Theophylline
Medicinal Chemistry
Molecular Weight
180.16
Molecular Formula
C7H8N4O2
IUPAC Name
1,3-dimethyl-7H-purine-2,6-dione
Pharmacognosy
Biological Source
Camellia sinensis (Tea)
Active Constituents
Theophylline, Caffeine
Pharmacology & Synthesis
Mechanism of Action
Competitive nonselective phosphodiesterase inhibitor; adenosine receptor antagonist.
Pharmacokinetics (ADME)
A: Complete oral absorption.
D: Narrow therapeutic index, wide Vd.
M: Hepatic via CYP1A2.
E: Renal.
Pharmacodynamics
Relaxes bronchial smooth muscle, stimulates CNS and cardiac muscle, mild diuretic.
Synthesis Pathway
Biosynthesized from xanthosine.
Safety, Warnings & Interactions
Adverse Effects
Nausea, tachycardia, arrhythmias, seizures, insomnia.
Contraindications
Active peptic ulcer, seizure disorders, severe arrhythmias.
Drug Interactions
Ciprofloxacin, cimetidine (significantly increase levels and risk of toxicity).
Pharmaceutics & Compendia
Dosage Forms
ER Tablets, Elixir, Injection
Official Compendia
IP, BP, USP