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Milly > Abx > Flashcards

Abx Flashcards

1
Q

Penicillins

  • MOA, ​
  • Side Effects
A

MOA:

  1. Bind penicillin binding proteins
  2. Block transpeptidase cross-linking of cell wall
  3. Activate autolytic enzymes (Bactericidal)

Side Effects:
Hypersensitivity reaction (with cross alergenicity)
Hemolytic anemia

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2
Q

Penicillin G / Penicillin V

  • Class
  • Target Organism/Use,
  • Administration route
A

Class - 1st generation PCNs

Target Orgs/Use:
Gram+ orgs (Grp A Strep, S. pneumoniae, Actinomyces);
Treponema pallidum (syphilis);
Bactericidal for Gram+ cocci, gram+ rods, gram- cocci and spirochetes

Administration:
PCN G - IV or IM (with anesthetic to increase t1/2)
PCN V - oral

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3
Q

Benzylpenicillin is AKA:

A

Penicillin G

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4
Q

Penicillin G is AKA:

A

Benzylpenicillin

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5
Q

penicillin V is AKA:

A

Phenoxymethylpenicillin

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6
Q

Methicillin / nafcillin / dicloxacillin / oxacillin

  • Class
  • Target Organisms/Use
  • Side Effects,
  • Administration route
A

Class -
2nd generation PCNs (narrow spectrum, b-lactamase resistant due to bulkier R-group)

Target Orgs/Use -
S. aureus (excep MRSA-altered penicillin binding protein)

Side Effects:
Methicillin - allergic interstitial nephritis Nafcillin/Oxacillin - hepatitis (some hepatic excretion)

Administration - Dicloxacillin oral

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7
Q

Amoxicillin/Ampicillin

  • Class,
  • Target Organisms/Use,
  • Side Effects,
  • Administration route
A

Class - Aminopenicillins - 3rd generation PCNs (wider spectrum than 1st gen, b-lactamase sensitive)

Target Orgs/Use:
Gram- rods and enterococcus:
“H.E.L.P.S. kill enterococcus” (H. flu, E. coli, Listeria, Proteus, Salmonella)
H. pylori triple therapy

Side Effects - hypersensitivity reactions, ampicillin rash, pseudomembranous colitis

Administration: Amoxicillin oral with food
Can be given with b-lactam inhibitor to enhance spectrum

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8
Q

Mezlocillin/Piperacillin

  • Class,
  • Target Orgs/Use
A

Class - 4th generation PCN (Ureidopenicillins) - Extended sprectrum, susceptible to b-lactamase (use w/ b-lactamase inhibitor)

Target Orgs/Use - Pseudomonas, and gram neg rods

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9
Q

Carbenicillin/Ticarcillin

  • Class,
  • Target Orgs/Use,
  • Side Effects
A

Class - 4th generation PCN (Carboxypenicillins) - Extended spectrum, b-lactamase sensitive (use w/ b-lactamase inhibitor)

Target Orgs/Use - Pseudomonas, gram neg rods

Side Effects - Disodium salts that can produce large salt load

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10
Q

Clavulanic acid/Sulbactam/Tazobactam

  • Class,
  • MOA,
  • Target Orgs/Use
A

Class - b-lactamase inhibitors (given in combination with b-lactam abx)

MOA - (No antimicrobial activity) covalent inhibitors of b-lactamase

Target Orgs/Use: Effective in conjunction with 3-4 gen PCN against Gram- b-lactamases and S. aureus
NOT effective for chromosomal b-lactamase of Pseudomonas, Enterobacter, Citrobacter, Serratia,

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11
Q

B-lactam Resistance mechanisms:

A

3 Strategies:

1. Decrease penetration - Gram- orgs let b-lactam in via porin - change porin to restrict entry (ex. Pseudomonas)

2. Alter PCN binding protein (ex. MRSA via mec locus, S. pneumoniae via transformation)

3. B-lactamase

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12
Q

Cephalosporins

  • MOA,
  • Side Effects
A

MOA - Bactericidal b-lactam drugs that inhibit cell wall synthesis, but less susceptible to penicillinases

Side Effects:

  • Hypersensitivity reaction (5-10% cross hypersensitivity with PCN)
  • Vitamin K deficiency (Cefotetan, Cefonicid, Cefoperazone)
  • Disulfuram-like reaction w/ethanol (Cefotetan, Cefonicid, Cefoperazone)
  • Increase the nephrotoxicity of Aminoglycosides
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13
Q

Cephalexin / Cephapirin / Cephalothin / Cefazolin

  • Class,
  • Target Orgs/Use,
  • Metabolism
A

Class - 1st gen Cephalosporins

Target Orgs/Use -
Gram+ cocci (MSSA, Streptococci),
Enterobacteriaceae (“PEcK” - Proteus, E. coli, Klebsiella)

Metabolism:
Cephalothin - deacylated by liver (not good for meningitis, b/c deacylated form competes with active form for transport to CSF)
Cephapirin - deacylated by liver but w/ active metabolites

