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Group Pharm II > 39-ABX Inhibitors of protein synthesis > Flashcards

39-ABX Inhibitors of protein synthesis Flashcards

1
Q

what new classes of antibiotics were created to inhibit penicillin resistant bacteria?

A

Aminoglycocydes, tetracyclines, and macrolides

ex. streptomycin- a macrolide

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2
Q

bacterial protein synthesis inhibitors

A

selectively block bacteria synthesis of proteins by targeting ribosomes in bacteria vs. humans

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3
Q

ribosomes have how many sub units?

A

2 subunits
prokaryotes (bacteria) = 50S and 30S
Humans= 40S and 60S

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4
Q

which antibiotics act on the 30S ribosome?

A

tetracyclines, aminoglycosides, spectinomycin (not used often)

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5
Q

which antibiotics act on the 50S subunit

A

macrolides, chloramphenicol, dalfoprisint and clindamycin

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6
Q

Tetracyclines:

T/F- do tetracyclines competitively block binding of tRNA to the 30 S subunit?

A

T

this prevents addition of new amino acids to growing chain

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7
Q

T/F- do aminoglycocydes and spectinomycin bind to 30S subunit?

A

T

interferes with initiation of protein synthesis

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8
Q

How do Macrolides, chloramphenicol and dalfpristin work?

A

block enzyme that catalyzes the bond between amino acid being formed by the bacteria

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9
Q

Drugs that act on 30S subunit: Tetracyclines, aminoglycocides, aminocyclitol

what are the 5 aminoglycocides?

A 
amikacin
gentamicin
neomycin
streptomycin
tobramycin
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10
Q

What class are the mycins?

A

aminoglycocide

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11
Q

What is the one anti-ribosomal drug that cannot be absorbed systemically?

A

aminoglycosides

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12
Q

can aminoglycocides be used topically?

A

yes - for infections on skin, mucous membranes and ocular tissue

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13
Q

Can aminoglycocides penetrate meninges?

A

poorly and if needed must be administered intrathecally

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14
Q

are aminoglycocides metabolized?

A

no

excreted by kidneys with little reabsorbtion. it is proportional to the GFR

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15
Q

what bugs are aminoglycocides indicated for?

A

aerobic gram neg bacilli

most commonly used drug agains G-

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16
Q

which of the 5 aminoglycocides is least toxic

A

streptomycin- but it is also the least active against most G- bacilli

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17
Q

what is streptomycin typicallly used to treat

A

TB and yersinia pestis, and Tularemia

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18
Q

which aminoglycocides is most active against strains of P. aeruginosa?

A

tobramycin

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19
Q

which aminoglycocides is most active against the family called bacteriaceae (e.coli, klebsiella, …)

A

Gentamycin

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20
Q

how is resistance to aminoglycocides caused?

A

inactivation of the drug, decreased binding sites and decreased uptake by porins

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21
Q

what are adverse effects of aminoglycocides

A

nephrotoxicity and ototoxicity

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22
Q

T/F aminoglyces are MCC of drug induced renal failure?

A

T

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23
Q

which aminoglyce is most nephrotoxic?

A

neomycin- it is limited to topical treatment for this reason

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24
Q

Triple antibiotic creams (topicals with neomycin) mixed with what?

A

neomycin, bacitracin and polymyxin
bacitracin-covers gram +
polymyxin-covers gram -
neomycin- covers both

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25
Q

Drugs that act on 30S subunit: Tetracyclines, aminoglycocides, aminocyclitol

what is aminocyclitol?

A

spectinomycin- (often an alternative to ceftrioxone in the treatment of gonorrhea)

similar structure to aminoglycocides

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26
Q

Drugs that act on 30S subunit: aminoglycocides, aminocyclitol, Tetracyclines,

what are some of the tetracyclines

A

doxycycline-
minocycline
tetracycline

tigecycline - this one is a compound and will be asked later

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27
Q

what is spectrum of tetracyclines

A

broad spectrum bacteriostatic that inhibit growth of gram + and Gram - , ricketsiae, spirochetes, mycoplasmas, chlamydiae

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28
Q

what is drug of choice for Rocky mountain spotted fever and LYME

A

tetracyclines

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29
Q

What else can tetracyclines treat?

A

mycoplasma pneumoneae, chlamydia, acne vulgaris, brucelosis, and others….

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30
Q

T/F tetracyclines are also added to some regimens to treat H. pylori and peptic ulcers

A

T

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31
Q

is there resistance to tetracyclines?

A

yes- because it was added to animal feed to promote weight gain. Fuckers!

32
Q

what are some ADRs of Tetracyclines?

A

discoloration of the teeth, nephrotoxicity, hepatotoxicity and sometime photosensitivity

33
Q

What is tigecycline?

A

it is a compound that has increased affinity for 30S ribosomes and decreased resistance mechanisms like other tetracyclines

34
Q

what is tigecycline indicated for?

A

Skin and soft tissue infections caused by MRSA, e.coli, b. frag, enterofaecalis

also complicated intra-abdominal infections

35
Q

Drugs that act on the 50S ribosomes

A

Macrolide antibiotics

ketolide antibiotics

36
Q

what ribosome do macrolides affect?

