Comparative Pharmacology
Head-to-head clinical analysis: CHOLEDYL SA versus THEOPHYL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CHOLEDYL SA versus THEOPHYL.
CHOLEDYL SA vs THEOPHYL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Choledyl SA (theophylline, sustained-release) is a methylxanthine that inhibits phosphodiesterase, increasing intracellular cAMP, and blocks adenosine receptors, leading to bronchodilation and anti-inflammatory effects.
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 mg orally every 12 hours (sustained-release); maximum 800 mg every 12 hours.
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: 7-9 hours in healthy adults; prolonged in hepatic cirrhosis (up to 30 hours), heart failure, COPD, and in neonates; shortened in smokers and cystic fibrosis.
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: 90% as unchanged drug and metabolites (theophylline metabolites including 1,3-dimethyluric acid, 3-methylxanthine, and 1-methyluric acid). Biliary/fecal: <10%.
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."