Term
When are carbapenems indicated? |
|
Definition
-serious polymicrobial and nosocomial infections due to highly resistant bacteria
-imipinem and meropenem (but not ertapenem) also have activity against pseudomonas |
|
|
Term
What are 4 down sides of carbapenems? |
|
Definition
-can be neurotoxic at higher doses (seizures)
-greater chance of superinfections
-high cost
-cross sensitivity in penillin-allergic pts |
|
|
Term
Which of the following is bacitracin active against:
gram + bacteria
gram - bacteria
anaerobic bacteria |
|
Definition
active against gram + bacteria only |
|
|
Term
What is a side affect if bacitracin is given systemically? |
|
Definition
highly nephrotoxic if given systemically |
|
|
Term
How is bacitracin administered? |
|
Definition
used in topical preparations
one of the ingredients in triple antibiotic ointment (also includes neomycin and polymyxin)
highly nephrotoxic if given systemically
poorly absorbed if given orally |
|
|
Term
When is bacitracin administered? |
|
Definition
only used in topical preparations to tx skin infections due to strep and staph |
|
|
Term
What medication is a unique cyclic lipopeptide active against g+ bacteria? |
|
Definition
|
|
Term
How is Daptomycin administered? |
|
Definition
|
|
Term
When is daptomycin indicated? |
|
Definition
old drug making comeback for tx vancomycin-resistant bacteria |
|
|
Term
What is the method of action of the following medications: -bacitracin -daptomycin (cubicin) -vancomycin |
|
Definition
inhibitors of cell wall synthesis |
|
|
Term
What medication is a glycopeptide with a high molecular weight? |
|
Definition
|
|
Term
What is the method of action of vancomycin? |
|
Definition
inhibits cell wall synthesis by blocking elongation of peptoglycan molecule |
|
|
Term
Which of the following are susceptible to vancomycin: gram+ gram- |
|
Definition
-bactericidal against most gram+ including those resistant to β-lactam Abiotics
-no activity against gram- bacteria |
|
|
Term
Is vancomycin bactericidal or bacteriostatic? |
|
Definition
bactericidal against most g+ bacteria including those resistant to β-lactam Abiotics |
|
|
Term
What bacteria are resistant to vancomycin and what concern involves this resistance? |
|
Definition
some enterococci have become resistant and are known as vancomycin-resistant enterococci or VRE
-Big worry that this mutant gene will be transferred to staph |
|
|
Term
How is vancomycin usually administered? |
|
Definition
-usually given IV
-not absorbed orally
-oral vancomycin remains in GI tract and only used to tx C. dif colitis |
|
|
Term
***How is vancomycin eliminated? |
|
Definition
-eliminated by kidney in direct proportion to creatinine clearance |
|
|
Term
Why must peak and trough levels be monitored in vancomycin tx? |
|
Definition
narrow TI- must monitor peak and trough levels |
|
|
Term
***What are 2 important adverse rxns associated w/vancomycin? |
|
Definition
1. Red man syndrome: infusion rxn due to massive histamine release if given too fast or in too high a dose (tx w/antihistamines) 2. Ototoxicity at higher doses |
|
|
Term
How do the following classes of drugs act against bacteria? -macrolides -ketolides -tetracyclines -aminoglycosides -misc: -clindamycin -quinupristin-dalfopristin -linezolid -mupirocin |
|
Definition
inhibitors of bacterial protein synthesis |
|
|
Term
***When is vancomycin indicated? |
|
Definition
-reserved for known or suspected infections due to MRSA
-also used in combination w/aminoglycoside for enterococcus infections
-oral vancomycin only used to tx pseudomembranous colitis secondary to C.dif (colitis caused by bacterial toxin) |
|
|
Term
What are 3 macrolides and how do they act against bacteria? |
|
Definition
-erythromycin -clarithromycin -azithromycin
inhibitor of bacterial protein synthesis |
|
|
Term
What is a ketolide and how does it act against bacteria? |
|
Definition
telithromycin (ketek): inhibitor of bacterial protein synthesis |
|
|
Term
What are some tetracycline medications and how do they act against bacteria? |
|
Definition
-tetracycline -doxycycline [also minocycline and tigecycline (tygacil)]
inhibitors of protein synthesis |
|
|
Term
What are 5 aminoglycosides and how do they act against bacteria? |
