Pharmaceutical and Radiopharmaceutical Agents (part 2)- Domain 3

Pertechnetate

active transport

Thyroid imaging, Meckel’s diverticulum scan, salivary gland imaging, gastric mucosa imaging

X- Pregnancy (relative), iodine therapy interference

IV injection

HDP- Oxidronate

chemisorption

Bone scan for metastases, fractures, infections

X- severe renal impairment, pregnancy

IV injection

MDP- Medronate

chemisorption

Bone scan for metastases, fractures, infections

X- severe renal impairment, pregnancy

IV injection

DTPA- Pentetate

compartmentalization, glomerular filtration

Renal function scan (GFR), brain death study, aerosol lung ventilation scan

IV for renal/brain imaging, nebulizer inhalation for lung

MAA- macroaggregated albumin

capillary blockade

Lung perfusion scan (V/Q scan), pre-Y90 therapy planning

X- Severe pulmonary hypertension, right-to-left cardiac shunt, pregnancy

slow IV injection, no blood, agitate syringe, pt is supine

Sulfur Colloid

phagocytosis

Liver-spleen imaging, gastric emptying study, lymphoscintigraphy (filtered SC)

X- Hypersensitivity to colloid or components

IV injection, oral w/eggs for gastrics

Membrofenin- Choletec

active transport

Hepatobiliary (HIDA) scan, gallbladder evaluation, GBEF

X- Severe hepatic dysfunction

IV injection

MAG3- Mertiatide

tubular secretion-active transport

Renal perfusion/function imaging

IV injection

PYP- Pyrophosphate

chemisorption

Cardiac amyloidosis imaging, old method for myocardial infarct imaging, blood pool imaging (tagged RBC substitute)

IV injection

Sestamibi- Cardiolite

passive diffusion

Myocardial perfusion imaging (stress/rest), parathyroid imaging

X- pregnancy

IV bolus

Tetrofosmin- Myoview

passive diffusion

Myocardial perfusion imaging (stress/rest)

X- pregnancy

IV bolus

DMSA- Succimer- Nephroscan

cortical binding

Renal cortical imaging (e.g., scarring, congenital anomalies)

IV injection

HMPAO- Ceretec- Exametazime

passive diffusion

Cerebral perfusion imaging (stroke, epilepsy),

IV

ECD- Bicisate- Neurolite

passive diffusion

Brain perfusion imaging (stroke assessment)

IV

Labeled RBC- Ultratag/PYP

GI bleeding study, cardiac blood pool imaging (MUGA)

X- Severe anemia

In vivo, in vitro, or modified in vivo RBC labeling and IV reinjection

HMPAO tagged WBC

cell sequestration

Infection imaging (e.g., osteomyelitis, abscess)

X- Severe leukopenia (low WBC count)

Blood drawn, WBCs labeled ex vivo with HMPAO, then reinjected

Tilmanocept- Lymphoseek

phagocytosis

Sentinel lymph node mapping in cancers (breast, melanoma, etc.)

Subcutaneous or intradermal injection near tumor site

I-123 sodium iodide

active transport

Thyroid uptake and imaging (hyperthyroidism, nodules), metastatic thyroid cancer evaluation

X- Pregnancy, breastfeeding, iodine allergy

Oral

I-131 sodium iodide

active tranport

Thyroid imaging, primary therapy for hyperthyroidism and thyroid cancer ablation

X- Pregnancy, breastfeeding, severe iodine allergy

Oral

I-123 Iobenguane- MIBG- AdreView

receptor binding

Imaging of neuroblastoma, pheochromocytoma, paraganglioma

X- Medications interfering with norepinephrine uptake (e.g., tricyclic antidepressants); pregnancy

IV injection; thyroid blockade required (potassium iodide tablets) to prevent free iodine uptake

I-123 Ioflupane- DatScan

receptor binding

Imaging to differentiate Parkinsons syndromes from essential tremor

X- pregnancy

IV injection; thyroid blockade recommended

In-111 chloride

radiolabeling

Bone marrow imaging (marrow distribution, marrow failure, transplant follow-up)

X- pregnancy

IV

In-111Oxine labeled WBC

cell sequestration

Imaging infection/inflammation (e.g., osteomyelitis, abscesses, infected prosthetics)

