Comparative Pharmacology
Head-to-head clinical analysis: AEROLATE SR versus THEO DUR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AEROLATE SR versus THEO DUR.
AEROLATE SR vs THEO-DUR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
AEROLATE SR is a sustained-release formulation of theophylline, a methylxanthine bronchodilator. It acts by inhibiting phosphodiesterase (PDE) isoenzymes, leading to increased intracellular cyclic AMP (cAMP) levels. This results in relaxation of bronchial smooth muscle and suppression of the response of airways to stimuli. Theophylline also has anti-inflammatory effects, including inhibition of late-phase allergen-induced responses and reduction of eosinophil infiltration.
Inhibits phosphodiesterase, increasing cAMP levels; antagonizes adenosine receptors; enhances contractility of skeletal and cardiac muscle, and relaxes bronchial smooth muscle.
400-800 mcg inhaled twice daily. For acute bronchospasm, 200-400 mcg as needed.
300-600 mg orally twice daily
None Documented
None Documented
Terminal elimination half-life 12 hours (range 10–15 h) in adults; prolonged in hepatic impairment (up to 24 h) and elderly.
Terminal elimination half-life: 3-9 hours in adults (smokers: 4-5 hours; nonsmokers: 6-9 hours); 20-30 hours in premature neonates; 1-5 hours in children. Prolonged in hepatic cirrhosis, heart failure, and with CYP1A2 inhibitors.
Renal: 60% as unchanged drug; biliary/fecal: 30% as metabolites; 10% as unchanged in feces.
Primarily hepatic metabolism by CYP1A2 and CYP3A4; renal excretion of unchanged drug accounts for approximately 10% in adults, up to 50% in neonates; biliary/fecal excretion negligible.
Category C
Category C
Bronchodilator
Bronchodilator