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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
Tetracycline / Minocycline / Doxycycline / Demeclocycline * Class, * MOA, * Target Orgs/Use, * Side Effects, * Administration, * Metabolism, * Resistance
_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
26
In Pharm, **parenteral** refers to:
routes *other than* the digestive tract.
27
Gentamicin / Neomycin / Amikacin / Tobramycin / Streptomycin * Class, * MOA, * Target Orgs/Use, * Side Effects, * Bioavailability, * Metabolism, * Resistance
_Class_ - Aminoglycosides (Inhibitor of protein synthesis) _MOA_ - Bactericidal; Binds **30**S 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)
28
Nalidixic Acid * Class, * MOA
Class - First generation Quinolone MOA - Bactericidal, Inhibits DNA Gyrase
29
Ciprofloxacin * Class, * MOA, * Target Orgs/Use, * Side Effects, * Administration, * Metabolism, * Resistance
_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 (**contra**indicated 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
30
Metronidazole * Class, * MOA, * Target Orgs/Uses, * Side Effects, * Resistance
_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
31
Rifampin * MOA, * Target Orgs/Uses, * Side Effects, * Bioavailability, Metabolism, * Resistance
_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 **red**ish/**orange** Induces Cyp-450 -\< reduce blood levels of many drugs **4 R**'s of Rifampin - **R**NA pol inhibitor, **R**evs up P450s, **R**ed body fluid, **R**apid resistance _Resistance_: **Enterobacteriaceae** family, and **Acinetobacter **and **Pseudomonas **genuses are intrinsically resistant to rifampicin.
32
Sulfonamides and Trimethoprim * MOA, * Target Orgs/Use, * Side Effects, * Bioavailability, Metabolism, * Resistance
_MOA_ - Bacteri*cidal* together (bacterio*static* 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 (**contra**indicated) Leukopenia, Granulocytopenia (alleviated w/ leucovorin rescue) _Resistance_ - Plasmid/transposon mediated altered target, decreased uptake, increased PABA precursor (outcompetes sulfonamide)
33
Polymyxin B, Polymyxin E (colistimethate) * MOA, * Target Orgs/Use, * Toxicity
_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
34
Isoniazid (INH) * MOA, * Target Orgs/Use, * Metabolism/Bioavailability * Side Effects
_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)
35
Pyrazinamide * MOA, * Target Orgs/Use
_MOA_ - bactericidal in acidic pH of phagolysosome (where TB engulfed by macrophages is found) _Target Orgs/Use_ - TB
36
Ethambutol * MOA, * Target Orgs/Use, * Side Effects
_MOA_ - Decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinsyltransferase _Target Orgs/Use_ - TB _Side Effect_ - Optic neuropathy (red-green color blindness)
37
Give the Antimycobacterial **Prophylaxis** and **Therapy** drug for each of these: * M. tb M. avium**/**intracellulare (MAC) * M. leprae
M. tb: Prophylaxis = INH Treatment = **R**ifampin, **I**NH, **P**yrazinamide, **E**thambutol ("*RIPE*" for treatment) M. avium-intracellulare: Prophylaxis - Azithromycin Treatment - Azithromycin, rifampin, ethambutol, streptomycin M. leprae: Prophylaxis - N/A Treatment - Dapsone, rifampin, clofazimine
38
Nonsurgical antimicrobial prophylaxis drug for: Meningococcal Infection
Rifampin
39
Nonsurgical antimicrobial prophylaxis drug for: Gonorrhea
Ceftriaxone
40
Nonsurgical antimicrobial prophylaxis drug for: Syphilis
Benzathine penicillin G
41
Nonsurgical antimicrobial prophylaxis drug for: Recurrent UTIs
TMP-SMX
42
Nonsurgical antimicrobial prophylaxis drug for: Pneumocystic jiroveci pneumonia
TMP-SMX
43
Nonsurgical antimicrobial prophylaxis drug for: Endocarditis w/ surgical or dental procedure
PCNs
44
``` Nonsurgical antimicrobial prophylaxis drug for: Pregnant women (35-37wks) w/ positive Grp B Strep culture ```
Intrapartum PCN
45
Treatment Regimen: H. pylori
2 Triple Therapy options: **1.** Metronidazole, Bismuth, Tetracycline or Amoxicillin **2.** Metronidazole, Omeprazole, Clarithromycin (more expensive)
46
Treatment Regimen: Pseudomonas aeruginosa
Aminoglycoside + **4th** gen PCN (Piperacillin, Ticarcillin)
47
List all the **classes**/categories of abx that work by wrecking cell-wall synthesis:
* bacitracin * carbapenems * cephalosporins * monobactams * penicillins * vancomycin
48
Cephalexin belongs to which **generation** of cephalosporins?
