THEOLAIR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for THEOLAIR (THEOLAIR).
Theophylline, the active ingredient in THEOLAIR, is a phosphodiesterase inhibitor that increases intracellular cAMP levels, leading to bronchodilation via smooth muscle relaxation. It also has anti-inflammatory effects and may enhance diaphragmatic contractility.
| Metabolism | Primarily hepatic via CYP1A2 and CYP3A4; also metabolized by N-demethylation and oxidation. Approximately 10% excreted unchanged in urine. |
| Excretion | Renal (10% unchanged); hepatic metabolism (90%) with metabolites excreted in urine |
| Half-life | Adults: 3-8 hours (mean 5.5); children: 1.5-5 hours; increased in hepatic cirrhosis, heart failure, and COPD; decreased in smokers |
| Protein binding | 40% bound, primarily to albumin |
| Volume of Distribution | 0.45 L/kg; approximates total body water; higher in infants |
| Bioavailability | Oral: 96% (immediate release); sustained release: 80-100% |
| Onset of Action | Oral: 15-30 min (non-sustained release); sustained release: 1-2 hours; IV: immediate |
| Duration of Action | Oral immediate release: 4-6 hours; sustained release: 8-12 hours; IV: varies with infusion rate |
Initial dose: 300 mg orally every 8-12 hours; titrate based on serum theophylline levels to achieve 5-15 mcg/mL. Maintenance: 400-600 mg/day in divided doses.
| Dosage form | TABLET |
| 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: reduce dose by 50%. Class C: reduce dose by 75% or use alternative. |
| Pediatric use | Children 1-9 years: starting dose 10-16 mg/kg/day orally in divided doses every 4-6 hours; max 600 mg/day. Children 9-16 years: 10-16 mg/kg/day; max 800 mg/day. Adjust based on serum levels (5-15 mcg/mL). |
| Geriatric use | Start at lower end of dosing range (300 mg/day), titrate slowly with close monitoring of serum levels due to decreased clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for THEOLAIR (THEOLAIR).
| Breastfeeding | Theophylline is excreted into breast milk with a milk-to-plasma (M/P) ratio of approximately 0.72. Concentrations in milk are about 60% of maternal serum. Breastfeeding is generally considered safe if maternal levels are therapeutic; however, irritability and insomnia in infants have been reported. Monitor infant for signs of caffeine-like effects. Use with caution, especially in preterm infants. |
| Teratogenic Risk | Theophylline (active ingredient in THEOLAIR) is classified as FDA Pregnancy Category C. Human data do not indicate a major teratogenic risk; however, a small increased risk of congenital anomalies cannot be excluded. First trimester: No consistent evidence of teratogenicity; some studies suggest possible association with cardiac defects. Second/third trimester: May cause fetal tachycardia, irritability, and jitteriness due to transplacental passage; neonatal withdrawal symptoms possible. Avoid use near term if possible. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to theophylline or any component of the formulation","Active peptic ulcer disease","Uncontrolled seizure disorders"]
| Precautions | ["Narrow therapeutic index; monitor serum theophylline levels to avoid toxicity.","Risk of serious cardiovascular events (e.g., arrhythmias, seizures) at high serum concentrations.","May exacerbate peptic ulcer disease.","Use caution in patients with hypoxemia, hypertension, or heart failure.","Drug interactions: cimetidine, fluoroquinolones, macrolides, and other CYP450 inhibitors increase levels; phenytoin, rifampin, and smoking decrease levels."] |
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| Fetal Monitoring | Monitor maternal serum theophylline levels (target 5–15 mcg/mL), heart rate, and respiratory status. Monitor fetal heart rate for tachycardia. Perform ultrasound for fetal growth and anatomy if used in first trimester. Assess neonatal vital signs and behavior after delivery. |
| Fertility Effects | No known adverse effects on fertility in humans. Animal studies have not shown impaired fertility. Theophylline does not appear to affect ovulation or spermatogenesis. However, uncontrolled asthma may impair maternal and fetal outcomes. |