ANTIMICROBIAL CHEMOTHERAPY Flashcards
What are the four main causes of death (disease ONLY)?
- AIDS: viral infection
- TB: bacterial infection
- Malaria: protozoal infection
- Cancer: uncontrolled cell proliferation
What is the aim of selective toxicity and explain how this affects treating microbes?
- Selective Toxicity - toxic to microbe but not to the host cell
- Bacteria - different cell structures from humans (cell walls) = easy to treat
- Protozoa are eukaryotic = similar cell structures = hard to treat
- Virus hijack cells = and become similar to humans = hardest to treat (and cancers too)
What the causative agent of Syphilis?
Treponema pallidum (spirochaete bacterium)
What happens when Syphilis is left untreated?
Damages brain, heart and nervous system and is eventually fatal
What was the FIRST treatment for Syphilis and who created it?
- Salvarsan (modification of Atoxyl - which cause blindness)
- Paul Ehrlich
- Salvarsan was supposed to cure trypanosomiasis (sleeping sickness)
What was the mechanism of action of Salvarsan?
- Salvarsan (prodrug) → oxophenarsine (oxidised slowly)
- Oxophenarsine reacts with thiol (R-S-H) groups in proteins, causing denaturation.
- thiol containing amino acids = methionine and cysteine
Why was neosalvarsan used instead of salvarsan in the treatment of syphilis?
- Neosalvarsan is more water soluble and less toxic than salvarsan (but was replaced by penicillin)
What’s the structure of Neosalvarsan (neoarsphenamine)?
What did Ehrlich contribute to modern chemotherapy? (3)
- Screening techniques: he applied simple tests to large number of compounds
- Structure activity relationships: synthesis of chemical variants of an active compound to try to improve activity.
- Prodrugs
What drug is used to treat MRSA and multi-resistant strep pneumoniae?
Vancomycin