Pentifylline

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Pentifylline

Chemical structure of Pentifylline

Pentifylline is a pharmaceutical drug that belongs to the class of xanthine derivatives. It is primarily used as a vasodilator and has applications in the treatment of various circulatory disorders.

Mechanism of Action

Pentifylline works by inhibiting the enzyme phosphodiesterase, which leads to an increase in cyclic adenosine monophosphate (cAMP) within cells. This results in vasodilation and improved blood flow, particularly in the microcirculation. The drug also has anti-inflammatory properties and can improve red blood cell deformability, which enhances oxygen delivery to tissues.

Clinical Uses

Pentifylline is used in the management of peripheral artery disease, particularly in patients with intermittent claudication. It helps to improve walking distance and reduce symptoms associated with poor blood flow. Additionally, pentifylline has been studied for its potential benefits in treating chronic venous insufficiency, diabetic neuropathy, and cerebrovascular disease.

Side Effects

Common side effects of pentifylline include nausea, dizziness, and headache. In some cases, patients may experience gastrointestinal disturbances such as diarrhea or vomiting. Rarely, pentifylline can cause allergic reactions or cardiovascular effects such as tachycardia.

Contraindications

Pentifylline is contraindicated in patients with a known hypersensitivity to xanthine derivatives. It should be used with caution in individuals with severe coronary artery disease, peptic ulcer disease, or bleeding disorders.

Pharmacokinetics

Pentifylline is well absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. It is metabolized to several active metabolites, which contribute to its therapeutic effects. The drug and its metabolites are primarily excreted in the urine.

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Contributors: Prab R. Tumpati, MD