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Defibrotide
- indication:Defibrotide is used to treat or prevent a failure of normal blood flow (occlusive venous disease, OVD) in the liver of patients who have had bone marrow transplants or received certain drugs such as oral estrogens, mercaptopurine, and many others.
- pharmacologypharmacology:
- mechanism: The drug appears to prevent the formation of blood clots and to help dissolve blood clots by increasing levels of prostaglandin I2, E2, and prostacyclin, altering platelet activity, increasing tissue plasminogen activator function, and decreasing activity of tissue plasminogen activator inhibitor. Prostaglandin I2 relaxes the smooth muscle of blood vessels and prevents platelets from adhering to each other. Prostaglandin E2 at certain concentrations also inhibits platelet aggregation. Moreover, the drug provides additional beneficial anti-inflammatory and antiischemic activities as recent sudies have shown. It is yet unclear, if the latter effects can be utilized clinically (e.g., treatment of ischemic stroke).
- toxicity:
- absorprion: Bioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%).
- halflife: t1/2-alpha = minutes (10-20 minutes in rat); t1/2-beta = a few hours
- roouteelimination:
- volumedistribution:
- clearance: