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98 Cards in this Set

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Antimicrobials that are bactericidal
"Pencillins/Cephalo and Vanco KILL, then GYRATE DEAFLY on the METRO"

Pencillins, Cephalosporins, Vancomycin, Fluoroquinolones, Aminoglycosides, Metronidazole
2 types of penicillin
Penicillin G - IV
Penicillin V - Oral
MOA of penicillins
B-lactam ABs that bind PCPs to block transpeptidase cross-linking of cell wall.
Use of penicillins
G+ and Syphilis
Methicillin, nafcillin, dicloxacillin
MOA, Use
MOA: penicillinase-resistant penicillins
Use: NARROW! S. aureus only (except MRSA)

"Use naf for staph"
Which antimicrobial commonly causes TIN?
Methicillin
Ampicillin and amoxicillin
MOA, Uses, and SEs
MOA: same as penicillins; AmOxicillin has better bioavailability

Uses: Certain G+ bac and G- rods.

"AMPed up penicillin"

SEs: HS, ampicillin rash, pseudomembranous colitis.
Pencillins for Pseudomonas (3)
TCP: Takes Care of Pseudomonas

Ticarcillin, Carbenicillin, Piperacillin

(Also works for G- rods)
Beta-lactamase inhibitors (3)
Clavulanic acid
Sulfbactam
Tazobactam

Often added to penicillin antibiotics to protect from destruction by B-lactamase (penicillinase)
Penicillin SEs
HS and hemolytic anemia
Cephalosporins
B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal. 4 generations.
Cephalosporins

1st generation, 2 drugs + bugs
Cefazolin, Cephalexin

G+ cocci + PEcK:
Proteus mirabilis, E. coli, Klebsiella
Cephalosporins

2nd generation, 1 drug + bugs
Cefoxitin

Less G+, more G- > 1st generation.

G+ cocci, HEN PEcKS:
H. influenza, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella pneumoniae, Serratia marcescens
Cephalosporins

3rd generation (2 drugs and uses)
Ceftriaxone, ceftazidime.

Serious G- infections resistant to other G-s.

Ceftriaxone -- meningitis and gonorrhea

Ceftazidime -- Pseudomonas
Cephalosporins

4th generation (drug + bugs)
Cefepime.
Similar activity against G+ bugs as 1st gen. Great x G-'s also.

Particularly for Pseudomonas
(S. Aureus, MDR Strep pneumoniae)
Cephalosporin Toxicity and Drug Interactions (4)
1. HS and cross-HS with penicillins
2. Vit K deficiency,
3. nephrotoxicity with AGs,
4. disulfiram-like rxn with ethanol.
PBPs
PBPs = transpeptidases

Bind to the D-Ala-D-Ala at the end of muropeptides (peptidoglycan precursors) to crosslink the peptidoglycan.

B-lactam antibiotics inhibit PBP crosslinking of PG.
Aztreonam
Monobactam that is resistant to B-lactamases.
Aztreonam uses
G- rods only!
Aztreonam SEs and 2 special populations
Pretty non-toxic, safe drug.

Use in penicillin-allergic pts or those with renal probs (can't tolerate AGs)

No cross-sensitivity w/penicillins or cephalosporins.
Synergistic with AGs.
Carbapenems (list 2 drugs)
1. Imipenem / cilastatin
Always administer with cilastatin
(inhibits renal dihydropeptiase I to
decrease iactivation of Imipenem
in renal tubules)

2. Meropenem
(stable to dihydropeptiase I)
Carbapenem MOA
BROAD spectrum, B-lactamase resistant B-lactam drugs (inhibit cell wall synthesis via PBP binding)
Carbapenem Uses and SEs
Last resort drug (life threatening)-- wide spectrum, but significant SEs.

SEs: Seizures (Meropenem is safer than Imipenem/Cilastatin though).
Vancomycin MOA
Bactericidal. Inhibits cell wall formation by binding D-Ala D-Ala portion of PG precursors.
Vancomycin Uses
G+ bugs only -- serious MDR organisms (e.g. S. aureus, C. difficile, Enterococci
Vanco resistance
AA mutation of D-ala D-ala to D-ala D-lac
Vanco toxicity
Well-tolerated, prevent SEs with slow infusion rate and pre-tx with antihistamines.

Nephro/Oto, Thrombophlebitis, DIFFUSE FLUSHING.
B lactam drugs
Penicillins, Cephalosporons, Monobactam, Carbapenems
30S and 50S protein synthesis inhibitors
AT CCELL

30S: Aminoglycosides, Tetracyclines
50S: Chloramphenicol, Clindamycin, Erythromycin, Lincomycin, Linezolid.