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14
Q

Cefuroxime/ Cefoxitin / Cefaclor / Cefotetan / Cefonicid

  • Class,
  • Target Orgs/Use,
  • Side Effects
A

Class - 2nd Generation Cephalosporins

Target Orgs/Use: More stable vs. gram- orgs (HEN PEcKS - Haemophilus influenzae, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia) than 1st-gen cephalosporins
Less active vs. Gram+ cocci/S.aureus than 1st-gen

Side Effects: (Cefotetan/Cefonicid - MTT side chain ) 1. Inhibits Vitamin K mediated gamma carboxylation

  1. Associated with Disulfuram-like reaction with alcohol (throbbing of neck, headache, nausea, etc)
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15
Q

Ceftazidime / Ceftriaxone / Cefotaxime / Cefoperazone

  • Class,
  • Target Orgs/Uses,
  • Side Effects,
  • Metabolism
A

Class - 3rd generation Cephalosporins

Target Orgs/Uses: Broader activity vs. Gram- Ceftriaxone - meningitis and gonorrhea
Ceftazidime - Pseudomonas

Side Effects: (Cefoperazone - MTT side chain)

  1. Inhibits Vitamin K mediated gamma carboxylation
  2. Associated with Disulfuram-like reaction with alcohol (throbbing of neck, headache, nausea, etc)
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16
Q

Cefepime

  • Class,
  • Target Orgs/Uses
A

Class - 4th generation Cephalosporin

_Target Orgs/Uses_: More resistant to destruction by chromosomal b-lactamase
Increased activity (over 3rd gen) vs. Pseudomonas and gram+
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17
Q

Aztreonam

  • Class,
  • MOA,
  • Target Orgs/Use,
  • Side Effects
A

Class - Monobactam

MOA -
b-lactam antibiotic (but only binds gram Neg transpeptidase PBP-3);
Inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking;
**resistant to (some, not all) b-lactamases
(synergistic** w/ aminoglycosides)

Target Orgs/Use -
Facultative Gram Neg bacteria (resistant to b-lactamase) -
Use for PCN-allergic pts; Safe to admininister aztreonam to patients with **hypersensitivity **(allergies) to penicillins and

those w/ renal insufficiency who cannot tolerate aminoglycosides;

Side Effects - Rare (diarrhea/rash),
NO cross-alergenicity with PCN,
Can trigger seizures in patients with history of seizures

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18
Q

Imipenem / Meropenem

  • Class,
  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Metabolism,
  • Resistance
A

Class - Carbapenem

MOA - b-lactam antibiotic resistant to all b-lactamases

Target Orgs/Use: Broadest spectrum abx (but side effects limit use)
Imipenem - More active vs. Gram+ cocci
Meropenem - More activity vs. Gram- rods

Side Effects: Cross reactivity with PCN
Imipenem must be infused slowly or causes GI distress
Imipenem causes seizures (pts at increase risk - renal insufficiency)

Metabolism: Imipenem - hydrolyzed by peptidase on renal tubular cells (coadmin with cilastatin - dipeptidase inhibitor)

Resistance: Pseudomonas - porin mutation Carbapenemase may arise

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19
Q

Vancomycin

  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Administration,
  • Metabolism,
  • Resistance
A

MOA - Inhibits cell wall mucopeptide formation, by binding to D-ala-D-ala portion of the cell wall precursors. Bactericidal.

Target Orgs/Use: Gram+ bacteria including MRSA and Enterococcus
Used for all gram+ infections in PCN allergic pt
Used oral to treat C. difficile

Side Effects: (NOT many)
Nephrotoxicity (especially with aminoglycosides)
Ototoxic
Thrombophlebitis
“Red man syndrome” (HM release) - diffuse flushing (prevent w/antiHM and slow infusion)

Administration - Given IV (except for to tx C. diff)

_Resistance_:
Block penetration (Gram- bacteria mode of resistance)   
Plasmid genes altering structure of cell wall to D-ala-D-lac (some Gram+ strains)
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20
Q

In Pharm, Intrathecal refers to:

A

a route of administration for drugs via an injection into the spinal canal,

more specifically into the subarachnoid space so that it reaches the CSF

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21
Q

Chloramphenicol

  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Resistance
A

MOA - Bacteriostatic, Inhibits protein synthesis by: binds to the 23S rRNA part of the 50S ribosome and inhibits peptide bond formation

Target Orgs/Use - Broad spectrum used in developing world (not used in US) for Meningitis (covers H. flu, N. meningiditis, S. pneumoniae)

Side Effects:
Dose-dependent irreversible aplastic anemia and reversible BM suppression,
“Gray baby syndrome” due to failure of glucuronidation in liver of neonates (can lead to circulatory collapse and death),
Hemolysis in pts with G6PD deficiency

Resistance - plasmid-encoded acetyl transferase that inactivates drug

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22
Q

Clindamycin

  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Resistance
A

MOA - Bacteriostatic, binds to 23S rRNA portion on the 50S ribosomal subunit and blocks chain elongation (peptide bond formation)

Target Orgs/Use - Anaerobes (above diaphragm - aspiration pneumonia/lung abscess)

Side Effects - Pseudomembranous colitis due to overgrowth of C. diff

Resistance - Plasmid encoded resistance due to methylation of 23S rRNA binding site, leading to decreased binding by clindamycin

