Comparative Pharmacology
Head-to-head clinical analysis: AEROLATE SR versus THEOPHYL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AEROLATE SR versus THEOPHYL.
AEROLATE SR vs THEOPHYL
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.
Theophylline is a methylxanthine that causes bronchodilation primarily through inhibition of phosphodiesterase (PDE) and antagonism of adenosine receptors. It also has mild anti-inflammatory effects and enhances mucociliary clearance.
400-800 mcg inhaled twice daily. For acute bronchospasm, 200-400 mcg as needed.
300 mg orally every 6 hours or 400-600 mg extended-release orally every 12-24 hours; intravenous loading dose 5-6 mg/kg over 20-30 minutes, then continuous infusion 0.4-0.6 mg/kg/h
None Documented
None Documented
Clinical Note
moderateTheophylline + Gatifloxacin
"The metabolism of Gatifloxacin can be decreased when combined with Theophylline."
Clinical Note
moderateTheophylline + Rosoxacin
"The metabolism of Rosoxacin can be decreased when combined with Theophylline."
Clinical Note
moderateTheophylline + Levofloxacin
"The metabolism of Levofloxacin can be decreased when combined with Theophylline."
Clinical Note
moderateTheophylline + Trovafloxacin
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: Adults nonsmokers: 6–12 h (mean 8.7 h); adult smokers: 4–5 h; children: 3–5 h; neonates: 20–30 h; hepatic cirrhosis: up to 30 h. Half-life increases with congestive heart failure, fever, and concurrent CYP1A2 inhibitors (e.g., cimetidine, fluvoxamine).
Renal: 60% as unchanged drug; biliary/fecal: 30% as metabolites; 10% as unchanged in feces.
Renal: 10% unchanged in adults (higher in neonates). Hepatic metabolism to inactive metabolites (1,3-dimethyluric acid, 3-methylxanthine, 1-methyluric acid) excreted renally; fecal excretion <5%.
Category C
Category C
Bronchodilator
Bronchodilator
"The metabolism of Trovafloxacin can be decreased when combined with Theophylline."