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77 Cards in this Set
- Front
- Back
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Pen G / V spectrum/use/difference
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Narrow spect penicillinase-susceptible agents. Strep, meningococci, gram+ bacilli, spirochetes. V is oral.
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Meth/Naf/Oxacillin spectrum/use
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Very-narrow penicillinase-resistant. Staph aureus/epidermidis.
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Ampicillin/Amoxicillin spectrum/use/special
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Wider spectrum penicillinase-susceptible. Use similar to Pen G + enterococci, listeria, E.Coli, proteus, hemophilus. Special- combine with penicillinase-inhibitors and/or aminoglycosides
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Piperacillin/Ticarcillin spectrum/use
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Wider spectrum penicllinase-susceptible. Gram- rods (psuedomonas, enterobacter, klebsiella). combine with penicillinase-inhibitors and/or aminoglycosides
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General specialties about Cephalosporins
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1. Almost all are used parenterally.
2. Major elimination is renal excretion (note Ceftriaxone is via bile) 3. 1st/2nd generations generally do not cross BBB even in inflammation |
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1st gen cephalo spectrum/use/examples
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Gram+ cocci, some E.coli and Klebsiella species. Cefazolin, Cephalexin (this one is ORAL!)
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2nd gen cephalo spectrum/use/examples
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Compared to 1st gen - less Gram+ coverage, extened Gram- coverage. Examples for use are for Bacteroides Fragilis and Hempophilus. Cefoxitin, Cefuroxime.
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3rd gen cephalo spectrum/use/examples
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Increased activity against Gram resistant to other Beta-Lactams.Penetrate BBB. Useful against Provdenica, Serratia, Neisseria, Hemophilus. Ceftazidime also against Pseudomonas and Ceftizoxime and Bacterodies. More examples - Ceftriaxone, Cefixime (ORAL!)
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4th gen cephalo spectrum/use/exmaples
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Combined Gram+ activity of 1st gen with Gram- activity of 3rd gen. Cefepime. More resistant to Beta-lactamses.
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Aztreonam - group, use, special
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Monobactam, Gram- only. Useful for Gram- rods as it is resistant to beta lactamases by Klebsiella, pseudomonas. Synergistic with aminoglycosides, renal clearance
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Carbapenems - spectrum, use, special
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Gram+ cocci, gram- rods, anaerobes. Good for pseudomonas and drug of choice for enterobacter. Imipenem Inactivated by renal dehydropeptidase I - use with Cilastatin. Meropenem is not inactivated.
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Beta-lactamase inhibitors - examples, use
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Calvulanic acid, sulbactam. Most active against plasmid-encoded resistance of gonococci, strep, E.coli
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Vancomycin - uses, administration possibilites, special
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MRSA, Pen-resistant pneumoocci, Clostridium difficle. Orally for bacterial enterocolitis or panenterally for all other uses. NOT absorbed from GI. Rapid IV infusion may cause diffuse flushing - Red Man syndrome.
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Fosfomycin - MOA, special
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Inhibitor of NAM formation. Excreted by the kidney with urinary levels exceeding the MIC.
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Chloramphenicol,Tetracyclins, Macrolides, Clindamycin, Streptogramins, Linezolid - MOA, which one is bactericidal
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30s - Tetracyclins, all others 50s. Linezolid - 23s rRNA of 50s. Streptogramins are bactericidal, all others bacteriostatic.
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Chloramphenicol - spectrum/use/toxicity
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Spectrum - wide, hemophilus-neisseria-bacteroids highly susceptible. Use-Limited due to toxicity, topical usually, backup drug for meningitis and rickettisa. Toxicity-GI, Aplastic anemia, Gray Baby
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Tetracyclins- spectrum/use/toxicity
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Spectrum- Broad, gram+,gram-,rickettsia/chlamydia/protozoa.
Use- Chlamydia/rickettsia/mycoplasma pneumonia. 2ndary for syphillis. Doxycycline- Lyme. Demeclocycline-renal ADH antagonist. Toxicity-GI, tooth enamel dysplaisa, hepato/renal toxicity,photosensitivty |
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Macrolides- spectrum/use/toxicity/special
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Spectrum- broad,campylobacter,chlamydia,legionella,gram+, some gram-, MAC,toxoplasma. Use-Mainly used for gram- infection such as Myocplasma,campyolobacter,legionella,bordetella.
