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DR.SUMITHA A MBBS.,MD
ASSISTANT PROFESSOR
PHARMACOLOGY
I. Used in vivo
A. Parenteral anticoagulants
(i) Indirect thrombin inhibitors: Heparin, Low
molecular weight heparins, Fondaparinux,
Danaparoid
(ii) Direct thrombin inhibitors: Lepirudin,
Bivalirudin, Argatroban
B. Oral anticoagulants
(i) Coumarin derivatives: Bishydroxycoumarin
Warfarin sod, Acenocoumarol
Ethylbiscoumacetate
ANTICOAGULANTS
ii) Indandione derivative: Phenindione.
(iii) Direct factor Xa inhibitors: Rivaroxaban
(iv) Oral direct thrombin inhibitor: Dabigatran
etexilate
II. Used in vitro
A. Heparin:
150 U to prevent clotting of 100 ml blood.
B. Calcium complexing agents: Sodium citrate
ORAL ANTICAGULANTS -WARFARIN
ORAL ANTICAGULANTS
Warfarin Dose
 Prophylaxis and treatment of venous thrombosis and its
extension, pulmonary embolism (PE)
 Initial dose: 2-5 mg PO qDay for 2 days.
 Initiate warfarin on day 1 or 2 of LMWH or
unfractionated heparin therapy and overlap until desired
INR,then discontinue heparin.
 Check INR after 2 days and adjust dose according to
results
 Maintenance dose - 2 and 10 mg/day
Adverse effects
 Bleeding-ecchymosis,hematuria,bleeding in git.
 Occurs if INR –Exceeds 4
 INR-International normalised ratio.
 INR-ratio of prothrombin time during treatment with
ora;l anticoagulant with normal value of prothrombin
In healthy people an INR of 1.1 or belowis normal.
2.Teratogenic effects:
Foetal warfarin syndrome- hypoplasia of nose.eye
socket,hand bones ,growth retardation.
3.Alopecia,dermatitis,diarrhoea
Adverse effects
 Bleeding-ecchymosis,hematuria,bleeding in git.
 Occurs if INR –Exceeds 4
 INR-International normalised ratio.
 INR-ratio of prothrombin time during treatment with
ora;l anticoagulant with normal value of prothrombin
In healthy people an INR of 1.1 or belowis normal.
2.Teratogenic effects:
Foetal warfarin syndrome- hypoplasia of nose.eye
socket,hand bones ,growth retardation.
3.Alopecia,dermatitis,diarrhoea
DRUG INTERACTIONS OF WARFARIN
Newer oral anticoagulants
Direct factor Xa inhibitors: Rivaroxaban,apixaban,Edoxaban
Apixaban-10 mg BD for 7 days followed by 5 mg BD.For TREATMENT
OF DVT and PE.
Oral direct thrombin inhibitor: Dabigatran
Etexilate.
Rapid onset and offset of therapeutic effect.
Short half life
No laboratory monitoring required
Lower risk of bleeding
Fewer drug interactions
Antithrombotic efficacy equal to warfarin.
 THANK YOU

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Oral anticoagulants

  • 1. DR.SUMITHA A MBBS.,MD ASSISTANT PROFESSOR PHARMACOLOGY
  • 2. I. Used in vivo A. Parenteral anticoagulants (i) Indirect thrombin inhibitors: Heparin, Low molecular weight heparins, Fondaparinux, Danaparoid (ii) Direct thrombin inhibitors: Lepirudin, Bivalirudin, Argatroban B. Oral anticoagulants (i) Coumarin derivatives: Bishydroxycoumarin Warfarin sod, Acenocoumarol Ethylbiscoumacetate ANTICOAGULANTS
  • 3. ii) Indandione derivative: Phenindione. (iii) Direct factor Xa inhibitors: Rivaroxaban (iv) Oral direct thrombin inhibitor: Dabigatran etexilate II. Used in vitro A. Heparin: 150 U to prevent clotting of 100 ml blood. B. Calcium complexing agents: Sodium citrate
  • 6. Warfarin Dose  Prophylaxis and treatment of venous thrombosis and its extension, pulmonary embolism (PE)  Initial dose: 2-5 mg PO qDay for 2 days.  Initiate warfarin on day 1 or 2 of LMWH or unfractionated heparin therapy and overlap until desired INR,then discontinue heparin.  Check INR after 2 days and adjust dose according to results  Maintenance dose - 2 and 10 mg/day
  • 7.
  • 8.
  • 9.
  • 10. Adverse effects  Bleeding-ecchymosis,hematuria,bleeding in git.  Occurs if INR –Exceeds 4  INR-International normalised ratio.  INR-ratio of prothrombin time during treatment with ora;l anticoagulant with normal value of prothrombin In healthy people an INR of 1.1 or belowis normal. 2.Teratogenic effects: Foetal warfarin syndrome- hypoplasia of nose.eye socket,hand bones ,growth retardation. 3.Alopecia,dermatitis,diarrhoea
  • 11. Adverse effects  Bleeding-ecchymosis,hematuria,bleeding in git.  Occurs if INR –Exceeds 4  INR-International normalised ratio.  INR-ratio of prothrombin time during treatment with ora;l anticoagulant with normal value of prothrombin In healthy people an INR of 1.1 or belowis normal. 2.Teratogenic effects: Foetal warfarin syndrome- hypoplasia of nose.eye socket,hand bones ,growth retardation. 3.Alopecia,dermatitis,diarrhoea
  • 12.
  • 14. Newer oral anticoagulants Direct factor Xa inhibitors: Rivaroxaban,apixaban,Edoxaban Apixaban-10 mg BD for 7 days followed by 5 mg BD.For TREATMENT OF DVT and PE. Oral direct thrombin inhibitor: Dabigatran Etexilate. Rapid onset and offset of therapeutic effect. Short half life No laboratory monitoring required Lower risk of bleeding Fewer drug interactions Antithrombotic efficacy equal to warfarin.
  • 15.