Term
| Chloramphenicol is a natural product with a _____ moiety. |
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Definition
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Term
| What are the mechanisms of resistance against chloramphenicol? |
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Definition
| acetylation, efflux, mutations in ribosomes |
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Term
| Is chloramphenicol bacteristatic or bactericidal? |
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Definition
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Term
| How is chloramphenicol administered? |
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Definition
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Term
| What is the distribution and excretion of chloramphenicol? |
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Definition
| wide distribution including the CSF; present in bile, milk, and placental fluid; rapidly excreted by kidneys |
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Term
| What diseases are treated by chloramphenicol? |
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Definition
| typhoid fever, bacterial meningitis, anaerobic infections, rickettsial disease (second choice drug) |
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Term
| What are the toxicities of chloramphenicol? |
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Definition
| hypersensitivity, hematological toxicity, GI, gray baby syndrome |
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Term
| What is the mortality rate of gray baby syndrome? |
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Definition
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Term
| How long after dose does gray baby syndrome show up? |
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Definition
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Term
| What drug interactions occur with chloramphenicol? |
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Definition
| prolongs half lives of warfarin, dicumerol, and anti retroviral protease inhibitors |
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Term
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Definition
| erythromycin (natural product), clarithromycin and azithromycin (semisynthetic derivatives) |
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Term
| Are macrolides bacteristatic or bactericidal? |
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Definition
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Term
| What are macrolides used to treat? |
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Definition
| effective against G+, atypical mycobacteria and some intracellular bugs; mycoplasma, legionaire's disease, chlamydia infections, diphtheria/pertusis, staph/strep, GI infections, tetanus, AIDS related infections |
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Term
| What are the mechanisms of resistance against macrolides? |
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Definition
| efflux, ribosomal protection, esterases, mutate ribosomes |
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Term
| How are macrolides administered? |
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Definition
| orally but gastric acid inactivates drugs so pills are coated; food delays adsorption of erythromycin and azithromycin |
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Term
| What is the distribution and excretion of macrolides? |
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Definition
| redaily diffuses in all intracellular fluids except CSF; crosses placenta and enters fetal circulation, secreted in breast milk, excreted by kidney and liver (through bile) |
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Term
| What does clarithromycin cover? |
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Definition
| more effective against staph and strep than erythromycin |
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Term
| Which macrolide can be given with food? |
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Definition
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Term
| What is azithromycin used for? |
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Definition
| slightly less effective against G+ but works better than other 2 against Haemophilus influenzae; good against atypical mycobacteria |
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Term
| What are the toxicities of macrolides? |
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Definition
| epigastric distress with large doses; cholestatic hepatitis |
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Term
| Macrolides potentiate teh effects of which drugs? |
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Definition
| carbamazepine, corticosteroids, cyclosporine, digoxin, ergot alkaloids, theophylline, triazolam, valproate, warfarin |
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Term
| How is clindamycin administered? |
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Definition
| orally, parenterally, or topically |
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Term
| T/F Food interferes with the absorption of clindamycin. |
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Definition
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Term
| What is the distribution and excretion of clindamycin? |
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Definition
| wide distribution excluding CSF, crosses placenta; accumulates in PMNs, alveolar macrophages, and pus; excreted by liver and kidneys |
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Term
| What is clindamycin used for? |
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Definition
| anaerobic infections (except brain abscesses), staph infections (including MRSA) |
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Term
| What are the side effects of clindamycin? |
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Definition
| diarrhea, pseudomembraneous colitis, toxic megacolon, skin rash, SJS, anaphylaxis |
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Term
| Streptogramins are derived from... |
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Definition
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Term
| What is the spectrum of the streptogramins? |
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Definition
| gram positive cocci= vancomycin resistant enterococci, MSSA, and strep infections |
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Term
| How are streptogramins administered? |
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Definition
| given IV in 5% dextrose in water |
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Term
| What is the distribution and excretion of the streptogramins? |
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Definition
| wide distribution with mostly hepatic excretion |
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Term
| What is the toxicity of streptogramins? |
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Definition
| infusion related pain and phlebitis; potentiates same drugs as macrolides |
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Term
| What type of molecule is linezolid? |
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Definition
| synthetic agent (an oxazolidinone) |
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Term
| What is the mechanism of action of linezolid? |
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Definition
| prevents assembly of ribosome |
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Term
| T/F Food interferes with the absorption of linezolid. |
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Definition
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Term
| How is linezolid administered? |
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Definition
| oral or IV= 100% absorption |
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Term
| What is the distribution and excretion of linezolid? |
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Definition
| distributed widely and excreted by the kidneys |
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Term
| What organisms does linezolid treat? |
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Definition
| G+ only; no anaerobes, treat VRE, MSSA, MRSA |
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Term
| What are the side effects of linezolid? |
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Definition
| well tolerated; minor GI complaints |
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Term
| What is the structure of vancomycin? |
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Definition
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Term
| What is vancomycin used for? |
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Definition
| G+ coverage only; treatment of MRSA |
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Term
| How is vancomycin administered? |
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Definition
| given IV over an hour or orally for pseudomembranous colitis |
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Term
| What is the distribution and excretion of vancomycin? |
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Definition
| widely distributed, secreted by the kidneys |
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Term
| What is Red-man syndrome? |
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Definition
| a complication occuring from infusing vancomycin too rapidly |
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Term