1st
49
Cephapirin belongs to what generation of cephalosporins?
1st
50
Cefazolin belongs to what generation of cephalosporins?
1st
51
Cefuroxime belongs to which generation of cephalosporins?
2nd
52
Cefoxitin belongs to which generation of cephalosporins?
2nd
53
Cefaclor belongs to which generation of cephalosporins?
2nd
54
Cefotetan belongs to which generation of cephalosporins?
2nd
55
Cefonicid belongs to which generation of cephalosporins?
2nd
56
List the Carboxypenicillins:
Carbenicillin Ticarcillin
57
List the Ureidopenicillins:
Azlocillin Mezlocillin Piperacillin
58
What mnemonic device helps you remember the target organisms for Aminopenicillins?
"H.E.L.P.S. kill enterococcus"
59
"H.E.L.P.S. kill enterococcus" is the mnemonic device for which *class/group *of drugs?
Aminopenicillins
60
What is the side effect of Methicillin?
allergic interstitial nephritis
61
What is the side effect of Nafcillin?
hepatitis (some hepatic excretion)
62
What is the side effect(s) of Oxacillin?
hepatitis (some hepatic excretion)
63
\_\_\_\_ is the first-line treatment of choice for **staphylococcal endocarditis** in patients with*out* artificial heart valves.
nafcillin or oxacillin
64
The recommended administration instructions/route for Amoxicillin:
oral, with food
65
What are the side effects of Aminopenicillins?
* hypersensitivity reactions, * ampicillin rash, * pseudomembranous colitis
66
What are the Target Orgs/Use for **Mez**locillin?
Pseudomonas, and other gram Neg bacteria (some gram Pos, also)
67
What are the Target Orgs/Use for **Piper**acillin?
Pseudomonas, and gram Neg bacteria
68
What are the Target Orgs/Use for Carbenicillin?
Pseudomonas, and gram Neg rods
69
What are the Target Orgs/Use for Ticarcillin?
Pseudomonas, and gram Neg rods
70
What is the Side Effects of Carbenicillin?
Carbenicillin is a **Disodium salt**, so it can produce large salt load in the body (watch out for CHF, or hypoKalemia)
71
What is the Side Effects of Ticarcillin?
Ticarcillin is a **Disodium** salt, so it can produce large **salt load** in the body
72
the N-methylthiotetrazole ("MTT") side-chain is found in some of the drugs belonging to this *group/class* of abx:
Cephalosporin
73
Why does the **MTT side-chain**, found in some cephalosporins, cause side effects?
it blocks the enzymes **Vitamin K Epoxide Reductase** (likely causing hypothrombinemia) and **Aldehyde dehydrogenase** (causing alcohol intolerance)
74
Name the bacteria against which **b-Lactamase Inhibitor** Drugs do Not work :
Clavulanic acid/Sulbactam/Tazobactam are NOT effective against the chromosomal b-lactamase of Serratia, Pseudomonas, Enterobacter, Citrobacter
75
What are the Target Orgs/Use for Clavulanic acid?
Effective, in conjunction with 3-4 gen PCN, against Gram- b-lactamases and S. aureus
76
Name a bacterium that resists b-Lactam drugs by changing its **porin** to restrict entry:
Pseudomonas
77
Name a bacterium that resists b-Lactam drugs by altering **PCN-binding protein**:
MRSA, S. pneumoniae
78
What are the side effects of Cephalosporins?
* **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
**1st**-Gen cephalosporins treat these organisms:
**Gram+** cocci (MSSA, Streptococci) and Enterobacteriaceae ("**PEcK**" - Proteus, E. coli, Klebsiella)
80
Noteworthy about the metabolism of Cepha**loth**in :
deacylated by liver (not good for **meningitis**, b/c deacylated form competes with active form for transport to CSF)
81
Noteworthy about the metabolism of Cepha**piri**n :
deacylated by liver but w/ active metabolites
82
List the drugs mentioned in the mnemonic "PEcK":
* Proteus, * E. coli, * Klebsiella
83
"PEcK" refers to bacteria that belong to this family:
Enterobacteriaceae
84
"HEN PEcKS" is the mnemonic device for these drugs:
Haemophilus influenzae, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia
85
**2nd**-Gen cephalosporins are Less active vs. _____ than 1st-gen.
Gram+ cocci/S.aureus
86
the target organisms for **2nd**-Generation Cephalosporins:
gram**-** orgs (**HEN PEcKS** = Haemophilus influenzae, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia)
87
What are the side effects of **2nd**-gen Cephalosporins?
