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Pharmacology of Infection & Immunity > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

Name the Aminoglycosides.

A

Gentamicin, Streptomycin

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2
Q

How do the aminoglycosides work?

A

Bind IRREVERSIBLY to the 16S rRNA in the 30S subunit of the ribsome leading to misreading of the codons along the mRNA. Also interferes with the translocation of tRNA from the A-site to the P-site.

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3
Q

What are aminoglycosides used for?

A

Septicaemia, Nosocomial RTI, complicated UTIs

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4
Q

What are the side effects of aminoglycosides?

A

Nephrotoxicity, Ototoxicity

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5
Q

What is the mode of resistance against aminoglycosides?

A

Enzymatic inactivation (Acetylation, phosphorylation, Adenylation)

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6
Q

How do the tetracyclines work?

A

Bind REVERSIBLY to the A-site on the 16S rRNA site of the 30S subunit of the ribosome. This inhibits the binding of tRNA to the A-site, which in turn inhibits protein synthesis.

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7
Q

What are tetracyclines used to treat?

A

Acne, RTI, Chlamydia, SSTIs, Mycoplasma, Periodontal disease.

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8
Q

What are the side effects associated with tetracyclines?

A

GIT and GIT superinfections, Deposition in bones and teeth (yellow band), Photosensitivity.

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9
Q

What are the names of the macrolides?

A

Erythromycin, Clarithromycin

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10
Q

How do the macrolides work?

A

Bind to the P-site on the 23S rRNA in the 50S subunit of the ribosome. Prevents translocation of the tRNA from the A-site to the P-site. Inhibits peptide bond formation.

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11
Q

What is the main mode of resistance against tetracyclines?

A

Efflux pumps

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12
Q

How do lincosamides work?

A

Similar to the of the macrolides - Bind to the P-site on the 23S rRNA in the 50S subunit of the ribosome. Prevents translocation of the tRNA from the A-site to the P-site. Inhibits peptide bond formation.

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13
Q

What do the lincosamides treat?

A

Staphylococcal Bone & Joint Infections, RTIs, peritonitis, Septicaemia

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14
Q

Side effect of Lincosamides?

A

C. Difficule Infection

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15
Q

How does Linezolid work?

A

Similar to macrolides - Bind to the P-site on the 23S rRNA in the 50S subunit of the ribosome. Prevents translocation of the tRNA from the A-site to the P-site. Inhibits peptide bond formation.

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16
Q

What is Linezolid used for?

A

Last resort antibiotic. Can be used against MRSA

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17
Q

How does Fusidic Acid work?

A

Prevents the turnover of elongation factor (EFG) of the ribosome. Prevents energy needed for translocation

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18
Q

What is fusidic acid used for?

A

Narrow spectrum staphyococcal infections - used topically for skin and eye infections.

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19
Q

How does chloramphenicol work?

A

Inhibits peptidyl transferase in the 23S rRNA region in the 50S subunit, inhibiting peptide bond formation.

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20
Q

How do the B-lactams work?

A

They bind to Penicillin Binding Proteins (PBPs). This prevents cross linking. They get incorporated into the side chain.
They also stimulate autolysins which break down the cell wall.

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21
Q

What are B-Lactam side effects?

A

Hypersensitivity, Neurotoxicity, Renal Failure, Diarrhoea, Psuedomembranous colitis, C. Difficule infections.

22
Q

What is Benzylpenicillin (Pen-G) used for?

A

Throat infections (nosocomial), endocarditis, and meningitis.

23
Q

What is amoxicillin used for?

A

RTIs, Oral Infections, Otitis Media, Sinusitis

24
Q

Why are cephalosporins limited in their use?

A

Risk of C. Difficule infections

25
Q

What are second generation Cephs used for?

A

Severe infections, and prophylaxis of infections after surgery

26
Q

What are 3rd Gen Cephs used for?

