Anticoagulant Drugs

Question 1

Anticoagulant Drugs Name

Answer 1

Indirect thrombin inhibitor(Prental)
1. UFH/Standard H/Regular Heparin
2. LMWH
* Enoxaparin
* Dalteparin
* Tinzaparin
Fondaparinux

Direct thrombin inhibitor(Parental)
1. Hirudin
2. Lepoirudin
3. Bovalirudin
4. Argatroban

Oral
Coumarin anticoagulant
1.Warfarin

Direct thrombin inhibitor(Oral)
Dabigatran

Direct factor Xa inhibitors
Rivaroxaban
apixaban
edoxaban
betrixaban

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Question 2

Heparin Why not Orally ?

Answer 2

1.(-) charge = less absorption
2.Digestion of heaprin by AMYLASE as its is a Mucopolysaccharide

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Question 3

Heparin why not IM ?

Answer 3

At the site of injection=HEMATOMA formation

IM injection = Bleeding = Dec coagulation = More bleeding =Hematoma

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Question 4

LMW heparin drugs ?

Answer 4

LMWH
* Enoxaparin
* Dalteparin
* Tinzaparin

hePARIN - All Drugs Contain PARIN

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Question 5

Heparin-Mechanism ?

Answer 5

H + ATIII = ATIII confromational change = ATIII more rapid interaction with factor IIa IXa Xa = ATIII-Cloting factor Complex formed = H/LMWH acts as a cofactor for ATIII = Inactivation of 3 clotting factor by ATIII = iNHIBIT blood coagulation

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Question 6

LMWH vs HMWH ?

Answer 6

HMWH inactivate =IIa IXa Xa factor
LMWH inactivate only Xa
Cause IIa IXa need - >= 18 monosaccharide
but LMWH have only 15

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Question 7

Indications /Clinical uses of Heparin ?
Say atleast 5

Answer 7

1. Acute MI
2. DVT
3. Unstable angina
4. Pulmonary embolism
5. DIC
6. Angiogram
7. Cerebral infraction

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Question 8

Adverse effects of Heparin ?

Answer 8

1. Hemorrhage
2. Hypersensitivity reactions
3. Thrombosis
4. Thrombocytopenia
5. Transient alopecia
6. Osteoporosis

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Question 9

Contraindications of Heparin ?

Answer 9

1. H induced thrombocytopenia
2. Hypersensitivity reactions
3. Uncontrolled HTN
4. Renal f
5. Hepatic f
6. CLD
7. Hemophilia
8. Purpura
9. Active bleeding
10. Pregnant women
11. TB

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Question 10

LMWH vs UFH

Answer 10

1. LMWH= Better SC bioavailability (70-80)%
2. Activated Partial Thromboplastin Time (APTT) not prolonged
3. Lab monitoring not required
4. 15 monosaccharide = Xa clot factor inactivate
5. Less = Frequent dose = A/E = Hemorrhagic complications = Thrombocytopenia
6. Better patient compliance = Suitable for out patient
7. T1/2 = Longer

Its Must 100%

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Question 11

Warfarin

Warfarin-Mechanism ?

Answer 11

Inactivate V-K epoxide reductase = Inhibit conversion of V-K EPOXIDE to its active form = Inhibit carboxylation of glutamic acid residue = II VII IX X (No activation) = Anticoagulant effetcs

2 7 9 10

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Question 12

Why warfarin Indirectly acting ?

Answer 12

Cause donot interfere with coagulation cascade - rather they inhibit V-K dependent clotting factors & anticoagulant effetcs

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Question 13

Indications /Clinical uses of Warfarin ??

Same as Heparin

Answer 13

1. MI
2. HF
3. PE
4. Systemic Embolism
5. DVT
6. Atrial fibrilation
7. TIA

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Question 14

Antidote of Warfarin ?

Answer 14

V-K

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Question 15

A/E of Warfarin ?

Answer 15

1.Bleeding disorder
2.Hypersensitivity
3.Rash
4.Alopecia
5.Purpura
6.Skin necrosis
7.Teratogenesis

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Question 16

Contraindications of Warfarin ?

Answer 16

1. Hemophilia
2. Purpura
3. Thrombocytopenia
4. Bleeding
5. Endocarditis
6. Renal f
7. Preganancy
8. TB
9. HTN

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Question 17

Drugs Promote bleeding ?

lecture note

Answer 17

1.Inhibtion of platelet= aspirin
2.Inhibition of clotting factor = heparin

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Question 18

Drugs that decrease warfarin activity ??

Answer 18

Promote clot factor activity = V-K
Reduce absorption = Colestipol
Induction of metabolizing enzymes = Phenytoin Barbiturates

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