indacaterol, inhaled/glycopyrrolate inhaled (Rx)

Brand and Other Names:Utibron Neohaler
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

indacaterol/glycopyrrolate

inhalation powder

  • (27.5mcg/15.6mcg)/capsule

Chronic Obstructive Pulmonary Disease (COPD)

Combination inhalant containing long-acting muscarinic antagonist (LAMA) plus a long-acting beta2-agonist (LABA) indicated for the long-term, maintenance treatment of airflow obstruction in patients with COPD, including chronic bronchitis and/or emphysema

Orally inhale contents of 1 capsule PO q12hr using the Neohaler device

Dosage Modifications

No dosage adjustment is required for geriatric patients, patients with mild and moderate hepatic impairment, or patients with mild-to-moderate renal impairment

Severe renal or hepatic impairment: Not studied

Dosing Considerations

Limitations of use: Not indicated for the relief of acute bronchospasm or for the treatment of asthma

Safety and efficacy not established

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Interactions

Interaction Checker

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            Adverse Effects

            1-10%

            Nasopharyngitis (4.1%)

            Hypertension (2%)

            Back pain (1.8%)

            Oropharyngeal pain (1.6%)

            Postmarketing Reports

            Angioedema

            Dysphonia

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            Warnings

            Black Box Warnings

            Long-acting beta2-adrenergic agonists (LABAs) increase the risk of asthma-related death

            Data from a large placebo-controlled US study that compared the safety of another LABA (salmeterol) or placebo added to usual asthma therapy showed an increase in asthma-related deaths in patients receiving salmeterol

            This finding with salmeterol is considered a class effect of all LABAs, including indacaterol

            Safety and efficacy of indacaterol/glycopyrrolate in patients with asthma have not been established

            Not indicated for the treatment of asthma

            Contraindications

            Hypersensitivity

            All LABAs are contraindicated in patients with asthma without use of an inhaled corticosteroid; indacaterol/glycopyrrolate is not indicated for the treatment of asthma

            Cautions

            Safety and efficacy in patients with asthma not established; not indicated for asthma; monotherapy [without inhaled corticosteroids (ICS)] for asthma is associated with an increased risk of asthma-related death (see Black Box Warnings)

            Available data do not suggest an increased risk of death with use of LABA in patients with COPD

            Should not be initiated in patients with acutely deteriorating or potentially life-threatening episodes of COPD; also do not use for the relief of acute symptoms (ie, as rescue therapy) for treating acute episodes of bronchospasm

            Do not use more often than recommended, at higher doses than recommended, or in conjunction with other medications containing LABAs, as an overdose may result

            Can produce paradoxical bronchospasm that may be life-threatening Immediate hypersensitivity reactions have been reported after administration of indacaterol or glycopyrrolate

            LABAs can produce clinically significant cardiovascular effects, including increases in pulse rate or systolic or diastolic blood pressure

            Caution with convulsive disorders, thyrotoxicosis, patients who are unusually responsive to sympathomimetic amines, narrow-angle glaucoma (may worsen), or urinary retention (eg, prostatic hyperplasia, bladder-neck obstruction); instruct patients to contact their physician immediately with worsening disease symptoms

            Doses of the related beta2-agonist albuterol, when administered IV, have been reported to aggravate preexisting diabetes mellitus and ketoacidosis

            LABAs may produce significant hypokalemia, which has the potential to produce adverse cardiovascular effect; in patients with severe COPD, hypokalemia may be potentiated by hypoxia and concomitant treatment, which may increase the susceptibility for cardiac arrhythmias

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            Pregnancy

            Pregnancy

            There are no adequate and well-controlled studies in humans with Utibron Neohaler or its individual components

            Animal studies have not shown teratogenicity

            Lactation

            Unknown if distributed in human breast milk

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the 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

            Glycopyrronium: Long-acting muscarinic antagonist (LAMA); often referred to as an anticholinergic; produces bronchodilation by inhibiting acetylcholine’s effect on muscarinic receptors in the airway smooth muscle

            Indacaterol: Long-acting beta2-agonist (LABA); stimulates intracellular adenyl cyclase, causing conversion of ATP to cyclic AMP; increased cyclic AMP levels cause relaxation of bronchial smooth muscle

            Absorption

            Absolute bioavailability: 43-45% (indacaterol)

            Peak plasma time: 5 minutes (glycopyrrolate); 15 minutes (indacaterol)

            Distribution

            Protein bound: 38-41% (glycopyrrolate); ~95% (indacaterol)

            Vd: 83-376 L (glycopyrrolate); 2361-2557 L (indacaterol)

            Metabolism

            Indacaterol

            • Metabolized by UGT1A to the phenolic O-glucuronide
            • Also undergoes hydroxylation (predominantly by CYP3A4)

            Glycopyrrolate

            • Hydroxylation of results in a variety of mono-and bishydroxylated metabolites and direct hydrolysis results in the formation of a carboxylic acid derivative (M9)
            • M9 is hydrolyzed by multiple CYP isoenzymes

            Elimination

            Half-life: 40-56 hr (indacaterol oral); 33-53 hr (glycopyrrolate inhaled)

            Renal clearance: 0.46-1.2 L/hr (indacaterol)

            Systemic clearance: 18.8-23.3 L/hr (indacaterol)

            Excretion

            • Indacaterol: 54% (unchanged) and 23% (metabolites) in feces
            • Glycopyrrolate: 60-70% urine; 30-40% nonrenal (mostly by metabolism; also biliary)

            Pharmacogenomics

            Indacaterol

            • The pharmacokinetics of indacaterol were prospectively investigated in subjects with the UGT1A1 (TA)7/(TA)7 genotype (low UGT1A1 expression; also referred to as *28) and the (TA)6, (TA)6 genotype
            • Steady-state AUC and Cmax were 1.2-fold higher in the [(TA)7, (TA)7] genotype, suggesting no relevant effect of UGT1A1 genotype of indacaterol exposure
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            Administration

            Instructions

            For oral inhalation only

            Do not swallow the capsules, as the intended effects on the lungs will not be obtained

            Capsules should only be used with the Neohaler device

            Should be administered at the same time of the day, (1 capsule in the morning and 1 capsule in the evening), every day

            More frequent administration or a greater number of inhalations (>1 capsule BID) is not recommended

            Storage

            Store in a dry place at controlled room temperature (77°F [25°C]); excursions permitted to 59-86°F (15-30°C)

            Store capsules in the blister package that they are packaged in, and only remove immediately before use with the Neohaler device

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            Formulary

            FormularyPatient Discounts

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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.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.