Antimicrobials Flashcards

(90 cards)

1
Q

Penicillin forms

A

Penicillin G (IV & IM), Pen V (oral)

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2
Q

Penicillin mech

A

bind pen-binding proteins (transpeptidases)

block transpeptidase cross-linking of peptidoglycan. activate autolytic enzymes

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3
Q

Penicillin use

A

gram (+) - S. pneumo, S. pyo, Actinomyces
Neisseria meningitidis, Treponema pallidum (+ syphilis in pregnant women)
Bactericidal for gram (+) cocci & rods, gram (-) cocci, spirochetes. NOT penicillinase resistant

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4
Q

Penicillin tox

A

hypersensitivity, hemolytic anemia

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5
Q

Penicillin Resistance

A

Beta-lactamases cleave Beta lactam ring

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6
Q

Penicillinase-resistant penicillins

A

oxacillin, nafcillin, dicloxacillin

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7
Q

oxacillin, nafcillin, dicloxacillin mech

A

same as penicillin. Narrow spectrum. Penicillinase resistant b/c bulky R-group blocks access

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8
Q

oxacillin, nafcillin, dicloxacillin use

A

S. aureus (except MRSA)

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9
Q

oxacillin, nafcillin, dicloxacillin resistance

A

MRSA resistant due to altered pen-binding protein target site

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10
Q

oxacillin, nafcillin, dicloxacillin tox

A

interstitial nephritis, hypersens

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11
Q

Aminopenicillins

A

ampicillin, amoxicillin

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12
Q

Aminopenicillin mech

A

same as penicillin. wider spectrum. Penicillinase sensitive. Combo w/CAST to protect against Beta-lactamase. amOxicillin has greater Oral availability.

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13
Q

Aminopenicillin use

A

Extended-spectrum penicillin:

HELPSS - H. flu, E. coli, Listeria, Proteus mirabilis, Salmonella, Shigella, enterococci

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14
Q

Aminopenicillin tox

A

pseudomembranous colitis, hypersens, ampicillin rash

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15
Q

Aminopenicillin resistance

A

Beta-lactamases cleave ring

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16
Q

Antipseudomonals

A

ticarcillin, piperacillin

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17
Q

ticarcillin, piperacillin mech

A

same as penicillin, extended spectrum

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18
Q

ticarcillin, piperacillin use

A

Pseudomonas spp. & gram (-) rods & anaerobics. Susceptible to penicillinase - use w/CAST.

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19
Q

ticarcillin, piperacillin tox

A

hypersensitivity reactions

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20
Q

Beta-lactamase inhibitors

A

CAST: Clavulanic Acid, Sulbactam, Tazobactam

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21
Q

Bacteroid (type & treatment)

A

gram (-), anaerobic rods

Tx: piperacillin, tazobactam

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22
Q

Cephalosporin mech

A

Beta-lactam drugs that inhibit cell wall synth but are less susceptible to penicillinases. Bactericidal.

