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Med Chem Cardio > Test 4: Chronic Heart Disease > Flashcards

Test 4: Chronic Heart Disease Flashcards

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1
Q

What is the drug class of Digoxin?

A. PDE inhibitor (positive inotropic)

B. Cardiac Glycoside (Positive inotropic)

C. Cardiac Glycoside (Negative inotropic)

D. PDE inhibitor (negative inotropic)

A

B

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2
Q

What is the MOA of Digoxin?

A. Inhibits membrane-bound Na/K/2Cl channels in the heart

B. Promotes ion movment of Na/K channel in cardiac muscle.

C. Inhibits membrane-bound Na/K ATPase pump to promote contractions

D. Inhibits membrane-bound Na/K ATPase pump in order to decrease contractions.

A

C

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3
Q

Cardiac glycosides consist of the nonsugar moiety known as ______ and a sugar moiety known as ______.

A. Glycone, Aglycone

B. Aglycone, Glycone

A

B

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4
Q

What is the name of the sugars that consist of the glycone portion of digoxin?

A. Glucose-3

B. Cellulose-3

C. Maltose-3

D. Digitoxose-3

A

D

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5
Q

The aglycone portion of digoxin is composed of_____

A. Steroid Nucleus

B. Sugar Nucleus

A

A

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6
Q

What is true about the structure cicled in digoxin? (select all)

A. This is the glycone portion of digoxin

B. Sugar-containing portion of digoxin

C. Aglycone portion of digoxin

D. Adds hydrophilicity to the digoxin

E. Adds lipophilicity to digoxin

A

C, E

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7
Q

In order from left to right what type of bonds are seen in the aglycone portion of digoxin?

A. Cis, Cis, Trans

B, Cis, CIs, Cis

C, Cis, Trans , Cis

D. Trans, Cis, Cis

A

C

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8
Q

Based on the structure of digoxin, which statements are true about this drug? (Select All)

A. Glycone portion of molecule is connected via glycosidic bonds

B. The bond that connects the glycone to the aglycone portion of the molecule is a glycosidic bond

C. Glycone portion of digoxin adds hydrophilicity and Aglycone portion adds Lipophilicity

D. The A:B Cis fusion, B:C Trans fusion and C:D Cis fusion are not necesary for digoxin activity

E. Digoxin contains an unsaturated lactone in the glycone portion of the drug.

F. There are a total of 3 glycosidic bonds in this drug molecule.

A

A, B, C, F

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9
Q

What type of functional group is circled here?

A. Saturated Lactone on 17th carbon

B. Unsaturated Lactone on 17th carbon

C. Saturated Lactam on 17th carbon

D. Unsaturated Lactam on 17th carbon

A

B

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10
Q

Based on the picture below which statement is NOT true regarding digoxin?

A. The AB Cis fusion, BC, Trans fusion and CD Cis fusion are required for the “U” shape conformation.

B. U-shape conformation is necessary for digoxin activity

C. The sugar and non-sugar structures are not needed to attain the “U” shape conformation

D. Glycosidic bonds cannot be replaced with other bonds in order to achieve this conformation.

A

C

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11
Q

Which statements are true regarding the circiled group in digoxin? (Select All)

A. It is known as an a,b-unsaturated lactone ring

B. Saturation of lactone increases biological activity

C. Saturation of lactone decreases biological activity

D. It is knonw as an a,b-unsaturated lactam ring

E. Saturation of the a,b-lactam ring increases biological activity

F. saturation of the a,b-lactam ring decreases biological activity

A

A, C

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12
Q

Hyperkalemia will caused _____ distribution of digoxin to heart and muscle and Hypokalemia will cause _____ digoxin distribution to heart and muscle.

A. Increased, Decreased

B. Decreased, Increased

A

B

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13
Q

In this metabolism of digoxin what is occuring here (Select all)

A. Sugar hydrolysis

B. Reduction of Lactone

C. Saturation of Lactone (addition of hydrogens)

D. Oxidation of Lactone (removal of hydrogens)

A

B, C

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14
Q

In the metabolism of Digoxin what is occuring here?

A. Sugar Hydrolysis

B. Sugar Reduction

C. Aglycone reduction

D. Glycone Reduction

A

A

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15
Q

T/F Molecules with higher numbers of glycosidic bonds have a lower chance of undergoing hydrolysis than molecules with lower numbers of glycosidic bonds

A

F

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16
Q

Which statements are true regarding Digoxin?

A. Excretion is primarily done in the kidneys

B. Good substrate for P-gp efflux pumps

C. Metabolism is limited

D. Should be used with caution in patients with renal dysfunction and has narrow therapeutic window

E. All of the above

A

E

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17
Q

Which drugs are considered P-gp inhibitors?

A. Quinidine

B. Amiodarine

C. Verapamil

D. All of the above

A

D

18
Q

When giving the a P-gp inhibitor with digoxin there will be a ____ in digoxin clearance, ____ in Digoxin serum concentrations and the patient will need a _____ in digoxin dose to prevent toxicity.

A. Increase, Decrese, Increase

B, Decrease, Increase, Decrease

C. Decrease, Decrease, Decrease

D. Increase, Decrease, Decrease

A

B

19
Q

Loop diuretics may cause _____ and lead to the _____ of the toxic effect of digoxin.

A. Hyokalemia, Enhancement

B. Hyperkalemia, Reduction

C. Hyperkalemia, Enhancement

D. Hyperkalemia, Enhancement

A

A

20
Q

Which of the drugs listed is a cardiac glycoside positive inotropic agent?

