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ClinSci IV > 6. Agents Targeting the Cell Wall and Membrane > Flashcards

6. Agents Targeting the Cell Wall and Membrane Flashcards

1
Q

amoxicillin, ampicillin, methicillin, nafcillin, oxacillin, penicillin G, penicillin V, piperacillin, ticarcillin

A

penicillins

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2
Q

cefazolin, cefaclor, cefdinir, cefixime, cefepime, cefotetan, cefuroxime, cephalexin, ceftaroline, ceftriaxone

A

cephalosporins

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3
Q

aztreonam

A

monobactam

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4
Q

vancomycin

A

glycopeptide

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5
Q

bacitracin

A

polypeptide

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6
Q

doripenem, ertapenem, imipenem, meropenem

A

carbapenems

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7
Q

fosfomycin

A

phosphoenolpyruvate

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8
Q

clavulanic acid, sulbactam, tazobactam

A

b-lactamase inhibitors

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9
Q

daptomycin

A

lipopeptides

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10
Q

polymyxin B

A

detergents

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11
Q

NAM-NAG pentapeptide

A

basic unit for cell wall synthesis

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12
Q

target for penicillins

A

penicillin binding proteins

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13
Q

baceriocidal, susceptible to acidic environment which impacts route of adminsitration, susceptible to B-lactamase enzyme. includes penicillins, cephalosporins, monobactams, and carbapenems

A

B-lactam agents

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14
Q

naturally occuring, varying spectrum of activity, causes hypersensitivity and diarrhea

A

penicillins

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15
Q

work on gram + and -, B-lactamase sensitive, acid unstable, parenteral adminsitration, renal adminstration requiring dose adjustments, minimal CSF penetration unless inflammation

A

pencillin G

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16
Q

narrow spectrum, gram + and gram - coverage, B-lactamase sensitive, acid stable, orally adminstered, renal dose adjustments, minimal CSF penetration unless inflammated

A

pencillin V

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17
Q

very narrow spectrum, gram + staph and strep coverage, B-lactamase resistant, parenteral or orally adminstered, no dose adjustment for elimination, penetrates CSF

A

methicillin, nafcillin, oxacillin

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18
Q

extended/broad spectrum, ampicillin, gram + and gram - cocci/rods coverage, B-lactamase sensitive, renal dose adjustments necessary, penetrate CSF if inflamed meninges in a newborn

A

ampicillin

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19
Q

extended/broad spectrum, gram + gram - cocci/rods coverage, B-lactamase sensitive, renal dose adjustements necessary

A

amoxicillin

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20
Q

extended/broad spectrum, availabile only in combination with beta-lactamase inhibitors, gram + and gram - cocci/rods coverage, B-lactamase sensitive, renal dose adjustments necessary

A

ticarcillin

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21
Q

extended/broad spectrum, available only in combination with beta-lactamase inhibitors, gram + gram -cocci/rods, B-lactamase sensitive, renal dose adjustments, good CSF penetration but not used for meningitis

A

piperacillin

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22
Q

inhibit bacterial B-lactamase, clavulanic acid, sulbactam, tazobactam, used in combination with pencillins to increase effectiveness, common combinations of amoxicillin/clavulanic acid (augmentin), ampicillin & sulbactam, or piperacillin & tazobactam, causes adverse effects similar to pencillin adminstered

A

B-lactamase inhibitors

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23
Q

increases with addition of B-lactamase inhibitors

A

penicillin spectrum of activity

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24
Q

penicillin, oxacillin/naficillin, cefazolin, cephalexin/cephadine, aztreonam, aminoglycosides, vancomycin, erythromycin, clindamycin, linezolid, quinuprisitin/dalfopristin, daptomycin, metronidazole

A

narrow spectrum antibiotics

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25
Q

ampicillin, cefotoxin, cefotetan, cefuroxime-axetil, cefaclor, ciprofloxacin, azithromycin, clarithromycin, telithromycin, trimethoprim sulfamethoxazole

A

moderately broad antibiotics

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26
Q

ampicillin sulbactam, amoxicillin/clavulanate, ceftriazone, cefotaxime, ceftizoxime, ceftazidime, cefixime, cefpodozime protexil, ceftaroline, tetracycline, doxycycline, chloramphenicol, levofloxacin

