Analysis of diuretics

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2. CONTENTS
 Introduction
 Physiology of urine formation
 Classification
• Drugs
• Structure activity relationship
• Mode of action
• Case study of Acetazolamide
 References
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3. INTRODUCTION
Diuretics are the agents which increase the rate & volume of urine
formation. These agents mainly act on nephrons and promotes the excretion of
excess fluid
These are indicated in the treatment of
1) Edema
2) Hypertention
3) Drug Posioning
Diuretics are very effective in the treatment of conditions like
 Chronic heart failure
 Nephrotic syndrome
 Chronic hepatic disease
 Hypertension
 Cirrhosis of liver 3

4. Physiologyof urine formation
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5. Classification
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1.Inhibitors of carbonic anhydrase
2.Benzothiadiazines
3.Sulfamoyl benzoic acid derivatives (high celling
agents)
4.Mercurials
5.Phenoxyacetic acids
6.Osmotic agents
7.Acidifying agents
8.Xanthines
9.Uricosuric diuretics
10.Potassium sparing agents

6. Carbonic Anhydrase Inhibitors
N N Acetazolamide: N-[5-(aminosulfonyl)-1,3,4-
thiadiazol-2-yl]acetamide
H3COCHN S SO2NH2
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N N Benzolamide: 5-(phenylsulfonylamino)-1,3,4-
thiadiazole-2-sulfonamide
H2NO2S S NHSO2Ph

7. SAR of Acetazolamide
N N Acetazolamide: N-[5-(aminosulfonyl)-1,3,4-
thiadiazol-2-yl]acetamide
H3COCHN S SO2NH2
1. SAR study reveals the importance of free amide, nitrogen, because
momo & disubstitution at SO2NH2 abolishes activity.
2. N group of sulphonamide remain unsubstituted for its activity.
3. The free SO2NH2 group is necessary to bind with zinc ion in the
enzyme. This drug enzyme complex is reversible type.
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MODE OF ACTION
 The acteazolamide thus causes loss of Na+, HCO3
- and K+. As a result
of this, there is decrease in extracellular fluid base which causes
metabolic acidosis. This results in loss of diuretic activity, Hence,
acetazolamide is self-limiting diuretic.

9. Physical And Chemical properties:
Molecular weight of this drug is 222.3g/mol
Description: Acetazolamide appears as a white to yellowish white fine crystalline powder . No order or taste.
Molecular formula: C4H6N4O3S2
.
Solubility:
Sparingly soluble in cold water.
Slightly soluble in alcohol.
Readily soluble in 1N sodium carbonate solution .
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Case Study Of Acetazolamide
History of acetazolamide:
Acetazolamide comes into medical use in 1952.
It is on the world health organization list of essential medicines, The most effective and safe
medicines needed in health system
Common brand names of acetazolamide are Diamox Sequels, Acetazolamide Novaplus,Diacarb.

10. UV spectroscopy of Acetazolamide :
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11. • Conclusion:
• The substituent group may not give rise to the absorption of UV radiation
themselves but their presence modifies the absorption of the principle
chromophore.
• The substituent that increase the intensity of absorption, and possible
wavelength are called as auxochrome,typical auxochrome include
methyl,hydroxyl,alkoxy,halogen and amino groups.
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12. IR Spectroscopy
• Infrared spectroscopy is the spectroscopy that deals with the infrared
region of the EMR spectrum that is light with a longer wavelength and
lower frequency than visible light (400-800nm).
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INFRARED RESIONS RANGE
Near IR 0.8-2.5µm
Mid IR 2.5- 15 µm
Far IR 15 to Onwards
Acetazolamide contains carbonyl group which is to be
detected by the ir spectroscopy.
Carbonyl group is consist of
aldehyde,ketone,acid,ester,amide,acid chloride and
anhydrides.
This group absorbs strongly in the range of 1850-1650cm

13. • Amides:
• c=o Stretch occurs at approx 1680-1630cm
• N-H stretching primary amide gives two band near 3350 and 3180cm
• N-H Bending occurs around 1640-1550cm for primary and secondary
amides.
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14. Aldehydes :
• Aldehyde show very strong band for the carbonyl group that appears in the
range of 1740-1725 for simple aliphatic aldehydes.
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15. IR SPECTRA OF ACETAZOLAMIDE
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Conclusion: From the IR study of Acetazolamide it is concluded that
it contains aldehyde and amides as a functional group.
C---O stretch of aldehyde
C---O stretch of amide
N---H stretch of amide

16. REFRENCE
1) Essential of Medical Pharmacology By K.D Tripathi
2)Principle of Medicinal Chemistry By Kadam, Mahadik
,Bothara.
3)International pharmacopoeia 9th Edition
4) Spectroscopy
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17. THANK YOU
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