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QuickView for salmeterol (compound)

Name: salmeterol
PubChem Compound ID: 10788224
Molecular formula: C25H37NO4
Molecular weight: 419.577 g/mol
Name: salmeterol
Name (isomeric): DB00938
Drug Type: small molecule
Salmeterolum [Latin]
Brand: Serevent, Salmetedur, Fujimycin, Astmerole, Arial, Aeromax
Brand name mixture: Advair 250 Diskus(Fluticasone Propionate + Salmeterol Xinafoate), Advair 250(Fluticasone Propionate + Salmeterol Xinafoate), Advair 100 Diskus(Fluticasone Propionate + Salmeterol Xinafoate), Advair 500 Diskus(Fluticasone Propionate + Salmeterol Xinafoate), Advair 125(Fluticasone Propionate + Salmeterol Xinafoate)
Category: Sympathomimetic, Adrenergic beta-Agonists, Bronchodilator Agents
CAS number: 89365-50-4
Indication: For the treatment of asthma and chronic obstructive pulmonary disease (COPD).
Salmeterol is a long acting beta2-adrenoceptor agonist (LABA), usually only prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed concurrently with a corticosteroid, such as beclometasone. The primary noticable difference of salmeterol to salbutamol is that the dur...
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Mechanism of Action:
Salmeterol's long, lipophilic side chain binds to exosites near beta(2)-receptors in the lungs and on bronchiolar smooth muscle, allowing the active portion of the molecule to remain at the receptor site, continually binding and releasing. Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and in...
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Absorption: Because of the small therapeutic dose, systemic levels of salmeterol are low or undetectable after inhalation of recommended doses.
Protein binding: 96%
Biotransformation: Hepatic, metabolized by hydroxylation via CYP3A4
Half Life: 5.5 hours
Toxicity: Symptoms of overdose include angina (chest pain), dizziness, dry mouth, fatigue, flu-like symptoms, headache, heart irregularities, high or low blood pressure, high blood sugar, insomnia, muscle cramps, nausea, nervousness, rapid heartbeat, seizures, and tremor. By the oral route, no deaths occurred in rats at 1,000 mg/kg (approximately 81,000 times the maximum recommended daily inhalation dose in adults and approximately 38,000 times the maximum recommended daily inhalation dose in children on a mg/m2 basis).
Affected organisms: Humans and other mammals
Drug interaction:
TelithromycinTelithromycin may reduce clearance of Salmeterol. Concomitant therapy is contraindicated.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor may increase the serum concentration of salmeterol by decreasing its metabolism. Consider alternate therapy.
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