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Used either to demonstrate Abnormalities in structure or Impairment of functions of body organs. The most widely used methods for non-invasive imaging are: (without exploratory surgery)
1. Scintigraphy (Nuclear medicine scanning) 2. Radiography (X-ray and Computed Topography (CT) 3. Ultrasonography (US) 4. Magnetic Resonance imaging (MRI)
Diagnostic agents are important adjuncts to the 1st three of these procedures.
Dr. Doaa Issa
Minimum osmotic effect 5. It should have maximum opacity to X-ray 2.Faculty of Pharmacy & Drug Manufacturing Pharos University Terminology Radiographic Procedure 1 2 3 4 5 6 7 8 9 10 Angiography Cholecystography Cholangiography Hepatography Urography Bronchography Lymphography Esophago graphy Histero salpin gography Myelography Tissue (Organ) Visualized Blood vessels Gall bladder Gall bladder and Bile ducts Liver Urinary tract Lungs Lymph nodes and vessels Esophagus Uterus and fallopian tubes Spinal cord & subarachiniod spaces Characteristics of an Ideal Diagnostic Agent: 1. Highly water soluble (for Urographic and Angiographic agents which are used as sodium or meglumine salts for I. Low viscosity 7. Chemically stable 3. Doaa Issa 2 .V. Selective tissue uptake Dr. Low toxicity 6. administration) 4.
Bronchographic Agents Dr. Agents used as X-ray contrast media Agents used to test for organ functions III. Agents used to determine blood volume IV.Myelographic Agents II. Doaa Issa 3 .V. Agents Used For Angiography and I. Agents Used to Outline Various Cavities I. Urography 4. II. Agents used for miscellaneous diagnostic tests Classification of XAgents used as X-ray contrast media 1. Agents Used To Outline the Gall Bladder and Bile Ducts 2. Agents Used To Outline the GIT 3.Faculty of Pharmacy & Drug Manufacturing Pharos University Classification of Diagnostic Agents I.
The Oral Contrast Agents Once in circulation.4. lopanoic Acid (Telepaque) Superior opacification with low toxicity It should be taken 14 hrs before X-ray examination After a fat free meal I I COOH H3C 2-(3-Amino-2. Agents Used To Outline the Gall Bladder and Bile Ducts A.and lipophilicity to allow intestinal absorption and hepatic excretion. converted into water soluble glucuronide conjugate Excreted in the bile and stored in the gall bladder I H2N 1.6-triiodobenzyl)butyric acid C2H5 H CHO + ( H5C2-CH2-CO)2 -O NO2 m-Nitrobenzaldehyde Rreduction Raney Ni Perkin's Cond. Doaa Issa 4 .4. They have enough hydro. Cholecystographic Agents All cholecystographic agents are analogs of 2.Faculty of Pharmacy & Drug Manufacturing Pharos University I. NaOC2H5/ Xylene -H2O NO2 COOH α-Ethyl-m-nitrocinnamic acid C2H5 COOH Iopanoic acid ICl/ Acetic acid NH2 Dr. Drugs Used As X-Ray Contrast Media 1.6-triiodophenylalkanoic acids. they bind to serum albumin In the liver.
the gallbladder has contracted. Doaa Issa 5 . After a fatty meal.4.Faculty of Pharmacy & Drug Manufacturing Pharos University 2.6-triiodophenyl)amino]2-methyl-propionic acid. the fundus and the neck of the gallbladder and cystic duct is filled with contrast medium and the common bile duct (arrows) N. Locetamic Acid (Cholebrine) I H2N I H3C O N I CH3 COOH Normal cholecystogram the contrast medium is seen evenly filling the gallbladder 3-[Acetyl(3-amino-2.B: Agents that lack substituents at the 5-position of the benzene ring generally bind strongly to serum albumin and are cleared through the liver whereas agents containing a substituent in the 5-position lack such binding and are generally excreted by the kidneys Dr.
Cholagiographic Agents o They are moderately strong dibasic tri-iodobenzoic acid dimers linked by a polymethylene chain of variable length.Faculty of Pharmacy & Drug Manufacturing Pharos University B.3’-(Adipoyldiimino)-bis-(2. o They are usually administered as meglumine salts to reduce adverse reactions. lodipamide Meglumine (Cholografin Meg) I COOH I O N H (CH2 )4 I O N H HO I OH OH 2 COOH I OH OH NH-CH3 I 3.6-triiodobenzoic acid) meglumine salt (Meglumine is N-methylglucamine) image showing the biliary tree and the main pancreatic duct Dr. Doaa Issa 6 .4. o They are water soluble and completely ionized at the physiological pH.
