Ace Inhibitors

Front 1

What is the role of renin in The Renin-Angiotensin Pathway?

Back 1

Converts Angiotensinogen into Angiotensin I

Front 2

What is the role of angiotensin converting enzyme (ACE)?

Back 2

Converts A I into active angiotensin I (A II)

Front 3

Properties of enalaprilat

Back 3

-Enalaprilat is 10-fold more potent than captopril
-Excellent IV activity, but very poor oral bioavailability
-Esterification → Enalapril with excellent oral bioavailability

Front 4

Angiotensin II

Back 4

Potent anteriolar vasoconstrictor & stimulates aldosterone relaese from adrenal glands
-Through aldosterone, causes renal Na+ retention
-Facilitates release of norepinephrine

Front 5

A II converting enzyme (ACE) inhibitors & antagonists

Back 5

Drugs Used in Hypertension
-belong to Angiotensin antagonists

Front 6

3 main groups of ACE inhibitors :

Back 6

1.Sulfhydryl-containing inhibitors (e.g., captopril; lone representative)
2.Dicarboxylate-containing inhibitors (e.g., enalapril)
3.Phosphonate-containing inhibitors (e.g., fosinopril, lone representative
-All effectively block conversion of angiotensin I to angiotensin II

Front 7

Is endogenous hypertensive agent

Back 7

A II

Front 8

Which is true of ACE inhibitors :
A)All groups have similar therapeutic & physiological effects
B)The groups differ primarily in potency & PK profiles
C)Constitutes an important class of drugs used in hypertension
D)All

Back 8

D).ALL

Front 9

First orally active ACE inhibitor developed

Back 9

Captopril
-Competitive inhibitor of ACE

Front 10

Two most common side-effects
of the Sulfhydryl-containing
ACE inhibitor - Captopril

Back 10

-Skin rashes
-Taste disturbances (e.g., metallic taste & loss of taste)
- Side-effects subdued on reduction of dose or discontinuation of captopril

Front 11

The only two ACE inhibitors that are not prodrugs

Back 11

Lisinopril & captopril

Front 12

Lisinopril, enalapril & captopril versus all other ACE inhibitors

Back 12

Lisinopril, enalapril & captopril contain pyrrolidine ring of proline.All others contain larger bicyclic or spiro ring systems

Front 13

Fosinoprilat

Back 13

-Phosphonate-Containing ACE Inhibitor
-More potent than captopril but less potent than enalaprilat

Front 14

Fosinopril

Back 14

A pro-drug that contain an (acyloxy)alkyl group allowing for better lipid solubility & improved bioavailability than Fosinoprilat

Front 15

Which of the following can be a Zinc binding group for an ACE inhibitor?
A) sulfhydryl
B)carboxylic acid
C) phosphonic acid
D)All

Back 15

D)All
-Sulfhydryl group shows superior binding to Zn

Front 16

Captopril & fosinopril are ---------- while all other ACE inhibitors are -----------.

Back 16

acidic drugs;
amphoteric

Front 17

common feature in all ACE inhibitors

Back 17

COOH attached to N-ring

Front 18

indicate the position of the amine group in Enalpril and Enalaprilat

Back 18

In its prodrug form(i.e Enalpril)
amine is adjacent to an ester
-Thus, less basic & primarily unionized at physiological pH
On the other hand,amine is adjacent to an ionized carboxylic acid following bioactivation(i.eEnalaprilat )
-that enhances both the basicity & ionization of amine

Front 19

True and False.All ACE inhibitor drugs possess good lipid solubility.

Back 19

False.Except for captopril, enalapril & lisinopril, all other ACE inhibitors drugs possess good lipid solubility.

Front 20

Which drug is marked as the only ACE inhibitor for IV administration?

Back 20

Enalaprilat .Much more hydrophilic