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translation occur in ribosome RNA converts to PRO (protein synthesis)
transcription occur in cytoplasm DNA converts to mRNA
bacteria cell wall, 50s/30s ribosomes, prokaryotic
gram - bacteria peptidoglycan, cell wall not on surface, porins
gram + bacteria cell wall thicker than gram-bacteria, has murein, peptidoglycan, induce beta-lactamases, cell wall located on surface of cell
porins channels on bacteria that allow abx to enter and leave bacteria cell
murein protein on the surface of cell wall of gram+, stains blue
human cell has cell membrane, eukaryotic
bacteriostatic stop growth/replication = cell death stasis = stop
bacteriocidal kills bacteria cidal = kill
peptidoglycan: n-acetylglucosamine acid n-acetylmuramic acid polymer, located between 2 cell membrane in the middle of gram - and +, strong, cross-linked chain made up of 2 AA to form polysaccharide chain, creates cell wall
beta-lactamases enzyme that breaks down beta lactams, makes abx inactive before it even reaches bacteria
beta-lactamases inhibitors given with PCN to expand spectrum (amoxicillin + clavulanic acid), spectrum determined by accompanying abx
clavulanic acid beta-lactamase inhibitor, bind with PCN (beta lactam) to expand spectrum of activity
sulbactam beta-lactamase inhibitor, bind with PCN (beta lactam) to expand spectrum of activity
tazobactam beta-lactamase inhibitor, bind with PCN (beta lactam) to expand spectrum of activity
transpepetidase enzyme linking two polymer chains together to form peptidoglycan, inhibited beta lactams to prevent formation, aka pcn binding pro
gene transfer multi-drug resistance to abx that spreads from one bacteria to another
beta-lactams and glycopeptide (vancomycin) inhibit cell wall synthesis, excreted via kidneys, absorption decreased by food: 1 hr before or 2 hrs after meal
vancomycin (glycopeptide, not a beta lactam) inhibit cell wall synthesis, bactericidal, poor GI absorption and PO bioavailability, active only against(MRSA, gram+), PO for C.Difficle colitis, no PCN allergy, ototoxicity(given w/AG), chills, fever, tissue irritation at site of injection (IV)
resistance to beta lactams (doesn't allow beta lactams to work) inactivated by beta lactamases, mutation of transpeptidase target,impaired penetration of abx into cell, drug efflux pumps
drug efflux pumps located in intestines and cell wall of bacteria, transport pump, dumps abx in and out of bacteria = cannot inhibit transpeptidase = growth of bacteria cell wall
Penicillin (PCN) beta-lactam, hapten, SE: pruritis, fever, skin rash, oral lesions, hypersensitivity; narrow spectrum, occur from yeast, fungus,resistant to b-lactamase degradation, active against gram + and - cocci, caution with kidneys
hapten small molecule that stimulates production of antibody molecules only when attach to a larger molecule (PCN)
Extended spectrum PCN beta lactam ampicillin, amoxicillin; fight gram - rods, E.coli, Samonella, susceptible to beta lactamases so use with b-lactamase inhibitors
Anti-Staphyloccal PCN beta lactam methicillin, nafcillin; resistant to staph beta lactamase, work against staph, strep, pneumococci
Amoxicillin extended spectrum PCN, beta lactam, absorption not decreased by food
Nafcillin PCN resistant ABX (penicillinase), anti-staphyloccal PCN, beta-lactam
Cephalosporins beta lactam, broader activity, stable against b-lactamases, 5 generations, made from mold, IV/PO, cross-reactivity to PCN so caution w/pts. allergic to PCN; excretion: renal/biliary
beta lactams penicillins, cephalosporins, monobactams, carbapenems
first generation cephalosporins beta-lactam,limited range of activity, active against g+ cocci
second and third generation cephalosporins beta-lactam, expanded gram-coverage, treat wide variety of infections, unknown to b-lactamases susceptibility
fourth generation cephalosporins beta-lactam; resistant to b-lactamases, CNS penetration: cross BBB, better against PCN resistant streptococci, similar to 3rd generation
fifth generation cephalosporins beta lactam,IV only, active against gram+(MRSA, VRSA, VISA), used for bacterial skin infections acute, community acquired pneumonia
monobactam beta-lactam, 1 ring, resistant to b-lactamase, no PCN cross-reactivity, active against gram-rods, inactive against gram+ and anaerobic bacteria
Aztreonam (Azactam) monobactam
Cefepime (Maxipime) 4th generation cephalosporin
Ceftaroline (Teflaro) 5th generation cephalosporin
Cefazolin (Ancef) 1st generation cephalosporin, IV/IM, used for surgical prophylaxis
Carbapenems beta lactam, resistant to b-lactamase, widest spectrum, prescribed with cilastin (primaxin)
Imipenem carbapenems (beta lactam)
