Labetalol

Dosage Forms & Strengths

injectable solution

• 5mg/mL

tablet

• 100mg
• 200mg
• 300mg

Hypertension

100 mg PO q12hr initially; increased by 100 mg q12hr every 2-3 days

Usual dosage range: 200-400 mg PO q12hr; not to exceed 2400 mg/day

Hypertensive Emergency

20 mg IV over 2 minutes initially, then 40-80 mg IV q10min; total dose not to exceed 300 mg

Alternative: 1-2 mg/min by continuous IV infusion; total dose of 300 mg has been used

Dosing Modifications

Renal impairment: Not studied; no supplement needed after dialysis

Hepatic impairment: Not studied; dosage reduction may be necessary

Dosing Considerations

Monitor blood pressure every 5-10 minutes

Dosage Forms & Strengths

injectable solution

• 5mg/mL

tablet

• 100mg
• 200mg
• 300mg

Hypertensive Emergency

0.4-1 mg/kg/hr by continuous IV infusion; not to exceed 3 mg/kg/hr 

Hypertension (Off-label)

1-3 mg/kg/day PO divided q12hr; not to exceed 1200 mg/day  

Alternative: 0.3-1 mg/kg intermittent IV bolus

Contraindications

Asthma or obstructive airway disease, severe bradycardia, 2°/3° heart block (without pacemaker), cardiogenic shock, bronchial asthma, uncompensated cardiac failure, hypersensitivity, sinus bradycardia, sick sinus syndrome without permanent pacemaker; conditions associated with prolonged and severe hypotension

Cautions

Use with caution in anesthesia or surgery (myocardial depression), bronchospastic disease (not recommended), cerebrovascular insufficiency, diabetes mellitus, hyperthyroidism or thyrotoxicosis, hepatic impairment, renal impairment, peripheral vascular disease, compromised left ventricular function, advanced age, heart failure, pheochromocytoma

Increased risk of stroke after surgery

Severe hepatic injury reported with use; with prolonged use, monitor liver function tests

Sudden discontinuance can exacerbate angina and lead to myocardial infarction

Use with caution in patients taking calcium channel blockers, cardiac glycosides, or inhaled anesthetics

Intraoperative floppy iris syndrome observed during cataract surgery in some patients treated with alpha1 blockers (labetalol is both an alpha and a beta blocker)

Hypotension with or without syncope may occur; monitor

Consider pre-existing conditions, such as, sick sinus syndrome before initiating therapy

Use caution in patients with history of severe anaphylaxis to allergens; patients taking beta-blockers may become more sensitive to repeated challenges; treatment with epinephrine in patients taking beta-blockers may be ineffective or promote undesirable effects

Use with caution in patients with myasthenia gravis, psoriasis, or psychiatric illness (may cause or exacerbate CNS depression)

Trandate (labetalol) Tablets, 100 mg, light orange, round, scored, film-coated tablets engraved on one side with “TRANDATE (labetalol) 100,” bottles of 100 (NDC 65483-391-10) and 500 (NDC 65483-391-50) and unit dose packs of 100 tablets (NDC 65483-391-11).

Trandate (labetalol) Tablets, 200 mg, white, round, scored, film-coated tablets engraved on one side with “TRANDATE (labetalol) 200,” bottles of 100 (NDC 65483-392-10) and 500 (NDC 65483-392-50) and unit dose packs of 100 tablets (NDC 65483-392-22).

Trandate (labetalol) Tablets, 300 mg, mid-orange, round, scored, film-coated tablets engraved on one side with “TRANDATE (labetalol) 300,” bottles of 100 (NDC 65483-393-10) and 500 (NDC 65483-393-50) and unit dose packs of 100 tablets (NDC 65483-393-33).

Trandate (labetalol) Tablets should be stored between 2° and 30°C (36° and 86°F). Trandate (labetalol) Tablets in the unit dose boxes should be protected from excessive moisture.

