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Indacaterol; Indications/Uses, Side effects, Drug Interactions, Pregnancy

Indacaterol is a novel, ultra-long-acting, (2)-adrenoceptor agonist developed for Novartis for the once-daily treatment of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) under the trade name Onbrez on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. Indacaterol is provided as a pure R-enantiomer, typically as the salt indacaterol maleate.

It was approved by the European Medicines Agency (EMA) under the trade name Onbrez Breezhaler on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD) (long-term data in patients with asthma are thus far lacking). It is delivered as an aerosol formulation through a dry powder inhaler

Mechanism of Action of Indacaterol

Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of the airways. This causes relaxation of the muscle, thereby increasing the diameter of the airways, which become constricted in asthma and COPD. It is also long acting due to its high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting – onset of action occurs within 5 minutes. The pharmacological effects of beta2-adrenoceptor agonist drugs, including indacaterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3’, 5’-adenosine monophosphate (cyclic monophosphate). Increased cyclic AMP levels cause relaxation of the bronchial smooth muscle. In vitro studies have shown that indacaterol has more than 24-fold greater agonist activity at beta2-receptors compared to beta1-receptors and 20-fold greater agonist activity compared to beta3-receptors. This selectivity profile is similar to formoterol. The clinical significance of these findings is unknown.

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Indications of Indacaterol

Chronic Obstructive Pulmonary Disease (COPD)
Bronchiectasis
Bronchospasm Prophylaxis
Bronchial asthma,
Chronic bronchitis,
Chronic bronchopulmonary disorders
Airflow obstruction in patients with chronic obstructive pulmonary disease (COPD),
Chronic bronchitis and/or emphysema.
indicated for maintenance bronchodilator treatment of airflow obstruction in adult patients with chronic obstructive pulmonary disease (COPD).
indicated for maintenance bronchodilator treatment of airflow obstruction in adult patients with chronic obstructive pulmonary disease (COPD).

Contra-Indications of Indacaterol

Thyrotoxicosis
Low amount of potassium in the blood
Diabetes
Ketoacidosis
Excess Body Acid
Low amount of potassium in the blood
High blood pressure
Diminished blood flow through arteries of the Heart
Prolonged QT interval on EKG
Abnormal heart rhythm
Abnormal EKG with QT changes from Birth
Kidney disease with the reduction in kidney function
Seizures
Paradoxical bronchospasm
Allergies to – Beta-Adrenergic Agents

Dosage of Indacaterol

Strengths: 75 mcg

Chronic Obstructive Pulmonary Disease – Maintenance

1 inhalation (75 mcg) orally once a day

Side Effects of Indacaterol

The most common

Arm, back, or jaw pain
Chest pain or tightness
dry mouth
trembling or shaking of the hands or feet
stomach pain or cramping
diarrhea
a headache
dizziness
confusion
stomach pain;
back pain, joint or muscle pain.
problems with your vision (including color vision);
sudden chest pain or trouble breathing;
pain or swelling in one or both legs;
a migraine headache;
pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
feeling like you might pass out.

More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

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Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

Drug Interactions of Indacaterol

Indacaterol may interact with the following drugs, supplements & may change the efficacy of drugs

antihistamines (e.g, cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
beta 2 agonists (e.g., salbutamol, formoterol, terbutaline)
beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
long-acting beta agonists (e.g., indacaterol, salmeterol)
citalopram
decongestant cold medications (e.g., phenylephrine, pseudoephedrine)
decongestant eye drops and nose sprays (e.g., naphazoline, oxymetazoline, xylometazoline)
oral steroids such as prednisone, dexamethasone methylprednisolone, and others
diuretics (e.g., furosemide, hydrochlorthiazide)
domperidone
escitalopram
ipratropium
macrolide antibiotics (e.g., clarithromycin, erythromycin, telithromycin)
methadone
mirabegron
monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
narcotics (e.g., codeine, morphine, oxycodone)
quinolone antibiotics (e.g., levofloxacin moxifloxacin ofloxacin)
serotonin antagonists (anti-emetic medications; e.g., ondansetron granisetron, )
theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
tolterodine
topiramate
tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
aminophylline
theophylline

Pregnancy Catagory of Indacaterol

FDA Pregnancy Category C

Pregnancy

Indacaterol falls into category C. There are no well-done studies that have been done in humans with indacaterol. But in animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

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Lactation

It is not known if indacaterol crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication.