THEOPHYLLINE 0.08% AND DEXTROSE 5% IN PLASTIC CONTAINER
Clinical safety rating: safe
Many drugs can increase (eg ciprofloxacin) or decrease (eg phenytoin) levels due to CYP1A2 metabolism Has a narrow therapeutic index and can cause seizures and arrhythmias in overdose.
Theophylline is a xanthine derivative that inhibits phosphodiesterase, leading to increased intracellular cAMP. It also antagonizes adenosine receptors, resulting in bronchodilation, anti-inflammatory effects, and stimulation of respiratory drive.
| Metabolism | Hepatic via CYP1A2 and CYP3A4; also by N-demethylation and oxidation. Significant interindividual variability. |
| Excretion | Renal (90% as metabolites, 10% unchanged). Biliary/fecal minimal. |
| Half-life | Adults: 6-12 h (mean 8.7 h); children: 3-5 h; neonates: 24-36 h. Prolonged in hepatic impairment, heart failure, COPD. |
| Protein binding | ~40% to albumin. |
| Volume of Distribution | 0.3-0.7 L/kg (total body water). Lower in premature infants. |
| Bioavailability | Oral: 96-100% (immediate-release). IV: 100%. |
| Onset of Action | Intravenous: 5-15 min; oral immediate-release: 30-60 min; oral extended-release: 2-4 h. |
| Duration of Action | Intravenous: 4-6 h; oral immediate-release: 6-8 h; oral extended-release: 8-12 h (up to 24 h with once-daily formulations). |
Adults: 0.4-0.6 mL/kg/hr intravenously continuous infusion, adjusted to achieve serum theophylline concentration of 10-20 mcg/mL. Loading dose: 5 mg/kg IV if no prior theophylline use.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment. However, use with caution in patients with renal failure due to risk of accumulation; monitor serum concentrations. |
| Liver impairment | Child-Pugh Class A: Reduce dose by 50%; Class B: Reduce dose by 75%; Class C: Avoid use or reduce by 80-90% with close monitoring. |
| Pediatric use | Infants <1 year: 0.2-0.5 mL/kg/hr; Children 1-9 years: 0.8-1.2 mL/kg/hr; Children 9-12 years: 0.6-0.8 mL/kg/hr; Adolescents 12-16 years: 0.5-0.7 mL/kg/hr IV continuous infusion, adjusting to serum levels of 5-15 mcg/mL. |
| Geriatric use | Elderly >60 years: Reduce initial infusion rate by 30-50% (e.g., 0.3-0.4 mL/kg/hr) due to decreased clearance; monitor serum concentrations closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Many drugs can increase (eg ciprofloxacin) or decrease (eg phenytoin) levels due to CYP1A2 metabolism Has a narrow therapeutic index and can cause seizures and arrhythmias in overdose.
| FDA category | Animal |
| Breastfeeding | Theophylline is excreted into breast milk (M/P ratio approximately 0.7). Infant dose is 1-2% of maternal weight-adjusted dose. May cause irritability or jitteriness in breastfed infants. Use with caution and monitor infant for signs of toxicity. |
| Teratogenic Risk |
■ FDA Black Box Warning
No FDA boxed warning specific to this formulation. However, theophylline has a narrow therapeutic index and requires monitoring for toxicity.
| Common Effects | COPD |
| Serious Effects |
["Hypersensitivity to theophylline or any component","Active seizure disorder not controlled by medication","Life-threatening cardiac arrhythmias (e.g., ventricular tachycardia)"]
| Precautions | ["Risk of serious or fatal toxicity if serum levels exceed therapeutic range (5-15 mcg/mL)","Increased seizure risk, especially in patients with pre-existing seizure disorders","Cardiac arrhythmias, including ventricular tachycardia and atrial fibrillation","Hypokalemia and hypercalcemia may occur","Use with caution in patients with peptic ulcer disease, hyperthyroidism, or hepatic impairment"] |
Loading safety data…
| Theophylline crosses the placenta. First trimester: No increased risk of major malformations in large cohort studies. Second and third trimesters: Associated with fetal tachycardia, jitteriness, and withdrawal symptoms in neonates exposed near term. Use only if clearly needed. |
| Fetal Monitoring | Monitor maternal serum theophylline concentrations, respiratory status, heart rate, and symptoms of toxicity. Fetal monitoring for heart rate and growth. Neonatal monitoring for jitteriness, tachycardia, and withdrawal if used near term. |
| Fertility Effects | No well-documented effects on human fertility. In animal studies, high doses caused reduced fertility; clinical significance unknown. |