Prometheus Laboratories Inc. Manufactured in Canada by WellSpring Pharmaceutical Canada Corp. Oakville, ON L6H 1M5 for Prometheus Laboratories Inc. San Diego, CA 92121. Revised: November 2010

Overdosage with labetalol HCl 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 HCl 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 beta2-agonist.

Seizures-administer diazepam.

In severe beta-blocker overdose resulting in hypotension and/or bradycardia, glucagon has been shown to be effective when administered in large doses (5 to 10 mg rapidly over 30 seconds, followed by continuous infusion of 5 mg per hour that can be reduced as the patient improves).

Neither hemodialysis nor peritoneal dialysis removes a significant amount of labetalol HCl from the general circulation ( < 1%).

The oral LD50 value of labetalol HCl in the mouse is approximately 600 mg/kg and in the rat is > 2 g/kg. The IV LD50 in these species is 50 to 60 mg/kg.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamines, and herbal supplements. Especially tell your doctor if you take:

• other medications for high blood pressure or heart disease
• cimetidine (Tagamet)
• nitroglycerin
• medications for asthma, headaches, allergies, colds, or pain
• vitamins

This is not a complete list of labetalol drug interactions. Ask your doctor or pharmacist for more information.

Do not stop taking labetalol without first talking to your doctor. Stopping suddenly may make your condition worse.

If you need surgery, tell the surgeon ahead of time that you are using labetalol. You may need to stop using the medicine for a short time.

Labetalol can affect your pupils during cataract surgery. Tell your eye surgeon ahead of time that you are using this medication. Do not stop using labetalol before surgery unless your surgeon tells you to.

Labetalol may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Labetalol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

You should not take labetalol if you are allergic to it, or if you have:

• asthma or chronic obstructive pulmonary disease (COPD;
• certain serious heart conditions such as"AV block" or slow heart rhythm; or
• conditions that cause very low blood pressure.

If you have any of these other conditions, you may need a labetalol dose adjustment or special tests:

• bronchitis, emphysema, sleep apnea, or other breathing problem;
• congestive heart failure;
• liver or kidney disease;
• diabetes; or
• pheochromocytoma (tumor of the adrenal gland).

FDA pregnancy category C. It is not known whether labetalol will harm an unborn baby. Labetalol may cause heart or lung problems in a newborn if the mother takes the medication during pregnancy. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Labetalol can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Your pharmacist can provide more information about labetalol.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Your blood pressure will need to be checked often, and you may need frequent medical tests at your doctor's office.

If you need surgery, tell the surgeon ahead of time that you are using labetalol.

Do not skip doses or stop taking labetalol without first talking to your doctor. Stopping suddenly may make your condition worse.

Labetalol can cause false results with certain lab tests of the urine. Tell any doctor who treats you that you are using labetalol.

Taking labetalol can make it harder for you to tell when your blood sugar is low. If you have diabetes, check your blood sugar regularly.

Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medicine for the rest of your life.

Store at room temperature away from moisture and heat.

Labetalol is only part of a complete program of treatment for hypertension that may also include diet, exercise, weight control, and other medications. Follow your diet, medication, and exercise routines very closely.

Take the missed dose as soon as you remember. Skip the missed dose if your next dose is less than 8 hours away. Do not take extra medicine to make up the missed dose.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

• Blurred vision or other changes in vision
• chills
• cold sweats
• confusion
• difficult or labored breathing
• dizziness, faintness, or lightheadedness when getting up from lying or sitting position
• shortness of breath
• swelling of face, fingers, feet, or lower legs
• tightness in chest
• wheezing

Get emergency help immediately if any of the following symptoms of overdose occur:

• Chest pain or discomfort
• lightheadedness, dizziness, or fainting
• slow or irregular heartbeat
• sweating
• unusual tiredness or weakness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Nausea

• Acid or sour stomach
• belching
• change in taste or bad, unusual, or unpleasant (after) taste
• decreased interest in sexual intercourse
• feeling of constant movement of self or surroundings
• headache
• heartburn
• inability to have or keep an erection
• indigestion
• lack or loss of strength
• loss in sexual ability, desire, drive, or performance
• not able to ejaculate semen
• rash
• sensation of spinning
• stomach discomfort, upset, or pain
• stuffy nose

• Burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
• diarrhea
• increased sweating
• vomiting

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Labetalol hydrochloride injection 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.