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23
Q

Linezolid

  • MOA,
  • Target Orgs/Use,
  • Side Effects
A

MOA - Binds 23S portion of 50S ribosomal subunit and blocks formation of initiation complex

Target Orgs/Use - Gram+ cocci (including MRSA, VRE and b-lactam resistant pneumococcal disease)

Side Effects - BM suppression, MAO inhibitor (toxicity with tyramine or other related drugs)

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24
Q

Erythromycin, Azithromycin, Clarithromycin

  • Class,
  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Resistance
A

Class - Macrolide (Inhibitor of protein synthesis), Azithromycin/Clarithromycin are long-acting

MOA - Bacteriostatic, binds to 23S rRNA on 50S ribosomal subunit and blocks chain elongation (blocks translocation)

_Target Orgs/Use_:
Atypical pneumonias (mycoplasma, chlamydia, legionella) URIs, STDs Gram+ cocci (strep infections in pts allergic to PCN) Neisseria
Azithromycin - MAC (M. avium intracellulare) prophylaxis and treatment

Side Effects:
Nausea/Diarrhea (motilin agonist) - worse w/ Erythromycin
Cholestatic hepatitis
Inhibits P-450 enzymes - increases concentration of warfarin and theophylline [*Azithromycin is an EXCEPTION b/c it does Not inhibit CYP3A4],
Eosinophilia, skin rash ,
QT prolongation (mostly Erythromycin) ,
Teratogen (Clarithromycin)

Resistance: Plasmid encoded resistance due to methylation of 23S rRNA -< decreased binding

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25
Q

Tetracycline / Minocycline / Doxycycline / Demeclocycline

  • Class,
  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Administration,
  • Metabolism,
  • Resistance
A

Class - Tetracycline (Inhibitor of protein synthesis)

MOA - Bacteriostatic, binds 30S ribosome and inhibits tRNA binding

Target Orgs/Use: Atypical orgs (Chlamydia, Mycoplasma pneumoniae, Rickettsia, Brucella, Leptospira, B. burgdorferi) H. pylori triple therapy Demeclocycline - ADH antagonist (diuretic in SIADH)

Side Effects:
Bind newly synthesized bone and discolors teeth (don’t give pregnant women/kids)
Photosensitivity
skin rash (esp Doxycycline)
GI distress

Administration: Given Oral (only doxycycline can be given IV - others cause thrombophlebitis)
Antacids, milk/dairy products inhibit absorption (divalent cations inhibit absorption)

Metabolism: Renal + hepatic excretion
Doxycycline hepatic excretion (can be used in pts w/renal failure)

Resistance - Decrease uptake into cells of increase efflux out of cell by plasmid-encoded transport pump

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26
Q

In Pharm, parenteral refers to:

A

routes other than the digestive tract.

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27
Q

Gentamicin / Neomycin / Amikacin / Tobramycin / Streptomycin

  • Class,
  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Bioavailability,
  • Metabolism,
  • Resistance
A

Class - Aminoglycosides (Inhibitor of protein synthesis)

MOA - Bactericidal; Binds 30S ribosomal subunit blocking formation of initiation complex (Low conc - mRNA misread, High conc - translation inhibited)

Target Orgs/Use: Active vs. organisms with ETC (use ETC to get in cell) Severe gram- rod infection, synergistic w/ b-lactam antibiotics (b-lactam facilitates entry) ,
Neomycin for bowel surgery

Side Effects:
Reversible nephrotoxicity (especially w/cephs) Irreversible ototoxicity (kill cochlear hair cells) - especially w/ loop diuretics;
Teratogen

Resistance:

  • *1.** Block penetration (Anaerobes, streptococci - no ETC so resistant)
  • *2.** Alter binding target (more common with Streptomycin)
  • *3.** Inactivate Abx by acetylation, phosphorylation or adenylation with enzyme (typically plasmid/transposon mediated)
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28
Q

Nalidixic Acid

  • Class,
  • MOA
A

Class - First generation Quinolone

MOA - Bactericidal, Inhibits DNA Gyrase

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29
Q

Ciprofloxacin

  • Class,
  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Administration,
  • Metabolism,
  • Resistance
A

Class - 2nd-gen Fluoroquinolone

MOA - Bactericidal, Inhibits DNA Gyrase

Target Orgs/Use -
Gram- rods of urinary/GI tracts (UTIs/Gastroenteritis) including Pseudomonas, Neisseria,
Some Gram+ orgs (e.g., MSSA but not MRSA)

Side Effects:
Tendonitis and tendon rupture (adults)
Leg cramps,
myalgias (kids)
Potential for cartilage damage (contraindicated in pregnancy and children)
GI upset,
superinfections,
skin rash,
headache,
dizziness
QT prolong,
Stevens-Johnson syndrome

Administration:
Do Not take w/ Oral or IV Antacids (Mg++ or Al+++), nor w/ iron, calcium, zinc, dairy, food,
HM blockers delay absorption

Resistance - Chromosomal-encoded mutation in DNA gyrase

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30
Q

Metronidazole

  • Class,
  • MOA,
  • Target Orgs/Uses,
  • Side Effects,
  • Resistance
A

Class - DNA Synthesis inhibitors

MOA - Bactericidal/antiprotozoal, Forms free radical toxic metabolites in the bacterial cell that damage DNA