The drug will appear in the bile after 15 min. A barium enema clearly displays a colonic herniation herniation Dr. Examination of the colon (given rectally as enema) The particle size of BaSO4 should be very fine otherwise any lumps will give false diagnosis of Non existing abnormalities.5 hours. Doaa Issa 7 . and the biliary ducts will appear within 25 min.V. 2. Agents Used To Outline the GIT Barium Sulfate (BaSO4) (Barium Meal) It is administered orally in the form of suspension It is used for: Detecting abnormalities of the esophagus and the stomach. The drug is highly bound to plasma proteins so it may produce hepato-toxicity and jaundice like symptoms.Faculty of Pharmacy & Drug Manufacturing Pharos University It is administered I. Maximum filling and opacification will take place within 2-2. as either the sodium or the meglumine salts when the oral drugs give unsatisfactory results.
Doaa Issa 8 . Agents Used For Angiography and I. USP) lothalamic meglumine injection (BP. Urography The use of radiographic agents for visualization of urinary tract and blood vessels is based on: The rapid renal excretion of water soluble iodinated benzoic acid salts (NO protein binding due to substitution at position 5) i. USP) I O H3C N H COOH I H N I O CH3 5-Acetamido-2.Faculty of Pharmacy & Drug Manufacturing Pharos University 3.6-triiodo-N-methyl-isophthalamic acid These are used in: Intravascular angiography Aortography Selective renal arteriography Urography Aortography Cerebral Angiography Dr. Iothalamic Acid Water soluble salts: lothalamic sodium injection (BP.4.V.
6-triiodobenzoicacid .It is used for angiocardiography.Faculty of Pharmacy & Drug Manufacturing Pharos University ii. aortography and urography .5-Diacetamido-2. Diatrizoic Acid Gastrografin O H3C COOH I I O N H N H CH3 I 3.4. Doaa Issa 9 .Gastrografin is a mixture of diatrizoate meglumine (66%) and diatrizoate sodium (10%) solution. may be used as an alternative to barium sulfate for radiographic examination of the GIT ( in allergic patient Barium might leak into the abdominal cavity) (oral or rectal administration) Synthesis of Diatrizoic acid COOH COOH COOH COOH Nitration O 2N SnCl2 NO 2 H N 2 1) ICl / Acetic acid I I NH-CO-CH3 I 2) Acetylation H 3 C-CO-HN NH2 Dr.
4. HO OH N I COCH3 5-[N-(2.Myelographic Agents They are both water and oil soluble contrast agents.N'-bis(2.6-triiodobenzene-1. Doaa Issa 10 .3-Dihydroxypropylacetamido)]N.3-dicarboxamide Dr. Water soluble agent: i.Faculty of Pharmacy & Drug Manufacturing Pharos University Iothalamic Acid COOH I O H3C N H I H N I O Diatrizoic Acid COOH I O I O N H I N H CH3 CH3 H3C lopanoic Acid I H2N Locetamic Acid I H2N I H3C O N I CH3 COOH I H3C O N I CH3 COOH 4. Agents Used to Outline Various Cavities I. used to opacify the spinal cord and subarachinoid spaces. lohexol (Omnipaque) I O H N I H N O OH OH OH OH It provides improved image details with low risk of toxicity.3-dihydroxypropyl)-2.
Faculty of Pharmacy & Drug Manufacturing Pharos University Oily agents are: : ii. II. the preparation coats the bronchial tree and the alveolar spaces and are excreted from lungs by coughing or absorption. Doaa Issa 11 . sometimes general anesthesia is required for administration and therefore their use is now limited. Irritation is the major drawback.Bronchographic Agents After intra-tracheal administration. Lipoidol (Ethiodized Oil) (Ethiodol) (Iodized Oil Injection) It is an Iodine addition product of vegetable oils: ethyl ester of fatty acids of poppy seed oil. It contains 35-42% of organically combined Iodine.5-diiodo-4-oxo-1. Propyliodone (Dinosil) Propyl 2-(3.4dihydropyridin-1-yl)acetate Dr.
