Term
| Penicillium notatum produces the only naturally occuring penicillin which is ________. |
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Definition
| penicillin G or benzylpencillin |
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Term
| What are teh dosage units of pencillin G? |
|
Definition
| IU, where 1 IU = 0.6 micrograms pure penicillin |
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Term
| P. chrysogenum produces what useful product? |
|
Definition
| 6-aminopenicillanic acid, raw material for semisynthetics |
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Term
| What are the dosage units of semisynthetic penicillins derived from 6-aminopenicillanic acid? |
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Definition
| dosage and potency based on weight |
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Term
| What determines the spectrum of activity of a particular penicillin? |
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Definition
| the R group added to the 6 aminopenicillanic acid core |
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|
Term
| Are penicillins bactericidal or bacteristatic? |
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Definition
|
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Term
| What are the mechanisms of resistance against penicillins? |
|
Definition
| alter affinity of transpeptidase, enzymatically cleave the beta-lactam ring, efflux pumps, poor penetration into cell |
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Term
| What is the basic mechanism of all penicillins? |
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Definition
|
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Term
| What body compartments do penicillins not go into? |
|
Definition
| CNS, prostatic fluid, and eye |
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|
Term
| Are penicillins effective against intracellular pathogens? |
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Definition
|
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Term
| What should you tell a patient on oral penicillin about how to take the drug? |
|
Definition
| on an empty stomach because food interferes with adsorption |
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Term
| How are penicillins eliminated from the body? |
|
Definition
| rapidly through the kidney, also secreted in breast milk |
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Term
| What is the spectrum of penicillins G and V? |
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Definition
| effective against aerobic gram positive organisms (ex= Strep pneumo, strep pyogenes, viridans strep endocarditis) except staphylococcus; Pen G active against meningococcus (not gonococcus) and anaerobes (except for bacteroides fragilis), and syphilis and other spirochetes |
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|
Term
| How are penicillins G and V administered? |
|
Definition
| 2/3 or oral pen G destroyed by stomach acid, Pen V is more resistant so more is delivered to serum |
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Term
| What other compounds are often given with penicillin G and V? |
|
Definition
| probenecid, procaine, or benzathine is often added to slow excretion |
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Term
| Describe the characteristic distribution patterns of Penicilin G and V. |
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Definition
| most drug is bound to serum albumin but significant amounts show up in liver, bile, kidney, semen, joint fluid, and lymph, etc. |
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Term
| In what patients should penicillin G and V be used with caution? |
|
Definition
| neonates and infants because renal function is not fully established |
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Term
| What happens if you give penicillin G or V to a patient in renal failure? |
|
Definition
| they clear the drug slower via the liver |
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|
Term
| How do you prevent viridans strep endocarditis? |
|
Definition
| prophylaxis with penicillins G and V |
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|
Term
| Name the Isoxazolyl penicillins? |
|
Definition
| oxacillin, cloxicillin, dicloxacillin, nafcillin |
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|
Term
| Why were isoxazolyl penicillins created? |
|
Definition
| to resist staphylococcal beta lactamases |
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|
Term
| How are isoxazolyl penicillins administered? |
|
Definition
| stable in stomach acid but usually given parentally for serious staph infections |
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|
Term
| T/F Isoxazolyl Penicillins cover MRSA. |
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Definition
|
|
Term
| T/F Abosrption, distribution and excretion of isoxazolyl penicillins mirrors that of Pen G and v. |
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Definition
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Term
| Name teh aminopenicillins. |
|
Definition
| ampicillin and amoxicillin |
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Term
| What is the spectrum of aminopenicillins. |
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Definition
| broad spectrum but not effective against beta-lactamase producers (beta lactamase inhibitors extend spectrum); upper respiratory infections, otitis media, uncomplicated UTI, acute bacterial meningitis in kids, typhoid fever |
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|
Term
| How can you administered aminopenicillins? |
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Definition
| both are acid resistant but amoxicillin is better absorbed, even with food |
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Term
| How are aminopenicillins distrubuted and excreted? |
|
Definition
| don't bind plasma proteins as much as predecessors, secreted through the kidney |
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Term
| What type of antibiotics are ticarcillin and piperacillin? |
|
Definition
| carboxypenicillin and ureidopenicillin |
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|
Term
| Can penicillins be used against pseudomonas? |
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Definition
|
|
Term
| Which penicillin has the broadest spectrum? |
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Definition
