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radiopharmaceuticals

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on 6 June 2014

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Transcript of radiopharmaceuticals

Introduction
Radiopharmaceuticals
Radiopharmaceuticals

Properties of an Ideal Diagnostic Radiopharmaceutical:
1. Types of Emission:
Pure Gamma Emitter

Types Of Radioactivity
1. Natural Radioactivity
nuclear reactions occurs spontaniously
Types:
A. charged partical reaction
by bombarding target materials with charged particles in particle accelarators such as cyclotrons.
B. photon induced reaction
The source of electromagnetic energy may be gamma-emitting radionuclide or high-voltage x-ray generator.

C. neutron induced reaction
It is the most widely used method
It is the bombardment of a nonradioactive target nucleus with a source of thermal neutrons.
the most widely used radionuclide generator in radiopharmacy is 99Mo-99mTc generator.
Cyclotron
2. Energy of Gamma Rays:

Ideal
: 100-250 keV e.g.
Tc-99m, I-123, In-111
3. Photon Abundance:
Should be high to minimize imaging time

4. Easy Availability:
Readily Available, Easily Produced & Inexpensive
5. Target to Non target Ratio:
It should be high to maximize the efficacy of diagnosis, minimize the radiation dose to the patient

7. Patient Safety:
Should exhibit no toxicity to the patient.

8. Preparation and Quality Control:
Should be simple with little manipulation.
No complicated equipment
No time consuming steps
properties of ideal therapeutic radiopharmaceutical
properties of ideal therapeutic radiopharmaceutical
Properties Of an Ideal Radiopharmaceuticals
1. Must be sterile and pyrogen free
2. Should be isotonic and have psycological pH
3. If radioactive, dose must be calibrated
Catagories of Radionuclides
1. Generator-produced
2. Thermal Neutron Reactor-produced
3. Cyclotron-produced
4. Fission reactor-produced.
Genrator produced Radioisotops:
Ga-68, Kr-81m, Rb-82, Tc-99m, and In-113m
, all of which are generator-produced radionuclides. Of particular note is Tc-99m.
A generator is a self-contained system housing a parent/daughter mixture in equilibrium, which is designed to yield the daughter for some purpose usually separate from the parent.
Thermal Neutron Reactor-produced
Radioisotopes used in Nuclear Medicine are almost all synthetic. For thermal neutron reactor-produced radioisotopes, reactor is source of thermal neutrons. An (n,gamma) reaction occurs.
Net effect:
increase of A number by 1 and no change in Z number. Same element is therefore present.
Example:
98Mo (n,gamma) 99Mo
Cyclotron Produced Radioisotopes:
A cyclotron is a source of high-energy protons, deuterons, and other particles. Various reactions takes place, e.g., (d,n), (p,pn), (p,5n), (p,a). Net effect: change in A number and/or Z number. A different element is usually formed.
Example:
14N (d,n)
15
O
Fission Reactor-Produced:
The final group of interest includes
Xe-133, Mo-99
, and
I-131
, all of which are byproducts of the fission of
U-235
.
Clinical Utility:
Radiopharmaceuticals have been used clinically for a wide variety of studies which generally fall into three categories
1. Static Studies
2.Dynamic Studies
3. In Vivo non imaging studies
Static Studies:
Study Type
Tracer
Region
Pathology
BONE SCAN
Tc Medronic acid, Tc-HDP
Whole Body
Bone Tumors, Fractures, Paget's Disease
LIVER SPLEEN SCAN
Tc-SC, Tc-MIAA
Abdomen
Tumors, Cysts, Hepatocellular Disease
BRAIN SCAN
Tc-HMPAO
Brain
Tumors, Trauma, Dementia
TUMOR SCAN
Ga-67 Citrate
Whole Body
Malignant Tumors, Metastatic Disease

Dynamic Studies:
STUDY TYPE
TRACER
REGION
Pathology
CARDIOANGIOGRAPHY
Tc-RBC, Tc-HSA
Chest
Aneurysms, Congenital Heart Defects, Myocardia Dyskinesia, Cardiomegaly
CEREBRAL BLOOD FLOW

TcO4

Head,Neck

Cerebral Death, AVM
CHOLECYSTOGRAPHY

Tc-DISIDA

Abdomen
Obstructive Disease
CISTERNOGRAM

In-111 DTPA

Head, Neck
Blockage, Slowed CSF Flow
GASTRIC EMPTYING

Tc-Ovalbumin, Tc-SC

Abdomen
Abnormal GE Rates
PULMONARY VENTILATION

Xe-133 gas

Upper Back

Obstructed Airways
VENOGRAM

Tc-MAA
Legs

Thrombosis
VOIDING CYSTOGRAM

Tc-SC

Abdomen

Urine Reflux, Incomplete Bladder Emptying
STUDY TYPE
3. In vivo non-imaging studies
TRACER
REGION

PATHOLOGY
CO2 BREATH TEST
C-14 CO2S
Breath
Glucose Intolerance
IRON TURNOVER
Fe-59

Whole Body

Abnormal Ferrokinetics

OCULAR P-32 UPTAKE
P-32 Na3PO4

Eyes
Ocular Melanoma
PLATELET SURVIVAL

In-111 Platelets

Blood
Abnormal Platelet Loss

RADIOACTIVE IODINE

I-NaI

Thyroid

Abnormal Uptake, Hyperthyroidism
Mechanism of Localization
Mechanism of localization depends on:
1. active transport
2. phagocytosis
3. capillary blockade
4. Cell Sequestration
5. Simple/exchange diffusion
6. Compartmental Localization
7. Chemisorption
8. Antigen/antibody reaction
9. Receptor-binding
Radionuclides used in Nuclear Medicine are all synthetic and fall into 4 general categories:
Radiopharmaceuticals are used in the field of nuclear medicine as tracers in the diagnosis and treatment of many diseases.
Radiopharmaceuticals are agents used to diagnose certain medical problems or treat certain diseases. They may be given to the patient in several different ways. For example, they may be given by mouth, given by injection, or placed into the eye or into the bladder.
2. Artificial Radioactivity
The property of radioactivity produced by particle bombardment or electromagnetic irradiation.
2.Artificial Radioactivity
6. Effective Half life:
short enough to minimize the radiation dose to patients and long enough to perform the procedure.



8. Inexpensive, readily available radiopharmaceutical.

9. Simple preparation and quality control if manufactured in house.
1. Types of emmission:
It must be pure beta emittor
2. Energy of Beta Rays:
3. Effective Half Life:
4. Target to Non Target Ratio:
having high target to non target ratio
5. Radiation Dose:
Minimal radiation dose to patient and Nuclear Medicine personnel
the therapeutic radiopharmaceutical should exhibit no toxicity to the patient.
6. Patient Safety
beta emitters with Emax >1 meV are preferred
the effective half-life should ideally be measured in hours or days as opposed to longer time units.
Thermal Neutron Reactor-produced
Biliary tract blockage
Technetium Tc 99m Disofenin, Technetium Tc 99m Lidofenin, Technetium Tc 99m Mebrofenin
Blood vessel diseases of the brain:
Ammonia N 13, Iofetamine I 123, Technetium Tc 99m Bicisate, Technetium Tc 99m Exametazime, Xenon Xe 133
Bone scan demonstrating typical features of Paget's disease
Bone Diseases (Paget's disease):
Sodium Fluoride F 18, Technetium Tc 99m Medronate, Technetium Tc 99m Oxidronate, Technetium Tc 99m Pyrophosphate, Technetium Tc 99m (Pyro- and trimeta-) Phosphates
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