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Chemotherapy > Bacteria IV > Flashcards

Bacteria IV Flashcards

1
Q

What do both these drugs do?

A

Interfere with the tetrahydrofolate pathway - an important precursor of DNA

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2
Q

What are sulphonamides?

A

Competitive inhibitors and alternate substrates for DHPS

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3
Q

Why are sulphonamides selective?

A

We do not perform this reaction

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4
Q

What does trimethoprim target?

A

Dihydrofolate reductase

Produces THF from DHF

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5
Q

What are the clinical applications of sulphonamides and trimethoprim?

A

Respiratory tract infections
Urinary tract infections
Digestive tract infections
Combination can be used for treatment/prophylaxis of pneumonia in HIV

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6
Q

How is sulphonamides administered?

A

Orally (long half lives)

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7
Q

How is trimethoprim administered?

A

Oral/IV

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8
Q

Which drug can cause Steven johnsons syndrome?

A

Sulphonamides

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9
Q

Which drugs target DNA topoisomerase?

A

Quinolones & fluoroquinolones

DNA gyrase and topoisomerase IV

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10
Q

What does gyrase do?

A

Negative supercoils

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11
Q

What does topoisomerase IV do?

A

Decatenating activity required for release of daughter chromosome produced during replication
Both enzymes catalyse ATP-dependent DNA double strand breakage-rejoining reactions

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12
Q

What is the primary target in gram negative bacteria?

A

Gyrase with it being reversed in gram-positive bacteria

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13
Q

What major side effect of quinolones is there?

A

Arthropathy - erosion of cartilage in joints but only demonstrated in young animals

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14
Q

What is the key part of the nitro heterocyclic drugs?

A

The core but only differs at the side group - the key part of the molecule is the nitro group

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15
Q

What does metronidazole do?

A

Potent bactericidal action against most obligate anaerobic bacteria
Active against some anaerobic facultative under anaerobic conditions

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16
Q

What happens to the nitro group in metronidazole?

A

Nitro group of drug reduced by low redox potential nitroreducatases

17
Q

What does metronidazole treat?

A

Intracellular abdominal infection, C.difficile, non-venereal genial infections, etc.

18
Q

How are nitrofurans activated?

A

Reduction
Not so dependent on anaerobic conditions
Oral only

19
Q

What does nitrofurans treat?

A

Urinary retract infections unable to tolerate beta lactams, sulphonamides and trimethoprim

20
Q

What does nitrofurans do under anaerobic conditions?

A

Produces double strand DNA breaks in human cells

21
Q

What drugs target transcription?

A

Rifamycin - targets RNA polymerase and binds the beta subunit of prokaryotic RNAP
Interferes with the initiation of transcription through steric hindrance

22
Q

Does Rifamycin resistance arise quickly?

A

Yes - by point mutation. Only used in combinations

23
Q

What does Rifamycin treat?

A

Tuberculosis, leprosy, penicillin resistance, s.pneumoniae and s.aureus

24
Q

What drugs target nucleotide metabolism?

A

Sulphonamides and trimethoprim

25
Q

What are the three types of nitro heterocyclic drugs?

A

Nitroimidazoles - metronidazole & tinidazole
Nitrofurans - nitrofurantoin
Nitrothiazoles

26
Q

What is the pathway for metronidazole?

A

Entry of drug into the cell
Reductive activation
Toxic effects of reduced intermediate products
Formation of inactive end product

27
Q

What are the toxic effects of metronidazole?

A

DNA damage
Oxidation
Strand breaks
Helix destabilisation

28
Q

What are the formulations for metronidazole?

A

Oral, IV, topical gel/cream

29
Q

What does metronidazole treat?

A

Anaerobic bacterial infections & protozoan infections

30
Q

What does metronidazole react with?

A

Alcohol - accumulation of acetaldehyde

31
Q

Can nitrofurans be used for recurrent urinary tract infections?

A

Yes

Chemotherapy (18 decks)

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