pharmacopeia
GET
/api/v1/drug/labetalol
2D structure
2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide
SMILES CC(CCC1=CC=CC=C1)NCC(C2=CC(=C(C=C2)O)C(=O)N)O
InChIKey SGUAFYQXFOLMHL-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Adrenergic alpha1-Antagonists; Adrenergic beta-Antagonists; Adrenergic beta1-Antagonists; Adrenergic beta2-Antagonists.

Indications

Sourced from openFDA
  • Labetalol hydrochloride tablets USP are indicated in the management of hypertension. Labetalol hydrochloride tablets USP may be used alone or in combination with other antihypertensive agents, especially thiazide and loop diuretics.ICD-10: I10

Contraindications

Sourced from openFDA
  • Labetalol hydrochloride is contraindicated in bronchial asthma, overt cardiac failure, greater-than-first-degree heart block, cardiogenic shock, severe bradycardia, other conditions associated with severe and prolonged hypotension, and in patients with a history of hypersensitivity to any component of the product [see Warnings] . Beta-blockers, even those with apparent cardioselectivity, should not be used in patients with a history of obstructive airway disease, including asthma.contraindicated

Dosage & administration

Sourced from openFDA

DOSAGE MUST BE INDIVIDUALIZED. The recommended initial dosage is 100 mg twice daily whether used alone or added to a diuretic regimen. After 2 or 3 days, using standing blood pressure as an indicator, dosage may be titrated in increments of 100 mg b.i.d.(twice daily) every 2 or 3 days. The usual maintenance dosage of labetalol hydrochloride tablets is between 200 mg and 400 mg twice daily. Since the full antihypertensive effect of labetalol hydrochloride tablets is usually seen within the first 1 to 3 hours of the initial dose or dose increment, the assurance of a lack of an exaggerated hypotensive response can be clinically established in the office setting. The antihypertensive effects of continued dosing can be measured at subsequent visits, approximately 12 hours after a dose, to determine whether further titration is necessary. Patients with severe hypertension may require from 1200 mg to 2400 mg per day, with or without thiazide diuretics. Should side effects (principally nausea or dizziness) occur with these doses administered b.i.d.(twice daily), the same total daily dose administered t.i.d. (three times daily) may improve tolerability and facilitate further titration. Titration increments should not exceed 200 mg b.i.d. (twice daily). When a diuretic is added, an additive antihypertensive effect can be expected. In some cases this may necessitate a labetalol hydrochloride tablet dosage adjustment. As with most antihypertensive drugs, optimal dosages of labetalol hydrochloride tablets are usually lower in patients also receiving a diuretic.

Warnings & precautions

Sourced from openFDA

Hepatic Injury Severe hepatocellular injury, confirmed by rechallenge in at least one case, occurs rarely with labetalol therapy. The hepatic injury is usually reversible, but hepatic necrosis and death have been reported. Injury has occurred after both short- and long-term treatment and may be slowly progressive despite minimal symptomatology. Similar hepatic events have been reported with a related research compound, dilevalol HCl, including two deaths. Dilevalol HCl is one of the four isomers of labetalol hydrochloride. Thus, for patients taking labetalol, periodic determination of suitable hepatic laboratory tests would be appropriate. Appropriate laboratory testing should be done at the first symptom or sign of liver dysfunction (e.g., pruritus, dark urine, persistent anorexia, jaundice, right upper quadrant tenderness, or unexplained "flu-like" symptoms). If the patient has laboratory evidence of liver injury or jaundice, labetalol should be stopped and not restarted. Cardiac Failure Sympathetic stimulation is a vital component supporting circulatory function in congestive heart failure. Beta-blockade carries a potential hazard of further depressing myocardial contractility and precipitating more severe failure. Although beta-blockers should be avoided in overt congestive heart failure, if necessary, labetalol hydrochloride can be used with caution in patients with a history of heart failure who are well compensated. Congestive heart failure has been observed in patients receiving labetalol hydrochloride.

