Theophylline/ephedrine

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Theophylline/Ephedrine

Theophylline chemical structure

Theophylline/ephedrine is a combination medication used primarily in the management of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). This combination leverages the bronchodilator effects of both theophylline and ephedrine to improve airflow and reduce symptoms associated with these conditions.

Pharmacology

Theophylline

Theophylline is a methylxanthine drug that acts as a bronchodilator. It works by inhibiting the enzyme phosphodiesterase, leading to an increase in intracellular cyclic adenosine monophosphate (cAMP). This results in relaxation of bronchial smooth muscle and dilation of the airways. Theophylline also has mild anti-inflammatory effects and can improve diaphragmatic contractility, which is beneficial in respiratory diseases.

Ephedrine

Ephedrine chemical structure

Ephedrine is a sympathomimetic amine that stimulates both alpha and beta-adrenergic receptors. Its primary action in the context of respiratory therapy is as a bronchodilator, achieved through beta-2 adrenergic receptor stimulation. This leads to relaxation of bronchial smooth muscle and improved airflow. Additionally, ephedrine has mild central nervous system stimulant effects, which can contribute to increased alertness and reduced fatigue in patients.

Clinical Use

The combination of theophylline and ephedrine is used to manage symptoms of asthma and COPD, particularly in patients who require additional bronchodilation beyond what is achieved with standard therapies such as inhaled corticosteroids and beta-agonists. This combination may be particularly useful in patients who experience nocturnal symptoms or who have difficulty using inhalers.

Dosage and Administration

Theophylline/ephedrine is typically administered orally in tablet form. The dosage is individualized based on the patient's response and tolerance to the medication. Monitoring of theophylline blood levels is often necessary to avoid toxicity, as the therapeutic range is narrow.

Side Effects

Common side effects of theophylline/ephedrine include nausea, vomiting, insomnia, and nervousness. More serious side effects can include tachycardia, arrhythmias, and seizures, particularly if theophylline levels become elevated. Patients should be monitored for signs of toxicity, and dosage adjustments should be made as necessary.

Contraindications and Precautions

Theophylline/ephedrine is contraindicated in patients with hypersensitivity to either component. Caution is advised in patients with cardiovascular disease, hypertension, hyperthyroidism, and diabetes mellitus. Drug interactions with other medications, such as cimetidine and fluoroquinolones, can affect theophylline levels and should be managed carefully.

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Contributors: Prab R. Tumpati, MD