Identification

Generic Name
Technetium Tc-99m ciprofloxacin
DrugBank Accession Number
DB05488
Background

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.

Type
Small Molecule
Groups
Investigational
Synonyms
  • 99mTc-ciprofloxacin
  • Infecton
  • Technetium (99mTc) ciprofloxacin
  • Technetium Tc 99m ciprofloxacin

Pharmacology

Indication

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

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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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

Adverse Effects
Adverseeffects
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Toxicity

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
AcarboseThe therapeutic efficacy of Acarbose can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
AceclofenacAceclofenac may increase the neuroexcitatory activities of Technetium Tc-99m ciprofloxacin.
AcemetacinAcemetacin may increase the neuroexcitatory activities of Technetium Tc-99m ciprofloxacin.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Technetium Tc-99m ciprofloxacin.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Acetylsalicylic acidAcetylsalicylic acid may increase the neuroexcitatory activities of Technetium Tc-99m ciprofloxacin.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Technetium Tc-99m ciprofloxacin.
AcyclovirThe metabolism of Acyclovir can be decreased when combined with Technetium Tc-99m ciprofloxacin.
AdenosineThe risk or severity of QTc prolongation can be increased when Adenosine is combined with Technetium Tc-99m ciprofloxacin.
Interactions
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Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
374107-43-4
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
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. [Article]
  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. [Article]
  3. Tossing G: 99mTc-ciprofloxacin DRAXIMAGE. IDrugs. 2004 Apr;7(4):374-9. [Article]
PubChem Substance
175427018

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

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

Targets

Drugtargets2
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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. [Article]

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. [Article]
  2. Flockhart Table of Drug Interactions [Link]
  3. Drug Interactions & Labeling - FDA [Link]

Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52