1. Inhibits Vitamin **K**-mediated **gamma carboxylation** 2. Associated with **Disulfuram-like reaction** with alcohol (throbbing of neck, headache, nausea, etc)
88
**Cefepime** is better than 3rd-gen cephalosporins at treating:
Pseudomonas and gram**+**
89
Ceftriaxone is used to treat:
meningitis and gonorrhea
90
Ceftazidime is used to treat:
Pseudomonas
91
Monobactams can fight these organisms:
They work only against **aero**bic Gram **Neg**ative bacteria (e.g., Neisseria, Pseudomonas).
92
What is the MOA of Aztreonam?
b-lactam; mucopeptide (cell wall) synthesis inhibitor; binds to gram Neg transpeptidase PBP-3
93
Aztreonam is synergistic with:
aminoglycosides
94
What drug(s) is synergistic with aminoglycosides?
Aztreonam
95
What Class does aztreonam belong to?
Monobactam
96
For which pts/cases do you use aztreonam?
Facultative Gram **Neg**; Use for **PCN-allergic** pts; & those w/ **renal insufficiency** who cannot tolerate aminoglycosides
97
What are the side fx of aztreonam?
diarrhea/rash (rare); Can trigger seizures in patients with history of seizures
98
Which abx drug(s) might cause seizures?
aztreonam; imipenem
99
What class does imipenem belong to?
carbapenem
100
What class does meropenem belong to?
carbapenem
101
Are carbapenem drugs resistant to b-lactamase?
Yes, they are resistant to all b-lactamases
102
For which pts do you use imipenem?
More active vs. Gram+ cocci
103
For which pts do you use meropenem?
More activity vs. Gram Neg rods
104
What are contraindications for carbapenems?
Cross-reactivity with PCN
105
Which macrolide is a teratogen?
clarithromycin
106
Erythromycin/Clarithromycin rev **[**up**/**down**]** the cytochrome P450 enzymes.
inhibits; i.e., revs ↓↓
107
What are side fx for carbapenems?
Imipenem must be infused slowly or causes GI distress; Imipenem causes seizures (pts at increase risk - renal insufficiency)
108
How is imipenem metabolized?
hydrolyzed by peptidase on renal tubular cells (so coadmin with **cilastatin**, a dipeptidase inhibitor)
109
\_\_\_\_\_ must be coadministered with cilastatin.
imipenem
110
Imipenem must be coadministered with \_\_\_\_\_.
cilastatin
111
What is the resistance mechanism against carbapenems?
Pseudomonas resists carbapenems via a porin mutation
112
\_\_\_\_\_ inhibits cell wall mucopeptide formation, by binding to D-ala-D-ala portion of the cell wall precursors.
vancomycin
113
What is the MOA of vancomycin?
Inhibits cell wall mucopeptide formation, by binding to D-ala-D-ala portion of the cell wall precursors. Bactericidal.
114
For which pts/cases do you use vancomycin?
Gram+ bacteria including **MRSA** and Entero**coccus**; Used for all gram**+** infections in **PCN-allergic** pt; Given orally to treat **C. difficile **
115
What are the side fx of Vancomycin?
Nephrotoxicity (especially with aminoglycosides); Ototoxic; Thrombophlebitis; "Red man syndrome" (HM release)
116
Which drug has "red man syndrome" as a side effect?
vancomycin
117
What is the admin route for vancomycin?
Given IV (except for to tx C. diff)
118
What is the resistance mechanism against vancomycin?
Block penetration (Gram **Neg** bacteria mode of resistance); Plasmid genes altering structure of cell wall to D-ala-D-lac (some Gram**+** strains)
119
Which drugs bind to the **23**S rRNA subunit of the **50**S ribosome?
chloramphenicol; clindamycin; linezolid the macrolides
120
What is the MOA of chloramphenicol?
Inhibits protein synthesis by: binding to the **23**S rRNA part of the 50S ribosome
121
For which pts do you use chloramphenicol?
