Antibacterial Agents 3: Protein Synthesis Inhibitors Flashcards

1
Q

Macrolides Drug Types

A

Erythromycin, clathromycin, azithromycin

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2
Q

Macrolides MoA

A

Binding to 50S ribosome, blocking translocation of peptidyle RNA

Passive Diffusion

Bacteriostatic

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3
Q

Macrolide

Erythromycin

Absorption

A

Absorption varies depending on salt form

Estolate appears more bioavailable in children than ethyle succinate

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4
Q

Macrolides

Clarithromycin

Absorption

A

Can be taken without regards to food

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5
Q

Macrolides

Azithromycin

Absorption

A

Taken without food

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6
Q

Macrolides

Distribution

A

Wide distribution
except brain and CSF

Traverses placenta

Azi/Clathro= High tissue penentrance, low plasma levels

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7
Q

Macrolides

Erithromycin

Metabolism/Excretion

A

Liver and excreted in bile

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8
Q

Macrolides

Clarithromycin

Metabolism/excretion

A

Metabolized to active so renal excretion

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9
Q

Macrolides

Azithromycin

MEtabolism/Excretion

A

Not metabolized, high tissue penetrance

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10
Q

Gram Positive Cocci

Streptococci and pneumococci

Macrolide Atbx uses

A

All

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11
Q

Gram Negative Cocci

Moraxella catarrhalis

Macrolide Atbx use

A

All

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12
Q

Bordetella pertussis

Macrolide Atbx uses

A

All

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13
Q

Heamophillus influenzae

Macrolide Atbx use

A

Azithromycin, Clathrithromycin

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14
Q

Helicobacter pylori

Marolide Atbx Use

A

Clarithromycin with PPI or H2 antagonist

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15
Q

Legionella

Macrolide atbx uses

A

Azithromycin

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16
Q

Mycobacterium avium

Macrolide atbx use

A

Clarithromycin and Azithromycin

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17
Q

Chlamydia

Macrolide atbx use

A

Azithromycin

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18
Q

Mycoplasma pneumoniae

Macrolide atbx use

A

All

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19
Q

Macrolides

Adverse Efects

A

Direct stimulation of gut motility, increasing activity
with erithro

Hepatotoxic

Prolongs QT interval

E and C inhibits p450

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20
Q

Telithromycin

A

Erithromycin derivative

Use only for community-acquired pneumonia that is atbx resistant

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21
Q

Tetracyclines

Drugs

A

Tetracycline, Doxycycline, Minocycline

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22
Q

Tetracyclines

MoA

A

Bacteriostatic

Reversible binding to bacterial 30S ribo subunit

Resistance: Change influx, block binding

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23
Q

Tetracyclines

Absorption

A

Best without food

Milk, Al3+, Ca2+, Mg2+, and Fe2+ salts impair absorption

Doxy best absorped

24
Q

Tetracycline

Destribution

A

Penetrant into most tissues, including fetus

variable protein binding

25
Q

Tetracyclines

Metabolism/Excretion

A

Concentrated in liver, secreted by bile (care liver function pts)

Most into urine except Docy and Mino

Breast milk excretion

26
Q

S. aureus

Tetracycline use

A

Doxy and tigecycline

27
Q

Moraxella Catarrhalis

Tetracycline Use

A

Doxy

28
Q

B. anthracis

Teracycline use

A

Doxy

29
Q

H. influenzae

Tetracycline use

A

Doxy

30
Q

H. pylori

Tetracycline use

A

Tetracycline

31
Q

Vibrio cholera

Tetracycline use

A

Doxy

32
Q

Propionobacterium acnes

Tetracycline use

A

Minocycline, doxycycline

33
Q

Chlamydia

Tetracycline use

A

Doxy

34
Q

Mycoplasma pneumoniae

Tetracycline use

A

Doxy

35
Q

Richettsia

Tetracycline Use

A

Doxy

36
Q

Borrelia burgdorferi

Tetracycline use

A

Doxy

37
Q

Tetracyclines

Adverse reactions

A

Avoid use in latter half of pregnancy and <8yo

Contraindicaed with antacids/iron supplments as it decreases bioavailablity

38
Q

Clindamycin

MoA

A

Inhibits protein synthesis by binding 50S ribosome

Bacteriostatic, cidal at high doses

39
Q

Clinda

Pharmacokinetics

A

Oral ok

Penetrates well, especially bone, not into CSF

Excreted in breast milk, metab’d by liver

40
Q

Clindamycin

Clinical use

A

Severe anaerobic infections

Streptococci, MSSA, MRSA, C. perfringens, B. fragilis

41
Q

Clinda

Adverse reactions

A

Can cause pseudomembranous colitis

42
Q

Aminoglycosides

Drugs

A

Streptomycin, tobramycin, gentamycin, amikacin, kanamycin, neomycin

43
Q

Aminoglycosides

MoA

A

Bacterio static, cidal at high concentration

Not effective against anaerobes

Combines with 30S ribosome

44
Q

Aminoglycosides

Absorption

A

Not Oral., best intramuscular

45
Q

Aminoglycosides

Distribution

A

Lmited to extracellular fluid

Excluded from CNS (unless inflamed) and eye

Accumulates in renal cortex and inner ear

46
Q

Aminoglycosides

Metabolism/excretion

A

Not metabolized, renal excretion

Post-antibiotic effect

47
Q

Aminoglycoside
Spectrum

Gram negative bacilli

A

Gentamicin, tobramycin, amikacin

P. aeruginosa, , enterobacter, e. coli,

Can use neomycin topically or for bowel sterilization

48
Q

Mycobacterium tuberculosis

Aminoglycosides

A

Streptomycin

49
Q

Enterococci

Aminoglycoide uses

A

Gentamycin

50
Q

Aminoglycosides

Toxicity

A

Very toxic

Eighth nerve damage

51
Q

Chloramphenicol

MoA

A

Binds to 50S ribosome

Bacteriostatic

Also inhibits mitochondrial 70S

52
Q

Cloramphenicol

Distrubution

A

Can readily enter CNS and CSF

53
Q

Chloramphenicols

Metab and excre

A

In fetus and neonate, unable to conjugate the drug, so toxic

Excreted in breastmilk

54
Q

Chloramphenicols

Adverse effects

A

Bone marrow toxixity (mitochondria)

Gray baby syndrome

55
Q

Linezolid

MoA

A

Binds to 50S but on a different site so no cross resistance

56
Q

Linezolids

Pharmacokinetics

A

Can be oral or IV

Readily distributed to tissue

Primarily metabolixed by nonenzymatic oxidation

57
Q

Linezolid

Adverse reactions

A

Possible thrombocytopenia

Inhibits MAO (Monoamine oxidase)