DANIL
HAMMOUDI.MD
SINOE
MEDICAL ASSOCIATION
USMLE
QUESTIONS:
volume
of distribution: Vd= TOTAL AMOUNT OF DRUG
IN BODY
[] OF DRUG IN THE
PASMA
-WARFARIN
EXERTS ITS ANTICOAGULANTS EFFECT BY:
***INHIBITING THE CARBOXYLATION OF
PRO-CLOTTING FACTORS
WARFARIN
BLOCKS THE VIT K-DEPENDENT STEP IN THE SYNTHESIS OF CLOTTING FACTORS BLOCKING
THE STEP OF VIT K REGENERATION BY AN EPOXIDE REDUCTASE REQUIRING NADH.
-THE
THERAPEUTIC EFFECT OF SODIUM WARFARIN IS DEPENDENT ON THE HALF LIVES OF ALL THE
FOLLOWING COAGULATION FACTORS:
***II
***VII
***IX
***X
·
SODIUM
WARFARIN IS THE PROTOTYPE OF THE COUMARIN DERIVED ANTICOAGULANTS.
·
8-12
HOURS ARE REQUIRED FOR ACTION .
·
IT IS
99% BOUND TO PLASMA ALBUMIN
·
METABOLIZED
IN THE LIVER-EXCRETED IN THE URINE AND FECES.
·
FACTORS
AFFECTING ACTIVITY:
***CONDITIONS THAT INCREASE THE
RESPONSE TO ANTICOAGULANTS INCLUDE :
+++VIT K DEFICIENCY
+++HYPERMETABOLIC STATES,SUCH
HYPERTHYROIDISM.
+++DEBILATING STATES, SUCH
CONGESTIVE HEART FAILURE
+++AGE: THE OLDER THE PATIENT,
THE GREATER THE RESPONSE TO THESE COAGULANTS.
***WARFARIN INDUCE MICROSOMIAL ENZYMES
***EXCESSIVELY REDUCED LEVELS OF
PROTHROMBIN WILL RESULT IN HEMORRHAGE.
***DURING PREGNANCY, VIT K DEPENDANT
FACTORS ARE INCREASED, RESULTING IN DECREASED RESPONSIVENESS TO ORAL ANTICOAGULANTS.
SINCE HEPARIN DOES NOT CROSS THE PLACENTA,
IT IS CONSIDERED SAFE FOR THE FETUS.
THERAPEUTIC
USES: ***SECONDARY PROPHYLACTIC TRT OF
VENOUS THROMBOSIS
PULMONARY EMBOLISM.
PREVENT THE RECURRENCE OR
EXTENSION OF VENOUS THROMBUS FORMATION .
-SINCE ORAL ANTOCOAGULANTS HAVE NO EFFECT
ON PLATELETS, THEY ARE NOT USED IN THE TRT OF TROMBOTIC DISEASE IN THE ARTERIAL
SYSTEM.
ADVERSE
EFFECTS: -WARFARIN NECROSIS =PAINFULL
ERYTHEMATOUS PATCH ON THE SKIN ,WHICH CAN PROGRESS TO GANGRENE. 3-10DAYS OCCURS
OF STARTING WARFARIN THERAPY.
THROMBI OCCUR IN THE VASCULATURE OF
AFFECTED TISSUE.
- A PURPLE TOE SYNDROME CAN
OCCUR 3-8 WEEKS AFTER STARTING WARFARIN THERAPY . IT IS CAUSED BY CHOLESTEROL
EMBOLI FROM ATHEROMATOUS PLAQUES, FOLLOWING BLEEDING INTO THE PLAQUES.
- WARFARIN IS CONTRE INDICATED
IN PREGNANCY BUT NOT FOR THE NURSING MOTHER SINCE IT IS NOT EXCRETED IN MILK.
REVERSAL
ANTICOAGULANT EFFECTS:
VIT K1
[PHYTONADIONE] WILL ENHANCE TO RECOVERY
FOR
SEVERE HEMORRHAGE , PHYTONADIONE IS GIVEN INTRAVENOUSLY . PT RETURN TO NORMAL
6-12 HOURS.
DRUGS
INTERACTIONS WITH ORAL ANTICOAGULANTS
DRUGS EFFECT ON RESPONSE
TO ANTI COAG MECHANISM |
acetylsalicylic
acid i
decreased ADP release by platelets ,IMPAIRING
PLATELET AGGREGATION |
BARBITURATES- D INDUCE DRUG MICROSOMAL METABOLIZING SYSTEM |
GLUTHEMIDE |
CHOLESTYRAMINE D DECREASE HYPOPROTHROMBINEMIA; INCREASE PLASMA
CLEARANCE OF DRUG. |
CIMETIDINE I UNKNOWN |
CLOFIBRATE I DECREASE
PLATELET ADHESIVENESS |
INCREASE TURNOVER OF
VITAMIN K-DEPENDENT FACTORS |
DISULFIRAM-METRONIDAZOLE I |
·
HEPARIN:
·
ANTITHROMBIN
FACTOR
·
IT IS
AN ANTIPLATELET DRUG
·
IT
HAS NO EFFECT ON THE SYNTHESIS OF BLOOD COAGULATION FACTORS
·
DOES
NOT BLOCK PROTHROMBIN SYNTHESIS IN THE LIVER AS DO THE ORAL ANTICOAGULANTS
·
IHIBITS
CONVERSION OF PT
·
INTERFERE
WITH FORMATION OF FIBRIN.
·
. PT
RET
MORE ON
ANTIGOAGULANTS COMING UP SOON
Monday,
May 14, 2001