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LABETalol

Classification

Selective alpha and non-selective beta-adrenergic blocker

Indications

CCP: Severe hypertension or hypertensive crisis

Contraindications

Known hypersensitivity to labetalol or any ingredient in the formulation
Bronchospastic airway disease
Obvious congestive heart failure
Second or third-degree heart block
Cardiogenic shock
Severe bradycardia
Other conditions associated with severe and prolonged hypotension

Adult dosages

CCP: Severe hypertension or hypertensive crisis

Initial goal of IV therapy is to reduce mean arterial BP by no more than 25% within minutes to 1 hour followed by further reduction if stable toward 160/100 to 110 mmHg within the following 2–6 hours, avoiding excessive declines in pressure that could precipitate renal, cerebral, or coronary insufficiency; if this BP is well tolerated and the patient is clinically stable, further gradual reductions toward normal can be implemented in the following 24–48 hours
Intravenous bolus dosing:
- 20-80 mg slow IV push
- Higher initial doses (1-2 mg/kg) are available, but 20 mg is recommended to minimize adverse events and risks associated with a rapid fall in blood pressure
- Additional doses can be given (20-80 mg) at 10 minute intervals until the desired supine blood pressure is reached, or to a total cumulative dose of 300 mg
Intravenous infusion dosing:
- 0.5-2 mg/min via continuous infusion; adjust flow rate based on blood pressure response
- Progressive, incremental IV infusion regimen (i.e., infusing 20, 40, 80, and 160 mg/hour for 1 hour at each dose level, or until the desired BP is achieved) has been used and may result in more gradual BP reduction, minimizing adverse effects compared with repeated IV injections of the drug; controlled comparisons of various IV administration methods are not available
- Maximum cumulative dose of 300 mg
Adjust dosage according to the severity of hypertension and the patient’s supine BP response and tolerance
Patients with aortic dissection should have systolic pressure reduced to < 100 mmHg if tolerated

Pediatric Considerations And Dosing

Follow weight-based dosing

Mechanism Of Action

Competitively blocks adrenergic stimulation of β-receptors within the myocardium (β₁-receptors) and within bronchial and vascular smooth muscle (β₂-receptors) and α₁-receptors within vascular smooth muscle.

Pharmacokinetics

Intravenous:

Onset:
- Following slow, direct IV injection, hypotensive effect is apparent within 2–5 minutes and usually maximal within 5–15 minutes
Peak:
- 5-15 minutes
Duration:
- Following slow, direct IV injection, the hypotensive effect generally persists for about 2–4 hours, although a longer duration of effect (i.e., up to 24 hours) has been reported in some patients

Adverse Effects

Symptomatic orthostatic hypotension
Dizziness or light headedness
Fatigue
Nausea or dyspepsia

Overdose

Management of overdose is consistent with the management of beta blocker toxicity. See CPG J07: Beta Blocker Toxicity for additional information.

Warning And Precautions

Use of LABETalol carries the risk of precipitating congestive heart failure. LABETalol may be used cautiously in patients with well-compensated heart failure (i.e., those whose heart failure is controlled with cardiac glycosides or diuretics).