ANTIMICROBIAL CHEMOTHERAPY Flashcards

1
Q

What are the four main causes of death (disease ONLY)?

A
  1. AIDS: viral infection
  2. TB: bacterial infection
  3. Malaria: protozoal infection
  4. Cancer: uncontrolled cell proliferation
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2
Q

What is the aim of selective toxicity and explain how this affects treating microbes?

A
  • 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)
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3
Q

What the causative agent of Syphilis?

A

Treponema pallidum (spirochaete bacterium)

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4
Q

What happens when Syphilis is left untreated?

A

Damages brain, heart and nervous system and is eventually fatal

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5
Q

What was the FIRST treatment for Syphilis and who created it?

A
  • Salvarsan (modification of Atoxyl - which cause blindness)
  • Paul Ehrlich
    • Salvarsan was supposed to cure trypanosomiasis (sleeping sickness)
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6
Q

What was the mechanism of action of Salvarsan?

A
  1. Salvarsan (prodrug) → oxophenarsine (oxidised slowly)
  2. Oxophenarsine reacts with thiol (R-S-H) groups in proteins, causing denaturation.
  • thiol containing amino acids = methionine and cysteine
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7
Q

Why was neosalvarsan used instead of salvarsan in the treatment of syphilis?

A
  • Neosalvarsan is more water soluble and less toxic than salvarsan (but was replaced by penicillin)
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8
Q

What’s the structure of Neosalvarsan (neoarsphenamine)?

A
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9
Q

What did Ehrlich contribute to modern chemotherapy? (3)

A
  • 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
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10
Q

What drug is used to treat MRSA and multi-resistant strep pneumoniae?

A

Vancomycin

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