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labetalol (Rx)Brand and Other Names:Trandate

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 5mg/mL

tablet

  • 100mg
  • 200mg
  • 300mg
more...

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
more...

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

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Interactions

Interaction Checker

labetalol and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Dizziness (1-20%)

            Lightheadedness (1-20%)

            Nausea (≤19%)

            Tingling sensation of scalp (4-12%)

            Fatigue (1-11%)

            1-10%

            Elevated serum blood urea nitrogen (BUN) (≤8%)

            Elevated serum creatinine (8%)

            Congestion of nasal sinus (1-6%)

            Orthostatic hypotension (1-5%)

            Absence of ejaculation (<5%)

            Paresthesia (<5%)

            Elevated liver enzymes (4%)

            Diaphoresis (≤4%)

            Edema (≤2%)

            Bronchospasm (1-2%)

            Dyspnea (1-2%)

            Pruritus (1%)

            Rash (1%)

            Altered taste sense (1%)

            Ventricular arrhythmia (1%; IV)

            Frequency Not Defined

            Angioedema

            Bradycardia

            Alopecia

            Cholestatic jaundice

            Depression

            Diabetes insipidus

            Hepatitis

            Raynaud syndrome

            Toxic myopathy

            Urinary retention

            Urticaria

            Raynaud phenomenon

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            Warnings

            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)

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Small amounts excreted; use with caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Nonselective beta blocker with intrinsic sympathomimetic activity; also alpha blocker

            Absorption

            Bioavailability: 25% (PO)

            Onset: PO, 20-120 min; IV, 2.5 min

            Duration: 100 mg, 8 hr; 300 mg, 12 hr

            Peak plasma time: 1-2 hr (PO)

            Peak effect: 15 min (IV); 1-4 hr (PO)

            Distribution

            Protein bound: 50%

            Vd: 3-16 L/kg (adults)

            Metabolism

            Metabolized mainly through conjugation to glucuronide metabolites

            Elimination

            Half-life: 6-8 hr (PO); 5.5 hr (IV)

            Excretion: Urine (55-60%), feces via bile

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            Administration

            IV Compatibilities

            Solution: Compatible with most common solvents

            Y-site: Alcohol 10% in D5W, amikacin, aminophylline, amiodarone, ampicillin, bivalirudin, butorphanol, calcium gluconate, cefazolin, ceftazidime, ceftizoxime, chloramphenicol, cimetidine, clindamycin, dexmedetomidine, diltiazem, dobutamine, dopamine, enalaprilat, epinephrine, erythromycin, esmolol, famotidine, fenoldopam, fentanyl, gatifloxacin, gentamicin, heparin (incompatible at 5 mg/mL), hetastarch, hydromorphone, insulin (?), lidocaine, linezolid, lorazepam, magnesium sulfate, meperidine, metronidazole, midazolam, milrinone, morphine, nicardipine, nitroglycerin, norepinephrine, oxacillin, penicillin G, piperacillin, potassium chloride, potassium phosphates, propofol, ranitidine, sodium acetate, sodium nitroprusside, tobramycin, trimethoprim-sulfamethoxazole, vancomycin, vecuronium

            IV Incompatibilities

            Solution: Sodium bicarbonate 5%

            Y-site: Amphotericin B cholesteryl sulfate, cefoperazone, ceftriaxone, furosemide, nafcillin, thiopental, warfarin

            IV Preparation

            Standard diluent: 500 mg/250 mL D5W

            Minimum volume: 250 mL D5W

            IV Administration

            Requires infusion pump

            Slow direct IV push administered over 2 minutes

            Loading infusions (2 mg/min) require close monitoring of HR and BP and are terminated after response occurs or a cumulative dose of 300 mg is reached

            Continuous infusions of 2-6 mg/hr have been used in some settings and should not be confused with loading infusions

            Storage

            Store at room temperature or under refrigeration (2-30°C [36-86°F])

            Protect from light and freezing

            Solution is clear to slightly yellow

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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