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Adrenergic receptor blocker (alpha and beta blocker)

How it worksLabetalol hydrochloride works by blocking both alpha-1 and beta-adrenergic receptors. This action helps to lower blood pressure.

Brand names:LABETALOL HYDROCHLORIDE

Used for
Control of blood pressure in severe hypertension
Conditions
Severe hypertension
Class
Alpha-blockerBeta-blockerAntihypertensiveAdrenergic receptor blocker (alpha and beta blocker)Cardiovascular SystemCentral Nervous SystemPeripheral Nervous SystemGastrointestinal SystemMetabolic SystemRespiratory SystemIntegumentary System

How to take

FormsInjection (Intravenous)
RoutesIntravenous

Dosage must be decided by a doctor based on how severe the high blood pressure is and how the patient responds. It is given as either repeated injections or a slow continuous infusion while the patient is lying down.

Patients must remain lying down during administration because blood pressure can drop significantly when standing up.

Key warnings

  • ·Liver injury: Rare but serious liver damage has been reported. Doctors may need to monitor liver function through blood tests.
  • ·Asthma/Airway issues: This drug should not be used in people with asthma or other obstructive airway diseases.
  • ·Heart conditions: It is not recommended for people with certain heart problems like severe slow heart rate or heart block.

Do not use if

  • ·Bronchial asthma
  • ·Overt cardiac failure
  • ·Severe slow heart rate (bradycardia)
  • ·Cardiogenic shock
  • ·Certain types of heart block

Side effects

Common

DizzinessNauseaFeeling sleepy or yawningSweatingNumbness or tingling of the skinVomitingFlushing

Serious

  • ·Liver injury (symptoms include jaundice, dark urine, or abdominal pain)
  • ·Severe slow heart rate (bradycardia)
  • ·Heart failure
  • ·Wheezing or breathing issues
  • ·Extreme drop in blood pressure

Seek help if

  • ·Jaundice or dark urine
  • ·Severe slow heart rate
  • ·Difficulty breathing or wheezing
  • ·Severe dizziness or fainting

Interactions

  • ·Other blood pressure medications may cause unexpected effects.
  • ·Tricyclic antidepressants might increase the risk of tremors.
  • ·Cimetidine may increase the amount of drug in your system.
  • ·Beta-blockers can make asthma inhalers less effective.

Special populations

PregnancyLabetalol should only be used during pregnancy if the potential benefits to the mother outweigh the risks to the baby. Animal studies showed some increased fetal loss at high doses.

BreastfeedingSmall amounts of this medicine pass into breast milk, so caution is advised when using it while nursing.

PediatricThe safety and effectiveness of labetalol in children have not been established.

Talk to your doctor

Monitor

  • ·Blood pressure (especially when standing)
  • ·Liver function (jaundice, dark urine, abdominal pain)
  • ·Heart rate (bradycardia)
  • ·Breathing (wheezing)

Questions to ask

  • ·How will this medication affect my blood pressure when I stand up?
  • ·Should I have my liver function tested while taking this?
  • ·How will this interact with my other blood pressure medicines?
  • ·Is it safe to continue breastfeeding while on this medication?

Pharmacokinetics

OnsetMaximum effect usually occurs within 5 minutes of each injection.
BioavailabilityCimetidine may increase the bioavailability of oral labetalol.
MetabolismInvolves hepatic metabolism; cimetidine may alter this.
ExcretionSmall amounts (0.004%) are excreted in human milk.

Practical

OverdoseAn overdose can cause dangerously low blood pressure and a very slow heart rate. Patients should be kept lying down with legs raised to help blood flow to the brain.

Ingredients

Allergens

sulfite

Inactive

anhydrous dextroseedetate disodiummethylparabenpropylparabencitric acid monohydratesodium hydroxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.