montelukast (Rx)

Brand and Other Names:Singulair
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 10mg

tablet, chewable

  • 4mg
  • 5mg

oral granules

  • 4mg/packet

Asthma

Indicated for prophylaxis and chronic treatment of asthma

10 mg (single 10-mg tablet) PO qPM

Exercise-Induced Bronchospasm

Indicated for prevention of exercise-induced bronchoconstriction (EIB)

10 mg PO 2 hr before exercise; do not take additional dose within 24 hours

If taking montelukast for another indication, do not take additional dose to prevent exercise-induced bronchospasm (EIB)

Allergic or Perennial Rhinitis

Indicated for symptomatic relief of seasonal or perennial allergic rhinitis

10 mg (single 10-mg tablet) PO qDay

Dosage Modifications

Renal impairment

  • Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast were not evaluated
  • No dosage adjustment recommended in patients with renal insufficiency

Hepatic impairment

  • Mild-to-moderate: No dosage adjustment necessary
  • Severe: Not evaluated

Dosage Forms & Strengths

tablet

  • 10mg

tablet, chewable

  • 4mg
  • 5mg

oral granules

  • 4mg/packet

Asthma

Prophylaxis and maintenance treatment in patients aged ≥12 months

<12 months: Safety and efficacy not established

12-24 months: 4 mg (granules) PO once daily in evening

2-6 years: 4 mg (chewable tablet or granules) PO once daily in evening

6-15 years: 5 mg (chewable tablet) PO once daily in evening

>15 years: 10 mg (conventional tablet) PO once daily in evening

Exercise-Induced Bronchospasm

Prophylaxis

6-15 years: 5 mg (chewable tablet) PO 2 hours before exercise; do not take additional dose within 24 hours

>15 years: 10 mg PO 2 hours before exercise; do not take additional dose within 24 hours

If taking drug for another indication, do not take additional dose to prevent EIB

Perennial Allergic Rhinitis

<6 months: Safety and efficacy not established

6-24 months: 4 mg (granules) PO once daily

2-6 years: 4 mg (chewable tablet or granules) PO once daily

6-15 years: 5 mg (chewable tablet) PO once daily

>15 years: 10 mg (conventional tablet) PO once daily

Seasonal Allergic Rhinitis

<2 years: Safety and efficacy not established

2-6 years: 5 mg (chewable tablet) or 4 mg (granules) PO once daily

6-15 years: 5 mg (chewable tablet) PO once daily

>15 years: 10 mg (conventional tablet) PO once daily

Dosage Modifications

Renal impairment

  • Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast were not evaluated
  • No dosage adjustment recommended in patients with renal insufficiency

Hepatic impairment

  • Mild-to-moderate: No dosage adjustment necessary
  • Severe: Not evaluated
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Interactions

Interaction Checker

and montelukast

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Some adverse drug reactions vary by age group

            >10%

            Headache (18.4%; similar to placebo)

            1-10%

            Abdominal pain (≥2%)

            Eczema (≥2%)

            Influenza (≥2%)

            Laryngitis (≥2%)

            Pharyngitis (≥2%)

            Viral infection (≥2%)

            Wheezing (≥2%)

            Dental pain (2%)

            Dizziness (2%)

            Dyspepsia (2%)

            Elevated liver function tests (2%)

            Fever (2%)

            Gastroenteritis (2%)

            Nasal congestion (2%)

            Otitis (2%)

            Rash (2%)

            Urticaria (2%)

            Bronchitis (≥1%)

            Cough (≥1%)

            Sinusitis (≥1%)

            Upper respiratory tract infection (≥1%)

            <1%

            Allergic granulomatous angiitis (Churg-Strauss syndrome; rare)

            Cholestatic hepatitis (rare)

            Aggressive behavior, altered behavior, suicidal thoughts

            Postmarketing Reports

            Hematologic: Increased bleeding tendency, thrombocytopenia

            Immunologic: Hypersensitivity reactions (eg, anaphylaxis, hepatic eosinophilic infiltration)

            Psychiatric: Agitation, including aggressive behavior or hostility, anxiousness, depression, disorientation, dream abnormalities, hallucinations, insomnia, tic, irritability, restlessness, somnambulism, suicidal thinking and behavior (including suicide), tremor, obsessive compulsive disorders

            Neurologic: Drowsiness, paresthesia or hypesthesia, seizures, dysphemia (stuttering)

            Cardiac: Palpitations

            Respiratory, thoracic, mediastinal: Epistaxis, pulmonary eosinophilia

            Gastrointestinal: Diarrhea, dyspepsia, nausea, pancreatitis, vomiting

            Hepatobiliary: Cases of cholestatic hepatitis, hepatocellular liver injury, and mixed-pattern liver injury have been reported, mostly occurring in combination with other confounding factors (eg, use of other medications, administration to patients who had underlying potential for liver disease [eg, alcohol use or other forms of hepatitis])

