Radiopharmaceutical


Radiopharmaceuticals, or medicinal radiocompounds, are a group of pharmaceutical drugs containing radioactive isotopes. Radiopharmaceuticals can be used as diagnostic and therapeutic agents. Radiopharmaceuticals emit radiation themselves, which is different from contrast media which absorb or alter external electromagnetism or ultrasound. Radiopharmacology is the branch of pharmacology that specializes in these agents.
The main group of these compounds are the radiotracers used to diagnose dysfunction in body tissues. While not all medical isotopes are radioactive, radiopharmaceuticals are the oldest and remain the most common of such drugs.

Drug nomenclature

As with other pharmaceutical drugs, there is standardization of the drug nomenclature for radiopharmaceuticals, although various standards coexist. The International Nonproprietary Names, United States Pharmacopeia names, and IUPAC names for these agents are usually similar other than trivial style differences. The details are explained at Radiopharmacology § Drug nomenclature for radiopharmaceuticals.

Specific radiopharmaceuticals

A list of nuclear medicine radiopharmaceuticals follows. Some radioisotopes are used in ionic or inert form without attachment to a pharmaceutical; these are also included. There is a section for each radioisotope with a table of radiopharmaceuticals using that radioisotope. The sections are ordered by atomic number of the radioisotope. Sections for the same element are then ordered by atomic mass number.

Hydrogen-3

3H or tritium is a beta emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
H3-waterTotal body waterOral or IVIn-vitroNon-imaging

Carbon-11

11C is a positron emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
C11-L-methyl-methionineBrain tumour imaging

Parathyroid imaging
IVIn-vivoImaging

Carbon-14

14C is a beta emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
C14-Glycocholic acidBreath test for small intestine bacterial overgrowthOralIn-vitroNon-imaging
C14-PABA Pancreatic studiesOralIn-vitroNon-imaging
C14-UreaBreath test to detect Helicobacter pyloriOralIn-vitroNon-imaging
C14-d-xyloseBreath test for small intestine bacterial overgrowthOralIn-vitroNon-imaging

Nitrogen-13

13N is a positron emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
N13-AmmoniaMyocardial blood flow imagingIVIn-vivoImaging

Oxygen-15

15O is a positron emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
O15-WaterCerebral blood flow imaging

Myocardial blood flow imaging
IV bolusIn-vivoImaging

Fluorine-18

18F is a positron emitter with a half-life of 109 minutes. It is produced in medical cyclotrons, usually from oxygen-18, and then chemically attached to a pharmaceutical formulation.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
F18-FDG Tumor imaging

Myocardial imaging
IVIn-vivoImaging
F18-Sodium FluorideBone imagingIVIn-vivoImaging
F18-FluorocholineProstate tumor imagingIVIn-vivoImaging
F18-DesmethoxyfallyprideDopamine receptor imagingIVIn-vivoImaging

Sodium-22

22Na is a positron and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Na22-Na+Electrolyte studiesOral or IVIn-vitroNon-imaging

Sodium-24

24Na is a beta and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Na24-Na+Electrolyte studiesOral or IVIn-vitroNon-imaging

Phosphorus-32

32P is a beta emitter.
NameTreatment ofRoute of administration
P32-PhosphatePolycythemia and related disordersIV or Oral

Calcium-47

47Ca is a beta and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Ca-47-Ca2+Bone metabolismIVIn-vitroNon-imaging

Chromium-51

51Cr is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Cr51-heart scan/blood volume[Red cell volume heart scan; sites of sequestration; gastrointestinal blood lossIVIn-vitroNon-imaging
Cr51-Cr3+Gastrointestinal protein lossIVIn-vitroNon-imaging
Cr51-EDTA Glomerular filtration rate measurementIVIn-vitroNon-imaging

Iron-59

59Fe is a beta and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Fe59-Fe2+ or Fe3+Iron metabolismIVIn-vitroNon-imaging

