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Intro to Pharmacology > Blood 2: Drugs Acting on the Blood and Blood Elements > Flashcards

Blood 2: Drugs Acting on the Blood and Blood Elements Flashcards

1
Q

Anti-coagulants are drugs are used to modify the cascade either when there is a ______ in coagulation or when there is ______ coagulation.

A

defect, unwanted

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2
Q

Examples of Anticoagulants:

A
  1. Heparin and LMWHs
    ❖ Dalteparin
    ❖ Enoxaparin
  2. Warfarin and Coumarin Derivates
    ❖ Dicumarol
    ❖ Acenocoumarol
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3
Q

List the steps of the clotting cascade

A

Different drugs act during different stages of the cascade.
Learn sights of action.

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4
Q

Inhibition of __________ is a key role in producing anticoagulant effects.

A

thrombin

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5
Q

Thrombin is a platelet ________.

A

activator

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6
Q

List the three steps of platelet aggregation.

A
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7
Q

How do these drugs affect the cascade?

A

These drugs have advantages over warfarin.
Dabigatran is a very promising drug. It is mostly used in humans and doses for animals are extrapolating.

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8
Q

Thrombin and Factor Xa Inhibitors are used on what species?

A

Factor Xa = Dogs, cats
Thrombin inhibitors = Dogs

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9
Q

What are the pros of Factor Xa Inhibitors?
▪ The PKs are ___________
▪ No ____________ is required
▪ Not affected by _________ changes
▪ Less ____-___ interaction (some molecules from ____ can influence coag factors produced).

A

▪ The PKs are predictable
▪ No monitoring is required
▪ Not affected by dietary changes
▪ Less drug-drug interaction (some molecules from diet can influence coag factors produced).

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10
Q

What are the cons of Factor Xa Inhibitors?
▪ ______ half-life
▪ Inability to _______ the bleeding
(new agent:_______)

A

▪Short half-life
▪ Inability to reverse the bleeding
(new agent: Andexanet)

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11
Q

What are the pros of Thrombin Inhibitor drugs?

A

Pros:
▪ Less drug-drug interaction (human)
▪ Reversal agent: Idarucizumab

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12
Q

What are the cons of Thrombin Inhibitor drugs?

A

▪ Adverse effects (bleeding)
▪ GI problems

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13
Q

List two examples of Factor Xa inhibitor drugs.

A

❖ Rivaroxaban
❖ Apixaban

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14
Q

List two examples of Thrombin inhibitor drugs.

A

❖ Dabigatran

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15
Q

Hemophilia is an _________ disorder, in which the blood does not _____ due to _________ clotting factors.

A

inherited, clot, insufficient

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16
Q

How is Hemophilia diagnosed?

A

Blood test measures how long it takes for blood to form a clot
Coagulation time test

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17
Q

How do you treat Hemophilia?
1. Blood ____________: Fresh frozen _______ (FFP) is the fluid portion of blood that contains all __________ factors. _____________ prepared from FFP, contains large amount of Factor ____ (_______________ factor).
They do not contain RBCs that have ______, ________ reaction is minimal.
Multiple transfusions throughout their _______.
Not _______ but with proper care, animal with hemophilia can live long and normal life. Do not want to ____ animal.

A
  1. Blood transfusion: Fresh frozen plasma (FFP) is the fluid portion of blood that contains all coagulation factors
    Cryoprecipitate prepared from FFP, contains large amount of
    Factor VIII (antihemophilia factor)
    They do not contain RBCs that have antigens, immune reaction is minimal
    Multiple transfusions throughout their lifetimes
    Not curable but with proper care, animal with hemophilia can live long and normal life. Do not want to breed animal.
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18
Q

Hemophilia A: lack (missing or defective) of factor _____.
- Genetic = ?
- the most _______ bleeding disorder.
- This is the most _____ form of the disease.

A

VIII, sex-linked –> carried in X
chromosome, inherited, severe

If female carries mutant and one normal gene, she will not have hemophilia. But she is a carrier. So she can pass this mutated X chromosome with mutated gene to son and daughter, but to son which has XY chromosome, Y chromosome does not have this gene so there is no protection and Male is hemophillic. More often HA is presented in males and rarely in females.

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19
Q

Symptoms of Hemophilia A:
▪ Spontaneously bleeding into ______ or _____ (________)
▪ Spontaneously bleeding under the ____ (__________)
▪ Hemorrhages into _____ or ________ cavity (can be _____)
▪ An _________ ________ from surgery site

A

muscles, joints, swelling, skin, hematoma, chest, abdominal, fatal, excessive bleeding

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20
Q

How is Hemophilia A diagnosed?
▪ During ______ or having ______
▪ In young animals who have extreme bleeding after _______ procedures (spay/neuter, vaccines)
▪ Abnormal bleeding of the _____
▪ Puppies and kittens who have severe deficiency of Factor ____
may be ________ or die _______ after the birth

A

surgery, trauma, routine, gums, VIII, stillborn, shortly

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21
Q

Factor VIII is a co-factor of Factor ____
for activation of Factor _____.