Target Orgs/Use:
“GET GAP”
G iardia E ntamoeba T richomonas vaginalis G ardnerella vaginalis A naerobes (except Actinomyces) H. p ylori (triple therapy w/ amoxicillin or tetracycline and bismuth)

Side Effects:
Associated with Disulfuram-like reaction with alcohol (throbbing of neck, headache, nausea, etc)
Metallic taste in the mouth

Resistance - Actinomyces intrinsically resistant

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31
Q

Rifampin

  • MOA,
  • Target Orgs/Uses,
  • Side Effects,
  • Bioavailability, Metabolism,
  • Resistance
A

MOA - Bactericidal, Inhibit DNA-dependent RNA polymerase (inhibit txn initiation)

Target Orgs/Use: Mycobacterium tb (Hansen’s disease) combo agent (rapid drug resistance if used alone);
Delays resistance to dapsone when used for leprosy;
Meningococcal and H. flu B prophylaxis

Side Effects/Metabolism:

Turns urine, tears, sweat redish/orange
Induces Cyp-450 -< reduce blood levels of many drugs 4 R’s of Rifampin - RNA pol inhibitor, Revs up P450s, Red body fluid, Rapid resistance

Resistance:
Enterobacteriaceae family, and **Acinetobacter **and **Pseudomonas **genuses are intrinsically resistant to rifampicin.

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32
Q

Sulfonamides and Trimethoprim

  • MOA,
  • Target Orgs/Use,
  • Side Effects,
  • Bioavailability, Metabolism,
  • Resistance
A

MOA - Bactericidal together (bacteriostatic alone), Competitively inhibit folate metabolism in different steps:
Trimethoprim inhibits DHFR;
Sulfonamides inhibit folate synthesis (block dihydropteroate synthetase)

Target Orgs/Use -
UTIs,
Prophylaxis and tx of PCP in AIDS pts,
Gram+ (including MRSA), Gram-, Salmonella, Shigella, Nocardia, Chlamydia

Side Effects:
Rash/skin reaction (as severe as SJS)
Hemolysis if G6PD deficient
Nephrotoxicity (interstitial nephritis)
Megaloblastic anemia
Displace other drugs from albumin (eg., warfarin)
Sulfa drugs - kernicterus in newborns (contraindicated)
Leukopenia,
Granulocytopenia (alleviated w/ leucovorin rescue)

Resistance - Plasmid/transposon mediated altered target, decreased uptake, increased PABA precursor (outcompetes sulfonamide)

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33
Q

Polymyxin B, Polymyxin E (colistimethate)

  • MOA,
  • Target Orgs/Use,
  • Toxicity
A

MOA - Bind cell membranes of bacteria and disrupt their osmotic properties (cationic, basic proteins that act like detergents)

Target Orgs/Use - Resistant gram- infection

Toxicity -
Neurotoxicity,
acute renal tubular necrosis

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34
Q

Isoniazid (INH)

  • MOA,
  • Target Orgs/Use,
  • Metabolism/Bioavailability
  • Side Effects
A

MOA - Decrease synthesis of mycolic acids (INH is a prodrug; use bacterial catalase peroxidase to convert INH to active metabolite)

Target Orgs/Use - M. tb prophylaxis and treatment (diff t1/2 in fast vs. slow acetylators)

Side Effects: (“INH” - I njures N eurons and H epatocytes) Hepatotoxicity
Neurotoxicity,
Lupus erythematosus (Pyridoxine (B6) can prevent)

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35
Q

Pyrazinamide

  • MOA,
  • Target Orgs/Use
A

MOA - bactericidal in acidic pH of phagolysosome (where TB engulfed by macrophages is found)

Target Orgs/Use - TB

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36
Q

Ethambutol

  • MOA,
  • Target Orgs/Use,
  • Side Effects
A

MOA - Decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinsyltransferase

Target Orgs/Use - TB

Side Effect - Optic neuropathy (red-green color blindness)

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37
Q

Give the Antimycobacterial Prophylaxis and Therapy drug for each of these:

  • M. tb M. avium/intracellulare (MAC)
  • M. leprae
A

M. tb:
Prophylaxis = INH
Treatment = Rifampin, INH, Pyrazinamide, Ethambutol (“RIPE” for treatment)

M. avium-intracellulare:
Prophylaxis - Azithromycin
Treatment - Azithromycin, rifampin, ethambutol, streptomycin

M. leprae:
Prophylaxis - N/A
Treatment - Dapsone, rifampin, clofazimine

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38
Q

Nonsurgical antimicrobial prophylaxis drug for: Meningococcal Infection

A

Rifampin

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39
Q

Nonsurgical antimicrobial prophylaxis drug for: Gonorrhea

A

Ceftriaxone

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40
Q

Nonsurgical antimicrobial prophylaxis drug for: Syphilis

A

Benzathine penicillin G

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41
Q

Nonsurgical antimicrobial prophylaxis drug for: Recurrent UTIs

A

TMP-SMX

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42
Q

Nonsurgical antimicrobial prophylaxis drug for: Pneumocystic jiroveci pneumonia

A

TMP-SMX

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43
Q

Nonsurgical antimicrobial prophylaxis drug for:
Endocarditis w/ surgical or dental procedure

