Shared Flashcard Set

Details

Overview of Antibacterial Agents, pp 6-11
Pharm Module I
147
Medical
Graduate
05/31/2009

Additional Medical Flashcards

 


 

Cards

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
Daptomycin (cubicin)
Term
How is Daptomycin administered?
Definition
only available IV
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
vancomycin
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
tid/qid
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
Azithromycin (Zithromax)
Term
How is Azithromycin (Zithromax) administered?
Definition
given both IV and orally
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
minimal adverse rxns
Term
What are the drug interactions of Azithromycin (Zithromax)?
Definition
No drug interactions
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
telithromycin
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
Telithromycin (Ketek)
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
doxycycline
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
very expensive
Term
What is a new tetracycline that was derived from minocycline and approved in 2005?
Definition
Tigecycline (Tygacil)
Term
How is tigecycline (tygacil) administered?
Definition
IV drug (not oral)
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
proteus, pseudomonas spp
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
bactericidal
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
short T1/2 of 2-3 hrs
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
bacteriostatic activity
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
only given IV
Term
How frequently must quinupristin/dalfopristin be administered?
Definition
every 8-12 hrs
Term
How is quinupristin/dalfopristin metabolized?
Definition
liver
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
bacteriostatic activity
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
liver
Term
What is the T1/2 of linezolid?
Definition
T1/2 of 4-6 hrs
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
ciprofloxacin (cipro)
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
norfloxacin
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
levofloxacin (levaquin)
Term
What is the most common fluoroquinolone used for a variety of serious infections?
Definition
levofloxacin (levaquin)
Term
What is T1/2 of levofloxacin (levaquin)?
Definition
T1/2 = 7 hrs
Term
How is levofloxacin (levaquin) eliminated?
Definition
renal elimination
Term
How frequently is Levofloxacin (Levaquin) administered?

What is the method of administration?
Definition
qd IV or oral
Term
Should Moxifloxacin (Avelox) be used for UTIs?
Definition
*NO*
Term
Which has better activity against anaerobic bacteria: levofloxacin (levaquin) or moxifloxacin (avelox)?
Definition
moxifloxacin (avelox)
Term
How frequently and by what route is moxifloxacin (avelox) administered?
Definition
qd iv or po
Term
What is the newest fluoroquinolone?
Definition
gemifloxacin (factive)
Term
How is gemifloxacin (factive) administered?
Definition
only available po
Term
How is gemifloxacin (factive) metabolized?
Definition
liver
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
bactericidal
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
po and iv
Term
How is TMP-SMX distributed?
Definition
well distributed in tissues including CSF
Term
How is TMP-SMX excreted?
Definition
50% excreted through kidneys
Term
What is T1/2 of TMP-SMX and how frequently is it administered?
Definition
T1/2 - 12 hrs, bid
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
bactericidal
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
available po and iv
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
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