Technetium Tc-99m ciprofloxacin

Identification

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Name
Technetium Tc-99m ciprofloxacin
Accession Number
DB05488
Type
Small Molecule
Groups
Investigational
Description

99mTc-Ciprofloxacin is a new formulation of ciprofloxacin (INFECTON), being investigated as a radioimaging agent for the potential diagnosis of infection, including fever of unknown origin, osteomyelitis, wound infection, abdominal abscess, pneumonia, appendicitis and tuberculosis. INFECTON combines the widely used antibiotic, ciprofloxacin, with Technetium ((99m)Tc), the most commonly used radioisotope in nuclear medical imaging There is currently controversy around the drug's ability to discriminate between sterile inflammation and bacterial versus nonbacterial infections.

Synonyms
  • 99mTc-ciprofloxacin
  • Infecton
  • Technetium (99mTc) ciprofloxacin
  • Technetium Tc 99m ciprofloxacin
Categories
UNII
Not Available
CAS number
374107-43-4
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Investigated for use/treatment in infectious and parasitic disease (unspecified).

Pharmacodynamics

This radiopharmaceutical diagnostic imaging agent is being investigated for its ability to uniquely detect and determine the location of bacterial infection in patients with difficult-to-diagnose signs and symptoms. This may be of use with the potential diagnosis of infection, including fever of unknown origin, osteomyelitis, wound infection, abdominal abscess, pneumonia, appendicitis and tuberculosis.

Mechanism of action

Ciprofloxacin is a fluoroquinolone antibiotic. The mechanism of action of these fluoroquinolones is not fully understood, but it has been postulated that the interaction of ciprofloxacin with bacterial DNA gyrase (a type II topoisomerase) prevents DNA uncoiling and subsequent DNA synthesis within bacteria. Ciprofloxacin demonstrates a significant antibiotic effect for both gram-negative and gram-positive bacteria in either stationary or growth phases of bacterial replication. However, the addition of the 99mTc atom likely affects the interaction of the ciprofloxacin molecule with the enzyme.

TargetActionsOrganism
UDNA gyrase subunit BNot AvailableEscherichia coli (strain K12)
UDNA topoisomerase 2-betaNot AvailableHumans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
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.
DrugInteraction
(R)-warfarinThe therapeutic efficacy of (R)-warfarin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
(S)-WarfarinThe therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
3-isobutyl-1-methyl-7H-xanthineThe metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Technetium Tc-99m ciprofloxacin.
4-hydroxycoumarinThe therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Technetium Tc-99m ciprofloxacin.
7-DeazaguanineThe metabolism of 7-Deazaguanine can be decreased when combined with Technetium Tc-99m ciprofloxacin.
7,9-DimethylguanineThe metabolism of 7,9-Dimethylguanine can be decreased when combined with Technetium Tc-99m ciprofloxacin.
8-azaguanineThe metabolism of 8-azaguanine can be decreased when combined with Technetium Tc-99m ciprofloxacin.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be decreased when combined with Technetium Tc-99m ciprofloxacin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
  1. Choe YM, Choe W, Lee KY, Ahn SI, Kim K, Cho YU, Choi SK, Hur YS, Kim SJ, Hong KC, Shin SH, Kim KR, Woo ZH: Tc-99m ciprofloxacin imaging in acute cholecystitis. World J Gastroenterol. 2007 Jun 21;13(23):3249-52. [PubMed:17589906]
  2. Markou P, Spyridonidis T: [The role of 99mTc-ciprofloxacin scan in infection imaging]. Hell J Nucl Med. 2005 May-Aug;8(2):74-80. [PubMed:16142247]
  3. Tossing G: 99mTc-ciprofloxacin DRAXIMAGE. IDrugs. 2004 Apr;7(4):374-9. [PubMed:15057643]
External Links
PubChem Substance
175427018

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Escherichia coli (strain K12)
Pharmacological action
Unknown
General Function
Magnesium ion binding
Specific Function
DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, inc...
Gene Name
gyrB
Uniprot ID
P0AES6
Uniprot Name
DNA gyrase subunit B
Molecular Weight
89949.195 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein kinase c binding
Specific Function
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks.
Gene Name
TOP2B
Uniprot ID
Q02880
Uniprot Name
DNA topoisomerase 2-beta
Molecular Weight
183265.825 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Batty KT, Davis TM, Ilett KF, Dusci LJ, Langton SR: The effect of ciprofloxacin on theophylline pharmacokinetics in healthy subjects. Br J Clin Pharmacol. 1995 Mar;39(3):305-11. [PubMed:7619673]
  2. Flockhart Table of Drug Interactions [Link]
  3. Drug Interactions & Labeling - FDA [Link]

Drug created on November 18, 2007 11:25 / Updated on January 02, 2020 05:37