Note- Azitromycin good for Hemophilus,moraxella,neisseria. Toxicity-GI,Hypersensitivty, P450 inhibition(digioxin,theophylline). Special- Azithromyicn HL is 2-4days ! |
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Telithromycin-use
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Similar spectrum to macrolides however less resistance is present. Useful in community-acquired pneumonia
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Clindamycin-Cross-resistance,use,toxicity
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Cross-resistance with macrolides and lincosamides is common. Use-severe anerobic infections such as Bacteroides and Toxoplasma. Toxicity-GI, Neutropenia,Pseudomembranous collitis
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Streptogramins-name of drugs, use, toxicity
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Quinupristin-Dalfopristin. Bactericidal. Use- MRSA, VRSA, resistant Enterococci. Toxicity-Arthralgia/Myalgia, Cyp3A4 inhibition.
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Linezolid- spectrum, cross resistance, toxicity
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Spectrum- Drug-resistant Gram+ including strains resistant to Vancomycin. NO cross-resistance. Toxicitiy- Thrombocytopenia/mneutropenia
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Aminoglycosides- Basis for once-daily protocol, pharmacokinetics
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Instead of the usual time-dependant acitivty of most AB, Aminoglycosides have a concentration-dependant activity. Also they feature a postantibiotic effect. 3rd- toxicity does depend on time a certian level is maintained. Is not absorbed orally. Do not cross BBB. Renal clearance, adjust in renal insuff.
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Aminoglycosides- work on? special? least susceptible AG to enzymatic inactivation by bacteria?
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Work on 30S, require oxygen to penetrate bacteria, synergistic with cell-wall synthesis inhibitors. Least resistance is found to Netilmicin.
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Aminoglycosides- Uses
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Large differences between different AG. Genta/Tobra useful in serious aerobic Gram- infections such as E.Coli, Enterobacter, Klebisella, Proteus...
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Aminoglycosides-Streptomycin good for? when should it be used?
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TB, plague, tularemia. Only when other drugs do not work, very toxic.
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Aminoglycosides- Toxicities, loop diuretics? Pregnancy?
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1.Ototoxicity- proportionate to plasma levels. Increased by loop diuretics !! CONTRAindicated in pregnancy - fetal ototoxic.
2.ATN 3.Rare curare-like neuromascular block-resp. paralysis |
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Sulfonamides - use/toxicity
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Use- UTIs, topical, IBDs, toxoplasma
Toxicity- Hypersensitivty, neutropenia, aplsatic anemia, nephrotoxic (precipitation) |
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Sulfonamides- special interactions
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Increases plasma levels of Warfarin and MTX due to protein binding competition, bilirubin levels also increased - kernicterus if used during 3rd trimester
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Fluoroquinolones - generations, spectrum,examples
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1st gen- norflox - UTIs
2nd gen - Cipro- wider action, also gonococcus, mycoplasma, some gram+ 3rd gen- Levoflox- greater gram+ activity ,slightly less gram-, some Strep pneumonia and some MRSA even 4th gen- Moxiflox- broadest spectrum, some anerobes |
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Fluoroquinolones- kinetics, clinical use
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Kinetics- good oral bioavail (however note norflox does not reach systemic levels very well), mostly renal clearance-adjust dose. HL in the range of 3-8h.
Clinical use- UTIs, GI, pseduomonas. Cipro-gonorrhea, Levo-community acquired pneumonia |
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Fluroquinolones- toxicity
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GI, superinfections, hepatotoxic. Also - cartilage problems in children/pregnancy, increased levels of Theophylline. Sparflox(3rd gen)- QT prolongation
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Name the 4 usual anti-mycobacterial drugs + 2 alternative drugs + the usual drug for leprosy
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Isoniazid, Rifampin, Ethambutol, Pyrazinamide. Alternatives- Streptomycin, Cipro. Leprosy- Dapsone
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Isoniazid- MOA, Kinetics, toxicity
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MOA- inhibition of Mycolic acid(cell wall component) synthesis. PK- Oral bio, variable acetylation (europe=slow). Toxic- neurotoxic(give pyridoxine prophy), hepatotoxic, hemolysis in G6PD
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Rifampin- MOA, other clinical uses, toxicity, special
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MOA- Inhibition of DNA-dependant RNA pol. PK- oral bio, colors feces orange. Also good for carrier states of meningococci. Toxic- light-chain proteinuria, nephritis, liver dysfunction. Strong p450 inducer. Special- Rifabutin is same but shows less drug interactions.
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Ethambutol- MOA, pk, toxicity
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MOA- Inhibits syhtnesis of Arabinogalactan(cell wall). Oral bio, dose reduction in renal failure. Toxic- visual disturbances, color blindness; peripheral neuritis
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Pyrazinamide- MOA, toxicity
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MOA- unknown, requires conversion via pyrazinamidases, BACTERIOSTATIC. Toxic- polyarthralgia, porphyria, hyperuricemia
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Dapsone- MOA- pk, toxicity
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MOA- inhibitions of folic acid synthesis, oral bio. Toxic- GI, methemoglobinemia, hemolysis. Acedapsone- several months repository
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MAC drugs
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Prophylaxis- Azithromycin/clarithtomycin. Tx- + ethambutol, rifabutin
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Name 4 antiherpes drugs, which ones are NOT dependant on virus kinases?
