levalbuterol (Rx)

Brand and Other Names:Xopenex, Xopenex HFA
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

nebulizer solution

  • 0.31mg/3mL
  • 0.63mg/3mL
  • 1.25mg/3mL
  • 1.25mg/0.5mL

aerosol

  • 45mcg/actuation

Bronchospasm

Nebulizer solution: 0.63 mg 3 times daily at intervals of 6-8 hr; may increase dose to 1.25 mg 3 times daily with close monitoring for adverse effects

Aerosol: 90 mcg (2 actuations of metered-dose inhaler) q4-6hr; 1 actuation q4hr may be sufficient; not to exceed 2 actuations q4hr

Dosage Modifications

Hepatic impairment: Not evaluated

Renal impairment: Caution when administering high doses of inhalation solution

Dosage Forms & Strengths

nebulizer solution

  • 0.31mg/3mL
  • 0.63mg/3mL
  • 1.25mg/3mL
  • 1.25mg/0.5mL

aerosol

  • 45mcg/actuation

Bronchospasm

Indicated for treatment or prevention of bronchospasm in adults, adolescents, and children ≥6 years (nebulized solution) or >4 years (HFA aerosol) with reversible obstructive airway disease

Nebulizer solution

  • <6 years: Not indicated; clinical trials with levalbuterol inhalation in this age group failed to meet the primary efficacy endpoint
  • ≥6 to <12 years: 0.31 mg q8hr; not to exceed 0.63 mg q8hr PRN
  • >12 years: 0.63 mg 3 times daily at intervals of 6-8 hr; may increase dose to 1.25 mg 3 times daily with close monitoring for adverse effects

Aerosol

  • <4 years: Safety and efficacy not established
  • ≥4 years: 90 mcg (2 actuations of metered-dose inhaler) q4-6hr PRN; in some patients, 1 inhalation (45 mg of levalbuterol free base) q4hr may be sufficient

Dosage Modifications

Hepatic impairment: Not evaluated

Renal impairment: Caution when administering high doses of inhalation solution

Nebulizer solution: 0.63 mg initially in patients >65 years

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Interactions

Interaction Checker

and levalbuterol

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (8-12%)

            Viral infection (7-12%)

            Rhinitis (3-11%)

            1-10%

            Pharyngitis (3-10%)

            Tremor (7%)

            Sinusitis (1-4%)

            Flu (1-4%)

            Dyspepsia (1-3%)

            Leg cramps (<3%)

            Generalized pain (2.8%)

            Nasal edema (2.8%)

            Nervousness (2.8%)

            Tachycardia (2.8%)

            Postmarketing Reports

            Dysphonia

            Gastroesophageal reflux disease, nausea

            Angioedema, anaphylaxis, rash, urticaria

            Chest pain, tachycardia, arrhythmias (including atrial fibrillation, supraventricular tachycardia, extrasystoles)

            Asthma, increased cough, dyspnea, dysphonia

            Metabolic acidosis

            Nervousness, tremor

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            Warnings

            Contraindications

            Hypersensitivity to levalbuterol or racemic albuterol

            Cautions

            Risk of paradoxical bronchospasm; this should be distinguished from inadequate response; discontinue and treat with alternate therapy if it occurs

            Has higher affinity for beta1- and beta2-adrenergic receptors than racemic albuterol has

            Risk of hypersensitivity reactions

            Use caution in hyperthyroidism; may increase thyroid activity

            Use with caution in diabetes mellitus (beta2 agonists may increase glucose)

            Risk of hypokalemia (usually transient); use with caution in hypokalemia

            Use with caution in patients with history of seizure disorders; therapy may increase CNS activity/excitation

            Exceeding the recommended dose may result in serious adverse effects, including fatalities

            Cardiovascular effects

            • Use with caution in cardiovascular disorder (eg, arrhythmias, hypertension, coronary insufficiency)
            • May cause elevation in blood pressure and heart rate; may cause CNS stimulation or excitation
            • May increase risk of arrhythmia and electrocardiogram changes, including ST segment depression, prolongation of the QTc interval, or flattening of the T wave

            Drug interaction overview

            • Short-acting bronchodilators
              • Avoid use
              • If additional adrenergic drugs are to be administered by any route, use with caution to avoid deleterious additive cardiovascular effects
            • Beta-blockers
              • Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-adrenergic agonists, but may produce severe bronchospasm in asthmatic patients.
              • Therefore, patients with asthma should not normally be treated with beta-blockers.
              • Under certain circumstances, cardioselective beta-blockers should be considered and may be used with caution
            • Diuretics
              • ECG changes or hypokalemia that may result from the administration of non-potassium-sparing diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded
            • Digoxin
              • Mean decreases of 16% and 22% in serum digoxin levels were demonstrated after single-dose IV and oral administration of racemic albuterol, respectively, to normal volunteers who had received digoxin for 10 days
            • Monoamine oxidase inhibitors or tricyclic antidepressants
              • Use extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, because the action of levalbuterol on the vascular system may be potentiated
              • Consider alternative therapy in patients taking MAO inhibitors or tricyclic antidepressants
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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies in pregnant women; there are clinical considerations with use in pregnant women

