Labetalol

Labetalol (brand name Trandate[1], Normodyne) is a beta blocker medication used to treat high blood pressure (hypertension), including high blood pressure in pregnancy.[1]

Labetalol
Clinical data
Pronunciation/ləˈbɛtəlɔːl/
Trade namesNormodyne, Trandate, others
AHFS/Drugs.comMonograph
MedlinePlusa685034
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth, intravenous
ATC code
Pharmacokinetic data
Bioavailability25%
Protein binding50%
MetabolismLiver pass metabolism,
Elimination half-lifeTablet: 6–8 hours; IV: 5.5 hours
ExcretionExcreted in urine, not removed by hemodialysis
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.048.401
Chemical and physical data
ChiralityRacemic mixture
  (verify)

This medicine can cause serious allergic reactions that require emergency treatment. Make sure the signs of these reactions are known: read allergic reaction symptoms of drugs.

Taking labetalol helps to prevent future heart disease, heart attacks and strokes in people with high blood pressure[1], because they are at a higher risk. It can also be used to prevent chest pain caused by angina.[1]

Labetalol was patented in 1966 and came into medical use in 1977.[2] It is available as a generic medication.[3] In 2021, it was the 213th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[4][5][6]

Function

Labetalol works by slowing down the heart rate and making it easier for the heart to pump blood around the body.[1]

Dose

This medicine is only available on prescription. It comes as tablets. It can also be given as an injection in hospital. Strength: Labetalol tablets come in different doses:[1]

  • 50mg
  • 100mg
  • 200mg
  • 400mg

The usual dose of labetalol for adults is between 400mg and 800mg a day, split into 2 doses.[1]

Dose can be increased up to 2,400mg a day. The dose may be increased every 1 to 2 weeks[1]. This is called titration. Once a dose works, it will usually stay the same amount.

It is usually not recommended to stop taking labetalol suddenly, especially if there is heart disease. This can make conditions worse.[1]

Conflicts (conditions/medicines)

New, current or past problems should be noticed before starting to take labetalol, such as:[1]

Other medicines

There are some medicines that may affect the way labetalol works:[1]

  • other medicines for high blood pressure – when taken together with labetalol, this can sometimes lower blood pressure too much, which may cause dizziness or fainting. If this keeps happening, tell a doctor. They may change the dose
  • other medicines that can lower blood pressure – these include some antidepressants, nitrates (for chest pain), baclofen (a muscle relaxant), medicines for an enlarged prostate, like tamsulosin, or medicines for Parkinson's disease, such as co-careldopa or levodopa
  • medicines for the heart, such as amiodarone, flecainide or digoxin
  • non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen – they can stop labetalol working properly
  • medicines for diabetes, particularly insulin – labetalol may make it more difficult to recognise the warning signs of low blood sugar. Speak to the doctor if low blood sugar levels without getting any of the usual warning signs happens. Check blood sugar after exercise, and follow the usual advice about checking it before driving or operating machinery
  • steroids like prednisolone
  • cough medicines that contain pseudoephedrine or xylometazoline
  • medicines for allergies, such as ephedrine, noradrenaline or adrenaline
  • medicines for asthma or chronic obstructive pulmonary disease (COPD)

There might be a problem taking some herbal remedies and supplements together with labetalol, especially ones that cause side effects like low blood pressure. But there is not enough information to say that other herbal remedies and supplements are safe to take with labetalol. They are usually not tested in the same way as pharmacy and prescription medicines.[1]

Side effects

Like all medicines, labetalol can cause side effects in some people, but many people have no side effects or only minor ones.[1] Labetanol can cause allergic reactions. These can be serious, and an ambulance should be called, or visit A&E if it is needed.

Common

The most common side effects of labetalol are feeling dizzy, sleepy or weak, headaches, cold fingers and toes, and feeling or being sick (nausea and vomiting). Sometimes also stomach pains. These usually happen at the start of treatment and do not last long.[1]

These common side effects of labetalol happen in more than 1 in 100 people.[1]

Severe/Serious

It does not happen often, but some people have serious side effects when taking labetalol.

Tell a doctor or call emergency help now if there are any of the symptoms:[1]

  • shortness of breath with a cough that gets worse with exercise (like walking up stairs)
  • swollen ankles or legs, or an irregular heartbeat. These are signs of heart problems
  • shortness of breath, wheezing and tightening of the chest. These can be signs of lung problems
  • whites of the eyes turn yellow, or skin turns yellow although this may be less noticeable on brown or black skin, or there is pale poo or dark pee. These can be signs of liver problems
  • unexplained bruising, or getting a bruise more easily than usual. These can be signs of low numbers of platelets in blood (thrombocytopenia)

References
  1. "Common questions about labetalol". nhs.uk. 2022-03-08. Retrieved 2024-05-30.
  2. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 463. ISBN 9783527607495.
  4. "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  5. "Labetalol - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  6. Source Wikipedia
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