II. Indications
-
Refractory Hypertension
- Effective outpatient agent in oral form patients with Refractory Hypertension
-
Hypertensive Emergency
-
Nicardipine has replaced intravenous Labetalol for Hypertensive Emergency
- Labetalol is difficult to achieve Blood Pressure control in Hypertensive Crisis despite titration
- Labetalol is short acting
- Labetalol is a preferred agent when compared with Hydaralazine and Clonidine
-
Nicardipine has replaced intravenous Labetalol for Hypertensive Emergency
III. Contraindications
IV. Pharmacokinetics
- Well absorbed and high first-pass metabolism (liver metabolism)
V. Mechanism
- Combination of classes (similar to Carvedilol)
- Lowers Blood Pressure without reflex Tachycardia
- Nonselective Beta Blocker (7 fold more beta than alpha activity)
- Binds vascular (and Bronchial) smooth muscle beta receptors
- Decreases Heart Rate, Cardiac Output and Blood Pressure
- Selective Alpha-1 Adrenergic Antagonist (weak compared with beta activity)
- Competitively binds vascular smooth muscle alpha-1 Adrenergic Receptors
- Blocks peripheral blood vessel Vasoconstriction
- Primary activity is as a negative inotrope
- Chronotropic effect is mild
VI. Dosing: Adults
- Adjust dose in liver and renal Impairment
- Oral
- Start: 100 mg orally twice daily
- Target: 200 to 600 mg orally twice daily
- Maximum: 2400 mg/day
- Intravenous Injection
- Start: 20 mg slow IV injection
- Next: 40-80 mg every 10 minutes as needed
- Cummulative Maximum: 200-300 mg
- Intravenous Infusion
- Start 0.5 to 2 mg/min IV up to cummulative maximum of 200-300 mg
VII. Dosing: Children (Not FDA approved)
- Oral
- Start: 4 mg/kg/day orally divided twice daily
- Maximum: 40 mg/kg/day up to adult maximum of 2400 mg
- Intravenous Infusion
- Dose: 0.3 to 1 mg/kg/dose up to 20 mg slow IV injection up to every 10 minutes
- Cummulative Maximum: 200-300 mg
- Intravenous Infusion
- Start 0.4 to 1 mg/kg/hour IV up to 3 mg/kg/hour
VIII. Adverse Effects
- May worsen acute exacerbations of Congestive Heart Failure
- Fatigue
- Erectile Dysfunction
- Orthostatic Hypotension
IX. Drug Interactions
- Systemic Beta Agonists
- Labetalol blocks bronchodilation
X. References
- Olson (2020) Clinical Pharmacology, MedMaster, Miami, p. 66
- Hamilton (2020) Tarascon Pocket Pharmacopeia, Jones and Bartlett, accessed on IOS, 4/9/2021
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Related Studies
| labetalol (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| LABETALOL HCL 100 MG TABLET | Generic | $0.22 each |
| LABETALOL HCL 200 MG TABLET | Generic | $0.26 each |
| LABETALOL HCL 300 MG TABLET | Generic | $0.47 each |
Ontology: Labetalol (C0022860)
| Definition (MSH) | A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS. |
| Definition (NCI) | A third generation selective alpha-1-adrenergic antagonist and non-selective beta-adrenergic antagonist with vasodilatory and antihypertensive properties. Labetalol competitively binds to alpha-1-adrenergic receptors in vascular smooth muscle, thereby inhibiting the adrenergic stimulation of endothelial cell function and vasoconstriction in peripheral blood vessels. This agent also binds to beta-receptors in the bronchial and vascular smooth muscle, resulting in a decrease in adrenergic stimulation. The result is a decrease in resting and exercise heart rates, cardiac output, and in both systolic and diastolic blood pressure, thereby resulting in vasodilation, and negative chronotropic and inotropic cardiac effects. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D007741 |
| SnomedCT | 372750000, 46547007 |
| LNC | LP16170-0, MTHU007202 |
| English | Labetalol, Labetolol, Benzamide, 2-hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)-, Labetalol [Chemical/Ingredient], labetolol, LABETALOL, beta blockers labetalol, labetalol (medication), labetalol, Labetalol (product), Labetalol (substance) |
| Swedish | Labetalol |
| Czech | labetalol |
| Finnish | Labetaloli |
| French | Labétolol, Labétalol |
| Russian | LABETALOL, AN 5158, АН 5158, ЛАБЕТАЛОЛ |
| Japanese | ラベタロール |
| Italian | Labetololo, Labetalolo |
| Croatian | LABETALOL |
| Polish | Labetalol |
| Spanish | ibidomida, labetalol (producto), labetalol (sustancia), labetalol, Labetalol |
| German | Labetalol |
| Portuguese | Labetalol |