| What is the MOA of daptomycin? |
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Definition
| a cyclic lipopeptide antibiotic that causes membrane depolarization and cell death |
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Term
| How is daptomycin administered? |
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Definition
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Term
| How is daptomycin excreted? |
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Definition
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Term
| What is the spectrum of daptomycin? |
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Definition
| aerobic G + Cocci infections (except for pneumonias): MRSA, MSSA, VRE |
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Term
| What are the side effects of daptomycin? |
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Definition
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Term
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Definition
| polymyxin B and E (colistin) |
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Term
| what is the MOA of polymyxins? |
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Definition
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Term
| Are polymyxins bacteristatic or bactericidal? |
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Definition
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Term
| What is the spectrum of polymyxins? |
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Definition
| Gram negative coverage but not proteus species |
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Term
| What is polymyxin B used for? |
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Definition
| topical use for skin, eye, and ear infections; little absorbtion |
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Term
| How is polymyxin E administered? |
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Definition
| given IV as a salvage drug |
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Term
| What are teh side effects of polymyxin E? |
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Definition
| nephrotoxic (mild and reversible) |
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Term
| Why is TB difficult to kill with antibiotics? |
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Definition
| slow growth, fortified cell wall, intracellular growth, very good at developing resistance to single agents |
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Term
| What are the first line TB drugs? |
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Definition
| isoniazid, rifampimpin, ethambutol, streptomycin, pyrazinomide |
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Term
| What are the second line drugs for TB? |
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Definition
| Cycloserine, Linezolid, Aminosalicylic acid, Moxi- or gati-floxacin, Ethionamide, Amikacin, kanamycin, capreomycin |
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Term
| What is the structure of isoniazid? |
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Definition
| synthetic hydrazide of isonicotinic acid |
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Term
| What is required for activation of isoniazid? |
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Definition
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Term
| Is isoniazid bacteriostatic or bacteriocidal? |
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Definition
| baceteriocidal for growing cells; static for resting cells |
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Term
| Whta is teh MOA of isoniazid? |
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Definition
| prevents synthesis of mycolic acids |
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Term
| How is isoniazid administered? |
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Definition
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Term
| What is the distribution and excretion of isoniazid? |
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Definition
| acetylated and secreted into urine; rate of secretion has a racial component |
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Term
| What are the toxicities of isoniazid? |
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Definition
| rash and fever, jaundice, peripheral neuritis |
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Term
| Where do the rifamycins come from? |
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Definition
| natural and semi derived frmo filamentous soil bacteria |
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Term
| What is the structure of rifamycins? |
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Definition
| complex macrocyclic antibiotics |
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Term
| Name the different rifamycins? |
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Definition
| rifabutin (for HIV +), rifapentine, rifampin=rifampicin, rifaximin |
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Term
| Are rifamycins bactericidal or bacteristatic? |
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Definition
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Term
| What is the MOA of rifamycins? |
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Definition
| inhibit DNA-dependent RNA polymerase |
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Term
| How do bacteria become resistant to rifamycins? |
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Definition
| resistance generated by altering target |
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Term
| How are rifamycins administered? |
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Definition
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Term
| Name a drug that interacts with rifamycins? |
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Definition
| aspirinwill interfere withthe absorbance of rifamycins |
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Term
| What are the side effects of rifamycins? |
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Definition
| can discolor body waste, saliva, and tears orange red |
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Term
| How are rifamycins distributed and excreted? |
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Definition
| wide distribution, can discolor body waste, saliva, tears orange-red; acetylated and then excreted into bile and ultimately pooped out |
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Term
| What is the use of rifampicin? |
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Definition
| treatment of TB, prophylaxis against meningococcus, staph infections |
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Term
| What is the use of rifabutin and rifapentine? |
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Definition
| TB therapy for HIV+ patients, MAC infections |
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Term
| What is rifaximin used for? |
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Definition
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Term
| What are the toxicities of rifampicin? |
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Definition
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Term
| What are the drug interactions with rifampicin? |
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Definition
| decreases half life of many drugs by inducing CYPs (HIV protease inhibitors and non-nucleoside RT inhibitors, corticosteroids, oral contraceptives) |
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Term
| What are the side effects of rifambutin? |
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Definition
| induces CYPs but not to the same degree as rifampicin, rash, red pee, neutropenia, leukopenia |
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Term
| What is the MOA of ethambutol? |
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Definition
| inhibits arabinosyl transferases involved in cell wall synthesis |
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Term
| How is ethambutol administered and excreted? |
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Definition
| orally; excreted mostly unchanged in the urine |
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Term
| What are the side effects of ethambutol? |
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Definition
| dose dependent diminished visual acuity |
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Term
| What is the structure of pyrazinamide? |
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Definition
| synthetic pyrazine analog of nicotinamide |
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Term
| What is the MOA of pyrazinamide? |
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Definition
| bactericidal at weak pH, where TB can be found in macrophages; inhibits fatty acid synthase I gene |
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Term
| How is pyrazinamide administered? |
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Definition
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Term
| What is the distribution and excretion of pyrazinimide? |
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Definition
| excellent penetration, hydrolyzed and hydroxylated before being excreted by kidneys |
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Term
| What are the side effects of pyrazinamide? |
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Definition
| hepatotoxicity, hyperuricemia=gout |
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