Radiopharmacology

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Radiopharmacology
Lead container for nuclear medications.jpg
Lead container for iodine-123 capsule
Other namesMedicinal radiochemistry
Specialty oncology

Radiopharmacology is radiochemistry applied to medicine and thus the pharmacology of radiopharmaceuticals (medicinal radiocompounds, that is, pharmaceutical drugs that are radioactive). Radiopharmaceuticals are used in the field of nuclear medicine as radioactive tracers in medical imaging and in therapy for many diseases (for example, brachytherapy). Many radiopharmaceuticals use technetium-99m (Tc-99m) which has many useful properties as a gamma-emitting tracer nuclide. In the book Technetium a total of 31 different radiopharmaceuticals based on Tc-99m are listed for imaging and functional studies of the brain, myocardium, thyroid, lungs, liver, gallbladder, kidneys, skeleton, blood and tumors. [1]

Contents

The term radioisotope, which in its general sense refers to any radioactive isotope (radionuclide), has historically been used to refer to all radiopharmaceuticals, and this usage remains common. Technically, however, many radiopharmaceuticals incorporate a radioactive tracer atom into a larger pharmaceutically-active molecule, which is localized in the body, after which the radionuclide tracer atom allows it to be easily detected with a gamma camera or similar gamma imaging device. An example is fludeoxyglucose in which fluorine-18 is incorporated into deoxyglucose. Some radioisotopes (for example gallium-67, gallium-68, and radioiodine) are used directly as soluble ionic salts, without further modification. This use relies on the chemical and biological properties of the radioisotope itself, to localize it within the body.

History

See nuclear medicine.

Production

Production of a radiopharmaceutical involves two processes:

Radionuclides used in radiopharmaceuticals are mostly radioactive isotopes of elements with atomic numbers less than that of bismuth, that is, they are radioactive isotopes of elements that also have one or more stable isotopes. These may be roughly divided into two classes:

Practical use

Because radiopharmeuticals require special licenses and handling techniques, they are often kept in local centers for medical radioisotope storage, often known as radiopharmacies. A radiopharmacist may dispense them from there, to local centers where they are handled at the practical medicine facility.

Drug nomenclature for radiopharmaceuticals

As with other pharmaceutical drugs, there is standardization of the drug nomenclature for radiopharmaceuticals, although various standards coexist. The International Nonproprietary Name (INN) gives the base drug name, followed by the radioisotope (as mass number, no space, element symbol) in parentheses with no superscript, followed by the ligand (if any). It is common to see square brackets and superscript superimposed onto the INN name, because chemical nomenclature (such as IUPAC nomenclature) uses those. The United States Pharmacopeia (USP) name gives the base drug name, followed by the radioisotope (as element symbol, space, mass number) with no parentheses, no hyphen, and no superscript, followed by the ligand (if any). The USP style is not the INN style, despite their being described as one and the same in some publications (e.g., AMA, [4] whose style for radiopharmaceuticals matches the USP style). The United States Pharmacopeial Convention is a sponsor organization of the USAN Council, and the USAN for a given drug is often the same as the USP name.

International Nonproprietary Name (INN) United States Pharmacopeia (USP)Comments
technetium (99mTc) sestamibi technetium Tc 99m sestamibi 
fludeoxyglucose (18F) fludeoxyglucose F 18 
sodium iodide (125I) sodium iodide I 125 
indium (111In) altumomab pentetate indium In 111 altumomab pentetate 

See also

Related Research Articles

Technetium Chemical element, symbol Tc and atomic number 43

Technetium is a chemical element with the symbol Tc and atomic number 43. It is the lightest element whose isotopes are all radioactive. Nearly all available technetium is produced as a synthetic element. Naturally occurring technetium is a spontaneous fission product in uranium ore and thorium ore, the most common source, or the product of neutron capture in molybdenum ores. This silvery gray, crystalline transition metal lies between manganese and rhenium in group 7 of the periodic table, and its chemical properties are intermediate between those of both adjacent elements. The most common naturally occurring isotope is 99Tc, in traces only.