            Pregnancy exposure registry

            • Monitors pregnancy outcomes in women exposed to asthma medication during pregnancy
            • To enroll in MotherToBaby Pregnancy Studies’ Asthma & Pregnancy Study or for more information about the registry, call 1-877-311-8972 or visit www.mothertobaby.org/ongoing-study/asthma

            Clinical considerations

            • In women with poorly or moderately controlled asthma, there is increased risk of preeclampsia in mother and prematurity, low birth weight, and small for gestational age in neonate
            • Closely monitor and adjust medication as necessary to maintain optimal control

            Lactation

            There are no available data on presence of levalbuterol in human milk, effects on breastfed child, or effects on milk production

            Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition

            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

            Beta2-receptor agonist with some beta1 activity; relaxes bronchial smooth muscle

            Absorption

            Peak plasma concentration

            • Single levalbuterol 1.25 mg solution: 1.1 ng/mL ([R]-albuterol)
            • Cumulative levalbuterol 5 mg solution: 4.5 ng/mL ([R]-albuterol)
            • Levalbuterol inhaler 90 mcg: 199 pg/mL

            Peak plasma time

            • Single levalbuterol 1.25 mg solution: 0.2 hr ([R]-albuterol)
            • Cumulative levalbuterol 5 mg solution: 0.2 hr ([R]-albuterol)

            AUC

            • Single levalbuterol 1.25 mg: 3.3 ng⋅hr/mL ([R]-albuterol)
            • Cumulative levalbuterol 5 mg: 17.4 ng⋅hr/mL ([R]-albuterol)
            • Levalbuterol inhaler 90 mcg: 695 ng⋅hr/mL

            Metabolism

            Published literature suggests that the primary enzyme responsible for the metabolism of albuterol enantiomers in humans is SULT1A3 (sulfotransferase)

            Elimination

            Primary route of elimination of albuterol enantiomers is through renal excretion (80% to 100%) of either the parent compound or the primary metabolite

            Excretion: Feces (< 20%)

            Following IV administration of racemic albuterol, between 25% and 46% of the (R)-albuterol fraction of the dose was excreted as unchanged (R)-albuterol in the urine

            Half-time

            • Single levalbuterol 1.25 mg: 3.3 hr ([R]-albuterol)
            • Cumulative levalbuterol 5 mg: 4 hr
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            Administration

            Oral Inhalation Preparation

            Aerosol inhaler

            • Priming
              • Prime inhaler before using for the first time and when inhaler has not been used for more than 3 days by releasing 4 test sprays into the air, away from the face
            • Cleaning
              • Wash the actuator with warm water and air-dry thoroughly at least once a week; may cease to deliver levalbuterol tartrate if not properly cleaned and dried thoroughly
              • Keep plastic actuator clean to prevent medication build-up and blockage
              • If actuator becomes blocked with levalbuterol tartrate, wash actuator to remove the blockage
              • The canister is fitted with a dose indicator, which indicates how many inhalations remain
              • When nearing the end of the usable inhalations, the color behind the number in the dose indicator window changes to red
              • Discard inhaler when dose indicator displays zero, corresponding to the use of 200 actuations

            Oral Inhalation Administration

            Oral inhalation only

            Aerosol inhaler

            • Shake well before use
            • Avoid spraying in the eyes
            • Check inside the mouthpiece of the actuator for objects
            • Shake the inhaler well for 5 seconds before use
            • Breathe out through mouth and push out as much air from lungs as possible
            • While breathing in deeply and slowly, press down on the center of the targeting rings until a spray of medicine has been released
            • Close your mouth and hold your breath for 10 seconds if possible; then breathe out gently
            • Wait about 1 min before next dose

            Nebulizer solution

            • Administer by nebulization using with a standard jet nebulizer (with a face mask or mouthpiece) connected to an air compressor
            • Drug compatibility (physical and chemical), efficacy, and safety of nebulizer solution when mixed with other drugs in a nebulizer have not been established
            • Safety and efficacy of nebulizer solution have been established in clinical trials when administered using the PARI LC Jet and PARI LC Plus nebulizers, and the PARI Master® Dura-Neb® 2000 and Dura-Neb® 3000 compressors

            Storage

            Aerosol inhaler

            • Store canister at 20-25ºC (68-77ºF)
            • Protect from freezing temperatures and direct sunlight
            • Do not use or store inhaler near heat or open flame; do not throw into a fire or an incinerator
            • Temperatures >120ºF may cause the canister to burst

            Nebulizer solution

            • Store in the protective foil pouch at 20-25ºC (68-77ºF)
            • Protect from light and excessive heat
            • Once foil pouch is opened, contents of the vial should be used immediately; discard any vial if the solution is not colorless
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            Formulary

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            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.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.