Notes on the Pharmacology of Bismuth, With Reference to Its Employment in the Therapy of Syphilis

Lomholt, Svend

doi:10.1136/sti.1.1.50

Cited by 2 publications

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“…At that time, bismuth was a component of a number of compounds employed for the treatment of syphilis. To determine their distribution within the body, de Hevesy introduced radioactive bismuth into the medications, inoculated them into the bloodstream of rabbits and followed their distribution and clearance from blood and tissues (Hevesy and Paneth, 1938;Lomholt, 1925). The concept of using a low-dose radioactive tracer to study a biochemical process in which it directly participates is still followed today in developing probes that target cell surface and intracellular receptors, enzymes and other molecules (Eckelman et al, 2008;Phelps, 2000;Rudin et al, 2005).…”

Section: Antimicrobial Drugs and Imaging Probesmentioning

confidence: 99%

Radiolabeled antiviral drugs and antibodies as virus-specific imaging probes

et al. 2010

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A number of small-molecule drugs inhibit viral replication by binding directly to virion structural proteins or to the active site of a viral enzyme, or are chemically modified by a viral enzyme before inhibiting a downstream process. Similarly, antibodies used to prevent or treat viral infections attach to epitopes on virions or on viral proteins expressed on the surface of infected cells. Such drugs and antibodies can therefore be thought of as probes for the detection of viral infections, suggesting that they might be used as radiolabeled tracers to visualize sites of viral replication by single-photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. A current example of this approach is the PET imaging of herpes simplex virus infections, in which the viral thymidine kinase phosphorylates radiolabeled thymidine analogues, trapping them within infected cells. One of many possible future applications might be the use of a radiolabeled hepatitis C protease inhibitor to image infection in animals or humans and provide a quantitative measure of viral burden. This article reviews the basic features of radionuclide imaging and the characteristics of ideal tracer molecules, and discusses how antiviral drugs and antibodies could be evaluated for their suitability as virus-specific imaging probes. The use of labeled drugs as low-dose tracers would provide an alternative application for compounds that have failed to advance to clinical use because of insufficient in vivo potency, an unsuitable pharmacokinetic profile or hepato- or nephrotoxicity.

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Section: Antimicrobial Drugs and Imaging Probesmentioning

confidence: 99%

Radiolabeled antiviral drugs and antibodies as virus-specific imaging probes

et al. 2010

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“…The internationalism of STIs is exemplified. Its author was Svend Lomholt of the Finsen Institute in Copenhagen 1. He wrote about the practical use of bismuth following early reports of Sazerac and Levaditi from 1921 in the French medical press.…”

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Syphilis: bismuth and the criminalisation of homosexuality

Waugh¹

2017

Sex Transm Infect

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Notes on the Pharmacology of Bismuth, With Reference to Its Employment in the Therapy of Syphilis

Cited by 2 publications

References 0 publications

Radiolabeled antiviral drugs and antibodies as virus-specific imaging probes

Radiolabeled antiviral drugs and antibodies as virus-specific imaging probes

Syphilis: bismuth and the criminalisation of homosexuality

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