Salmeterol

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Serevent; Belgium: Serevent; Bulgaria: Serevent; Cyprus: Serevent; Czech Republic: Serevent; Denmark: Serevent; Estonia: Serevent; Finland: Serevent; France: Serevent; Germany: Aeromax, Salmemax, Salmet, Salmetan, Salmeterol, Salmetol, Salmex, Salmexide, Serevent; Greece: Serevent; Hungary: Serevent; Ireland: Serevent; Italy: Arial, Salmetedur, Serevent; Latvia: Serevent; Lithuania: Salmeterol, Serevent; Luxembourg: Serevent; Malta: Serevent; Netherlands: Salmeterol, Serevent; Poland: Pulmoterol, Salmetik, Serevent; Portugal: Dilamax, Serevent, Ultrabeta; Romania: Serevent; Slovakia: Serevent; Slovenia: Serevent; Spain: Beglan, Betamican, Inaspir, Serevent; Sweden: Serevent; UK: Serevent.

North America

Canada: Serevent; USA: Serevent.

Latin America

Argentina: Serevent; Brazil: Serevent; Mexico: Serevent.

Asia

Japan: Serevent.

Drug combinations

Salmeterol and Fluticasone

Chemistry

Salmeterol: C~25~H~37~NO~4~. Mw: 415.57. 1,3-Benzenedimethanol, 4-hydroxy-α^1^-[[[6-(4-phenylbutoxy)hexyl]amino]methyl-, (±)-. CAS-89365-50-4 (1985).

Salmeterol Xinafoate: C~25~H~37~NO~4~.C~11~H~8~O~3~. Mw:603.75. 1,3-Benzenedimethanol, 4-hydroxy-α1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-, (±)-, 1-hydroxy-2-naphthalenecarboxylate; CAS-94749-08-3 (1990).

Pharmacologic Category

Sympathomimetic (Adrenergic) Agents; Selective β~2~-Adrenergic Agonists. Long-Acting β~2~-Adrenergic Agonist. (ATC-Code: R03AC12).

Mechanism of action

A long-acting, synthetic, sympathomimetic amine bronchodilator. Stimulates β~2~-adrenergic receptors, with little or no effect on α-, β~1~-, or β~3~-adrenergic receptors. Increases concentrations of cAMP. Relaxes bronchial smooth muscle, suppresses some aspects of inflammation, and stimulates airway epithelial ciliary function. Decreases airway resistance and airway reactivity to histamine. Inhibits release of proinflammatory mediators (e.g. histamine, leukotrienes C~4~ and D~4~, prostaglandin D~2~) in human lung tissue. Has little effect on heart rate.

Therapeutic use

Maintenance treatment of asthma. Prevention of bronchospasm with reversible obstructive airway disease. Prevention of exercise-induced bronchospasm. Maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease.

Pregnancy and lactiation implications

Animal studies demonstrated (dose-dependent) teratogenicity. There are no adequate studies in pregnant women. β-Agonists may interfere with uterine contractility if administered during labor. Use only if clearly needed. Enters breast milk (use with caution in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to salmeterol or any component of the formulation.

Warnings and precautions

Long-acting β~2~-agonists may increase risk of asthma-related deaths. Rarely, paradoxical bronchospasm may occur with use of inhaled bronchodilating agents. Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm) reported. Reports exist of laryngeal spasm, irritation, and swelling (stridor, choking) with use. Do not use for acute asthmatic symptoms. Do not initiate in significantly worsening or acutely deteriorating asthma (severe respiratory events reported). Salmeterol should only be used as adjuvant therapy in patients not adequately controlled on inhaled corticosteroids or whose disease requires two maintenance therapies. Corticosteroids should not be stopped or reduced when salmeterol is initiated. Salmeterol not a substitute for inhaled or systemic corticosteroids and should not be used as monotherapy. Use with caution in cardiovascular disease (β-agonists may cause elevation in blood pressure, heart rate and result in CNS stimulation/excitation; may also increase risk of arrhythmias). Use with caution in diabetes mellitus (may increase serum glucose). Use with caution in glaucoma (may elevate intraocular pressure). Use with caution in hepatic impairment. Use with caution in hyperthyroidism (may stimulate thyroid activity). Use with caution in hypokalemia (β~2~-agonists may decrease serum potassium). Use with caution in seizure disorders. Powder for oral inhalation contains lactose (risk of anaphylactic reactions). Salmeterol should not be used more than twice daily (do not use with other long-acting β~2~-agonists).

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