A

IX, X

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22
Q

Hemophilia B: lack (missing or defective) of Factor ____ (_______ Factor)
- genetic

A

IX, Christmas, Sex linked gene of X chromosomes. Females are carriers, symptomatic.

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23
Q

Symptoms of Hemophilia B:
▪ The same as HA but _____ disease
▪ ___________ bleeding into the ______, _________, or _______
▪ Not noticed until they become ______ Less _______ severe.

A

milder, Spontaneous, thorax, abdomen, brain, emergent, clinically

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24
Q

Which breeds of dogs and cats are susceptible to developing HB?

A

Labrador Retrievers
German Shepherds
Mixed-breed dogs
British short-haired cats
Siamese mix cats

Over 25 dog breeds can have HB.

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25
Q

Hemophilia C: an extremely rear deficiency of Factor ____.

A

XI, which is in chromosome 4 and is not sex related.

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26
Q

Symptoms of Hemophilia C:
▪ Bleeding is induced by _______ or ______
▪ Bleeding can be delayed for up to ? ________ in showing symptoms

A

trauma, surgery, 4 days, Duration

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27
Q

Which dog breeds are susceptible to Hemophilia C?

A
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28
Q

vW disease (VWD) is the most common _____ blood clotting disease in pet dogs. vWF protein is a specific _______ ______ in blood which is important for platelet adhesion.

A

inherited, clotting protein

29
Q

Which species depicted below is predisposed to a blood-factor disease?

A

Shetland sheepdog affected with severe (type 3) vWD

30
Q

VWD is not a?

A

Hemophilia

31
Q

Function of Platelets (_____________)
❖ Help to maintain _________ and _________ integrity
❖ Aid in healing injured _______ _______-
❖ Play role in ________

A

Thrombocytes, hemostasis, capillary,, blood vessels, inflammation

32
Q

Steps of platelet activation :

A

▪ Adhesion
▪ Shape changes
▪ Secretion of the granule contents
▪ Biosynthesis of labile mediators
▪ Aggregation
▪ Exposure of acidic phospholipid

33
Q

Healthy vascular endothelium prevents ?

A

platelet adhesion

34
Q

Platelets adhere to _________ or _________ areas and become activated changing _____ and exposing _______ charged
___________ and __________ (GP) ____/ _____ receptors, and synthesis and release of various mediators (?), which activate other platelets causing __________.

A

diseased, damaged, shape, negatively, phospholipids, glycoprotein, lIb/Illa, ADP, Thromboxane A, aggregation

35
Q

Aggregation entails _________ binding to and bridging between GP_____/_______ receptors on _________ platelets. These receptors can be targeted by? ____

A

fibrinogen, llb/IIIa, adjacent, Drugs

36
Q

Activated platelets constitute a focus for ________ formation

A

fibrin

37
Q

____________ factors and ________ factors are necessary for repair, but also implicated in ___________, are released during platelet ___________.

A

Chemotactic, growth, artherogenesis, activation

38
Q

Thrombosis is the pathological formation a “____________” plug
within the vasculature in the ________ of bleeding

A

hemostatic, absence

39
Q

3 predisposing factors to Thrombosis:
❖ Injury to the ?
❖ Altered blood _____
❖ Abnormal ________ of the blood

A

vessel wall, flow, coagulability

40
Q

Arterial thrombus: ___________, can interrupt blood flow causing _______ (________). Carotid emboli goes to an _____ in ______ or other organs causing _______ or ________.

A

atherosclerosis, ischemia, infarction, artery, brain, stroke, death

41
Q

Venous Thrombus: steams away in the flow into circulation
forming an _________, which goes to pulmonary _____ causing pulmonary _____.

A

embolus, artery, embolism

42
Q

A thrombus is a ________ _________ that occurs inside a blood vessel, and the word embolism describes
that the clot has traveled through a blood vessel to a location ____ from where it formed

A

blood clot, far

43
Q

Thrombotic diseases in animals:
Aortic Thromboembolism in cats

A
44
Q

Thrombotic diseases in animals:

A

❖ Feline cardiomyopathy
❖ Pulmonary endarteritis associated with heartworm disease
❖ Membranous glomerulonephritis
❖ Mild DIC (disseminated intravascular coagulopathy)
❖ Pulmonary thromboembolism
❖ Vasculitis
❖ Laminitis (horses)
❖ Navicular disease (horses)

Paisley Loves Fighting Meagan Very Much, Poor Nugget :(

45
Q

Antiplatelet drugs ______ platelet function

A

reduce

46
Q

Examples of antiplatelet drugs?

