Cardio: antiPlat., antiCoag., Thrombolytic Drugs Flashcards Preview

Pharmacology > Cardio: antiPlat., antiCoag., Thrombolytic Drugs > Flashcards

Flashcards in Cardio: antiPlat., antiCoag., Thrombolytic Drugs Deck (15)
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1

  • Permanently Acylates COX enzymes (irreversibly inhibit COX-1 and COX-2), prevents the conversion of Arachidonic acid to Prostaglandins and TXA2
  • AA  → COX-1 → PGH2 → TXA2 (potent agonist that induces platelet aggregation - in the platelet membrane
  • ↓ Risk of CHD
  • Used to treat Unstable Angina
  • Side Effects: GI bleeding, Ulcers, Peptic Ulcer Disease, occasionaly triggers Allergies as Asthma, Reye syndrome in children, Tinnitus at very high doses

Aspirin

2

  • Class Thienopyridines which are irreversible antagonists of the ADP  (P2Y1 and P2Y12) on the platelet surface
  • Activated by Hepatic P450 of the receptors: ↑ IP3, ↓cAMP
    → promotes expression of GPIIb/IIa (figrinogen recptor)
  • Used w/ Asprin for additional activity after Acute Coronary Syndrome (ACS), MI or after a Stent
  • Best choice when pt. allergic to Aspirin
  • Pts. w/ CYP2C19 and CYP3A4 are poor activators
  • SEx: Upset Stomach, Neurotropenia, Thrombocytopenia

Chopidogrel (Plavix)

Prasurgel (Effient)

Ticlopidine

3

  • reversible ADP-receptor antagonist 
  • Circumvents CYP450 activation
  • Pts. should NOT skip doses
  • Better efficacy than Clopidogrel

Ticagrelor

4

  • Inhibits Adenosine uptake by the platelet
  • increases cGMP and cAMP phoshodiesterases (PDEs)
  • Vasodilator which may lead to Headaches
  • Post operative prophylaxis of Thromboemboli w/ heart valves when given w/ alone.
  • Slow release w/ Asprin is phrophylactic for Stroke
  • SEx: Hypersensitivity, Hypotension

Dipyridamole

5

  • Binds to glycoprotein -  GPIIB/IIIA on platelets and prevents interaction between fibrinogen and IIb/IIIa
  • Fab fragment of monoclonal Ab directed toward GPIIB/IIIA protein → blocks interaction of platelets w/ vasculature and w/ each other → prevents thrombis for up to one week after administration
  • SEx: Excessive bleeding, Major Hemorrhage
  • A synthetic reversible, non-peptide inhibitor is also available.

Abciximab

Tirofiban

Eptifibatide

6

  • Secreted by Mast cells
  • Bind antithrombin proteins present in normal blood and dramatically enhance their activity
  • Catalyzes the activation of Antithrombin III - decrease activity of Factor IIa and Factor Xa
  • Immediate onset when given IV
  • Not cleared by the Kidneys
  • Negatively charged, sulfated mucopolysaccharides (glycosaminoglycans)
  • Tx: DVT, PE, MI,
  • SEx: HIT (antidote - Protamine sulfate)

Heparin

7

  • All drugs of this class end in -parin
  • Does not inhibit Thrombin, mainly inhibits Factor Xa which  means that aPPT is not monitored
  • Synthetic selective inhibitor of activated Factor Xa
  • Cleared by the Kidneys
  • Never given INTRAMUSCULARLY

Low MW Heparin

Fondaparinux (synthetic)

8

  • Synthetic derivative of hirudin (leeches salivary gland)
  • Reversible, direct Thrombin inhibitor
  • Inhibit Fibrin-bound as well as Circulating Thrombin
  • Alternative if pt. has HIT
  • Affects both aPTT and INR
  • Cleared by Kidneys

Lepirudin

Bivalirudin

9

  • Most frequently used Anticoagulant
  • Inhibits γ carboxylation of Vit. K-dependent clotting factors (Coag. Factors X, IX, VII, and II and Protein C and S), back to its active Hydroquinone form, inhibiting the carboxylation, depleting the co-factor of the rxn
  • Levorotary S-form is 4x more potent
  • No effect on already synthesized and carboxylated coag. factors
  • Tx: MI, reduced LVf, AF, Prosthetic heart valves, V Thromb
  • NO PREGNANCY: birth defect and abortion,
  • Extreme caution in pts. w/ Hepatic or Renal disease

Warfarin (Coumadin)

10

Dabigatran

Rivaroxaban

Apixiban

11

  • Thrombolytic drug that activates Plasminogen
    --> Plasmin
  • A protein produced by streptococci
  • Forms a stable complex w/ Plasminogen facilitating its conversion into plasmin not bound to fibrin clots
  • Tx: Acute MI, Stroke, PE
  • SEx: Surgery, Recent/Current bleeding, History of cranial bleeds, Allergic response in ~5% of patients.

Streptokinase (bacteria)

12

  • Fibrin-specific
  • Only activates Plasminogen molecules that are bound to fibrin clots
  • It does not induce systemic activation of plasmin, only on the Thrombus
  • Tx: Coronary Thrombolysis, Multiple PEs, DVTs, Acute MI, Stroke
  • SEx: Bleeding, Hemorrhage
  • Contra: Surgery, GI tract bleeding, Aneurysm, Hypertension, Active bleeding, etc.

Tissue Plasminogen Activator (tPA)

13

  • Inhibits PDE3, which ↑ cAMP levels and ↑ PKA activation
  • Vasodilation inhibits platelet aggregation
  • Indicated for intermittent claudication due to Peripheral Arterial Disease
  • Caution when used with drugs that inhibit CYP3A4 and CYP2C19

Cilostazol

14

  • Cleared by Hepatic CYP450s from the Liver
  • Use with caution in pts. w/ compromised Liver funtion
  • May lead to elevate INR values
  • Indicated for use in pts. in HIT-induced thrombosis and during Angioplasty

Argatroban

15

  • An enzyme produced by human kidney
  • Purified from cultured Kidney cells
  • Directly converts Plasminogen into Plasmin

Urokinase