DESCRIPTION-
Formoterol (INN) or eformoterol (former BAN) is a long-acting β2 agonist (LABA) used in the management of asthma and COPD. It is marketed in three forms: a dry-powder inhaler, a metered-dose inhaler and an inhalation solution, under various trade names including Atock, Atimos/Atimos Modulite, Foradil/Foradile, Oxeze/Oxis, and Perforomist. It is also marketed in the combination formulations budesonide/formoterol and mometasone/formoterol.
Formoterol is a long-acting β2 agonist that has an extended duration of action (up to 12 hours) compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4–6 hours. LABAs such as formoterol are used as "symptom controllers" to supplement prophylactic corticosteroid therapy. A "reliever" short-acting β2 agonist (e.g., salbutamol) is still required, since LABAs are not recommended for the treatment of acute asthma.
MECHANISM OF ACTION-
The pharmacologic effects of beta2-adrenoceptor agonist drugs, including formoterol, 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 cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibits the release of pro-inflammatory mast-cell mediators such as histamine and leukotrienes.
HALF LIFE – 10 HRS
DOSAGE-
- 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.
DRUG INTRACTION-
- FORMOTEROL+ACEBUTOLOL -The risk or severity of adverse effects can be increased when Acebutolol is combined with Formoterol.
- Formoterol + Atomoxetine - Atomoxetine may increase the tachycardic activities of Formoterol.
- FORMOTEROL+GOSERELIN-Formoterol may increase the QTc-prolonging activities of Goserelin.
REFERENCE-
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no- 133, 224
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