Meningitis | (covers H. flu, N. meningiditis, S. pneumoniae)
122
What are the side fx of chloramphenicol?
aplastic anemia; reversible BM suppression; "Gray baby syndrome"; Hemolysis in pts with G6PD deficiency
123
With which drugs do you see "gray baby syndrome" side effect?
chloramphenicol
124
What is the resistance mechanism against chloramphenicol?
plasmid-encoded acetyl transferase that inactivates drug
125
What is the MOA of clindamycin?
binds to **23**S rRNA portion on the 50S ribosomal subunit
126
127
For what pts/cases do you use clindamycin?
Anaerobes (above diaphragm - aspiration pneumonia/lung abscess)
128
What is the side effect of clindamycin?
Pseudomembranous colitis due to overgrowth of C. diff
129
What is the resistance mechanism against clindamycin?
Plasmid-encoded resistance due to **methylation** of 23S rRNA binding site, leading to decreased binding by clindamycin
130
What is the MOA of linezolid?
Binds **23**S portion of 50S ribosomal subunit and blocks formation of initiation complex
131
For which pts/diseases do you use linezolid?
Gram**+** cocci (including **MRSA**, **VRE**)
132
What are the side effects of linezolid?
BM suppression, MAO inhibitor (toxicity with tyramine or other related drugs)
133
List the macrolides:
Erythromycin, Azithromycin, Clarithromycin
134
Which macrolides are long-acting?
Azithromycin, Clarithromycin
135
What is the MOA of the macrolides?
binds to 23S rRNA on 50S ribosomal subunit (blocks translocation)
136
What is the MOA of azithromycin?
binds to **23**S rRNA on 50S ribosomal subunit (blocks **translocation**)
137
For which pts/cases do you use macrolides?
Atypical *pneumonias* (mycoplasma, chlamydia, legionella); U**R**I's, STDs, Gram**+** cocci (strep infections in pts allergic to PCN), Neisseria, **Azithromycin** - MAC (M. avium, intracellulare) prophylaxis and treatment
138
What drug(s) do you give for atypical pneumonias?
macrolides
139
What drug(s) do you give for **MAC** (M. avium, intracellulare) prophylaxis and treatment ?
azithromycin
140
What are the side effects of macrolides?
Nausea/Diarrhea (motilin agonist) - worse w/ **Ery**thromycin; Cholestatic hepatitis; Inhibits **P-450** enzymes - increases concentration of warfarin and theophylline [\***Az**ithromycin is an EXCEPTION b/c it does Not inhibit CYP3A4]; Eosinophilia, QT prolongation (mostly **Er**ythromycin) , Teratogen (**Clar**ithromycin)
141
Which macrolide does NOT interact with cytochrome P450 enzymes?
azithromycin
142
What is the resistance mechanism against macrolides?
Plasmid encoded resistance due to methylation of 23S rRNA
143
What is the MOA of the tetracyclines?
binds 30S ribosome and inhibits tRNA binding
144
For which pts/cases do you use tetracyclines?
Atypical organisms (Chlamydia, Mycoplasma pneumoniae, Rickettsia, Brucella, Leptospira, B. burgdorferi); H. pylori triple therapy; **Demeclo**cycline - ADH antagonist (diuretic in **SIADH**)
145
What are the side fx of tetracyclines?
Bind newly synthesized bone and discolors teeth (don't give pregnant women/kids); Photosensitivity; skin rash (esp **Doxy**cycline); GI distress
146
For which pts/cases do you give metronidazole?
"**GET GAP**" ## Footnote **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
What is the route of administration for tetracyclines?
Given Oral | (only **doxy**cycline can be given IV - others cause thrombophlebitis)
148
What advice do you give to a patient who's given tetracyclines?
Antacids, milk/dairy products inhibit absorption (divalent cations inhibit absorption)
149
What advice do you give to a patient who's prescribed ciprofloxacin?
Do Not take w/ Oral or IV Antacids (Mg++ or Al+++), nor w/ iron, calcium, zinc, dairy, food, HM blockers delay absorption
150
(1) Which tetracyclines can be used in pts with renal failure? (2) Why?
doxycycline; b/c doxy has hepatic excretion
151
How are tetracyclines excreted?
Renal + hepatic excretion; Doxycycline hepatic excretion (can be used in pts w/renal failure)
152
List the aminoglycoside drugs:
Amikacin / Gentamicin / Neomycin / Streptomycin / Tobramycin
153
What is the MOA of aminoglycosides?
Binds **30**S ribosomal subunit, blocking formation of **initiation complex**
154
For which cases/pts would you prescribe aminoglycosides?
