No

Beta₂ Agonist

Maintenance treatment of asthma and in prevention of bronchospasm in patients >12 years of age with reversible obstructive airway disease, including patients with symptoms of nocturnal asthma, who require regular treatment with inhaled, short-acting beta₂ agonists; prevention of exercise-induced bronchospasm; treatment of COPD-induced bronchospasm

C

Hypersensitivity to salmeterol, adrenergic amines or any ingredients; need for acute bronchodilation; within 2 weeks of MAO inhibitor use

Salmeterol is not meant to relieve acute asthmatic symptoms. Acute episodes should be treated with short-acting beta₂ agonist. Do not increase the frequency of salmeterol. Cardiovascular effects are not common with salmeterol when used in recommended doses. All beta agonists may cause elevation in blood pressure, heart rate, and result in excitement (CNS). Use with caution in patients with prostatic hypertrophy, diabetes, cardiovascular disorders, convulsive disorders, thyrotoxicosis, or others who are sensitive to the effects of sympathomimetic amines. Paroxysmal bronchospasm (which can be fatal) has been reported with this and other inhaled agents. If this occurs, discontinue treatment. The elderly may be at greater risk of cardiovascular side effects; safety and efficacy have not been established in children <12 years of age.

>10%:

Central nervous system: Headache

Respiratory: Pharyngitis

1% to 10%:

Cardiovascular: Tachycardia, palpitations, elevation or depression of blood pressure, cardiac arrhythmias

Central nervous system: Nervousness, CNS stimulation, hyperactivity, insomnia, malaise, dizziness

Gastrointestinal: GI upset, diarrhea, nausea

Neuromuscular & skeletal: Tremors (may be more common in the elderly), myalgias, back pain, arthralgia

Respiratory: Upper respiratory infection, cough, bronchitis

<1%: Immediate hypersensitivity reactions (rash, urticaria, bronchospasm)

Decontaminate using lavage/activated charcoal

Beta-blockers can be used for hyperadrenergic signs (use with caution in patients with bronchospasm)

Prudent use of a cardioselective beta-adrenergic blocker (eg, atenolol or metoprolol); keep in mind the potential for induction of bronchoconstriction in an asthmatic. Dialysis has not been shown to be of value in the treatment of an overdose with this agent.

CYP3A3/4 enzyme substrate

Increased toxicity (cardiovascular): MAO inhibitors, tricyclic antidepressants

Aerosol: Store at 15°C to 30°C (59°F to 86°F); store cannister with nozzle down; shake well before each use

Inhalation powder: Store at controlled room temperature 20°C to 25°C (68°F to 77°F) in a dry place away from direct heat or sunlight

Relaxes bronchial smooth muscle by selective action on beta₂-receptors with little effect on heart rate; because salmeterol acts locally in the lung, therapeutic effect is not predicted by plasma levels

Onset of action: 5-20 minutes (average 10 minutes)

Peak effect: 2-4 hours

Duration: 12 hours

Protein binding: 94% to 98%

Metabolism: Hydroxylated in liver

Half-life: 3-4 hours

Inhalation: 42 mcg (2 puffs) twice daily (12 hours apart) for maintenance and prevention of symptoms of asthma

Prevention of exercise-induced asthma: 42 mcg (2 puffs) 30-60 minutes prior to exercise; additional doses should not be used for 12 hours

COPD: Adults: For maintenance treatment of bronchospasm associated with COPD (including chronic bronchitis and emphysema): 2 inhalations (42 mcg) twice daily (morning and evening - 12 hours apart); do not use a spacer with the inhalation powder

Inhalation: Shake well before use

Pulmonary function tests, blood pressure, pulse, CNS stimulation

May cause nervousness, dizziness, hyperactivity, or insomnia

Salmeterol is a sympathomimetic; use MAOIs and TCAs with caution

No information available to require special precautions

No effects or complications reported

Use exactly as directed (see Administration below). Do not use more often than recommended (excessive use may result in tolerance, overdose may result in serious adverse effects) and do not discontinue without consulting prescriber. Do not use for acute attacks. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience nervousness, dizziness, or fatigue (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth, stomach upset (frequent small meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report unresolved GI upset; dizziness or fatigue; vision changes; chest pain, rapid heartbeat, or palpitations; insomnia; nervousness or hyperactivity; muscle cramping, tremors, or pain; unusual cough; or rash (hypersensitivity). Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Not to be used for the relief of acute attacks. Monitor lung sounds, pulse, blood pressure. Before using, the inhaler must be shaken well. Observe for wheezing after administration; if this occurs, call physician.

Aerosol, oral, as xinafoate: 21 mcg/spray [60 inhalations] (6.5 g), [120 inhalations] (13 g)

Inhaler: 25 mcg/metered inhalation

Powder for inhalation, oral (Serevent® Diskus®): 50 mcg [46 mcg/inhalation] (60 doses)

Bone RC, "Another Word of Caution Regarding a new Long-Acting Bronchodilator," JAMA, 1995, 273(12):967-8.

Brogden RN and Faulds D, "Salmeterol Xinafoate: A Review of Its Pharmacological Properties and Therapeutic Potential in Reversible Obstructive Airways Disease," Drugs, 1991, 42(5):895-912.

Clark CE, Ferguson AD, and Siddorn JA, "Respiratory Arrests in Young Asthmatics on Salmeterol," Respir Med, 1993, 87(3):227-8.

Devoy MA, Fuller RW, and Palmer JB, "Are There any Detrimental Effects of the Use of Inhaled Long-Acting Beta-2-Agonists in the Treatment of Asthma?" Chest, 1995, 107(4):1116-24.

Hatton MQ, Allen MB, Mellor EJ, et al, "Salmeterol Rash," Lancet, 1991, 337(8750):1169-70.

Johnson M, "The Pharmacology of Salmeterol," Lung, 1990, 168(Suppl):115-9.

Meyer JM, Wenzel CL, and Kradjan WA, "Salmeterol: A Novel, Long-Acting Beta₂-Agonist," Ann Pharmacother, 1993, 27(12):1478-87.