Adverse reactions

Sourced from openFDA

Most adverse effects are mild and transient and occur early in the course of treatment. In controlled clinical trials of 3 to 4 months' duration, discontinuation of labetalol hydrochloride due to one or more adverse effects was required in 7% of all patients. In these same trials, other agents with solely beta-blocking activity used in the control groups led to discontinuation in 8% to 10% of patients, and a centrally acting alpha-agonist led to discontinuation in 30% of patients. The incidence rates of adverse reactions listed in the following table were derived from multicenter, controlled clinical trials comparing labetalol hydrochloride, placebo, metoprolol, and propranolol over treatment periods of 3 and 4 months. Where the frequency of adverse effects for labetalol hydrochloride and placebo is similar, causal relationship is uncertain. The rates are based on adverse reactions considered probably drug related by the investigator. If all reports are considered, the rates are somewhat higher (e.g., dizziness, 20%; nausea, 14%; fatigue, 11%), but the overall conclusions are unchanged.

Overdosage

Sourced from openFDA

Overdosage with labetalol hydrochloride causes excessive hypotension that is posture sensitive and, sometimes, excessive bradycardia. Patients should be placed supine and their legs raised, if necessary, to improve the blood supply to the brain. If overdosage with labetalol hydrochloride follows oral ingestion, gastric lavage or pharmacologically induced emesis (using syrup of ipecac) may be useful for removal of the drug shortly after ingestion. The following additional measures should be employed if necessary: Excessive bradycardia Administer atropine or epinephrine. Cardiac failure Administer a digitalis glycoside and a diuretic. Dopamine or dobutamine may also be useful. Hypotension Administer vasopressors, e.g., norepinephrine. There is pharmacologic evidence that norepinephrine may be the drug of choice. Bronchospasm Administer epinephrine and/or an aerosolized beta 2 -agonist. Seizures Administer diazepam.

Approval history

Sourced from openFDA
  • Aug 3, 1998ANDAANDA074787Heritage Pharma
  • Aug 3, 1998ANDAANDA075133Watson Labs
  • May 28, 1999ANDAANDA075303Hikma
  • Jul 29, 1999ANDAANDA075215Andas 5 Holding
  • Nov 29, 1999ANDAANDA075239Hospira
  • Nov 29, 1999ANDAANDA075240Hospira
  • Jul 5, 2002ANDAANDA076051Baxter Hlthcare Corp
  • Nov 9, 2020NDANDA213330Hikma

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
12,986 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective1,0077.8%
  2. 2Maternal Exposure During Pregnancy9417.2%
  3. 3Foetal Exposure During Pregnancy9367.2%
  4. 4Hypertension7315.6%
  5. 5Premature Baby7185.5%
  6. 6Off Label Use6765.2%
  7. 7Chronic Kidney Disease6455.0%
  8. 8Exposure During Pregnancy6344.9%
  9. 9Acute Kidney Injury6284.8%
  10. 10Fatigue5954.6%
  11. 11Renal Failure5774.4%
  12. 12Nausea5254.0%
  13. 13Premature Delivery4963.8%
  14. 14Headache4943.8%
  15. 15Dyspnoea4893.8%

Literature

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Recent PubMed references pinned to Labetalol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 94 ClinicalTrials.gov registrations naming Labetalol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Labetalol. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Labetalol work?
Mechanism-of-action classes: Adrenergic alpha1-Antagonists; Adrenergic beta-Antagonists; Adrenergic beta1-Antagonists; Adrenergic beta2-Antagonists.
What is Labetalol used for?
According to FDA labeling, Labetalol carries indications including: Labetalol hydrochloride tablets USP are indicated in the management of hypertension. Labetalol hydrochloride tablets USP may be used alone or in combination with other antihypertensive agents, especially thiazide and loop diuretics.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Labetalol?
Labetalol is classified as Alpha and beta blocking agents, beta-Adrenergic Blocker, Adrenergic alpha1-Antagonists, Adrenergic beta-Antagonists, Adrenergic beta1-Antagonists, Adrenergic beta2-Antagonists, Arterial Vasodilation, Decreased Blood Pressure, Negative Chronotropy, Negative Inotropy.
What are the brand names for Labetalol?
Labetalol is marketed under brand names including Trandate.
What are the contraindications for Labetalol?
Labetalol labeling lists contraindications including: Labetalol hydrochloride is contraindicated in bronchial asthma, overt cardiac failure, greater-than-first-degree heart block, cardiogenic shock, severe bradycardia, other conditions associated with severe and prolonged hypotension, and in patients with a history of hypersensitivity to any component of the product [see Warnings] . Beta-blockers, even those with apparent cardioselectivity, should not be used in patients with a history of obstructive airway disease, including asthma.. Always consult the full prescribing information and a clinician.
Note. Data for labetalol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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