Theophylline

Generic Details

Generic Name

Theophylline

Other Names

  • Aminophylline

Drug Class

  • Methylxanthine

Chemical Formula

C7H8N4O2

Molecular Weight

180.16 g/mol

Mechanism of Action

  • Phosphodiesterase inhibitor
  • Adenosine receptor antagonist

Indications

  • Asthma
  • Chronic obstructive pulmonary disease (COPD)
  • Bronchospasm

Common Dosage Forms

  • Tablet
  • Capsule
  • Injection
  • Oral solution

Typical Dosage

  • 200-400 mg every 6-8 hours

Pediatric Dosage

  • 6 mg/kg every 6 hours

Geriatric Dosage

  • Lower starting doses may be required due to decreased clearance

Side Effects

  • Nausea
  • Vomiting
  • Headache
  • Insomnia
  • Restlessness
  • Tachycardia
  • Seizures (rare)

Contraindications

  • Hypersensitivity to theophylline
  • Acute myocardial infarction

Pregnancy Category

  • C

Lactation Safety

  • Limited data - caution advised

Drug Interactions

  • Ciprofloxacin
  • Cimetidine
  • Phenytoin
  • Rifampin

Overdose Symptoms

  • Severe nausea
  • Vomiting
  • Tremors
  • Cardiac arrhythmias
  • Seizures

Antidote for Overdose

  • Activated charcoal
  • Diazepam for seizures

Storage Conditions

  • Store at room temperature away from moisture and heat

Pharmacokinetics

  • Absorption: Rapid and complete
  • Distribution: Crosses blood-brain barrier, widely distributed in the body
  • Metabolism: Mainly hepatic - CYP1A2
  • Excretion: Primarily by the kidneys

Precautions

  • Monitor serum levels regularly
  • Avoid abrupt discontinuation
  • Caution in patients with liver or kidney disease

Warnings

  • Narrow therapeutic index - monitor levels closely

Others

  • Avoid or limit caffeine consumption as it can increase the risk of side effects or toxicity.