Nuclear pharmacy

Radiopharmaceuticals: drug products that contain radioactive elements. They

have (mainly) diagnostic applications; however, they are also used in
therapeutic purposes.

Radionuclide: the radioactive component of a radiopharmaceutical.

Radionuclides undergo spontaneous radioactive decay accopanied by the
release of energy. There are four major types of radiation emitted through this
process: alpha, beta, gamma and x-rays. Alpha and beta radiations are not
useful in medical imaging and most radiopharmaceuticals use penetrating
gamma radiation.

Half-lives of radiopharmaceuticals:
a. Physical half-life: the amount of time necessary for the radioactive
atoms to decay to one half their original number.
b. Biological half-life: the amount of time necessary for the body to
eliminate one half of the administered dose.
c. Effective half-life: the time requred for an administered dose to be
reduced to one half due to both physical decay and biological
elimination.

Optimal radiopharmaceuticals:
1- With half lives short enough to minimize patient exposure yet
long enough to collect imaging information.
2- Incorporate a gamma emitting radionuclide.
3- Localized rapidly in the organ system of interest.
4- Available and cost-effective.

Sodium pertechnetate technetium-99m (99mTc) generator:

- the most commonly used radionuclide in diagnostic
imaging today.
- Produced by the radioactive decay of molybdenum-99
(99Mo).
Generation: 99Mo parent is absorbed on an alumina ion exchange column, and
the 99mTc formed from its decay is exchanged for the chloride ion available in
normal saline eluate solution as sodium pertechnetate Na(99mTcO4). Then,
reduction of 99mTc+7 is done (most commonly by stannus).
Decay data: 6 hrs physiacal half life, emitting gamma radiation.
Uses: imaging stydies of brain, thyroid, salivary gland, placenta, blood pool
(I.V.) and nasolacrimal imaging (instilled into the lacrimal canal).
a) Sulfur colloid is used for liver scanning
b) Macro-aggregated albumin is used for lung scanning
c) Gluceptate, succimer & pentetate are used for kidney scanning
d) Sestamibi & tetrofosmin for heart.
e) Medronate, oxidronate & pyrophosphate for bone.
 f) disofenin, lidofenin & mebrofenin for hepatobiliary.
g) exametazine & bicisate for brain imaging.
h) Exametazine for WBCs labelling.
i) Sestamibi for breast.
j) Apcitide for DVT.
k) Tc-99m arcitumomab Fab fragment: for colorectal cancer.

Radiopharmaceuticals for imaging purposes:

Organ Radionuclide used

Heart Perfusion agents for cardiac imaging: thallous chloride,
technetium-99m sestamibi & tetrofosmin, rubidium chloride,
ammonia N-13.
To measure cardiac function: 99mTc labeled RBCs,
pyrophosphate injection and 99mTc albumin injection.
MI imaging: pyrophosphates & phosphates.
99m
Bone Tc medronate, oxidronate & pyrophosphate.
Lung Perfusion imaging: 99mTc albumin aggregate.
Ventilation imaging: Xenon 133Xe & 127Xe, Krypton 81mKr and
99m
Tc pentetate (radioaerosol).
Liver Reticuloendothelial: 99mTc sulfur colloid.
Hepatobiliary: iminodiacetic acid derivatives (lidocaine
analog) 99mTc disofenin, lidofenin & mebrofenin.
Kidney Agents cleared by glomerular filteration: 99mTc pentetate &
sodium iothalmate 125I.
Tubular secretion agents: 131I hippuran & 99mTc.
Renal cortical imaging: 99mTc gluceptate & succimer.
131 123
Thyroid I, I, Na99mTcO4.
Brain Cerebral perfusion: 99mTc exametazine & bicisate.
Cerebral metabolism: 18F fludeoxyglucose.
Cerebral neurotransmitter imaging: 18F fluorodopa.
CSF dynamics: 111In-pentetate.
Infection & Gallium citrate Ga-67: areas with WBCs localization
inflammation WBC labeling agents: 111In oxyquinolone, 99mTc exametazine.
99m
Breast Tc sestamibi.
99m
DVT Tc apcitide.
Tumors Gallium citrate Ga-67, In-111 pentetreotide, Iobenguane I-131,
thallous chloride, fludeoxyglucose F-18.
Murine monoclonal Antibodies: In-111 satumomab pendetide
(colorectal & ovarian), In-111 capromab pendetide (prostatic),
Tc-99m arcitumomab Fab fragment (colrectal). Risk of
producing human anti-murine antibodies with the first two
agents.
Radiopharmaceuticals for therapeutic purposes:

Agent Uses
Chromium phosphate P-32 Peritonial or pleural effusions caused by metastatic
suspension disease & ovarian and prostatic cancer.
Sodium phosphate P-32 Polycythemia rubra vera, metastatic bone pain.
solution
Sodium iodide I-131 Hyperthyoidism and thyroid carcinoma.
Stronium 89Sr chloride & Alleviation of bone pain due to metastatic bone
Samarium-153 lexidronan pain.

Biotechnologic Products
Basic terminology:
Colony-stimulating factors (CSFs): a class of glycoprotein hormones that
regulate the differentiation and formation of blood cells from precursor cells.
Cytokines: a group of special proteins (non antibodies) released by cells to
trigger action in other cells.
Lymphokine: any class of soluble proteins produced by some WBCs and
stimulate other WBCs as part of the immune response.
Tumor necrosis factor (TNF): a lymphokine produced by macrophages. It
can be activated to kill tumor cells.
Interferon: a class of glycoproteins produced by animal cells in response to
viral infection.
Interleukin: a group of proteins synthesized by macrophages and T
lymphocytes in response to antigens and other stimulation.

DNA ligase: seals single-stranded nicks between nucleotides in double

stranded DNA.
DNA polymerase: catalyzes the synthesis of DNA. It uses a single strand of
DNA as the template and uses nucleotides as the substrates.
DNA gyrase: responsible for DNA super coiling.
Plasmid: a circular piece of duplex DNA that is not part of a chromosome and
can replicate independently. Plasmids can be used as vectors for transfer of
DNA in recombinant DNA technology.
Recombinant DNA (rDNA): a hybrid DNA that is formed when pieces of
DNA from different sources are joined. The process is termed gene splicing.
Restriction endonuclease: an enzyme that cleaves DNA at sequence specific
sites.
Antisense DNA: a complementary strand of DNA that is specifically
synthesized to attach to the sense DNA and prevent genetic transcription.
Examples of biotechnologic products: (full details in CPR pages 200-204)

Drug Indication
Human insulin Diabetes
Somatrem, somatotropin & Human GH deficiency in children
Human growth hormone Short stature.
Interferon-alpha-2a Leukemia & AIDs related Kaposi sarcoma
Interferon-alpha-2b Leukemia & lymphoma
Chronic hepatitis C
Muromonab-CD3 Acute kidney transplant rejection
Daclizumab, Basiliximab Prophylaxis of acute graft rejection after renal
transplantation.
Erythropietin Anaemia associated with CRF, AIDS, zidovudine
administation, chemotherapy & cancer.
Antihemophilic factor Hemophilia
Filgrastim & Sargramostim Bone marrow transplant
Abciximab & Eptifibatide Glycoprotein IIb/IIIa receptor antagonist
Alteplase, Reteplase Thrombolytic
Infliximab Inflammatory bowel diseases & RA.
Etanercept Rheumatoid arthritis (RA).

N.B. Biotechnologic products are commonly stored in a cool place after

reconstitution.