A

PCNs

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44
Q 
Nonsurgical antimicrobial prophylaxis drug for:
Pregnant women (35-37wks) w/ positive Grp B Strep culture
A

Intrapartum PCN

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45
Q

Treatment Regimen: H. pylori

A

2 Triple Therapy options:

1. Metronidazole, Bismuth, Tetracycline or Amoxicillin

2. Metronidazole, Omeprazole, Clarithromycin (more expensive)

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46
Q

Treatment Regimen: Pseudomonas aeruginosa

A

Aminoglycoside

+

4th gen PCN (Piperacillin, Ticarcillin)

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47
Q

List all the classes/categories of abx that work by wrecking cell-wall synthesis:

A
  • bacitracin
  • carbapenems
  • cephalosporins
  • monobactams
  • penicillins
  • vancomycin
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48
Q

Cephalexin belongs to which generation of cephalosporins?

A

1st

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49
Q

Cephapirin belongs to what generation of cephalosporins?

A

1st

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50
Q

Cefazolin belongs to what generation of cephalosporins?

A

1st

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51
Q

Cefuroxime belongs to which generation of cephalosporins?

A

2nd

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52
Q

Cefoxitin belongs to which generation of cephalosporins?

A

2nd

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53
Q

Cefaclor belongs to which generation of cephalosporins?

A

2nd

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54
Q

Cefotetan belongs to which generation of cephalosporins?

A

2nd

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55
Q

Cefonicid belongs to which generation of cephalosporins?

A

2nd

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56
Q

List the Carboxypenicillins:

A

Carbenicillin
Ticarcillin

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57
Q

List the Ureidopenicillins:

A

Azlocillin
Mezlocillin
Piperacillin

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58
Q

What mnemonic device helps you remember the target organisms for Aminopenicillins?

A

“H.E.L.P.S. kill enterococcus”

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59
Q

“H.E.L.P.S. kill enterococcus” is the mnemonic device for which *class/group *of drugs?

A

Aminopenicillins

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60
Q

What is the side effect of Methicillin?

A

allergic interstitial nephritis

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61
Q

What is the side effect of Nafcillin?

A

hepatitis (some hepatic excretion)

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62
Q

What is the side effect(s) of Oxacillin?

A

hepatitis (some hepatic excretion)

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63
Q

____ is the first-line treatment of choice for staphylococcal endocarditis in patients without artificial heart valves.

A

nafcillin or oxacillin

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64
Q

The recommended administration instructions/route for Amoxicillin:

A

oral, with food

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65
Q

What are the side effects of Aminopenicillins?

A
  • hypersensitivity reactions,
  • ampicillin rash,
  • pseudomembranous colitis
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66
Q

What are the Target Orgs/Use for Mezlocillin?

A

Pseudomonas, and other

gram Neg bacteria

(some gram Pos, also)

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67
Q

What are the Target Orgs/Use for Piperacillin?

A

Pseudomonas, and

gram Neg bacteria

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68
Q

What are the Target Orgs/Use for Carbenicillin?

A

Pseudomonas, and

gram Neg rods

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69
Q

What are the Target Orgs/Use for Ticarcillin?

A

Pseudomonas, and

gram Neg rods

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70
Q

What is the Side Effects of Carbenicillin?

A

Carbenicillin is a Disodium salt, so it can produce large salt load in the body

(watch out for CHF, or hypoKalemia)

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71
Q

What is the Side Effects of Ticarcillin?

A

Ticarcillin is a Disodium salt, so it can produce large salt load in the body

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72
Q

the N-methylthiotetrazole (“MTT”) side-chain is found in some of the drugs belonging to this group/class of abx:

A

Cephalosporin

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73
Q

Why does the MTT side-chain, found in some cephalosporins, cause side effects?

A

it blocks the enzymes Vitamin K Epoxide Reductase (likely causing hypothrombinemia) and Aldehyde dehydrogenase (causing alcohol intolerance)

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74
Q

Name the bacteria against which b-Lactamase Inhibitor Drugs do Not work :

A

Clavulanic acid/Sulbactam/Tazobactam are NOT effective against the chromosomal b-lactamase of

Serratia,

Pseudomonas,

Enterobacter,

Citrobacter

75
Q

What are the Target Orgs/Use for Clavulanic acid?

A

Effective, in conjunction with 3-4 gen PCN, against

Gram- b-lactamases and

S. aureus

76
Q

Name a bacterium that resists b-Lactam drugs by changing its porin to restrict entry:

A

Pseudomonas

77
Q

Name a bacterium that resists b-Lactam drugs by altering PCN-binding protein:

A

MRSA,

S. pneumoniae

78
Q

What are the side effects of Cephalosporins?

