Pentoxifylline (PTXF) is a vasoactive agent that improves the flow of blood by reducing its viscosity.
It is FDA approved for the symptomatic treatment of:
Pentoxifylline is also used off-label for the treatment of:
Pentoxifylline and its metabolites decrease blood viscosity and improve the blood flow and peripheral tissue oxygenation. The precise mechanism of action by which it leads to symptom improvement remains yet to be determined. However, several pathways are likely involved.
Several animal studies have demonstrated the role of pentoxifylline in attenuating ischemia-reperfusion injury, drug-induced nephrotoxicity, infection, and inflammation.
Multiple clinical studies have demonstrated the role of anti-inflammatory, anti-fibrotic, and hemorheological properties of pentoxifylline in various disease states.
Generic name: Pentoxifylline
Chemical name: 3,7-dihydro-3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6-dione.
Solubility: Pentoxifylline is soluble in chloroform, methanol, and water.
Oral administration and absorption: Pentoxifylline is rapidly and completely absorbed in the gastrointestinal tract after oral administration. It is usually recommended with meals (food or milk) to minimize gastrointestinal irritation. It is usually a sustained releasing tablets that have an early peak plasma pentoxifylline concentration two to three hours of post-administration.
Metabolism: Erythrocytes and liver extensively metabolize pentoxifylline to its active metabolites (M1).
Excretion: Pentoxifylline and its metabolites are primarily eliminated by the kidneys and less than 5% by feces. On the other hand, its key metabolites are secreted in breast milk also. The half-life of pentoxifylline is about 0.4 hours to 0.8 hours, and its metabolites are about 1 to 1.5 hours.
The most common adverse effect of pentoxifylline is nausea and vomiting. Other common side effects are:
Medication interactions associated with pentoxifylline:
Pentoxifylline may potentiate the effect of antihypertensive agents. A dose reduction of antihypertensives should merit consideration with careful monitoring of blood pressure.
Pentoxifylline can enhance the anti glycemic action of antidiabetic agents. Pentoxifylline has demonstrated to inhibit ATP-sensitive K channels similar to glyburide in diabetic rats. A dose reduction of anti glycemic agents and glucose monitoring is recommended.
Pentoxifylline can increase the risk of bleeding in patients taking warfarin or antiplatelet agents.
Pentoxifylline increases the plasma levels of theophylline. It may cause excess central nervous stimulation when administered with other xanthine derivatives.
The use of pentoxifylline in patients below 18 years of age is not advised because its safety profile and efficacy have not been established. The older population have a higher peak plasma levels of the metabolites of pentoxifylline. Pentoxifylline crosses the placenta in mice; evidence in humans is lacking. Therefore, it is not recommended in pregnant women unless the benefits outweigh the risks. Pentoxifylline and its metabolites are secreted in milk; hence it should be avoided in nursing women. It is classified as FDA risk category C.
Older patients are at higher risk of side effects from pentoxifylline. Careful monitoring of blood pressure and glucose level is recommended when administering pentoxifylline in patients on antihypertensive and antidiabetic medications. They are at high risk for hypotension, falls, and hypoglycemia. Patients with liver disease should also receive close follow-up with periodic laboratory monitoring. There is an increased risk of side effects in patients with diminished renal function, CrCl < 80mL/min. The patients who are at increased risk of bleeding should be advised of potential signs and symptoms of bleeding and monitored with periodic laboratory data. Clinicians should exercise caution with patients who have cardiac arrhythmias and low blood pressure.
There is no reported antidote for this medication. The drug prescriber should discontinue the drug in suspected cases of toxicity. There are reports of adverse effects of pentoxifylline in patients on chronic hemodialysis.
Appropriate patient selection for pentoxifylline therapy may require consultation with a physician or a surgeon. A pharmacist plays a crucial role in determining the proper dose of medication to minimize side effects. Both nurse's and dietician's roles are vital in patient education to ensure medication compliance and modification of risk factors related to atherosclerotic disease. An interprofessional team approach and care coordination are crucial for the best patient outcomes.
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