|
Definition
-gentamycin -tobramycin -amikacin -streptomycin -neomycin
inhibitors of bacterial protein synthesis |
|
|
Term
***What are 4 misc inhibitors of bacterial protein synthesis? |
|
Definition
-clindamycin -quinupristin-dalfopristin -linezolid -mupirocin |
|
|
Term
What is the method of action of macrolide antibiotics? |
|
Definition
reversibly bind to 50s ribosomal subunit |
|
|
Term
Do macrolide antibiotics act via bacteriostatic or bactericidal mechanisms? |
|
Definition
usually bacteriostatic effect |
|
|
Term
***When are macrolide Abiotics indicated? |
|
Definition
1. Strep and staph
-resistance gradually increasing
2. some activity against h. influenzae and bordetella
3. Activity against atypical bacteria (mycoplasm, legionella, chlamydophyla) that cause atypcial pneumonia
4. for upper and lower respiratory infections potentially due to atypical bacteria
-azithromycin used extensively in hospitals for pneumonia
5. for penicillin-allergic pts
6. For Chalmydia trachomatis STD infections
7. Clarithromycin for Mycobacterium Avian Complex (MAC) |
|
|
Term
How is erythromycin administered? |
|
Definition
-IV form rarely used anymore
-orally available as base, stearate, estolate, and ethylsuccinated salts |
|
|
Term
How frequently must erythromycin be administered? |
|
Definition
|
|
Term
***What are some adverse effects of erythromycin? |
|
Definition
-oral form has dose-dependent effect on intestinal peristalsis causing ab pain and diarrhea
-high doses can cause ototoxicity |
|
|
Term
What are some drug interactions involved with erythromycin and clarithromycin? |
|
Definition
clarithromycin has the same drug interactions as erythromycin!
1. inhibits CYP 450 3A4 enzyme reponsible for metabolizing 50% of drugs
2. will increase serum levels of
statins,
bezodiazepines,
Ca2+ channel blockers,
cyclosporine, and many more |
|
|
Term
Which is absorbed better: Clarithromycin (biaxin) or erythromycin? |
|
Definition
Clarithromycin (biaxin)- now generic
-very similar to erythromycin but better absorbed
-higher serum levels and lower GI levels
-less GI adverse effects |
|
|
Term
How is clarithromycin administered, and how frequently is it administered? |
|
Definition
not available as IV
can be given bid |
|
|
Term
What is the most popular and the safest macrolide Abiotic? |
|
Definition
|
|
Term
How is Azithromycin (Zithromax) administered? |
|
Definition
|
|
Term
What is the T1/2 of Azithromycin (Zithromax)?
How frequently is it administered?
For how long must it be administered? |
|
Definition
has T1/2 of 60 hrs,
requires loading dose and once daily dosing (Z-pack)
only have to give for 3 to 5 days |
|
|
Term
What are the adverse reactions of Azithromycin? |
|
Definition
|
|
Term
What are the drug interactions of Azithromycin (Zithromax)? |
|
Definition
|
|
Term
What non-macrolide Abiotic is very similar in structure and function to erythromycin? |
|
Definition
Telithromycin (Ketek), a Ketolide Abiotic |
|
|
Term
Which has a higher affinity for the 50s ribosomal subunit: erythromycin or telithromycin? |
|
Definition
|
|
Term
***Describe the activity of Telithromycin (Ketek). |
|
Definition
Same activity as macrolides but has activity against penicillin and macrolide-resistant Strep pneumonia |
|
|
Term
***Describe the adverse rxns and drug interactions of Telithromycin (Ketek). |
|
Definition
same adverse rxns and drug interactions as erythromycin:
-oral form has dose-dependent effect on intestinal peristalsis causing ab pain and diarrhea
-higher doses cause otoxicity
-inhibits CYP 450 3A4 enzyme responsible for metabolizing 50% of drugs
-will increase serum levels of statins, benzodiazepines, Ca2+ channel blockers, cyclosporines, and many more
ALSO, recent concern regarding cases of hepatotoxicity and whether safety studies were properly performed |
|
|
Term
What drug was involved in fabrication of study results by Dr. Maria "Anne" Kirkman Campbell? |
|
Definition
|
|
Term
What is the method of action of tetracyclines? |
|
Definition
reversibly bind to the 30s ribosomal subunit of bacteria |
|
|
Term
Do tetracyclines act via a bactericidal or bacteriostatic mechanism? |
|
Definition
usually bacteriostatic effect |
|
|
Term
When are tetracyclines indicated? |
|
Definition