A radionuclide is a nuclide that has excess nuclear energy, making it unstable. This excess energy can be used in one of three ways: emitted from the nucleus as gamma radiation; transferred to one of its electrons to release it as a conversion electron; or used to create and emit a new particle from the nucleus. During those processes, the radionuclide is said to undergo radioactive decay. These emissions are considered ionizing radiation because they are powerful enough to liberate an electron from another atom. The radioactive decay can produce a stable nuclide or will sometimes produce a new unstable radionuclide which may undergo further decay. Radioactive decay is a random process at the level of single atoms: it is impossible to predict when one particular atom will decay. However, for a collection of atoms of a single nuclide the decay rate, and thus the half-life (t1/2) for that collection, can be calculated from their measured decay constants. The range of the half-lives of radioactive atoms has no known limits and spans a time range of over 55 orders of magnitude.

A synthetic radioisotope is a radionuclide that is not found in nature: no natural process or mechanism exists which produces it, or it is so unstable that it decays away in a very short period of time. Examples include technetium-95 and promethium-146. Many of these are found in, and harvested from, spent nuclear fuel assemblies. Some must be manufactured in particle accelerators.

Single-photon emission computed tomography Nuclear medicine tomographic imaging technique

Single-photon emission computed tomography is a nuclear medicine tomographic imaging technique using gamma rays. It is very similar to conventional nuclear medicine planar imaging using a gamma camera, but is able to provide true 3D information. This information is typically presented as cross-sectional slices through the patient, but can be freely reformatted or manipulated as required.

Nuclear medicine Medical specialty

Nuclear medicine is a medical specialty involving the application of radioactive substances in the diagnosis and treatment of disease. Nuclear imaging, in a sense, is "radiology done inside out" or "endoradiology" because it records radiation emitting from within the body rather than radiation that is generated by external sources like X-rays. In addition, nuclear medicine scans differ from radiology, as the emphasis is not on imaging anatomy, but on the function. For such reason, it is called a physiological imaging modality. Single photon emission computed tomography (SPECT) and positron emission tomography (PET) scans are the two most common imaging modalities in nuclear medicine.

A radioactive tracer, radiotracer, or radioactive label is a chemical compound in which one or more atoms have been replaced by a radionuclide so by virtue of its radioactive decay it can be used to explore the mechanism of chemical reactions by tracing the path that the radioisotope follows from reactants to products. Radiolabeling or radiotracing is thus the radioactive form of isotopic labeling. In biological contexts, use of radioisotope tracers are sometimes called radioisotope feeding experiments.

Scintigraphy Diagnostic imaging test in nuclear medicine

Scintigraphy, also known as a gamma scan, is a diagnostic test in nuclear medicine, where radioisotopes attached to drugs that travel to a specific organ or tissue (radiopharmaceuticals) are taken internally and the emitted gamma radiation is captured by external detectors to form two-dimensional images in a similar process to the capture of x-ray images. In contrast, SPECT and positron emission tomography (PET) form 3-dimensional images and are therefore classified as separate techniques from scintigraphy, although they also use gamma cameras to detect internal radiation. Scintigraphy is unlike a diagnostic X-ray where external radiation is passed through the body to form an image.

Technetium-99m generator A device used to extract the short-lived radioactive isotope Tc-99m from a longer-lived Mo-99 source

A technetium-99m generator, or colloquially a technetium cow or moly cow, is a device used to extract the metastable isotope 99mTc of technetium from a decaying sample of molybdenum-99. 99Mo has a half-life of 66 hours and can be easily transported over long distances to hospitals where its decay product technetium-99m is extracted and used for a variety of nuclear medicine diagnostic procedures, where its short half-life is very useful.

Isotopes of iodine Nuclides with atomic number of 53 but with different mass numbers

There are 37 known isotopes of iodine (53I) from 108I to 144I; all undergo radioactive decay except 127I, which is stable. Iodine is thus a monoisotopic element.