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23
Q

Organisms not covered by cephalosporins

A

are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA, Enterococci

Exception: ceftaroline covers MRSA

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24
Q

1st generation Cephalosporins

A

cefazolin, cephalexin

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25
1st gen Cephalosporins use
gram (+) cocci | PEcK - Proteus mirabilis, E. coli, Klebsiella pneumo
26
Cefazolin use
prior to surgery to prevent S. aureus wound infections
27
2nd gen cephalosporins
cefoxitin, cefaclor, cefuroxime
28
2nd gen cephalosporins use
gram (+) cocci | HEN PEcKS - H. flu, Enterobacter, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumo, Serratia marcescens
29
3rd gen cephalosporins
ceftriaxone, cefotaxime, ceftazidime
30
3rd gen cephalosporins use
serious gram (-) infections resistant to other Beta-lactams.
31
Ceftriaxone use
meningitis & gonorrhea
32
Ceftazidime use
psuedomonas
33
4th gen cephalosporins
cefepime
34
4th gen cephalosporin use
increased activity against pseudomonas & gram (+) organisms
35
Cephalosporin tox
Vit K deficiency, Hypersensitivity reactions, low cross-reactivity with penicillins, increased nephrotoxicity of aminoglycosides.
36
Aztreonam mech
monobactam resistant to Beta-lactamases. prevents peptidoglycan cross-linking by binding PBP3. Synergystic w/aminoglycosides. No cross-allergenicity w/penicillins.
37
Aztreonam use
Gram (-) Rods ONLY (Klebsiella, E. coli, Serratia, Shigella, Salmonella, Proteus, Pseudomonas, H. pylori). No activity against gram (+)s or anaerobes. For penicillin allergic patients and those with renal insufficinecy who cannot tolerate aminoglycosides.
38
Aztreonam tox
usually nontoxic. GI upset.
39
Imipenim/cilastatin, meropenem mech
Imipenem is broad-spectrum, Beta-lactamase resistant carbapenem. Always administered w/cilastatin (inhibitor of renal dehydropeptidase I) to decrease inactivation of drug in renal tubules.
40
Carbapenems
Imipenim/cilastatin, meropenem, ertapenem, doripenem
41
Imipenem/cilastatin, meropenem use
gram (+) cocci, gram (-) rods, anaerobes. Wide spectrum, but significant side effect
42
Imipenem/cilastatin, meropenem tox
GI distress, rash, CNS tox (seizures) at high plasma levels | **meropenem has reduced risk of seizures & is stable to dehydropeptidase I
43
Vancomycin mech
Inhibits cell wall peptidoglycal formation by binding D-ala D-ala portion of cell wall precursors. Bactericidal.
44
Vancomycin use
Gram (+) only. serious, multidrug resistant organisms including MRSA, enterococci, & C. diff. (oral dose for membranous colitis)
45
Vancomycin tox
Nephrotox, Ototox, Thrombophlebitis, diffuse flushing (Red Man Syndrome - prevent with pretx antihistamines & slow infusion rate). Well tolerated in general - NOT many problems.
46
Vancomycin resistance
AA change of D-ala D-ala to D-ala D-lac.
47
30S inhibitors
Aminoglycosides (bactericidal) | Tetracyclines (bacteriostatic)
48
50S inhibitors
Chloramphenicol, Clindamycin (static) Erythromycin (macrolides) (static) Linezolid (variable)
49
Aminoglycosides
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin "Mean" (aminoglycosides) GNATS caNNOT kill anaerobes
50
Aminoglycoside mech
B.cidal; inhibits formation of initiation complex -> misreading of mRNA; also blocks translocation. Require O2 for uptake (ineffective against anaerobes.
51
Aminoglycoside use
Severe gram (-) infections. Synergystic w/Beta-lactam antibiotics. Neomycin for bowel surgery
52
Aminoglycoside tox
Nephrotox (especially w/cephalosporins), Neuromuscular blockade, Ototox (esp w/loop diuretics), Teratogen "Mean" (aminoglycosides) GNATS caNNOT kill anaerobes
53
Aminoglycoside resistance
transferase enzymes that inactivate the drug by acetylation, p'lation, adenylation
54
Tetracyclines
Tetracycline, doxycycline, demeclocycline, minocycline.
55
Demeclocycline
ADH antagonist; acts as a diuretic in SIADH. Rarely used as antibiotic even though is classified as tetracycline.
56
Tetracycline mech
B.static. Binds 30S @ A site to prevent attachment of aminoacyl-tRNA. Limited CNS penetration. Doxycycline is fecally eliminated - can be used in pts w/renal fail. Do not take w/milk, antacids, iron-containing preps b/c divalent cations inhibit its absorption in the gut.
57
Tetracycline use
