CHOLEDYL SA
Clinical safety rating
cautionComprehensive clinical and safety monograph for CHOLEDYL SA (CHOLEDYL SA).
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.
| Metabolism | Primarily hepatic via CYP1A2, with minor contributions from CYP2E1 and CYP3A4; exhibits nonlinear pharmacokinetics at higher concentrations. |
| Excretion | Renal: 90% as unchanged drug and metabolites (theophylline metabolites including 1,3-dimethyluric acid, 3-methylxanthine, and 1-methyluric acid). Biliary/fecal: <10%. |
| Half-life | 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. |
| Protein binding | 55-60% bound, primarily to albumin. |
| Volume of Distribution | 0.45 L/kg (0.3-0.7 L/kg). Reflects distribution into total body water, with lower Vd in obese patients when adjusted for ideal body weight. |
| Bioavailability | Oral: 100% for choline theophyllinate (Choledyl) as it is completely absorbed; the sustained-action formulation (Choledyl SA) has equivalent bioavailability to immediate-release. |
| Onset of Action | Oral: Peak bronchodilation occurs 1-2 hours post-dose; clinical effect may begin within 30 minutes. |
| Duration of Action | Duration: 8-12 hours for sustained-action formulation (Choledyl SA). Clinical note: Requires monitoring of serum theophylline levels (target 10-20 mcg/mL) to maintain efficacy and avoid toxicity. |
| Molecular Weight | 283.33 |
400 mg orally every 12 hours (sustained-release); maximum 800 mg every 12 hours.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 50-80 mL/min: 50% of usual dose; GFR <50 mL/min: avoid use due to accumulation of choline and theophylline. |
| Liver impairment | Child-Pugh A: 50% of usual dose; Child-Pugh B: 25% of usual dose; Child-Pugh C: contraindicated. |
| Pediatric use | Not recommended for use in children under 12 years due to lack of safety data. |
| Geriatric use | Initiate at 400 mg every 12 hours; titrate slowly with monitoring of serum theophylline levels due to reduced clearance. |
| 1st trimester | Limited data; use only if clearly needed. No known teratogenicity in animal studies. |
| 2nd trimester | Use with caution; monitor for maternal tachycardia and fetal effects. |
| 3rd trimester | Avoid near term due to risk of neonatal jitteriness and tachycardia. |
Clinical note
Comprehensive clinical and safety monograph for CHOLEDYL SA (CHOLEDYL SA).
| Placental transfer | Crosses placenta; detectable in fetal serum at levels similar to maternal. |
| Breastfeeding | Choledyl (oxtriphylline) is excreted into breast milk in small amounts. Use with caution; monitor infant for irritability and sleep disturbances. Consider alternative therapies. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category C. No adequate studies in pregnant women. In animal studies, theophylline (active metabolite) caused fetal toxicity at high doses. First trimester: risk unknown; use only if benefit outweighs risk. Second/third trimester: possible fetal tachycardia and irritability; avoid near term due to potential neonatal apnea, jitteriness, and withdrawal symptoms. |
| Fetal Monitoring | Monitor maternal serum theophylline levels (target 5-15 mcg/mL), pulmonary function tests, and signs of toxicity (nausea, tachycardia, arrhythmias). Fetal monitoring: heart rate assessment for tachycardia; consider non-stress test if maternal levels high or signs of toxicity. Preterm infants: risk of apnea and bradycardia. |
| Fertility Effects | Limited data. Theophylline may affect uterine contractility; no direct evidence of impaired fertility in humans. Animal studies showed no significant reproductive toxicity at doses used clinically. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to oxtriphylline or other xanthinesAcute myocardial infarctionHypertrophic obstructive cardiomyopathySeizure disorder (unless adequately controlled)
| Precautions | Theophylline has narrow therapeutic index; serum levels must be monitored to avoid toxicity (toxicity risk increases above 20 mcg/mL)., Concomitant use with other xanthines may potentiate toxicity., Use with caution in patients with cardiovascular disease (e.g., arrhythmias), seizure disorders, hepatic impairment, or peptic ulcer disease., Drug interactions: CYP1A2 inhibitors (e.g., ciprofloxacin, fluvoxamine) increase theophylline levels; CYP1A2 inducers (e.g., phenytoin, rifampin) decrease levels., Risk of hypokalemia and hypophosphatemia with high doses or prolonged use. |
| Food/Dietary | Avoid high-fat meals that may alter absorption. Caffeine (coffee, tea, cola, chocolate) potentiates adverse effects. Charcoal-broiled foods can increase theophylline metabolism. |
| Clinical Pearls | Choledyl SA (oxtriphylline) is a sustained-release theophylline salt. Monitor serum theophylline levels (target 5-15 mcg/mL). Avoid in active peptic ulcer disease and seizure disorders. Cigarette smoking induces metabolism, requiring dose adjustments. Use with caution in patients with hepatic impairment, cardiac disease, or hypothyroidism. |
| Patient Advice | Take exactly as prescribed; do not crush or chew the sustained-release tablets. · Avoid excessive consumption of caffeine-containing foods and beverages (coffee, tea, cola, chocolate) as they may increase side effects. · Notify your doctor if you experience nausea, vomiting, insomnia, rapid heart rate, or seizures. · Do not stop taking abruptly; dose tapering may be needed. · Inform your doctor if you smoke or stop smoking, as dose adjustments may be required. |
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