Indacaterol - Uses, Dose, Side effects

Indacaterol is a long-acting beta-adrenoceptor agonist (LABA) that is used for the once-daily maintenance treatment of chronic obstructive pulmonary disease (COPD). It acts by binding to and stimulating the beta-2 adrenergic receptors in the smooth muscle of the airways, leading to relaxation and bronchodilation. This helps to improve airflow and reduce symptoms in patients with COPD.

Novartis created the ultra-long-acting beta-agonist called Indacaterol. Patients with uncontrolled COPD use it as an oral inhalation medication once daily (chronic obstructive pulmonary disease). This condition reduces the restriction of airflow that causes coughing, chest tightness, wheezing, and shortness of breath.

Indications of Indacaterol:

  • Chronic obstructive pulmonary disease:
    • It is indicated to use as a long-term maintenance medication for patients with COPD (chronic obstructive pulmonary disease), which includes chronic bronchitis and emphysema.

Indacaterol dose in adults:

Indacaterol dosage for chronic obstructive pulmonary disease maintenance:

How to take it:

  • Use a special device to inhale the dry powder.
  • Inhale the contents of 1 capsule, which contains 75 mcg, once every day.

Important to know:

  • The 2018 GOLD Guidelines suggest taking between 75 to 300 mcg of indacaterol once daily.

Indacaterol use in Children:

The drug's effectiveness and safety in children have not been shown.

Pregnancy Risk Factor C

  • Tests on animals didn't show any harmful effects on babies they were carrying.
  • However, beta-agonists (like this medicine) might affect the tightening and relaxing of the womb if given during childbirth.

Indacaterol use during breastfeeding:

  • We don't know if indacaterol gets into breast milk.
  • So, the company that makes it advises being careful when giving this medicine to women who are breastfeeding.

Indacaterol Dose adjustment in Renal Disease:

  • Adjustment in the dose is not necessary.

Indacaterol Dose in Liver Disease:

  • If someone has a mild or moderate health problem, they can take the medicine as usual.
  • If someone has a severe health problem, the company that makes the medicine hasn't given any special instructions on how much to take (because they haven't studied it in such cases).

Common Side Effects of Indacaterol:

  • Respiratory:
    • Cough

Less Common Side Effects of Indacaterol:

  • Central nervous system:
    • Headache
  • Respiratory:
    • Nasopharyngitis
    • Oropharyngeal pain
  • Gastrointestinal:
    • Nausea

Contraindications to Indacaterol:

  • Don't use indacaterol if you're allergic to it or any part of the medicine.
  • Don't use it by itself to treat asthma without also using an inhaled steroid medicine.

Warnings and precautions

Asthma-related Deaths:

  • Using a LABA (like indacaterol) by itself for asthma is not safe.
  • In a big study in the US, another LABA called salmeterol increased the number of asthma-related deaths when used on its own.
  • This risk is thought to apply to all LABAs, not just salmeterol.
  • However, when LABAs are combined with an inhaled steroid in one inhaler, the risk of serious asthma problems doesn't seem to be higher than using just the inhaled steroid.
  • Current advice suggests using an inhaled steroid first before adding a LABA.
  • A newer study showed that combining salmeterol and an inhaled steroid in one inhaler did not increase serious asthma problems. Plus, those using the combination had fewer severe asthma attacks than those using only the steroid.
  • Indacaterol is not meant for treating asthma.
  • For patients with COPD, using LABAs does not appear to increase the risk of death.

Bronchospasm

  • Sometimes, when using inhaled medicines meant to open up the airways, the opposite can happen, causing the airways to tighten suddenly.
  • This unexpected reaction can be very dangerous.
  • If this happens, stop using the medicine right away and start a different treatment.

Hypersensitivity

  • Some people have had sudden allergic reactions like trouble breathing or swallowing, swelling of the tongue, lips, or face, hives, or a skin rash after taking the medicine.
  • If this happens, stop the medicine right away.

Deaths and serious effects:

  • Don't take more than the advised amount, don't use it too often, and don't use it with other similar medicines.
  • Taking too much can lead to severe health problems or even death.

