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98 Cards in this Set
- Front
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Antimicrobials that are bactericidal
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"Pencillins/Cephalo and Vanco KILL, then GYRATE DEAFLY on the METRO"
Pencillins, Cephalosporins, Vancomycin, Fluoroquinolones, Aminoglycosides, Metronidazole |
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2 types of penicillin
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Penicillin G - IV
Penicillin V - Oral |
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MOA of penicillins
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B-lactam ABs that bind PCPs to block transpeptidase cross-linking of cell wall.
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Use of penicillins
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G+ and Syphilis
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Methicillin, nafcillin, dicloxacillin
MOA, Use |
MOA: penicillinase-resistant penicillins
Use: NARROW! S. aureus only (except MRSA) "Use naf for staph" |
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Which antimicrobial commonly causes TIN?
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Methicillin
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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. |
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Pencillins for Pseudomonas (3)
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TCP: Takes Care of Pseudomonas
Ticarcillin, Carbenicillin, Piperacillin (Also works for G- rods) |
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Beta-lactamase inhibitors (3)
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Clavulanic acid
Sulfbactam Tazobactam Often added to penicillin antibiotics to protect from destruction by B-lactamase (penicillinase) |
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Penicillin SEs
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HS and hemolytic anemia
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Cephalosporins
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B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal. 4 generations.
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Cephalosporins
1st generation, 2 drugs + bugs |
Cefazolin, Cephalexin
G+ cocci + PEcK: Proteus mirabilis, E. coli, Klebsiella |
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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 |
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Cephalosporins
3rd generation (2 drugs and uses) |
Ceftriaxone, ceftazidime.
Serious G- infections resistant to other G-s. Ceftriaxone -- meningitis and gonorrhea Ceftazidime -- Pseudomonas |
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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) |
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Cephalosporin Toxicity and Drug Interactions (4)
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1. HS and cross-HS with penicillins
2. Vit K deficiency, 3. nephrotoxicity with AGs, 4. disulfiram-like rxn with ethanol. |
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PBPs
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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. |
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Aztreonam
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Monobactam that is resistant to B-lactamases.
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Aztreonam uses
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G- rods only!
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Aztreonam SEs and 2 special populations
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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. |
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Carbapenems (list 2 drugs)
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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) |
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Carbapenem MOA
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BROAD spectrum, B-lactamase resistant B-lactam drugs (inhibit cell wall synthesis via PBP binding)
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Carbapenem Uses and SEs
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Last resort drug (life threatening)-- wide spectrum, but significant SEs.
SEs: Seizures (Meropenem is safer than Imipenem/Cilastatin though). |
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Vancomycin MOA
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Bactericidal. Inhibits cell wall formation by binding D-Ala D-Ala portion of PG precursors.
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Vancomycin Uses
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G+ bugs only -- serious MDR organisms (e.g. S. aureus, C. difficile, Enterococci
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Vanco resistance
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AA mutation of D-ala D-ala to D-ala D-lac
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Vanco toxicity
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Well-tolerated, prevent SEs with slow infusion rate and pre-tx with antihistamines.
Nephro/Oto, Thrombophlebitis, DIFFUSE FLUSHING. |
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B lactam drugs
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Penicillins, Cephalosporons, Monobactam, Carbapenems
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30S and 50S protein synthesis inhibitors
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AT CCELL
30S: Aminoglycosides, Tetracyclines 50S: Chloramphenicol, Clindamycin, Erythromycin, Lincomycin, Linezolid. All are bacteriostatic except AG (bactericidal). |
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Aminoglycosides (5)
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Gentamicin
Neomcin Streptomycin Tobramycin Amikacin |
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Used before bowel surgery to decrease bacteria. Very nephrotoxic so no IV.
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Neomycin, an AG
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Aminoglycosides MOA
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30S inhibitor, bactericidal.
Inhibits formation of inititation complex and causes mRNA misreading. Requires O2 for uptake. |
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Aminoglycosides uses
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ONLY severe
aerobic G- rod infections |
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AG toxicities (3) and drug interactions
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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. |
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4 tetracyclines
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Tetracycline, doxycycline, demeclocyline, minocycline.
