This document discusses diagnostic agents used in medicine. It begins by introducing diagnostic agents and their uses in detecting tissue abnormalities and testing organ function. It then classifies diagnostic agents as radiopharmaceuticals, which are radioactive compounds used in diagnosis and treatment, and radiological contrast media, which make tissues more visible on scans. The document goes on to provide examples and properties of various radiopharmaceuticals and contrast agents, describing their uses, syntheses, and characteristics. It concludes by mentioning some diagnostic chemicals used to test organ functions like the kidney and liver.

1. DIAGNOSTIC
AGENTS
PREARED BY : KASABE AKSHAY
( M. PHARM 1ST YEAR )
DEPARTMENT : PHARMACEUTICAL
CHEMISTRY
( ADVANCED ORGANIC CHEMISTRY)
COLLEGE NAME : PRAVARA RURAL
COLLEGE OF PHARMACY PRAVARANAGAR
, LONI

2. CONTENTS
 Introduction
 Classification
 Radiopharmaceuticals
 Radiological Contrast Media
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3. INTRODUCTION
 Radioactivity is the radioactive decay (radiation) of
some elements like radium, polonium etc.
 Alpha, Beta, gamma and X rays are types of
radiation
 Radiation technology or radiography - important tool
for diagnosis as well as in therapy (mainly for cancer
therapy and radio immuno assay)
 Diagnostic agents are mainly used to detect the
abnormalities in the tissue structure and to check
defective functioning of body organs.
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4. INTRODUCTION
 Diagnostic agents are chemical or substances used
to detect abnormalities in tissue and organs or to
test on organ function.
 Do not have medicinal & pharmacological effects
 X-ray film used for radiography
 Radio opaque
 Some of used in organ visualization
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5. INTRODUCTION
1) Angiography-Blood vessels
2) Arthrography-Joints
3) Bronchography-Lungs
4) Cholangiography-Gall bladder and bile duct
5) Hepatography-Liver
6) Lymphography-Lymph nodes & vessels
7) Myelography-Brain & spinal cord
8) Pyelography-Kidney and ureter
9) Splenohepatography-Liver & spleen
10) Urography-Urinary tract 5
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7. RADIOPHARMACEUTICALS
(RADIO ISOTOPES)
 radioactive compounds
 used for diagnosis & therapeutics treatment of
human diseases
 given by various routes (mouth, injection, eye,
bladder) in small amounts
 dosage can variate depend on type of test
 given under direct supervision of a specialist doctor
 Unit: Curie, becquerrels
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8. RADIOPHARMACEUTICALS
 Ideal Properties:
 Easy availability
 Short effective half life
 Particle emission is adequate
 High target to non-target activity ratio
 No pharmacological effect
 Sterile & pyrogen free
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9. RADIOPHARMACEUTICALS
 Examples of Radiopharmaceuticals
(For Diagnostic purpose)
1. Biliary tract blockage: Tc99m disofenin
2. Blood volume studies: Sod. chromate Cr51
3. Blood vessel disease: Sod. pertechnetate Tc99m
4. Bone diseases: Sod. Fluoride F18
5. Bone marrow disease: Cr51, Tc99m sulfur collloid
6. Brain disease & tumors: Indium Iu111
7. Cancer tumor: Gallium citrate Ga67, Sod. Fluoride
F18
8. Heart disease: Ammonia N13, Rubidium Rb82,
Thallus chloride Tl201 9
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10. RADIOPHARMACEUTICALS
9. Kidney disease: Iodohippurate sod. I125, Tc99m
10. Liver disease: Ammonia N13, Tc99m, Albumin
colloid
11. Lung disease: Krypton Kr81m, Xe133
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11. RADIOLOGICAL CONTRAST MEDIA
(RADIO OPAQUE AGENTS)
 Having property of opacifying X-ray radiations
 Any substance which when administered to a
patient improves the visualization of an organ or
tissue is called a contrast media.
 Either inorganic as well as organic
Classification
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12. RADIOLOGICAL CONTRAST MEDIA
A) Positive contrast media:
 having ability to absorb X-rays (eg. Radioopaques)
Subdivided:
i. Heavy Metals & their salts (Inorganic)
ii. Iodized oils
iii. Iodinated organic compounds (Organic)
a) water soluble contrast media
b) water insoluble contrast media
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13. RADIOLOGICAL CONTRAST MEDIA
B) Negative contrast media:
 Transparent to X-rays
 Renders the structure of a tissue more translucent
 eg. Air, Oxygen, Nitrogen etc.
 Usually not used for diagnostis purpose
 Iodine compounds are usually more useful
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14. RADIOLOGICAL CONTRAST MEDIA
 Characteristics:
 Adequate radioopacity which require iodine content
50% or more
 High water solubility (40% and above)
 Low viscosity, no osmotic effect
 Ability to administered & excretion
 Chemical stability
 Minimum toxicity & patient acceptance
 Readily available & low cost
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15. RADIOLOGICAL CONTRAST MEDIA
