Technetium Tc-99m pyrophosphate

Identification

Name
Technetium Tc-99m pyrophosphate
Accession Number
DB09165  (DB09417)
Type
Small Molecule
Groups
Approved
Description

A radionuclide imaging agent used primarily in scintigraphy or tomography of the heart to evaluate the extent of the necrotic myocardial process. It has also been used in noninvasive tests for the distribution of organ involvement in different types of amyloidosis and for the evaluation of muscle necrosis in the extremities.

Structure
Thumb
Synonyms
  • Technetium (99mTc) pyrophosphate
  • Technetium TC 99M Pyrophosphate
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Kit for the Preparation of Technetium Tc99m PyrophosphateInjection12 mg/10mLIntravenousPharmalucence, Inc.1987-06-30Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Technescan PYPTechnetium Tc-99m pyrophosphate (11.9 mg/10mL) + Stannous chloride dihydrate (3.2 mg/10mL)Injection, powder, lyophilized, for solutionIntravenousMallinckrodt2009-03-202017-07-01Us
Categories
UNII
5L76I61H2B
CAS number
52997-54-3
Weight
Average: 272.847
Monoisotopic: 272.81818089
Chemical Formula
O7P2Tc
InChI Key
OOGKGVXDDGJCPO-NLQOEHMXSA-J
InChI
InChI=1S/H4O7P2.Tc/c1-8(2,3)7-9(4,5)6;/h(H2,1,2,3)(H2,4,5,6);/q;+4/p-4/i;1+2
IUPAC Name
(99Tc)technetium(4+) ion (phosphonooxy)phosphonate
SMILES
[99Tc+4].[O-]P([O-])(=O)OP([O-])([O-])=O

Pharmacology

Indication

For use as a skeletal imaging agent used to demonstrate areas of altered osteogenesis, and a cardiac imaging agent used as an adjunct in the diagnosis of acute myocardial infarction [Label]. May also be used to image gated blood pools and detect gastrointetinal bleeding.

Associated Conditions
Pharmacodynamics

Technetium Tc-99m pyrophosphate collects in areas of altered osteogenesis and injured myocardium. It also has an affinity for red blood cells, enabling imaging of blood pools.

Mechanism of action

It is thought that technetium Tc-99m pyrophosphate is adsorbed onto the surface of amorphous calcium phosphate deposits [1], insoluble hydroxyapatite crystals, and possibly other organic macromolecules. This would result in selective localization to necrotic muscle tissue such as that of a myocardial infarction where calcium deposition has begun as a result of cell damage. In areas of altered osteogenesis where hydroxyapatite formation is actively occuring, the surface area to volume ratio is high and favors a greater amount of technetium Tc-99m pyrophosphate to the surface of the crystals than in other areas of bone where crystal formation is less active. The localization of technetium Tc-99m pyrophosphate to these areas allows for their specific radioimaging.

TargetActionsOrganism
NHydroxyapatite
ligand
Human
NAmorphous calcium phosphate
ligand
Homo sapiens
Absorption

1-2h after injection approximately 40-50% is localized to the skeleton and 0.01-0.02% per gram to acutely infarcted myocardium [Label].

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination

Approximately 40% of the dose is excreted in the urine within 24h [Label].

Half life
Not Available
Clearance
Not Available
Toxicity

Adverse reactions such as flushing, hypotension, fever, chills, nausea, vomiting and dizziness, as well as hypersensitivity reactions such as itching and various skin rashes have been noted [Label]. Technetium Tc-99m pyrophosphate is a radiopharmaceutical and carries the risk of radiation toxicity if inappropriately dosed.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AcarboseAcarbose may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AclidiniumAclidinium may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AcrivastineTechnetium Tc-99m pyrophosphate may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirAcyclovir may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
AdefovirAdefovir may decrease the excretion rate of Technetium Tc-99m pyrophosphate which could result in a higher serum level.
Food Interactions
Not Available

References

General References
  1. Buja LM, Tofe AJ, Kulkarni PV, Mukherjee A, Parkey RW, Francis MD, Bonte FJ, Willerson JT: Sites and mechanisms of localization of technetium-99m phosphorus radiopharmaceuticals in acute myocardial infarcts and other tissues. J Clin Invest. 1977 Sep;60(3):724-40. [PubMed:893676]
External Links
PubChem Compound
6452753
PubChem Substance
347827829
ATC Codes
V09BA03 — Technetium (99mtc) pyrophosphate
FDA label
Download (104 KB)
MSDS
Download (28.3 KB)

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
InjectionIntravenous12 mg/10mL
Injection, powder, lyophilized, for solutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleMSDS
Radioactivity (mCi/mL)2FDA Label
Predicted Properties
PropertyValueSource
Water Solubility10.8 mg/mLALOGPS
logP1.43ALOGPS
logP-1.4ChemAxon
logS-1.6ALOGPS
pKa (Strongest Acidic)1.7ChemAxon
Physiological Charge-3ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area135.61 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity21.04 m3·mol-1ChemAxon
Polarizability9.03 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available

Taxonomy

Description
This compound belongs to the class of inorganic compounds known as transition metal pyrophosphates. These are inorganic compounds in which the largest oxoanion is pyrophosphate, and in which the heaviest atom not in an oxoanion is a transition metal.
Kingdom
Inorganic compounds
Super Class
Mixed metal/non-metal compounds
Class
Transition metal oxoanionic compounds
Sub Class
Transition metal pyrophosphates
Direct Parent
Transition metal pyrophosphates
Alternative Parents
Inorganic salts / Inorganic oxides
Substituents
Transition metal pyrophosphate / Inorganic oxide / Inorganic salt
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Small molecule
Organism
Human
Pharmacological action
No
Actions
Ligand
References
  1. Buja LM, Tofe AJ, Kulkarni PV, Mukherjee A, Parkey RW, Francis MD, Bonte FJ, Willerson JT: Sites and mechanisms of localization of technetium-99m phosphorus radiopharmaceuticals in acute myocardial infarcts and other tissues. J Clin Invest. 1977 Sep;60(3):724-40. [PubMed:893676]
Kind
Small molecule
Organism
Homo sapiens
Pharmacological action
No
Actions
Ligand
References
  1. Buja LM, Tofe AJ, Kulkarni PV, Mukherjee A, Parkey RW, Francis MD, Bonte FJ, Willerson JT: Sites and mechanisms of localization of technetium-99m phosphorus radiopharmaceuticals in acute myocardial infarcts and other tissues. J Clin Invest. 1977 Sep;60(3):724-40. [PubMed:893676]

Drug created on October 05, 2015 11:05 / Updated on November 02, 2018 06:59