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Antibiotics-MSI
Cell Wall Active Ab, Folate Inhib, Antifun, Protein Synthesis inhib, immunosupp
| Question | Answer |
|---|---|
| Penicillin G | Natural Penicillin, IV, GAS |
| Penicillin V | Natural Penicillin, P.O., better absorbed, resistant to gastric enzymes |
| Procaine(Benzathine) Penicillin | IM, SLOW absorption |
| Methicillin | Anti-staph, resistant to penicillinases, can have MRSA |
| Oxacillin | anti-staph penicillin, IV, given in hospital for systemic staph infection(second to nafcillin) |
| Nafcillin | anti-staph penicillin, IV, given in hospital for systemic staph infection |
| (Di)cloxacillin | anti-staph penicillin, P.O., mild, localized staph/strep infection, soft tissue/skin |
| Ampicillin | Aminopenicillin, IV, E.coli(child meningitis), H. flu, salmonella |
| Amoxicillin | aminopenicillin, p.o., better absorbed, UTI, otitis medica |
| Piperacillin | antipseudomonal penicillin(treat difficult gram -), pseudomonas, less Na than carbenicillin |
| Carbenicillin | antipseudomonal penicillin, treat difficult gram - bacteria, extremely high sodium load bad for heart pts. |
| Cefazolin | 1st gen. cephalosporin, gram +, does not get into CNS, IV, use if have penicillin allergy, does not cause vein thrombosis |
| Cephalexin | 1st gen. cephalosporin, gram +, po, skin and soft tissue infections of staph/strep |
| Cefamandole | 2nd gen. cephalosporin, gram - active(decreased gram + compared to 1st gen), H. flu |
| Cefuroxime | 2nd gen. cephalosporin, gram -, gets into CNS well, child meningitis |
| Cefoxitin | 2nd gen cephalosporin, anaerobic bacteria |
| Cefotetan | 2nd gen. cephalosporin, anaerobic bacteria |
| Natural Penicillins | most useful against gram +, penicillin G(IV), penicillin V(po) |
| Anti-Staphylococcal Penicillins | resistant to penicillinases, methicillin, oxacillin(IV), nafcillin(IV), (Di)cloxacillin(po) |
| Aminopenicillins | developed to attack gram - bacteria(E.coli & enteric), not good at attacking pseudomonas & other difficult gram - bacteria, ampicillin(IV), amoxicillin(po) |
| Anti-pseudomonal penicillins | developed to treat difficult gram - and pseudomonas, ticarcillin, piperacillin |
| 1st Generation Cephalosporins | active against gram +, does not get into CNS, not active against MRSA, cefazolin(IV), cephalexin(po) |
| 2nd Generation Cephalosporins | 2 types: 1. those with activity against gram -, 2. those active against anerobic bacteria, decreased activity against gram +, cefamandole, cefuroxime, cefoxitin, cefotetan |
| 3rd Generation Cephalosporins | active against gram -, penetrates CNS, Cefotaxime, Ceftriaxone, Ceftazidime, Cefepime, Moxalactam |
| Cephalosporins with NMTT side chain | N-methyl thiotetrazole side chain responsible for several ADRs including bleeding and an atabuse effect, moxalactam, cefotetan, cefamandole, cefoperazone |
| Cefotaxime | 3rd gen. cephalosporin, child meningitis |
| Ceftriaxone | 3rd gen. cephalosporin, long t1/2, pneumococci(meningitis) |
| Cetazidime | 3rd gen cephalosporin, pseudomonas aeruginosa |
| Cefepime | 3rd gen cephalosporin, pseudomonas aeruginosa |
| Moxalactam | 3rd gen cephalosporin, pseudomonas aeruginosa, life-threatening bleeding, antabuse effect |
| Carbapenems | gram +, gram -, aerobic, anaerobic, fairly resistant to beta-lactamases, imipenem, meropenum |
| Imipenum | carbapenem, broad spectrum, H. flu, enterobacteriae, child meningitis, must be formulated with cilastatin to preserve antibacterial activity and avoid nephrotoxicity, pseudomonas can become rapidly resistant to imipenem, don't use if not necessary |
| Meropenum | carbapenum, similar to imipenem except is not degraded by dihydropeptidase |
| Dihydropeptidase | degrades imipenum to a by-product with no antibacterial effects and produces a nephrotoxic agent, must combine imipenem with cilastatin to prevent attack of imipenem by dihydropeptidase |
| Monobactams | gram - including pseudomonas, no activity against gram + or anaerobic, aminoglycoside-like without toxicity, only one in US: aztreonam |
| Aztreonam | only monobactam available in US, gram - including pseudomonas, no gram + or anaerobic, aminoglycoside-like without toxicity |
| 4 Resistance Mechanisms to beta-lactam antibiotics | 1. enzymes from bacteria degrade Ab, 2. mutations in penicillin binding proteins, 3. mutations in bacterial porins(mediate Ab entrance), 4. efflux pumps |
