THEOCLEAR-80
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for THEOCLEAR-80 (THEOCLEAR-80).
| Breastfeeding | Theophylline excreted into breast milk; milk-to-plasma ratio approximately 0.7. Peak milk levels occur 1-2 hours after dose. Reported infant adverse effects include irritability and jitteriness. Weigh risks vs benefits; monitor infant for signs of theophylline toxicity. Avoid if infant has compromised cardiovascular status. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to theophylline, active seizure disorder, uncontrolled arrhythmias.
| Precautions | Monitor serum theophylline levels due to narrow therapeutic index; risk of toxicity with concurrent medications or conditions affecting metabolism. |
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| 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. |