The document discusses anticoagulant drugs and their use, mechanisms, and side effects. It focuses on warfarin and heparin. Warfarin acts indirectly by interfering with vitamin K, lowering clotting factors. Heparin activates antithrombin III to inactivate coagulation factors. They are used to treat conditions involving blood clots and prevent clotting during procedures. Risks include bleeding as overdose is the most serious complication. Bridge therapy with heparin is used prior to surgery to reduce thromboembolism risk when discontinuing long-term anticoagulants.

1. Presentation on Pharmacology
ANTI
COAGULANTS
Apollo College of Pharmacy
Anjora Durg (2022-2023)
Guided by
Subiya khan
Saurav Anand Kaushik
Khileshwari Sahu
Sukhdas Jangade
Mr. Hari Prasad Sonwani
Submitted by

2. Perioperative management of patients on warfarin or antiplatelet therapy
involves assessing and balancing individual risks for thromboembolism
and bleeding.
Discontinuing anticoagulant and antiplatelet therapis usually necessary
for major surgery but increases the risk of thrombotic events.
Bridge therapy -ie, the temporary use of intravenous unfractionated
heparin (IV UFH) or low-molecular- weight heparin (LMWH) prior to
surgery in place of warfarin-, is an effective means of reducing the risk
of thromboembolism but may increase the risk of bleeding.
Introduction

3. Classification

4. Oral
Act indirectly by interfering with the synthesis of vit K
dependent clotting factors in liver.
Apparently behave as competitive antagonists of vit K and
lower the plasma levels of functional clotting factors in a
dose-dependent manner.
they inhibit the enzyme vit K epoxide reductase (VKOR) and
interfere with regeneration of the active hydroquinone form of
vit K which acts as a cofactor for the enzyme y-glutamyl
carboxylase.

6. Parenteral
Parenteral anticoagulants—unfractionated and low-molecular-
weight heparin—primarily are used to prevent and treat VTE
(deep vein thrombosis [DVT] and pulmonary embolism [PE])
associated with medical conditions such as atrial fibrillation,
heart disease, and atherosclerosis; they’re also used to
prevent clotting during dialysis and extracorporeal
circulation.

8. Functions
anticoagulant, Substance that prevents blood from clotting by
suppressing the synthesis or function of various clotting
factors

9. Mechanism of Action
1) Heparin : It prevent blood cloting in vivo (inside the body) as well
as in Vitro.
It Activates antithrombin III, which inactivates factors IX, and X in this
way coagulation is prevented.
2) Coumarin: Coagulation factors II, VII, IX and X are present in inactive
form, until they are carboxylated. These drugs act on Vitamin K and
prevent the synthesis of chemical that carboxylate these factors

12. Indications
To treat unstable angina.
To prevent coagulation in Heart failure.
To dissolve the clot in blood vessels.
Pulmonary embolism.
To prevent clotting during open heart surgery.

13. Contraindications
Bleeding disorders, history of heparin induced
thrombocytopenia.
Severe hypertension, threatened abortion, piles, g.i. ulcers.
Subacute bacterial endocarditis, large malignancies,
tuberculosis.
Ocular and neurosurgery, lumbar puncture.
Chronic alcoholics, cirrhosis, renal failure.

14. Recent trauma, recent surgery, recent abortion, recent stroke
severe Hypertension, severe Diabetes, severe liver damage,
peptic ulcer, and bleeding disorder.

15. Heparin Dose 5000-10000 unit /ml i.v
Warfarin Does 5-10 mg/d

17. Uses
Deep vein thrombosis (DVT) and pulmonary embolism (PE)
Myocardial infarction (MI)
Unstable angina
Rheumatic heart disease; Atrial fibrillation (AF)
Cerebrovascular disease
Vascular surgery, prosthetic heart valves, retinal vessel thrombosis,
extracorporeal circulation, haemodialysis
Defibrination syndrome or 'disseminated intravascular coagulation'

18. Adverse Effect
Bleeding due to overdose - most serious complication.
Thrombocytopenia - mild and transient.
Transient and reversible alopecia is infrequent. Serum
transaminase levels may rise.
Osteoporosis - long-term use of relatively high doses.
Hypersensitivity reactions - rare.

20. HEPARIN
Heparin is a non-uniform mixture of straight chain
mucopolysaccharides with MW 10,000 to 20,000.
It contains polymers of two sulfated disaccharide units:
D-glucosamine-L-iduronic acid
D-glucosamine-D-glucuronic acid
It is present in all tissues containing mast cells; richest
sources are lung, liver and intestinal mucosa.

22. ANTICOAGULANT ACTION OF
HEPARIN
HEPARIN
Activates plasma AT III
Heparin-AT III complex
↓
Binds to clotting factors of intrinsic and common pathways
(Xa, Ila, IXa, Xla, XIla and XIIIa) and inactivates them

23. OTHER ACTIONS OF HEPARIN
Heparin in higher doses inhibits platelet aggregation and
prolongs bleeding time.
Heparin in lower doses helps in lipaemia clearing.

24. PHARMACOKINETICS
Heparin is not absorbed orally.
If Injected i.v. - acts instantaneously.
After s.c. injection anticoagulant effect develops after ~60
min.
Bioavailability of s.c. heparin is inconsistent.
Heparin does not cross blood-brain barrier or placenta (it is
the anticoagulant of choice during pregnancy).

25. PREPARATION
Just 0.2 mL of sodium (lithium) heparin (1000 IU/mL) added to
5 mL of blood will give a final heparin concentration of 40
IU/mL blood, sufficient for anticoagulation. The principle
disadvantage of liquid heparin is a potential for error if blood
is over-diluted with heparin.

26. DOSAGE
Heparin Dose 5000-10000 unit /ml i.v

27. THERAPEUTIC USES
Anticoagulants are medicines that help prevent
blood clots. They're given to people at a high
risk of getting clots, to reduce their chances of
developing serious conditions such as strokes
and heart attacks. A blood clot is a seal created
by the blood to stop bleeding from wounds.

29. SIDE EFFECTS
chest pain,
irregular heartbeats,
shortness of breath,
dizziness,
anxiety,
sweating,

30. unusual bleeding or bruising,
severe pain or swelling in your stomach, lower back or
growing,
dark or blue-colored skin on your hands or
feet,
nausea,
vomiting,
loss of appetite,
unusual tiredness

32. References
TRIPATHI, K.D.(2018). ESSENTIALS OF MEDICAL PHARMECOLOGY
(8TH ED.).JAYPEE BROTHERS MEDICAL
PHARMACOLOGY OF ANTICOAGULANTS FROM SLIDESHARE.NET

33. THANK
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