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Pharmacology 381 > Anticoagulants > Flashcards

Anticoagulants Flashcards

1
Q

Thrombus

A

clot adheres to vessel wall

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2
Q

Embolus

A

Intravascular clot that floats in vessel

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3
Q

Virchow’s triad

A
  • Injury to blood vessel
  • Altered blood flow
  • Abnormal coagulability of blood
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4
Q

Intrinsic Coagulation cascade

A

XII>XIIa>XIa>IXa>VIIIa> Xa> Xa+Va> conversion of prothrombin to thrombin> fibrinogen and platelets to site of injury

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5
Q

Extrinsic coagulation cascade

A

Tissue factor+ VIIa>Xa> intrinsic pathway combination

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6
Q

Main event in coagulation

A

Conversion of soluble fibrinogen to insoluble fibrin

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7
Q

MOA that maintains resting state of platelet

A

Endothelium release prostacyclin> synthesis of cAMP> stabilizes inactive GIIb/IIIa receptor and inhibits release of granules

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8
Q

Platelets after injury

A

Adhere to collagen on subendothelial surface> release ADP, thromboxane A2 and serotonin> platelets recruited to platelet plug> Increase levels of Ca2+> Release of granules, activation of thromboxane A2 synthesis and activation of GIIb/IIIa receptors

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9
Q

Anticoagulants

A
  • Heparin
  • LMWH
  • Warfarin
  • Antithrombin III-independent anticoagulants
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10
Q

MOA of Heparin

A
  • Activate antithrombin III and accelerated its action by 1000 fold. Which inhibits thrombin (IIa) and factor Xa
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11
Q

Onset duration of heparin

A

IV: immediate
Subcutaneous: 60min delay
* LMWH: longer half life
- LMWH: does not need to be monitored- predictable effects

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12
Q

Heparin side effects

A

-Haemorrhage
- Thrombocytopenia
- Hyperaldosteronism
- Hypersensitivity reactions

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13
Q

MO of warfarin (oral)

A

Inhibits vitamin K epoxide reductase> Interferes with post translational y-carboxylation of glutamic acid residues on clotting factors II, VII, IX and X> in turn reduces synthesis of vitamin K dependent coagulation factors

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14
Q

Drugs that reduce effect of warfarin

A
  • Vitamin K
  • Rifampicin
  • Cholestyramine
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15
Q

Drugs that potentiate effects of warfarin

A
  • Amiodarone
  • Aspirin
  • Chloral hydrate
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16
Q

Warfarin side effects

A
  • Haemorrhage
  • Purple toe
  • induced skin necrosis
17
Q

Reversing effects of warfarin

A
  • Vitamin K
  • Oral activated charcoal
  • Frozen plasma
  • Oral cholestyramine
18
Q

antithrombin III independent hirudins

A
  • Derived from medical leech
    -Lepirudin> irreersibly bind to fibrin-binding & thrombin catalytic sites
  • Bivalirudin> aspirin+clopidogrel
19
Q

Antithrombin III independent drugs excluding hirudins

A
  • Dabigatran etexilate
  • Rivaroxaban
  • Apixaban
20
Q

Antithrombin III independent drug adverse effects

A
  • bleeding
  • nausea
  • anaemia
21
Q

Antiplatelet drugs

A
  • Aspirin
  • Dipyridamole
  • Adenosine receptor antagonist
  • Glycoprotein IIb/IIIa receptor antagonist
22
Q

MOA of aspirin

A

Irreversibly acetylates COX-I> inhibits platelet thromboxane 2 synthesis, preventing platelet aggregtion

23
Q

Chronic use of aspirin

A
  • combine with proton pump inhibitor
  • Decreased reabsorption in the stomach
24
Q

MOA of dipyridamole

A

Blocks adenosine uptake into RBC> inhibits phosphodiesterase and thromboxane A2 synthesis> inhibits platelet activation. also increases activity of aspirin.

25
Q

Adenosine receptor antagonist drugs and their MOA

A
  • Thienopyridine
  • prasugrel, clopidogrel (combinations with aspirin)
  • irreversible adenosine receptor antagonist> inhibit platelet aggregation
26
Q

GPIIa/IIIb receptor antagonist drugs

A
  • Abciximab
  • Tirofiban
  • Eptifibatide
27
Q

Fibrinolytic system

A

Plasminogen activators> cleave plasminogen to release plasmin> plasmin fibrin and fibrinogen> fibrin degradation products (FDP)

28
Q

Fibrinolytic classes and their drugs

A
  • tPA: alteplase, retaplase
  • Streptokinases: anistreplase
  • Urokinase
29
Q

MOA of fibrinolytics

A

Activate conversion of plasminogen> breaks cross-links between fibrin> dissolves clots> reopen occluded arteries

Pharmacology 381 (7 decks)

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