Theophylline: Uses, Interactions, Mechanism of Action

Theophylline: Uses, Interactions, Mechanism of Action

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A methylxanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Mechanistically, theophylline acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. Theophylline is marketed under several brand names such as Uniphyl and Theochron, and it is indicated mainly for asthma, bronchospasm, and COPD.

Theophylline is a xanthine used to manage the symptoms of asthma, COPD, and other lung conditions caused by reversible airflow obstruction.

Indication

Associated Conditions

Associated Therapies

Contraindications & Blackbox Warnings

Pharmacodynamics

Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects).

Mechanism of action

Absorption

Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form.

Volume of distribution

• 0.3 to 0.7 L/kg

Protein binding

40%, primarily to albumin.

Metabolism

Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity.

Hover over products below to view reaction partners

• Theophylline

  • 1-Methylxanthine

  • 3-methylxanthine

  • 1,3-dimethyluric acid

  • Caffeine

Route of elimination

Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults.

Half-life

8 hours

Clearance

• 0.29 mL/kg/min [Premature neonates, postnatal age 3-15 days]
• 0.64 mL/kg/min [Premature neonates, postnatal 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 [hypothyroid]
• 0.8 mL/kg/min [hyperthyroid]

Adverse Effects

Toxicity

Symptoms of overdose include seizures, arrhythmias, and GI effects.

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Pathways

PathwayCategoryCaffeine MetabolismMetabolic

Pharmacogenomic Effects/ADRs

Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetailsCytochrome P450 1A2-(G/A)

(A;A)

/

(G;A)

A Allele

Effect

Directly Studied

Patients with this genotype have reduced metabolism of theophylline.Details

Theophylline | Bronchodilator, Asthma, COPD