THEOCLEAR-80
Clinical safety rating
cautionComprehensive clinical and safety monograph for THEOCLEAR-80 (THEOCLEAR-80).
Inhibits phosphodiesterase, increasing cAMP levels, leading to bronchodilation and reduced airway inflammation.
| Metabolism | Primarily hepatic via CYP1A2 and to a lesser extent CYP3A4. |
| Excretion | Renal: approximately 10% unchanged; hepatic metabolism accounts for ~90% of elimination; metabolites excreted in urine. |
| Half-life | 3–8 hours in adults (mean ~5 h); prolonged in heart failure, liver disease, and COPD; decreased in smokers (4–5 h) and children. |
| Protein binding | Approximately 40% bound, primarily to albumin. |
| Volume of Distribution | 0.3–0.7 L/kg (mean 0.45 L/kg); approximates total body water. |
| Bioavailability | Oral: 96–100% (immediate-release); food may affect rate but not extent. |
| Onset of Action | Oral immediate-release: 30–60 min; IV: within 15 min. |
| Duration of Action | Oral immediate-release: 4–6 h; sustained-release: 8–12 h; duration varies with formulation and metabolism. |
| Molecular Weight | 180.16 |
Oral: 400-800 mg every 6-8 hours; extended-release formulation given every 12 hours. Target serum concentration 10-20 mcg/mL.
| Dosage form | SYRUP |
| Renal impairment | GFR <30 mL/min: reduce dose by 50% and monitor serum levels. GFR 30-50 mL/min: reduce dose by 25%. |
| Liver impairment | Child-Pugh Class B or C: reduce dose by 50% and monitor levels; contraindicated in severe hepatic impairment. |
| Pediatric use | Weight-based: 5-10 mg/kg/dose every 6 hours; maximum 300 mg/day for infants <1 year, 600 mg/day for children 1-9 years, 800 mg/day for adolescents. |
| Geriatric use | Start at lowest effective dose; monitor serum levels closely due to reduced clearance; maximum 400 mg/day initially, titrate slowly. |
| 1st trimester | Theophylline crosses the placenta. Use only if clearly needed. Limited human data but no evidence of major malformations. Risk of neonatal toxicity if used near term. |
| 2nd trimester | Continue if necessary for maternal asthma control. Monitor maternal serum levels to avoid toxicity. |
| 3rd trimester | Use with caution; neonatal effects including irritability, jitteriness, and transient tachypnea have been reported. Consider fetal heart rate monitoring if high doses are used. |
Clinical note
Comprehensive clinical and safety monograph for THEOCLEAR-80 (THEOCLEAR-80).
| Placental transfer | Theophylline crosses the placenta readily, achieving fetal serum concentrations similar to maternal levels. |
| Breastfeeding | Theophylline is excreted into breast milk in small amounts (approximately 10% of maternal serum concentration). Caution is advised, especially in premature infants or those with impaired hepatic function. Monitor infant for signs of irritability or sleep disturbance. |
| Lactation Rating | L2 (Probably Compatible) |
| Teratogenic Risk | Theophylline (THEOCLEAR-80) is FDA Pregnancy Category C. In first trimester, no well-controlled studies; animal studies show increased fetal resorptions and delayed skeletal ossification at high doses. Second and third trimesters: possible increased risk of fetal tachycardia and jitteriness due to placental transfer; neonatal theophylline levels approximate maternal levels. Avoid use unless clearly needed. |
| Fetal Monitoring | Monitor maternal serum theophylline levels (target 5-15 mcg/mL), respiratory status, heart rate, and symptoms of toxicity (nausea, vomiting, tachycardia, arrhythmias). Fetal monitoring: assess fetal heart rate and growth via ultrasound; evaluate for fetal tachycardia. Neonatal monitoring: observe for irritability, jitteriness, tachycardia after delivery. |
| Fertility Effects | Theophylline has not been reported to significantly impair fertility in humans. Animal studies have not shown adverse effects on fertility at therapeutic doses. No known impact on oogenesis or spermatogenesis. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to theophylline or any component of the formulationAcute porphyriaSevere tachyarrhythmiasUncontrolled seizuresActive peptic ulcer diseaseHistory of seizure disorder (unless adequately controlled)
| Precautions | Monitor serum theophylline levels due to narrow therapeutic index; risk of toxicity with concurrent medications or conditions affecting metabolism. |
| Food/Dietary | Avoid large amounts of caffeine-containing foods and beverages (coffee, tea, chocolate, cola). Charcoal-broiled foods may reduce theophylline absorption. High-protein, low-carbohydrate diets may alter clearance. Grapefruit juice may increase theophylline levels; avoid concurrent use. |
| Clinical Pearls | Theophylline (THEOCLEAR-80) has a narrow therapeutic index (10-20 mcg/mL). Monitor serum levels closely, especially in patients with hepatic impairment, heart failure, or those on drugs that alter its metabolism (e.g., ciprofloxacin, cimetidine, fluvoxamine). Smoking induces metabolism, requiring higher doses. Do not crush or chew extended-release tablets. |
| Patient Advice | Take this medication exactly as prescribed, usually every 12 hours for extended-release forms. · Do not crush, chew, or break the tablets; swallow them whole. · Avoid excessive caffeine intake (coffee, tea, chocolate, cola) as it may increase side effects. · Notify your doctor if you experience nausea, vomiting, insomnia, palpitations, or seizures. · Do not stop taking this medicine abruptly without consulting your doctor. · Keep a consistent schedule and do not change brands or formulations without medical advice. |
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