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

Medically reviewed by Drugs.com on Jun 21, 2024. Written by ASHP.

Introduction

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

Administration

Administration

Administer orally, preferably with meals.

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

Dosage

Adults

Peripheral Vascular Disease

Oral

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

Contraindications

• History of intolerance to pentoxyphylline or to xanthine derivatives such as caffeine, theophylline, or theobromine.

• Recent cerebral and/or retinal hemorrhage.

Warnings/Precautions

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

Pregnancy

Category C.

Lactation

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

Pentoxifylline Pharmacokinetics

Absorption

Bioavailability

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.

Onset

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

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.

Distribution

Extent

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

Elimination

Metabolism

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.

Half-life

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.

Stability

Storage

Oral

Tablets

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

Actions and Spectrum

• Increases erythrocyte flexibility (deformability) and reduces the viscosity of whole blood, which decreases total systemic vascular resistance, improves blood flow, and increases tissue oxygenation in patients with peripheral vascular disease.

• Affects the electrolyte balance of erythrocytes which may improve erythrocyte flexibility and blood flow.

• May improve poststenotic blood flow in relatively poorly perfused tissue. Improves resting blood flow and reactive hyperemia. Increases peak flow of reactive hyperemia in the extremities indicating an increase in reserve blood flow which is associated with some increase in walking distance.

• Improves regional and hemispheric cerebral blood flow, particularly in ischemic areas where microcirculation is impaired. Increases oxygen and glucose supply, eliminates or reduces perivascular edema, and enhances cellular function in some patients with cerebrovascular insufficiency.

Advice to Patients

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

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

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