Cardiovascular disease

  • Be extra careful when using this medicine if you have heart problems, like irregular heartbeats, weak heart, or high blood pressure.
  • This medicine can raise blood pressure and make the heart beat faster.
  • It can also cause changes in heart test results.

Use it in the right way:

  • Don't use this medicine during sudden breathing problems with COPD.
  • Don't start using it if someone's COPD is getting rapidly worse.
  • We don't know if using this type of medicine raises the risk of death for COPD patients. But from what we do know, it doesn't seem to increase that risk.

Diabetes:

  • If you have diabetes, be careful using this medicine.
  • It can raise blood sugar levels and make existing diabetes issues worse.

Hyperthyroidism:

  • If you have an overactive thyroid, be careful using this medicine.
  • It might make the thyroid even more active.

Hypokalemia

  • If you have low potassium levels, be cautious using this medicine.
  • It might reduce your potassium levels even more for a short time.

Seizures:

  • If you have a condition that causes seizures, be careful using this medicine.
  • It might make the brain more active or excited, possibly leading to seizures.

Indacaterol: Drug Interaction

Risk Factor C (Monitor therapy)

AtoMOXetine

Possibly makes beta2-agonists' tachycardic impact stronger.

AtoMOXetine

Could make sympathomimetics' hypertensive effects stronger. The tachycardic impact of sympathomimetics may be increased by atoMOXetine.

Atosiban

Beta2-Agonists may intensify Atosiban's harmful or hazardous effects. Particularly, pulmonary edema and/or dyspnea may be at higher risk.

Beta-Blockers (Beta1 Selective)

May lessen beta2-agonists' bronchodilator effects. Particular attention should be paid to nonselective beta-blockers or beta1 selective beta-blockers at larger doses.

Betahistine

May lessen beta2-agonists' therapeutic efficacy.

Caffeine and Caffeine Containing Products

May intensify Indacaterol's harmful or hazardous effects. The hypokalemic impact of indacaterol may be enhanced by caffeine and products containing caffeine.

Cannabinoid-Containing Products

Perhaps makes sympathomimetics' tachycardic effect stronger. Cannabidiol is an exception.

Corticosteroids (Systemic)

The effect of corticosteroids being hypokalemic may be enhanced by indacaterol (Systemic).

Doxofylline

Sympathomimetic drugs may intensify Doxofylline's harmful or hazardous effects.

Guanethidine

Could make sympathomimetics more arrhythmogenic. Guanethidine might make sympathomimetic drugs more hypertensive.

Haloperidol

QT-prolonging drugs may increase the QTc-prolonging effects of haloperidol (Indeterminate Risk - Caution).

Loop Diuretics

Beta2-Agonists may increase the hypokalemic effects of loop diuretics.

Monoamine Oxidase Inhibitors

May intensify the hazardous or harmful effects of beta2-agonists.

QT-prolonging Agents (Highest Risk)

QT-prolonging Agents may improve the QTc-prolonging activity of QT-prolonging Agents (Indeterminate Risk - Caution) (Highest Risk). Management: Monitor for QTc interval prolongation and cardiac arrhythmias when these drugs are used together. Patients who have extra risk factors may be even more susceptible to QTc prolongation.

Solriamfetol

Sympathomimetics may intensify Solriamfetol's hypertensive effects.

Sympathomimetics

Could intensify the hazardous or harmful effects of other sympathomimetics. Could make sympathomimetics' hypertensive effects stronger.

Tedizolid

The tachycardic impact of sympathomimetics may be increased by tedizolid.

Theophylline Derivatives

May intensify Indacaterol's harmful or hazardous effects. The hypokalemic action of indacaterol may be strengthened by theophylline derivatives.

Thiazide and Thiazide-Like Diuretics

Thiazide and Thiazide-Like Diuretics may have an enhanced hypokalemic impact when beta2-Agonists are present.

Tricyclic Antidepressants

May intensify the hazardous or harmful effects of beta2-agonists.

Risk Factor D (Consider therapy modification)

Cocaine (Topical)

Could make sympathomimetics' hypertensive effects stronger. Management: Whenever possible, look at alternatives to using this combo. When used concurrently, keep a close eye out for noticeably elevated blood pressure or heart rate as well as any signs of myocardial ischemia.

