LECTURER DEPT OF PHARMACY PRACTICE, SRM COLLEGE OF PHARMACY INTRODUCTION DEFINITION: Radiopharmaceuticals are the radioactive substances or radioactive drugs used for diagnostic or therapeutic inventions. PRINCILPLE: y Unstable or radioactive isotopes have a property to decompose or decay by emission of nuclear particles and some of them are used in diagnostic or therapeutic interventions. y The three main types of radiation decay are α particles , β particles , γ photons. α particles have the largest mass and charge of the 3 typesof radiation consisting of two protons and two neutrons thus being identical with the He nucleur. β particles are electrons . They are not as destructive as α particles but can be used therapeutically. γ rays are electromagnetic vibrations comparable with light but of much shorter λ .because of their short wavelength and high energy, they are very penetrating. Thus , the clinical utility of a radiopharmaceuticals is determined mainly by a physical properties of radionucleide.(eg. Radiation, energy, half life) For therapeutic use, however radionucleides should emit particulate radiation(i.e.β particles),which deposits the radiation within the target organ. Radioiodine is a prime example and used for the hyperthyroidism and eradication of metastatic disease of thyroid gland.
Since Iodine 131 emits both β and γ radiation, it can be used
diagnostically(γ rays) and therapeutically(β rays).
Fraction of nuclei disintegrating with time is always
constant on progressively fewer atoms are left. DIAGNOSTIC IMAGING Therapeutic isotopes are utilised for their destructive effects on tissue.It is necessary that they have sufficient energy to penetrate throughout the tissue being treated, but radioactivity spreading to surrounding tissue is undesirable, however and difficult to control. ¾ Radiopharmaceuticals are used to diagnose the presence of disease or evaluate the progression of disease following a specific therapy intervention. Radiopharmaceuticals can also be used to evaluate drug induced toxicity and to a lesser extent have been used to treat diseased tissue with radiation.
¾ Imaging procedures are classified either as dynamic
and static. Dynamic study provides useful info through the rate of accumulation and removal of radiopharmaceutical from a specific organ.A static study provides perfusion and morphological status of organs assessing adequacy of blood flow, organ size, shape, position, chances of space occupying lessions etc. USES OF RADIOPHARMACEUTICALS Diagnostic uses y serves as traces y when introduce into the body,emit radiation that is subsequently detected and measured e.g. to analyse thyroid function‐radioactive iodine(orally)the thyroid is then scanned to determine radioiodine concentration and location.Greter than normal update by the thyroid indicates hyperthyroidism. Therapeutic uses y Radioisotopes are used as internal or external radiation sources to treat disorders such as hyperthyroidism and cancer. y Internal radiation source y Radioisotopes administered orally or intravenously or implanted in the target tissue or organ will roduce radiation that destroyes disease results and prevents new tissue growth. y External radiation source y Radiotion used for therapy in cancer patients. Use of radiopharmaceuticals in different organ systems Pulmonary systems used in lung perfusion scans,to detect acute pulmonary embolism and ventillation scans which help differentiate pulmonary embolism from chronic obsructive pulmonary disease examples 1)macro-aggregated albumin 2)Xenon 133 gas Skeletal systems nuclear bone scans are particularly valuable for detecting cancer metastasis. The radionuclei is absorbed onto hydroxy appetite bone matrix via chemisorption. E.g.methylene diphosphamate stanus chloride. Hepatobilliary system Various radiopharmaceuticals used are as follows: y Sulphur cloride y Iodine 131 sobium rose pengal y Disofenin Renal system y glucoheptonic acid y DMSA( 2,3 dimer- capto succinic acid) y DTPA(diethylene triamine pentacetic acid) Cardiovascular system y pyrophosphate y Thallous chloride 201 miscellaneous agents y Sodium iodide 123 y Gallium citrate 67 Criteria for a optimal radiopharmaceutical y Should have a relatively short half life y Should emit γ paricles y The energy should range from 30-300 kilo electron volts. y Metabolic stability-1st order kinetics –to localize the target site differ vein metabolised y Organ specificity y Excretion y Availability y Technitium 99m is currently the most widely accepted radioisotope for imaging studies. Half life of radiopharmaceuticals y Physical half-life refers to the time needed for a radioactive substance to lose 50% of its activity through decay. y Biological half-life refers to the time needed for the body to eliminate 50% of the radioactive substance. y The combined effect of physical and biological half-life determines the effective half-life required for the radioactivity of an administered radioisotope to decrease by 50%.