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RESPIRATORY SYSTEM › DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES › OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES › Xanthines
aminophylline
R03DA05
Forms & Strengths
- Injection: 250 mg/10 mL (25 mg/mL)
- Oral liquid: 105 mg/5 mL
Adult Dosing
- Acute bronchospasm (IV): Loading dose 5 mg/kg over 20-30 minutes, followed by maintenance infusion.
- Maintenance (IV): 0.5-0.7 mg/kg/hour adjusted based on serum concentrations (target 10-20 mcg/mL).
- Oral: 250-500 mg every 6-8 hours.
Pediatric Dosing
- Acute bronchospasm (IV, ages 1-9 years): Loading dose 5 mg/kg, maintenance 1 mg/kg/hour.
- Acute bronchospasm (IV, ages >9 years): Loading dose 5 mg/kg, maintenance 0.8 mg/kg/hour.
- Neonatal apnea: Loading dose 5 mg/kg (as aminophylline), maintenance 1-2 mg/kg every 8-12 hours.
Indications
- Reversible airflow obstruction associated with asthma and chronic obstructive pulmonary disease (COPD)
- Apnea of prematurity
Mechanism of Action
- Non-selective phosphodiesterase (PDE) inhibitor increasing intracellular cAMP, leading to bronchial smooth muscle relaxation.
- Competitive antagonist at adenosine receptors, contributing to central respiratory stimulation and bronchodilation.
Contraindications
- Hypersensitivity to aminophylline, theophylline, or ethylenediamine
- Active peptic ulcer disease
- Uncontrolled seizure disorders
Adverse Reactions
- Tachycardia, palpitations, arrhythmias
- Nervousness, tremor, headache, insomnia
- Nausea, vomiting, dyspepsia, gastroesophageal reflux
- Seizures and severe hypotension in toxicity
Drug Interactions
- CYP1A2 inhibitors (e.g., cimetidine, ciprofloxacin, erythromycin) increase theophylline levels.
- CYP1A2 inducers (e.g., rifampin, carbamazepine, smoking) decrease theophylline levels.
- Lithium clearance is increased, leading to reduced lithium efficacy.
- Beta-blockers may antagonize the bronchodilating effects of aminophylline.
Curated Content: Needs Vetting Before Put to Clinical Use