Pentoxifylline (Pentoxyphylline)

Peripheral vascular disease
Adult: As modified-release formulation: 400 mg tid (normally for at least 8 wk), may reduce to 400 mg bid if GI or CNS adverse effects occur.
Renal impairment: Moderate impairment (CrCl about 60 ml/min): 400 mg bid; severe impairment (CrCl about 20 ml/min): 400 mg once daily; may reduce further to 400 mg once every other day if needed.
Hepatic impairment: Dose reduction may be needed in severe impairment.

Special Populations: Adjust dose in patients with impaired renal function or severe hepatic impairment.
Previous hypersensitivity reactions to xanthine-related products e.g. caffeine, theophylline and theobromine. Recent cerebral and/or retinal haemorrhage. Porphyria.
Warnings / Precautions
Avoid use in patients with severe cardiac arrhythmias or acute MI. Caution when used in patients with ischaemic heart disease or hypotension. Impaired renal or hepatic function. Start at lower dose in elderly; safety and efficacy not established in children. Tablets should not be chewed, crushed or broken; swallow whole. Pregnancy, lactation.
Adverse Reactions
Nausea, vomiting, dizziness, headache, flushing; angina, palpitations; occasional cardiac arrhythmias; hepatitis, jaundice; blood dyscrasias reported; agitation; sleep disturbances; hypotension; thrombocytopenia; intrahepatic cholestasis.
Potentially Fatal: Fatal haemorrhage (cerebral and GI tract); anaphylactoid reaction.
Overdose Reactions
Symptoms: Occur 4-5 hr after ingestion; duration approx 12 hr; hypotension, flushing, convulsions, deep sleep, agitation, bradycardia and heart block. Treatment: Supportive and symptom specific.
Drug Interactions
Concurrent use with ciprofloxacin may increase the adverse effect of pentoxifylline. Concurrent use may increase serum levels of theophylline derivatives.
Potentially Fatal: May increase risk of adverse effect when used with ketorolac.
See Below for More pentoxifylline Drug Interactions
Lab Interactions
False-positive theophylline levels.
Food Interactions
Food: May reduce rate but not extent of absorption; administer with meals to minimise GI effects.
Mechanism of Actions
Pentoxifylline reduces blood viscosity by increasing deformability of leukocytes and erythrocytes; and decreasing neutrophil adhesion/activation. It also improves microcirculation and peripheral tissue oxygenation through better blood flow. It has also been used in cerebrovascular disorders.
Absorption: Well absorbed in the GI tract. Time to peak in serum: 2-4 hr.
Distribution: Pentoxifylline and metabolites: Enter breast milk.
Metabolism: Hepatic and via erythrocytes; some metabolites are active. Undergoes extensive 1st pass metabolism.
Excretion: Mainly via urine; less than 4% recovered in faeces. Apparent half-life of pentoxifylline: 0.4-0.8 hr; for metabolites: 1-1.6 hr.
Should be taken with food.
Storage Conditions
Oral: Store at 15-30 °C.
ATC Classification
C04AD03 - pentoxifylline ; Belongs to the class of purine derivative agents. Used as peripheral vasodilators.
Oral: Store at 15-30 °C.
Available As
  • Pentoxifylline (Pentoxyphylline) 20 mg
  • Pentoxifylline (Pentoxyphylline) 300 mg
  • Pentoxifylline (Pentoxyphylline) 400 mg
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