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Acyclovir, Gancyclovir, Cidofovir, Foscarnet, Vidarabine. NOT dependant on viruse kinases --> Cidofovir, Foscarnet
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Acyclovir - use, toxcitiy, congeneres
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Use- HSV, VZV. herpes lesions, herpes encephalitis, prophylaxis. Toxic - delerium, tremor, nephrotoxic.Congeners- Famciclovir, Valcyclovir (longer HL)
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Ganciclovir- use, toxicitry
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Use- HSV, CMV. Use in CMV retinitis and CMV in IC patients. Toxic- Leukopenia, thrombocytopenai, hepatic dys
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Cidofovir - use, toxicity
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CMV, HSV, Adenovirus, Papillomavirus. Serious nephrotoxicity
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Foscarnet- use, toxicity
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Inhibits viral RNA pol and HIV RT. Use in HSV, CMV. Toxic- nephrotoxic, cNS
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Vidarabine- MOA, activity, use, toxic
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Adenine analog, HSV, VZV, CMV. Used in severe HSV, VZV. Toxic- GI, hepatic
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Name 2 NRTIs + MOA, use, toxicity
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Zidovudine (ZDV, AZT)- also used for prophylaxis needle stick etc, Toxic- BM suppression,. hepatitis.
Didanosine- oral bioavail reduced by food. Toxic- Pancreatitis. Abacavir- serious hypersensitivty reactions |
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Name 2 NNRTIs + MOA, use, toxicity
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Nevirapine- effecitve in preventing vertical trans, hypersensitivty reactions.
Delavirdine- drug interactions a major problem, teratogenic in animals |
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Name 2 Protease Inhibitors - explain
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Indinavir- good orally, thrombocytopenia, nephrolithiasis.
Ritonavir- hepatic clearance. Can inhibit Cyp3A metabolism of other PI and therefore is used in combination with them to allow lower levels |
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Enfuvirtide- what is it, when is it used ?
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a synthetic peptide that binds to gp41 of HIV and prevents fusion. Used in presistent HIB-1 replication.
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Name 3 drugs for influenza, explain
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Amantadine, Rimantadine, Oseltamivir. Amantadine/rima prevent uncoating of Influenza A . Can be used both for tx and prophy. Rimantadine- longer HL, no renal dose adjustemnet necessary.
Oseltamivir- NA inhibitors of Influenza A + B. Decrease viral spread. |
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Name 4 agents used for viral hepatitis
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Inf-alpha, adefovir, lamivudine, ribavirin.
Inf-alpha: activation of host ribonucleases and KN cells, useful in chronic HBV and in HCV. Toxic- neutropenia, alopecia, thyroid dys. Adefovir- HBV DNA pol inhibition. No resistance known. Nephrotoxic and steatosis. Lamivudine- HIV RT inhibitor. Good for chronic HBV- suppresses replication, non toxic almost. Ribavirin- Influenza A,B. Parainfluenza, RSV, Paramyxo, HCV, HIV. Prevents mRNA capping, block RNA-dependent RNA pol. Toxic- Hemolytic anemia, TERATOGENIC- CI in pregnancy. |
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Chloroquine- MOA, use, toxicity
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Causes accumulation of Heme (toxic). Blood schizonticide - not useful against resistant falciparum. Also useful in RA. Toxic- skin lesions, neuropathies, psychosis, porpghyria
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Quinine- MOA, use, toxicity
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MOA- Blood schizonticide, block DNA replication. USeful against falciparum together with Doxycycline/Clindamycin. Sever infections may require Quinidine.
Toxic- Cinchonism, Blackwater fever, CI in pregnancy. |
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Mefloquine- use, toxicity
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Use- prophy in areas with chloroquine resistance, and an alternative to Quinine for Falciparum. Toxic- Cardiac conduction defects, seizures.
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Primaquine- MOA, use, toxicity
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MOA- creates cellular oxidants, tissue schizonticide. Use in conjunction with a blood schizonticide. CI in pregnancy.
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Name antifolate drugs used in Malaria
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Pyrimethamine, Proguanil, Sulfadoxine, Dapsone. Shortest HL Proguanil (12h).Pyrimethamine+Sulfadoxine = Fansidar , good for chloroquine-resistant strains
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Name 2 tissue amebicides and 2 luminal amebicides
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tissue - Emetines, Metronidazole. Luminal- Diloxanide Furoate, Iodoquinol
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Diloxanide Furoate - use, Emetines- MOA, use.
