Antibacterials Flashcards

1
Q

Lactulose

A

MOA: degraded by intestinal flora to lactic acid and other acids
Effect: acids trap the ammonia in the GIT so it cannot enter circulation and exacerbate the encephalopathy
Uses: hepatic encephalopathy, use as osmotic laxative, prebiotic
SE: osmotic diarrhea, flatulence, abd pn

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2
Q

Quinolones Drug Interactions

A

Theophylline, NSAIDS, corticosteroids = enhanced toxicity of quinolones
3rd and 4th gen = raide serum levels of Warfarin, Caffeine and Cyclosporine

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3
Q

Clindamycin PK and SE

A

PK: PO or IV, good penetration (gets to abscesses/bones)
SE: C. difficile, GI sx’s, skin rash, neutropenia and impaired liver fxn

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4
Q

2nd Gen Quinolones

A

Ciprofloxacin
Spectrum: extended G-ve activity, some G+ve, and some atypicals
DOC: anthrax
Use: ETEC, Pseudomonas (CF pt’s), meningitis prophylaxis (alt to Ceftriaxone and Rifampin)

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5
Q

Cefaclor / Cefoxitin / Cefotetan / Cefamandole

A

2nd generation Cephalosporins
Active against: H.influenzae, Enterobacter, some Neisseria
Use: sinusitis, otitis infections and LTIs
Cefotetan/Cefoxitin use: prophylaxis and therapy of abd/pelvic cavity infections

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6
Q

Sulfonamides PK, SE, CI

A

PK: PO or topical, acetylated in liver, eliminated via urine
SE: photosensitivity, crystalluria, HS rxn, hematopoietic disturgances (G6PD), kernicterus
CI: newborns/infants < 2 yo
Drug interaction: displace Warfarin, Phenytoin and Methotrexate from albumin

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7
Q

Tetracyclines (names)

A

Doxycycline / Minocycline / Tetracycline

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8
Q

Concentration-dependent Killing

A

Bigger the dose the better effect (covalent bonding so it doesnt matter if you keep giving it, the blockade is already in place)
*e.g. - aminoglycosides

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9
Q

Oxacillin

A

Excretion: renal and biliary
SE: hepatitis
Use: meningitis s/p trauma or surgery (S. aureus)

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10
Q

Aminoglycosides PK and SEs

A

PK: once daily admin, IV only, well distributed, high levels in renal cortex and inner ear
Excretion: kidney
SE: ototoxicity, nephrotoxicity, NM blockade
CI: MG (bc of NM blockade), pregnancy (unless benefits outweigh risks)

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11
Q

Tetracyclines DOC

A

Chlamydia, M. pneumoniae, Lyme dz, cholera, anthrax prophylaxis, RMSF, Typhus
Combo therapy for: H. pylori eradication, Malaria prophylaxis/tx, tx plague, Tularemia, Brucellosis

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12
Q

Polymyxin B

A
Spectrum: G-ve (bactericidal)
MOA: acts as detergent, attach to and distrupt the cell membrane, binds and inactivates endotoxin
Effect: cell lysis
Use: topically for skin infections
SE: nephrotoxic if given systemically
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13
Q

Ampicillin / Amoxicillin

A

‘Extended spectrum penicillins’
MOA: sensitive to β-lactamases, so activity is enhanced w/ β-lactamase inhibitor
PK: Amoxicillin has higher oral bioavailability than other penicillins
Use: children and pregnancy for acute otitis media, GAS pharyngitis, pneumonia, skin infection, UTIs, URIs (H. flu and S. pneumo)
SE: maculopapular rash, C. difficile

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14
Q

Neomycin

A

Use: bowel surgery, adjunct in hepatic encephalopathy, topical infections
SE: dermatitis

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15
Q

Cephalosporins SE

A

Pain @ infections ite, thrombophlebitis, superinfections (C. difficile), kernicterus (pregnancy)

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16
Q

Tetracyclines PK and SE

A

PK: variable PO absorption (decreased by divalent and trivalent cations)
Excretion: kidney
SE: teratogenic (category D), N/V/D, discoloration and hypoplasia of teeth, stunting growth, fetal hepatotoxicity, photosensitization, dizziness

