Radiopharmaceuticals

Pharmaceutical Inorganic Chemistry, B.Pharmacy I year I semester Subject

1. Radiopharmaceuticals
Mrs. DipaliKulkarni
Assistant Professor,
YashInstitute of Pharmacy,
Aurangabad.

2. Measurement of radioactivity,
study of radio isotopes –
Sodium iodide 131,
Storage conditions,
precautions &
Pharmaceutical application of radioactive substance .

3. Radiopharmaceuticalsareused in variousbranches
like,
1)Diagnosticapplications(Radioactive tracers)
2)Radiotherapy(RadioisotopesinTherapy)
3)Sterilization(Pharmaceuticalsandsurgicalinstruments)
4)Research.(Biologicalandmedicinalstudiesbyuseof
radioactiveisotopesas tracers)
5)AnalyticalApplications.
Applicationsofradiopharmaceuticalsinpharmacy:

4. 1.Phosphorus32:Usedfordiagnosisofcancer.
2.Chromium51:Usedfordiagnosisofredcellsurvival&
volume.
itisalsoUsedtoestimateGIbloodlossesthroughstoolor
urine.
3.Co57,58usedmeasurementofabsorptionofvit.B
12
DiagnosisofPerniciousanemia.
4.Iodine131:Determination ofThyroid function
.
Diagnosticapplications

5. Radioactivetracers find use inmedicinefordiagnostic
purposes.
1.Labelledcyanocobalaminefindsuseformeasuringthe
glomerularfiltrationrate.
2.Ferriccitrateinjection findsuseforthe diagnosisof
haematologicaldisorders.
3.Colloidalgold injectionisuseddiagnosticallytostudy blood
circulationinliver.
4.Sodiumiodideinjectionfindsuseindiagnosisofproper
functioningofthyroid gland.
5.Sodiumiodohippurateinjectionfindsuseinthestudyof
renalfunction.
6.SodiumroseBengalinjectionfinds useasdiagnosticagent
totestliverfunction.

6. Thetherapeuticallyusedradioisotopeshavebeenfoundto
dependmainlyon their abilitytoionizeatoms.
Theenergymeasurementinvolvedinradiationandresultingin
ionizationmay be expressedinmillionsof electronvoltscalled
MeV.
Thestrengthofalpha, betaandgamma raysin expressed inMeV.
Allradiationsbringabout ionization ofatoms intheirpaths.
Theradiationofshortwavelength(gammarays)ishavinghigh
penetrating powerthanlongwavelength(betarays).
ThegreatertheMeVoftherays,themoredestructiveit
becomestothe surroundingtissues.
RADIOPHARMACEUTICALSCANDESTROYMALFUNCTIONING
CELLS.
Thismethodoftherapyiscalledradiotherapy.Itcanbeusedfor
bothbenign and malignantcancers.
Radiotherapy

7. Someradioisotopearehaveabilityto destroy
the disease without destroying healthy tissues.
a)Iodine 131: Used in the treatment of
hyperthyroidism
b)Usedinthetreatment ofthyroidcancer.
C)Cobalt60:Usedintreatmentofcancerinvolvingcervix,
vagina,uterus,bladder,mouth,tongueandlips.
d)Phosphorus 32: Used in treatment of various typesof
cancerin polycythaemia (erythrocytosis) &Leukemia.
Radiotherapy

8. Examples:
Gold(
198
Au)treatmentofabdominalandpleuraleffusionsassociated with
malignanttumours.Itisgiven intheformof colloidalgoldsuspension.
Gold(
198
Au)treatmentofcarcinoma ofuterusand urinarybladder.
Cobaltlabelledcyanocobalamine(vitaminB12)isusedindiagnosisof
perniciousanaemia.
Sodiumiodide preparationfindsuseintreatmentofthyroiddisorders.
Calcium is usedtostudybonestructureandincarcinoma of bone.
Strontium90is usedindiagnosisofsuperficialcarcinomas.
Radioisotopesmaybeusedinternallyorexternally.
Iftheradioisotopeareusedexternallyorusedasimplantsinsealedcapsuleina
tissue,thedosecouldbeterminatedbyremovalorsources.
Iftheyaregiveninternally,asunsealedsources,thedosecannotbestoppedby
theremovalofthesource.
Thetotaldoseintherapeuticapplicationsmaybecalculatedonthebasisof
effectivehalflifeoftheisotope,concentrationoftheisotopeandthetypeand
energyoftheradiationemitted.