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Diloxanide Furoate- mild intestinal amebiasis.
Emetines- Block protein synthesis, use in severe intestinal or hepatic amebiasis |
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Iodoquinol - use, toxicity. Metronidazole- MOA, use, toxicity
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Iodoquinol- mild to severe intestinal infections, toxic- thyroid enlargement, peripheral neuropathy. Metronidazole- Forms reactive cytotoxic products, useful in severe intestinal wall disease and hepatic/other amebiasis. Also used in trichomonas, Giardia, Gardnerella, H.Pylori.
Toxicity- Leukopenia, ataxia, disulfiram-like reaction |
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Name 4 drugs for Pneumocytstosis and Toxoplasmosis
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Pentamidine, TMP-SMX, Pyrimethamine/sulfonamides, Atovaquone
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Pentamidine- MOA, use, toxicity
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MOA- unknown, might interfere with glycolysis or AA metabolism. use- Prophy and tx of Pneumocystosis, hemolymphatic stage of T.Gambiense/Rhodesiense. Toxic- resp. depression, hypotension, neutropenia, hepatitiis, pancreatitis, anemia
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Pyrimethamine+Sulfadiazine -use, toxicity
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Use- Toxoplasma gondii tx & prophy, prophy against pneumocystosis in AIDS patients. Toxic- glossitis, seizures, megaloblastic anemia, thrombocytopenia
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Atovaquone- MAO, use
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Inhibits mitochondrial electron transport+folate metabolism. Use- pneumocytsis pneumonia. As Malarone (with Proganul) for prophy & tx of chloroquine-resistant malaria
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Name 4 drugs for Trypanosoma
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Pentamidine, Melarsoprol, Nifurtimox, Suramin
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Melarsoprol- MOa, use. Nifurtimox- MOA, use
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Melarsoprol- organic aresnical, useful in African sleeping sickness. Nifurtimox- Inhibits trypanthione reducatase. Useful in American sleeping sickness, African one, and mucocutaneous leishmaniasis
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What is the main drug for Leishmaniasis, what is its MOA and toxicity. What are alternative drugs ?
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Sodium Stibogluconate. MOA- inhibition of glycolysis and effects on nucleic acid metabolism. Toxic- QT prolongation. Alternatives- Pentamidine, Metronidazole, Amphotericin B
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Name 5 antihelmintic drugs
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Albendazole, Mebendazole, Diethylcarbamazine, Ivermectin, Piperazine, Pyrantel Pamoate
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Albendazole- MOA, use
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MOA- unclear, blocks glucose uptake, inhibits microtubule assembly. Use- wide, ascaris, necator, enterobius, trichuris, filiriasis.
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Diethylcarbamazine- mOA, use, toxicity
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MOA- unclear, use- loa loa, elephentiasis, alternative for onchocerca. Toxic- mainly reaction to dying filariae - Mazzotti Reaction (hypotension, pyrexia, muslce pain..)
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Ivermectin- MOA, use, toxicity
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MOA- enhanced GABA transmission, flacid paralysis. Selective- does not cross BBB. Use- onchocerca, strongyloidosis, filiarsis. Toxic- Mazzotti reaction
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Mebendazole- MOA, use, toxic
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Same as Albendazole - glucose uptake inhibition, microtubules assembly inhibition. Use- Ascariasis, Enterobius, Trichuris. Toxic- CI in pregnancy
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Piperazine- MOA, use, toxic
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GABA agonist. use- ascaris. toxic- DO NOT use in patients with seizures
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Pyrantel Pamoate- MOA, use, toxicity
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MOA- Nicotinic receptors activation - depolarizing blockade. Use- wide
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Name a few trematodes and 2 drugs to treat their infections
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Schistosoma, Clonorchis, Paragonimus. Main drug- Praziquantel. Alternative drugs- Bithinol, Metrifonate
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Praziquantel- MOA, use, toxicity
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MOA- Increaesd calcium permeability. Use- wide - trematodes+cestodes(tenia, diphylobothrium, echinococcus). Toxic- headache, malaise, fever. CI in ocular cysticercosis (??)
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Name a few cestodes and the drug of choice against them
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Taenia saginata, solium; Diphylobothrium Latum, Echinococcus. Drug of choice - Praziquantel + Niclosamide
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Niclosamide- MOA, use, toxicity
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MOA- Oxidative phospohrylation uncoupling. Use- all cestodes, however NOT GOOD for cysticercosis or echinococcus hydatid cyst.
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