AEROLATE SR
Clinical safety rating
cautionComprehensive clinical and safety monograph for AEROLATE SR (AEROLATE SR).
AEROLATE SR is a sustained-release formulation of theophylline, a methylxanthine bronchodilator. It acts by inhibiting phosphodiesterase (PDE) isoenzymes, leading to increased intracellular cyclic AMP (cAMP) levels. This results in relaxation of bronchial smooth muscle and suppression of the response of airways to stimuli. Theophylline also has anti-inflammatory effects, including inhibition of late-phase allergen-induced responses and reduction of eosinophil infiltration.
| Metabolism | Primarily hepatic via cytochrome P450 enzymes (CYP1A2, CYP2E1, and CYP3A4). Theophylline is metabolized to 1,3-dimethyluric acid, 1-methyluric acid, and 3-methylxanthine. |
| Excretion | Renal: 60% as unchanged drug; biliary/fecal: 30% as metabolites; 10% as unchanged in feces. |
| Half-life | Terminal elimination half-life 12 hours (range 10–15 h) in adults; prolonged in hepatic impairment (up to 24 h) and elderly. |
| Protein binding | 55–65% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 0.4–0.6 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral: 90–100% for sustained-release formulation; food decreases rate but not extent (AUC unchanged). |
| Onset of Action | Oral: 30–60 minutes for bronchodilation (peak at 2–4 h). |
| Duration of Action | Sustained-release formulation: 12–24 hours; clinical bronchodilation maintained for 12 h in most patients. |
| Molecular Weight | 206.28 |
400-800 mcg inhaled twice daily. For acute bronchospasm, 200-400 mcg as needed.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | Use with caution in severe hepatic impairment (Child-Pugh class C); consider dose reduction by 50%. |
| Pediatric use | Children 6-12 years: 200-400 mcg inhaled twice daily. Children over 12 years: same as adult dose. |
| Geriatric use | Start at lower end of dosing range (400 mcg twice daily) and titrate to response; monitor for systemic effects. |
| 1st trimester | Category C: Risk cannot be ruled out. Animal reproduction studies have shown an adverse effect on the fetus, but there are no adequate and well-controlled studies in humans. Use only if potential benefit justifies potential risk. |
| 2nd trimester | Category C: Similar risks as first trimester. May cause premature closure of ductus arteriosus in third trimester; avoid use during second trimester if possible. |
| 3rd trimester | Category C/D: Avoid use, especially near term, due to risk of premature closure of ductus arteriosus and inhibition of uterine contractions. |
Clinical note
Comprehensive clinical and safety monograph for AEROLATE SR (AEROLATE SR).
| Placental transfer | Crosses the placenta; fetal concentrations are approximately 0.5-1.5% of maternal serum levels after oral administration. Higher transfer may occur with chronic use or near term. |
| Breastfeeding | Excreted in human milk in low concentrations; adverse effects in nursing infants are unlikely with maternal use at therapeutic doses. However, due to potential NSAID-related adverse effects (e.g., renal dysfunction, gastrointestinal bleeding), caution is advised, especially with prolonged use. The American Academy of Pediatrics considers ibuprofen compatible with breastfeeding. |
| Lactation Rating | L1 (Safer) |
| Teratogenic Risk | Pregnancy Category C. In first trimester: insufficient human data; animal studies show adverse effects at high doses. Second and third trimesters: may cause fetal tachycardia, hypoglycemia, and reduced uterine contractility; avoid use near term due to potential for neonatal bradycardia and hypoglycemia. |
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and serum potassium. Fetal monitoring for heart rate and growth if used chronically. Assess for signs of preterm labor if administered for tocolysis. |
| Fertility Effects | No evidence of impaired fertility in humans. Animal studies show no significant reproductive toxicity at therapeutic doses. |
■ FDA Black Box Warning
No FDA black box warning exists for this drug.
| Serious Effects |
Hypersensitivity to ibuprofen or any NSAIDHistory of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsActive peptic ulcer disease or gastrointestinal bleedingSevere heart failure (NYHA Class IV)Severe renal impairment (CrCl <30 mL/min)Severe hepatic impairment (Child-Pugh Class C)Treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery
| Precautions | Theophylline has a narrow therapeutic index; serum levels must be monitored to avoid toxicity. Toxicity can include seizures, cardiac arrhythmias, and death. Caution in patients with heart failure, hepatic impairment, or those over 55 years. Risk of toxicity increased by concurrent medications such as cimetidine, fluoroquinolones, and macrolides. |
| Food/Dietary | High-fat meals may delay absorption. Avoid charcoal-grilled foods and large amounts of caffeine. Grapefruit juice may increase theophylline levels; limit intake. |
| Clinical Pearls | AEROLATE SR contains theophylline; narrow therapeutic index (10-20 mcg/mL). Monitor serum levels, especially with CYP1A2 inhibitors (e.g., ciprofloxacin, fluvoxamine) or inducers (e.g., carbamazepine, phenytoin). SR formulation avoids peak-trough fluctuations; do not crush or chew. Caution in heart failure, hepatic impairment, and elderly. |
| Patient Advice | Take exactly as prescribed; do not crush or chew the sustained-release tablet. · Do not stop suddenly; sudden withdrawal may worsen breathing. · Avoid excessive caffeine (coffee, tea, chocolate) as it may increase side effects. · Report nausea, vomiting, insomnia, palpitations, or seizures immediately. · Keep regular appointments for blood level monitoring. |
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