|
|
Term
| How should ticarcillin and piperacillin be administered? |
|
Definition
|
|
Term
| What is the use of ticarcillin and piperacillin? |
|
Definition
| broad spectrum, used for serious infections; ticarcillin is anti-pseudomonas |
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|
Term
| What are teh symptoms of hypersensitivity to penicillins? |
|
Definition
| rash, fever, bronchospasms, vasculitis, serum sickness, exfoliative dermatitis, SJS, anaphylaxis |
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Term
| How do you treat a hypersensitivity reaction to penicillin? |
|
Definition
| rahses will disappear when drug is withdrawn or can treat with antihistamines; for patients with allergies, switch to a different class of antibiotics or try to desensitize |
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|
Term
| What are the toxicities of penicillin? |
|
Definition
| hypersensitivity rxn, pain and sterile inflammation at injection site, pseudomonas colitis |
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Term
| What happens if you give penicillin to patients in renal failure? |
|
Definition
| if given in large dosese you can cause lethargy, confusion, twitching, seizures |
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Term
| A sudden release of procaine can cause what symptoms? |
|
Definition
| dizziness, tinnitus, headache, and hallucinations |
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Term
| What is the structure of cephalosporins? |
|
Definition
| base molecule is 7-aminocephalosporanic acid; R groups determine spectrum of activity and pharmacological properties |
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Term
| T/F The mechanism of action/resistance and class pharmacology of cephalosporins is essentially the same as penicillins. |
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Definition
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Term
| Name the first generation cephalosporins. |
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Definition
| cefazolin, cephalexin, cephadroxil |
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Term
| What are the uses of first generation cephalosporins. |
|
Definition
| excellent against suscetible staph and strep (esp skin and soft tissue infections); modest activity against gram negatives |
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Term
| How are first generation cephalosporins administered? |
|
Definition
| cephazolin is given parenterally, cephadroxil and cephalexin enterally |
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Term
| Describe the distribution, metabolism and excretion of cephalosporins. |
|
Definition
| more than half of the drug is bound to plasma proteins, excreted by kidneys unmetabolized |
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Term
| Name the second generation cephalosporins? |
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Definition
| cefaclor, cefuroxime, cefprozil |
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Term
| Which organisms and diseases are second generation cephalosporins used to treat? |
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Definition
| modest activity against G+, increased activity aginst G-, works against anaerobes; respiratory tract infections, intra-abdominal infections, pelvic inflammatory disease, diabetic foot ulcers |
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Term
| How are second generation cephalosporins administered and excreted? |
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Definition
| cefaclor and cefprozil given orally; absorption and excretion same as first generation |
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Term
| Name the third generation cephalosporins? |
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Definition
| ceftaxime, ceftriaxzone, cefoperazone, cefpodoxime |
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|
Term
| What is the spectrum of third generation cephalosporins? |
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Definition
| broad spectrum, drug of choice for serious infections, no effect against listeria and beta-lactamase producing pneumococci; bacterial meningitis, lyme disease, life-threatening G- sepsis |
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|
Term
| Name a fourth generation cephalosporin. |
|
Definition
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|
Term
| What are the uses of fourth generation cephalosporins? |
|
Definition
| same antimicrobial spectrum as third generation but resists more beta-lactamases; good for nosocomial infections |
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|
Term
| How are third generation cephalosporins administered? |
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Definition
| cefpodoxime given orally; cefotaxime, ceftriaxone, and cefoperazone given parentally |
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|
Term
| How are third generation cephalosporins excreted? |
|
Definition
|
|
Term
| How are fourth generation cephalosporins administered? |
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Definition
|
|
Term
| Which fluid compartment do cephalosporins penetrate? |
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Definition
|
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Term
| What are the toxicities/contraindications of cephalosporins? |
|
Definition
| hypersensitivity reactions uncommon, essentially same as for penicillins; 6-10% cross reactivity between the two classes |
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|
Term
| What is the basic structure of carbapenems? |
|
Definition
| beta-lactam ring is fused to a 5 member ring system |
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Term
| Carbapenems' effect on microbes and pharmacology is similar to what other antibiotic? |
|
Definition
|
|
Term
|
Definition
| imipenem, meropenem, ertapenem, doripenem |
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|
Term
| What is the spectrum of imipenem? |
|
Definition
| broad spectrum including anaerobes and psuedomonas aeruginosa |
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|
Term
| How are carbapanems administered? |
|
Definition
| parentally; imipenem must be combined with cilastatin to be absorbed; meropenem, ertapenem and doripenem are similar to imipenem but don't need co-administration with cilastatin |
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|
