loading safety data…