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Immunity, Infection and Disease > Inhibitors of Microbial Protein Synthesis II > Flashcards

Inhibitors of Microbial Protein Synthesis II Flashcards

1
Q

Tetracycline Adverse Reactions

A

nausia, diarrhea, superinfections, enamel dysplasia and abnormal bone growth in fetus, hepatic disease in pregnancy, photosensativity, vestibulotoxicity

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2
Q

Primary use of tetracyclines

A

mycoplasma pneumonia, Chlamydia, and Rickettsiae

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3
Q

Newest Tetracycline

A

Tigecycline is a glycylcycline approved for MRSA and complicated intra-abdominal and skin infections, only injections once daily; gram negative bacteria with efflux pump and tetracycline resistant strains are susceptible

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4
Q

Macrolides

A

Erythromycin, azithromycin, and clarithromycin

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5
Q

Macrolides Mechanism of Action

A

bind 50s and block translocation of peptidyl-tRNA from acceptor to donor site, also blocks formation of initiation complex

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6
Q

Macrolide Resistance

A

Across the class, three mechanisms: reduced permeability of cell membrane efflux, enterobacteria esterases metabolize drug, modified binding site (methylase adds methyl to site, also resistance to lincosamides and streptogramin B)

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7
Q

Macrolide Adverse Reactions

A

GI irritation, rashes, eosinophilia, hypersensativity cholestatic hepatitis, pregnant hepatitis

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8
Q

Tetracycline Interactions

A

Polyvalent cations and cholestyramine/cholestipol cholesterol lowering resins that bind tetracyclines

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9
Q

Macrolide Clinical Uses

A

moderate spectrum bacteriostatic only for rapidly multiplying organisms, mycoplasma pneumoniae, Chlamydia, H. Pylori, prophylaxis, corynebacterial infections

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10
Q

Ketolides

A

Synthetic macrolides for community pneumonia, bacterial sinusitis and chronic bronchitis but associated with liver failure and exacerbbation of myasthenia gravis

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11
Q

Fidaxomicin

A

narrow spectrum macrolide that inhibits bacterial RNA polymerase and has no systemic absorption

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12
Q

Linosamide (Clindamycin) Mechanism of Action

A

blocks translocation of peptidyl tRNA from acceptor site to donor site so charged tRNA cannot access receptor site (similar to macrolides)

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13
Q

Linosamide Resistance

A

Methylation for 50s binding site and enzymatic inactivation, cross resistance with macrolides

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14
Q

Lincosamides Adverse Reactions

A

GI irritation worsened by any peristalsis inhibitors, hepatic dysfunction, neutropenia, rash, thrombophlebitis at injection site, superinfections

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15
Q

Lincosamides Interactions

A

Macrolides have same MOA so together each drug is less effective

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16
Q

Primary clinical use for Lincosamides

A

Bacteriostatic used to treat severe anaerobic gram negative infections

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17
Q

Treatments for Clostridium difficile

A
  1. oral metronidazole for mild/moderate or oral vancomycin for severe, 2. fidaxomicin, 3. Investigating humanized neutralizing mAb against toxins A and B
18
Q

Qinupristin-dalfopristin

A

30:70 combination of streptogramin B (Q) and A (D) that has a longer duration than one drug alone

19
Q

Quinupristin-dalfopristin Mechanism of Action

A

bind 50s and constric exit channel on ribosome

20
Q

Quinupristin-dalfopristin Resistance

A

enzymatic inactivation of dalfopristin, modification of quinupristin binding site, binding interference, efflux interference

21
Q

Quinupristin-dalfopristin Adverse Reactions

A

pain at infusion site and arthralgia-myalgia

22
Q

Quinupristin-dalfopristin Interactions

A

Potent inhibitors of CYP34A so may increase plasma levels of many drugs

23
Q

Quinupristin-dalfopristin clinical uses

A

bactericidal reserved for treating resistant organisms: penicillin resistant pneumococci, VRSA, MRSA, vancomycin resistant Enterococcus faecium, methicillin caused skin infections

24
Q

Oxazolidinone (linezolid) mechanism of action

A

binds unique site, 23s of 50s, and blocks formation of tRNA-ribosome-mRNA complex

25
Q

Oxazolinfinones Resistance

A

Mutation of 23s ribosomal binding site, only enterococci so far

26
Q

What protein inhibitors are adjusted in Renal insufficiency and which are not?

A

tetracyclines except doxycycline, azithromycin, clarithromycin, licosamides, aminoglycosides, and cyclic lipopeptides must be adjusted

27
Q

Oxazolidinones Adverse Reactions

A

Thrombocytopenia, optic/peripheral neuropathy and lactic acidosis with prolonged use

28
Q

Oxazolindinones Interacitons

A

MAO inhibitor so enhances serotonergic drug effects, do not give oxazolindinone and serotonergic simultaneously

29
Q

Oxazolidinones clinical uses

A

bacteriostatic for enterococci and staphlococci, bactericidal for streptococci, active agains gram possitives resistant to beta lactams and vancomycin so reserved for treating resistant organisms and uses as last resort for multi-drug resistant strains

30
Q

Aminoglycosides

A

Amikacin, Gentomicin, Streptomycin, Tobramycin, Neomycin, Netilmicin, Paromomycin

31
Q

Aminoglycosides Resistance

A

Varying susceptibility to inactivating transferases, impaired cell entry, and changes in binding site

32
Q

Aminglycosides Adverse Reactions

A

Irreversible ototoxicity, auditory impairment from amikacin and kanamycin and vestibular impairment from gentamicin and streptomycin, reversible nephrotoxicity from gentomicin and tobramycin, neuromuscular blockade, and skin reactions

33
Q

Aminoglycosides Interactions

A

Other nephrotoxic drugs, loop diuretics increase ototoxicity, and synergy with beta lactam antibiotics

34
Q

Aminoglycoside Clinical Uses

A

bactericidal for aerobic gram negative bacteria

35
Q

Aminocyclitols (spectinomycin) Mechanism of Action

A

bind 30s but are not bactericidal and do not cause misreading

36
Q

Why are adverse reactions, interactions, and resistance rare for aminocyclitols?

A

Drug given as a single 2g IM injection dose

37
Q

Clinical uses of Aminocyclitols

A

Bacteriostatic against gram positive and negative but just used as alternative therapy for gonorrhea in patients allergic to other therapies, Aminocyclitos have no cross resistance with other gonorrheal antibiotics

38
Q

Cyclic lipopeptides (Daptomycin) Mechanism of Action

A

depolarize bacterial cell membrane causing loss of potential and potassium reflux leading to cell death.

39
Q

Cyclic Lipopetides Resistance/Interactions

A

None

40
Q

Cyclic Lipopeptides Adverse Reactions

A

Injection pain, GI, fever, CNS effects, elevated CPK which requires monitoring, decreased nerve conduction velocity, cardio-respiratory events, discontinue if muscle weakness, pain, or myopathy

41
Q

Cyclic Lipepeptides Clinical Uses

A

Bactericidal agains gram possitives including MRSA and vancomycin resistant Enterococcus faecalis, treatment for complicates skin and skin structure infections

Immunity, Infection and Disease (86 decks)

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