A

❑ Aspirin
❑ Clopidogrel
❑ Abciximab
(mab = moniclonal antibodies)

47
Q

Aspirin and Clopidogrel
* Both have _____ risk for serious hemorrhage
* Require less monitoring compared to ___________

A

low, warfarin

48
Q

Drug is at location they are working at mostly.

A

ADP is a platelet activator that causes platelet shape change, aggregation, and generation of thromboxan A2 which is secreted by COX 1

Aspirin inhibits COX and TXA2
Clopidogrel binds to P2Y12 receptor on adenosine recpetor and Abci = make MAB to GP IIb and IIIa
Activated platelets they have receptors GP IIIa?

49
Q

Aspirin (___________ ________) is an _______.

A

acetylsalicylic acid, NSAID

50
Q

Aspirin Blocks platelet __________ and ___________ in thromboembolic disease.

A

activation, aggregation

51
Q

Aspirin Has ________ and ________ effects

A

analgesic, antipyretic

52
Q

Aspirin is rapidly absorbed _____, protein binding is ______.

A

orally, extensive

53
Q

Salicylate is metabolized by the _____ enzyme. ____ lack the enzyme and therefore the t1/2 is ________ and less frequent _______ is required compared to ___.
* Salicylate / metabolites are excreted by the ________

A

liver, Cats, prolonged,, dosing, dog, kidney

54
Q

Adverse effects of Aspirin:

A

▪ Vomiting
▪ Ulceration
▪ Hematemesis
▪ **Serious GI bleeding (COX1 protects HI so if you inhibit this –> ulceration).

55
Q

Dogs do not respond to _______- doses of Aspirin in different studies. Dose for animals is not solidified.

A

low

56
Q

MOA: Aspirin at low doses ________ inhibits platelet ________ thereby preventing the formation of ?

A

irreversibly, cyclooxygenase, thromboxane A2.

57
Q

How does Aspirin act on COX at low doses? High doses?

A
58
Q

Aspirin is ___________, so in general esp in high doses can bind to COX ___ –> _______ –> reduces _________

A

nonselective, 2, analgesia, inflammation

59
Q

___________ (Plavix ) is a ______, its active metabolite blocks platelet _________.

A

Clopidogrel, prodrug,, aggregation

60
Q

What is Clopidogrel used for in cats? Dogs?

A

Cats: thrombi, embolic events
Dogs: hypercoagulable state

61
Q

Clopidogrel adverse effects?

A

▪ Vomiting
▪ Anorexia
▪ Diarrhea

62
Q

Clopidogrel MOA
Clopidogrel is an inhibitor of platelet ___________ and ________ through the ___________ binding of its active metabolite to the ______ class of adenosine receptors on platelets.

A

activation, aggregation, irreversible, P2Y12

63
Q

Only done in humans so far.
Dogs have the same SIPS as humans. Not known is dogs share the same metabolic pathway as humans.

Binds to ADP-P2Y12 receptor.

A
64
Q

_________ and Clopidogrel are used together
Clopidogrel is preferable in Vet Med (species?)

A

Aspirin, dogs, cats, horses, rabbits, calves

Clopidogrel is low cost

65
Q

Clopidogrel
▪ The tablet is fixed dose of 75 mg
▪ Effective inhibition of platelet _________ in dogs, superior to _____.
▪ In some dogs, which may have variants of _______ receptor, clopidogrel effects may be ______ or _____. Why? B/c need this receptor for Clopidogrel to bind to it. If no receptor, need much ______ doses of drugs –> _____ effects.

A

aggregation, aspirin, P2Y12, absent, diminished, higher, adverse

66
Q

Ticlopidine: is also _______ receptor inhibitor. _____ used in animals b/c not enough information. In cats, it produces ______ effects.

not anticoag? Works on platelets? Is that right?

A

P2Y12, Rarely, adverse

67
Q

Abciximab is a _________ __________ ___________ ____/____ receptor antibody
used to prevent _______ during percutaneous coronary intervention

A

monoclonal anti-glycoprotein, IIb/IIIa, thrombosis

68
Q

Abciximab MOA inhibits platelet __________ by ________ binding to platelet ____/____ receptor
▪ For prevention of cardiac ______ events in patients undergoing
percutaneous coronary intervention
▪ To prevent myocardial _____ in some patients
▪ For thrombolysis in some patients
_____ ____/___, which is expressed on the surface of human platelets, is a member of the _____ family of cell surface adhesion molecules. It plays a critical role in the binding of _______ (factor __), _____ and other
adhesive molecules to platelets, and subsequent platelet aggregation

A

aggregation, reversibly, IIb/IIIa , ischemic, infarction, GPIIb/IIIa, integrin, fibrinogen, I, von Willebrand factor (vWF)

69
Q

Aspirin inhibits COX 1 and TXA2
Clo binds to P2Y12 receptor in adenosine molecule
Abciximab which is moniclonal AB against GP 2b3A on the platelet.

A

Intro to Pharmacology (31 decks)

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