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17
Q

Calvulanic acid / Sulbactam / Tazobactam

A

MOA: β-lactamas inhibitors
Effect: bind to and inactivate β-lactamases
Use: used in fixed combinations w/ specific penicillins but never used as abx themselves

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18
Q

Quinolones PK, SE, CI

A

PK: good oral bioavailability, high Vd, divalent cations interfere w/ absorption, adjust dose w/ renal dysfunction pt
SE: connective tissue damage (tendon rupture), peripheral neuropathy, QT prolongation, superinfections
CI: pregnancy/nursing mother, children < 18

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19
Q

Fosfomycin

A

MOA: inhibition of enolpyruvate transferase
Effect: inhibits CW synthesis
Admin: PO
Use: uncomplicated lower UTI

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20
Q

Aminoglycosides MOA

A

Amikacin / Gentamicin / Tobramycin / Streptomycin / Neomycin
Bactericidal, assoc. w/ serious toxicities so used mostly in combo w/ other Rx
MOA: passively diffuse across membrane of G-ve, then actively transported (O2 dependent) across cytoplasmic membrane then bind irreversibly (covalently) to 30S subunit of ribosome
Effect: prevent complex formation = prevent transcription = death of organism

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21
Q

Penicillin V

A

Administration: PO
Use: URIs, skin infections d/t strep
DOC: GAS pharyngitis
SE: +ve Coomb’s Test

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22
Q

β-lactamase inhibitors

A

Protect penicillins (β-lactams) from inactivation

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23
Q

Vancomycin

A

MOA: binds D-Ala-D-Ala pentapeptide terminus of PG, inhibits transglycosylation
Effect: inhibits CW synthesis and prevents elongation/polymerization of PG
Spectrum: G+ve only (MRSA, enterococci, PRSP)
Resistance G-ve (intrinsic), plasmid-mediated changes in drug permeability, modification of attachment site (adding D-lactate to terminus)

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24
Q

Minimal Bactericidal Concentration (MBC)

A

Lowest concentration of abx that results in a 99.9% decline in colony count after overnight incubation
*MBC of truly bactericidal agent is = to or slightly above the MIC

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25
Q

Respiratory Quinolones

A

Levofloxacin / Moxifloxacin / Gemifloxcin (3rd and 4th gen)
Target: S. pneumoniae, H. influenzae, M. catarrhalis
Use: when 1st line agents have failed, in presence of comorbidities, inpt management

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26
Q

Tetracyclines

A

MOA: entry via passive diffusion and energy-dependent transport, then bind the 30S subunit of ribosome to prevent attachment of animoacyl tRNA
Effect: protein synthesis halted = bacteriostatic
Spectrum: aerobic and anaerobic G+ve and G-ve
Resistance: impaired influx or increased efflux (plasmid-encoded), enzymatic inactivation, proteins that interfere w/ binding
Use: severe acne, rosacea, syphilis (pt’s w/ penicillin allergy)

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27
Q

Nafcillin

A

Excretion: primarily in bile
PK: not good for PO administration

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28
Q

Penicillins SEs

A

HS rxn, diarrhea, interstitial nephritis, hepatitis

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29
Q

Linezolid PK and SE

A

PK: PO, weak inhibitor of MAO, high Vd
SE: BM suppression, neuropathy, lactic acidosis
CI: caution when coadministration of drugs to increase adrenergic and serotonergic neurotransmitter levels

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30
Q

Penicillins resistance

A

Inactivation by β-lactamase, modification of target PBP, impaired penetration, increased efflux by pumps
*MRSA: altered target PBPs (low affinity for β-lactam abs)

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31
Q

Bacitracin

A
MOA: interferes w/ CW synthesis
Active against: G+ve organisms 
Admin: topical use mainly
Use: skin infections etc
SE: nephrotoxic
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32
Q

Macrolides

A

Erythromycin / Clarithromycin / Azithromycin / Telithromycin
Bacteriostatic (bactericidal @ high concentration)
MOA: reversibly bind 23S rRNA of 50S subunit (same binding site as Clindamycin and Chloramphenicol)
Effect: blocks translocation halting transcription

