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Antibiotics
Immunity
| Term | Definition |
|---|---|
| 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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