All are bacteriostatic except AG (bactericidal).
Aminoglycosides (5)
Gentamicin
Neomcin
Streptomycin
Tobramycin
Amikacin
Used before bowel surgery to decrease bacteria. Very nephrotoxic so no IV.
Neomycin, an AG
Aminoglycosides MOA
30S inhibitor, bactericidal.

Inhibits formation of inititation complex and causes mRNA misreading. Requires O2 for uptake.
Aminoglycosides uses
ONLY severe

aerobic G- rod infections
AG toxicities (3) and drug interactions
1. nephro (esp. with cephalosporins)
2. ototoxicity (esp with loop diuretics)
3. teratogen

Use Aztreonam in patients who cannot tolerate AGs due to synergistic effect.
4 tetracyclines
Tetracycline, doxycycline, demeclocyline, minocycline.
Tetracycline MOA
30S inhibitor, bacteriostatic.
Prevents attachment of aminoacyl-tRNA synthetase
Demeclocycline
ADH antagonist - diuretic in SIADH.
Can you give doxycycline to patients with renal failure?
Yes! It is fecally eliminated.
Do not take tetracyclines with ____
milk, antacids, or iron-containing preparations

divalent cations inhibit tetracyline absorption in gut
Tetracycline SEs
GI, teeth discoloration, inhibits bone growth in children, photosensitivity, contraindicated in pregnancy.

(Doxy should not be used in children <8 unless they have RMSF)
T/F Tetracylines are effective against Rickettsia and Chlamydia.
True -- they accumulate inrtacellularly

(thus, resistance is via plasmid-encoded transport pumps)
Macrolides (3)
Erythromycin, Azithromycin, Clarithromycin
Macrolide MOA
50S inhibitor, bacteriostatic.

Blocks translocation by binding 23S of 50S ribosomal subunit.

Resistance: Methylation of 23 rRNA binding site.
Macrolide uses
Many -- URIs, STDs, G+ cocci, Neisseria... ATYPICAL PNEUMONIAS. (Myco, Chlamydia, Legionella)
Macrolide toxicity
Prolonged QT (esp erythro), GI, rashes, acute cholestatic hepatitis, eosinophilia.
Macrolides increase concentrations of what 2 drugs?
theophyllines and oral anticoagulants
Chloramphenicol
50S inhibitor, bacteriostatic.

Inhibits 50S peptidyltransferase activity (ribozyme that forms peptide links b/w AAs).
Chloramphenicol

Use
Meningitis

Conservative use due to toxicties, but cheap so used in 3rd world.
Chloramphenicol Toxicity
BM -- anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome in preemies
Gray baby syndrome
Chloramphenicol toxicity in preemies because they lack liver UDP-glucuronyl transferase.

Hypotension, cyanosis, CV collapse
Chloramphenicol resistance
plasmid-encoded chloramphenicol acetyltransferase (CAT)
Clindamycin MOA
50S inhibitor, bacteriostatic.

Inhibits ribosomal translocation (like macrolides)
Which 2 antimicrobials inhibit ribosomal translocation by binding 50S rRNA?
Macrolides (Erythromycin, Zpak, Clarithromycin) and Clindamycin
Clindamycin use
Anaerobic infections (Bacteroides, C. perfringens) in aspiration pneumonia or lung abscesses.

Treats anaerobes ABOVE diaphragm (vs. metro -- anaerobes BELOW diaphragm)
Sulfonamides MOA
Sulfamethaxole (SMX), sulfisoxasole, sulfadiazine.

MOA: PABA antimetabolite, inhibits dihydropteroate synthetase. Bacteriostatic.

DHP synthetase: PABA + pteridine --> DHF --> THF --> Thymine, purines, proteins
Sulfonamides Uses
G+, G-, Nocardia, Chlamydia, UTIs, etc.
Sulfonamides SEs
1. Hemolysis if G6PD deficient
2. Nephrotoxicity (TIN)
3. Photosensitivity
4. Kernicterus in infants (unconjugated BR --> jaundice + neuro probs)
5. Displaces drugs from albumin (e.g. warfarin)
Sulfonamides resistance
Altered bacterial dihydropteroate synthetase; increased PABA synthesis
Sulfonamides share synergy with what other anti-microbial and anti-protozoan drug?
Trimethoprim and pyrimethamine (inhibit DHFR, downstream of DHP synthetase)
Tx for Nocardia and Actinomyces
SNAP!
Sulfa Nocardia
Actinomyces Penicillin
Trimethoprim MOA
Inhibits DHFR. Bacteriostatic.

Use in combo with sulfonamides to cause sequential block of folate synthesis.
Trimethoprim Uses
Pneumocystis jiroveci, Shig/Salmonella, recurrent UTIs
Trimethoprim toxicity
TMP-Treats Marrow Poorly.

