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Pentoxifylline/Oxpentifylline; Uses, Dosage, Side Effects

Pentoxifylline is a methylxanthine derivative with hemorrheologic and immunomodulating properties. Pentoxifylline inhibits phosphodiesterase, resulting in increased levels of cyclic adenosine monophosphate (cAMP) in erythrocytes, endothelium, and the surrounding tissues. This leads to vasodilation, improves erythrocyte flexibility, and enhances blood flow. In addition, the increased level of cAMP in platelets inhibits platelet aggregation, which may contribute to a reduction in blood viscosity. This agent also inhibits production of tumor necrosis factor-alpha and interferon-gamma, while it induces Th2-like (T-helper 2) cytokine production, thereby inhibiting Th1-mediated (T-helper 1) inflammatory and autoimmune responses.

Pentoxifylline, also known as oxpentifylline, is a xanthine derivative used as a drug to treat muscle pain in people with peripheral artery disease. A methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production.

Mechanism of Action of Pentoxifylline/Oxpentifylline

Pentoxifylline inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, pentoxifylline also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. It is also a non selective adenosine receptor antagonist.

Pentoxifylline is a methylxanthine derivative with hemorrheologic and immunomodulating properties. Pentoxifylline inhibits phosphodiesterase, resulting in increased levels of cyclic adenosine monophosphate (cAMP) in erythrocytes, endothelium, and the surrounding tissues. This leads to vasodilation, improves erythrocyte flexibility, and enhances blood flow. In addition, the increased level of cAMP in platelets inhibits platelet aggregation, which may contribute to a reduction in blood viscosity. This agent also inhibits production of tumor necrosis factor-alpha and interferon-gamma, while it induces Th2-like (T-helper 2) cytokine production, thereby inhibiting Th1-mediated (T-helper 1) inflammatory and autoimmune responses.

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Indications of Pentoxifylline/Oxpentifylline

Intermittent Claudication
Venous Leg Ulcer (VLU)
Severe alcoholic liver disease

Contra-Indications of Pentoxifylline/Oxpentifylline

Increased risk of bleeding
Retinal hemorrhage
Stroke caused by Bleeding in the Brain
Kidney disease with a reduction in kidney function

The Dosage of Pentoxifylline/Oxpentifylline

Strengths: 400 mg

Intermittent Claudication

400 mg orally 3 times a day. If adverse effects develop, reducing the dose to 400 mg twice a day is recommended.

Side Effects of Pentoxifylline/Oxpentifylline

The most common

Common

Rare

Drug Interactions

Pentoxifylline may interact with following drugs, supplements & may change the efficacy of drugs

alcohol
angiotensin receptor blockers (ARBs; e.g., irbesartan, losartan)
anticancer medications (e.g., carboplatin, cyclophosphamide, fluorouracil)
azathioprine
“azole” antifungals (e.g., fluconazole, ketoconazole, voriconazole)
carbamazepine
cephalosporins (e.g., cefazolin, cefoperazone, cefotetan, cefoxitin)
clopidogrel
corticosteroids (e.g., hydrocortisone, prednisone)
COX-II inhibitors (celecoxib, rofecoxib)
estrogen-containing medications (e.g., birth control pills)
gliclazide
glucagon
glucosamine
heparin
macrolide antibiotics (e.g., azithromycin, clarithromycin,
methyldopa
metronidazole
mirtazapine
multivitamins
nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., diclofenac, ibuprofen,naproxen)
omega-3 fatty acid
peginterferon alfa-2b
penicillins (e.g., ampicillin, cloxacillin, penicillin G, piperacillin, ticarcillin)
pentoxifylline
phenobarbital
phenytoin
progestins (e.g., levonorgestrel, progesterone)
proton pump inhibitors (e.g., lansoprazole, omeprazole)
quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
ranitidine
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
“statins” (e.g., fluvastatin, lovastatin, simvastatin)
tetracyclines (e.g., doxycycline, minocycline, tetracycline)
tolterodine
tramadol
tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
zafirlukast

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Pregnancy & Lactation of Pentoxifylline/Oxpentifylline

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

Pentoxifylline passes into breast milk. If breastfeeding-feeding and are taking pentoxifylline, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.