-active against rickettsiae, chlamydiae, mycoplasma, and some protozoa
-lyme disease (tick-borne) -erichiosis (tick-borne) -rocky mt spotted fever (tick-borne) -atypical pneumonia -pid -tetracycline and monocycline for acne |
|
|
Term
***What are 4 important adverse rxns of tetracyclines? |
|
Definition
-GI irritation
-Photosensitivity rxns
-Discoloration of tooth enamel in children and fetus -Hepatotoxicity possible w/extended use |
|
|
Term
What is an important drug interaction with tetracyclines? |
|
Definition
-cations such as ca2+ will bind to tetracyclines and prevent absorption
-avoid giving dairy products or antacids |
|
|
Term
***Which drug from the tetracycline class is rarely used now and why is this? |
|
Definition
tetracyline is rarely used now b/c of lower bioavailability and short T1/2- have to give qid |
|
|
Term
Which medication is the most popular tetracycline? |
|
Definition
|
|
Term
How is doxycycline administered? |
|
Definition
give both IV and oral (good bioequivalence) |
|
|
Term
***What is the T1/2 of doxycycline? How frequently must it be administered? |
|
Definition
long T1/2 and can be given qd or bid depending on infection |
|
|
Term
Minocycline is popular for what disease? |
|
Definition
popular for acne due to high distribution to skin |
|
|
Term
How expensive is minocycline? |
|
Definition
|
|
Term
What is a new tetracycline that was derived from minocycline and approved in 2005? |
|
Definition
|
|
Term
How is tigecycline (tygacil) administered? |
|
Definition
|
|
Term
What drug is not affected by the 2 major mechanisms of tetracycline resistance?
Is this medication bactericidal or bacteriostatic? |
|
Definition
Tigecycline (Tygacil)
- but still only bacteriostatic activity |
|
|
Term
Is Tigecycline (Tygacil) active against g+, g- or anaerobic bacteria? |
|
Definition
Active against g+ including MRSA, g-, and anaerobic bacteria |
|
|
Term
Tigecycline (Tygacil) is inactive against what 2 bacterial spp? |
|
Definition
|
|
Term
***When is Tigecycline (Tygacil) indicated? |
|
Definition
g+ (including MRSA), g-, anaerobic
not active against pseudomonas or proteus spp
reserve for Abiotic-resistant infections |
|
|
Term
What is the MOA of Aminoglycoside Abiotics? |
|
Definition
bind irreversibly to 30s ribosomal subunit of bacteria |
|
|
Term
Do Aminoglycoside Abiotics act via bactericidal or bacteriostatic mechanisms? |
|
Definition
|
|
Term
***When are Aminoglycoside Abiotics indicated?
|
|
Definition
g-, including pseudomonas
strep are resistant to agents when used alone
synergistic activity when combined w/β-lactam Abiotics
bacteremia, pneumonia, intra-ab infections, and other serious infections due to g- bacteria |
|
|
Term
How are aminoglycoside Abiotics administered? |
|
Definition
only available for IV or IM use- unable to be absorbed orally |
|
|
Term
What is the T1/2 of Aminoglycoside Abiotics? |
|
Definition
|
|
Term
How frequently are aminoglycoside Abiotics administered? |
|
Definition
give high dose qd due to concentration-dependent effect on bacterial killing
monitor peak and trough levels due to narrow therapeutic index |
|
|
Term
How are aminoglycoside Abiotics eliminated? |
|
Definition
eliminated renally and accumulate in renal failure
monitor peak and trough levels due to narrow TI |
|
|
Term
Does clindamycin act via bactericidal or bacteriostatic mechanisms? |
|
Definition
|
|
Term
What are 2 drugs with a narrow TI? |
|
Definition
Vancomycin, Aminoglycoside Abiotics |
|
|
Term
***What are some adverse rxns of Aminoglycoside Abiotics? |
|
Definition
very nephrotoxic- can accumulate in renal tubules and cause acute renal failure
also ototoxic at high doses for extended periods of time
|
|
|
Term
What are the 3 most common aminoglycoside Abiotics? |
|
Definition
gentamicin
tobramcin
amikacin |
|
|
Term
When is tobramycin indicated? |
|
Definition
most active fro Pseudomoas aeruginosa
also available as inhaled form for cystic fibrosis pts w/pseudomonas pneumonia |
|
|
Term
How is neomycin administered? |
|
Definition
most toxic and never administered IV
used in topical formulas in combination w/other Abiotics
oral form sometimes used for prophylaxis before elective bowel surgery |
|
|
Term
What was the first aminoglycoside?
