LORAZEPAM INTENSOL

Clinical safety rating: avoid

CNS depressants including alcohol and opioids increase sedation risk Abrupt discontinuation can cause withdrawal symptoms.

How it works

Benzodiazepine that enhances 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	Primarily hepatic via glucuronidation (UGT2B7, UGT2B15) to inactive metabolites.
Excretion	Renal excretion of glucuronide conjugates; <1% unchanged drug excreted renally. Fecal elimination accounts for approximately 10% of administered dose.
Half-life	Terminal elimination half-life is 12-15 hours in healthy adults; prolonged in elderly (15-20 hours) and patients with hepatic impairment (up to 30-40 hours).
Protein binding	Approximately 85-90% bound to albumin.
Volume of Distribution	1.0-1.3 L/kg; distribution into tissues including brain.
Bioavailability	Oral (Intensol): approximately 90% (rapidly and completely absorbed). Intramuscular: 80-100%.
Onset of Action	Intensol (oral concentrate): 20-30 minutes. Intramuscular: 15-30 minutes. Intravenous: 2-5 minutes.
Duration of Action	Duration of clinical effect: 6-8 hours for anxiolysis; sedation may persist up to 12 hours.

Classification & Brands

Dosing & administration

0.5-2 mg orally every 6-8 hours as needed. Maximum 4 mg/day.

Dosage form	CONCENTRATE
Renal impairment	GFR 10-50 mL/min: no adjustment needed. GFR <10 mL/min: caution, risk of accumulation; use 50% of usual dose.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid or use with extreme caution.
Pediatric use	0.05-0.1 mg/kg/dose orally every 4-8 hours as needed; maximum single dose 2 mg.
Geriatric use	Initial dose 0.5 mg orally once daily, titrate slowly; maximum 2 mg/day in divided doses. Avoid prolonged use due to fall risk and cognitive impairment.

Use during pregnancy

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

Clinical note

CNS depressants including alcohol and opioids increase sedation risk Abrupt discontinuation can cause withdrawal symptoms.

FDA category	Positive
Breastfeeding	Lorazepam is excreted into breast milk in low amounts. Milk-to-plasma ratio is approximately 0.15-0.23. Although generally considered compatible with breastfeeding, monitor for infant sedation, poor feeding, and weight gain. Use lowest effective dose for shortest duration.
Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing for patients for whom alternative treatment options are inadequate.

Side Effect Profile

Common Effects	insomnia
Serious Effects

Absolute Contraindications

["Hypersensitivity to benzodiazepines","Acute narrow-angle glaucoma","Severe respiratory insufficiency (e.g., COPD, sleep apnea)","Myasthenia gravis","Concomitant use with protease inhibitors (e.g., atazanavir, ritonavir)"]

Clinical Precautions

Precautions

["Risk of respiratory depression, especially with other CNS depressants","Dependence and withdrawal reactions with prolonged use","Paradoxical reactions (e.g., hyperactivity, aggression)","Use with caution in hepatic or renal impairment","Elderly patients more sensitive to effects (e.g., falls, cognitive impairment)"]

Clinical Tips & Counseling

Drug interactions

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LORAZEPAM INTENSOL

Clinical safety rating: avoid

CNS depressants including alcohol and opioids increase sedation risk Abrupt discontinuation can cause withdrawal symptoms.

How it works

Benzodiazepine that enhances 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	Primarily hepatic via glucuronidation (UGT2B7, UGT2B15) to inactive metabolites.
Excretion	Renal excretion of glucuronide conjugates; <1% unchanged drug excreted renally. Fecal elimination accounts for approximately 10% of administered dose.
Half-life	Terminal elimination half-life is 12-15 hours in healthy adults; prolonged in elderly (15-20 hours) and patients with hepatic impairment (up to 30-40 hours).
Protein binding	Approximately 85-90% bound to albumin.
Volume of Distribution	1.0-1.3 L/kg; distribution into tissues including brain.
Bioavailability	Oral (Intensol): approximately 90% (rapidly and completely absorbed). Intramuscular: 80-100%.
Onset of Action	Intensol (oral concentrate): 20-30 minutes. Intramuscular: 15-30 minutes. Intravenous: 2-5 minutes.
Duration of Action	Duration of clinical effect: 6-8 hours for anxiolysis; sedation may persist up to 12 hours.

Classification & Brands

Dosing & administration

0.5-2 mg orally every 6-8 hours as needed. Maximum 4 mg/day.

Dosage form	CONCENTRATE
Renal impairment	GFR 10-50 mL/min: no adjustment needed. GFR <10 mL/min: caution, risk of accumulation; use 50% of usual dose.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid or use with extreme caution.
Pediatric use	0.05-0.1 mg/kg/dose orally every 4-8 hours as needed; maximum single dose 2 mg.
Geriatric use	Initial dose 0.5 mg orally once daily, titrate slowly; maximum 2 mg/day in divided doses. Avoid prolonged use due to fall risk and cognitive impairment.

Use during pregnancy

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

Clinical note

CNS depressants including alcohol and opioids increase sedation risk Abrupt discontinuation can cause withdrawal symptoms.

FDA category	Positive
Breastfeeding	Lorazepam is excreted into breast milk in low amounts. Milk-to-plasma ratio is approximately 0.15-0.23. Although generally considered compatible with breastfeeding, monitor for infant sedation, poor feeding, and weight gain. Use lowest effective dose for shortest duration.
Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Common Effects	insomnia
Serious Effects