Cobalt-57

57Co is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Co57-Cyanocobalamin Gastrointestinal absorptionOralIn-vitroNon-imaging

Cobalt-58

58Co is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Co58-Cyanocobalamin Gastrointestinal absorptionOralIn-vitroNon-imaging

Gallium-67

67Ga is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Ga67-Ga3+Tumor imagingIVIn-vivoImaging
Ga67-Ga3+Infection/inflammation imagingIVIn-vivoImaging

Gallium-68

68Ga is a positron emitter, with a 68-minute half-life, produced by elution from germanium-68 in a gallium-68 generator or by proton irradiation of zinc-68.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Ga68-Dotatoc or DotatateNeuroendocrine tumor imagingIVIn-vivoImaging
Ga68-PSMAProstate cancer imagingIVIn-vivoImaging

Selenium-75

75Se is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Se75-SelenorcholesterolAdrenal gland imagingIVIn-vivoImaging
Se75-SeHCAT Bile salt absorptionOralIn-vivoImaging

Krypton-81m

81Krm is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging the radioactive substance
Kr81m-GasLung ventilation imagingInhalationIn-vivoImaging
Kr-81m-Aqueous solutionLung perfusion imagingIVIn-vivoImaging

Rubidium-82

82Rb is a positron and gamma emitter.
NameInvestigation ofRoute of administration
Rb-82 chlorideMyocardial ImagingIV

Strontium-89

89Sr is a beta emitter.
NameTreatment ofRoute of administration
Sr89-ChlorideBone metastasesIV

Yttrium-90

90Y is a beta emitter.
NameTreatment ofRoute of administration
Y90-SilicateArthritic conditionsIntra-articular
Y90-SilicateMalignant diseaseIntracavitary

Technetium-99m

Technetium-99m is a gamma emitter. It is obtained on-site at the imaging center as the soluble pertechnetate which is eluted from a technetium-99m generator, and then either used directly as this soluble salt, or else used to synthesize a number of technetium-99m-based radiopharmaceuticals.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Tc99m-pertechnetateThyroid uptake and thyroid imaging

Stomach and salivary gland imaging

Meckel's diverticulum imaging

Brain imaging

Micturating cystogram

First pass blood flow imaging

First pass peripheral vascular imaging
IVIn-vivoImaging
Tc99m-pertechnetateLacrimal imagingEye dropsIn-vivoImaging
Tc99m-Human albuminCardiac blood pool imagingIVIn-vivoImaging
Tc99m-Human albuminPeripheral vascular imagingIVIn-vivoImaging
Tc99m-Human albumin macroaggregates or microspheresLung perfusion imagingIVIn-vivoImaging
Tc99m-Human albumin macroaggregates or microspheresLung perfusion imaging with venographyIVIn-vivoImaging
Tc99m-Phosphonates and phosphates Bone imagingIVIn-vivoImaging
Tc99m-Phosphonates and phosphatesMyocardial imagingIVIn-vivoImaging
Tc99m-DTPA Renal imaging
First pass blood flow studies
Brain imaging
IVIn-vivoImaging
Tc99m-DTPA Lung ventilation imagingAerosol inhalationIn-vivoImaging
Tc99m-DMSA Tumor imagingIVIn-vivoImaging
Tc99m-DMSA Renal imagingIVIn-vivoImaging
Tc99m-ColloidBone marrow imaging

GI Bleeding
IVIn-vivoImaging
Tc99m-ColloidLymph node imagingInterstitialIn-vivoImaging
Tc99m-ColloidEsophageal transit and reflux imaging

Gastric emptying imaging
OralIn-vivoImaging
Tc99m-ColloidLacrimal imagingEye dropsIn-vivoImaging
Tc99m-HIDA Functional biliary system imagingIVIn-vivoImaging
Tc99m-Denatured red blood cellsRed cell volume