Megaloblastic anemia, leukopenia, granulocytopenia.
Trimeth OD tx/se px
Alleviate with supplemental folinic acid (leucovorin rescue)

Same for MTX and 5-FU.
Sulfa drug allergies (6)
1. Sulfa - something
2. Thiazides
3. Acetazolamide
4. Furosemide
5. Celecoxib (sulfa NSAID, COX2 (-))
6. Probenecid (uricosuric gout tx)
Fluoroquinolones
"Floxacins" (e.g. Ciprofloxacin) and
Nalidixic Acid (quinolone)
Fluoroquinolones MOA
Inhibits DNA gyrase (topoisomerase II). Bacteriocidal.
Fluoroquinolones toxicity
Contraindicated in pregnant women and children.

Tendonitis, tendon rupture, leg cramps, myalgias, cartilage damage.
Fluoroquinolones should not be taken with _____-
antacids
Resistance to fluroquinolones.
Mutation in DNA gyrase.
Metronidazole MOA
Forms ROS to damage bacterial DNA. Bactericidal.
Metronidazole Uses
Anaerobic infections below diaphragm (Clindamycin for anaerobes above diaphragm)


GET GAP on the H. METRO!
Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (Bacteroids, Clostridium)

H. pylori triple therapy (with bismuth and amoxicillin/tetracycline)
H. pylori treatment
Triple therapy
1. Metro + Bismuth + Tetracycline/Amoxicillin

2. Metro + Omeprazole + Clarithromycin

Some combo basically (amoxi, clarithro, metro, PPI)
Metronidazole Toxicity
Disulfiram like reaction with ROH, metallic taste

(don't drink on trains, they're made of metal)
Polymyxins MOA
Binds cell membranes of bacteria and disrupt osmotic properties. Cationic, basic proteins that act like detergents.
Polymixins Use
Resistant G- infections
Polymyxins SEs
Neurotoxicity, ATN.
Drugs that cause TIN commonly (4)
Methicillin, NSAIDS, sulfonamides, rifampin.
Mycobacterium TB, Avium, Leprae

Prophylaxis
TB: INH
MAI: Z-pak
Leprae: n/a
M. TB treatment (4)
TB is RIPE for treatment.

Rifampin, INH, Pyrazinamide, Ethambutol
MAI treatment (4)
ARES is a gay dude with AIDS.

Azithromycin, Rifampin, Ethambutol, Streptomycin.
M. leprae treatment (3)
Dapsone, Rifampin, Clofazimine.
Cycloserine
2nd line therapy for TB
Pyrazinamide -- where does it act? Clinical use?
Tx: TB (RIPE)

Effective in acidic pH of phagolysosomes where TB is found (macrophages).
Ethambutol MOA
Decreases carb polymerization of mycobacterium wall by blocking arabinosyltransferase.

Tx: M. TB and MAI.

"Ethambutol is Arabic alcohol, made near the Carb Wall of Myco"
Ethambutol SEs
optic neuropathy (red green color blindness)

FYI: RIPE drugs -- hepatotoxicity.
INH MOA
decreased synthesis of mycolic acids in mycobacteria

needs bacteria catalase-peroxidase to activate

"My Vietnamese Cat, Pero Inh"
INH v Ethambutol uses
INH - M. TB; the only agent used as solo prophylaxis against TB.
Ethambutol - M. TB and MAI.
INH SEs
1. INH - Injures Neurons and Hepatocytes
2. Lupus
3. Vitamin B6 (pyridoxine / PLP) deficiency and subsequent B3 (niacin / NAD) deficiency. Supplement B6.
Rifampin MOA
Inhibits DNA-dependent RNA polymerase
Rifampin uses
1. All 3 Mycos
Delays resistance to dapsone for leprosy.
2. Meningococcal prophylaxis (neisseria)
3. H. Flu type B prophylaxis.
Rifampin SEs
Hepatotoxicity and drug rxns

4Rs of Rifampin:
RNA polymerase inhibitor
Revs up microsomal P450
Red/orange body fluids (safe)
Rapid resistance is used alone
Prophylaxis for meningococcal (n. meningitis meningitis!)
Rifampin
Prophylaxis for gonorrhea in newborns with skanky mommies
Ceftriaxone
(erythromycin eye drops)
Hx of UTIs
TMP-SMX
Pneumocystic jiroveci pneumonia prophylaxis
TMP-SMX = DOC

Aerosolized pentamidine
Prophylaxis for endocarditis with surgical or dental procedures
Penicillins
VRE treatment (2)
linezolid and streptogramins