A
  • Hypersensitivity reaction (5-10% cross hypersensitivity with PCN)
  • Vitamin K deficiency (Cefotetan, Cefonicid, Cefoperazone)
  • Disulfuram-like reaction w/ethanol (Cefotetan, Cefonicid, Cefoperazone)
  • Increase the nephrotoxicity of Aminoglycosides
79
Q

1st-Gen cephalosporins treat these organisms:

A

Gram+ cocci (MSSA, Streptococci) and Enterobacteriaceae (“PEcK” - Proteus, E. coli, Klebsiella)

80
Q

Noteworthy about the metabolism of Cephalothin :

A

deacylated by liver

(not good for meningitis, b/c deacylated form competes with active form for transport to CSF)

81
Q

Noteworthy about the metabolism of Cephapirin :

A

deacylated by liver but w/ active metabolites

82
Q

List the drugs mentioned in the mnemonic “PEcK”:

A
  • Proteus,
  • E. coli,
  • Klebsiella
83
Q

“PEcK” refers to bacteria that belong to this family:

A

Enterobacteriaceae

84
Q

“HEN PEcKS” is the mnemonic device for these drugs:

A

Haemophilus influenzae,

Enterobacter,

Neisseria,

Proteus,

E. coli,

Klebsiella,

Serratia

85
Q

2nd-Gen cephalosporins are Less active vs. _____ than 1st-gen.

A

Gram+ cocci/S.aureus

86
Q

the target organisms for 2nd-Generation Cephalosporins:

A

gram- orgs (HEN PEcKS = Haemophilus influenzae, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia)

87
Q

What are the side effects of 2nd-gen Cephalosporins?

A
  1. Inhibits Vitamin K-mediated gamma carboxylation
  2. Associated with Disulfuram-like reaction with alcohol (throbbing of neck, headache, nausea, etc)
88
Q

Cefepime is better than 3rd-gen cephalosporins at treating:

A

Pseudomonas and

gram+

89
Q

Ceftriaxone is used to treat:

A

meningitis and

gonorrhea

90
Q

Ceftazidime is used to treat:

A

Pseudomonas

91
Q

Monobactams can fight these organisms:

A

They work only against aerobic Gram Negative bacteria

(e.g., Neisseria, Pseudomonas).

92
Q

What is the MOA of Aztreonam?

A

b-lactam;
mucopeptide (cell wall) synthesis inhibitor;
binds to gram Neg transpeptidase PBP-3

93
Q

Aztreonam is synergistic with:

A

aminoglycosides

94
Q

What drug(s) is synergistic with aminoglycosides?

A

Aztreonam

95
Q

What Class does aztreonam belong to?

A

Monobactam

96
Q

For which pts/cases do you use aztreonam?

A

Facultative Gram Neg;
Use for PCN-allergic pts; &
those w/ renal insufficiency who cannot tolerate aminoglycosides

97
Q

What are the side fx of aztreonam?

A

diarrhea/rash (rare);
Can trigger seizures in patients with history of seizures

98
Q

Which abx drug(s) might cause seizures?

A

aztreonam;
imipenem

99
Q

What class does imipenem belong to?

A

carbapenem

100
Q

What class does meropenem belong to?

A

carbapenem

101
Q

Are carbapenem drugs resistant to b-lactamase?

A

Yes, they are resistant to all b-lactamases

102
Q

For which pts do you use imipenem?

A

More active vs. Gram+ cocci

103
Q

For which pts do you use meropenem?

A

More activity vs. Gram Neg rods

104
Q

What are contraindications for carbapenems?

A

Cross-reactivity with PCN

105
Q

Which macrolide is a teratogen?

A

clarithromycin

106
Q

Erythromycin/Clarithromycin rev [up/down] the cytochrome P450 enzymes.

A

inhibits; i.e., revs ↓↓

107
Q

What are side fx for carbapenems?

A

Imipenem must be infused slowly or causes GI distress;

Imipenem causes seizures (pts at increase risk - renal insufficiency)

108
Q

How is imipenem metabolized?

A

hydrolyzed by peptidase on renal tubular cells (so coadmin with cilastatin, a dipeptidase inhibitor)

109
Q

_____ must be coadministered with cilastatin.

A

imipenem

110
Q

Imipenem must be coadministered with _____.

A

cilastatin

111
Q

What is the resistance mechanism against carbapenems?

A

Pseudomonas resists carbapenems via a porin mutation

112
Q

_____ inhibits cell wall mucopeptide formation, by binding to D-ala-D-ala portion of the cell wall precursors.

A

vancomycin

113
Q

What is the MOA of vancomycin?

A

Inhibits cell wall mucopeptide formation, by binding to D-ala-D-ala portion of the cell wall precursors. Bactericidal.

114
Q

For which pts/cases do you use vancomycin?

A

Gram+ bacteria including MRSA and Enterococcus;

Used for all gram+ infections in PCN-allergic pt;

Given orally to treat **C. difficile **

115
Q

What are the side fx of Vancomycin?

A

Nephrotoxicity (especially with aminoglycosides);

Ototoxic;

Thrombophlebitis;

“Red man syndrome” (HM release)

116
Q

Which drug has “red man syndrome” as a side effect?

A

vancomycin

117
Q

What is the admin route for vancomycin?

A

Given IV (except for to tx C. diff)

118
Q

What is the resistance mechanism against vancomycin?

A

Block penetration (Gram Neg bacteria mode of resistance);

Plasmid genes altering structure of cell wall to D-ala-D-lac (some Gram+ strains)

119
Q

Which drugs bind to the 23S rRNA subunit of the 50S ribosome?

A

chloramphenicol;

clindamycin;

linezolid

the macrolides

120
Q

What is the MOA of chloramphenicol?

