Olodaterol; Indications, Contraindications Olodaterol Indications Contraindications/ 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 signaling, 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. Mechanism of Action of Olodaterol 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. Indications of Olodaterol 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. 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. Contra-Indications of Olodaterol 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 Dosage of Olodaterol Strengths: 2.5 mcg/inh Chronic Obstructive Pulmonary Disease 5 mcg (2 inhalations) orally once a day Side Effects of Olodaterol 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 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 Olodaterol Olodaterol 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, hydrochlorothiazide) domperidone escitalopram ipratropium macrolide antibiotics (e.g., clarithromycin, erythromycin, telithromycin) methadone mirabegron monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine) 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 tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine) aminophylline theophylline Pregnancy Catagory of Olodaterol FDA Pregnancy Category C Pregnancy This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Lactation It is not known if olodaterol – tiotropium passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children. References DrugBank http://www.drugbank.ca/drugs/DB09080 http://www.drugbank.ca/drugs/DB09080#enzymes http://www.drugbank.ca/drugs/DB09080#targets ClinicalTrials.gov https://clinicaltrials.gov/ FDA Pharm Classes https://www.accessdata.fda.gov/spl/data/1833ecbb-9c1f-4a47-bdbf-2a3c5e78c8ec/1833ecbb-9c1f-4a47-bdbf-2a3c5e78c8ec.xml https://www.fda.gov/ForIndustry/DataStandards/StructuredProductLabeling/ucm162549.ht FDA/SPL Indexing Data https://www.fda.gov/ForIndustry/DataStandards/SubstanceRegistrationSystem-UniqueIngredientIdentifierUNII/ European Chemicals Agency (ECHA) https://echa.europa.eu/information-on-chemicals/cl-inventory-database/-/discli/details/253709 European Chemicals Agency – ECHA https://www.echa.europa.eu/web/guest/information-on-chemicals/cl-inventory-database/-/discli/details/253709 FDA Medication Guides https://www.fda.gov/downloads/Drugs/DrugSafety/UCM531282.pdf FDA Orange Book https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm PubMed Health http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0023570/ Show More