Pentoxifylline

FDA label, Rising Pharma Holdings, Inc., oral, effective 2026-05-15. Full label on DailyMed

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Quoted from the FDA label. Product labels differ by manufacturer and change over time; confirm against the label for the product you are using.

Blood Viscosity Reducer

Dosing in kidney impairment

Digestive and central nervous system side effects are dose related. If patients develop these effects it is recommended that the dosage be lowered to one tablet twice a day (800 mg/day). If side effects persist at this lower dosage, the administration of pentoxifylline extended-release tablets should be discontinued. In patients with severe renal impairment (creatinine clearance below 30 mL/min) reduce dose to 400 mg once a day.

Drug interactions

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Label text (3 paragraphs)

Bleeding has been reported in patients treated with pentoxifylline extended-release tablets with or without concomitant NSAIDs, anticoagulants, or platelet aggregation inhibitors. Increased prothrombin time has been reported in patients concomitantly treated with pentoxifylline and vitamin K antagonists. Monitoring of anticoagulant activity in these patients is recommended when pentoxifylline is introduced or the dose is changed. Concomitant administration of pentoxifylline extended-release tablets and theophylline-containing drugs leads to increased theophylline levels and theophylline toxicity in some individuals.

Monitor theophylline levels when starting pentoxifylline extended-release tablets or changing dose. Concomitant administration of strong CYP1A2 inhibitors (including e.g., ciprofloxacin or fluvoxamine) may increase the exposure to pentoxifylline (see ADVERSE REACTIONS). Pentoxifylline extended-release tablets have been used concurrently with antihypertensive drugs, beta blockers, digitalis, diuretics, and antiarrhythmics, without observed problems. Small decreases in blood pressure have been observed in some patients treated with pentoxifylline extended-release tablets; periodic systemic blood pressure monitoring is recommended for patients receiving concomitant antihypertensive therapy.

If indicated, dosage of the antihypertensive agents should be reduced. Postmarketing cases of increased anticoagulant activity have been reported in patients concomitantly treated with pentoxifylline and vitamin K antagonists. Monitoring of anticoagulant activity in these patients is recommended when pentoxifylline is introduced or the dose is changed. Concomitant administration with cimetidine is reported to increase the average steady state plasma concentration of pentoxifylline (~25%) and the Metabolite I (~30%).

Contraindications

Pentoxifylline extended-release tablets should not be used in patients with recent cerebral and/or retinal hemorrhage or in patients who have previously exhibited intolerance to this product or methylxanthines such as caffeine, theophylline, and theobromine.

Safety data

Reported adverse events (FAERS)

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Source: FDA Adverse Event Reporting System via openFDA

Liver injury (LiverTox)

D

Likelihood score D: Possible rare cause of clinically apparent liver injury.

Pentoxifylline is a xanthine derivative that decreases the viscosity of blood and is used to treat symptoms of intermittent claudication due to peripheral vascular disease. Pentoxifylline has not been associated with serum enzyme elevations during therapy, but in several isolated case reports has been linked to clinically apparent liver injury.

ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.

Source: LiverTox: Pentoxifylline (NIDDK, public domain)Chapter updated Jun 24, 2020

Pregnancy and lactation

Pregnancy

Pregnancy: Teratogenicity studies have been performed in rats and rabbits using oral doses up to 576 mg/kg and 264 mg/kg, respectively. On a weight basis, these doses are 24 and 11 times the maximum recommended human daily dose (MRHD); on a body-surface-area basis, they are 4.2 and 3.5 times the MRHD. No evidence of fetal malformation was observed. Increased resorption was seen in rats of the 576 mg/kg group. There are no adequate and well controlled studies in pregnant women. Pentoxifylline extended-release tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation

Pentoxifylline and its metabolites are excreted in human milk. Because of the potential for tumorigenicity shown for pentoxifylline in rats, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Breastfeeding (LactMed)

Limited data indicate that pentoxifylline is poorly excreted into breastmilk. It would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months.

Source: LactMed: Pentoxifylline (NICHD, public domain)Revised Jul 20, 2020

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