A

50S

37
Q

what are some macrolides?

A

azythromycin
clarithromycin
erythromycin

38
Q

how are macrolides usually administered?

A

orally but…..

erythromycin and azythromycin can be IV for serious infections like legionaires

39
Q

when given orally is erythromycin bioavailable?

A

not so much. it is better topically

40
Q

is clarythromycin and Azythromycin bio available from the gut?

A

yes and they achieve higher tissue concentrations this way

41
Q

are macrolides metabolized?

A

yes - by the liver and excreted in bile and urine

42
Q

what are some of the indications for macrolides?

A

G- and G+ bacteria that cause respiratory tract infections and pneumoniae

Group A strep, pneumococci, chlamydiae, legionella

43
Q

are macrolides effective against Klebsiella? (typical pneumonia)

A

no

44
Q

which macrolide is used for chlamydial urethritis?

A

1 x dose of Azythromycin

45
Q

which macrolide is most effective against H. pylori causing peptic ulcer disease?

A

Clarythromycin

46
Q

what other drug mentions is added to regimens of H. pylori?

A

tetracyclines

47
Q

is there resistance to macrolides?

A

it is gradually increasing

48
Q

how have bacteria become resistant?

A

decreased binding to 50S ribosome, enzymatic inactivation, increased bacterial efflux

49
Q

which bacteria are resistant?

A

most staphylococci, and pneumococci are increasingly resistant

50
Q

what are the adverse effects of macrolides?

A

largely devoid of toxicity- but can cause stomatitis (inflamm. of the mouth) nausea, anorexia, abdominal discomfort and diarrhea

51
Q

what ADRs does erythromycin have on the gut

A

it binds to receptors for Motilin decreasing peristalsis. this causes N/V/D

52
Q

do macrolides have drug interactions?

A

erythromycin and clarythromicin inhibit Cytochrome P450

53
Q

T/F if erythro and clarythromycin interact with carbemezapine (anticonvulsant) it will cause life threatening toxicity?

A

T- carbemezipine toxicity

54
Q

other macrolide interactions?

A

simvistatin, and lovastatin

55
Q

what is the second class of drug that works on the 50 S ribosome besides macrolides?

A

Keolides antibiotics
telithromycin
clindamycin
chloramphenicol

56
Q

Are ketolide abx similar to macrolides?

A

yes they are similar in structure and act of 50S ribosome

57
Q

example of ketolide abx

A

telithromycin- more stable in the stomach and increased ribosomal binding affinity. less susceptable to bacterial efflux

58
Q

what are some indications for telithromycin?

A

approved for mild to moderate CAP-community acquired pneumoniea
streptococcus pneumoniae, chlamydia, and mycoplasma pneumoniea.

59
Q

ADR’s of telithromycin

A

most common is Diarrhea and Nausea

hepatotoxicity, and QT interval prolongation, respiratory failure and myasthenia gravis, LOC

60
Q

what class is clindamycin?

A

a ketolide drug belonging to macrolides group

61
Q

what does clindamycin cover?

A

G+ cocci, aerobic organisms such as B. frag and clostridium difficile

62
Q

how is clindamycin administered

A

orally, parenterally, or topically

63
Q

ADRs for clindamycin?

A

severe diarrhea caused by c. diff and pseudomembranous colitis which can cause death

64
Q

what is chloramphenicol?

A

it is a drug that acts on 50S ribosome but unlike macrolides.

65
Q

what makes chlormaphenicol different?

A

it is highly lipophilic, well absorbed in gut, and concentrates in CNS.

66
Q

because it concentrates in CNS what is it affective against?

A

meningitis

67
Q

what can chloramphenicol cause in neonates?

A

gray baby syndrome- reduce the dose

68
Q

what is gray baby syndrom characterized by?

A

cyanosis, weakness, respiratory depression, hypotension, and shock

69
Q

other adverse effects of chloramphenicol include?

A

2 forms of anemia

  1. dose dependent anemia- reversible
  2. fatal aplastic anemia- not reversible
70
Q

T/F chloramphenicol is narrow spectrum abx?

A

F it is broad spectrum and is active against pneumococci, meningococci, and H. influenzae

all the MCC of meningitis

71
Q

Quinupristin- Dalfopristin

A

are the only streptogramin abx available.

72
Q

what do Quinupristin- Dalfopristin do

A

they synergystically inhibit bacterial protein synthesis

one prevents addition of new aminoacids
other blocks bond formation

73
Q

what are other protein synthesis inhibitors?

A

linezolid,

mupiricin-bactroban

74
Q

what is linezolid indicated for?

A

Vanco resistant E. faecium pneumonia

75
Q

ADRs of linezolid

A

thrombocytopenia, serotonin toxicity

76
Q

what is mupiricin?

A

bactroban

77
Q

what is mupiricin effective against?

A

staphylocci, group B hemolytic strep, empetigo

and nasal MRSA!!! boom

Group Pharm II (8 decks)

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