Arformoterol; Indications, Dosage, Side Effects, Drug Interaction ,Pregnancy

Mechanism of Action of Arformoterol

While it is recognized that β2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and β1-receptors are the predominant receptors in the heart, data indicate that there are also β2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective β2-agonists may have cardiac effects. The pharmacologic effects of β2-adrenoceptor agonist drugs, including arformoterol, 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 AMP). Increased intracellular cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of proinflammatory mediators from cells, especially from mast cells. In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-response.

or

While it is recognized that β2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and β1-receptors are the predominant receptors in the heart, data indicate that there are also β2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective β2-agonists may have cardiac effects. The pharmacologic effects of β2-adrenoceptor agonist drugs, including arformoterol, 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 AMP). Increased intracellular cyclic AMPlevels cause relaxation of bronchial smooth muscle and inhibition of release of proinflammatory mediators from cells, especially from mast cells. In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-response.

Indications of Arformoterol

• 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.
• Long-term, twice daily (morning and evening) administration in the maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.
• A bronchodilator used for the long-term, symptomatic treatment of reversible bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.
• Maintenance therapy of asthma together with a separate rapid-acting bronchodilator as rescue

Contra-Indications of Arformoterol

• 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
• Allergies to Beta-Adrenergic Agents

Dosage of Arformoterol

Strengths: 15 mcg/2 mL

Chronic Obstructive Pulmonary Disease – Maintenance

• 15 mcg inhaled by nebulization twice daily (morning and evening).
• Maximum Daily Dose: 30 mcg

Side Effects of Arformoterol

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

Arformoterol 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, hydrochlorthiazide)
• 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 Arformoterol

FDA Pregnancy Category C

Pregnancy

In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Lactation

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