A

Meningitis, Infantile sepsis, gonorrhoea, nosocomial infections

27
Q

What are carbapenems used for? (imipenem, meropenem)

A

Septicaemia, HAP, Complicated UTIs and SSTIs.

28
Q

What are the names of the glycopeptides?

A

Vancomycin, Teicoplanin

29
Q

How do the glycopeptides work?

A

Binds to D-Ala–D-Ala and prevents cross linking

30
Q

What are the glycopeptides used for?

A

Systemic Infections caused by B-lactam resistant organisms. Vancomycin can be used to treat C.Difficule when taken orally (because it does’t get absorbed)

31
Q

What are the side effects of glycopeptides?

A

Renal toxicity, Ototoxicity, Blood disorders, Anaphylactoid reactions

32
Q

How does Cycloserine work?

A

Inhibits enzymes involved in the peptidoglycan synthesis - alanine racemase & D-Ala-D-Ala ligaase

33
Q

What are the side effects of cycloserine?

A

CNS effects, liver damage, rashes

34
Q

How do polymixins work?

A

They disrupt the membrane by binding to the Lipid A component of LPS causing disruption of the membrane so cytoplasmic contents leak out.

35
Q

What are polymixins used for?

A

Gram Negative bacterial infections (Gram positive bacteria do not have LPS)

36
Q

How does daptomycin work?

A

Aggregates at the membrane of the cell and causes a pore to form, leading to the leakage of cytosolic contents.

37
Q

How do sulfonamides work?

A

Inhibit dihydropterate synthase.

38
Q

How does trimethoprim work?

A

Inihibits dihydrofolate reductase

39
Q

What is trimethoprim used to treat?

A

Acne and UTIs

40
Q

What is the mechanism of action for Fluoroquinolones?

A

Inhibit DNA gyrase and Topoisomerase IV

41
Q

What are the fluoroquinolones used for?

A

Chlamydia, Mycobaceteria, RTI, UTI, GIT, Systemic G-ve infections

42
Q

What are the side effects of the flurooquinolones?

A

GIT,

Interacts with CYP450, therefore interactions with loads of drugs.

43
Q

What is Rifampicin’s mechanism of action?

A

Inhibits DNA polymerase.

44
Q

What is Rifampicin used to treat?

A

Tuberculosis (1st line in RIPE), Staphylococcal bone and joint infections.

45
Q

What are the side effects of Rifampicin?

A

Hepatotoxicity, Fever, Rash, Hypersensitivity, Orange-Red colour secretions.

46
Q

How do nitroimidazoles work?

A

Causes disruption of the DNA

47
Q

What are Nitroimidazoles used for?

A

C. Difficule infections, Some Genital tract infections, SSTIs where anaerobes are suspected, Abdominal and dental infections.

48
Q

What are the side effects of metronidazole?

A

GIT, Candida superinfections, CNS: peripheral neuropathy, dizziness, confusion. Hypersensitivity, Genito-urinary.

49
Q

What are the 6 opportunistic bacteria?

A 
Enterococcus faecium 
Staphylococcus aureus
Klebsiella pneumonia 
Acinetobacter buamanii
Pseudomonas aeruginosa
Enterobacter
50
Q

Highlight the mechanisms of resistance against B-lactam drugs

A

B-lactamases: Limited spectrum - TEM-1 &2, Extended spectrum: CTX-M, NDM-1 (mainly found in E Coli)

Altered Target site: MRSA - PBP2 –> PBP2a

Altered Uptake: decrease in number and size of pores - only found in G-ve bacteria

51
Q

What is the mode of resistance to Vancomycin?

A

Altered target site: D-Ala – D-Ala mutates to D-Ala – D-Lactate. Means the Vancomycin cannot bind as tighly (x1000 less affinity) due to one less hydrogen bond

52
Q

What is the mode of resistance for Nucleic Acid Synthesis inhibitors?

A

Altered target site: Enzymes are modified to have less affinity for the drug.

Pharmacology of Infection & Immunity (1 decks)

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