Coagulation Pharm

Question 1

• Uses? (3)
  1. ) Prevent thrombin formation: Pathway affected? Complications? (3) 1.) Countered with? 2.) Can be due to? % pts? Less common in? 3.) Due to? Alternative?
  2. ) Fibrinolytic to lyse: Pathway affected?
  3. ) Anti plt’s?

Answer 1

• Orevent plaque, DVT, A fib thrombi
• Fibrinogen –> fibrin; 1.) Bleeding; Protamine sulfate to bind up (-) charge 2.) Heparin induced thrombocytopenia; Ab’s attacking plt’s; 3-5%; LMWH 3.) Allergic Rxn; oversulfated chondroitin
• Drugs from leeches
  2. ) Plasmin to breakup fibrin
  3. ) ASA and such

Question 2

Unfractionated Heparin:

• Found where naturally?
• Structure?
• M of A?
• Absorption? (2)
• Half life?
• Cross placenta?
• Usage? (4)
• AR?

Answer 2

• Mast cells
• Proteoglycan linked with ploysaccharide with high (-) charge density which decreases bio
• Binds antithrombin 3 and thrombin which increases rate of thrombin inactivation; high decay of 9a,10a, 12a
• No absorbed GI; IV; or subcut for slower
• Short
• No
• DVT, PE, stent, dialysis
• Bleeding, allergic, thrombocytopenia

Question 3

LMW Heparins:

• 3 drugs?
• Structure?
• M of A?
• Absorption?
• 1/2 life? Bio avail?
• Usage?
• AR?

Answer 3

• levonax, nadroparin, dalteparin
• Proteoglycan linked with deploymerization (1/3 size)
• Binds and inactivates F10 by antithrombin; cannot inhibit thrombin
• SQ
• Higher; more predictable
• DVT, PE, stent, dialysis
• Bleeding, allergic, thrombocytopenia

Question 4

Fondaparinax:

• Structure?
• M of A?
• Absorption?
• 1/2 life? Bio avail?
• Usage? (2)
• AR?

Answer 4

• Minimal sequence in heparin to bind anti thrombin
• Binds and inactivates F10 by antithrombin; cannot inhibit thrombin
• SQ
• Higher; more predictable
• DVT, PE, stent, dialysis
• Bleeding, allergic, thrombocytopenia; also used with anticoagulants and fibrinolytics

Question 5

Warfarin:

• Structure?
• M of A?
• Absorption?
• Half life?
• Bio avail?
• Takes how long until effective?
• Usage? (3)
• AR? (3)

Answer 5

• Vitamin K analogue
• Inhibit use of vit k as cofactor; F2,7,9,10 can’t gamma carbox and therefore can’t bind Ca (non functional)
• Po
• Long
• Good
• 2-3 days
• Prevent DVT, A fib, heart valve
• hemmorhage, can’t be used with pregnancy, many drug-drug interactions

Question 6

Fibinolytic agents (Urokinase/Streptokinase):

• M of A?
• Usage? (4)
• AR?

Answer 6

• Convert plasminogen to plasmin to degrade fibrin clots
• MI within 12 hours; within 3 hours
• Breaks up all clots

Question 7

• Anti- platelets:
• ASA M of A?
• ADP receptor antagonist M of A?
• GP2b3A inhibitors M of A?

Answer 7

• Irreversibly inactivates COX to prevent TXA2
• Bind ADP receptor inihibiting secretion of alpha granules blocking GP2B3A
• Blocks receptor used for fibrin