Olodaterol
Olodaterol Uses, Dosage, Side Effects, Food Interaction and all others data.
Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs. Beta2-adrenergic receptors are membrane-bound receptors that are normally activated by endogenous epinephrine whose signalling, via a downstream L-type calcium channel interaction, mediates smooth muscle relaxation and bronchodilation. Activation of the receptor stimulates an associated G protein which then activates adenylate cyclase, catalyzing the formation of cyclic adenosine monophosphate (cAMP) and protein kinase A (PKA). Elevation of these two molecules induces bronchodilation by relaxation of airway smooth muscles. It is by this mechanism that olodaterol is used for the treatment of chronic obstructive pulmonary disease (COPD) and the progressive airflow obstruction that is characteristic of it. Treatment with bronchodilators helps to mitigate associated symptoms such as shortness of breath, cough, and sputum production. Single doses of olodaterol have been shown to improve forced expiratory volume in 1 sec (FEV1) for 24 h in patients with COPD, allowing once daily dosing. A once-a-day treatment with a LABA has several advantages over short-acting bronchodilators and twice-daily LABAs including improved convenience and compliance and improved airflow over a 24-hour period. Despite similarities in symptoms, olodaterol is not indicated for the treatment of acute exacerbations of COPD or for the treatment of asthma.
Olodaterol is a potent agonist of the human beta2-adrenergic receptor in vitro, and is highly selective for this receptor, with much lower levels of activity at the b1- and b3-adrenergic receptors that are commonly expressed on cardiac smooth muscle and adipose tissue, respectively. Binding to the receptor causes smooth muscle relaxation in the lungs and bronchodilation. It has also been shown to potently reverse active bronchoconstriction.
| Trade Name | Olodaterol |
| Availability | Prescription only |
| Generic | Olodaterol |
| Olodaterol Other Names | Olodaterol |
| Related Drugs | Trelegy Ellipta, ProAir Digihaler, prednisone, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA, Spiriva, Anoro Ellipta |
| Weight | 2.5mcg/inh |
| Type | Inhalation aerosol, inhalation |
| Formula | C21H26N2O5 |
| Weight | Average: 386.448 Monoisotopic: 386.184171945 |
| Protein binding | In vitro binding of olodaterol to human plasma proteins is independent of concentration and is approximately 60%. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Olodaterol is a long-acting beta2-adrenergic agonist used in the management of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.
Olodaterol is indicated for use in chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema. It is not indicated for the treatment of acute exacerbations of COPD or for the treatment of asthma.
Olodaterol is also used to associated treatment for these conditions: Chronic Obstructive Pulmonary Disease (COPD)
How Olodaterol works
Olodaterol is a long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs. Beta2-adrenergic receptors are membrane-bound receptors that are normally activated by endogenous epinephrine whose signalling, via a downstream L-type calcium channel interaction, mediates smooth muscle relaxation and bronchodilation. Activation of the receptor stimulates an associated G protein which then activates adenylate cyclase, catalyzing the formation of cyclic adenosine monophosphate (cAMP) and protein kinase A (PKA). Elevation of these two molecules induces bronchodilation by relaxation of airway smooth muscles.
Toxicity
Adverse drug reactions that occurred at a frequency greater than 2% include nasopharyngitis (11.3%), upper respiratory tract infection (8.2%), bronchitis (4.7%), urinary tract infection (2.5%), cough (4.2%), dizziness (2.3%), rash (2.2%), diarrhea (2.9%), back pain (3.5%), and arthralgia (2.1%).
Food Interaction
No interactions found.Olodaterol 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.
Olodaterol Drug Interaction
Moderate: umeclidinium / vilanterol, fluticasone / vilanterol, albuterol / ipratropium, metoprolol, metoprolol, formoterol, budesonide / formoterolUnknown: mometasone, mometasone, amoxicillin / clavulanate, aztreonam, arginine, levocarnitine, guaifenesin, acetaminophen, bifidobacterium infantis / lactobacillus acidophilus, beclomethasone, tiotropium, cyanocobalamin, cholecalciferol
Olodaterol Disease Interaction
Major: asthmaModerate: hepatic impairment, cardiovascular, diabetes, hypokalemia, seizures
Volume of Distribution
The volume of distribution is high (1110 L), suggesting extensive distribution into tissue.
Elimination Route
Olodaterol reaches maximum plasma concentrations generally within 10 to 20 minutes following drug inhalation. In healthy volunteers, the absolute bioavailability of olodaterol following inhalation was estimated to be approximately 30%, whereas the absolute bioavailability was below 1% when given as an oral solution. Thus, the systemic availability of olodaterol after inhalation is mainly determined by lung absorption, while any swallowed portion of the dose only negligibly contributes to systemic exposure.
Half Life
The terminal half-life following intravenous administration is 22 hours. The terminal half-life following inhalation in contrast is about 45 hours, indicating that the latter is determined by absorption rather than by elimination processes.
Clearance
Total clearance of olodaterol in healthy volunteers is 872 mL/min, and renal clearance is 173 mL/min.
Elimination Route
Following intravenous administration of [14C]-labeled olodaterol, 38% of the radioactive dose was recovered in the urine and 53% was recovered in feces. The amount of unchanged olodaterol recovered in the urine after intravenous administration was 19%. Following oral administration, only 9% of olodaterol and/or its metabolites was recovered in urine, while the major portion was recovered in feces (84%).
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