When is it indicated?
How is it administered? |
|
Definition
Streptomycin used IV or IM as 2nd line therapy for active TB |
|
|
Term
What is the MOA of clindamycin (cleocin)? |
|
Definition
binds to the same 50s ribosomal subunit as macrolide Abiotics |
|
|
Term
When is clindamycin indicated? |
|
Definition
inhibits strep, staph, pneumococci; inhibits anaerobic bacteria such as bacteroides fragilis and clostridium perfringies; anaerobic infections such as intra-ab wounds, gyn infections, abscesses, and aspiration pneumonia; for g+ infections in penicillin-allergic pts; for newly discovered community-aquired MRSA |
|
|
Term
***What are some important adverse rxns associated w/clindamycin (cleocin)? |
|
Definition
GI upset such as nausea and diarrhea *primary antibiotic to cause antibiotic-associated PMC* |
|
|
Term
How is clindamycin (cleocin) administered, and how is it metabolized? |
|
Definition
can be given iv or po
metabolized by liver |
|
|
Term
What is the MOA of quinupristin/dalfopristin? |
|
Definition
unique streptogramin molicules that act *synergistically* to inhibit bact prot synthesis at 50s ribosomal subunit |
|
|
Term
When are quinupristin/dalfopristin indicated? Do they act via a bactericidal or bacteriostatic mechanism? |
|
Definition
bactericidal against strep and staph; bacteriostatic againsts enterococcus faecium; reserved for use in serious infections caused by multidrug-resistant strep, MRSA and VRE |
|
|
Term
How are quinupristin/dalfopristin administered? |
|
Definition
|
|
Term
How frequently must quinupristin/dalfopristin be administered? |
|
Definition
|
|
Term
How is quinupristin/dalfopristin metabolized? |
|
Definition
|
|
Term
***What are important adverse rxns to quinupristin/dalfopristin? |
|
Definition
infusion-related pain and myalgias |
|
|
Term
What are some important drug interactions with quinupristin/dalfopristin? |
|
Definition
like erythromycin, inhibits CYP 450 3A4 enzyme that metabolizes many drugs |
|
|
Term
What is the MOA of linezolid (zyvox)? |
|
Definition
oxazolidinedione with unique activity against bacterial 50s subunit of bacteria. |
|
|
Term
Does linezolid (Zyvox) act via bactericidal or bacteriostatic mechanisms? |
|
Definition
|
|
Term
When is linezolid indicated? |
|
Definition
active against maost g+, including most strains resistant to other abiotics.
resistance may occur w/overuse.
should be reserved for infections caused by multidrug-resistant bacteria such as VRE and MRSA. |
|
|
Term
How is linezolid (Zyvox) administered? |
|
Definition
given oral or IV with 100% bioavailability |
|
|
Term
How is linezolid (Zyvox) metabolized? |
|
Definition
|
|
Term
What is the T1/2 of linezolid? |
|
Definition
|
|
Term
What is an important adverse rxn of linezolid (Zyvox)? |
|
Definition
*hematologic toxicity* can cause thrombocytopenia and neutropenia w/extended use |
|
|
Term
What is the cost of linezolid? |
|
Definition
$1000 for 1 week oral therapy |
|
|
Term
How is mupirocin (bactroban) related to other Abiotics? |
|
Definition
unrelated to other Abiotics |
|
|
Term
***How is mupirocin (bactroban) administered? |
|
Definition
only used in *topical* preparations for tx *staph* infections. special *nasal formula* available to eliminate carriage of MRSA |
|
|
Term
When is mupirocin (bactroban) indicated? |
|
Definition
should be reserved for suspected or definite MRSA to avoid development of resistance.
