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Chemotherapeutic Agents > Nucleic Synthesis II > Flashcards

Nucleic Synthesis II Flashcards

1
Q

What is the concept of anti-metabolites?

A

Chemotherapy based on synthesis of small molecules that are functional analogues of cell metabolites, that can inhibit metabolic pathways

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2
Q

What is essential for folic acid synthesis in bacteria?

A

PABA

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3
Q

What is folic acid required for?

A

Synthesis of precursors of DNA and RNA

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4
Q

What is Sulphonamides spectrum of activity?

A

Bacteriostatic against G+ve and G-ve bacteria
Bactericidal at higher concentrations
Poor activity against anaerobes

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5
Q

What chemical group of Sulphonamide gets modified?

A

The R group - increases activity and modifies some pharmacological properties

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6
Q

What is an example of a Sulphonamide?

A

Prontosil and thiazides

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7
Q

What are sulphonamides mechanism of action?

A

Competitively inhibit PABA binding with dihydropteroate synthase - prevents formation of DHF
Formation of folate gets inhibited
Stops further replication

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8
Q

How are sulphonamides administered?

A

oral
I.V.
Topical

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9
Q

How are sulphonamides absorbed?

A

Across GIT bar sulfasalazine

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10
Q

How are sulphonamides distributed?

A

Widely distributed

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11
Q

How are sulphonamides metabolised?

A

Acetylated and conjugated in liver

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12
Q

How are sulphonamides excreted?

A

Glomerular filtration and secretion in kidney
Eliminated in breast milk

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13
Q

What are the clinical uses of sulphonamides?

A

UTIs
Burns
Malaria

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14
Q

What are the s/e of sulphonamides?

A

GIT distress
Nephrotoxicity
Hypersensitivity reactions
Haematological toxicity
Hepatotoxicty
Kerniceturus

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15
Q

What are some drug interactions of Sulphonamides?

A

Inhibition of CYP2C9 - reduced clearance of warfarin

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16
Q

How does resistance to Sulphonamides occur?

A

Mutation or transfer of resistance by plasmids

17
Q

What is Co-trimoxazole?

A

Fixed dose combination of sulfamethoxazole and trimethoprim

18
Q

What is Co[trimoxazole’s mechanism of action?

A

Blocks folate metabolism
Bactericidal

19
Q

How is Co-trimoxazole administered?

A

Oral
I.V.

20
Q

How is Co-trimoxazole distributed?

A

Widely distributed

21
Q

How is Co-trimoxazole metabolised?

A

Liver

22
Q

How is Co-trimoxazole excreted?

A

urine

23
Q

What are Co-trimoxazole clinical uses?

A

Active against many sulphonamide resistant strains
Pneumocystis carrini

Chemotherapeutic Agents (14 decks)

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