Technetium Tc-99m oxidronate
Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- Technetium Tc-99m oxidronate
- DrugBank Accession Number
- DB09139
- Background
Technetium Tc-99m oxidronate, also known as 99mTc-methylene diphosphonate, is a radiopharmaceutical agent. A radiopharmaceutical is defined as a medicinal formulation containing radioisotopes that are used in major clinical areas for diagnosis and/or therapy.2 The radiopharmaceuticals based on technetium-99m are widely used for diagnostic purposes because 99mTc has a versatile chemistry which allows it to produce an extense variety of complexes with specific characteristics.3 These complexes are formed by the binding of 99mTc to metal atoms of an organic molecule. The group oxidronate falls into the category of diphosphonates whose structure allows them to bind to calcium.4 Thus, technetium Tc-99m oxidronate is a powerful detection tool for abnormal osteogenesis by skeletal scintigraphy.5 It was developed by Mallinkrodt nuclear and FDA approved on February 18, 1981.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 290.906
Monoisotopic: 290.865131083 - Chemical Formula
- CH6O7P2Tc
- Synonyms
- 99mtc-HDP
- Oxidronic acid 99mtc-complex
- Technetium (99mTc) oxidronate
- Technetium 99mtc oxidronate
- Technetium Tc 99m oxidronate
Pharmacology
- Indication
Technetium Tc-99m oxidronate is indicated in adult and pediatric patients to be used in skeletal imaging for diagnosis of areas that can present altered osteogenesis. When administered intravenously, it is able to generate a clear image of the bones which allows the physician to diagnose any bone problem.6 It is important to point out that this drug has to be manipulated only under the service of a nuclear specialist.5 The approved indications for a bone scan are 1) visualization of tumor metastasis in bone, 2) osteomyelitis, 3) fracture, 4) stress fracture, 5) avascular necrosis, 6) osteoporosis and 7) prosthetic joint evaluation. From all the major indications, the detection of a metastatic disease is the most common because it presents a 95% of sensitivity and lesion detection can be done 6 months earlier than with X-ray studies.4
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Osteogenesis imperfecta •••••••••••• •••••• ••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
The technetium is generated in a molibdene generator. Technetium Tc-99m presents a reduction of gamma emission after 6 hours and it is considered a quasi-stable molecule.5 The visualization of bone lesions is possible since there is an altered uptake in areas of abnormal osteogenesis.4 The principal photon used for detection is the gamma-2 with an energy of 140.5 keV.5 Its use for bone examination should be performed 2 hours after initial injection with a recommended activity on the range of 370-740 MBq.8
- Mechanism of action
The exact mechanism for bone uptake of technetium Tc-99m oxidronate is unknown. The most accepted mechanism is the localization of 99m-Tc on the surface of hydroxyapatite crystals of bone by chemisorption. Chemisorption is explained as a type of adsorption that involves a chemical reaction between the surface and the adsorbate in which new strong interactions form electronic bonds at the adsorbent surface.1 The presented chemisorption are regulated by the blood flow and blood concentration because it restrains the delivery of the agent in the uptake sites.4
- Absorption
Technetium Tc-99m oxidronate is rapidly absorbed and cleared from blood plasma to reach the skeleton.7 After 27 min of intravenous administration, a range of 45-50% of the technetium Tc-99m oxidronate is accumulated in the skeleton, reaching maximum accumulation at 1-hour post injection and remaining constant until 72 hours postinjection.8
- Volume of distribution
The distribution of technetium Tc-99m oxidronate at 1-hour post injection is mainly in the bones and secondary in the liver and kidneys.3
- Protein binding
The protein binding has been reported to be around 20-30% after 2-3 hours of intravenous administration.8
- Metabolism
Technetium Tc-99m oxidronate is a diphosphonate. There have been reports showing that diphosphonates form very stable Tc(IV) complexes which provide them with a very high in vivo stability and a very low degradation.8
- Route of elimination
It is recommended to empty bladder completely just prior to technetium Tc-99m oxidronate administration. It is as well recommended to drink abundant water and to empty bladder as often as possible to reduce radiation exposure in the bladder wall. The total radioactivity in blood between 5 min and 24 hours goes from 40% to 2.3% respectively. Technetium Tc-99m oxidronate whole body retention after 24 hours is a ratio of 36.6% which indicates that this drug, unlike other bone radiopharmaceuticals, presents a greater uptake. The glomerular filtration of technetium Tc-99m oxidronate can reach a 60% of the administered dose after 6 hours of the initial dose. The cumulative activity excreted in the urine after 24 hours is of approximately 59% suggesting a ratio of femur-to-muscle of 35.8
- Half-life
The elimination of technetium Tc-99m oxidronate is marked by the presence of three different half-times which are: 1) rapid phase of 3.5 min, 2) intermediate phase of 27 min and 3) slow phase of 144 min.8
- Clearance
During the first 24 hours of technetium Tc-99m oxidronate administration, it is observed a rapid clearance from blood and non-osseous tissues. The dosage gets accumulated in skeleton and urine.7
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
There has not been performed long-term animal studies to evaluate carcinogenic potential or an effect in fertility in males or females.7
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Technetium Tc-99m oxidronate which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Technetium Tc-99m oxidronate which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Technetium Tc-99m oxidronate which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Technetium Tc-99m oxidronate which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Technetium Tc-99m oxidronate which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
Categories
- ATC Codes
- V09BA01 — Technetium (99mtc) oxidronic acid
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as bisphosphonates. These are organic compounds containing two phosphonate groups linked together through a carbon atoms.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Organic phosphonic acids and derivatives
- Sub Class
- Bisphosphonates
- Direct Parent
- Bisphosphonates
- Alternative Parents
- Organic phosphonic acids / Organic transition metal salts / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organic oxides / Hydrocarbon derivatives
- Substituents
- Aliphatic acyclic compound / Bisphosphonate / Hydrocarbon derivative / Organic oxide / Organic oxygen compound / Organic salt / Organic transition metal salt / Organooxygen compound / Organophosphonic acid / Organophosphorus compound
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- MG4KI49HHJ
- CAS number
- 72945-61-0
- InChI Key
- SIJNDWFHVBDXDY-NLQOEHMXSA-N
- InChI
- InChI=1S/CH6O7P2.Tc/c2-1(9(3,4)5)10(6,7)8;/h1-2H,(H2,3,4,5)(H2,6,7,8);/i;1+2
- IUPAC Name
- [hydroxy(phosphono)methyl]phosphonic acid (⁹⁹Tc)technetium
- SMILES
- [99Tc].OC(P(O)(O)=O)P(O)(O)=O
References
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 0ºC (reconstituted) 'MSDS' boiling point (°C) 100ºC (reconstituted) 'MSDS' water solubility Soluble 'MSDS' Radioactivity (mCi/mL) 100000 'MSDS' - Predicted Properties
Property Value Source Water Solubility 13.5 mg/mL ALOGPS logP -1.1 ALOGPS logP -2 Chemaxon logS -1.2 ALOGPS pKa (Strongest Acidic) 0.75 Chemaxon pKa (Strongest Basic) -5 Chemaxon Physiological Charge -3 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 5 Chemaxon Polar Surface Area 135.29 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 29.72 m3·mol-1 Chemaxon Polarizability 11.94 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Tc-99m compounds [Link]
Drug created at September 30, 2015 16:50 / Updated at November 03, 2020 01:20