Download Tutorial - 3: Diuretics

Medicinal Chemistry-III, Tutorial - 3
Medicinal Chemistry – III
Tutorial – 3 (Home Work)
DIURETICS
1. Define and classify diuretics. Give two examples of each class of diuretics.
2. What is the site of action and mechanism of action of carbonic anhydrase inhibitors (CAIs)?
Give two examples.
3. Write the mechanism of action, three (3) clinical indications and three (3) side effects of
Methazolamide.
4. What the site of action and mechanism of action of loop diuretics? Give two examples of
drug as loop diuretics. Write three (3) clinical indications and three (3) side effects of loop
diuretics.
5. What is the advantage of loop diuretics over carbonic anhydrase inhibitors (CAIs)?
6. Write the structure activity relationship (SAR) of 5-Sulfamoyl-2- and -3-aminobenzoic acid
derivatives.
7. What is the advantage of ethacrynic acid over other sulfamoyl containing diuretics?
8. Write the site of action and mechanism of action of thiazide diuretics. Give two examples
of thiazide diuretics. Write clinical indications and side effects of thiazide diuretics.
9. Write the structure activity relationship (SAR) of thiazide diuretics.
10. What is the difference and similarity between thiazide diuretics and thiazide-like diuretics?
Give one example of thiazide-like diuretics.
11. Write the site of action and mechanism of action of potassium-sparing diuretics. Give two
nexamples. Write clinical indications and side effects of potassium-sparing diuretics.
12. What are osmotic diuretics? Give two examples.Write four features of osmotic diuretics.
Medicinal Chemistry-III, Tutorial - 3
A
CH3
B
H2NO2S
N C CH3
H
O
S
H2NO2S
C
N C CH3
O
S
Cl
D
CL
Cl
NH CH2
O
CH2COOH
O
CH2
C
H2NO2S
H3CH2C
COOH
C
O
Cl
N
H2NO2S
S
E
O
F
H
21
19 11
10
3
4
5
8
7
6
S
H2N
NH
O
8
1
7
N
N
6
N
4
5
S
NH2
N3
15
H
2
20
16
9
2
O
17
13
14
1
H2NO2S
O
O
12 18O
H
N
NH
O
G
Cl
NH2
CH3
O
OH
I
J
OH
OH
HO
OH
OH
3
Cl
2
4
OH
1
H2NO2S
5
6
1
HN
2
3
O
13. Compound ______ and _______ are carbonic anhydrase inhibitors (CAIs). Compound ___
is more potent CAI than compound _______.
14. Compound _______ acts as diuretic at site _________ and causes metabolic acidosis as
one of the major side effect.
15. The name of the compound C is ____________________ and acts at site ________ in the
______________________________________ of nephron. The advantage of compound
C as compared to compounds A and B is that it does not cause ______________________.
16. Compound ____________ can be given as a diuretic to those patients who are
hypersensitive to sulphur containing drugs.
17. Compound/s __________ can be given as a diuretic to a patient suffering from
hyperuricemia.
18. Compound/s ______________ is/are not preferred drug of choice for a patient suffering
from hyperuricemia because they can cause ________________________ as side effect.
Medicinal Chemistry-III, Tutorial - 3
19. Compound ____________ is an example of hydrothiazide and its name is _____________.
20. The name of the compound J is ____________________ and it is an example of
_________________________ diuretics and it acts at site _________ in the
__________________________________________ and __________________________
of the nephron. The efficacy, electrolyte excretion pattern, and adverse effects of compound
J is similar to _______________________ diuretics.
21. The metabolites of compound ___________ is equiefficacious diuretics. The name of the
metabolites are ___________________________________________________________.
22. Diuretic drug/s ________________ can also be used for the treatment of anion overdose,
hyperkalemia and hypercalcemia.
23. Compounds ________________ can block Na+ / K+ / 2Cl- cotransporter at site ________
in the _____________________________________________ of the nephron.
24. The diuretics drug/s _____________ can also be used for urinary alkalinization to increase
the excretion of uric acid and also for the treatment of Glaucoma and acute mountain
sickness.
25. Compound ____________ is an example of thiazide and its name is __________________
and it acts at site ____ in the __________________________________________ and
____________________________________________ of the nephron.
26. Compounds __________ are generally given in combination with other diuretics to reduce
their hypokalemic (potassium loss) side effects.
27. The name of the compound G is ____________________ and it shows diuretic effect by
antagonizing _________________ in the _____________________________ of kidney.
28. Compound _____ is metabolized to _____________________ which is an active
aldosterone antagonist.
29. Compound ________ has structural similarity to folic acid and certain dihydrofolate
reductase (DHFR) inhibitors but cannot be used as an anticancer agent.
30. Compound ________ has structural similarity to folic acid and certain DHFR inhibitors but
used as a diuretic agent mainly in combination with other diuretics __________________
to reduce ________________________________________.
31. Compounds _________________________ and _____ show hypokalemic side effect
which can be reduced if they are used in combination of compound ________ or ______.
32. Compound _____ can prevent the reabsorption of up to 28% of the filtered load of water.
33. The name of the compound I is ________________ and it is an _____________ diuretic.