| Beta-lactamase Inhibitor Combinations | effective against beta-lactamases from gram + and gram - organisms, NOT against beta-lactamases encoded by the chromosome of gram -(pseudomonas and serratia), useful against staph, strep, enteric gram - and most anaerobes |
| Ampicillin/Sulbactam | beta-lactamase inhibitor combination, IV, active against gram -, staph and anaerobes |
| Amoxicillin/Clavulanate | beta-lactamase inhibitor combination, PO, active against gram -, staph and anaerobes |
| Ticarcillin/Clavulanate | beta-lactamase inhibitor combination, active against gram -, staph and anaerobes |
| Piperacillin/Tazobactam | most frequently used beta-lactamase inhibitor combination, active against gram -, staph and anaerobes |
| Glycopeptides | active against gram +, staph, strep and MRSA!!, used to be active against enterococci but recent emergence of vancomycin resistant enterococci(VRE-use penicillin + aminoglycoside), vancomycin, ONLY USEFUL IF BACTERIA IS NOT SENSITIVE TO BETA-LACTAM DRUGS |
| Vancomycin | glycopeptide, gram +, staph, strep, MRSA, VRE |
| MRSA | Vancomycin |
| VRE | Penicillin + Aminoglycoside |
| Folic Acid Inhibitors | Sulfonamides, DHF reductase inhibitors, bacteria need to synthesize folic acid while humans only use preformed folic acid, combo of these drugs can give synergistic affect |
| Sulfonamides | Folic Acid Inhibitor, competitive inhibitor of PABA, treat UTI, malaria, sulfanilimide, sulfamethoxazole, sulfisoxazole, sulfadiazine |
| Sulfanilamide | sulfonimide(folic acid inhibitor), competitive inhibitor of PABA |
| Sulfamethoxazole | sulfonimide(folic acid inhibitor), competitive inhibitor of PABA |
| Sulfisoxazole | sulfonimide(folic acid inhibitor), competitive inhibitor of PABA, quickly excreted in urine (UTI) |
| Sulfadiazine | sulfonimide(folic acid inhibitor), competitive inhibitor of PABA, gets into CNS(used to be used to treat meningitis) |
| Dihydrofolate Reductase Inhibitors | Inhibit reduction of DHF to THF, trimethoprim, pyrimethamine, trimetrexate |
| Trimethoprim | DHF reductase inhibitor(folic acid inhibitor), used by itself or in combo with sulfamethoxazole, drug concentrated in urine(UTI), used in HIV pts to prevent pneumocystis, variety of illnesses |
| Pyrimethamine | DHF reductase inhibitor, toxoplasmosis, malaria |
| Trimetrexate | DHF reductase inhibitor(folic acid inhibitor), if can't use trimethoprim + sulfamethoxazole |
| Antifungals | Most work by interfering with ergosterol synthesis or use |
| Polyenes | antifungal drug that combines with preformed ergosterol and disrupts the membrane of the fungus |
| Azoles | antifungal, inhibits the synthesis of ergosterol by blocking the demethylation of lanosterol to give ergosterol, ketoconazole, fluconazole, itraconazole, clotrimazole, voriconazole |
| Amphotericin B | polyene(antifungal), IV, used for systemic fungal infections, VERY long t1/2(weeks/months), can be put in liposomes to decrease toxicity |
| Nystatin | polyene(antifungal), topical, candida infections of oral cavity |
| Ketoconazole | azole(antifungal), po, inhibits the synthesis of ergosterol by blocking the demethylation of lanosterol |
| Fluconazole | azole(antifungal), inhibits the synthesis of ergosterol by blocking the demethylation of lanosterol, candida infections, UTI, vaginitis |
| Itraconazole | azole(antifungal), replaces ketoconazole, inhibits the synthesis of ergosterol by blocking the demethylation of lanosterol |
| Clotrimazole | azole(antifungal), inhibits the synthesis of ergosterol by blocking the demethylation of lanosterol |
| Voriconazole | azole(antifungal), inhibits the synthesis of ergosterol by blocking the demethylation of lanosterol, broaden azole activity(not just yeast phase), aspergillus and candida |
| Terbinifine | Antifungal, blocks conversion of squalene to lanosterol by inhibiting squalene epoxidase, used for dermatophyte infections, sole indication: onychomycosis |
| Echinocandins-Caspofungin | antifungal drug that blocks the synthesis of B(1,2)-D-glucan, a component of the fungal cell wall, used for aspergillus and candida infections |
| Rifampicin | Inhibitor of RNA polymerase, resistance develops rapidly, long t1/2, wide distribution, enterohepatic circulation, stains everything orange, induces p450, treat Tb, "tolerant" organisms |