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33
Q

Amoxicillin DOC

A

For endocarditis prophylaxis during dental or respiratory tract procedures (S. viridans)
*Amoxicillin + clavulanic acid is prophylactic for bites

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34
Q

Aminoglycosides DOC

A

Used in combo - septicemia, nosocomial RTIs, complicated UTIs, endocarditis
*once organism is identified these abx are usually d/c’d

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35
Q

Ampicillin Use/SE

A

Used in combo w/ Aminoglycosides to tx Enterococcus and Listeria (meningitis)
SE: pseudomembranous colitis

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36
Q

Chloramphenicol Uses

A

Serious infections resistant to less toxic drugs, or if it can reach the site of infection better it can be used, infections w/ VRE, topical tx of eye infections

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37
Q

Penicillins G Procaine

A

Developed to prolong duration of Penicilling G
Administration: given IM, seldom used (increases resistance)
PK: t1/2 = 12-24h

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38
Q

Co-trimoxazole (TMP-SMX)

A

Trimethoprim + Sulfamethoxazole = bactericidal
MOA: synergistic inhibition of sequential steps in folic acid synthesis
PK: PO, high Vd
DOC: uncomplicated UTIs, PCP, Nocardiosis
Use: toxoplasmosis (alt drug), URI d/t H. inflluenzae, M. catarrhalis
SE: dermatologic, GI, hematolytic anemia, high incidence of SE in AIDS pt
CI: pregnancy

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39
Q

Penicillin G Benzathine

A

Prolongs duration of Penicillin G
Administration: IM
PK: t1/2 = 3-4 wks
DOC: Syphilis, and RF prophylaxis

40
Q

1st Gen Quinolones

A

Nalidixic acid
Spectrum: moderate G-ve activity
Use: uncomplicated UTIs

41
Q

CW Synthesis Inhibitors

A

Require actively proliferating bacteria

42
Q

3rd Gen Quinolones

A

Levofloxacin
Spectrum: G-ve, G+ve, atypicals but especially S. pneumoniae
Use: DOC for prostatitis (E. coli), non-syphilis STDs, CAP, TB, sinusitis, bronchitis

43
Q

Minimal Inhibitory Concentration (MIC)

A

lowest concentration of abx that prevents visible growth of a bacteria (so you have to target above the MIC)

44
Q

Quinolones MOA and Resistance

A

MOA: enter via porins, inhibit topoisomerase II aka DNA gyrase (G-ve) and IV (G+ve)
Effect: inhibit DNA replication
Resistance: efflux pumps, diff subunits of the enzyme target, cross-resistance

45
Q

Sulfonamides

A

MOA: structural PABA analogues so they competitively inhibit dihydropteroate synthase
Effect: inhibition of folic acid synthesis
Resistance: altered enzyme, decreased permeability
Use: topical for infections, PO for simple UTIs

46
Q

4th Gen Quinolones

A

Gemifloxacin / Moxifloxacin
Spectrum: G+ve and anaerobes
Use: CAP

47
Q

Trimethoprim

A

MOA: similar structure to folic acid, inhibits bacterial dihydrofolate reductase
Effect: inhibits purine, pyrimidine and AA synthesis
Spectrum: G+ve and G-ve (bacteriostatic)
Use: UTIs, bacterial prostatitis and vaginitis
PK: excreted via kidney, reaches high concentrations in sex fluids
CI: pregnancy (bc anti-folate effects)

48
Q

Tx of Hepatic Encephalopathy

A

PO Neomycin, Lactulose, PO Vancomycin, PO Metronidazole, Rifaximin (the abx are aiming to reduce the # of intestinal bacteria that are responsible for responsible for the production of ammonia)

49
Q

Ceftriaxone / Cefoperazone / Cefotaxime / Cefatazimide / Cefixime

A

3rd generation cephalosporins
Active against: G-ve cocci, Enterobacteriacae, Neisseria, H. influenzae, Pseudomonas
Cefotaxime/Ceftriaxone: active against pneumococci
Use: prophylaxis fo meningitis, tx Lyme dz
DOC: gonorrhea, meningitis d/t ampicillin-resistant H. influenzae
PK: only generations that reaches adequate levels in CSF

