Theophylline is indicated for use in mild-to-moderate persistent asthma, and is sometimes used in conjunction with an inhaled corticosteroid for an exacerbation. Due to its bronchodilatory effects it has been indicated for COPD and infant apnea.
This drug is a competitive nonselective phosphodiesterase inhibitor. Phosphodiesterase works to break down cAMP to AMP (increased levels of cAMP lead to bronchodilation). Inhibition of this enzyme also inhibits TNF-a, leukotrienes and inflammation.
Inhibition of phosphodiesterase protects cAMP from degradation, increasing its availability. Increased cAMP influences bronchodilation, making this drug useful in asthma and other respiratory conditions.
This drug has a very narrow therapeutic index and patients taking this medication can develop cardiac abnormalities such as arrhythmia or tachycardia. These effects can manifest due to the adenosine-blocking effects of the drug.
Theophylline has a very narrow therapeutic index, and patients taking this medication can develop CNS symptoms such as dizziness, lightheadedness, irritability, and in severe toxicities, seizure.
Patients with heart ailments should be considered when prescribing this medication, as Theophylline blocks the A1, A2 and A3 adenosine receptors in the heart. This may cause arrhythmias to occur in patients who were taking adenosine previously.
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