Pharmacology Flashcards
Mechanism of action of Aprepitant
Blocks neurokinin-1 receptors in the brain, preventing substance P release.
Antiemetic for chemotherapy-induced N/V
Mechanism of action of Hydroxyurea
Inhibits ribonucleotide reductase → ↓DNA synthesis (S-phase specific).
Also ↑ HbF
Mechanism of action of Argstroban, Dabigatran and Lepirudin
Direct thrombin inhibitors.
Inhibit activity of free and clot-associated thrombin.
Do not require antithrombin III
Development of IgG vs heparin-bound platelet factor 4. The complex activates platelets → thrombosis and thrombocytopenia
Heparin-induced thrombocytopenia (HIT) type 2
Mechanism of action of Vincristine
Vinca alkaloid that binds β-tubulin and inhibits its polymerization into microtubules.
M-phase arrest
Mechanism of action of Warfarin
Inhibits epoxide reductase.
Interferes with γ carboxylation of vit K dependent clotting factors
Mechanism of action of Bleomycin and mention the most important adverse effect
Antitumor antibiotic that induces free radical formation, so breaks in DNA strands.
Causes pulmonary fibrosis
Mechanism of action of Abciximab
Binds to glycoprotein receptor IIb/IIIa (fibrinogen receptor) on activated platelets, preventing aggregation
Mechanism of action of Bortezomib
Proteasome inhibitor, induce arrest at G2-M phase and apoptosis. There’s accumulation of misfolded proteins → cytotoxic effects
Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase receptor
Herceptin.
Trastuzumab
Mechanism of action of Unfractionated Heparin
Activates antithrombin, ↓ action of IIa (thrombin) and factor Xa. Binds both antithrombin and thrombin
Association between CLL and BCL-2
BCL-2 is an antiapoptotic protein. CLL overexpresses BCL-2 → ↓ caspase activation → tumorigenesis
How do you monitor warfarin effect?
With INR and PT
Why is desmopressin used as treatment of von Willebrand disease?
Because it ↑ vWF release from endothelial cells and ↑ factor VIII levels (tx in hemophilia A)
Mechanism of action of Bevacizumab
Monoclonal antibody against VEGF. Inhibits angiogenesis
Why is the warfarin therapeutic effect delayed 3-5 days?
Because it blocks generation of new clotting factors, until preexisting ones are consumed. This is why there’s risk of initial hypercoagulation
Pancytopenia characterized by anemia, leukopenia and thrombocytopenia with normal cell morphology and hypocellular bone marrow, caused by radiation, viral agents, CBZ, etc
Aplastic anemia
How to treat Heparin and warfarin overdose, respectively
Heparin rapid antidote: protamine sulfate
Warfarin rapid reversal: fresh frozen plasma or PCC
Mechanism of action of Etoposide
Inhibits topoisomerase II → ↑ DNA degradation (cell cycle arrest in G2 and S phases)