Theophylline: Uses, Interactions, Mechanism of Action

May. 27, 2024

Theophylline: Uses, Interactions, Mechanism of Action

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Derived from tea, theophylline is a methylxanthine compound known for its diuretic, smooth muscle relaxant, bronchial dilation, and cardiac and central nervous system stimulant properties. At a molecular level, theophylline functions as a phosphodiesterase inhibitor, adenosine receptor antagonist, and histone deacetylase activator. It is sold under various brand names like Uniphyl and Theochron and chiefly prescribed for asthma, bronchospasm, and COPD management.

Theophylline is a xanthine class drug utilized to alleviate the symptoms associated with asthma, COPD, and other respiratory conditions characterized by reversible airflow obstruction.

Primary Indications

Conditions Treated

Therapeutic Combinations

Contraindications & Warnings

Drug Pharmacodynamics

Theophylline, chemically akin to caffeine and theobromine, is employed to treat asthma and bronchospasm. It has two main actions on the airways of patients suffering from reversible (asthmatic) obstruction: relaxing the smooth muscles (bronchodilation) and reducing the airway's response to external stimuli (non-bronchodilator prophylactic effects).

Mechanism of Action

Absorption Patterns

Theophylline is swiftly and fully absorbed following oral administration, either in solution or immediate-release solid oral dosage forms.

Distribution Volume

0.3 to 0.7 L/kg

Protein Binding Characteristics

40%, mainly binding to albumin.

Metabolic Pathways

Theophylline is metabolized primarily in the liver. Its biotransformation involves demethylation to 1-methylxanthine and 3-methylxanthine, and hydroxylation to 1,3-dimethyluric acid. Further metabolism of 1-methylxanthine to 1-methyluric acid is catalyzed by xanthine oxidase. About 6% of theophylline dosage is converted to caffeine. Among its metabolites, only caffeine and 3-methylxanthine exhibit pharmacologic activity.

Hover over products below to view reaction partners

Theophylline
- 1-Methylxanthine
- 3-Methylxanthine
- Link to Guangxing
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- Caffeine

Elimination Routes

Theophylline does not undergo significant pre-systemic elimination and freely distributes into fat-free tissues. It is mainly metabolized in the liver. In neonates, approximately 50% of the theophylline dose is excreted unchanged by the kidneys, compared to about 10% in older children and adults.

Effective Half-life

The half-life of theophylline is approximately 8 hours.

Clearance Rates

0.29 mL/kg/min [Premature neonates, age 3-15 days]
0.64 mL/kg/min [Premature neonates, age 25-57 days]
1.7 mL/kg/min [Children 1-4 years]
1.6 mL/kg/min [Children 4-12 years]
0.9 mL/kg/min [Children 13-15 years]
1.4 mL/kg/min [Children 16-17 years]
0.65 mL/kg/min [Adults (16-60 years), otherwise healthy non-smoking asthmatics]
0.41 mL/kg/min [Elderly (>60 years), non-smokers with normal cardiac, liver, and renal function]
0.33 mL/kg/min [Acute pulmonary edema]
0.54 mL/kg/min [COPD >60 years, stable, non-smoker >1 year]
0.48 mL/kg/min [COPD with cor pulmonale]
1.25 mL/kg/min [Cystic fibrosis (14-28 years)]
0.31 mL/kg/min [Liver disease cirrhosis]
0.35 mL/kg/min [Acute hepatitis]
0.65 mL/kg/min [Cholestasis]
0.47 mL/kg/min [Sepsis with multi-organ failure]
0.38 mL/kg/min [Hypothyroidism]
0.8 mL/kg/min [Hyperthyroidism]

Potential Side Effects

Toxicity Risks