A

Inhibits protein synthesis by: binding to the 23S rRNA part of the 50S ribosome

121
Q

For which pts do you use chloramphenicol?

A

Meningitis

(covers H. flu, N. meningiditis, S. pneumoniae)

122
Q

What are the side fx of chloramphenicol?

A

aplastic anemia;

reversible BM suppression;

“Gray baby syndrome”;

Hemolysis in pts with G6PD deficiency

123
Q

With which drugs do you see “gray baby syndrome” side effect?

A

chloramphenicol

124
Q

What is the resistance mechanism against chloramphenicol?

A

plasmid-encoded acetyl transferase that inactivates drug

125
Q

What is the MOA of clindamycin?

A

binds to 23S rRNA portion on the 50S ribosomal subunit

126
Q
A
127
Q

For what pts/cases do you use clindamycin?

A

Anaerobes (above diaphragm - aspiration pneumonia/lung abscess)

128
Q

What is the side effect of clindamycin?

A

Pseudomembranous colitis due to overgrowth of C. diff

129
Q

What is the resistance mechanism against clindamycin?

A

Plasmid-encoded resistance due to methylation of 23S rRNA binding site, leading to decreased binding by clindamycin

130
Q

What is the MOA of linezolid?

A

Binds 23S portion of 50S ribosomal subunit and blocks formation of initiation complex

131
Q

For which pts/diseases do you use linezolid?

A

Gram+ cocci (including MRSA, VRE)

132
Q

What are the side effects of linezolid?

A

BM suppression,

MAO inhibitor (toxicity with tyramine or other related drugs)

133
Q

List the macrolides:

A

Erythromycin, Azithromycin, Clarithromycin

134
Q

Which macrolides are long-acting?

A

Azithromycin, Clarithromycin

135
Q

What is the MOA of the macrolides?

A

binds to 23S rRNA on 50S ribosomal subunit (blocks translocation)

136
Q

What is the MOA of azithromycin?

A

binds to 23S rRNA on 50S ribosomal subunit (blocks translocation)

137
Q

For which pts/cases do you use macrolides?

A

Atypical pneumonias (mycoplasma, chlamydia, legionella);

URI’s,

STDs,

Gram+ cocci (strep infections in pts allergic to PCN),

Neisseria,

Azithromycin - MAC (M. avium, intracellulare) prophylaxis and treatment

138
Q

What drug(s) do you give for atypical pneumonias?

A

macrolides

139
Q

What drug(s) do you give for MAC (M. avium, intracellulare) prophylaxis and treatment ?

A

azithromycin

140
Q

What are the side effects of macrolides?

A

Nausea/Diarrhea (motilin agonist) - worse w/ Erythromycin;

Cholestatic hepatitis;

Inhibits P-450 enzymes - increases concentration of warfarin and theophylline [*Azithromycin is an EXCEPTION b/c it does Not inhibit CYP3A4];

Eosinophilia,

QT prolongation (mostly Erythromycin) ,

Teratogen (Clarithromycin)

141
Q

Which macrolide does NOT interact with cytochrome P450 enzymes?

A

azithromycin

142
Q

What is the resistance mechanism against macrolides?

A

Plasmid encoded resistance due to methylation of 23S rRNA

143
Q

What is the MOA of the tetracyclines?

A

binds 30S ribosome and inhibits tRNA binding

144
Q

For which pts/cases do you use tetracyclines?

A

Atypical organisms (Chlamydia, Mycoplasma pneumoniae, Rickettsia, Brucella, Leptospira, B. burgdorferi);

H. pylori triple therapy;

Demeclocycline - ADH antagonist (diuretic in SIADH)

145
Q

What are the side fx of tetracyclines?

A

Bind newly synthesized bone and discolors teeth (don’t give pregnant women/kids);

Photosensitivity;

skin rash (esp Doxycycline);

GI distress

146
Q

For which pts/cases do you give metronidazole?

A

“GET GAP”

G iardia
E ntamoeba
T richomonas vaginalis
G ardnerella vaginalis
A naerobes (except Actinomyces)
H. p ylori (triple therapy w/ amoxicillin or tetracycline and bismuth)

147
Q

What is the route of administration for tetracyclines?

A

Given Oral

(only doxycycline can be given IV - others cause thrombophlebitis)

148
Q

What advice do you give to a patient who’s given tetracyclines?

A

Antacids, milk/dairy products inhibit absorption (divalent cations inhibit absorption)

149
Q

What advice do you give to a patient who’s prescribed ciprofloxacin?

A

Do Not take w/ Oral or IV Antacids (Mg++ or Al+++), nor w/ iron, calcium, zinc, dairy, food,

HM blockers delay absorption

150
Q

(1) Which tetracyclines can be used in pts with renal failure?
(2) Why?

A

doxycycline; b/c doxy has hepatic excretion

151
Q

How are tetracyclines excreted?

A

Renal + hepatic excretion;

Doxycycline hepatic excretion (can be used in pts w/renal failure)

152
Q

List the aminoglycoside drugs:

A

Amikacin / Gentamicin / Neomycin / Streptomycin / Tobramycin

153
Q

What is the MOA of aminoglycosides?

