ANTICOAGULANTS

NATURAL ANTICOAGULANT MECHANISM

• ANTITHROMBIN

• PROTEIN C

• THROMBOMODULIN

• PROSTAGLANDIN I2

• TISSUE FACTOR PATHWAY INHIBITOR

 PARENTERAL ANTICOAGULANT THERAPY
(HEPARIN AND DERIVATIVES)
• STANDARD – HEPARIN

• LMWH – ENOXAPARIN, DALTEPARIN

• SYNTHETIC HEPARIN DERIVATIVES – FONDAPARINUX,

IDRAPARINUX
 PARENTERAL ANTICOAGULANT (HEPARIN)

• HEPARIN IS COMMONLY EXTRACTED FROM PORCINE

INTESTINAL MUCOSA OR BOVINE LUNG
 MECHANISM OF ACTION
• ENHANCES THE ACTIVITY OF ANTITHROMBIN – ON
THROMBIN, FACTORS IXA AND XA

• HEPARIN INCREASES THE RATE OF THE THROMBIN-

ANTITHROMBIN REACTION AT LEAST A THOUSANDFOLD BY
SERVING AS A CATALYTIC TEMPLATE TO WHICH BOTH THE
INHIBITOR AND THE PROTEASE BIND
 OTHER EFFECTS

• PLATELET INHIBITION – PROLONGS BLEEDING TIME

• INCREASED LIPOPROTEIN LIPASE ACTIVITY

• REBOUND HYPERLIPIDEMIA
 CLINICAL USES
• DEEP VENOUS THROMBOSIS/ PULMONARY EMBOLISM (
CONCURRENT ORAL THERAPY)

• USA, ACUTE MI

• POST PTCA, STENTING

• DURING USAGE OF CPB IN CARDIAC SURGERIES

• DIC

• DOC DURING PREGNANCY

 LMWH

• PERMIT ADMINISTRATION IN A FIXED OR WEIGHT-ADJUSTED

DOSAGE

• MONITORING IS NOT DONE ROUTINELY

• HIGH RISK OF FETAL MALFORMATIONS

• LOWER INCIDENCE OF HEPARIN INDUCED THROMBOCYTOPENIA

 SYNTHETIC
• LONG HALF LIFE -17 TO 21 HOURS/ IDRAPARINUX (5-6 DAYS)
• AFTER HIP AND KNEE SURGERY
 ADR

• BLEEDING

• HIT

• RESISTANCE

• REDUCTION IN ALDOSTERONE

• OSTEOPOROSIS
 OTHER PARENTERAL AGENTS

• LEPIRUDIN

• ARGATROBAN

• DANAPAROID

• DROTRECOGIN ALPHA
 ORAL ANTICOAGULANT( WARFARIN)
• COUMARIN
• ACTS AS ANTIDOTE FOR VITAMIN K – INHIBITS THE ACTIVATION OF
VITAMIN K DEPENDENT COAGULATION FACTORS LIKE II, VII, IX AND X
 DRUG INTERACTIONS

• DECREASES METABOLISM – ERYTHROMYCIN,

KETOCONAZOLE, AMIODARONE, ISONIAZID
• INCREASES METABOLISM – BARBITURATES, RIFAMPICIN
• ANTIBIOTICS REDUCE INTESTINAL FLORA
• NSAIDS
• OLD AGE
 ADR
• BLEEDING
• TERATOGENICITY
• PURPLE TOE SYNDROME
• SKIN NECROSIS
 CLINICAL USES
• DVT/ PE
• ORTHOPAEDIC SURGERIES
• MI
• PROSTHETIC VALVES
• CHRONIC AF