Active vs. organisms with ETC (use ETC to get in cell); Severe gram **Neg** rod infection; **Neo**mycin for **bowel** surgery
155
What are the side effects of aminoglycosides?
Reversible **nephro**toxicity (especially w/ cephs) Irreversible **oto**toxicity (kill cochlear hair cells) - especially w/ loop diuretics; Teratogen
156
What class is nalidixic acid? ## Footnote
First-generation Quinolone
157
What is the MOA of nalidixic acid?
Bactericidal, Inhibits DNA **Gyrase**
158
What class is ciprofloxacin?
2nd-gen Fluoroquinolone
159
What is the MOA of ciprofloxacin?
Bactericidal, Inhibits DNA **Gyrase **
160
For what cases/pts do you use ciprofloxacin?
Gram **Neg** rods of **urinary/GI** tracts (UTIs/Gastroenteritis) including: Pseudomonas, Neisseria; Some Gram**+** orgs (e.g., **MSSA** but not MRSA)
161
Ciprofloxacin is contraindicated for these pts:
pregnant women and children
162
What do you advise a pt who's given ciprofloxacin?
Do Not take w/ Oral or IV Antacids (Mg++ or Al+++), nor w/ iron, calcium, zinc, dairy, food; HM blockers delay absorption
163
What class is Metronidazole?
DNA Synthesis inhibitors
164
What is the MOA of Metronidazole?
Bactericidal/anti**protozoa**l, Forms **free radical** toxic metabolites in the bacterial cell that damage **DNA**
165
What are the side fx of metronidazole?
Associated with **Disulfuram-like** reaction with **alcohol** (throbbing of neck, headache, nausea, etc); **Metallic taste** in the mouth
166
Which organisms are resistant to metronidazole?
actinomyces
167
What is the MOA of rifampin?
Inhibit DNA-dependent RNA polymerase (inhibit txn initiation)
168
For what cases/pts do you use rifampin?
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
What are the side fx of rifampin?
Turns urine, tears, sweat **reddish/orange** Induces Cyp-450 - reduce blood levels of many drugs 4 R's of Rifampin - **R**NA pol inhibitor, **R**evs up P450s, **R**ed body fluid, **R**apid resistance
170
What organisms are resistant to rifampin?
**Enterobacteriaceae** family, and **Acineto**bacter and **Pseudomonas** genuses are intrinsically resistant to rifampicin
171
What is the MOA of Sulfonamides and Trimethoprim?
Bacteri*CIDAL* together (bacterio*STATIC* alone), Competitively inhibit **folate** metabolism in different steps: Trimethoprim inhibits **DHFR**; Sulfonamides inhibit folate synthesis (block **dihydropteroate synthetase**)
172
For which cases/pts do you use Sulfonamides and Trimethoprim?
UTI's, Prophylaxis and tx of PCP in AIDS pts, Gram+ (including MRSA), Gram-, Salmonella, Shigella, Nocardia, Chlamydia
173
What are the side fx of Sulfonamides and Trimethoprim?
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
(1) In which pts is TMP-SMX contraindicated? (2) Why?
Sulfa drugs cause **kernicterus** in **newborns** (Contraindicated in newborns)
175
Why do sulfonamide drugs cause kernicterus?
Because sulfonamides displace bilirubin from serum albumin
176
What is the MOA of Polymyxin B, Polymyxin E (colistimethate)?
Bind cell membranes of bacteria and disrupt their osmotic properties
177
What are the side fx of Polymyxin B, Polymyxin E ?
Toxicity - Neurotoxicity, acute renal tubular necrosis
178
What is the MOA of INH?
Decrease synthesis of mycolic acids
179
What enzyme activates INH?
bacterial catalase peroxidase converts INH to active metabolite
180
What are the side fx of INH?
("INH" - **I** njures **N** eurons and **H** epatocytes) **Hepato**toxicity, **Neuro**toxicity, Drug-induced **lupus** erythematosus
181
What is the MOA of Pyrazinamide?
bactericidal in acidic pH of phagolysosome (where TB engulfed by macrophages is found)
182
For which cases/pts do you use Pyrazinamide?
TB
183
What is the MOA of ethambutol?
Decrease carbohydrate polymerization of mycobacterium cell wall by blocking **arabinsyltransferase**
184
What are the side fx of ethambutol?
Optic neuropathy (red-green color blindness)

Milly (13 decks)

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