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Oral anti coagulants ppt

UNDER GRADUATE CLASS ON ORAL ANTICOAGULANTS

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Oral anti coagulants ppt

  1. 1. ORAL ANTICOAGULANTS Dr. RENJU.S.RAVI MD
  2. 2. HEMOSTASIS
  3. 3. PLATELET PLUG FORMATION
  4. 4. COAGULATION CASCADE
  5. 5. ANTICOAGULANTS I) USED INVIVO PARENTERAL  Unfractionated heparin (UFH)  Low molecular weight heparin(LMWH) – Enoxaparin, Dalteparin, Ardeparin, Nadroparin, Pamparin, Reviparin, Tinzaparin  Heparinoids- heparan sulfate, danaproid, ancrod  Fondaparinux  Direct thrombin inhibitor – lepirudin, argatroban bivalirudin  Drotrecogin Alfa – human recombinant activated protein C
  6. 6. ORAL  Coumarin derivatives- bishydroxycoumarin, Warfarin, acenocoumarol, ethylbiscoumacetate  Indanedione derivative- Phenindione II)USED INVITRO  Heparin- 150 U for 100 ml blood  Calcium complexing agents – sodium citrate, sodium oxalate, sodium edetate
  7. 7. WARFARIN  Discovered after report of hemorrhagic disorder in cattle ingested spoiled sweet clover (d/t dicoumarol) – Campbell & Link  Racemic mixture of R & S isomers f. II, VII, IX,X Carboxylated f.II,VII,IX,X
  8. 8. WARFARIN  Rapid, complete absorption from GIT  Plasma half life 36-42 hrs  >97% PPB  S isomer oxidative metabolised by CYP2C9  2 variants CYP2C9*2,CYP2C9*3 – reduced activity
  9. 9. WARFARIN cont…  Crosses placenta  Resistance with advanced GI Cancer & hereditary  Started at 5-10 mg dose along with parenteral anticoagulant for 5 days  Monitored by PT with target INR 2-3; 2.5 – 3.5 in pts with mechanical prosthetic valves
  10. 10. DRUG INTERACTIONS
  11. 11.  Long acting sulfonamides, Phenytoin, Indomethacin, Probenecid, phenylbutazone displace warfarin from plasma protein binding
  12. 12. SIDE EFFECTS  BLEEDING withhold drug - INR 3.5-4.5 asymptomatic S/L vit K - INR > 4.5 1 mg vit K - INR 4.9 – 9 2 -3 mg vit K - INR >9 10 mg slow IV along with FFP if excessively high  SKIN NECROSIS – in pts with cong or acq def of protein C/S  TERATOGENIC EFFECTS – nasal hypoplasia, stippled epiphysis
  13. 13. OTHER COUMARIN DERIVATIVES  Bishydroxy coumarin (Dicoumarol) Slowly absorbed, poor GI tolerance  Acenocoumarol half life 24 hrs, acts rapidly S/E – spontaneous haemorrhage, stomatitis, dermatitis, alopecia  Ethyl biscoumacetate (Tromexane) Rapid & brief action, difficult to maintain S/E - spontaneous haemorrhage, alopecia
  14. 14. ORAL DTI  Advantages incl predictable PK, so fixed dosing can be given and routine monitoring unnecessary  Do not interact with P450 interacting drugs  Rapid onset & offset of action  XIMELAGATRAN – first oral DTI approved but withdrawn d/t hepatotoxicity  DABIGATRAN- recently approved in Europe for Px of VTE in pts undergone hip, knee surgery Equivalent efficacy & safety to LMWH No routine monitoring required
  15. 15. ORAL FACTOR Xa INHIBITOR RIVAROXIBAN  First oral factor Xa inhibitor to reach phase III trial  Safety & efficacy atleast equivalent or better to LMWH for preventing DVT  NO routine monitoring necessary  Also in trial for Rχ of Venous thromboembolism & prevention of stroke in AF

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