NDC 47781-586-29

Labetalol HCL Injection, USP

100 mg/20 mL

(5 mg/mL)

FOR INTRAVENOUS INJECTION ONLY 

Labetalol Hydrochloride 20 ml vial label

Blocks alpha-, beta1-, and beta2-adrenergic receptor sites; elevated renins are reduced. The ratios of alpha- to beta-blockade differ depending on the route of administration: 1:3 (oral) and 1:7 (IV).

Absorption

Complete

Distribution

Apparent Vd: Adults: 2.5 to 15.7 L/kg (Goa 1989)

Metabolism

Hepatic, primarily via glucuronide conjugation; extensive first-pass effect

Excretion

Urine (55% to 60% as glucuronide conjugates, <5% as unchanged drug [Goa 1989]); feces (12% to 27% as metabolites) (Goa 1989)

Elimination is reduced in elderly patients.

Hypertensive emergency in pregnancy

Based on the American College of Obstetricians and Gynecologists (ACOG) guidelines on the management of hypertension in pregnancy, the use of labetalol is effective and recommended as a treatment option in pregnant and postpartum patients who are experiencing acute onset, severe hypertension with preeclampsia or eclampsia [ACOG 2015].

Subarachnoid hemorrhage

Clinical guidelines recommend use of antihypertensives during the period between onset of SAH and surgical obliteration. Clinical study results and institutional experience are generally supportive of labetalol use in SAH. Nicardipine appears to have more beneficial outcomes than sodium nitroprusside and labetalol; however, only a small number of studies have compared the agents directly. Additional large-scale, multicenter, randomized controlled studies with more standardized interventions are needed to assess efficacy and safety of labetalol for SAH antihypertensive therapy.

Additional Off-Label Uses

Hypertension during acute ischemic stroke; Pediatric hypertension; Chronic hypertension in pregnancy

Note: Use care with labetalol continuous IV infusions; the rate of administration is different for pediatric patients (mg/kg/hour) versus adult patients (mg/minute).

Hypertension (off-label): Children and Adolescents: Limited data available:

Oral: Initial: 1 to 3 mg/kg/day, in 2 divided doses; maximum daily dose: 10 to 12 mg/kg/day, up to 1,200 mg/day (NHLBI 2011)

IV (intermittent bolus): 0.2 to 1 mg/kg/dose; maximum dose: 40 mg; use should be reserved for severe hypertension (NHBPEP 2004).

Hypertensive emergency: Infants, Children, and Adolescents: Continuous IV infusion: 0.25 to 3 mg/kg/hour; initiate at lower end of range and titrate up slowly (NHBPEP 2004). One retrospective study in infants and children ≤24 months of age observed reductions in blood pressure at doses up to 0.59 mg/kg/hour with little additional benefit at higher doses (Thomas 2011).

Parenteral: Continuous IV infusion: Further dilute in a compatible solution (eg, D5W, NS) to a concentration of 1 mg/mL; higher concentrations up to 3.75 mg/mL have been shown to be stable (Yuen 1983).