A

broad spectrum antibiotics

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27
Q

ticarcillin-clavulanate, piperacillin-tazobactam, cefepime, ceftazidime-avibactam, cefoperazone-sulbactam, ceftolozane-tazobactam, imipenem, meropenem, doripenem, ertapenem, gatifloxacin, moxifloxacin, tigecycline

A

very broad spectrum antibiotics

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28
Q

used if penicillins are not tolerated, more resistant to B-lactamase than penicillins however resistance on the rise, grouped based on spectrum of activity, bind and inhibit pencillin binding proteins, can cause hypersensitivity and diarrhea, 1st generation covers gram + cocci, second generation covers gram + and some organisms, 3rd generation covers gram +/- cocci and many gram - rods, other generations cover gram +/- & resistant organisms

A

cephalosporins

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29
Q

1st generation, covers many gram + cocci, resistance by B-lactamase, parenteral administration, long half life, good for intramuscular injection, no CSF penetration

A

cefazolin

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30
Q

1st generation, covers many gram + cocci, resistance by B-lactamase, oral adminstration, no CSF penetration

A

cephalexin

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31
Q

2nd generation, covers gram + and some gram -, not used as much as 1st or 3rd generation, less resistance by B-lactamase by first generation, parenteral administration

A

cefotetan

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32
Q

2nd generation, covers gram + and some gram -, not used as much as 1st or 3rd generation, less resistance by B-lactamase by first generation, oral administration

A

cefaclor

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33
Q

2nd generation, covers gram + and some gram -, not used as much as 1st or 3rd generation, less resistance by B-lactamase by first generation, parenteral administration, will penetrate CSF

A

cefuroxime

34
Q

3rd generation, covers gram + and - cocci, and many gram - rods, not as good as 1st generation for gram +, increases resistance by B-lactamase, parenteral adminsitration with long half life, penetrates CSF

A

ceftriaxone

35
Q

3rd generation, covers gram + and - cocci, and many gram - rods, not as good as 1st generation for gram +, increases resistance by B-lactamase, parenteral adminsitration, penetrates CSF

A

cefotaxime

36
Q

3rd generation, covers gram + and - cocci, and many gram - rods, not as good as 1st generation for gram +, increases resistance by B-lactamase, oral administration

A

cefdinir

37
Q

3rd generation, covers gram + and - cocci, and many gram - rods, not as good as 1st generation for gram +, increases resistance by B-lactamase, oral administration

A

cefixime

38
Q

4th generation, anti-pseudomonal, gram + gram - and multiresistant gram - coverage, very strong resistance by B-lactamase, parenteral adminstration, renal dose adjustments necessary, penetrates CSF

A

cefepime

39
Q

anti-MRSA, similar to 3rd generation with extended gram + coverage, parenteral adminstration, renal dose adjustment necessary

A

ceftaroline

40
Q

only one is approved in the USA, covers only gram - rods, penetrates CSF, treats serious infections like pneumonia, menigitis, and sepsis, resistance by B-lactamase, binds and inhibits penicillin-binding proteins, causes hypersensitivity reactions and cough

A

aztreonam

41
Q

broadest spectrum of all B-lactam antibiotics, includes gram - and gram +, most potent B-lactam antibiotic, resistance by B-lactamase but is also suseceptible to carbapenemase, imipenem inactivated in the kidney so adminstered with cilastatin to prevent inactivation, key effect is to penetrate tissue and fluids very well including CSF, is important for empiric treatment of life threating infections, also used in cancer, nosocomial pneumonia, intra-abdominal infections, UTIs, and skin/soft tissue infections, binds to and inhibits all pencillin binding proteins, causes nausea, vomiting, diarrhea, confusion, tremors, seizures

A

carbapenems/ doripenem, imipenem, ertapenem, meropenem

42
Q

natural compound, broad spectrum for gram + bacteria, treats MRSA, enterococci, and c.diff, good tissue penetration except for CNS, due to resistance development oral use is limited to c.diff, delivered by slow IV infusion, prevents elongation of peptidoglycan cell wall structure by binding to D-ala D-ala pentapeptide and acts as steric inhibitor, causes flushing red neck/red man syndrome, abdominal pain, ototoxicity and renal failure

