Generic
Pentoxifylline
3 brands available in the market
At a glance
Pentoxifylline is a peripheral vasodilator used for the treatment of peripheral vascular disease (poor circulation to the arms and legs) and intermittent claudication (pain on walking or at rest caused by poor circulation to the legs). It improves blood flow by decreasing blood viscosity.
Description
Pentoxifylline and its metabolites improve the flow properties of blood by decreasing its viscosity. In patients with chronic peripheral arterial disease, this increases blood flow to the affected microcirculation and enhances tissue oxygenation. It produces dose-related hemorrheologic effects, lowering blood viscosity, and improving erythrocyte flexibility.
Indications
- Peripheral arterial occlusive disease (PAOD) of arteriosclerotic or diabetic origin (with intermittent claudication and rest pain)
- Trophic lesions (e.g., leg ulcers and gangrene)
- Cerebral vascular diseases
- Circulatory disturbances of the eye in conjunction with degenerative vascular disorders
Therapeutic class
Peripheral Vasodilator drugs: Intermittent Claudication
Pharmacological class
Hemorrheologic Agent
Pharmacology
Pentoxifylline reduces blood viscosity, improves erythrocyte flexibility, and increases leukocyte deformability. It inhibits neutrophil adhesion and activation and enhances tissue oxygenation.
Mechanism of action
Improves microcirculation and tissue oxygenation by reducing blood viscosity and increasing leukocyte and erythrocyte deformability.
Dosage
Adult Dose (Oral):
- Usual dose: 400 mg 2-3 times daily (modified-release)
- Normally for at least 8 weeks
- May reduce to 400 mg twice daily if GI or CNS adverse effects occur
- Dose reduction may be needed in severe hepatic impairment
- Renal impairment (CrCl ~60 mL/min): 400 mg twice daily; (CrCl ~20 mL/min): 400 mg once daily; may reduce to 400 mg every other day if needed
Pediatric Dose: Safety and efficacy not established.
Administration
- Take with food or shortly after a meal with sufficient liquid (approx. ½ glass)
- Swallow tablet whole; do not chew, crush or break
- Take at the same time each day
Missed dose
If you miss a dose, skip it and continue with your normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Nausea
- Vomiting
- Diarrhea
- Constipation
- Abdominal distension
- Heartburn
- Stomach discomfort
- Flushing
- Headache
- Dizziness
- Weakness
- Lightheadedness
Precautions & warnings
- May decrease alertness, affect vision, or cause sleepiness and dizziness; do not drive if these occur
- Caution in severe cardiac arrhythmias, myocardial infarction, hypotension
- Caution in renal impairment (CrCl <30 mL/min) and severe hepatic impairment
- Caution with anticoagulants, antiplatelet agents, antidiabetic agents, ciprofloxacin, theophylline
- Increased bleeding risk
- Avoid use during pregnancy and lactation
Contraindications
- Previous hypersensitivity to xanthine-related products (e.g., caffeine, theophylline, theobromine)
- Recent cerebral and/or retinal hemorrhage
- Porphyria
- Massive bleeding
- Extensive retinal bleeding
Drug interactions
- Ciprofloxacin: May increase adverse effects of pentoxifylline
- Theophylline: May increase serum levels
- Insulin or oral antidiabetics: Blood-sugar-lowering effect potentiated
- Anti-vitamin K (warfarin): Increased anticoagulant activity
- Antihypertensive agents: Blood-pressure-lowering effect increased
- Platelet aggregation inhibitors (clopidogrel, etc.): Increased bleeding risk
- Cimetidine: May increase plasma concentration of pentoxifylline
- Potentially fatal: May increase risk of adverse effect when used with ketorolac
Food interactions
Take with food for better absorption; it is not known whether it is safe to consume alcohol.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects. Doctor will weigh benefits and risks before prescribing.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests no significant risk. Pentoxifylline passes into breast milk in minute quantities.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose reduction by 30-50% may be necessary in CrCl <30 mL/min; consult your doctor.
Hepatic Impairment: Dose reduction necessary in severe liver function impairment; consult your doctor.
Overdose effects
Initial symptoms of acute overdose: nausea, dizziness, tachycardia, or fall in blood pressure. Other signs: fever, agitation, flush, loss of consciousness, areflexia, tonic-clonic convulsions, coffee-ground vomiting (GI bleeding). No specific antidote; gastric lavage and activated charcoal.
Storage conditions
Store in a cool and dry place, away from light; do not use after expiry date; keep out of reach of children.
Chemical structure
Pentoxifylline