A. Milrinone

B. Inamrinone

C. Dopamine

D. Dobutamine

E. Digoxin

A

E

21
Q

What enzyme is responsible for cleaving the ATP to cAMP shown in the picture?

A. Esterases

B. Adenylate Cyclase

C. Reductases

A

B

22
Q

The enzyme _____ is responsible for ______ cAMP by converting it into AMP

A. Adenylate cyclase, activating

B. Adenylate cyclase, inactivating

C. PDE, Inactivating

D. PDE, Activating

A

C

23
Q

Based on the picture provided what can you expect to see with the inactivation of the PDE enzyme? (Select All)

A. Increased levels of AMP

B. Decreased levels of cAMP

C. Increased levels of cAMP

D. Decreased levels of AMP

A

C, D

24
Q

The two circled structures of milrinone are ______ and thus the drug is knonwn as a ______ derivative

A. Pyrazine, Dipyrazine

B. Pyridine, Dipyridine

C. Pyrazine, Pyrazine

D. Pyrimidine, Dipyrimidine

A

B

25
Q

In comparison to Inamirone, Milrinone:

A. Has fewer side effects and excreted primarily in urine

B. Is more potent than inamirone

C. Has greater selectivity of PDE3

D. Used for short-term IV management

E. All of the above

A

E

26
Q

When anylizing the structure of Dopamine the red group is knonw as a _____ and can be metabolized by ____

A. Catechol, COMT

B. Catechol, MAO

C. Catechol, Esterases

D. Catechol, Reductases

A

A

27
Q

When analyizing the structure of Dopamine the group circled in blue is a ____ and can undergo metabolism by the enzyme _____

A. Secondary Amine, MAO

B. Primary Amine, MAO

C. Tertiary Amine, MAO

D. Quarternary Amine, MAO

A

B

28
Q

When comparing the structures of Dopamine and Dobutamine we can infer that: (Select All)

A. Dobutamine will undergo MAO metabolism more easily than dopamine

B. Dopamine will undergo MAO metabolism more easily than dobutamine

C. Dobutamine will primarily be metabolized by MAO

D. Dobutamine will primarily be metabolized by COMT

E. Dobutamine is known as an N-Substituted dopamine analog

A

B, D, E

29
Q

In the structure of morphine what is the red portion known as?

A. Tri-benzne derivative

B. Glucuronide derivative

C. Phenanthrene derivative

A

C

30
Q

Morphine can undergo ______ at these positions and form an _____ morphine-6-glucuronide and an _____ morphine-3-glucuronide

A. Glucuronidation, Inactive, Active

B. Glucuronidation, Active, Inactive

A

B

31
Q

Main side effects of morphine include: (select all)

A. Respiratory Depression

B. Respiratory Elevation

C. Hypertension

D. Hypotension

A

A, D

32
Q

Morphine is known as an ______

A. Alpha 1 agonist

B. B1 antagonist

C. µ-opiod agonist

D. µ-opiod antagonist

A

C

33
Q

Based on the reaction seen with sacubitril which statements are true? (Select All)

A. Sacubitril is an active drug

B. Sacubitril is a prodrug

C. Sacubitril has to undergo ester hydrolysis

D. Sacubitrilat is the inactive form of sacubitril

E. Sacubitrilat is the active form of sacubitril

F. Sacubitrilat contains 2 carboxylic functional groups and sacubitril contains only one and an ester

A

B, C, E, F

34
Q

What enzyme is needed to form the active metabolite Sacubitrilat?

A. Esterase

B. Reductase

C. MAO

D. COMT

A

A

35
Q

What is the MOA of Sacubitril?

A. Induces the activity of Neprilysin, reducing the Breakdown of ANP

B. Induces the activity of Neprilysin, Increasing the Breakdown of ANP

C. Inhibits the activity of Neprilysin, Increasing the the breakdown of ANP

D. Inhibits the activity of Neprilysin, Reducing the Breakdown of ANP

A

D

36
Q

What is the blue structure knonwn as in Ivabradine?

A. Benazepin-2-one

B. Pyrolle-benzne

C. Lactam-o-Benzene

D. Soup-er-man

A

A

37
Q

What is the MOA of Ivabradine (Corlanor)?

A. Blocks Type-L Ca+ channels in the SA node

B. Blocks If-type Ca+ channels in the SA node

C. Blocks If-type Na+ channels in the SA node

D. Blocks Type-L Na+ channels in the SA node

A

C

38
Q

Which of the following is true regarding Ivabradine (Corlanor)? (Select All)

A. Major metabolite is an N-desmethylated derivative

B. Primarily metabolized by CYP3A4

C. Itraconazole will decrease Ivabradine plasma concentrations

D. St. John’s wort, rifampicin and barbituates decrease plasma concentrations of Ivabradine

E. Clarithromycin will decrease Ivabradine plasma concentrations

A

A, B, D

39
Q

Which of the following agents are CYP3A inhibitors?

A. St. Johns Wort

B. Rifampicin

C. Itraconazole

D. Clarithromycin

E. Grapefruit juice

F. Nlfinavir

A

C, D, E, F

40
Q

Which of the following drugs are CYP3A4 inducers?

A. St. Johns Wort

B. Itraconazole

C. Clarithromycin

D. Rifampicin

E. Barbituates

F. Grapefruit juice

A

A, D, E

Med Chem Cardio (4 decks)

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