Spleen imaging
IVIn-vitroNon-imaging
Tc99m-Whole red blood cellsGI bleeding

Cardiac blood pool imaging

Peripheral vascular imaging
IVIn-vivoImaging
Tc99m-MAG3 Renal imaging

First pass blood flow imaging
IVIn-vivoImaging
Tc99m-Exametazime Cerebral blood flow imagingIVIn-vivoImaging
Tc99m-Exametazime labelled leucocytesInfection/inflammation imagingIVIn-vivoImaging
Tc99m-Sestamibi Parathyroid imaging

Non-specific tumor imaging

Thyroid tumor imaging

Breast imaging

Myocardial imaging
IVIn-vivoImaging
Tc99m-Sulesomab Infection/inflammation imagingIVIn-vivoImaging
Tc99m-TechnegasLung ventilation imagingInhalationIn-vivoImaging
Tc99m-Human immunoglobulinInfection/inflammation imagingIVIn-vivoImaging
Tc99m-TetrofosminParathyroid imaging

Myocardial imaging
IVIn-vivoImaging
Tc99m-ECD Brain imaging-----IVIn-vivoImaging

Indium-111

111In is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
In111-DTPA Ventriculo-peritoneal shunt intraperitoneal injectionIn-vivoImaging the radioactive substance
In111-DTPA CisternographyIntra-cisternalIn-vivoImaging
In111-LeukocytesInfection/inflammation imagingIVIn-vivoImaging
In111-PlateletsThrombus imagingIVIn-vivoImaging
In111-PentetreotideSomatostatin receptor imagingIVIn-vivoImaging
In111-OctreotideSomatostatin receptor imaging IVIn-vivoImaging

Iodine-123

Iodine-123 is a gamma emitter. It is used only diagnostically, as its radiation is penetrating and short-lived.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
I123-IodideThyroid uptakeOral or IVIn-vivoNon-imaging
I123-IodideThyroid imaging

Thyroid metastases imaging
Oral or IVIn-vivoImaging
I123-o-IodohippurateRenal imagingIVIn-vivoImaging
I123-MIBG Neuroectodermal tumour imagingIVIn-vivoImaging
I123-FP-CITSPECT imaging of Parkinson's DiseaseIVIn-vivoImaging

Iodine-125

125I is a gamma emitter with a long half-life of 59.4 days. Iodine-123 is preferred for imaging, so I-125 is used diagnostically only when the test requires a longer period to prepare the radiopharmaceutical and trace it, such as a fibrinogen scan to diagnose clotting. I-125's gamma radiation is of medium penetration, making it more useful as a therapeutic isotope for brachytherapy implant of radioisotope capsules for local treatment of cancers.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
I125-fibrinogenClot imagingIVIn-vivoImaging

Iodine-131

131I is a beta and gamma emitter. It is used both to destroy thyroid and thyroid cancer tissues, and also other neuroendocrine tissues when used in MIBG. It can also be seen by a gamma camera, and can serve as a diagnostic imaging tracer, when treatment is also being attempted at the same time. However iodine-123 is usually preferred when only imaging is desired.

Xenon-133

133Xe is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Xe133-gasLung ventilation studiesInhalationIn-vivoImaging
Xe133 in isotonic sodium chloride solutionCerebral blood flowIVIn-vivoImaging

Samarium-153

153Sm is a beta and gamma emitter.
NameTreatment ofRoute of administration
Sm153-EDTMP Bone metastasesIV

Erbium-169

169Er is a beta emitter.
NameTreatment ofRoute of administration
Er169-ColloidArthritic conditionsIntra-articular

Lutetium-177

177Lu is a beta emitter.
NameTreatment ofRoute of administrationIn-vitro / in-vivo
177Lu-DOTA-TATEgastroenteropancreatic neuroendocrine tumors IVIn-vivo

Thallium-201

201Tl is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging
Tl201-Tl+Non-specific tumor imaging

Thyroid tumor imaging

Myocardial imaging

Parathyroid imaging
IVIn-vivoImaging

Radium-223

223Ra is an alpha emitter.
NameTreatment ofRoute of administration
Ra223 cation metastatic cancer in boneIV