PED1003/L23 Selective Toxicity & Antibiotics Flashcards

1
Q

How do bacteriostatic drugs affect the number of total and viable cells?

A

Stops changes in both

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2
Q

Why has the number of new antibiotics reaching the market dropped dramatically in the last 10 years? (3)

A

Resistance reduces effective life of a product
Too little profit
Government restrictions
Lack of new biological targets

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3
Q

How do bacteriolytic drugs affect the number of total and viable cells?

A

Decrease both

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4
Q

How do bacteriocidal drugs affect the number of total and viable cells?

A

Drop in viable cells
Total cells remain the same

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5
Q

Give 3 common bacterial targets.

A

Cell membrane
Cell wall
Protein synthesis
RNA polymerase
DNA synthesis
Folate metabolism

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6
Q

Describe the structure of a B-lactam ring.

A

Cyclic amide with heteroatomic ring structure consisting of 3 carbon atoms and 1 nitrogen atom

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7
Q

Describe early penicillins. (3)

A

Acid labile
Not well-absorbed via oral route
Parenteral route - slow IV, high availability
Narrow spectrum of activity - Gram +ves and few Gram -ves

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8
Q

What did the amino group in penicillin facilitate?

A

Penetration of outer membrane of Gram -ve bacteria

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9
Q

How do B-lactam antibiotics work? (3)

A

Inhibit transpeptidases responsible for creating cross-linkage of peptidoglycan cell wall
Bacteria swell and rupture
Only effective against multiplying organisms

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10
Q

Which 2 amino acids are joined in a transpeptidation reaction?

A

Lys - Gly

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11
Q

Describe the absorption of penicillin. (2)

A

Varies orally
Delayed release preparations available

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12
Q

Describe the distribution of penicillin. (3)

A

Widely distributed throughout
Concentrations in tissues and body fluids vary
Do not normally enter CSF

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13
Q

What is the half-life of penicillin?

A

30-80 mins

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14
Q

Describe the excretion of penicillin. (3)

A

Mainly through kidney with 90% excreted by tubular secretion
Clearance reduced in neonates
Reduce excretion rate by use of probenecid which inhibits tubular secretion

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15
Q

Give 2 adverse reactions to penicillin.

A

Hypersensitivity
GIT disturbance
Haemostatic effect

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16
Q

Which 2 enzymes are involved in folate biosynthesis?

A

Dihydropteroate synthetase
Dihydrofolate reductase

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17
Q

Give the intermediates in folate biosynthesis. (5)

A

pABA
Folate
Tetrahydrofolate
Synthesis of thymidylate
DNA

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18
Q

Describe how sulphonamide works. (2)

A

Similar structure to pABA
Competitive inhibitor for enzyme dihydropteroate synthetase

19
Q

What enzyme is inhibited by trimethoprim?

A

Dihydrofolate reductase

20
Q

Why is suphonamide selective? (2)

A

Bacteria must synthesise folic acid
Humans can take it from environment

21
Q

Describe the absorption of sulphonamides.

A

80-100% given orally absorbed from stomach and intestines

22
Q

Describe the distribution of sulphonamides.

A

Widely distributed including CNS

23
Q

Describe the metabolism of sulphonamides.

A

Occurs in liver by N-acetylation

24
Q

Describe the excretion of sulphonamides.

A

In urine - 30 mins

25
Q

Give an adverse reaction to sulphonamides.

A

Photosensitivity
Stevens-Johnson syndrome
Hemopoietic disturbances

26
Q

How do fluoroquinolones work? (2)

A

Target DNA replication via type II topoisomerases
Effective against Gram +ve and -ves

27
Q

Which enzymes are inhibited in Gram +ve and -ve bacteria by fluoroquinolones?

A

+ve - DNA-gyrase
-ve - DNA topoisomerase IV

28
Q

Describe the absorption of quinolones.

A

Oral admin most effective

29
Q

Describe the distribution of quinolones.

A

Very well absorbed in GI tract

30
Q

Describe the metabolism of quinolones.

A

Potent inhibitor of CYP1A2 -> drug-drug interactions

31
Q

Describe the excretion of quinolones.

A

Mainly excreted in tubular secretion

32
Q

Give an adverse reaction to quinolones.

A

Hypersensitivity
GIT disturbance

33
Q

How do macrolides work? (4)

A

Target bacterial ribosomes and protein synthesis
Block translocation
Bind to site near RNA exit terminal
Causes peptidyl-transferase RNA drop-off

34
Q

Describe the absorption of macrolides.

A

Oral admin protected tablets to avoid interaction by gastric juice

35
Q

Describe the distribution of macrolides. (3)

A

Diffuses readily into most tissues
Does not cross BBB
Crosses placenta

36
Q

Describe the metabolism of macrolides. (2)

A

Metabolised by demethylation (CYP3A4)
Can potentiate effects of other drugs

37
Q

Describe the secretion of macrolides.

A

Excreted in bile

38
Q

Give an adverse reaction of macrolides.

A

Cholestatic hepatitis (prolonged use)
GIT disturbances at large doses
Transitory auditory impairment
Hypersensitivity reactions

39
Q

How do tetracyclines work? (4)

A

Interrupt elongation phase of protein synthesis
Several binding sites of 30S RNA subunit
Sterically inhibits transfer RNA binding
Unbinds, rebinds, futile loop

40
Q

Describe the absorption of tetracyclines. (2)

A

Greater in fasting state
Inhibited by concurrent ingestion of dairy products, metal ions and certain antacids

41
Q

Describe the distribution of tetracyclines.

A

Widely distributed entering most tissues

42
Q

Describe the metabolism of tetracyclines.

A

Excreted via bile and in kidneys via glomerular filtration

43
Q

Describe the excretion of tetracyclines.

A

6-18 hour half-life