50
Q

Daptomycin

A

MOA: binds to cell membrane via Ca2+ dependent insertion of lipid tail
Effect: depolarization of cell membrane w/ K+ efflux = cell death
Spectrum: resistant G+ve (MRSA, enterococci, VRE, VRSA)
Inactive against: G-ve (ineffective in tx of pneumonia too)

51
Q

Cefepime

A

4th generation Cephalosporins
Admin: IV only
Active against: wide spectrum (H. influenza, Neisseria, E. coli, S.pneumo, Proteus, Pseudomonas)
Use: mixed infections w/ susceptible organisms

52
Q

Abx Combinations (antagonistic or nah)

A

NOT to give: tetracyclines (static) + β-lactam (cidal) = nothing happens if you’re targeting one bacteria
DO give: macrolide (static) + β-lactam (cidal) = good bc macrolide is for atypicals and β-lactam is targeting S. pneumoniae (diff bacteria are targets)

53
Q

Ceftaroline

A

5th generation Cephalosporin
Admin: IV only
Active against: MRSA, similar spectrum to 3rd generations
Use: skin and soft tissue infections d/t MRSA, particularly w/ G-ve confection, CAP (when first-line agents are unsuccessful)

54
Q

Time-dependent Killing

A

Exposure to the drug for longer will cause more of an effect (four small doses better than one big dose)
*e.g. - penicillins, cephalosporins

55
Q

Clindamycin Uses

A

Anaerobic infections, skin and soft tissue infections (Strep, Staph, and some MRSA), combo w/ Primaquine as alt in PCP, combo w/ Pyrimethamine as alt tx for brain Toxoplasmosis, prophylaxis of IE in valvular pt’s w/ penicillin allergy

56
Q

Macrolides Resistance

A

Decreased influx or increased efflux, production of esterase that hydrolyzes the drug, modification of binding site (plasmid encoded)
*complete cross resistance of all macrolides except Telithromycin), partial cross-resistance w/ clindamycin and streptogramins

57
Q

Telithromycin

A

Resistance: no cross-resistance like other macrolides
SE: fatal hepatotoxicity, exacerbations of MG, visual disturbances *(so dont use this abx for minor illnesses)

58
Q

Carbapenems

A

Resistant: β-lactamases
PK: admin IV only,
Active against: penicillinase-producing G+ve, aerobes and anaerobes, Pseudomonas
Inactive against: carbapenemase producers, MRSA
DOC: Enterobacter infections, extended spectrum β-lactamase producing G-ve organisms
SE: N/V/D, sz, allergic rxns

59
Q

CW Synthesis Inhibitors (names)

A

β-lactam abx (penicillins, cephalosporins, carbapenems, monobactams), Vancomycin, Daptomycin, Bacitracin, Fosfomycin

60
Q

Mupirocin

A

Spectrum: G+ve cocci including MRSA and streptococci (but not enterococci)
PK: topical/intranasal
MOA: binds isoleucyl transfer-RNA syhtnetase
Effect: inhibit protein synthesis
Use: intranasal to eradicate nasal colonization w /MRSA, topically to t impetigo or skin infections

61
Q

Vancomycin PK and SE

A

PK: poor oral absorption, given via slow IV infusion, penetrates CSF, Excretion: kidneys
SE: “Red man” syndrome (mediated by histamine release if infused too quickly), ototoxicity, nephrotoxicity

62
Q

Ertapenem

A

Not active against Pseudomonas

63
Q

Metranidazole

A

Bactericidal
Spectrum: anaerobes (bacteriodes and Clostridium)
MOA: requires anaerobic conditions to work, undergoes reduction by ferredoxin
Effect: forms cytotoxic products that interfere w/ nucleic acid synthesis
DOC: C. difficile infections, Bacteriodes, Giardia, Trichomonas
Use: anaerobic/mixed abd infections, vaginitis, brain abscesses, H. pylori eradication (below diaphragm anaerobe infections)

64
Q

Cefamandole / Cefoperazone / Cefotetan SEs

A

Contain methyl-thiotetrazole group and thus can cause hypoprothrombinemia (vitamin K can prevent this), and Disulfiram-like reactions (pt should avoid EtOH)