Linezolid

Could make sympathomimetics' hypertensive effects stronger. Reduce initial sympathomimetic doses and keep a close eye out for patients taking linezolid who exhibit an elevated pressor response. There are currently no suggestions for specific dose adjustments.

Methacholine

Long-Acting Beta2-Agonists may reduce methacholine's therapeutic efficacy. Treatment: Wait 36 hours before using methacholine when taking long-acting beta-agonists.

Risk Factor X (Avoid combination)

Beta-Blockers (Nonselective)

May lessen beta2-agonists' bronchodilator effects.

Loxapine

Medication for respiratory illness may worsen the side effects or dangers of loxapine. In other words, using agents to treat respiratory disease is likely a sign of someone who is more likely to be vulnerable to severe bronchospasm from loxapine inhalation. Management: This only pertains to the Adasuve-branded inhaled loxapine formulation. This prohibition does not apply to loxapine formulations that are not breathed in.

Beta2-Agonists (Long-Acting)

May intensify the negative or harmful effects of additional beta2-agonists (Long-Acting).

Monitor:

Lung Tests:

  • FEV (how much air you can exhale quickly)
  • FVC (total air you exhale)
  • Other breathing tests

Blood Tests:

  • Potassium levels
  • Sugar (glucose) levels

Heart and Blood Pressure:

  • Blood pressure measurements
  • Heart rate (pulse)

Brain Activity:

  • Look out for signs of increased brain excitement or stimulation

Use of Other Inhalers:

  • Keep track if you're using short-acting breath inhalers more often. It might mean your condition is getting worse.

How to administer Indacaterol?

  • Type of Inhaler: This is a dry powder inhaler.
  • When to Use: Inhale it at the same time every day.
  • Inhaler Names: It's called "Neohaler" in the US and "Onbrez Breezhaler" in Canada.

Important Steps:

  • Don't swallow the capsules.
  • Every time you get a new prescription, you'll also get a new inhaler. Use that new one.
  • Only take a capsule out of its packaging right before you're going to use it.
  • Put the capsule in the inhaler's special spot and close it until you hear a click.
  • Press the red buttons on the sides of the inhaler once to break open the capsule.
  • Inhale the powder from the capsule. If there's still powder left, inhale again.
  • Don't wash the part you put in your mouth. Keep the inhaler dry.
  • If you ever open a capsule and expose it to air but don't use it right away, throw it away.

Mechanism of action of Indacaterol:

  • It works mainly on special spots (called beta-receptors) in the lungs to relax the muscles there.
  • This helps open up the airways.
  • It doesn't affect the heart much, so your heartbeat stays mostly the same.

Starts Working:

  • You'll start feeling its effects about 5 minutes after using it.

Strongest Effect:

  • It works the best after about 1 to 4 hours.

Lasts:

  • The effects stay for a whole day, about 24 hours.

Getting into the Body:

  • When you breathe it in, about 43% to 45% of the medicine gets into your bloodstream.

Joined to Proteins:

  • Around 95% of the medicine attaches itself to proteins in your body.

Broken Down:

  • Your liver breaks it down. This involves certain enzymes like CYP3A4, CYP2D6, and CYP1A1.

Leaving the Body:

  • It takes quite a while for the medicine to leave your body. The time it takes is around 40 to 56 hours.

Peak Time in Blood:

  • It reaches its highest levels in your blood after around 15 minutes.

Leaving the Body, Part 2:

  • Most of it leaves through your feces (over 90%, with about 54% of it unchanged) and a small bit through your urine (less than 2% unchanged).

International Brands of Indacaterol:

  • Arcapta Neohaler
  • Onbrez Breezhaler
  • Dilinda
  • Hirobriz Breezhaler
  • Introventa
  • Onbrez
  • Onbrez Breezhaler
  • Onbrise Breezhaler
  • Onbrize
  • Onbrize Breezhaler
  • Onriva
  • Oslif

Indacaterol Brand Names in Pakistan:

OnBreze Breezehaler

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