Doaa Issa 12 . urine samples are collected and analyzed for the drug content. Glomerular Filtration Rate can be measured by the renal plasma clearance of mannitol and creatinine. Agents used to test for organ functions 1. i. Aminohippurate Injection (USP) H N COOH N-(4-Aminobenzoyl)glycine sodium saltH2 N It is used as sodium salt in the form of injection with pH range of 7.0 -7. Agents Used to Test for Renal Functions The rate of excretion of some drugs in the urine has been proposed to be a Measure Of The Functional Capacity of the kidneys.2 for the Determination Of Tubular Functional Capacity (TFC) Synthesis of Aminohippuric acid CO -Cl H2 NCH2COOH Pyridine NO 2 NO 2 CONHCH2COOH Reduction Zn/HCl NH2 CONHCH2COOH O Dr. After administration of the drug.Faculty of Pharmacy & Drug Manufacturing Pharos University II. For example.
Faculty of Pharmacy & Drug Manufacturing Pharos University ii. Inulin It is present in the form of 10% inulin and 0. lodohippurate Sodium N-(2-lodobenzoyl)glycine sodium salt CONHCH2COONa I132 Performance of kidneys can be determined by injecting a radioactive compound which can be quickly and exclusively excreted by kidneys Renal malfunction can be indicated when the measured activities in the two kidneys are unequal iii. HO OH OH OH OH OH It is used to as diagnostic agent for kidney function and also as osmotic diuretic. Doaa Issa 13 . excreted unchanged and not reabsorbed by the tubules. iv. Dr. Mannitol (BP and USP) It is obtained commercially by the catalytic reduction of glucose.8% NaCI injection It is used to evaluate the glomerular filtration rate (GFR) because it is filtered by the glomeruli.
Dr.3%) Injection * Mannitol is treated with a known excess of KIO4 in the presence of H2SO4 where it will be oxidized into HCHO and HCOOH. blood sample …. C6H14O6+ KIO4 + H2SO4 HCHO + HCOOH + HIO3 + 8 H2O * unconsumed KIO4 and HIO3 / Kl equivalent amount of I2 titrated with Na2S2O3 * NaCl is determined by applying Volhard's method. The dye content in the alkalinized serum is measured. Agents Used to Test for Liver Functions They are drugs that are administered I. 30 min after.V..3’-disulfonate Br Br O O SO3 Na Br Br OH It is the best agent used to test for liver function.Faculty of Pharmacy & Drug Manufacturing Pharos University Assay of Mannitol (5 or 10%) and NaCl (0. Doaa Issa 14 . Normal liver can remove most of the amount of the injected dye within 30 min. The rate of clearance of these substances from the plasma is the measure of the excretory capacity of the liver. SO3 Na HO It is administered IV…. These drugs are excreted mainly through the liver. 2. to test for liver function. Sulfobromophthalein Sodium Disodium salt of phenol tetrabromophthalein3. i.
Doaa Issa 15 . 3. USP method: Spectrophotometrically.C.Faculty of Pharmacy & Drug Manufacturing Pharos University Synthesis of Sulfobromophthalein Sodium O O + Br Br Br Br Br O O O Fusion Br Br O O SO3 Na O Br Br OH SO3 Na Drug 1.M or S. for chemical testing of low gastric secretion as it increases HCl secretion. Agents Used to Test for Gastric Functions In some cases it may be indicated to test whether the stomach can efficiently secrete HCl or not. alkalinized with Na2CO3 then the formed color is measured at 580 nm. Sulphonation 2. Hypoacidity Hyperacidity Pernicious Anemia Cancer Gastric ulcer Deudenal ulcer Betazole Hydrochloride (Histalog) 3-(2-Aminoethyl)-1H-pyrazole NH2 2 Isosteric with histamine The drug is administered either I. NH2 N N H N N H HCl Betazole Histamine Dr. The sample is dissolved in H2O. Na Br Br Br O O OH OH salt formation HO Assay of Sulfobromophthalein OH Oxygen flask method for either Br or S contents.
Faculty of Pharmacy & Drug Manufacturing Pharos University ORGAN IMAGING 2.6-TRIIODO PH.4.ALKANOIC CHOLECYSTO GRAPHY CHOLANGIO GRAPHY ANGIO/URO GRAPHY MYELO GRAPHY BRONCHO GRAPHY DIMER 3.Br. Doaa Issa 16 .PHTHALEINE STOMACH BETAZOLE IODOHIPPURATE OSMOTICDIAGNOSTIC TUBULAR CAPACITY INULIN MANNITOL MALFUNCT ION GLOMERULAR FILTERATION Dr.5-SUBS BENZOIC IOTHALAMIC ACID PROPYL IODONE LOCETAMIC ACID IODIPAMIDE IOHEXOL IOPANOIC ACID DIATRIZOIC ACID LIPOIDOL ORGAN FUNCTIONING RENAL AMINOHIPPURATE LIVER SULFO.