65
Q

Tigecycline

A

MOA: similar to tetracyclines
Spectrum: work against MDR G+ve, some G-ve and anaerobic organisms
Resistance: Proteus and Pseudomonas (efflux pumps)
Use: complicated skin and intra-abd infections
PK: IV only
Elimination: bile
SE: N/V/D, discoloration of teeth, dizziness, photosensitivity (all same as tetracyclines)
CI: pregnancy and children < 8yo

66
Q

Streptogramins

A

Quinupristin / Dalfopristin (alone they’re bacteriostatic)
*given together as combo so they are bactericidal
MOA: they bind to separate sites on 50S ribosome
Spectrum: G+ve cocci, MDR bacteria (Streptococci, PRSP, MRSA, E. faecium)
PK: IV only, penetrates Mϕ and PMNs, inhibit CYP-3A4
Use: restricted to tx of infections d/t drug resistant Staph or VRE
SE: GI sx’s, HA, infusion related sx’s

67
Q

Penicillin + Aminoglycoside

A

MOA: synergistic bc penicillins facilitate movement of aminoglycosides through the CW
Administration: placed in different infusion fluid (diff IVs etc)
Use: empiric tx for infective endocarditis

68
Q

Methicillin / Nafcillin / Oxacillin / Dicloxacillin

A

Resistance: β-lactamase resistant
Use: β-lactamase producing staphylococci, first line for staph endocarditis
Excretion: via bile bc they’re lipid soluble

69
Q

Penicillins

A

Structure: β-lactam ring
MOA: bactericidal; inhibit last step in PG synth through binding PBPs in cytoplasmic membrane and autolysin production
Effect: CW synthesis disrupted, bacterial lysis induced
Spectrum: ability to reach target PBPs based on size/charge/hydrophobicity, Gram staining (+ve is more sensitive in penicillins)

70
Q

Metranidazole PK and SE

A

PK: PO, IV, rectal or topical; high Vd
Elimination: hepatic
SE: GI sx’s, neuropathy, dark urine, metallic taste, Disulfiram-like effect (avoid EtOH)
CI: 1st trimester

71
Q

Imipenem PK and SE

A

PK: nephrotoxic bc of its metabolism by dehydropeptidase I so must be given w/ enzyme inhibitor (Cilastatin) to prevent the metabolism and nephrotoxicity
SE: seizures at high levels

72
Q

Doxycycline

A

Lipid soluble so preferred for parenteral administration and good choice for STDs and prostatitis
Excretion: bile
SE: dizziness

73
Q

Ceftriaxone and Cefoperazone Elimination

A

Excreted by bile not kidneys

74
Q

Macrolides DOC

A

M. pneumonie

75
Q

Linezolid

A

*Bacteriostatic for most organisms, -cidal for Strep and C. perfringens
Spectrum: G+ve including MRSA and VRE, some activity against M. tuberculosis
MOA: binds unique site on 23S ribosomal RNA of 50S subunit (no cross-resistance)
Effect: inhibits formation of 70S initiation complex = halting transcription
Resistance: decreased binding, point mutation of RNA
Use: tx MRD infections

76
Q

Best drugs for targeting anaerobes?

A

Clindamycin (infections above diaphragm) and Metranidazole (infections below diaphragm)

77
Q

Macrolides Spectrum

A

G+ve (some activity against G-ve), similar to penicillins (Erythromycin has smaller spectrum than the other 3)

78
Q

Streptomycin DOC

A

Plague (Y. pestis)

79
Q

Macrolides PK and SE

A

PK: CYP inhibition (EXCEPT for Azithromycin)
SE: GI irritation, hepatic probs (erythromycin and azithromycin, QT prolongation, anyphylaxis is rare

80
Q

Sulfasalazine Use

A

PO for UC, enteritis, IBD

81
Q

Macrolides Uses

A

Tx of CAP, tx of URT or soft tissue infections (Staph, H. influenzae, S. pneumoniae, enterococci), used in pt w/ penicillin allergy

82
Q

Cefazolin / Cephalexin

A

1st generation Cephalosporins
Active against: G+ve cocci, Proteus, E. coli, Klebsiella
Resistant: staph penicillinase
Use: penicillin G substitutes
DOC (Cefazolin): parenterally for surgical prophylaxis

