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formoterol (Perforomist)

 

Classes: Beta2 Agonists

Dosing and uses of Perforomist (formoterol)

 

Adult dosage forms and strengths

solution for inhalation

  • 20mcg/2mL

 

Chronic Obstructive Pulmonary Disease (COPD)

Indicated for long-term maintenance treatment of bronchoconstriction in patients with COPd

Perforomist: 20 mcg inhaled via nebulizer q12hr

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Perforomist (formoterol) adverse (side) effects

>10%

Viral infection (17.2%)

 

1-10%

Bronchitis (4.6%)

Chest infection (2.7%)

Dyspnea (2.1%)

Chest pain (1.9%)

Tremor (1.9%)

Dizziness (1.6%)

 

Frequency not defined

Angina

Arrhythmias

Hypo/hypertension

Tachycardia

Hypokalemia

Hyperglycemia

Metabolic acidosis

Headache

Insomnia

Paradoxical bronchospasm

Severe asthma exacerbation

 

Postmarketing Reports

Immune system disorders: Rare reports of anaphylactic reactions, including severe hypotension and angioedema

Metabolism and nutrition disorders: Hypokalemia, hyperglycemia

Respiratory, thoracic and mediastinal disorders: Cough

Skin and subcutaneous tissue disorders: Rash

Cardiac disorders: Angina pectoris, cardiac arrhythmias (eg, atrial fibrillation, ventricular extrasystoles, tachyarrhythmia)

Investigations: Electrocardiogram QT prolonged, blood pressure increased (including hypertension)

 

Warnings

Black box warnings

Long-acting beta2-adrenergic agonists (LABAs) increase the risk of asthma-related death

A placebo-controlled study with another long-acting beta2-adrenergic agonist (salmeterol) showed an increase in asthma-related deaths in patients receiving salmeteroL

The finding of an increased risk of asthma-related death with salmeterol is considered a class effect of LABAs, including formoterol, the active ingredient in Perforomist

The safety and efficacy of Perforomist in patients with asthma have not been established

All LABAs, including Perforomist, are contraindicated in patients with asthma without use of a long-term asthma control medication

 

Contraindications

Hypersensitivity

Tachycardia secondary to heart condition

 

Cautions

Coexisting conditions including cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, hypertension, aneurysm, and pheochromocytoma; convulsive disorders; thyrotoxicosis; patients who are unusually responsive to sympathomimetic amines

Risk of transient hypokalemia

May increase risk of severe, potentially fatal asthma attacks

Do not use for relief of acute COPD symptoms

Concomitant short-acting beta2-agonists can be used as needed for acute relief

Life-threatening paradoxical bronchospasm can occur; discontinue immediately

Immediate hypersensitivity reactions may occur (eg, anaphylactic reactions, urticaria, angioedema, rash, bronchospasm)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: not known if excreted in breast milk, use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Perforomist (formoterol)

Mechanism of action

Long-acting selective beta-2 agonist

Bronchial smooth muscle relaxation

 

Absorption

Peak Plasma Time: 5 min

Peak Plasma Concentration: 92 pg/mL

 

Distribution

Protein Bound: 61-64%

 

Metabolism

Metabolized by CYP2D6, CYP2C19, CYP2C9, CYP2A6

 

Elimination

Half-Life: 10 hr

Clearance: 150 mL/min

Excretion: Urine 66%; feces 33%