Protein Synthesis Inhibitors Flashcards

1
Q

Macrolides MOA

A

Inhibition of protein synthesis, binds 50S ribosomal subunit, selective toxicity - no binding to mamillian ribosome. Bacteriostatic

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2
Q

Macrolide Examples

A

Erythromycin
Clarithromycin
Azithromycin

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3
Q

Macrolide distribution

A

Wide, except for CNS. Crosses placenta

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4
Q

Erythromycin Metabolism/excretion

A

Liver, excreted in bile. Avoid in liver disease.

Excreted in breast milk - check infants for thrush

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5
Q

Clarithromycin metabolism/excretion

A

Renally eliminated, may require adjustment

Excreted in breast milk - check infants for thrush

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6
Q

Macrolide uses, gram + cocci

A

alternative in penicillin allergic patients

Streptococci (phayngitis), pneumococci (pneumonia)

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7
Q

Macrolide uses, gram - cocci

A

Moraxella catarrhalis (otitis media, community acquired pneumonia)

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8
Q

Macrolide uses, gram - bacilli

A

H. influenzae –> upper respiratory infections, bronchitis

Azithromycin and Clarithromycin are the best

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9
Q

Macrolide uses, atypicals

A
Chlmydia (trachoma, community acquired pneumonia, urethritis) -- Azithromycin 
Mycoplasma pneumoniae (community-acquired pneumonia)
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10
Q

Azythromycin Metabolism

A

NOT metabolized, high tissue penetration

Excreted in breast milk, check infant for thrush

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11
Q

Macrolide drug interactions

A

Erythromycin and clarithromycin are inhibitors of cytochrome p450

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12
Q

Macrolide heart ADR

A

prolongs the QT interval – caution with other QT-prolonging drugs

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13
Q

Tetracycline MOA

A

Inhibition of bacterial protein synthesis, binds 30S ribosome, selective toxicity due to human cell ability to efflux the drug. Bacteriostatic

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14
Q

Tetracycline Examples

A

Doxycycline

Minocycline

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15
Q

Tetracycline Absorption

A

Give on an empty stomach, impaired by milk products

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16
Q

Tetracycline distribution

A

Tissue and fluid penetration is excellent - including placental and fetal circulation

17
Q

Tetracycline Metabolism/excretion

A

Concentrates in liver, use with caution in liver impairement.
Doxycycline is choice for those with renal disease

18
Q

Doxycycline use, gram + cocci

A

Methicillin resistant staphylococcus aureus (skin infection, pneumonia)
Most organisms are resistant

19
Q

Doxycycline use, gram - cocci

A
Moraxella catarrhalis (otitis media, CAP)
Most organisms are resistant
20
Q

Doxycycline uses, gram - baccili

A
Heamophilis Influenzae (otitis media, CAP)
Helicobacter pylori (peptic ulcer disease)
21
Q

Doxycycline use, atypicals

A
Chlamydia (trachoma, urethritis, CAP)
Mycoplasma pneumoniae (CAP)
22
Q

Tetracycline ADR

A

Teeth and bones! Avoid in later half of pregnancy and in children under 8 years old.
Photosensitivity
Yeast overgrowth

23
Q

Tetracycline DDI

A

Antacids or iron supplements - decreases bioavailability by forming insoluble salts in the stomach

24
Q

Clindamycin MOA

A

Inhibition of protein synthesis by binding to 50S ribosome

Bacteriostatic

25
Q

Clindamycin Distribution

A

Penetrates most tissues well, ESPECIALLY BONE

NOT into CSF,

26
Q

Clindamycin metabolism

A

Hepatic.

Excreted in breast milk

27
Q

Clindamycin use, gram + cocci

A

Streptococci ( pneumonia, pharyngitis)
MSSA
MRSA

28
Q

Clindamycin use, anaerobes

A

Bacteroides fragilis (abcesses)

29
Q

Clindamycin ADR

A

Pseudomembranous colitis - allows Clostridium difficile to become overgrown

30
Q

Aminoglycoside MOA

A

Inhibits protein synthesis initiation, is transported into bacteria, requiring O2 so NOT effective against anaerobes
Bactericidal, concentration dependent.

31
Q

Aminoglycoside Examples

A

Tobramycin

Gentamycin

32
Q

Aminoglycoside Absorption

A

Not absorbed orally, too polar.

IM or IV

33
Q

Aminoglycoside distribution

A

Limited to ECF, excluded from the CNS and eye but inflammation increases its penetration
Accumulates in renal cortex and inner ear

34
Q

Aminoglycoside metabolism/ecretion

A

Not metabolized, purely excreted by kidneys - renal dosing necessary

35
Q

Aminoglycoside uses, gram negative

A

Pseudomonas aeruginosa

E. coli (UTI*)

36
Q

Aminoglycoside ADR

A

Ototoxic

Renal toxic