Fluoride ion F-18
Identification
- Summary
Fluoride ion F-18 is a diagnostic radiopharmaceutical agent used as a bone imaging agent to delineate areas of altered osteogenesis.
- Brand Names
- Sodium Fluoride F-18
- Generic Name
- Fluoride ion F-18
- DrugBank Accession Number
- DB09398
- Background
Sodium Fluoride F 18 Injection is a positron emitting radiopharmaceutical, no-carrier added. It contains radioactive fluoride F 18 that is used for diagnostic purposes in conjunction with positron emission tomography (PET) imaging and is administered by intravenous injection. Its primary indication is for bone imaging. Increased deposition around joints can occur in arthritis and following trauma and increased deposition in bone has been noted around fracture sites, in osteomyelitis, fibrous dysplasia, spondylitis tuberculosa, and Paget's disease. No adverse reactions have been reported.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 18.0015
Monoisotopic: 18.001486247 - Chemical Formula
- F
- Synonyms
- (18F)-Fluoride
- 18F-Fluoride
- Fluoride-18 anion
Pharmacology
- Indication
18F is used as a bone imaging agent to define areas of altered osteogenic activity. It has been indicated for back pain and otherwise unexplained bone pain, child abuse, abnormal radiographic or laboratory findings, osteomyelitis, trauma, inflammatory and degenerative arthritis, avascular necrosis. Osteonecrosis of the mandible, condylar hyperplasia, and metabolic bone disease are also among the indications for fluoride imaging.
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- Contraindications & Blackbox Warnings
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- Pharmacodynamics
Deposition of 18F fluoride in bone appears to be primarily a function of blood flow to the bone and the efficiency of the bone in extracting the 18F from the blood perfusing the bone. Increased fluorine F 18 ion deposition around joints can occur in arthritis or following trauma; increased deposition has also been documented in bone around fracture sites, in osteomyelities, fibrous dysplasia, spondylitis tuberculosa, Paget's disease, hyperstosis frontalis interna, myositis, ossificans, and in rapidly growing epiphyses. The tendency for fluorine F 18 ions to accumulate in the vicinity of primary and metastatic malignancy in bone has proven clinically useful in detection of such lesions
- Mechanism of action
18F-fluoride is a highly sensitive bone-seeking PET tracer used for detection of skeletal abnormalities. The uptake mechanism of 18F-fluoride has better pharmacokinetic characteristics (compared to other elements) including faster blood clearance and 2-fold higher uptake in bone. Uptake of 18F-fluoride reflects blood flow and bone remodeling.
- Absorption
Following intravenous administration, Sodium Fluoride F 18 injection provides fluorine F 18 ions that rapidly equilibrate, primarily within the extracellular fluid space.
- Volume of distribution
0.5-0.7 L/Kg
- Protein binding
Fluorine F 18 ions do not appear to be bound to serum proteins
- Metabolism
First, the 18F- exchanges for an OH- ion on the surface of the hydroxyapatite matrix of bone and this is followed by migration of the 18F- into the crystalline matrix of the bone where it is retained until the bone is remodelled.
- Route of elimination
Fluorine F 18 ions are rapidly eliminated via the renal system. 20% or more of the fluorine F 18 ions are cleared from the body in the urine within the first 2 hours after intravenous administration.
- Half-life
110 min.
- Clearance
Renal clearance for fluoride is 48-147 mL/min, depending upon urinary flow and pH.
- Adverse Effects
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- Toxicity
The lethal dose of NaF to the average adult has been estimated to be between 32 to 64 mg fluoride/kg body weight.
- 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.Not Available
- Food Interactions
- No interactions found.
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.
