OXTRIPHYLLINE PEDIATRIC
Clinical safety rating
cautionComprehensive clinical and safety monograph for OXTRIPHYLLINE PEDIATRIC (OXTRIPHYLLINE PEDIATRIC).
Xanthine derivative that inhibits phosphodiesterase, increasing cyclic AMP levels; antagonizes adenosine receptors, leading to bronchodilation, central nervous system stimulation, and positive inotropic effects.
| Metabolism | Hepatic via CYP1A2, CYP2E1, and CYP3A4; major metabolite is 1-methyl-3-propylxanthine; exhibits non-linear kinetics at high doses. |
| Excretion | Renal (70-80% as unchanged drug, 10-15% as metabolites); biliary/fecal (<10%) |
| Half-life | Neonates: 24-36 hours; Infants 1-6 months: 14-29 hours; Children 6-12 months: 9-18 hours; Children 1-9 years: 3-6 hours; Adults: 7-12 hours. Half-life prolonged in hepatic impairment, CHF, and COPD. |
| Protein binding | 55-65% (primarily albumin). |
| Volume of Distribution | 0.4-0.6 L/kg (increased in premature neonates and hepatic disease). |
| Bioavailability | Oral immediate-release: 90-100%; Sustained-release: 80-95% (relative to immediate-release). |
| Onset of Action | Oral (immediate-release): 30-60 minutes on empty stomach; 60-90 minutes with food. Intravenous: 15-30 minutes. |
| Duration of Action | Oral (immediate-release): 4-6 hours; Sustained-release: 8-12 hours. Variable with formulation and individual metabolism. |
| Molecular Weight | 283.33 |
200 mg orally every 6-8 hours; extended-release: 400-600 mg orally every 12 hours.
| Dosage form | SYRUP |
| Renal impairment | No specific guidelines; consider dose reduction in severe renal impairment (GFR <30 mL/min) to avoid accumulation. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: reduce dose by 75% or avoid use. |
| Pediatric use | 1-9 years: 4 mg/kg/dose orally every 6 hours; 9-16 years: 3 mg/kg/dose orally every 6 hours; adjust based on serum theophylline levels (target 5-15 mcg/mL). |
| Geriatric use | Start at 200 mg orally every 12 hours (extended-release) and titrate slowly; monitor serum theophylline levels closely due to reduced clearance. |
| 1st trimester | Limited human data; animal studies show some teratogenicity at high doses. Use only if clearly needed. |
| 2nd trimester | Use with caution; may increase fetal heart rate and cause irritability. |
| 3rd trimester | Use with caution near term; may cause neonatal jitteriness, tachycardia, and vomiting. |
Clinical note
Comprehensive clinical and safety monograph for OXTRIPHYLLINE PEDIATRIC (OXTRIPHYLLINE PEDIATRIC).
| Placental transfer | Crosses placenta; cord blood levels similar to maternal serum levels. |
| Breastfeeding | Oxtriphylline is the choline salt of theophylline; excreted into breast milk in small amounts. Infant serum levels are generally low (<10% of maternal levels). Monitor infant for irritability or insomnia. Consider benefits vs. risks. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Oxtriphylline, a theophylline derivative, is classified as pregnancy category C. First trimester: Limited data, no known major malformations in humans; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: No specific risks, but maternal respiratory depression and fetal tachycardia may occur with high doses. Perinatal: Apnea, irritability, and jitteriness reported in neonates due to transplacental passage. |
| Fetal Monitoring | Maternal: Serum theophylline levels (target 5-15 mcg/mL), heart rate, respiratory rate, signs of toxicity (tachycardia, nausea, seizures). Fetal/neonatal: Heart rate monitoring for tachycardia (maternal high levels), assessment for apnea or irritability in newborns if exposed near term. |
| Fertility Effects | No evidence of impaired fertility in humans. Animal studies: No adverse effects on reproductive function at therapeutic doses. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
Hypersensitivity to oxtriphylline or theophyllineActive peptic ulcer diseaseSeizure disorder (unless adequately controlled)
| Precautions | Risk of toxicity (seizures, cardiac arrhythmias) at serum levels >20 mcg/mL, Reduce dose in hepatic impairment, heart failure, and with drugs that inhibit metabolism (e.g., cimetidine, ciprofloxacin), Monitor serum theophylline concentrations |
| Food/Dietary | Avoid large amounts of caffeine-containing foods and beverages (coffee, tea, cola, chocolate). High-fat meals may delay absorption; consistency in timing relative to meals is recommended. Charcoal-broiled foods and a high-protein diet may increase theophylline clearance, reducing efficacy. |
| Clinical Pearls | Oxtriphylline is the choline salt of theophylline, providing 64% anhydrous theophylline by weight. Monitor serum theophylline levels, maintaining therapeutic range 5-15 mcg/mL. Avoid in patients with active peptic ulcer disease or seizure disorders unless on anticonvulsants. Taper dose to avoid rebound bronchospasm. Use with caution in hepatic impairment, COPD, and elderly, as clearance is reduced. |
| Patient Advice | Take this medication exactly as prescribed; do not crush or chew extended-release tablets. · Avoid taking with large amounts of caffeine (coffee, tea, cola, chocolate) as it may increase side effects like nausea, jitteriness, and insomnia. · Report symptoms of toxicity: persistent nausea, vomiting, severe headache, rapid or irregular heartbeat, or seizures. · Do not change brands or formulations without consulting your healthcare provider. · Inform all healthcare providers that you are taking this medication. |
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