Cilastin (primaxin) inhibits dehydropeptidase (which inhibits imipenem, renal enzyme located in renal tubules occur during reabsorption)
Inhibit bacterial DNA synthesis antifolate, DNA gyrase inhibitors (fluoroquinolones), sulfonamides, trimethoprim-sulfamethoxazole (TMP-SMX),pyrimethamine
Antifolate inhibit bacterial DNA synthesis, no production of purines and nucleic acids = no DNA
Sulfonamides inhibit bacterial DNA synthesis,rarely used, compete with PABA for dihydopteroate synthase enzyme, widespread resistance (mutation), fever, skin rash, dermatitis, photosensitivity, crystalluria(sulfa in urine), bone marrow suppression, stevens-Johnson
trimethoprim-sulfamethoxazole (tmp-smx) inhibit bacterial DNA synthesis, PO/IV, eliminated in urine, used for UTI, broad spectrum, synergism, trimethoprim: concentrates in vaginal and prostatic fluid
pyrimethamine inhibit bacterial DNA synthesis, uses: leshmaniasis, toxoplasmosis
fluoroquinolones inhibit bacterial DNA(gyrase)synthesis prevent uncoiling of DNA,replication, transcription,absorbtion decreased by antacids,resistance: mutation of DNA gyrase; QT elongation, hypokalemia, avoid class 1,2 antiarrhythmics, N/V/D, damage growing cartilage
DNA gyrase topolsomerase that removes DNA supercoils so it may be transcribed and replicated
inhibit bacterial translation (PRO synthesis: RNA into PRO) tetracyclines, macrolides, lincosamides, streptogramines, oxazolidinones, aminoglycosides; may effect PRO synthesis in human cells
tetracyclines (-cyclines) inhibit bacterial translation, AE:bone/teeth (low ca+), discolored teeth r/t UV absorb, N/V, photosensitivity, bacteriostatic,wide spectrum, gram-/+, excretion:bile/urine, PO absorbtion decrease by dairy products, antacids, bismuth
macrolides inhibit bacterial translation, attach to 50 s ribosome, AE:torades de pointes; broad spectrum, excellent lung penetration, bacteriostatic-low doses, bactericidial-high doses SE:liver effects, N/V/D;chlamydia, legionella, S.pneumonia; stimulate GI activity
erythromycin macrolide,inhibit bacterial translation, short-half life (q6h), excreted in bile/feces, with clindamycin (cleocin) inhibit CYP450 enzymes
clarithromycin macrolide,inhibit bacterial translation, metabolized in liver, longer half-life (6hrs); h.pylori, m.avium, m.leprae, toxoplasma gondii, h. influenza, lower incidence of GI intolerance (compared to erythromycin)
azithromycin macrolide; inhibit bacterial translation, long half-life(3 days), food decrease absorption, well tolerated PO, rapidly absorbed; antacids, Mg+, aluminum delay absorption and peak serum concentration, but do not alter bioavailability
erythromycin, azithromycin (Zithromax), clarithromycin (biaxin) macrolides
lincosamides cleocin-clindamycin, inhibit bacterial translation
Clindamycin (cleocin) similar to erythromycin inhibit bacterial translation,lincosamides; strept,staph,skin/soft tissue infections w/MRSA,severe anaerobic infections (ulcerations,peptic ulcers);pseudomembranous colitis w/Cdiff-found in normal intestine flora not killed by PO cleocin so it overgrows
Streptogramins: Quinupristin-dalfopristin inhibit bacterial translation, 30:70 mixture(2 chemicals), bactericidal,active IV against multi-resistant gram+ (vanco resistant infection), little mild toxicity: arthralgia, myalgia
oxazolidinones: Linezolid (Zyvox) inhibit bacterial translation; active against drug resistant gram+(MRSA, VRE), AE: mild, reversible neutropenia, mild thrombocytopenia
Aminoglycosides inhibit bacterial translation,bacteriocidal, gram-,used w/beta-lactam, vanco:extended coverage, synergistic, overcome resistance, confuse bacteria; SE: nephrotoxicity,ototoxicity (like vanco), poor GI absorption, resistance: mutation
streptomycin, gentamicin, tobramycin, netilmicin, neomycin, kanamycin, amikacin aminoglycosides
streptomycin aminoglycosides, inhibit bacterial translation,2nd line tx for TB, nontuberculous infections-give IM in combo with PO tetracycline, AE: vestibular fxn (vertigo, loss of balance); cause deafness in newborns
gentamicin aminoglycosides, inhibit bacterial translation, g-/+, resistance: mutation, inactivation of enzymes, decrease drug permeability to penetrate cell
tobramycin aminoglycosides, inhibit bacterial translation
netilmicin aminoglycosides, inhibit bacterial translation, protected from enzymatic degradation, same characteristics as gentamicin and tobramycin, no longer used in U.S.
neomycin/kanamycin aminoglycosides, inhibit bacterial translation,used for bowel prep for sx, poorly absorbed in GI, excreted in feces/renal, intestinal flora suppressed given PO,
Amikacin aminoglycosides, inhibit bacterial translation,resistant to many enzymes that inactivate gentamicin/tobramycin
Created by: cburrows



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