            Dermatologic: Angioedema, bruising, erythema multiforme, erythema nodosum, pruritus, urticaria

            Musculoskeletal: Arthralgia, myalgia (including muscle cramps)

            General: Edema

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            Warnings

            Black Box Warnings

            FDA announcement March 4, 2020

            • Serious neuropsychiatric events that may include suicidal thoughts or actions have been reported in patients taking montelukast
            • Only use montelukast for allergic rhinitis in patients who have an inadequate response or intolerance to alternative therapies
            • Consider risks and benefits when prescribing or continuing treatment
            • Advise all patients of the risk of neuropsychiatric events when prescribing
            • Discontinue and contact a health care professional immediately if changes in behavior or new neuropsychiatric symptoms, suicidal thoughts, or behavior occur
            • Monitor for neuropsychiatric symptoms
            • Events have occurred in patients with and without pre-existing psychiatric disease

            Contraindications

            Hypersensitivity

            Cautions

            Not to be given for acute asthma attacks, including status asthmaticus

            Advise patients to have appropriate rescue medication available

            Inhaled corticosteroid may be reduced gradually; do not abruptly substitute montelukast for inhaled or oral corticosteroids

            Patients with known aspirin sensitivity should continue to avoid aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) while taking montelukast; not to be given for treatment of bronchoconstriction resulting from aspirin or NSAID intake

            Neuropsychiatric events reported, including agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, hallucinations, insomnia, irritability, memory impairment, restlessness, somnambulism, suicidal thinking and behavior (including suicide), tic, and tremor; prescribers should carefully evaluate the risks and benefits of continuing treatment if such events occur

            Systemic eosinophilia reported, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome; these events are usually (but not always) associated with tapering of PO corticosteroid therapy

            Use with caution in phenylketonuria; 4-mg and 5-mg chewable tablets contain phenylalanine

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            Pregnancy & Lactation

            Pregnancy

            Available data from published prospective and retrospective cohort studies over decades in pregnant women have not established a drug-associated risk of major birth defects

            Animal data

            • In animal reproduction studies, no adverse developmental effects were observed with oral administration to pregnant rats and rabbits during organogenesis at doses approximately 100 and 110 times, respectively, the maximum recommended human daily oral dose (MRHDOD) based on AUCs
            • Poorly or moderately controlled asthma in pregnancy increases maternal risk of perinatal adverse outcomes such as preeclampsia and infant prematurity, low birth weight, and small for gestational age

            Lactation

            A published clinical lactation study reports presence of montelukast in human milk; data available on effects of drug on infants, either directly or through breast milk, do not suggest a significant risk of adverse events from exposure; effects of drug on milk production are unknown; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from treatment 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

            Blocks binding of leukotriene D4 to its receptor; alters pathophysiology associated with inflammatory process that contributes to signs and symptoms of asthma

            Absorption

            Bioavailability: 64% (mean)

            Peak plasma time: Tablet, 3-4 hr; chewable tablet, 2-2.5 hr; granules, 1-3 hr

            Distribution

            Protein bound: >99%

            Vd: 8-11 L

            Metabolism

            Metabolized by CYP3A4 and CYP2C9

            Elimination

            Half-life: 2.7-5.5 hr

            Clearance: 45 mL/min

            Excretion: Feces (86%), urine (0.2%)

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            Administration

            Oral Administration

            Take with or without food

            Patients with both asthma and allergic rhinitis should take only 1 dose qPM

            Asthma or EIB: Administer in the evening

            Allergic rhinitis: Individualize administration time to suit patient’s needs

            Oral granules

            • Administer either directly in the mouth, dissolve in 1 teaspoonful (5 mL) of cold or room temperature baby formula or breast milk, or mix with a spoonful of cold or room temperature soft foods
            • Based on stability studies, only applesauce, carrots, rice, or ice cream should be used
            • Do not open packet until ready to use
            • After opening, the full dose (with or without mixing with baby formula, breast milk, or food) must be administered within 15 min
            • If mixed with baby formula, breast milk, or food, do not store oral granules for future use; discard any unused portion
            • Oral granules are not intended to be dissolved in any liquid other than baby formula or breast milk for administration; however, liquids may be taken subsequent to administration

            Storage

            All formulations: Store at 25ºC (77°ºF), excursions permitted to 15-30ºC (59-86ºF)

            Protect from moisture and light

            Store in original package

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            Formulary

            FormularyPatient Discounts

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
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            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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.