Angiotensin Converting Enzyme (ACE) inhibitors cause blood vessels to relax, thereby reducing blood pressure. Although Captopril is part of the group of antihypertensive drugs widely used as ACE inhibitors, new research is constantly being carried out with the aim of selecting compounds that are more kinetically advantageous than Captopril. Therefore, a BioPharma employee selected some prototypes and performed kinetic tests, finding the result shown in the figure below. Based on the statement and the graphic above, mark the incorrect alternative. A) It is a graph for determining kinetic parameters according to Lineweaver-Burk. In that case, the coefficient a B) Comparing the prototypes with the reference drug, Prototype 1 has a higher Vmax value. C) Comparing the prototypes with the reference drug, Prototype 2 has a lower Vmax value. D) Captopril has a Vmax of approximately 0.730 and Km of approximately 0.669. E) The two prototypes have Km values lower than those of Captopril and, therefore, were not considered advantageous to replace the reference drug. F) The value of the Michaelian constant (Km) can also be estimated through the extrapolation of the line in the graph, up to the negative part of the X axis. The value of the intersection point is considered the – (1/km), being considered to find the value of km. G)Prototype 2 has a lower km value and therefore greater affinity with ACE, and can be considered an advantageous drug to replace Captopril.

Principles Of Pharmacology Med Assist

6th Edition

ISBN:9781337512442

Author:RICE

Publisher:RICE

Chapter2: Decimal Fractions

Section: Chapter Questions

Problem 8RP

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Angiotensin Converting Enzyme (ACE) inhibitors cause blood vessels to relax, thereby reducing blood pressure. Although Captopril is part of the group of antihypertensive drugs widely used as ACE inhibitors, new research is constantly being carried out with the aim of selecting compounds that are more kinetically advantageous than Captopril. Therefore, a BioPharma employee selected some prototypes and performed kinetic tests, finding the result shown in the figure below. Based on the statement and the graphic above, mark the incorrect alternative. A) It is a graph for determining kinetic parameters according to Lineweaver-Burk. In that case, the coefficient a B) Comparing the prototypes with the reference drug, Prototype 1 has a higher Vmax value. C) Comparing the prototypes with the reference drug, Prototype 2 has a lower Vmax value. D) Captopril has a Vmax of approximately 0.730 and Km of approximately 0.669. E) The two prototypes have Km values lower than those of Captopril and, therefore, were not considered advantageous to replace the reference drug. F) The value of the Michaelian constant (Km) can also be estimated through the extrapolation of the line in the graph, up to the negative part of the X axis. The value of the intersection point is considered the – (1/km), being considered to find the value of km. G)Prototype 2 has a lower km value and therefore greater affinity with ACE, and can be considered an advantageous drug to replace Captopril.

9.
Ρrototipo 2
y = 0,9456x + 2,3229
8
Captopril
y-0,9162x + 1,3683
7
1
1. Km
1
Protótipo 1
y = 0,6816x + 0,2673
V
Vmaz" Vmaz (S]
3.
.*****
-1
5
1/[S]

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