BRONKODYL
Clinical safety rating
cautionComprehensive clinical and safety monograph for BRONKODYL (BRONKODYL).
Bronkodyl contains theophylline, a xanthine derivative. It acts as a bronchodilator by inhibiting phosphodiesterase, increasing cyclic AMP levels, leading to relaxation of bronchial smooth muscle. Additionally, it blocks adenosine receptors and may have anti-inflammatory effects.
| Metabolism | Primarily hepatic via cytochrome P450 enzymes, mainly CYP1A2 and CYP3A4. Metabolized to 3-methylxanthine, 1-methyluric acid, and 1,3-dimethyluric acid. |
| Excretion | Renal: approximately 90% as theophylline and its metabolites (1,3-dimethyluric acid, 3-methylxanthine, 1-methyluric acid); biliary/fecal: <10%. |
| Half-life | Terminal elimination half-life is 3–8 hours in non-smoking adults, 1–5 hours in smokers, and 20–30 hours in premature neonates; clinical context: half-life increases in hepatic impairment, heart failure, and with certain medications (e.g., cimetidine, fluoroquinolones). |
| Protein binding | Approximately 40% bound to plasma albumin. |
| Volume of Distribution | 0.3–0.7 L/kg; clinical meaning: distributes into total body water, with higher Vd in neonates and patients with hepatic cirrhosis. |
| Bioavailability | Oral (immediate-release): 80–100%; oral (sustained-release): 80–100% (subject to first-pass metabolism); rectal: approximately 80%. |
| Onset of Action | Oral (immediate-release): 30–60 minutes; oral (sustained-release): 60–120 minutes; intravenous: immediate (within minutes). |
| Duration of Action | Oral (immediate-release): 4–6 hours; oral (sustained-release): 8–12 hours; intravenous: 4–6 hours; clinical note: duration is dose-dependent and influenced by clearance. |
| Molecular Weight | 225.28 |
Theophylline extended-release: 300-600 mg orally every 12 hours; target serum concentration 5-15 mcg/mL.
| Dosage form | CAPSULE |
| Renal impairment | For GFR <30 mL/min: reduce dose by 50% and monitor serum levels; for GFR 30-60 mL/min: reduce dose by 25%. |
| Liver impairment | Child-Pugh class B: reduce dose by 50%; Child-Pugh class C: reduce dose by 75% or use alternative agent. |
| Pediatric use | Loading dose: 5-7 mg/kg IV over 30 minutes; maintenance: 0.5-1 mg/kg/hour IV continuous infusion or 10-20 mg/kg/day orally divided every 8-12 hours; adjust to achieve serum levels 5-10 mcg/mL. |
| Geriatric use | Start at lower end of dosing range (300 mg/day) and titrate slowly; monitor serum theophylline levels closely due to reduced clearance. |
| 1st trimester | Insufficient human data; avoid unless potential benefit outweighs risk. Animal studies show no teratogenic effects at therapeutic doses. |
| 2nd trimester | Use with caution if clearly needed; monitor maternal heart rate and blood pressure. |
| 3rd trimester | Use near term may cause tachycardia in the fetus; avoid if delivery is imminent. |
Clinical note
Comprehensive clinical and safety monograph for BRONKODYL (BRONKODYL).
| Placental transfer | Crosses the placenta; limited data suggest fetal concentrations are similar to maternal levels. |
| Breastfeeding | Excreted into breast milk in small amounts; risk of infant stimulation is low at usual maternal doses. However, consider alternative bronchodilators with a better safety profile. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | BRONKODYL (theophylline) is FDA Pregnancy Category C. First trimester: No well-controlled studies; animal studies show no consistent teratogenicity. Second and third trimesters: Possible fetal tachycardia and jitteriness with maternal high doses; risk of neonatal withdrawal if used near term. |
| Fetal Monitoring | Monitor maternal serum theophylline levels (target 5-15 mcg/mL), fetal heart rate and movement patterns, and neonatal heart rate and behavior after delivery. Signs of maternal toxicity: tachycardia, nausea, vomiting, seizures. Signs of fetal/neonatal toxicity: tachycardia, jitteriness, feeding difficulty. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies showed no impairment of fertility at therapeutic doses. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to theophylline or any component of the formulationActive peptic ulcer diseaseSeizure disorder (uncontrolled)
| Precautions | Risk of toxicity due to narrow therapeutic index; monitor serum theophylline levels. Use caution in patients with peptic ulcer, seizure disorders, cardiac arrhythmias, or hepatic impairment. Smoking and certain drugs alter metabolism. |
| Food/Dietary | High-fat meals may delay absorption; take consistently with food to avoid fluctuations. Charcoal-grilled foods and a high-protein, low-carbohydrate diet can increase metabolism of theophylline, reducing efficacy. Avoid concurrent use with caffeine-containing foods/beverages due to additive CNS stimulation. |
| Clinical Pearls | BRONKODYL (theophylline) has a narrow therapeutic index; serum levels should be monitored (target 5-15 mcg/mL). Avoid in patients with active peptic ulcer, seizure disorders, or uncontrolled arrhythmias. Cimetidine, ciprofloxacin, and macrolides increase theophylline levels; smoking and rifampin decrease them. Use with caution in heart failure, hepatic impairment, and in elderly patients, as clearance is reduced. |
| Patient Advice | Take this medication exactly as prescribed; do not double doses if missed. · Avoid consuming large amounts of caffeine (coffee, tea, cola, chocolate) as it may increase side effects. · Report symptoms of toxicity: nausea, vomiting, insomnia, tremors, palpitations, or seizures. · Do not change brands or formulations without consulting your doctor, as bioavailability may differ. · Regular blood tests are necessary to monitor theophylline levels. |
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