Indacaterol


Concise Prescribing Info
Indications/Uses
Maintenance therapy in chronic obstructive pulmonary disease.
Dosage/Direction for Use
Adult : Inhalation As inhalation cap: 1 cap (150 mcg) once daily via inhaler device, at the same time each day. Severe: 300 mcg once daily. Max: 300 mcg/day.
Dosage Details
Inhalation/Respiratory
Chronic obstructive pulmonary disease
Adult: Maintenance: As inhalation cap: 1 cap (150 mcg) once daily via inhaler device, at the same time each day. Severe: 300 mcg once daily. Max: 300 mcg daily.
Special Patient Group
Pharmacogenomics:

Indacaterol is metabolised by uridine diphosphate glucuronosyltransferase 1 family, polypeptide A1 (UGT1A1) enzyme via glucuronidation into phenolic O-glucuronide metabolite.

According to FDA-approved drug label, patients with UGT1A1 (TA)7/(TA)7 (*28/*28) low expression genotype have 1.2-fold higher steady-state AUC and Cmax than in patients with (TA)6/(TA)6 (*1/*1) genotype. This suggests that UGT1A1 genotype has no significant effect in the exposure of indacaterol.
Contraindications
As monotherapy in the treatment of asthma. Concomitant use with other long-acting ß2-adrenergic agonists.
Special Precautions
Patient with CV disorders (e.g. coronary artery disease, acute MI, cardiac arrhythmias, hypertension, known or suspected QT interval prolongation); convulsive disorders, hyperthyroidism, diabetes mellitus, hypokalaemia. Pregnancy and lactation. Not indicated for the relief of acute bronchospasm.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. swelling of tongue, lips and face, rash, urticaria, difficulty in breathing or swallowing), hypokalaemia, hyperglycaemia, new-onset or exacerbation of diabetes mellitus, increased pulse rate or blood pressure, ECG changes (e.g. flattening of T wave, QT interval prolongation, ST-segment depression).
Cardiac disorders: Chest pain, palpitations, tachycardia.
Metabolism and nutrition disorders: Peripheral oedema.
Musculoskeletal and connective tissue disorders: Muscle spasm, musculoskeletal pain.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, nasopharyngitis, sinusitis, cough, oropharyngeal pain, rhinorrhoea.
Potentially Fatal: Paradoxical bronchospasm.
Inhalation/Respiratory: C
MonitoringParameters
Monitor forced expiratory volume in the 1st second (FEV1), forced vital capacity (FVC), other pulmonary function tests; serum K, blood glucose, blood pressure, heart rate. Monitor deterioration of COPD and re-evaluate therapy as needed.
Overdosage
Symptoms: Increased pulse rate, systolic blood pressure, QTc interval; other exaggerated adverse effects (e.g. tachycardia, palpitations, headache, ventricular arrhythmias, hypokalaemia, hyperglycaemia). Management: Supportive and symptomatic treatment. Administer cardioselective β-blockers under physician supervision. Monitor cardiac function.
Drug Interactions
Sympathetic effects may be potentiated with sympathomimetic agents. Enhanced hypokalaemic effect of methylxanthine derivatives, steroids or non-potassium-sparing diuretics (loop or thiazide diuretics). Increased risk of prolonged QTc interval with MAOIs, TCAs, or other agents known to prolong QTc interval. Antagonistic effect with ß-adrenergic blockers. Increased serum concentration with inhibitors of CYP3A4 and P-glycoprotein (e.g. ketoconazole, erythromycin, verapamil, ritonavir).
Action
Description: Indacaterol is a long-acting β2-adrenergic agonist. It acts by stimulating intracellular adenyl cyclase thus increasing the level of cyclic 5’-adenosine monophosphate (AMP) resulting in the relaxation of bronchial smooth muscle. Indacaterol is a long-acting ß2-adrenergic agonist. It acts by stimulating intracellular adenyl cyclase thus increasing the level of cyclic 5’-adenosine monophosphate (AMP) resulting in the relaxation of bronchial smooth muscle.
Onset: 5 minutes.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Bioavailability: 43-45%. Time to peak plasma concentration: Approx 15 minutes.
Distribution: Volume of distribution: 2,557 L (IV). Plasma protein binding: Approx 95%.
Metabolism: Metabolised in the liver by CYP3A4, CYP2D6 and CYP1A1 to hydroxylated indacaterol and by UGT1A1 to phenolic O-glucuronides.
Excretion: Via faeces (>90%; 54% as unchanged drug, 23% as hydroxylated metabolites); urine (<2% as unchanged drug). Elimination half-life: 40-56 hours.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store below 30°C. Protect from light and moisture.
ATC Classification
R03AC18 - indacaterol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Disclaimer: This information is independently developed by MIMS based on Indacaterol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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