A

vancomycin

43
Q

polypeptide, targets a variety of gram + bacteria, use is restricted to topical and opthalmic ointments, combined with other antimicrobial agents like neomycin, polymyxin B, and hydrocortisone, blocks incorporation of amino acids and nucleic acids into the cell wall, causes hypersensitivity reactions but rare

A

bacitracin

44
Q

phosphoenolpyruvate, broad spectrum of activity and includes gram - and gram + bacteria, commonly used in the treatment of uncomplicated urinary tract infection in females, safe during pregnancy, blocks early step in cell wall synthesis by preventing synthesis of UOP-N-acetylmuramic acid, causes hypersensitivity reactions but is rare

A

fosfomycin

45
Q

targets the membrane, cyclic lipopeptide, useful against gram+ organisms including MRSA, commonly used for treatment of complicated skin and soft tissue infections as well as bacteremia and endocarditis, binds to membrane and causes depolarization of the membrane and is bactericidal, insertion into membrane is Ca++ dependent, causes myopathy and rhabdomyolysis

A

daptomycin

46
Q

targets membrane, detergent, used topically to treat skin infections in combination with bactracin, spectrum of activity similar to primarily gram - bacteria, binds to phospholipids in the cell membrane and disrupts structure, specifically LPS, rarely has adverse effects if administered topically

A

polymyxin B

47
Q

doxycycline, minocycline, tetracycline, tigecycline

A

aminoglycosides

48
Q

amikacin, gentamycin, kanamycin, neomycin, streptocmycin, tobramycin

A

aminoglycosides

49
Q

azithromycin, clarithromycin, erythromycin

A

macrolides

50
Q

clindamycin, chloramphenicol, linezolid

A

other protein synthesis inhbitors

51
Q

include aminoglycosides, macrolides, tetracyline, and some others, some bacteriostatic but can also be bactericidal, disrupt process of translation by targeting molecu.ar machinery ribosomal subunit 50s and 30s needed to translate mRNA to protein

A

protein synthesis inhibitors

52
Q

charged tRNA binds to A site > peptidyl tRNA and peptide bond form between growing aminao acid chain and amino acid in A site > newly uncharged tRNA exits > amino acid chain elongates +1 and translocates to P site

A

prokaryotic translation

53
Q

generally narrow spectrum with bactericidal effect, uptake is oxygen dependent only working on aerobic organisms, used in combination with B-lactam antibiotics to treat serious gram - infections and are not absorbed well from the gut, binds to 30s and perhaps 50s ribisomes blocking formation of initiation complex disrupting mRNA and 30s binding which would occur prior to step 1 of prokaryotic translation, causes nephortoxicity by renal tubular necrosis and ototoxicity

A

amingoglycosides/ streptomycin, gentamicin, kanamycin, amikacin, tobramycin, neomycin

54
Q

aminoglycosides, gram + and gram - aerobic organisms, primarily used for gram - aerobic organisms, used also in pneumonia and UTI, resistance by expression of enzymes altering chemical structure of the drug, adminstered intramuscularly, subq, or topic, poor absorption from the GI tract, eliminated through urine as a parent compound, kidney function affects half life

A

streptomycin, gentamycin, kanamycin, amikacin, tobramycin, and neomycin

55
Q

macrocyclic lactone ring structure including natural compounds and semisynthetics, covers mostly gram + and some gram -, overall narrow in spectrum of activity, concentrates in lungs, tonsils, and cervix, spectrum increases as A>C>E, binds to 50s and impairs translocation to the P site, causes stomach cramps, nausea, vomiting, diarrhea due to motilin activity, prolongs QT interval, skin hypersensitivity reactions

A

erythromycin, clarithomycin, azithromycin

56
Q

macrolide, narrow spectrum but broadest of all macolides, used in pneumonia, pharyngitis, sinusitis, tonsillitis, STDs, resistance by drug efflux, changes in drug binding to 50s ribosomes, oral and IV administration, concetrations in many tissues like the lungs, tonsils, and cervix, long half life up to 68 hours