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Tetracycline MOA
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30S inhibitor, bacteriostatic.
Prevents attachment of aminoacyl-tRNA synthetase |
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Demeclocycline
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ADH antagonist - diuretic in SIADH.
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Can you give doxycycline to patients with renal failure?
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Yes! It is fecally eliminated.
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Do not take tetracyclines with ____
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milk, antacids, or iron-containing preparations
divalent cations inhibit tetracyline absorption in gut |
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Tetracycline SEs
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GI, teeth discoloration, inhibits bone growth in children, photosensitivity, contraindicated in pregnancy.
(Doxy should not be used in children <8 unless they have RMSF) |
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T/F Tetracylines are effective against Rickettsia and Chlamydia.
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True -- they accumulate inrtacellularly
(thus, resistance is via plasmid-encoded transport pumps) |
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Macrolides (3)
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Erythromycin, Azithromycin, Clarithromycin
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Macrolide MOA
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50S inhibitor, bacteriostatic.
Blocks translocation by binding 23S of 50S ribosomal subunit. Resistance: Methylation of 23 rRNA binding site. |
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Macrolide uses
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Many -- URIs, STDs, G+ cocci, Neisseria... ATYPICAL PNEUMONIAS. (Myco, Chlamydia, Legionella)
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Macrolide toxicity
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Prolonged QT (esp erythro), GI, rashes, acute cholestatic hepatitis, eosinophilia.
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Macrolides increase concentrations of what 2 drugs?
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theophyllines and oral anticoagulants
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Chloramphenicol
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50S inhibitor, bacteriostatic.
Inhibits 50S peptidyltransferase activity (ribozyme that forms peptide links b/w AAs). |
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Chloramphenicol
Use |
Meningitis
Conservative use due to toxicties, but cheap so used in 3rd world. |
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Chloramphenicol Toxicity
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BM -- anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome in preemies
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Gray baby syndrome
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Chloramphenicol toxicity in preemies because they lack liver UDP-glucuronyl transferase.
Hypotension, cyanosis, CV collapse |
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Chloramphenicol resistance
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plasmid-encoded chloramphenicol acetyltransferase (CAT)
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Clindamycin MOA
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50S inhibitor, bacteriostatic.
Inhibits ribosomal translocation (like macrolides) |
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Which 2 antimicrobials inhibit ribosomal translocation by binding 50S rRNA?
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Macrolides (Erythromycin, Zpak, Clarithromycin) and Clindamycin
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Clindamycin use
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Anaerobic infections (Bacteroides, C. perfringens) in aspiration pneumonia or lung abscesses.
Treats anaerobes ABOVE diaphragm (vs. metro -- anaerobes BELOW diaphragm) |
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Sulfonamides MOA
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Sulfamethaxole (SMX), sulfisoxasole, sulfadiazine.
MOA: PABA antimetabolite, inhibits dihydropteroate synthetase. Bacteriostatic. DHP synthetase: PABA + pteridine --> DHF --> THF --> Thymine, purines, proteins |
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Sulfonamides Uses
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G+, G-, Nocardia, Chlamydia, UTIs, etc.
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Sulfonamides SEs
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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) |
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Sulfonamides resistance
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Altered bacterial dihydropteroate synthetase; increased PABA synthesis
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Sulfonamides share synergy with what other anti-microbial and anti-protozoan drug?
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Trimethoprim and pyrimethamine (inhibit DHFR, downstream of DHP synthetase)
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Tx for Nocardia and Actinomyces
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SNAP!
Sulfa Nocardia Actinomyces Penicillin |
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Trimethoprim MOA
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Inhibits DHFR. Bacteriostatic.
Use in combo with sulfonamides to cause sequential block of folate synthesis. |
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Trimethoprim Uses
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Pneumocystis jiroveci, Shig/Salmonella, recurrent UTIs
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Trimethoprim toxicity
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TMP-Treats Marrow Poorly.
