Antibiotics Flashcards

1
Q

What are the antibiotics?

A

They are chemical produced by a microorganism that kill or inhibit the growth of another microorganisms.

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2
Q

What is the antimicrobial agent?

A

Chemical that killd or inhibits the growth of microorganisms.

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3
Q

Source of antibiotics:

A

Chemical sources and naural sources (~80%).

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4
Q

ABs from Chemical sources:

A

Sufonamides, quinolones, Trimethoprim, oxazolidinones.

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5
Q

AbBs from natural source:

A

Penicillins, cephalosporins, carbapenems, Aminoglycosides, Tetracyclines, macrolides, Glycopeptides, chloramphenicol.

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6
Q

Beta-lactams target:

A

PBPs in cell wall

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7
Q

Mactolides target :

A

rRNA

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8
Q

Aminoglycosides target:

A

Protein synthesis

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9
Q

Rifamycins target

A

RNA polymerase

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10
Q

Trimethroprim target:

A

Dihydrofolate reductase

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11
Q

Fluoroquinolones target:

A

DNA gyrase, topoisomerase IV

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12
Q

Glycopeptides target:

A

Cell wall peptidoglycan synthesis

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13
Q

Total targets for antimicrobial activity:

A

10-15 targets

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14
Q

Bacteria have approx …. essential genes:

A

200

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15
Q

Antibiotics are classified several ways:

A

Mechanism of action, mode of action and spectrum of activity.

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16
Q

Toxic metabolites for bacteria:

A

Metronidazole

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17
Q

Drugs act on cell wall:

A

Penicillins, cephalosporins, carbapemems, glycopeptides.

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18
Q

Drug acts on RNA polymerase :

A

Rifampin

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19
Q

Drug acts on DNA Gyrase:

A

Fluroquinolones

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20
Q

Drug acts on protein synthesis:

A

Nitrofurantoin

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21
Q

Drugs act on 50s ribosome

A

Macrolides

Lincosamides

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22
Q

Drugs act on 30s Ribosome

A

Aminoglycosides

Tetracyclines

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23
Q

Drugs act on folic acid pathway:

A

TMP/SMX

Dapsone sulfoxone

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24
Q

Drugs act on mycolic acid pathway

A

Isoniazide

Ethambutol

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25
Q

Pencillin and cephalosporins Mode of action

A

They bind and block peptidase involved in cross-linking the glycan molecules

26
Q

Mode of action of vancomycin

A

Hinders peptidoglycan elongation

27
Q

Cycloserine mode of action

A

It inhibits the formation of the basic peptidoglycan subunits

28
Q

Structure of penicillin:

A

Thiazolidine ring
Beta lactam ring
Variable side chain (R group)

29
Q

Semisynthetic penicillin

A

Ampicillin and carbenicillin

30
Q

R group in penicillin:

A

It is responsible for the activity of the drug

31
Q

Penicillin enters to the cell through ….. and bind to ….

A

Porins, PBP

32
Q

After penicillin binding to PBP:

A

PBP can no longer synthesize protein essential to integrity of cell wall

33
Q

Drug has similar structure to penicillin but enhanced stability:

A

Cephalosporins

34
Q

Cephalosporins Gen that not given orally and easy to be resistence:

A

1st gen (cefalotin and cefalexin)

35
Q

Cephalosporins gen that more G-ves and more stable against beta-lactamases:

A

2nd gen (cefuroxime and ceftoxin)

36
Q

Cephalosporins gen that have broad spectrum against G-ves, useful in hospital-acquired infections and can penetrate CNS:

A

3rd gen( cefotaxime and ceftazidime)

37
Q

Cephalosporins gen that have extended spectrum against G+ves and can pemetrate G-ve outer membrane:

A

4th gen (cefepime and cefepirome)

38
Q

Anti- pseudomonal, less susceptible to development of resistance and are referred to as anti-MRSA cephalosporins.

A

5th gen (ceftaroline and ceftobiprole)

39
Q

E.g of Macrolides :

A

Erythromycin, clarithromycin, azithromycin

40
Q

Macrolides coverage:

A

GP except Enterococcus.
GN: legionella, B. Pertussis
Atypical : chlamydophila and mycoplasma

41
Q

Mechanism of action of macrolides :

A

They bind to 50s ribosomal subunit inhibiting protein synthesis

42
Q

Why clarithromycin and azithromycin used rarely?

A

Due to Gi upset

43
Q

E.g of lincosamides:

A

Clindamycin, chloramphenicol and linezolid

44
Q

Lincosamide has broad spectrum:

A

Chloramphenicol

45
Q

Clindamycin coverages:

A

GP except Enterococcus
Most community-acquired MRSA
Anaerobes

46
Q

Chloramphenicol coverages:

A

GP, GN and anaerobes (broad spectrum.

47
Q

Linezolid coverages:

A

GP including VRE + MRSA

48
Q

Mechanism of action of clindamycin:

A

It inhibits peptide bond formation at 50s ribososme

49
Q

Mechanism of action of chloramphenicol:

A

It inhibits peptidyl transferase action of tRNA at 50s ribosome

50
Q

Mechanism of action of linezolid:

A

It binds to 50s ribosome and prevents functional 70s initiation conplex

51
Q

E.g of Aminoglycosides:

A

Gentamicin, tobramycin, amikacin

52
Q

Aminoglycosides coverage

A

GN aerobic bacilli

Include pseudomonas

53
Q

Mechanism of action of aminoglycosides

A

They bind 30s subunits of ribosome inhibiting protein synthesis

54
Q

Contraindication of aminoglycosides:

A

Pre-existing hearing loss and renal dysfunction

55
Q

AE of aminoglycosides:

A

Nephrotoxicity (reversible)
Ototoxicity (irreversible)
Most is vestibular toxicity

56
Q

Aminoglycosides indications:

A

GP infection

Used with b-lactam or vancomycin in eterococcal infection

57
Q

Tetracyclines used in:

A

(Atypical bacteria)

GP, syphilis, Chlamydophila, Rickettsia, mycoplasma

58
Q

Mechanism of action if tetracyclines:

A

Binds 30s subunit of ribosome inhibiting protein synthesis

59
Q

E.g of topoisomerase inhibitors:

A

Flouroquinolones
Rifampin
Metronidazole

60
Q

What is the quinolones?

A
Nalidixic acid (comletely synthetic)
A nitrogen atom within a heterocyclic structure
61
Q

Mechanism of action of Quinolones:

A

Inhibits DNA gyrase (unwinds supercoiled DNA helix prior to trsnscription + replication)

62
Q

Quinolones using

A

It active against most Gram-

And used in treatment of uncomplicated UTIs