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P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Food *
LI - Lab *
Pentoxifylline by Aventis under the brand name Trental. Its chemical name is 1-(5-oxohexyl)-3, 7-dimethylxanthine. Pentoxifylline is a xanthine derivative. Other brand names include Pentox, Pentoxil, and Flexital.
Pentoxifylline is used to improve blood flow in patients with circulation problems to reduce aching, cramping, and tiredness in the hands and feet. It works by decreasing the thickness (viscosity) of blood. This change allows blood to flow more easily, especially in the small blood vessels of the hands and feet.
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.
Well absorbed in the GI tract. Time to peak in serum: 2-4 hours.
Pentoxifylline and metabolites: Enter breast milk.
Hepatic and via erythrocytes; some metabolites are active. Undergoes extensive 1st pass metabolism.
Mainly via urine; less than 4% recovered in faeces. Apparent half-life of pentoxifylline: 0.4-0.8 hours; for metabolites: 1-1.6 hours.
Information Not Available
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.
Periodically monitor patients with risk factors complicated by hemorrhage (eg, recent surgery, peptic ulceration, cerebral and retinal bleeding) for bleeding, including hematocrit and hemoglobin; patients receiving warfarin should have more frequent monitoring of PT.
Symptoms: Occur 4-5 hours after ingestion; duration approx 12 hours; hypotension, flushing, convulsions, deep sleep, agitation, bradycardia and heart block. Treatment: Supportive and symptom specific.
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.
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.
May reduce rate but not extent of absorption; administer with meals to minimise GI effects.
Peripheral vascular disease
Adult: As modified-release formulation: 400 mg tid (normally for at least 8 weeks), 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.
Should be taken with food
Contraindicated in pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Contraindicated in lactation
Safety and efficacy not established
Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Previous hypersensitivity reactions to xanthine-related products e.g. caffeine, theophylline and theobromine. Recent cerebral and/or retinal haemorrhage. Porphyria.
Store at 15-30 °C
Store at 15-30 °C