A

Binds 30S ribosomal subunit, blocking formation of initiation complex

154
Q

For which cases/pts would you prescribe aminoglycosides?

A

Active vs. organisms with ETC (use ETC to get in cell);

Severe gram Neg rod infection;

Neomycin for bowel surgery

155
Q

What are the side effects of aminoglycosides?

A

Reversible nephrotoxicity (especially w/ cephs)

Irreversible ototoxicity (kill cochlear hair cells) - especially w/ loop diuretics;

Teratogen

156
Q

What class is nalidixic acid?

A

First-generation Quinolone

157
Q

What is the MOA of nalidixic acid?

A

Bactericidal, Inhibits DNA Gyrase

158
Q

What class is ciprofloxacin?

A

2nd-gen Fluoroquinolone

159
Q

What is the MOA of ciprofloxacin?

A

Bactericidal, Inhibits DNA **Gyrase **

160
Q

For what cases/pts do you use ciprofloxacin?

A

Gram Neg rods of urinary/GI tracts (UTIs/Gastroenteritis) including: Pseudomonas, Neisseria;

Some Gram+ orgs (e.g., MSSA but not MRSA)

161
Q

Ciprofloxacin is contraindicated for these pts:

A

pregnant women and children

162
Q

What do you advise a pt who’s given ciprofloxacin?

A

Do Not take w/ Oral or IV Antacids (Mg++ or Al+++), nor w/ iron, calcium, zinc, dairy, food;

HM blockers delay absorption

163
Q

What class is Metronidazole?

A

DNA Synthesis inhibitors

164
Q

What is the MOA of Metronidazole?

A

Bactericidal/antiprotozoal,

Forms free radical toxic metabolites in the bacterial cell that damage DNA

165
Q

What are the side fx of metronidazole?

A

Associated with Disulfuram-like reaction with alcohol (throbbing of neck, headache, nausea, etc);

Metallic taste in the mouth

166
Q

Which organisms are resistant to metronidazole?

A

actinomyces

167
Q

What is the MOA of rifampin?

A

Inhibit DNA-dependent RNA polymerase (inhibit txn initiation)

168
Q

For what cases/pts do you use rifampin?

A

Mycobacterium tb (Hansen’s disease) combo agent (rapid drug resistance if used alone);

Delays resistance to dapsone when used for leprosy;

​Meningococcal and H. flu B prophylaxis

169
Q

What are the side fx of rifampin?

A

Turns urine, tears, sweat reddish/orange

Induces Cyp-450 - reduce blood levels of many drugs

4 R’s of Rifampin - RNA pol inhibitor, Revs up P450s, Red body fluid, Rapid resistance

170
Q

What organisms are resistant to rifampin?

A

Enterobacteriaceae family, and

Acinetobacter and Pseudomonas genuses are intrinsically resistant to rifampicin

171
Q

What is the MOA of Sulfonamides and Trimethoprim?

A

BacteriCIDAL together (bacterioSTATIC alone),

Competitively inhibit folate metabolism in different steps: Trimethoprim inhibits DHFR;
Sulfonamides inhibit folate synthesis (block dihydropteroate synthetase)

172
Q

For which cases/pts do you use Sulfonamides and Trimethoprim?

A

UTI’s,

Prophylaxis and tx of PCP in AIDS pts,

Gram+ (including MRSA), Gram-, Salmonella, Shigella, Nocardia, Chlamydia

173
Q

What are the side fx of Sulfonamides and Trimethoprim?

A

Rash/skin reaction (as severe as SJS)

Hemolysis if G6PD-deficient

Nephrotoxicity (interstitial nephritis)

Megaloblastic anemia

Displace other drugs from albumin (eg., warfarin)

Sulfa drugs - kernicterus in newborns (Contraindicated)

Leukopenia,

Granulocytopenia (alleviated w/ leucovorin rescue)

174
Q

(1) In which pts is TMP-SMX contraindicated?
(2) Why?

A

Sulfa drugs cause kernicterus in newborns (Contraindicated in newborns)

175
Q

Why do sulfonamide drugs cause kernicterus?

A

Because sulfonamides displace bilirubin from serum albumin

176
Q

What is the MOA of Polymyxin B, Polymyxin E (colistimethate)?

A

Bind cell membranes of bacteria and disrupt their osmotic properties

177
Q

What are the side fx of Polymyxin B, Polymyxin E ?

A

Toxicity - Neurotoxicity, acute renal tubular necrosis

178
Q

What is the MOA of INH?

A

Decrease synthesis of mycolic acids

179
Q

What enzyme activates INH?

A

bacterial catalase peroxidase converts INH to active metabolite

180
Q

What are the side fx of INH?

A

(“INH” - I njures N eurons and H epatocytes)

Hepatotoxicity,

Neurotoxicity,

Drug-induced lupus erythematosus

181
Q

What is the MOA of Pyrazinamide?

A

bactericidal in acidic pH of phagolysosome (where TB engulfed by macrophages is found)

182
Q

For which cases/pts do you use Pyrazinamide?

A

TB

183
Q

What is the MOA of ethambutol?

A

Decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinsyltransferase

184
Q

What are the side fx of ethambutol?

A

Optic neuropathy (red-green color blindness)

Milly (13 decks)

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