A

azithromycin

57
Q

macrolide, narrow spectrum but broader than erythromycin, pneumonia, pharyngitis, sinusitis, STDs, resistance by drug efflux and changes in drug binding to the 50s ribosome, oral administration

A

clarithromycin

58
Q

macrolides, narrowest spectrum, pneumonia, pharyngitis, tonsillitis, STDs, resistance by drug efflux or changes in drug binding to 50S ribosome, oral adminstration, eliminated by liver metabolism thus hepatic dosing considerations - not renal

A

erythromycin

59
Q

four ring structure, broad spectrum with bacteriostatic effect, binds 30S subunit of ribosome and prevents binding of new aminoacyl-tRNA, causes nutrient interactions with calcium which results in disrupted growth of calcified tissue (bone, teeth) particularly during growth with discoloration of the teeth, disrupts normal flora, causes nausea, vomiting, diarrhrea, skin hypersensitivity and photosensitivity, also acts as a chelator preventing absorption of divalent cations

A

tetracyclines

60
Q

tetracycline, broad spectrum, used in patients with pencillin allergy, STDS, acne, resistance by drug efflux, adminstered orally, eliminated by the kidney so renal considerations, binds to di and tri valent cations such as calcium and aluminum so food delays absorption

A

tetracycline

61
Q

tetracycline, broad spectrum, used in patients with pencillin allergy, STDS, acne, resistance by drug efflux, adminstered orally, IV and topically, eliminated hepatically and renally so impairment considerations, binds di and trivalent cations such as calcium and aluminum so food delays absorption

A

minocycline

62
Q

tetracycline, broad spectrum, used in patients with pencillin allergy, STDS, acne, resistance by drug efflux, adminstered IV, severe hepatic insufficiency requires dose adjustements, binds di and trivalent cations such as calcium and aluminum, food delays absorption

A

tigecycline

63
Q

tetracycline, broad spectrum, used in patients with pencillin allergy, STDS, acne, resistance by drug efflux, adminstered orally and IV, no hepatic metabolism so there are no hepatic or renal considerations, can bind di and trivalent cations such as calcium and aluminum, however no food restrictions

A

doxycycline

64
Q

relatively narrow spectrum, commonly used in treatment of soft tissue infections caused by strep and staph, also used when treating community acquired MRSA of the skin and soft tissue, binds to 50S subunit of the ribosome and prevents formation of initiation complexes and also blocks translocation step, causes nausea, vomiting, diarrhea, and c.diff infection, also causes skin rashes

A

clindamycin

65
Q

broad spectrum antibiotic exerting bacteriostatic effect, rarely used except for serious infections such as typhys and rocky mountain spotted fever, also used to treat eye infections, binds to 50S subunit of the ribosome and prevents transpeptidation or peptidyl bone formation, causes suppression of red blood cell production, gray baby syndrome due to lack of glucuonic acid production, nausea, vomiting, diarrhea, and superinfection of oral and vaginal candidiasis

A

chloramphenicol

66
Q

effective against most gram + organisms but not very effective for most gram -, effective against penicillin/methicillin/vancomycine resistant strains, inhibits protein synthesis by binding to the P site of the 50S ribosome and inhibits the formation of the ribosomal fMet-tRNA complex blocking first tRNA amino acid binding, causes myelosuppression resulting in anemia, leukopenia, pancytopenia, and thrombocytopenia, inhibits monoamine oxidase so affects these drugs

A

linezolid

67
Q

narrow spectrum with gram + coverage, used in skin and soft tissue infections including CA-MRSA, cross resistance with macrolides because of similar mechanism of action, administered IV IM and topically, eliminated primarily hepatically, good tissue penetration particularly in abscesses, but no good CSF penetration

A

clindamycin

68
Q

broad spectrum, good against anaerobic bacteria, resistance by expression of inactivating enzymes, administered oral, IV, and topically, eliminated by the liver and excreted by the kidneys, well absorbed orally and widely distributed, penetrates CSF

A

choramphenicol

69
Q

mostly gram + coverage, has some resistant organisms, adminstered orally and IV, no dosage adjustments necessary, 100% bio-availability after oral administration so oral and IV dose are the same

