II. Indications
- Blood Pressure Management in Pregnancy
-
Refractory Hypertension
- Effective outpatient agent in oral form patients with Refractory Hypertension
-
Hypertensive Emergency
- Labetalol is a preferred agent when compared with Hydaralazine and Clonidine
-
Nicardipine and Clevidipine have replaced intravenous Labetalol for Hypertensive Emergency
- Labetalol is difficult to achieve Blood Pressure control in Hypertensive Crisis despite titration
- Labetalol is short acting
III. Contraindications
IV. Pharmacokinetics
- Not lipophilic
- Hepatic metabolism
-
Bioavailability 20 to 40%
- Well absorbed but high first-pass hepatic metabolism
- Bioavailability increased when taken with food
V. Mechanism
- Not Cardioselective
- Primary activity is as a negative inotrope
- Chronotropic effect is mild
- 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
VI. Dosing: Adults
- Adjust dose in liver and renal Impairment
- Oral
- 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. Safety
- Pregnancy Category C
- Safe in Lactation
XI. Resources
- Labetalol Injection (DailyMed)
- Labetalol Tablet (DailyMed)
XII. References
- (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
- Olson (2020) Clinical Pharmacology, MedMaster, Miami, p. 66
- Hamilton (2020) Tarascon Pocket Pharmacopeia, Jones and Bartlett, accessed on IOS, 4/9/2021
Images: Related links to external sites (from Bing)
Related Studies
| labetalol (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| LABETALOL HCL 100 MG TABLET | Generic | $0.12 each |
| LABETALOL HCL 200 MG TABLET | Generic | $0.16 each |
| LABETALOL HCL 300 MG TABLET | Generic | $0.21 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 |
Ontology: Trandate (C0592195)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D007741 |
| English | Faro Brand of Labetalol Hydrochloride, trandate, Celltech Brand of Labetalol Hydrochloride, Glaxo Wellcome Brand of Labetalol Hydrochloride, GlaxoSmithKline Brand of Labetalol Hydrochloride, Kern Brand of Labetalol Hydrochloride, Shire Brand of Labetalol Hydrochloride, Sigma Brand of Labetalol Hydrochloride, Trandate |
