Transcript Anticoagulants, Thrombolytics Agents and Antiplatelet Drugs

Newer Antiplatelet Agents
Epifibatide
Tirofiban
Etc.
Benedict R. Lucchesi, M.D., Ph.D.
Department of Pharmacology
University of Michigan Medical School
Epifibatide (Integrelin™)
• Integrelin - a cyclic peptide antagonist, has
been administered to humans with positive
results.
• Must be administered by continuous
infusion 1.0 to 1.5 mg/kg/min.
• Short duration of action - recovery of
platelet function within 2-4 hours after
termination of the infusion.
Tirofiban (Aggrastat™)
• Development based on anti-clotting
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components in the venom of an
African snake, the saw-scaled viper.
Antiplatelet function in humans
Indicated for use in patients with
unstable angina and non-Q-wave
myocardial infarction.
Used with heparin and aspirin for
treatment of acute coronary
syndrome.
Must be administered by continuous
infusion.
DMP728 - a Low Molecular Weight Platelet GPIIb/IIIa
Fibrinogen Receptor Antagonist Incorporating the RGD Sequence
Arginine
DMP728
Structure
Glycine
NH
O
O
H2N
N
H
N
H
O
N
OH
HN
Aspartate
2-Aminobutyrate
NH
O
HN
O
O
•CH3SO3
3-Amino methyl benzoic acid
Essential Thrombocythemia
Anagrelide (Argylin™)
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A life-threatening condition characterized by elevated blood platelet
counts. This condition results in an abnormally high incidence of
adverse events associated with thrombosis (blood clotting), including
heart attack and stroke - incidence in U.S. is 7 / 100,000 individuals.
ANAGRELEIDE is indicated for the treatment of essential
thrombocythemia to reduce elevated platelet counts and the risk of
thrombosis.
Therapeutic doses do not produce significant changes in white or
red cell counts and has not been shown to be leukemogenic.
The drug's labeling provides guidelines for treatment of
asymptomatic young adults with essential thrombocythemia.
The most frequently reported adverse reactions were mild and selflimiting and included headache, palpitations, diarrhea, and
abdominal pain.