| Clofazimine | Inhibitor of RNA polymerase, related to rifampicin, long t1/2, red/brown stain, treat leprosy |
| Quinolones | Inhibitors of DNA synthesis/replication, inhibit DNA gyrase and topoisomerase(therefore inhibit supercoiling and unwinding), gram - ONLY, poor tissue penetration, atypical bacteria |
| Fluroquinolones | Inhibitors of DNA synthesis/replication, well absorbed orally, reserved for serious infections that are resistant to other antibiotics |
| Acylovir | Inhibitor of DNA & RNA synthesis, clincal use as an anti-viral |
| Metronidazole | DNA breakage inducer, treat trichomonal infections, anaerobic bacteria, diffuses well, antabuse-like reaction |
| Linezolid | Inhibitor of aa-tRNA synthetase, inhibits formation of fmet-tRNA, gram + ONLY, used in bacteria resistant to other Ab(MRSA, VRE, resistant pneumococci), $$$$ |
| Mupirocin | Inhibitor of aa-tRNA Synthetase, used only for gram + skin infections |
| Aminoglycosides | Inhibitors of the Initiation complex, misreading of genetic code, resistance develops rapidly, no po absorption, does not penetrate CSF, renal elimination, gram -, oral form to sterilize gut, TOXICITY(ear, renal, neural) |
| Tetracyclines | Inhibitor of Initiation complex, broad spectrum, po, chelates bone & teeth(Ca2+), phototoxicity, renal and liver disease, increased intracranial pressure in infants |
| Chloraphenicol | Inhibitor of Peptide Bond Formation and Elongation, inhibits peptidyl synthetase, needs to be conjugated or will cause cardiotoxicity |
| Clindamycin | Inhibitor of Peptide Bond Formation and Elongation, inhibitor of peptidy synthetase, restricted to gram +, MAY CAUSE PSEUDOMEMBRANOUS COLITIS |
| Erythromycin | Macrolide, inhibits translocase, gram + infections in pts allergic to beta-lactam Ab, mycoplasma infections, impetigo(staph, strep), Legionnaire's bacillus, Pertusis(especially carriers), unstable in gastric juices |
| Clarithromycin | macrolide, inhibit translocase, modify lactone ring of erythromycin and expand spectrum |
| Azithromycin | macrolide, inhibit translocase, modify lactone ring of erythromycin and expand spectrum and resist gastric upset, otitis media/sinusitis, community acquired ammonia |
| Quinupristin & Dalfopristin(Q/D) | given together, inhibits translocase, restricted to gram + cocci, 2 uses: 1. VRE, 2. skin infections with staph/strep, $$$$ |
| Isonazid | Tb, inhibits synthesis of mycolic acid(unique in mycobacteria cell wall), toxicity=decreased B6 utilization, must supplement |
| Immunosuppressive Agents | suppress aberrant or unwanted immune response in autoimmune diseases, transplant rejection and GVHD |
| Corticosteroids in B cell response | Immunosuppressive Agents, ((methyl)prednisone, dexamethasone), cytolytic for lymphocytes, decrease circulating Ig levels, inhibit macrophage function |
| Intravenous Immunoglobulin | allows saturation of Fc receptors on phagocytes and neutralizes auto-antibodies |
| Splenectomy | decrease rate of platelet-ab clearance |
| Cyclophosphamide | cytotoxic agent that induces DNA strand breaks |
| Rituximab | antilymphocyte antibody that is specific for B cells and targets CD20 on cell surface in B cells actively producing antibodies |
| Cyclosporine | cytokine suppressive agent, inhibits calcineurin resulting in blocking of the transcription of the IL-2 gene, impairs the T cell response |
| Azathioprine | Cytotoxic agent, purine analog that is incorporated into DNA and prevents transcription leading to early cell death |
| Tacrolimus | cytokine suppressive agent, inhibits calcineurin resulting in blocking of the transcription of the IL-2 gene, impairs the T cell response, more potent than cyclosporine |
| Rapamycin | inhibits the translation of IL-2 mRNA, blocks CD28 costimulatory molecule, synergistic with tacrolimus or cyclosporine |
| Corticosteroids in T cell response | inhibit leukocyte adhesion to endothelium, inhibit PMN migration, decrease lymphocyte traffic |
| Corticosteroids in GVHD | interfere with IL-1, IL-2 production, stabilize lysosomal membrane, decrease capillary permeability, inhibit histamine release, inhibit kinin and complement systems |
| Daclizumab | antilymphocyte antibody that targets the IL-2 receptor on T cells |
| Overall Adverse Affects of Immunosuppressive Agents | Opportunistic Infections and Malignant Lymphoma |
Created by:
akline01
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