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PODA2 MedChem Thrombolytics

Total questions: 44

Worksheet time: 30mins

Name
Class
Date
1.

What factor is the common pidpoint for the Intrinsic and Extrinsic pathways?

a)

Factor X

b)

Factor II

c)

Factor IX

d)

Factor VII

2.

What type of bond is formed between Glutamine and Lysine when it is combined to form the cross-linked insoluble fibrin?

a)

Ionic

b)

Hydrogen

c)

Isopeptide

d)

Covalent

3.

What enzyme is the catalyst that forms isopeptide bonds between lysine and glutamine side chains of distinct fibrin molecules

a)

transamidase

b)

hydroxylase

c)

Factor XIIIa

d)

Factor IIa

4.

What forms of VitaminK do coumarins inhibit the conversion of?

a)

Vitamin K (hydroxyquinone)

b)

Vitamin K (quinone)

c)

Vitamin K 2,3-epoxide

5.

What enzymes do coumarins inhibit in Vitamin K conversion?

a)

Vitamin K 2,3- quinone reductase

b)

Vitamin K dependant carboxylase

c)

Vitmain K 2,3- epoxide reductase (VKORC1)

6.

What is the active confirmation of warfarin?

a)

epoxide

b)

dibenzene

c)

cyclic hemiketal

d)

coumarin

7.

Is warfarina weak acid or base?

a)

Acid

b)

Base

8.

A substitution of what carbon of warfarin affects its pharmacokinetics and toxilogic properties?

a)

5

b)

4

c)

3

d)

2

9.

What confirmation of warfarin is 4 times more potent?

a)

R

b)

S

10.

What enzyme is responsible for primarily metabolizing the S isomer of warfarin?

a)

CYP3A4

b)

CYP1A2

c)

CYP2C19

d)

CYP2C9

11.

What enzyme is responsible for primarily metabolizing the R isomer of warfarin?

a)

CYP3A4

b)

CYP1A2

c)

CYP2C19

d)

CYP2C9

12.

What medications are CYP2C9 inhibiotrs?

a)

Metronidiazole

b)

Cordarone

c)

Diflucan

d)

Trimethoprim / Sulfamethoxazole

13.

Individuals with what variants require reduced warfarin dosing?

a)

VKORC1

b)

CYP2C9

c)

VKORC2

d)

CYP2C19

14.

Warfarin is what type of analog

a)

Lactone

b)

Lactam

c)

Cyclic Ester

d)

Cyclic Amide

15.

What is warfarin's bioavaialbilty percentage?

a)

50%

b)

60%

c)

75%

d)

100%

16.

Describe warfarin's MOA

4 lines
17.

Warfarin has how many chiral centers

a)

1

b)

2

c)

3

d)

none

18.

What are examples of CYP2C9 inducers?

a)

Barbiturates

b)

St John's Wort

c)

Rifampin

d)

Phenytoin

19.

What are the three types of Heparin anticoagulants?

a)

Unfractionated heparin,

b)

Low molecular Weight Haparin

c)

Dabigitran

d)

Fondiparinux

20.

Heparin is composed of a heterogeneous mixture of straight-chain,____ , and ____ charged mucopolysaccharides of a molecular weight range of 5 to 30 kd

a)

Sulfated

b)

Oxidated

c)

Negatively

d)

Positivley

21.

T/F: Heparin is derived from animals?

a)

True

b)

False

22.

Is heparin an acid or base?

a)

Acid

b)

Base

23.

What salt form of heparin is used in blood sample collection tubes but not in vivo?

a)

Calcium

b)

Sodium

c)

Lithium

24.

Heparin cannot be given orally due to stomach acids breaking it down. What parenteral for should heparin not be given?

a)

IV

b)

SC

c)

IM

25.

The binding between heparin and antithrombin III consists of ____ bonding between sulfate and carboxylate anions

a)

Ionic

b)

Covalent

c)

Hydrogen

d)

Van der Waals

26.

What amino acids in antithrombin III are invloved in binding with heparin

a)

Argenine

b)

Lysine

c)

Guanine

d)

Leucine

27.

Why does haprain have only 30% bioavailability compared to enoxaparin's 90%?

a)

Heparin has specific binding compred to enoxaparin

b)

Heparin has nonspecific binding compred to enoxaparin

c)

Enoxaparin has more specific binding compred to heparin

d)

Enoxaparin has nonspecific binding compred to heparin

28.

What are the two metabolic reactions of heparin?

a)

Oxidation

b)

Polymerization

c)

Rapid depolymerization

d)

Desulfation

29.

What protein does heparin have a very high affinity for?

a)

Antithrombin I

b)

Antithrombin II

c)

Antithrombin III

d)

Antithrombin IV

30.

What Factor is LMWH selective for?

a)

XIIa

b)

IIa

c)

XIIa

d)

Xa

31.

What is Arixtra's MOA?

a)

binds to antithrombin III

b)

inactivates antithrombin III

c)

activates antithrombin III

d)

Indirect inhibitor of activated factor Xa

32.

Select the correct order of molecular weight of the heparin products below largest to smallest

a)

UFH, Fondaparinux, LMWH

b)

Fondiparinux, LMWH, UFH

c)

LMWH, UFH, Fondiparinux

d)

UFH, LMWH, Fondiparinux

33.

This heparin product is excreted unchanged through the kidneys.

a)

Heparin porcine

b)

Heparin bovine

c)

Enoxaparin

d)

Fondiparinux

34.

What characteristics do all heparin products share?

a)

Basis

b)

Sulfated, saccharides

c)

Negatively charged physiol pH

d)

Acidic

35.

Which heparin products undergo depolymerization and desulfonation metabilism in the liver?

a)

UFH

b)

LMWH

c)

Fondiparinux

36.

Where does the direct thrombin inhinitor Hirudin derived from?

(a)  

37.

T/F: Direct thrombin inhibitors bind to and inactivate only free thrombin

a)

True

b)

False

38.

Which direct thrombin inhibitors are synthetic non-peptides?

a)

Bivalirudin

b)

Hirudin

c)

Argatroban

d)

Dabigitran

39.

Select the correct grouping of binding in the DTIs below

a)

Bivalent- Desirudin, Bivalirudin, Argatroban

b)

Bivalent- Argatroban, Dabigatran etexilate, Bivalirudin

c)

Univalent- Argatroban, Bivalirudin, Hirudin

d)

Univalent- Argatroban, Dabigatran etexilate

40.

What DTIs below have reverisble binding?

a)

Bivalirudin

b)

Argatroban

c)

Dabigitran etexilate

d)

Hirudin

41.

What DTI is short acting, has a rapid onset and is less immunogenic?

a)

Argatroban

b)

Dabigitran

c)

Bivalrudin

d)

Desirudin

42.

What amino acid is attached to argatroban?

a)

Argenine

b)

Lysine

c)

Asparagine

d)

Glysine

43.

Which DTI is a double prodrug?

a)

Argatroban

b)

Dabigatran etexilate

c)

Bivalirudin

d)

Leprirudin

44.

Why is Pradaxa manufactured as a tarttaric acid?

a)

Increase bioavailability

b)

Provide an acidic environment to increase bioavailabilty

c)

Protect from degredation

d)

Protect the stomach

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