salmeterol

Absorption: Minimal systemic absorption follows inhalation.

Distribution: Action is primarily local.

Metabolism/Excretion: Metabolized in the liver via the CYP3A4 isoenzyme; 60% excreted in feces, 25% excreted in urine.

Half-Life: 3–4 hr.

Time/Action Profile ⬆ ⬇

(bronchodilation)

ROUTE	ONSET	PEAK	DURATION
Inhaln	10–25 min	3–4 hr	12 hr‡

‡9 hr in adolescents.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to salmeterol or milk proteins;
Acute attack of asthma (onset of action is delayed);
Patients not receiving a inhaled corticosteroid (↑ risk of asthma-related death);
Patients whose asthma is currently controlled on low- or medium-dose inhaled corticosteroid therapy.

Use Cautiously in:

Cardiovascular disease (including angina and hypertension);
Seizure disorders;
Diabetes;
Glaucoma;
Hyperthyroidism;
Pheochromocytoma;
Excessive use (may lead to tolerance and paradoxical bronchospasm);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; may inhibit contractions during labor;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Children 4 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, tachycardia

GI: abdominal pain, diarrhea, nausea

MS: muscle cramps/soreness

Neuro: headache, nervousness, tremor

Resp: cough, paradoxical bronchospasm

Interactions ⬆ ⬇

Drug-drug:

Beta blockers may ↓ therapeutic effects.
MAO inhibitors and tricyclic antidepressants may potentiate cardiovascular effects.
Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, ritonavir, atazanavir, clarithromycin, nefazodone, or nelfinavir, may ↑ levels and the risk of toxicity; concurrent use not recommended.

Drug-Natural Products:

Use with caffeine-containing herbs (cola nut, guarana, mate, tea, coffee) ↑ stimulant effect.

Route/Dosage ⬆ ⬇

Asthma

Inhaln
(Adults and Children ≥4 yr): 50 mcg (1 inhalation) twice daily (approximately 12 hr apart).

Prevention of Exercise-Induced Bronchospasm

Inhaln
(Adults and Children ≥4 yr): 50 mcg (1 inhalation) ≥30 min before exercise; additional doses should not be used for ≥12 hr.

COPD

Inhaln
(Adults ): 50 mcg (1 inhalation) twice daily (approximately 12 hr apart).

Availability ⬆ ⬇

Powder for oral inhalation: 50 mcg/blister
In combination with: fluticasone (Advair Diskus, Advair HFA, AirDuo Digihaler, AirDuo RespiClick, Wixela Inhub). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess lung sounds, pulse, and BP before administration and periodically during therapy.
Monitor pulmonary function tests before initiating therapy and periodically during therapy.
Observe for paradoxical bronchospasm (wheezing, dyspnea, tightness in chest) and hypersensitivity reaction (rash; urticaria; swelling of the face, lips, or eyelids). Frequently occurs with first use of new canister or vial. If condition occurs, withhold medication and notify physician or other health care professional immediately.

Lab Test Considerations:

May cause ↑ serum glucose concentrations; occurs rarely with recommended doses and is more pronounced with frequent use of high doses.
- May cause ↓ serum potassium concentrations, which are usually transient and dose related; rarely occurs at recommended doses and is more pronounced with frequent use of high doses.

Toxicity and Overdose:

Symptoms of overdose include persistent agitation, chest pain or discomfort, decreased BP, dizziness, hyperglycemia, hypokalemia, seizures, tachyarrhythmias, persistent trembling, and vomiting.
- Treatment includes discontinuing salmeterol and other beta-adrenergic agonists and providing symptomatic, supportive therapy. Cardioselective beta blockers are used cautiously because they may induce bronchospasm.

Implementation ⬆ ⬇

Salmeterol should be used along with an inhaled corticosteroid, not as monotherapy. Patients taking salmeterol twice daily should not use additional doses for exercise-induced bronchospasm.
Inhaln: Once removed from foil overwrap, discard diskus when every blister has been used or 6 wk have passed, whichever comes first.

Patient/Family Teaching ⬆ ⬇

Advise patient to take salmeterol as directed. Do not use more than the prescribed dose. If a regularly scheduled dose is missed, use as soon as possible and resume regular schedule. Do not double doses. If symptoms occur before next dose is due, use a rapid-acting inhaled bronchodilator.
Instruct patient using powder for inhalation never to exhale into diskus device and always to hold device in a level horizontal position. Mouthpiece should be kept dry; never wash.
Caution patient not to use salmeterol to treat acute symptoms. A rapid-acting inhaled beta-adrenergic bronchodilator should be used for relief of acute asthma attacks.
Advise patients on chronic therapy not to use additional salmeterol to prevent exercise-induced bronchospasm. Patients using salmeterol for prevention of exercise-induced bronchospasm should not use additional doses of salmeterol for 12 hr after prophylactic administration.
Advise patient to notify health care professional immediately if difficulty in breathing persists after use of salmeterol, if condition worsens, if more inhalations of rapid-acting bronchodilator than usual are needed to relieve an acute attack, or if using 4 or more inhalations of a rapid-acting bronchodilator for 2 or more consecutive days or more than 1 canister in an 8-wk period.
Salmeterol should be used with inhaled corticosteroids and is not a substitute for corticosteroids or adrenergic bronchodilators. Advise patients using inhalation or systemic corticosteroids to consult health care professional before stopping or reducing therapy.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Emphasize the importance of regular follow-up exams to determine progress during therapy.

Evaluation/Desired Outcomes ⬆ ⬇

Prevention of bronchospasm or reduction of frequency of acute asthma attacks in patients with chronic asthma. Improvement in asthma control can occur within 15 min of starting therapy, but full benefit may take 1 wk or longer. Time to onset and degree of symptom relief will vary with individual.
Prevention of exercise-induced asthma.
Prevention of bronchospasm in COPD.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