- Product Ingredients
Ingredient UNII CAS InChI Key Sodium fluoride F-18 9L75099X6R 22554-99-0 PUZPDOWCWNUUKD-ULWFUOSBSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sodium Fluoride F 18 Injection, solution 475 mCi/1mL Intravenous Triad Isotopes, Inc. 2010-11-20 2010-11-20 US Sodium FluorideF 18 F 18 Injection 200 mg/1mL Intravenous Children's Hospital Of Michigan 2012-06-12 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous Sofie Co. 2011-12-08 Not applicable US Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous Ucsf Radiopharmaceutical Facility 2009-11-01 Not applicable US Sodium Fluoride F 18 Injection, solution 200 mCi/1mL Intravenous JUBILANT DRAX IMAGE RADIOPHARMACIES, INC. DBA JUBILANT RADIOPHARMA 2011-01-26 Not applicable US Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous BAMF Health Inc. 2022-12-06 Not applicable US Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous Essential Isotopes LLC 2011-01-01 Not applicable US Sodium Fluoride F 18 Injection, solution 200 mCi/1mL Intravenous Biomedical Research Foundation Of Northwest Louisiana 2015-01-22 Not applicable US Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous Houston Cyclotron Partners Lp Dba Cyclotope 2011-12-08 2020-05-11 US Sodium Fluoride F 18 Injection 600 mCi/1mL Intravenous THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 2014-11-19 Not applicable US Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous Precision Nuclear Llc 2011-01-01 Not applicable US Sodium Fluoride F 18 Injection 200 mCi/1mL Intravenous NukeMed, Inc. dba SpectronRx 2015-04-24 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Sodium Fluoride F 18 Sodium fluoride F-18 (475 mCi/1mL) Injection, solution Intravenous Triad Isotopes, Inc. 2010-11-20 2010-11-20 US Sodium FluorideF 18 F 18 Sodium fluoride F-18 (200 mg/1mL) Injection Intravenous Children's Hospital Of Michigan 2012-06-12 Not applicable US
Categories
- ATC Codes
- V09IX06 — Sodium fluoride (18f)
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of inorganic compounds known as homogeneous halogens. These are inorganic non-metallic compounds in which the largest atom is a nobel gas.
- Kingdom
- Inorganic compounds
- Super Class
- Homogeneous non-metal compounds
- Class
- Homogeneous halogens
- Sub Class
- Not Available
- Direct Parent
- Homogeneous halogens
- Alternative Parents
- Not Available
- Substituents
- Homogeneous halogen
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 4M4WE5N2GE
- CAS number
- 67862-54-8
- InChI Key
- KRHYYFGTRYWZRS-BJUDXGSMSA-M
- InChI
- InChI=1S/FH/h1H/p-1/i1-1
- IUPAC Name
- (18F)fluoride
- SMILES
- [18F-]
References
- General References
- External Links
- PubChem Compound
- 23690531
- PubChem Substance
- 347827843
- ChemSpider
- 8373100
- 1546273
- ChEMBL
- CHEMBL1248
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Prevention Atherosclerosis / Cardiovascular Disease (CVD) / Molecular Imaging 1 3 Completed Diagnostic Bone Metastases 1 3 Completed Diagnostic Bone Metastases From Breast or Prostate Cancer 1 2 Completed Diagnostic Cancer 1 2 Completed Diagnostic Neoplasms of the Prostate 1 2 Enrolling by Invitation Diagnostic Metastatic Prostate Cancer / Neoplasms of the Prostate / Prostate Cancer 1 2 Recruiting Treatment Hereditary leiomyomatosis renal cell carcinoma / Papillary Renal Cell Carcinoma / Renal Cell Carcinoma (RCC) / Sporadic Papillary Renal Cell Carcinoma / Stage III Renal Cell Cancer AJCC v8 / Stage IV Renal Cell Cancer AJCC v8 1 2 Unknown Status Diagnostic Artery Stenosis, Carotid 1 1 Completed Diagnostic Metastatic Prostate Cancer 1 1 Terminated Diagnostic Hormone Resistant Prostate Cancer / Metastatic Carcinoma of the Prostate / Metastatic Malignant Neoplasm in the Bone 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet 0.25 mg Injection, solution Parenteral 2 GBq/ml Injection, solution Intravenous Injection Intravenous 10 mCi/1mL Injection Intravenous 600 mCi/1mL Injection Intravenous 91.5 mCi/1mL Injection, solution Intravenous 200 mCi/1mL Injection, solution Intravenous 475 mCi/1mL Injection Intravenous 200 mCi/1mL Injection, solution Intravenous 10-200 mCi/ML Injection Intravenous 200 mg/1mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source logP 0.15 Chemaxon pKa (Strongest Acidic) 3.17 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 0 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 0 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 0.87 m3·mol-1 Chemaxon Polarizability 0.44 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Drug created at November 30, 2015 19:10 / Updated at June 12, 2020 16:52