Caterol
Caterol Uses, Dosage, Side Effects, Food Interaction and all others data.
Caterol is a long acting β2-adrenergic agonist. It relaxes the bronchial smooth muscle by selective action on β2-receptor which acts locally in the lungs and with little effect on heart rate.
When inhaled, Caterol acts locally in the lung as a bronchodilator. The pharmacological effects of β2-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 monophosphate. Increased cyclic AMP levels cause relaxation of bronchial smooth muscle.
Bronchodilator drugs are the foundation for the treatment of chronic obstructive pulmonary disease. The principal inhaled bronchodilator treatments used are β(2) -agonists and anticholinergics, either alone or in combination. Currently available β(2) -agonists are of either short duration and used multiple times/day, or of long duration, which requires twice-daily administration. Caterol is considered an ultra-long-acting β(2) -agonist and was recently approved for use in the United States. Its duration of action is approximately 24 hours, allowing for once-daily administration. Furthermore, this chiral compound it is given as the R-enantiomer and acts as a full agonist. Cough was the most commonly reported adverse effect with use of indacaterol. Compared to salmeterol, it has 35% more agonist activity. Cough usually occurred within 15 seconds of inhalation of the drug, lasted around 6 seconds, was not associated with bronchospasm, and did not cause discontinuation of the drug. Otherwise, the drug's safety profile was similar to that of other bronchodilators. [PMID: 22499359]
| Trade Name | Caterol |
| Availability | Discontinued |
| Generic | Indacaterol |
| Indacaterol Other Names | Indacaterol |
| Related Drugs | ProAir Digihaler, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA, Spiriva |
| Weight | 75mcg |
| Type | Inhalation Capsule |
| Formula | C24H28N2O3 |
| Weight | Average: 392.4907 Monoisotopic: 392.209992772 |
| Protein binding | The in vitro human serum and plasma protein binding was 94.1-95.3% and 95.1-96.2%, respectively. |
| Groups | Approved |
| Therapeutic Class | Long-acting selective β2-adrenoceptor stimulants |
| Manufacturer | Incepta Pharmaceuticals Limited |
| Available Country | Bangladesh |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Caterol is used for the treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.
Caterol is a long-acting β2-adrenergic agonist used for long-term, once-daily maintenance bronchodilator treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.
Caterol is also used to associated treatment for these conditions: Asthma, Chronic Obstructive Pulmonary Disease (COPD), Maintenance
How Caterol works
Caterol 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. Caterol 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 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.
Dosage
Caterol dosage
Caterol capsules must not be swallowed as the intended effects on the lungs will not be obtained. The contents of Caterol capsules are only for oral inhalation and should only be used with thedevice.
The recommended dosage of Caterol is the once-daily inhalation of the contents of one 75/150 mcg Caterol capsule using the device.
Caterol should be administered once daily every day at the same time of the day by the orally inhaled route only. If a dose is missed, the next dose should be taken as soon as it is remembered. Do not use Caterol more than one time every 24 hours.
Side Effects
The most commonly reported adverse effects were cough, nasopharyngitis, headache, nausea, oropharyngeal pain. Some other also reported of hypersensitivity reactions, paradoxical bronchospasm, tachycardia, pruritis and dizziness.
Toxicity
The expected signs and symptoms associated with overdosage of indacaterol are those of excessive beta-adrenergic stimulation and occurrence or exaggeration of any of the signs and symptoms, e.g., angina, hypertension or hypotension, tachycardia, with rates up to 200 bpm, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis and insomnia. As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose of indacaterol.
Precaution
Rarely, serious (sometimes fatal) breathing problems have happened to people with asthma using a long-acting inhaled beta agonist (salmeterol). Since Caterol is similar to salmeterol, it might cause these serious breathing problems. Caterol has not been shown to be safe or effective to treat asthma and is not approved for this use.
Interaction
Caterol shows interaction with Adrenergic Drugs, Xanthine Derivatives, Steroids, or Diuretics. Concomitant treatment with xanthine derivatives, steroids, or diuretics may potentiate any hypokalemic effect of Caterol. The ECG changes or hypokalemia that may result from the administration of non-potassium sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by β2-agonists. Caterol, as with other β2-agonists, should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors, tricyclic antidepressants, or other drugs known to prolong the QTc interval. β-adrenergic receptor antagonists (beta-blockers) and Caterol may interfere with the effect of each other when administered concurrently.