A

linezolid

70
Q

sulfur containing compounds, broad spectrum covering gram + and gram - bacteria, not frequently used as a single agent, do not effect mammalian cells because they depend upon exogenous folate and do not synthesize folate, resistance in bacteria can occur if excess PABA is produced, sulfonamide uptake is altered, or sulfonamide binding to dihydropteroate synthase is altered, works by competing with PABA for dihydropteroate synthase and blocks dihydrofolic acid synthesis and this DNA synthase, causes skin hypersensitivity, photosensitivity, steven-johnson syndrome presenting as serious/fatal skin and mucous membrane eruption, also nausea, vomiting, diarrhea, and urine preciptates causing crystalluria, hematuria, and obstruction

A

sulfonamides - sulfadiazine/sulfamethoxazole/sulfamethizole

71
Q

pyrimidine compunds including trimethoprim and primethamien, covers gram - bacteria, resistance in bacteria may occur if there is change in drug uptake or reduced reductase binding, inhibitor of bacterial dihydrofolate reductase in impaired DNA synthesis, causes bone marrow suppression, megaloblastic anemia, leukopenia, and granulocytopenia, also nausea, vomiting, and diarrhea

A

trimethoprim/pyrimethamine - antifolates

72
Q

combination, commonly used to treat urinary tract infection and prostatitis, in addition at lower doses used prophylactially to treat recurrent urinary tract infection, in addition is effective in treating pneumonia, shigellosis, and systemic salmonella infections, works by synergistic effect of combining trimethoprim-sulfamethoxazole, causes same adverse effect of each of the individual agents

A

trimethoprim sulfamethoxazole - TMP/SMX

73
Q

synthetic flourinated compounds, broad spectrum antibiotics covering gram + and gram - bacteria, used in the treatment of urinary, gastrointestinal and respiratory infections as well as some sexually transmitted diseases like gonorrhea, effective against anthrax, works by disrupting the winding of DNA and the separation of DNA strands during transcription and replication specifically inhibiting topoisomerase II (DNA gyrase) and topoisomerase IV, causes nausea, vomiting, diarrhea, drug-nutrient interactions by binding divalent cations and preventing absorption, prolongs QT interval, causes rash, itching, photosensitivity, also causes tendinopathy in adults and arthropathy due to growing cartilage

A

fluoroquinolones/ ciprofloxacin and levofloxacin

74
Q

least active fluoroquinolone

A

norfloxacin

75
Q

fluoroquinolone working well against gram - with some activity against gram +

A

ciprofloxacin, levofloxacin, ofloxacin

76
Q

best activity against gram +

A

gatifloxacin, gemifloxacin, moxifloxacin

77
Q

unknown mechanism of action which is antibacterial and antiprotozoal, coverage limited to anaerobic bacteria, good tissue penetration and distribution, used in the treatment of abdominal infections, vaginitis, c. diff colitis, and brain abscess, works as a prodrug inactive until taken up by the organism and undergoes chemical reduction, reaction metabolites bind to DNA and disrupt function and cause damage, causes nausea, vomiting, diarrhea, affects metabolism with disulfiram effect so avoid alcohol, also causes neuropathy

A

metronidazole - DNA damaging agent

78
Q

antifolate with broad spectrum coverage, used for UTI, resistance by changes in folate synthesis pathway or drug uptake, adminstered orally, renal impairment increases half life so renal considerations necessary, although renal clearance decreases, can still be used to treat kidney infection,

A

sulfamethoxazole

79
Q

antifolate with gram - coverage, used in UTI, resistance by changes in folate synthesis pathway or drug uptake, administered orally, half life increases with renal impairment

A

trimethoprim

80
Q

fluoroquinolone with broad spectrum activity, used in UTI, abdominal, respiratory, skin and soft tissue infections, and anthrax, resistance is by changes in drug targets or drug efflux pumps, administered orally or IV, no hepatic elimination adjustments necesssary, but minor change to half life with renal impairment, is absorbed well and avoids first pass metabolism

A

ciprofloxacin

81
Q

covers anaerobic organisms and c. diff infection, resistance is by mutations in the rdxA gene, adminstered orally, IV and topically, no elimination dose adjustments necessary

A

metronidazole

ClinSci IV (43 decks)

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