formoterol
Formoterol is a long-acting bronchodilator that relaxes muscles in the airways to improve breathing. Formoterol inhalation is used to prevent bronchospasm in people with reversible obstructive airways disease, including symptoms of night-time asthma.
It is also used in people with chronic obstructive pulmonary disease (COPD) such as emphysema and chronic bronchitis.
Mechanism of effect
Relaxes bronchial smooth muscle by selective action on beta2 receptors with little effect on heart rate. Formoterol has a long-acting effect.
Pharmacodynamic
Formoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator.
Pharmacokinetics
Absorption: Rapidly into plasma. Metabolism: Hepatic via direct glucuronidation and O-demethylation; CYP2D6, CYP2C19, CYP2C8/9, CYP2A6 involved in O-demethylation.
Excretion: Children 5-12 years: Urine (6% as unchanged drug, 7% to 9% as direct glucuronide metabolites).Adults: Urine (15% to 18% as direct glucuronide metabolites, 2% to 10% as unchanged drug). Onset of Action: Powder for inhalation: Within 3 minutes.
Peak effect: Powder for inhalation: 80% of peak effect within 15 minutes; Solution for nebulization: 2 hours.
Half-Life Elimination: Powder: ~10-14 hours; Nebulized solution: ~7 hours. Protein Binding: 61% to 64% in vitro at higher concentrations than achieved with usual dosing.
Drug indications
Bronchospasm Prophylaxis , Asthma - Maintenance , Chronic Obstructive Pulmonary Disease - MaintenanceDosage
Usual Adult Dose for Bronchospasm Prophylaxis
To prevent exercise induced bronchospasm:
12 mcg (1 inhalation) of powder at least 15 minutes before exercise as needed. Additional doses should not be taken for 12 hours.
Usual Adult Dose for Asthma - Maintenance
12 mcg (1 inhalation) of powder every 12 hours. Total daily dose should not exceed 24 mcg.
Usual Adult Dose for Chronic Obstructive Pulmonary Disease - Maintenance
formoterol 12 mcg inhalation capsule:
12 mcg (1 inhalation) of powder every 12 hours. Total daily dose should not exceed 24 mcg.
formoterol 20 mcg/2 mL inhalation solution:
one 20 microgram/2 mL vial via jet nebulizer with a facemask or mouthpiece every 12 hours.
Usual Pediatric Dose for Bronchospasm Prophylaxis
To prevent exercise induced bronchospasm:
5 years or older: 12 mcg (1 inhalation) of powder at least 15 minutes before exercise as needed. Additional doses should not be taken for 12 hours.
Usual Pediatric Dose for Asthma - Maintenance
5 years or older:
12 mcg (1 inhalation) of powder every 12 hours. Total daily dose should not exceed 24 mcg.
Drug contraindications
hypersensitivity to drug or its components. , acute episodes of asthma or COPD , status asthmaticus , monotherapy in the treatment of asthma , tachyarrhythmiasSide effects
nausea , Headache , insomnia , chest pain , abdominal pain , dizziness , vomiting , rash , Diarrhea , Dyspnea , pruritus , dyspepsia , sinusitis , respiratory tract infection , fever , anxiety , bronchitis , Tremor , Hypokalemia , Hyperglycemia , pharyngitis , voice disorder , Muscle cramps , tonsillitisInteractions
Drospirenone , Atomoxetine , Amitriptyline , Aminophiline , Acetaminophen+caffeine , Acetaminophen+caffein+acetylsalic , Acetaminophan+caffeine+ibuprofen , Bisoprolol , Droperidol , Procainamide , Indapamide , Inotuzumab , Citalopram , Fluticasone , Fluticasone propinate , Labetalol , Midodrine , Carvedilol , Ipratropium bromide , Propranolol , Tranylcypromine , Salbutamol , Salmeterol , Sotalol , sparfloxacin , Entrectinib , AtosibanAlerts
1-Long-acting beta2-agonists (LABAs) increase the risk of asthma-related deaths. Formoterol should only be used in asthma patients as adjuvant therapy in patients who are currently receiving but are not adequately controlled on a long-term asthma control medication (ie, an inhaled corticosteroid).
2-Use with caution in patients with diabetes mellitus, Cardiovascular disease, Exercise-induced bronchospasm, Hyperthyroidism, Hypokalemia, Pheochromocytoma, Seizures.
Points of recommendation
1- Discuss specific use of drug and side effects with patient as it relates to treatment
2- Patient may experience diarrhea. Have patient report immediately to prescriber signs of high blood sugar (confusion, feeling sleepy, more thirst, hunger, passing urine more often, flushing, fast breathing, or breath that smells like fruit), signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat), angina, tachycardia, anxiety, severe dizziness, passing out, fast breathing, chills, pharyngitis, severe headache, severe nausea, vomiting, severe abdominal pain, change in voice, or difficulty breathing, wheezing, or coughing after use
3- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat).
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