Technetium (43Tc) is one of the two elements with Z < 83 that have no stable isotopes; the other such element is promethium. It is primarily artificial, with only trace quantities existing in nature produced by spontaneous fission or neutron capture by molybdenum. The first isotopes to be synthesized were 97Tc and 99Tc in 1936, the first artificial element to be produced. The most stable radioisotopes are 97Tc, 98Tc, and 99Tc.

Molybdenum (42Mo) has 33 known isotopes, ranging in atomic mass from 83 to 115, as well as four metastable nuclear isomers. Seven isotopes occur naturally, with atomic masses of 92, 94, 95, 96, 97, 98, and 100. All unstable isotopes of molybdenum decay into isotopes of zirconium, niobium, technetium, and ruthenium.

Sodium pertechnetate Chemical compound

Sodium pertechnetate is the inorganic compound with the formula NaTcO4. This colourless salt contains the pertechnetate anion, TcO
4
. The radioactive 99m
Tc
O
4
anion is an important radiopharmaceutical for diagnostic use. The advantages to 99m
Tc
include its short half-life of 6 hours and the low radiation exposure to the patient, which allow a patient to be injected with activities of more than 30 millicuries. Na[99m
Tc
O
4
]
is a precursor to a variety of derivatives that are used to image different parts of the body.

Radionuclides which emit gamma radiation are valuable in a range of different industrial, scientific and medical technologies. This article lists some common gamma-emitting radionuclides of technological importance, and their properties.

Iodine-125 (125I) is a radioisotope of iodine which has uses in biological assays, nuclear medicine imaging and in radiation therapy as brachytherapy to treat a number of conditions, including prostate cancer, uveal melanomas, and brain tumors. It is the second longest-lived radioisotope of iodine, after iodine-129.

Iodine-123 (123I) is a radioactive isotope of iodine used in nuclear medicine imaging, including single-photon emission computed tomography (SPECT) or SPECT/CT exams. The isotope's half-life is 13.22 hours; the decay by electron capture to tellurium-123 emits gamma radiation with a predominant energy of 159 keV. In medical applications, the radiation is detected by a gamma camera. The isotope is typically applied as iodide-123, the anionic form.

Technetium-99m Metastable nuclear isomer of technetium-99

Technetium-99m (99mTc) is a metastable nuclear isomer of technetium-99, symbolized as 99mTc, that is used in tens of millions of medical diagnostic procedures annually, making it the most commonly used medical radioisotope in the world.

Perfusion is the passage of fluid through the lymphatic system or blood vessels to an organ or a tissue. The practice of perfusion scanning is the process by which this perfusion can be observed, recorded and quantified. The term perfusion scanning encompasses a wide range of medical imaging modalities.

A germanium-68/gallium-68 generator is a device used to extract the positron-emitting isotope 68Ga of gallium from a source of decaying germanium-68. The parent isotope 68Ge has a half-life of 271 days and can be easily utilized for in-hospital production of generator produced 68Ga. Its decay product gallium-68 is extracted and used for certain positron emission tomography nuclear medicine diagnostic procedures, where the radioisotope's relatively short half-life and emission of positrons for creation of 3-dimensional PET scans, are useful.

A medical isotope is an isotope used in medicine.

Radiopharmaceutical Pharmaceutical drug which emits radiation, used as a diagnostic or therapeutic agent

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.

References

  1. Schwochau, Klaus. Technetium. Wiley-VCH (2000). ISBN   3-527-29496-1
  2. "Canada's Chalk River Reactor coming back online will not solve long-term isotope shortage in hospitals, researchers say".
  3. "Archived copy" (PDF). Archived from the original (PDF) on 2018-03-13. Retrieved 2014-09-21.{{cite web}}: CS1 maint: archived copy as title (link)
  4. Iverson, Cheryl, et al. (eds) (2007), "15.9.2 Radiopharmaceuticals", AMA Manual of Style (10th ed.), Oxford, Oxfordshire: Oxford University Press, ISBN   978-0-19-517633-9.{{citation}}: |first= has generic name (help)

Further reading