LABETALOL HYDROCHLORIDE IN SODIUM CHLORIDE

Clinical safety rating: safe

No significant drug interactions Can cause hypernatremia and fluid overload.

How it works

Labetalol is a competitive antagonist at both beta-adrenoceptors (beta1 and beta2) and alpha1-adrenoceptors, leading to decreased cardiac output, peripheral vascular resistance, and reduced blood pressure.

What the body does with it

Metabolism	Extensively metabolized in the liver via glucuronidation (direct conjugation) and also via CYP2D6 (minor pathway).
Excretion	Primarily renal (90-95% as unchanged drug and glucuronide conjugates) and a small amount in feces (<5%).
Half-life	Terminal elimination half-life is 6-8 hours; may be prolonged in elderly, hepatic impairment, or renal impairment (up to 16 hours).
Protein binding	Approximately 50% bound to albumin.
Volume of Distribution	Vd is 0.5-1.2 L/kg; distributes extensively into tissues, including crossing the placenta and entering breast milk.
Bioavailability	Oral: 25-40% due to extensive first-pass metabolism; Intravenous: 100%.
Onset of Action	Intravenous: 5-10 minutes; Oral: 20-40 minutes.
Duration of Action	Intravenous: 2-6 hours; Oral: 8-12 hours (dose dependent).

Classification & Brands

Dosing & administration

Intravenous: Initially 20 mg (0.25 mg/kg for 70 kg) over 2 minutes, then 40-80 mg every 10 minutes until desired response or total 300 mg; or continuous infusion at 0.5-2 mg/min titrated to blood pressure. Switch to oral when stable.

Dosage form	SOLUTION
Renal impairment	No specific dose adjustment required for GFR >15 mL/min; for GFR <15 mL/min or dialysis, use with caution and consider reducing dose. Monitor for hypotension and bradycardia.
Liver impairment	Child-Pugh A: No adjustment required. Child-Pugh B: Reduce dose by 50% and titrate slowly. Child-Pugh C: Contraindicated due to extensive hepatic metabolism.
Pediatric use	Intravenous: 0.2-0.5 mg/kg/dose every 10 minutes as needed, up to 1 mg/kg total. Continuous infusion: 0.25-3 mg/kg/hour. Maximum single dose: 1 mg/kg.
Geriatric use	Start with low end of dosing range (e.g., 10-20 mg IV initial), titrate cautiously due to increased sensitivity and risk of hypotension, bradycardia, and bronchospasm.

Use during pregnancy

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

Clinical note

No significant drug interactions Can cause hypernatremia and fluid overload.

FDA category	Animal
Breastfeeding	Excreted into breast milk in small amounts; average milk-to-plasma ratio (M/P) 0.15-0.80. Considered compatible with breastfeeding by American Academy of Pediatrics, but monitor infant for bradycardia and hypotension.
Teratogenic Risk	First trimester: Limited human data; animal studies show no major teratogenic effects at clinically relevant doses. Second and third trimesters: Associated with fetal bradycardia, hypotension, hypoglycemia, and intrauterine growth restriction due to beta-blockade. Risk of preterm delivery and respiratory depression at birth.

Warnings & precautions

■ FDA Black Box Warning

No FDA boxed warning.

Side Effect Profile

Common Effects	fluid replacement
Serious Effects

Absolute Contraindications

Hypersensitivity to labetalol; bronchial asthma; overt cardiac failure; cardiogenic shock; severe bradycardia; heart block greater than first degree; severe hypotension.

Clinical Precautions

Precautions

May cause bronchospasm in patients with asthma/COPD; may mask symptoms of hypoglycemia or thyrotoxicosis; may cause severe bradycardia; discontinue if signs of hepatic injury occur; use caution in patients with heart failure or diabetes.

Clinical Tips & Counseling

Drug interactions

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LABETALOL HYDROCHLORIDE IN SODIUM CHLORIDE

Clinical safety rating: safe

No significant drug interactions Can cause hypernatremia and fluid overload.

How it works

What the body does with it

Metabolism	Extensively metabolized in the liver via glucuronidation (direct conjugation) and also via CYP2D6 (minor pathway).
Excretion	Primarily renal (90-95% as unchanged drug and glucuronide conjugates) and a small amount in feces (<5%).
Half-life	Terminal elimination half-life is 6-8 hours; may be prolonged in elderly, hepatic impairment, or renal impairment (up to 16 hours).
Protein binding	Approximately 50% bound to albumin.
Volume of Distribution	Vd is 0.5-1.2 L/kg; distributes extensively into tissues, including crossing the placenta and entering breast milk.
Bioavailability	Oral: 25-40% due to extensive first-pass metabolism; Intravenous: 100%.
Onset of Action	Intravenous: 5-10 minutes; Oral: 20-40 minutes.
Duration of Action	Intravenous: 2-6 hours; Oral: 8-12 hours (dose dependent).

Classification & Brands

Dosing & administration

Dosage form	SOLUTION
Renal impairment	No specific dose adjustment required for GFR >15 mL/min; for GFR <15 mL/min or dialysis, use with caution and consider reducing dose. Monitor for hypotension and bradycardia.
Liver impairment	Child-Pugh A: No adjustment required. Child-Pugh B: Reduce dose by 50% and titrate slowly. Child-Pugh C: Contraindicated due to extensive hepatic metabolism.
Pediatric use	Intravenous: 0.2-0.5 mg/kg/dose every 10 minutes as needed, up to 1 mg/kg total. Continuous infusion: 0.25-3 mg/kg/hour. Maximum single dose: 1 mg/kg.
Geriatric use	Start with low end of dosing range (e.g., 10-20 mg IV initial), titrate cautiously due to increased sensitivity and risk of hypotension, bradycardia, and bronchospasm.

Use during pregnancy

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

Clinical note

No significant drug interactions Can cause hypernatremia and fluid overload.

FDA category	Animal
Breastfeeding	Excreted into breast milk in small amounts; average milk-to-plasma ratio (M/P) 0.15-0.80. Considered compatible with breastfeeding by American Academy of Pediatrics, but monitor infant for bradycardia and hypotension.
Teratogenic Risk	First trimester: Limited human data; animal studies show no major teratogenic effects at clinically relevant doses. Second and third trimesters: Associated with fetal bradycardia, hypotension, hypoglycemia, and intrauterine growth restriction due to beta-blockade. Risk of preterm delivery and respiratory depression at birth.

Warnings & precautions

■ FDA Black Box Warning

No FDA boxed warning.

Side Effect Profile

Common Effects	fluid replacement
Serious Effects

Absolute Contraindications

Hypersensitivity to labetalol; bronchial asthma; overt cardiac failure; cardiogenic shock; severe bradycardia; heart block greater than first degree; severe hypotension.