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Pentoxifylline (Monograph)

Brand names: Pentoxil, TRENtal
Drug class: Hemorrheologic Agents
VA class: CV900
Molecular formula: C13H18N4O3
CAS number: 6493-05-6

Medically reviewed by on Jun 21, 2023. Written by ASHP.


Hemorrheologic agent; a synthetic xanthine derivative.

Uses for Pentoxifylline

Peripheral Vascular Disease

Used for the symptomatic treatment of intermittent claudication associated with peripheral vascular disease (i.e., chronic occlusive arterial disease of the extremities). May improve function of the extremities and symptoms of the disease (e.g., improvement in walking distance and duration; reductions in severity and occurrence of paresthesia and trophic ulcers ). Does not affect other symptoms associated with claudication such as cramping, tiredness, tightness, and pain during exercise. Pentoxifylline should not replace more definitive therapy for peripheral vascular disease such as smoking cessation, weight loss, exercise therapy, or surgical bypass or removal of arterial obstructions when indicated.

Cerebrovascular Disease

Also has been used for the management of acute and chronic cerebrovascular insufficiency [off-label] . Improves psychopathologic symptoms (e.g., those associated with aging, stroke, TIAs), including memory loss, disorientation, constructional apraxia, impaired practical reasoning, motor impairment, and dizziness. Reduces the incidence of recurrence of TIAs.

Male Infertility

Used in a limited number of patients for the treatment of male fertility disorders [off-label], including asthenospermia [off-label] and idiopathic oligospermia [off-label]. Increases the duration of activity of ejaculated spermatozoa.

Pentoxifylline Dosage and Administration



Administer orally, preferably with meals.

An aluminum and magnesium hydroxides antacid can be administered concomitantly to reduce intolerable GI effects.



Peripheral Vascular Disease

400 mg 3 times daily. Continue for at least 8 weeks to determine efficacy. Reduce dosage to 400 mg twice daily if adverse GI and/or CNS effects develop. Discontinue if adverse effects persist at this lower dosage. Efficacy was demonstrated in clinical studies of 6-months duration.

Cautions for Pentoxifylline



General Precautions

Cardiovascular Effects

Other manifestations of arteriosclerotic disease may be exhibited frequently in patients with chronic occlusive arterial disease. Angina, hypotension, and arrhythmia reported occasionally in patients with concomitant coronary artery and/or cerebrovascular disease; consider the possibility that such effects may occur.

Hematologic Effects

Periodic examination for signs of bleeding (e.g., hemoglobin and hematocrit determinations) recommended in patients who have risk factors potentially complicated by hemorrhage (e.g., recent surgery, peptic ulceration, cerebral and/or retinal bleeding).

Specific Populations


Category C.


Distributed into milk. Discontinue nursing or the drug, taking into account the importance of the drug to the woman.

Pediatric Use

Safety and efficacy not established.

Common Adverse Effects

Dyspepsia, nausea, dizziness.

Drug Interactions

Specific Drugs





Potential pharmacokinetic interaction (reduced bioavailability of several metabolites)

Interaction not clinically important; concomitant administration may reduce intolerable GI effects

Antiarrhythmic agents

Interaction not observed

Anticoagulants, oral (warfarin)

Possible bleeding an/or prolonged PT

Determine prothrombin time more frequently during concomitant therapy

Antidiabetic agents

Interaction not observed

Antihypertensive agents

Possible additive antihypertensive effect

Periodic monitoring of systemic blood pressure recommended; if required, reduce antihypertensive dosage

β-Adrenergic blocking agents

Interaction not observed

Cardiac Glycosides

Interaction not observed


Interaction not observed

Platelet-aggregation inhibitors

Possible bleeding and/or prolonged PT


Possible increased theophylline levels and possible theophylline toxicity

Closely monitor and adjust theophylline dosage as needed

Pentoxifylline Pharmacokinetics



Rapidly and almost completely absorbed following oral administration, with peak plasma concentrations usually attained within 1 hour.

Mean absolute bioavailability is 33% in healthy men.


Symptomatic relief may occur within 2–4 weeks following initiation of therapy. The therapeutic effects result principally from an action on newly formed erythrocytes rather than on circulating mature erythrocytes. Allow at least 8 weeks to determine full therapeutic efficacy.


Food increases mean peak plasma concentrations and mean AUC.

Special Populations

Peak plasma concentrations and mean absolute bioavailability were substantially increased, and time to peak concentration was prolonged in adults with hepatic cirrhosis.

Increased AUC in patients 60–68 years of age, compared to younger adults.



Not known whether pentoxifylline or its metabolites cross the placenta. Pentoxifylline and its metabolites are distributed into milk.



Extensively metabolized in erythrocytes and the liver to active metabolites , principally via reduction, oxidation, and demethylation.

Elimination Route

Eliminated in urine (95%) and feces (4%), principally as metabolites.


0.4–0.8 hours.

Special Populations

Prolonged elimination in adults with hepatic cirrhosis.

Decreased elimination rate in patients 60–68 years of age, compared with younger adults.





Tight, light-resistant containers at 15–30°C.

Actions and Spectrum

Advice to Patients


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name



Dosage Forms


Brand Names



Tablets, extended-release, film-coated

400 mg*

Pentoxifylline Extended-release Tablets




TRENtal (with povidone)


AHFS DI Essentials™. © Copyright 2024, Selected Revisions July 1, 2006. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.

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