A) Heavy metals and salts:
High atomic number and radioopaque
eg.
i) Barium Sulphate (BaSO4)
-Low systematic toxicity
-Low water solubility
-Lack of osmotic activity
-Used for examination of GIT
-Used as suspension or thick cream
-Orally or through rectal route
-sod.citrate is added to stabilize preparation
-Sorbitol added to enhance function 15
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16. RADIOLOGICAL CONTRAST MEDIA
ii) Metallic salt (Tantalum oxide for Bronchography &
esophagography), (calcium tungstate) & (barium
titanate for stomach, small intestine, esophagus)
iii) Ferrites(Fe2O3):
-about 80% opacity than that of BaSO4
-contain Zn, Cu, Mn, Ni and Mg
-used for Bronchi, stomach & small intestine studies
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17. RADIOLOGICAL CONTRAST MEDIA
B) Iodized oils:
 Preparation: Iodination of vegetable oils with
hydroiodic acid give iodized oils
 Iodinated fatty acid derivatives
 Yellow to amber colored oils
 Decompose on exposure to light and air
 Upon administration liberate inorganic iodine in
body which appear in urine
 Used in hepatography, lymphography &
hepatospleenography
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18. RADIOLOGICAL CONTRAST MEDIA
c) Organic Iodine Compound:
 Most widely used
 Tetra iodo phenolphthalein was 1st agent
 Amount of iodine is important for opacity
Subclassification:
a) Water soluble contrast media
b) Water insoluble contrast media
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19. CLASSIFICATION
(BASED ON CHEMICAL FEATURES)
a. Triiodobenzoate-metrizoate
b. Triiodoisophthalamates-Iothalamic acid
c. Triiodophenyl alkanoates-Ipodates
d. Triiodophenoxy alkanoates-Iopronic acid
e. Triiodobenzamide-Metrizamide
f. Triiodo anilides-Iocetamic acid
g. Dimeric triiodobenzoates-Iodipamide
h. Dimeric triiodoisophthalamates-Iosefamic acid
i. Other dimers & polymers-Iozomic acid
j. Diiodophenyl alkanoates-Iodoalphionic acid
k. Diiodopyridones-Propylidone
l. Iodophthaleins-Iodophthalein
m. Miscellaneous-Iodohippurate sodium
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20. RADIOLOGICAL CONTRAST MEDIA
a) Water soluble contrast media:
eg. Diatrizoate sodium
Diatrizoate meglumine
Sodium iothalamate
Metrizoic acid
Iodipamide
Ipodate sodium
Iodohippurate sodium
-mainly used for urography & angiography
-administered by retrograde method (i.e.by
mechanical means)
-mild toxicity
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21. RADIOLOGICAL CONTRAST MEDIA
b) Water insoluble contrast media
eg. Iopanoic acid
Propyliodone
Iophendylate
Iocetamic acid
Iodoxamide
-very slightly water soluble
-mainly used for cholecystography, bronchography and
myelography
-patient should not drink or eat before Six hrs.
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22. RADIOLOGICAL CONTRAST MEDIA
a) Water soluble contrast media:
1. Diatrizoate sodium:
 Sodium salt of substituted triiodo benzoic acid
 Iodine content : abt 62%
 Used for angiography & urography
 Also available as meglumine salt
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23. SYNTHESIS OF DIATRIZOATE SODIUM
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24. RADIOLOGICAL CONTRAST MEDIA
2. Sodium Iothalamate:
 Structural isomer of diatrizoic acid
 One actamide (CH3CONH-) group replaced by
methyl carbamoyl (-CONHCH3)group
 Available as meglumine salt
 Used in angiography
 Chem. Name: sodium 3-acetamido-2,4,6-triiodo-5-
(methylcarbamoyl)benzoate
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25. SYNTHESIS OF SODIUM IOTHALAMATE
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26. RADIOLOGICAL CONTRAST MEDIA
3) Ipodate sodium:
4) Iodipamide:
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27. RADIOLOGICAL CONTRAST MEDIA
5) Iodohippurate sodium:
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28. RADIOLOGICAL CONTRAST MEDIA
b) Water insoluble contrast media
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29. DIAGNOSTIC CHEMICALS
a) For kidney function:
 p-amino hippuric acid, Inulin, Phenosulphophthalein
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30. DIAGNOSTIC CHEMICALS
b) For liver function:
 Rose Bengal, Sulphobromophthalein sodium
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31. DIAGNOSTIC CHEMICALS
c) For gastric function:
 Histamine phosphate, Pentagastrin, Xylose
d) For cardiac function:
 Evans blue dye
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(CH3)3N-CO-CO- Beta -Ala-Trp-Met-Asp-Phe-NH2
Pentagastrin
Short acting, very potent & half life 10 min

32. DIAGNOSTIC CHEMICALS
e) Miscellaneous:
i) Fluorescein sodium
-used for ophthalmological
studies
ii) Congo red
iii) Erythrosin sodium
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33. DIAGNOSTIC DRUGS
a) Phentolamine & Tyramine: pheochromocytoma
b) Dexamethazone: Endocrine gland dysfunction
c) Mannitol: Renal function
d) L-arginine: growth hormone secretion
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