Borrelia burgdoferi, M. pneumo, Rickettsia, Chlamydia. Accumulation intracellularly makes effective against latter 2.
58
Tetracycline Tox
GI distress, discoloration of teeth & inhibition of bone growth in children. Photosensitivity. Contraindicated in pregnancy.
59
Tetracycline resistance
decreased uptake into cells or increased efflux out of cell by plasmid encoded transport pumps.
60
Macrolides
Azithromycin, clarithromycin, erythromycin
61
Azithromycin, clarithromycin, erythromycin MECH
Inhibit protein synth by blocking translocation ("macroslides"); bind 23S rRNA of the 50S ribosomal subunit. B.static. Accumuates in WBCs that transport to site of infection.
62
Azithromycin, clarithromycin, erythromycin USE
Atypical pneumonias (Mycoplasma, Chlamydia, Legionella), STDs (chlam), gram (+) cocci (strep infections in pts allergic to pen)
63
Azithromycin, clarithromycin, erythromycin TOX
MACRO: dysMotility, Arrythmia -> long QT, Cholestatic hepatitis, Rash, eOsinOphilia. Increases serum [ ] of theophyllines, oral anticoags
64
Azithromycin, clarithromycin, erythromycin RESIST
Methylation of 23S rRNA binding site.
65
Chloramphenicol mech
blocks peptidyltransferase at 50S ribosomal subunit. B.static
66
Chloramphenicol use
Meningitis (H. flu, neisseria men, S. pneumo). Conservative owing to tox. Used in developing countries due to low $
67
Chloramphenicol tox
``` Anemia (dose dependent) Aplastic anemia (dose independent, pancytopenia) gray baby syndrome in premies - lack liver UDP-glucuronyl transferase ```
68
Chloramphenicol Resist
Plasmid-encoded acetyltransferase that inactivates drug
69
Clindamycin mech
blocks peptide transfer (transpeptidation) at 50S ribosomal subunit. B.static
70
Clindmycin use
Anaerobic infections (Bacteroides fragilis, C. perfringens) in aspiration pneumonia or lung abcesses or oral infection w/mouth anaerobes.
71
Clindamycin tox
pseudomembranous colitis (C. diff overgrowth), fever, diarrhea
72
Sulfonamides
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine
73
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine. MECH
PABA metabolites inhibit dihydropteroate synthase. B.static.
74
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine. USE
gram (+), gram (-), Nocardia, Chlamydia, Triple sulfas or SMX for simple UTI
75
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine. TOX
Hypersensitivity rxns, hemolysis w/G6PD deficiency, nephrotox (tubulointerstitial nephritis), photosens, kernicterus in infants, displace other drugs from albumin (ex-warfarin)
76
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine. RESIST
Altered enz (bacterial dihydropteroate synthase), decreased uptake, or increased PABA synth
77
Trimethoprim MECH
Inhibits bacterial dihydrofolate reductase. b.static
78
Trimethoprim USE
Used in combo w/SMX, causes sequential block of folate synth. Combo used for UTIs, shigella, salmonella, pneumocystis jirovecii pneumonia (Tx & prophy)
79
Trimethoprim TOX
Megaloblastic anemia, leukopenia, granulocytopenia. Alleivate w/supplemental folinic acid = leucovorin rescue
80
Fluoroquines
Ciprofloxacin, norfloxacin, levofloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin (fluoroquinolones), nalidixic acid (quinolone)
81
Fluoroquinolones MECH
Inhibit DNA gyrase (topo II), and topo IV. B.cidal. Must not be taken w/antacids.
82
Fluoroquinolones USE
gram (-) rods of urinary & GI tracts (pseudomonas), neisseria, some gram (+)
83
Fluoroquinolones TOX
GI upset, superinfections, skin rashes, headache, dizziness, tendonitis, tendon rupture, leg cramps, myalgias. Long QT. Tendon rupture age >60 or if taking prednisone.
84
Fluoroquinolones Contraindications
Pregnant women & children -> damaged cartilage.
85
Fluoroquinolones RESIST
Chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps.
86
Metronidazole MECH
Forms free radical toxic metabolites in the bacterial cell that damage DNA. B.cidal, antiprotozoal.
87
Metronidazole USE
Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (bacteroides, C. diff), H. Pylori (w/proton pump inhibitor & clarithromycin as triple therapy) GET GAP on the Metro Treats anaerobic BELOW diaphragm Clindamycin tx ABOVE diaphragm
88
Metronidazole TOX
Disulfiram-like rxn with alcohol; headache, metallic taste
89
MRSA tx
vancomycin
90
VRE tx
linezolid & streptogamins (quinupristin/dalfopristin)