Megaloblastic anemia, leukopenia, granulocytopenia. |
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Trimeth OD tx/se px
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Alleviate with supplemental folinic acid (leucovorin rescue)
Same for MTX and 5-FU. |
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Sulfa drug allergies (6)
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1. Sulfa - something
2. Thiazides 3. Acetazolamide 4. Furosemide 5. Celecoxib (sulfa NSAID, COX2 (-)) 6. Probenecid (uricosuric gout tx) |
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Fluoroquinolones
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"Floxacins" (e.g. Ciprofloxacin) and
Nalidixic Acid (quinolone) |
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Fluoroquinolones MOA
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Inhibits DNA gyrase (topoisomerase II). Bacteriocidal.
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Fluoroquinolones toxicity
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Contraindicated in pregnant women and children.
Tendonitis, tendon rupture, leg cramps, myalgias, cartilage damage. |
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Fluoroquinolones should not be taken with _____-
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antacids
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Resistance to fluroquinolones.
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Mutation in DNA gyrase.
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Metronidazole MOA
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Forms ROS to damage bacterial DNA. Bactericidal.
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Metronidazole Uses
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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) |
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H. pylori treatment
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Triple therapy
1. Metro + Bismuth + Tetracycline/Amoxicillin 2. Metro + Omeprazole + Clarithromycin Some combo basically (amoxi, clarithro, metro, PPI) |
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Metronidazole Toxicity
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Disulfiram like reaction with ROH, metallic taste
(don't drink on trains, they're made of metal) |
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Polymyxins MOA
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Binds cell membranes of bacteria and disrupt osmotic properties. Cationic, basic proteins that act like detergents.
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Polymixins Use
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Resistant G- infections
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Polymyxins SEs
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Neurotoxicity, ATN.
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Drugs that cause TIN commonly (4)
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Methicillin, NSAIDS, sulfonamides, rifampin.
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Mycobacterium TB, Avium, Leprae
Prophylaxis |
TB: INH
MAI: Z-pak Leprae: n/a |
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M. TB treatment (4)
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TB is RIPE for treatment.
Rifampin, INH, Pyrazinamide, Ethambutol |
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MAI treatment (4)
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ARES is a gay dude with AIDS.
Azithromycin, Rifampin, Ethambutol, Streptomycin. |
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M. leprae treatment (3)
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Dapsone, Rifampin, Clofazimine.
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Cycloserine
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2nd line therapy for TB
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Pyrazinamide -- where does it act? Clinical use?
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Tx: TB (RIPE)
Effective in acidic pH of phagolysosomes where TB is found (macrophages). |
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Ethambutol MOA
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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" |
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Ethambutol SEs
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optic neuropathy (red green color blindness)
FYI: RIPE drugs -- hepatotoxicity. |
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INH MOA
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decreased synthesis of mycolic acids in mycobacteria
needs bacteria catalase-peroxidase to activate "My Vietnamese Cat, Pero Inh" |
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INH v Ethambutol uses
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INH - M. TB; the only agent used as solo prophylaxis against TB.
Ethambutol - M. TB and MAI. |
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INH SEs
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1. INH - Injures Neurons and Hepatocytes
2. Lupus 3. Vitamin B6 (pyridoxine / PLP) deficiency and subsequent B3 (niacin / NAD) deficiency. Supplement B6. |
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Rifampin MOA
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Inhibits DNA-dependent RNA polymerase
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Rifampin uses
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1. All 3 Mycos
Delays resistance to dapsone for leprosy. 2. Meningococcal prophylaxis (neisseria) 3. H. Flu type B prophylaxis. |
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Rifampin SEs
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Hepatotoxicity and drug rxns
4Rs of Rifampin: RNA polymerase inhibitor Revs up microsomal P450 Red/orange body fluids (safe) Rapid resistance is used alone |
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Prophylaxis for meningococcal (n. meningitis meningitis!)
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Rifampin
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Prophylaxis for gonorrhea in newborns with skanky mommies
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Ceftriaxone
(erythromycin eye drops) |
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Hx of UTIs
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TMP-SMX
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Pneumocystic jiroveci pneumonia prophylaxis
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TMP-SMX = DOC
Aerosolized pentamidine |
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Prophylaxis for endocarditis with surgical or dental procedures
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Penicillins
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VRE treatment (2)
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linezolid and streptogramins
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