Anticoagulant, classification of anticoagulant
Classification of Heparin and Warfarin ( mechanism of action, clinical use,pharmacokinetics, adverse drug reaction,contraindications)
2. WHAT ARE ANTI-COAGULANTS ?
ANTI-COAGULANTS are the drugs that helps
prevent the blood clot.
Why do we give anticoagulants ?
Anti – coagulants are given to those people
who are at high risk of getting clots.
To reduce their chances of developing serious
conditions like strokes and heart attacks .
These are also known as BLOOD THINNERS
3. MECHANISM OF
ACTION
• They act by inhibiting the action of
coagulation factors .
• They interfere the synthesis of
coagulation factors .
7. HEPARIN
HEPARIN is a non-uniform mixture of poly-saccharide with molecular weight of 10000 to 20000 Dalton .
It is used to decrease the clotting ability of the blood and help prevent harmful clots
from forming in blood vessels .
It was discovered by JAY MCLEAN in 1916.
The source of the commercial heparin is mucosa of pig intestine and ox liver.
It contains polymer of two sulphated disaccharide unit –
• D-glucosamine – L – iduronic acid
• D-glucosamine – D – glucuronic acid .
8. MECHANISM OF ACTION
HEPARIN binds to and then activates confirmational change in
ANTITHROMBIN III (AT)
HEPARIN – AT III COMPLEX binds to clotting factors of INTRINSIC and
COMMON PATHWAYS and inactivates them .
ANTICOAGULATION EFFECT QUICKLY
HEPARIN – AT III COMPLEX binds to clotting factors – Xa, IIa, IXa, XIa and
XIIa and inactivates them
9. PHARMACOKINETICS
1. Large highly ionized molecule ; not absorbed orally.
2. Instantaneous Anticoagulant effect after IV injection.
3. Effect in about 60 min after subcutaneous injection.
4. Does not cross Blood – brain barrier and placenta.
5. Metabolized in LIVER BY HEPARINASE.
6. Excreted in urine – t1/2 is 1 hr after IV injection.
7. Heparin binds nonspecifically to plasma proteins ,
mono-nuclear cells and endothelial cells.
CLINICAL USAGE
1. ANTI- COAGULANT
2. ANTI-PLATELET
3. LIPAEMIA CLEARING
10. ADVERSE EFFECTS
1 BLEEDING : a .HEMATURIA , b. GINGIVAL BLEEDING , c. EPISTAXIS ,
d . HEMOPTYSIS ,e . MELENA .
Severe dosage of HEPARIN can be treated with PROTAMINE SULPHATE .
!
3.OSTEOPOROSIS
2. THROMBOCYTOPENIA
a b c
d e
12. WARFARIN
WARFARIN is an oral anticoagulant which shows effect in in
vivo condition .
It was first used as an anti-coagulant in1951.
The commercial preparation of WARFARIN is a mixture of
DEXTRO (R) and LEVO (S) rotatory and the S form is more
potent than R form .
13. MECHANISM OF ACTION
It acts by interfering with the synthesis of vitamin K and vitK dependent clotting
factor in liver .
They inhibit the enzyme vit K EPOXIDE REDUCTASE and interfere with regeneration
of the active HYDROQUINONE form of vit K , which act as a co-factor for the enzyme
ALPHA GLUTAMYL CARBOXYLASE.
14. PHARMACOKINETICS
ABDORPTION:
ORALLY RAPIDLY AND
COMPLETELY
99% PROTEIN
BOUND
DISTRIBUTION METABOLISM :
BY MICROSOMAL
ENZYME IN LIVER
EXCRETION :
IN URINE
t1/2 – 2-4 HRS .
ADVERSE DRUG EFFECT
1 . HEMATURIA 2. HAEMORRHAGE 3. ECCHYMOSIS
4 . BLEEDING IN
BRAIN AND GIT
15. CONTRAINDICATIONS
I. IT SHOULD NOT BE GIVEN DURING PREGNANCY.
II. WARFARIN GIVEN IN EARLY PREGNANCY INCREASES BIRTH
DEFECTS.
III. GIVEN LATER IN PREGNANCY CAN CAUSE CNS DEFECTS, FETAL
HAEMORRHAGE AND FETAL DEATH.
16. REFERENCE
• ESSENTIALS OF MEDICAL PHARMACOLOGY 6TH ED – K.D TRIPATHI
• Dr. Shikha Parmar classes – https://youtube.be/AJzIHV1FOgU
• - https://youtube.be/VuA_J_oErnE
• Slideshare.net – ANTICOAGULANTS BY INDRAJ SAINI.
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