Term
| How is imipenem excreted? |
|
Definition
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|
Term
| Name the antibiotic that is a monobactam. |
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Definition
|
|
Term
| What is the spectrum of aztreonam? |
|
Definition
| works only on gram negatives, including pseudomonas aeruginosa, useful for treating G- infections that require a beta lactam because it does not elicit hypersensitivity |
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Term
| What are the toxicities/contraindications of carbapenems? |
|
Definition
| nausea and vomiting, hypersensitivity reactions (essentially the same as for penicillins, exception is the monobactam) |
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|
Term
| What is the structure of aminoglycosides? |
|
Definition
| two or more amino sugars attached to a hexose nucleus |
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|
Term
| What is the coverage of aminoglycosides? |
|
Definition
|
|
Term
| What is the MOA of aminoglycosides? |
|
Definition
| bactericidal protein synthesis inhibitor |
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|
Term
| What are the mechanisms of resistance against aminoglycosides? |
|
Definition
| enzymatic modification, impaired uptake, mutation in ribosome |
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|
Term
| How are aminoglycosides administered? |
|
Definition
|
|
Term
| What are important characteristics of distribution of aminoglycosides? |
|
Definition
| poor penetration inside cells, CSF, and eye; accumulation in perilymph and endolymph of inner ear |
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|
Term
| How are aminoglycosides excreted? |
|
Definition
|
|
Term
| What is streptomycin used for? |
|
Definition
| anti-TB drug; useful for bacterial endocarditis +b-lactam, tularemia, plague |
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|
Term
| Name the aminoglycosides. |
|
Definition
| streptomycin, gentamicin, tobramycin, netilmicin, amickacin |
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|
Term
| What is the spectrum against gentamicin? |
|
Definition
|
|
Term
| What is the spectrum against tobramycin? |
|
Definition
|
|
Term
| Which aminoglycosides are good against gentamicin resistant bugs? |
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Definition
|
|
Term
| Aminoglycosides + a beta lactam can be used to treat what kinds of disease? |
|
Definition
| UTI,community acquired pneumonia, meningitis, dialysis associated peritonitis, bacterial endocarditis, sepsis, topical infections (keratitis) |
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|
Term
| What are teh toxicities of aminoglycosides? |
|
Definition
| ototoxic (auditory and vestibular dysfunction), nephrotoxic, rarely= neuromuscular blockade and hypersensitivity |
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|
Term
| Where do tetracyclines come from? |
|
Definition
| natural producs of streptomyces or semisynthetic derivatives |
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|
Term
| What is the use of tetracyclines? |
|
Definition
| anaerobes, intracellular and atypical bacteria |
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|
Term
| Are tetracyclines bacteriastatic or bactericidal? |
|
Definition
|
|
Term
| How does resistance against tetracyclines occur? |
|
Definition
| decreased influx or active efflux, production of protection protein, enzymatic inactivation |
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|
Term
| How are tetracyclines administered? |
|
Definition
| oral or parenteral; absorbance incomplete |
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|
Term
| Describe the distribution of tetracyclines. |
|
Definition
| wide distribution in tissues and fluids; including CSF |
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|
Term
| Can tetracyclines cross the placenta? |
|
Definition
|
|
Term
| Where are tetracyclines excreted? |
|
Definition
| most excreted by the kidneys, others are concentrated into bile and excreted into feces; also can be excreted in breast milk |
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|
Term
| Are tetracyclines well absorbed from the intestines? |
|
Definition
| tetracycline, oxytetracycline and democycline are incompletely absorbed(60-80%), minocycline and doxycycline are completely absorbed (95-100%) |
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|
Term
| How are tetracyclines secreted? |
|
Definition
| tetracycline, oxytetracycline, democycline are primarily excreted through the kidneys; minocycline and doxycycline are excreted through the liver |
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|
Term
|
Definition
| tetracycline, oxytetracycline, democycline, minocycline, doxycycline |
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|
Term
| What is the structure of tigecycline? |
|
Definition
| a glycylcyline antibiotic derived from minocycline |
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|
Term
| What is the use of tigecycline? |
|
Definition
| broad spectrum (G+= G-; not P aeruginosa or proteus); complicated intraabdominal infections or soft tissue infections |
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|
Term
| What are hte toxicities/side effects of tigecycline? |
|
Definition
|
|
Term
| What are the therapeutic uses of tetracyclines? |
|
Definition
| rickettsial infections, mycoplasma infections, chlamydia infections (intracellular!); bacillary infections (anthrax, brucellosis, tularemia, choelra), and spirochete infections (syphilis, yaws, lyme disease, relapsing fever) |
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|
Term
| What antibiotic can be used to treat rosacea? |
|
Definition
| doxycycline d/t antiinflammatory activity |
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|
Term
| What are the toxicities of tetracyclines? |
|
Definition
| gastrointestinal (nausea, vomiting, etc. helped with food), photosensitivity, hepatic toxicity with large doses (worse when pregnant), renal toxicity (fanconi syndrome), deposits in tooth dentine and enamel forming brown bands; thrombophlebitis, various WBC dystrophies, increased intracranial pressure in neonates, hypersensitivity rxns |
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|
Term
| In which patients are tetracyclines contraindicated? |
|
Definition
| children or women who are pregnant or nursing |
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