also used for impetigo caused by strep or staph. |
|
|
Term
What class do the following antibiotics fall under? norfloxacin ciprofloxacin ofloxacin lomefloxacin enoxacin |
|
Definition
1st gen DNA gyrase inhibitors- fluoroquinolone Abiotics |
|
|
Term
Which class do the following medications fall under? levofloxacin (levauin) moxifloxacin (avelox) gemifloxacin (factive) |
|
Definition
2nd generation DNA gyrase inhibitors- fluoroquinolone abiotics |
|
|
Term
What category does trovofloxacin (trovan) fall under? |
|
Definition
restricted bacterial dna gyrase inhibitor- fluoroquinolone abiotics |
|
|
Term
What category do the following medications fall under? gatifloxacin (tequin) sparfloxacin (zagam) grepafloxacin (raxar) |
|
Definition
withdrawn dna gyrase inhibitors- fluoroquinolone abiotics |
|
|
Term
What is the MOA for bacterial dna gyrase inhibitors- fluoroquinolone abiotics? |
|
Definition
inhibit dna gyrase and topoisomerase that are essential for maintaing bacterial dna structure and function |
|
|
Term
Do fluoroquinolone abiotics act via bactericidal or bacteriostatic mechanisms? |
|
Definition
bactericidal activity against most g- bacteria |
|
|
Term
When are fluoroquinolone abiotics indicated? |
|
Definition
g- active against atypical bacteria;
2nd gen agents also have good activity against g+ bacteria (except staph) complicated UTI and prostatitis;
serious infections secondary to g- bacteria such as bacteriemia and intra-ab infections;
2nd gen agents used for severe pneumonia;
infectious diarrhea secondary to salmonella and shigella;
penicillin-resistant to anthrax |
|
|
Term
How are fluoroquinolone abiotics administered? |
|
Definition
most available as both IV and oral forms |
|
|
Term
How do fluoroquinolones distribute and how are they excreted? |
|
Definition
distribute well into most tissues; excreted renally |
|
|
Term
What are some important adverse rxns of fluoroquinolones? |
|
Definition
cause arthropathy in developing animals- avoid in children less than 18 years old and during pregnancy.
achilles tendon rupture.
neurotoxic in high doses (irritability seizures). |
|
|
Term
***What are some important drug rxns with fluoroquinolones? |
|
Definition
absorption of oral dosage forms inhibited by cations such as ca2+, mg2+, Fe, and Zn (multivitamins and anacids). inhibit metabolism of caffeine and theophylline. |
|
|
Term
What is the most commonly used 1st gen fluoroquinolone abiotic? |
|
Definition
|
|
Term
What is Ciprofloxacin (Cipro)'s advantage? |
|
Definition
only quinolone with activity against Pseudomonas aeruginosa |
|
|
Term
***What are the disadvantages of ciprofloxacin (cipro)? |
|
Definition
-poor activity against g+ -shorter T1/2 requires bid dosing IV or oral |
|
|
Term
What was the 1st fluoroquinolone? |
|
Definition
|
|
Term
When is norfloxacin indicated? |
|
Definition
still used for UTI's- does not achieve high enough serum levels for systemic infections. |
|
|
Term
What are also known as "respiratory fluoroquinolones"? |
|
Definition
2nd gen fluoroquinolone abiotics |
|
|
Term
***Against what bacteria are 2nd gen fluroquinolones active? |
|
Definition
besides g- activity, they are active against most bacteria responsible for respiratory infections including atypical bacteria and multidrug-resistant strep pneumonia |
|
|
Term
What drug ist he L-isomer of ofloxacin? |
|
Definition
|
|
Term
What is the most common fluoroquinolone used for a variety of serious infections? |
|
Definition
|
|
Term
What is T1/2 of levofloxacin (levaquin)? |
|
Definition
|
|
Term
How is levofloxacin (levaquin) eliminated? |
|
Definition
|
|
Term
How frequently is Levofloxacin (Levaquin) administered?
