Indications
Maintenance treatment to prevent bronchospasm in
chronic obstructive pulmonary disease (COPD) including
chronic bronchitis and emphysema.
Action
Produces accumulation of cyclic adenosine monophosphate
(cAMP) at beta-adrenergic receptors, resulting in
relaxation of airway smooth muscle. Relatively specific
for beta2 (pulmonary) receptors. Therapeutic Effects:
Bronchodilation.
Pharmacokinetics
Absorption: Following inhalation, majority of inhaled
drug is swallowed and absorbed.
Distribution: Unknown.
Metabolism and Excretion: Mostly metabolized
by the liver; 10–18% excreted unchanged in urine.
Half-life: 10 hr.
TIME/ACTION PROFILE (bronchodilation)
ROUTE ONSET PEAK DURATION
Inhaln 15 min 1–3 hr 12 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Acute attack
of asthma (onset of action is delayed); Patients not receiving
a long-term asthma-control medication (e.g. inhaled
corticosteroid).
Use Cautiously in: Cardiovascular disease (including
angina, hypertension, and arrhythmias); Diabetes;
Seizure disorders; Glaucoma; Hyperthyroidism; Pheochromocytoma;
Excessive use (may lead to tolerance
and paradoxical bronchospasm); OB, Lactation, Pedi:
Pregnancy, lactation, or children 5 yr (may inhibit
contractions during labor; use only if potential benefits
outweigh risks; in children, a fixed-dose combination
product containing formoterol and an inhaled corticosteroid
should be strongly considered to ensure adherence).
Adverse Reactions/Side Effects
CNS: dizziness, fatigue, headache, insomnia, malaise,
nervousness. Resp: ASTHMA-RELATED DEATH, PARADOXICAL
BRONCHOSPASM. CV: angina, arrhythmias, hypertension,
hypotension, palpitations, tachycardia. GI: dry
mouth, nausea. F and E: hypokalemia.Metab: hyperglycemia,
metabolic acidosis. MS: muscle cramps.
Neuro: tremor. Derm: rash. Misc: allergic reactions
including ANAPHYLAXIS.
Interactions
Drug-Drug: Concurrent use with MAO inhibitors,
tricyclic antidepressants, or other agents that may
prolong the QTc interval may result in serious arrhythmias
and should be undertaken with extreme caution.
qrisk of hypokalemia with theophylline, corticosteroids,
potassium-losing diuretics. Beta
blockers mayptherapeutic effects.qadrenergic effects
may occur with concurrent use of adrenergics.
Route/Dosage
Inhaln (Adults): 20 mcg/2 mL-unit-dose vial twice
daily via jet nebulizer.
Availability
Dry powder capsules for inhalation (Foradil
Aerolizer): 12 mcg. Inhalation solution for
nebulization (Perforomist): 20 mcg/2 mL. Powder
for oral inhalation (Oxeze Turbuhaler): 6 mcg/
inhalation (60 metered doses), 12 mcg/inhalation
(60 metered doses). In combination with: budesonide
(Symbicort); glycopyrrolate (Bevespi Aerosphere);
mometasone (Dulera); see Appendix B.
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