83
Q

Daptomycin Uses, PK, SE

A

Use: severe infections d/t MRSA or VRE, tx of complicated skin infections d/t S. aureus
PK: IV only, eliminated by kidneys
SE: constipation, nausea, HA, insomnia, rhabdomyolysis (so monitor CK and d/c coadministratoin of statins)

84
Q

Vancomycin Uses

A

Tx infections d/t β-lactam resistant G+ve (or pt’s allergic to β-lactams), used in combo w/ aminoglycoside for empirical tx of IE ❤️, enterococcal endocarditis or PRSP, given PO for tx of Staph enterocolitis or abx-assoc C. difficile

85
Q

Fidaxomicin

A

Spectrum: C. difficile
MOA: binds and inhibits RNA polymerase
Effect: inhibits protein synthesis
Use: tx recurrent C. difficile in adults

86
Q

Carbenicillin / Ticarcillin / Piperacillin

A

‘Antipseudomonal’
Spectrum: broad but especially Pseudomonas
MOA: often combined w/ β-lactamase inhibitor
Use: injectible tx for G-ve, tx of moderate-severe infections of susceptible organisms

87
Q

Erythromycin

A

PK: less PO absorption, shorter t1/2, less bioavailability than other macrolides, CYP inhibitor
DOC: Whooping cough (Bordatella pertussis)
SE: hepatic probs

88
Q

Chloramphenicol

A

MOA: enters via active transport and reversibly binds 50S subunit (site adjacent to site of macrolides and clindamycin)
Effect: inhibits peptidyltransferase = stops protein synthesis (bacteriostatic)
Spectrum: broad (G+ve and G-ve, aerobes and anaerobes), esp N. meningitidis, H. influenzae, Salmonella and baceriodes
Resistance: acetyltransferases inactivate drug, changes in membrane permeability

89
Q

Aminoglycosides Resistance

A

Inactivate drug by acetylation, phosphorylation and adenylation (plasmid-encoded), altered receptor protein on 30S subunit

90
Q

Aztreonam SEs

A

Skin rashes or elevation of serum aminotransferases and GI upset,

91
Q

Chloramphenicol PK and SE

A

PK: PO, IV and topical, high Vd (enters CSF), inhibits CYP-3A4 and CYP-2C9
SE: GI sx’s, BM suppression (dose-related), Gray baby syndrome d/t drug accumulation in newborns

92
Q

Penicillins G

A

aka Benzylpenicillin
Administration: IV only
Active against: G+ve cocci (not staph), Listeria, C. perfringens, Neisseria sp, anaerobes
DOC: syphilis, strep (esp RF), pneumococci
SE: +ve Coombs’ Test

93
Q

Cephalosporins

A

β-lactam
MOA: same as penicillin (bactericidal)
Inactive against: LAME (Legionella/Listeria, actinobacter, Mycoplasma, Enterococcus)
PK: mainly admin IV, elimination mainly by kidneys

94
Q

Nitrofurantoin

A

Bacteriostatic/bactericidal
Spectrum: G+ve and G-ve (specifically E. coli)
MOA: reduced then the drug intermediate causes DNA damage
Effect: cell lysis
Use: prophylaxis and tx of lower UTI
PK: rapid elimination
SE: anorexia, N/V, neuropathies, hemolytic anemia (G6PD), colors urine brown
CI: renal insufficiency, pregnancy after 38 wks gestation, infants < 1 mo

95
Q

Clindamycin

A

MOA: binds 50S subunit (same as macrolides)
Effect: inhibits translocation (bacteriostatic)
Spectrum: good for G+ve anaerobes, bacteriodes and G+ve aerobes
Resistance: modified receptor site, enzymatic inactivation, G-ve aerobes and enterococci intrinsically resistant
*cross-resistant w/ macrolides

96
Q

Aztreonam

A

Monobactam
MOA: same as all
PK: IV or IM, via inhalation in CF pt’s, penetrates CSF
Elimination: urine
Spectrum: aerobic G-ve rods only (Pseudomonas esp)
Inactive against: G+ve and anaerobes
Resistance: β-lactamases
Use: UTI, LTI, septicemia, skin/suture infections, intraabd infections, gym infections d/t susceptible G-ve’s