Diagnostic Agents

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DIAGNOSTIC AGENTS Prepared by: Sanjay Patel, Assist. Professor, Atmiya Institute of Pharmacy, Rajkot Gujarat (India): 

DIAGNOSTIC AGENTS Prepared by: Sanjay Patel, Assist. Professor, Atmiya Institute of Pharmacy, Rajkot Gujarat (India)

CONTENTS: 

CONTENTS Introduction Classification Radiopharmaceuticals Radiological Contrast Media 2 Atmiya Institute of Pharmacy, Rajkot

Introduction: 

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. 3 Atmiya Institute of Pharmacy, Rajkot

Introduction: 

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 4 Atmiya Institute of Pharmacy, Rajkot

Introduction: 

Introduction Angiography-Blood vessels Arthrography-Joints Bronchography-Lungs Cholangiography-Gall bladder and bile duct Hepatography-Liver Lymphography-Lymph nodes & vessels Myelography-Brain & spinal cord Pyelography-Kidney and ureter Splenohepatography-Liver & spleen Urography-Urinary tract 5 Atmiya Institute of Pharmacy, Rajkot

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6 Atmiya Institute of Pharmacy, Rajkot

Radiopharmaceuticals (Radio isotopes): 

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 7 Atmiya Institute of Pharmacy, Rajkot

Radiopharmaceuticals: 

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 8 Atmiya Institute of Pharmacy, Rajkot

Radiopharmaceuticals: 

Radiopharmaceuticals Examples of Radiopharmaceuticals (For Diagnostic purpose) Biliary tract blockage: Tc 99 m disofenin Blood volume studies: Sod. chromate Cr 51 Blood vessel disease: Sod. pertechnetate Tc 99 m Bone diseases: Sod. Fluoride F 18 Bone marrow disease: Cr 51 , Tc 99 m sulfur collloid Brain disease & tumors: Indium Iu 111 Cancer tumor: Gallium citrate Ga 67 , Sod. Fluoride F 18 Heart disease: Ammonia N 13 , Rubidium Rb 82 , Thallus chloride Tl 201 9 Atmiya Institute of Pharmacy, Rajkot

Radiopharmaceuticals: 

Radiopharmaceuticals Kidney disease: Iodohippurate sod. I 125 , Tc 99 m Liver disease: Ammonia N 13 , Tc 99 m, Albumin colloid Lung disease: Krypton Kr 81 m, Xe 133 10 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media (Radio opaque agents): 

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 11 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media Positive contrast media: having ability to absorb X-rays ( eg . Radioopaques ) Subdivided: Heavy Metals & their salts (Inorganic) Iodized oils Iodinated organic compounds (Organic) a) water soluble contrast media b) water insoluble contrast media 12 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

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 13 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

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 14 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

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 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media ii) Metallic salt (Tantalum oxide for Bronchography & esophagography), (calcium tungstate) & (barium titanate for stomach, small intestine, esophagus) iii) Ferrites(Fe 2 O 3 ) : -about 80% opacity than that of BaSO 4 -contain Zn, Cu, Mn, Ni and Mg -used for Bronchi, stomach & small intestine studies 16 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

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 17 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media c) Organic Iodine Compound: Most widely used Tetra iodo phenolphthalein was 1 st agent Amount of iodine is important for opacity Subclassification : Water soluble contrast media Water insoluble contrast media 18 Atmiya Institute of Pharmacy, Rajkot

Classification (Based on chemical features): 

Classification (Based on chemical features) Triiodobenzoate-metrizoate Triiodoisophthalamates-Iothalamic acid Triiodophenyl alkanoates-Ipodates Triiodophenoxy alkanoates-Iopronic acid Triiodobenzamide-Metrizamide Triiodo anilides-Iocetamic acid Dimeric triiodobenzoates-Iodipamide Dimeric triiodoisophthalamates-Iosefamic acid Other dimers & polymers-Iozomic acid Diiodophenyl alkanoates-Iodoalphionic acid Diiodopyridones-Propylidone Iodophthaleins-Iodophthalein Miscellaneous-Iodohippurate sodium 19 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

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 20 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

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. 21 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media Water soluble contrast media: Diatrizoate sodium: Sodium salt of substituted triiodo benzoic acid Iodine content : abt 62% Used for angiography & urography Also available as meglumine salt 22 Atmiya Institute of Pharmacy, Rajkot

Synthesis of Diatrizoate sodium: 

Synthesis of Diatrizoate sodium 23 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media Sodium Iothalamate: Structural isomer of diatrizoic acid One actamide (CH 3 CONH-) group replaced by methyl carbamoyl (-CONHCH 3 )group Available as meglumine salt Used in angiography Chem. Name: sodium 3-acetamido-2,4,6-triiodo-5-(methylcarbamoyl)benzoate 24 Atmiya Institute of Pharmacy, Rajkot

Synthesis of sodium iothalamate: 

Synthesis of sodium iothalamate 25 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media Ipodate sodium: Iodipamide : 26 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media 5) Iodohippurate sodium: 27 Atmiya Institute of Pharmacy, Rajkot

Radiological Contrast Media: 

Radiological Contrast Media b) Water insoluble contrast media 28 Atmiya Institute of Pharmacy, Rajkot

Diagnostic Chemicals: 

Diagnostic Chemicals a) For kidney function: p-amino hippuric acid, Inulin, Phenosulphophthalein 29 Atmiya Institute of Pharmacy, Rajkot

Diagnostic Chemicals: 

Diagnostic Chemicals b) For liver function: Rose Bengal, Sulphobromophthalein sodium 30 Atmiya Institute of Pharmacy, Rajkot

Diagnostic Chemicals: 

Diagnostic Chemicals c) For gastric function: Histamine phosphate, Pentagastrin , Xylose d) For cardiac function: Evans blue dye 31 Atmiya Institute of Pharmacy, Rajkot (CH 3 ) 3 N-CO-CO- Beta -Ala-Trp-Met-Asp-Phe-NH 2 Pentagastrin Short acting, very potent & half life 10 min

Diagnostic Chemicals: 

Diagnostic Chemicals e) Miscellaneous: Fluorescein sodium -used for ophthalmological studies ii) Congo red iii) Erythrosin sodium 32 Atmiya Institute of Pharmacy, Rajkot

Diagnostic drugs: 

Diagnostic drugs Phentolamine & Tyramine: pheochromocytoma Dexamethazone: Endocrine gland dysfunction Mannitol: Renal function L-arginine: growth hormone secretion 33 Atmiya Institute of Pharmacy, Rajkot

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Thank you 34 Atmiya Institute of Pharmacy, Rajkot

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Atmiya Institute of Pharmacy, Rajkot 35