Applies to labetalol: compounding powder, intravenous solution, oral tablet

Cardiovascular

Common (1% to 10%): Edema, postural hypotension
Frequency not reported: Bradycardia, heart block, heart failure, hypotension, ankle edema, increase of an existing intermittent claudication, postural hypotension, cold or cyanotic extremities, Raynaud's phenomenon, paresthesia of the extremities, syncope[Ref]

Dermatologic

Uncommon (0.1% to 1%): Increased sweating
Frequency not reported: Systemic lupus erythematosus, rashes (e.g., generalized maculopapular, lichenoid, urticarial, bullous lichen planus, psoriaform, facial erythema, Peyronie's disease, reversible alopecia)[Ref]

Endocrine

Frequency not reported: Masking of the normal response to hypoglycemia (sweating and tachycardia); this may be important in some patients with diabetes mellitus[Ref]

Gastrointestinal

Common (1% to 10%): Nausea, dyspepsia, vomiting
Uncommon (0.1% to 1%): Diarrhea
Frequency not reported: Epigastric pain[Ref]

Genitourinary

Common (1% to 10%): Ejaculation failure, impotence
Frequency not reported: Difficulty in micturition (including acute urinary bladder retention)[Ref]

Hepatic

Common (1% to 10%): Transient elevations of liver function tests
Frequency not reported: Hepatic necrosis, hepatitis, cholestatic jaundice[Ref]

Hypersensitivity

Rare (less than 0.1%): Hypersensitivity (e.g., rash, urticaria, pruritus, angioedema, dyspnea), anaphylactoid reactions[Ref]

Immunologic

Frequency not reported: Antimitochondrial antibodies[Ref]

Metabolic

Very rare (less than 0.01%): Hyperkalemia[Ref]

Musculoskeletal

Frequency not reported: Muscle cramps, toxic myopathy[Ref]

Nervous system

Very common (10% or more): Dizziness (11%)
Common (1% to 10%): Headache, taste distortion, vertigo, paresthesia, scalp tingling
Uncommon (0.1% to 1%): Drowsiness
Frequency not reported: Tremor[Ref]

Ocular

Common (1% to 10%): Vision abnormality
Frequency not reported: Dry eyes
Postmarketing reports: Intraoperative Floppy Iris Syndrome (IFIS) observed during cataract surgery[Ref]

Respiratory

Common (1% to 10%): Nasal stuffiness, dyspnea
Frequency not reported: Bronchospasm, interstitial lung disease[Ref]

Other

Common (1% to 10%): Fatigue, asthenia
Frequency not reported: Positive antinuclear factor[Ref]

Psychiatric

Frequency not reported: Depressed mood and lethargy, hallucinations, psychoses, confusion, sleep disturbances, nightmares[Ref]

Some side effects of labetalol may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Data not available

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Dizziness, nausea, fatigue, tingling of the scalp or skin, and fluid retention are the most commonly reported side effects.
• Labetalol lowers blood pressure more when standing than when sitting or lying down. This may cause postural hypotension (a noticeable drop in blood pressure when going from a sitting to a standing position). Symptoms may include dizziness.
• Labetalol is also not suitable for people with certain heart conditions including cardiac failure, slow heartbeat (bradycardia), peripheral circulatory disorders (conditions that cause reduced blood flow to the hands or feet), and severe low blood pressure.
• Sudden discontinuation of labetalol has been associated with an exacerbation of angina, and occasionally heart attacks and arrhythmias. Dosage needs to be tapered off slowly.
• Labetalol can cause narrowing of the airways (bronchoconstriction) in people with asthma or other respiratory disease. Avoid.
• Elderly people may be more sensitive to the effects of labetalol. Generally, lower maintenance dosages are needed.
• Rarely, may cause potentially fatal liver damage.
• Can mask symptoms of hypoglycemia (such as a fast heartbeat), so should be used with caution in people with diabetes. Insulin dosages may also need adjusting.
• May cause an intraoperative floppy iris syndrome during cataract surgery.
• May interact with some medications including other medications used for the treatment of arrhythmias or angina.
• May interfere with some lab tests including amphetamine tests.

Notes: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. For a complete list of all side effects, click here.

Labetalol works on both alpha and beta receptors in the heart to lower blood pressure. Heart rate is only mildly affected, but dizziness may be reported when going from a sitting or lying down position to standing.