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.
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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.
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
- back pain
- constipation
- muscle aches
- Nausea and vomiting
- Severe stomach ache
- diarrhoea,
- anorexia,
- flatulence,
- headache,
- dizziness,
- heartburn
- joint pain
Common
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Mouth sores
- Vaginal thrush
- Skin rash
- Headache
Rare
- Chest pain
- irregular heartbeat
- Drowsiness
- flushing
- faintness
- unusual excitement
- convulsions (seizures)
- Dizziness
- headache
- nausea or vomiting
- stomach discomfort
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
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.
References
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