Food Interaction
No interactions found.Caterol Hypertension interaction
[Moderate] Adrenergic bronchodilators can stimulate cardiovascular beta- 1 and beta- 2 receptors, resulting in adverse effects such as tachycardia, palpitation, peripheral vasodilation, blood pressure changes, and ECG changes (e.g., flattening of the T wave; prolongation of the QT interval; ST segment depression).
Direct stimulation of cardiac tissues is mediated by beta- 1 receptors and thus less likely to occur with beta-2-selective agents such as albuterol.
However, beta-2-selectivity is not absolute and can be lost with larger doses.
High dosages of these agents have been associated with precipitation or aggravation of angina, myocardial ischemia, and cardiac arrhythmias.
Therapy with adrenergic bronchodilators should be administered cautiously in patients with sensitivity to sympathomimetic amines, hyperthyroidism, and The recommended dosages should not be exceeded.
Caterol Drug Interaction
Moderate: umeclidinium / vilanterol, fluticasone / vilanterol, albuterol / ipratropium, albuterolUnknown: charcoal, bifidobacterium infantis, ipratropium, amoxicillin / clavulanate, dicyclomine, multivitamin with minerals, tadalafil, loratadine, fentanyl, sodium iodide, atorvastatin, acetaminophen, tiotropium, tiotropium, cyanocobalamin, ascorbic acid
Caterol Disease Interaction
Volume of Distribution
After intravenous infusion the volume of distribution (Vz) of indacaterol was 2,361 L to 2,557 L indicating an extensive distribution.
Elimination Route
The median time to reach peak serum concentrations of indacaterol was approximately 15 minutes after single or repeated inhaled doses. Absolute bioavailability of indacaterol after an inhaled dose was on average 43-45%.
Half Life
Caterol serum concentrations declined in a multi-phasic manner with an average terminal half-life ranging from 45.5 to 126 hours. The effective half-life, calculated from the accumulation of indacaterol after repeated dosing with once daily doses between 75 mcg and 600 mcg ranged from 40 to 56 hours which is consistent with the observed time-to-steady state of approximately 12-15 days.
Clearance
Renal clearance of indacaterol is, on average, between 0.46 and 1.2 L/h. Serum clearance of indacaterol is 18.8 L/h to 23.3 L/h.
Elimination Route
Renal clearance plays a minor role (about 2 to 6% of systemic clearance) in the elimination of systemically available indacaterol. In a human ADME study where indacaterol was given orally, the fecal route of excretion was dominant over the urinary route. Caterol was excreted into human feces primarily as unchanged parent drug (54% of the dose) and, to a lesser extent, hydroxylated indacaterol metabolites (23% of the dose).
Pregnancy & Breastfeeding use
Pregnancy Category C. There are no adequate and well-controlled studies with Caterol powder in pregnant women. Caterol powder should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known that the active component of Caterol powder, Caterol is excreted in human milk. Because many drugs are excreted in human milk and because Caterol has been detected in the milk of lactating rats, caution should be exercised when Caterol powder is administered to nursing women.
Contraindication
All LABA are contraindicated in patients with asthma without use of a long-term asthma control medication. Caterol powder is not indicated for the treatment of asthma. Caterol is contraindicated in patients with a history of hypersensitivity to Caterol or to any of the ingredients.
Special Warning
Geriatric patients: No dosage adjustment is required for geriatric patients, patients with mild and moderate hepatic impairment, or renal impaired patients.
Hepatic impairment: No data are available for subjects with severe hepatic impairment.
Hepatic use: Not indicated for use in the hepatic impairment. Safety and efficacy have not been established.
Acute Overdose
The expected signs and symptoms associated with over dosage of Caterol powder are those of excessive beta-adrenergic stimulation and occurrence or exaggeration of any of the signs and symptoms, e.g., angina, hypertension or hypotension, tachycardia, with rates up to 200 bpm, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis and insomnia. As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an over dose of Caterol powder.
Storage Condition
Caterol capsules must always be stored in the blister, and only removed immediately before use. Keep in a cool & dry place. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Caterol
Caterol contains Indacaterol see full prescribing information from innovator Caterol Monograph, Caterol MSDS, Caterol FDA label