What is the method of administration? |
|
Definition
|
|
Term
Should Moxifloxacin (Avelox) be used for UTIs? |
|
Definition
|
|
Term
Which has better activity against anaerobic bacteria: levofloxacin (levaquin) or moxifloxacin (avelox)? |
|
Definition
|
|
Term
How frequently and by what route is moxifloxacin (avelox) administered? |
|
Definition
|
|
Term
What is the newest fluoroquinolone? |
|
Definition
|
|
Term
How is gemifloxacin (factive) administered? |
|
Definition
|
|
Term
How is gemifloxacin (factive) metabolized? |
|
Definition
|
|
Term
What is an adverse rxn of gemifloxacin (factive)? |
|
Definition
greater incidence of rash (32% v. 4% w/cipro in women <40yo) |
|
|
Term
What is the only oral sulfonamide still used as an abiotic and how is it available? |
|
Definition
SMX is the only oral sulfonamide still used as an antibacterial agent and is only available in combination w/TMP |
|
|
Term
What is the MOA of TMP-SMX? |
|
Definition
sequential inhibition of bacterial folic A synthesis preventing DNA synthesis (human cells do not synthesize this A) |
|
|
Term
***What bacteria are susceptible to TMP-SMX? |
|
Definition
bactericidal activity against most g+ and g- including CA-MRSA. Active against nocardia, pneumoncystis jiroveci. |
|
|
Term
Does TMP-SMX act via bactericidal or bacteristatic mechanisms? |
|
Definition
|
|
Term
***Against what does TMP-SMX have no activity? |
|
Definition
no activity against enterococci, atypical bacteria, anaerobic bacteria, or P. aeruginosa |
|
|
Term
***When is TMP-SMX indicated? |
|
Definition
primary drug for UTIs. secondary drug for upper and lower respiratory tract infections, sepsis, meningitis, travelers diarrhea, typhoid, cholera |
|
|
Term
How is TMP-SMX administered? |
|
Definition
|
|
Term
How is TMP-SMX distributed? |
|
Definition
well distributed in tissues including CSF |
|
|
Term
|
Definition
50% excreted through kidneys |
|
|
Term
What is T1/2 of TMP-SMX and how frequently is it administered? |
|
Definition
|
|
Term
***What are some important adverse rxns to TMP-SMX? |
|
Definition
hsn- can use TMP alone for UTI's. severe hsn include exfoliative dermatitis and stevens-johnson syndrome. high doses for p jiroveci infections in AIDS: can cause thrombocytopenia and neutropenia, high incidence of allergic rxns, and hyperkalemia. |
|
|
Term
***What are some important drug interactions with TMP-SMX? |
|
Definition
can increase serum levels and toxicity of warfarin, phenytoin, and oral sulfonylureas (for diabetes) |
|
|
Term
***When is Nitrofurantoin (macrodantin) indicated? |
|
Definition
only used for lower UTIs. bactericidal against e.coli, enterococcus, and other common UTI orgs. |
|
|
Term
Does nitrofurantoin (macrodantin) act via bactericidal or bacteriostatic mechanisms? |
|
Definition
|
|
Term
What are some side effects of Nitrofurantoin (macrodantin)? |
|
Definition
commonly causes GI irritation, nausea, and vomiting
should avoid in elderly due to increased risk of pneumonitis and neuropathy
contraindicated in renal failure |
|
|
Term
***When is nitrofurantoin (macrodantin) contraindicated? |
|
Definition
should avoid in elderly due to increased risk of pneumonitis and neuropathy. contraindicated in renal failure. |
|
|
Term
How is Metronidazole (flagyl) administered? |
|
Definition
|
|
Term
***When is metronidazole (flagyl) indicated? |
|
Definition
antiprotozoal drug. best single agent to tx anaerobic infections, including intra-ab infections and c. dif colitis |
|
|
Term
What is a drug interaction with Metronidazole (flagyl)? |
|
Definition
avoid EtOH- while taking: disulfiram-like effect |
|
|