X- Severe leukopenia (low WBC count)

Blood drawn from patient, WBCs isolated and labeled with In-111 oxine, labeled cells reinjected into patient

In-111- Pentetate- DTPA

compartmentalization

Cisternography (CSF leak detection, hydrocephalus evaluation)

X- Active CNS infection (meningitis), pregnancy

Intrathecal injection (lumbar puncture)

In-111 pentetreotide- Octreoscan

receptor binding

Localization of neuroendocrine tumors (carcinoid, gastrinoma, insulinoma, pheochromocytoma)

X- pregnancy

IV

Ga-67 citrate

Receptor Binding (Transferrin / Chemotaxis)

Infection/inflammation imaging (e.g., fever of unknown origin), lymphoma staging, tumor imaging

X- pregnancy

IV

Tl-201 thallous chloride

active transport

Myocardial perfusion imaging, tumor imaging (thyroid, brain tumors)

X- pregnancy

IV

Xe-133 gas

compartmentalization

Pulmonary ventilation imaging (part of V/Q scan)

X- Severe pulmonary disease, pregnancy

Inhalation

Cu-64- Dotatate- Detectnet

receptor binding

PET imaging of neuroendocrine tumors

X- pregnancy

IV

F-18 FDG

active transport (metabolism/glucose analog)

Oncology (tumor imaging), infection/inflammation imaging, neurology (epilepsy, dementia)

X- too high blood sugar, pregnancy

IV

F-18 Florbetaben- Neuraceq

receptor binding

Imaging β-amyloid plaque density (Alzheimer's disease diagnosis)

IV

F-18 Florbetapir- Amyvid

receptor binding

Alzheimer’s disease evaluation

IV

F-18 Flutemetamol- Vizamyl

receptor binding

Alzheimer’s disease evaluation

IV

F-18 Sodium Fluoride- NaF

Bone metastasis imaging (superior resolution to Tc-99m MDP)

X- pregnancy

IV

F-18 Fluciclovine- Axumin

amino acid transporter

Prostate cancer recurrence imaging

IV

F-18 Flortaucipir- Tauvid

receptor binding

Imaging tau pathology in Alzheimer’s disease

IV

F-18 Piflufoflastat- Pylarify

bind to PSMA receptors

Prostate cancer imaging

IV

F-18 Fluorodopa

decarboxylase, dopaminergic nerve terminals

PET imaging for Parkinson’s disease and neuroendocrine tumors

IV

F-18 Fluoroestradiol- Cerianna

receptor binding, breast cancer cells

Imaging estrogen receptor–positive breast cancer

IV

Ga-68 Dotatate- Netspot

endocytosis

PET imaging of neuroendocrine tumors

IV

Ga-68 Dotatoc

endocytosis

Neuroendocrine tumor imaging

IV

Ga-68 Gozetotide- Illuccix, Locametz

bind to PSMA receptors

Prostate cancer imaging

IV

N-13 Ammonia

passive diffusion

Myocardial perfusion PET imaging

IV

Rb-82 chloride- Rubyfill, Cardiogen

active transport

PET myocardial perfusion imaging

X- Severe hyperkalemia; pregnancy

IV infusion

Lu-177 dotatate- Lutathera

receptor binding, endocytosis

Gastroenteropancreatic neuroendocrine tumors (GEP-NETs)

X- Pregnancy, renal impairment, myelosuppression

IV infusion every 8 weeks × 4 doses

Lu-177 Vipivotide tetraxetan- Pluvicto

bind to PSMA receptors

PSMA-positive metastatic castration-resistant prostate cancer (mCRPC)

X- severe bone marrow suppression

IV infusion every 6 weeks × 6 doses

Ra-223- Radium dichloride- Xofigo

chemisorption

Bone metastases from prostate cancer

X- Visceral metastases, bone marrow suppression

IV injection every 4 weeks × 6 doses

Sr-89 chloride- Metastron

chemisorption

Painful bone metastases (especially prostate or breast cancer)

X- Bone marrow suppression, pregnancy

IV

Y-90 microspheres- SIR-Spheres, TheraSpheres

implantation

Primary liver cancer (HCC) or liver-dominant metastases

X- Hepatic dysfunction, extrahepatic shunting (GI/lung), pregnancy

Intra-arterial via hepatic artery catheterization