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Protein synthesis inhibitors- individual facts > Protein synthesis inhibitors > Flashcards

Protein synthesis inhibitors Flashcards

1
Q

Name oxazolidinones

A

Linezolid

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2
Q

Mechanism of linezolid

A

Bacteriostatic

Binds 50S subunit and prevents formation of initiation complex

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3
Q

Spectrum of linezolid

A

Gram+, MRSA, Vanco-resistant enterococci

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4
Q

Side effects of linezolid

A

Bone marrow suppression, inhibits monoamine oxidase leading to serotonin syndrome (Don’t treat w/ SSRI)

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5
Q

Resistance to linezolid

A

Alteration of 23S rRNA of 50S subunit to prevent binding

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6
Q

Name Aminoglycosides

A

Gentamicin, Amikacin, Tobramycin

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7
Q

Mechanism of Aminoglycosides

Gentamicin, Amikacin, Tobramycin

A

Bactericidal, prevents formation of initiation complex, causes misreading of mRNA, induces early termination

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8
Q

Spectrum of Aminoglycosides

Gentamicin, Amikacin, Tobramycin

A

Extended spectrum

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9
Q

Side effects of Aminoglycosides

Gentamicin, Amikacin, Tobramycin

A

Tubular necrosis: ototoxicity and nephrotoxicity

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10
Q

Resistance to Aminoglycosides

Gentamicin, Amikacin, Tobramycin

A

Intrinsic: failure of antibiotic to enter cell (needs facilitated transport)
Acquired: acquisition of enzyme to inactivate the drug (amikacin is less suscetible to enzyme)

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11
Q

Notes on Aminoglycosides

Gentamicin, Amikacin, Tobramycin

A

Poor absorption in GI, usually administered IV, does not cross BBB. REQUIRES ENERGY TO ENTER CELL- TREAT W/ ANTIBIOTIC TO DESTROY CELL MEMBRANE

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12
Q

Name tetracyclines

A

Tetracyclin, doxycycline, minocycline

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13
Q

Mechanism of tetracyclines

Tetracyclin, doxycycline, minocycline

A

Bacteriostatic- binds to 30S subunit preventing attachment of aminoacyl-tRNA

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14
Q

spectrum of tetracyclines

Tetracyclin, doxycycline, minocycline

A

Broad: B. burgdorfei, H. pylori, Mycoplasma, Chlamydia

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15
Q

Side effects of tetracyclines

Tetracyclin, doxycycline, minocycline

A

Chelates metal ions (Calcium), GI irritation, photosensitivity, discoleration of teet, inhibits bone growth. Don’t prescribe during pregnancy.

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16
Q

Resistance to tetracyclines

Tetracyclin, doxycycline, minocycline

A

Increased efflux, ribosomal protection proteins protect A site from drug

17
Q

Notes on tetracyclines

Tetracyclin, doxycycline, minocycline

A

don’t treat during pregnancy

18
Q

Mechanism of Chloramphenicol

A

Bacteriostatic- binds 50S preventing peptide bond formation- kills peptidyltransferase reaction

19
Q

Spectrum of Chloramphenicol

A

Extended spectrum- but limited due to toxicity

20
Q

Chloramphenicol side effects

A

Toxic, bone marrow depression, aplastic anemia, grey baby syndrome

21
Q

Resistance to chloramphenicol

A

Reduces membrane permeability, acetyltransferase modifies drug

22
Q

Notes on chloramphenicol

A

don’t use on newborn babies because of immature liver- high likelihood of toxicity

23
Q

Name macrolides

A

erythromycin, azithromycin, clarithromycin

24
Q

Macrolide mechanism

erythromycin, azithromycin, clarithromycin

A

Bacteriostatic- inhibits translocation by binding to 23S rRNA of 50S subunit

25
Q

Macrolide spectrum

erythromycin, azithromycin, clarithromycin

A

Broad- coverage of respiratory pathogens, pharyngitis, pneumonia, otitis media, Chlamydia (single dose)

26
Q

Macrolide side effects

erythromycin, azithromycin, clarithromycin

A

GI discomfort, inhibitor of CYP3A4 (except azithromycin), Clarithromycin not safe during pregnancy, Azithro can cause pyloric stenosis in infants

27
Q

Resistance to macrolides

erythromycin, azithromycin, clarithromycin

A

Methylation of 23S rRNA site, increased efflux, hydrolysis of macrolides by esterases

28
Q

Name lincosamide

A

Clindamycin

29
Q

Clindamycin mechanism

A

Bacteriostatic- blocks translocation of 50S ribosomal subunit

30
Q

Clindamycin spectrum

A

Gram+, including anaerobic bacteria, skin and soft tissue infections, Acne vulgaris

31
Q

Clindamycin side effects

A

Diarrhea, abdominal pain, mucus and blood in stool, superinfection with C. diff

32
Q

Resistance to clindamycin

A

Mutation in ribosome methylation of rRNA, cross resistance to macrolides and streptogrammins, enzymes can inactivate the drug

33
Q

Name Streptogrammins

A

Quinipristin, Dalfopristin

34
Q

Streptogrammins mechanism

Quinipristin, Dalfopristin

A

Combined bactericidal for some organisms, bind 50S to inhibit translocation

35
Q

Streptogrammins spectrum

Quinipristin, Dalfopristin

A

Multiple drug-resistant Gram+

36
Q

Streptogrammins side effects

Quinipristin, Dalfopristin

A

High incidence of arthalgias, inhibits CYP3A4 and likely has significant drug interactions

37
Q

Resistance to streptogrammins

Quinipristin, Dalfopristin

A

Ribosomal methylase inhibits binding of drug, Enzymes inactivate drug, efflux, cross resistance with macrocodes and clindamycin

38
Q

Notes on streptogrammins

Quinipristin, Dalfopristin

A

Always treat together.

Protein synthesis inhibitors- individual facts (1 decks)

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