Generic
Theophylline
48 brands available in the market
At a glance
Theophylline is a bronchodilator used for the prevention and treatment of asthma and COPD. It relaxes bronchial smooth muscle by inhibiting phosphodiesterase and widens airways.
Description
Theophylline is a methylxanthine bronchodilator that competitively inhibits phosphodiesterase, increasing intracellular cAMP. It relaxes bronchial smooth muscle, increases diaphragmatic muscle contraction force, and suppresses airway response to stimuli.
Indications
- Control of acute asthma
- Management of chronic asthma (symptomatic and prophylactic)
- Control of nocturnal asthma and early morning wheezing
- Management of COPD (chronic bronchitis and emphysema)
- Control of apnea of prematurity
Therapeutic class
Bronchodilators
Pharmacological class
Methylxanthine
Pharmacology
Theophylline inhibits phosphodiesterase, increasing intracellular cAMP, which relaxes bronchial smooth muscle and dilates airways. It also increases diaphragmatic muscle contraction force and reduces airway hyperreactivity.
Mechanism of action
Relaxes bronchial smooth muscle and dilates airways by inhibiting phosphodiesterase.
Dosage
Adult Dose (Oral):
- Loading dose: 5 mg/kg (if no prior theophylline)
- Maintenance: 10-16 mg/kg/day
- Start: 300-400 mg/day (1-2 divided doses); after 3 days increase to 400-600 mg/day if tolerated; max 600 mg/day
- SR/CR: 200/300 mg every 12 hours; 400 mg once daily in the evening
Pediatric Dose (Oral):
- 1.5-6 months: 10 mg/kg/day (divided)
- 6-12 months: 12-18 mg/kg/day (divided)
- 1-9 years: 8 mg/kg every 8 hours (ER)
- 9-12 years: 6.4 mg/kg every 8 hours (ER)
- 12-16 years: 5.6 mg/kg every 8 hours (ER)
Administration
- Take with food (preferably with the evening meal)
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
- Individualize dose based on serum theophylline concentration monitoring
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Nausea, vomiting
- Headache
- Stomach upset
- Restlessness
- Insomnia, hypotension
- CNS stimulation and diuresis (especially in children)
Precautions & warnings
- Caution in liver/kidney disease, heart disease
- Smoking alters theophylline clearance
- Avoid high-caffeine products (coffee, tea, dark chocolate) – increases side effects
- Avoid alcohol and smoking
Contraindications
- Hypersensitivity to xanthine derivatives
- Porphyria
Drug interactions
- Allopurinol, cimetidine, ciprofloxacin, erythromycin, OCs: Increased plasma concentrations
- Phenytoin, rifampicin, barbiturates, carbamazepine: Decreased plasma concentrations
- Corticosteroids and diuretics: Potentiate hypokalemia
- β-blockers: Increased bronchospasm
Food interactions
Alcohol is unsafe with Theophylline; consult your doctor.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; use only if clearly needed; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Safe during breastfeeding; human studies show insignificant passage into breast milk; avoid breastfeeding for 2-4 hours if possible; consult your doctor.
Pediatric use
Indicated for children (age and weight-based dosing)
Geriatric use
Elderly: Use lower doses
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment needed; consult your doctor.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed; consult your doctor.
Overdose effects
Overdose may cause nausea, tachycardia, arrhythmias, seizures; provide symptomatic treatment; activated charcoal; monitor serum theophylline levels.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Theophylline