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Olodaterol; Uses, Dosage, Side Effects, Interactions

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.

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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

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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 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.

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