9. UsedforsterilizationofPharmaceuticalsintheirfinal
packedcontainers,thermolabiledrugs
Hormones,Vitamins,Antibiotics,Surgicaldressings,
Disposablesyringes.
Noheatorchemicalgetsinvolved.
Examples:Cobalt 60:Used for the sterilization of
disposablesyringes,catheters and surgicaldressings
and surgical instruments inhospitals.
Sterilization

10. Usedinbiochemical reactions,
may be used for detection of mechanism of
reactions.
Ex: Iodine131,
Sodium 24,
Phosphorus32.
5)Analytical:Playsmajor role whendealing with
dilutesolutions.
Research

12. Calcium(Ca-44andCa-45)radioactivecalciumusedtostudybone structure
and intreatmentof carcinoma of bone.
Strontium-90 Used intheradiotherapyof superficialcarcinomas.
Cyanocobalamine(Co-57)Used inthe diagnosisof perniciousanaemia.
Calcium-47 Itishavinghalflifeof4.7days.Itisusedin
calcium absorptionstudies.
Cyanocobalamine
(Co-60Solution
USP)
Usedtostudyabsorptionanddepositionof
vitaminB12 in normal individuals.
Gold (Au-198)solutionFindsuseinestimationofreticuloendothelial
activity.
Iron(Fe-59) Findsuseinresearchstudiesaboututilization
and absorptionof Iron salts.

13. Labeling,handlingandstorageof
radiopharmaceuticals
Name of Radioisotope.
Ex.I131
Strength in Microcurieor Milicurieper mililitre
at given time and date RADIOACTIVE..Indicates
Warning.
Name And Percentage of any bactericide added.
if not the statement must be there that the
product (INJECTION) does not contain any
bactericide.
Expiry date and name of manufacturer.

14. Radioactive Materials
Must Never Be Touch
With Hand But
Smoking ,Eating & drinking
Activities Should Not Be
Carried Out In The
Laboratory
Protective Clothing Or
Shielding Must Be Used
While Handling The
Radioactive Material
Handled By Means Of
Forceps Or Suitable
Instruments.

15. RadioactiveMaterials
Should Be Kept In
Suitable Labeled
Containers Shielded
By Lead Bricks And
Preferably In
RemoteArea.
Storage

17. Usedasadiagnosticaidforstudyingthe functioningofthe
thyroidgland.
Usedinscanningthethyroidfordeterminingthesize,position
and possibletumour location.
Usedinthetreatmentofseverecardiacdisease(Sodium
iodideI-131),which reducesworkload onheart.
Radioactive iodineinthyroidcarcinoma(cancer):The
isotopeisusedmost frequently afterthe surgicalremoval
ofcancertotreatanyresidual tumour tissues.
Usesof SodiumiodideI-131

18. Iron59is a betaand gamma emittingisotope.
Usedindiagnosistostudytheironmetabolismandtostudy
theredbloodcell formation.
Thepreparationisadministeredorallyforstudyingthe
absorptionofiron fromGIT.
AdministeredI.Vtostudyincorporationofironin
formationofredblood cells.
Usedtostudytheformationanddestructionofspleen,liver
etc.fromoutside thebody.
Iron59

19. Def:Thesearechemicalcompoundswhichhave
abilitytoabsorbXraysandblockthepassage
itthroughtissues.
➢Usedfordescribingthebodystructuresofthe
particularpartintheformofimage.
➢Xraysarecapableofpassingthroughmost
softtissues,butbones,cartilagesandteeth's
arecapableofblockingthepassageofXrays.
Xraysareelectromagneticradiationsand
interactwithelectrostaticfieldofelectronsof
anatom.
Radiopaque(ContrastMedia):

20. Radiopaquesare administered like Barium sulphate
and Iodine for diagnosisofdiseasesinsoft tissues
which shows image of that organ.
They do Not have Pharmacodynamic effect in the
body.

21. Chem. Form.:BaSO
4Mol.Wt.:233.39
Synonyms:Bariisulfas,Barium meal.
Properties:
➢Itisfine,heavy,white,odourless,tasteless,bulky powder,
freefromgrittyparticles.
➢Practicallyinsolublein water&organicsolvents.
➢Very slightly soluble in acids, alkalies & many salt
solutions.
➢Solubleinconc.Sulphuricacidwiththe
formationofbisulphate salt.
BaSO
4+ H
2SO
4 Ba(HSO
4)
2
Barium sulphate

22. ➢UsedasaradiopaqueCONTRASTMEDIAfortheXRay
examinationofvariousorgans.
➢Itisadministeredintheformofsuspension.Itisinsoluble
saltisnotabsorbed.
➢RoentgenographicorFluoroscopic.
➢inthediagnosisofstructuralandmotilityofInteriorpart
ofthealimentarycanal,fromthemouthtothe
duodenum.

23. Precautions:
▪Barium sulphate may be used
cautiouslyinelderly patients.
▪Onceabsorbed inbloodcanproduced
Cardiacarrest.
Storage:Storeinwellclosedcontainers.
Dosageforms:
•Suspension:
•Singledosepowder.
•Single disposable, prefilled cups asenemakit.
Dose:1)60-450gm(Oral). 2)150-750gm(Rectal).