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74 Cards in this Set

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antimicrobial classes

from:
- applied therapeutics 8th edition
- efactsonline (feb 2009) plus
- APhA manual 5th ed
cephalosporins - (four generations)
carbacephems - 1 drug
monobactams - 1 drug
penems - 3 drugs
aminoglycosides - 6 drugs
quinolones - 8 ish drugs

folate inhibitors - a few drugs
- sulfas - 2 ish
- trimethoprim (Trimpex)

those that are in a class by themselves:
- daptomycin (Cidecin)
- vancomycin (Vanocin)
- metronidazole (Flagyl)
antimicrobial classes

protein synthesis inhibitors
protein systhesis inhibitors
- macrolides - 3 drugs
- tetracyclines - 4 drugs
- ketolides - 1 drug
- miscellaneous - 4 drugs
- linezolid (Zyvox)
- dalfopristin/quinuprostin (Synercid)
- clindamycin (Cleocin)
- chloramphenicol (Chloromycetin)
antimicrobial classes

penicillins
penicillins
- natural - 2
- aminopenicillins - 3
- penicillinase resistant penicillins - 5
- carboxypenicillins - 2
- ureidopenicillins - 3
- combos with beta lactams - 4
aminoglycosides

players and dosage forms
amikacin (Amikin) IV, IM
gentamicin (Garamycin) IV, IM
kanamycin IV, PO
neomycin (Mycifradin) PO
netlimicin (Netromycin) IV, IM
streptomycin IM
tobramycin (Nebcin) IV, IM
aminoglycosides

adverse drug events
nephrotoxicity (reversible)
- inc BUN and Scr
- 10-25% of pts
- risk factors
- renal dysf(n)
- prolonged duration of tx
- elevated trough concentrations
- amikacin > 8 mcg/ml
- genta and tobra > 2 mcg/ml

ototoxicity (auditory and vestibular sx)
- tinnitus, loss of high frequency

neuromuscular blockade (uncommon)
aminoglycosides

target serum concentrations
- peaks and troughs

amikacin, gentamicin and tobramicin
amikacin
- peak 15-30 mcg/ml
- trough <= 5mcg/ml

gentamicin and tobramycin
- peak 4-10 mcg/ml
- trought <= 2 mcg/ml
aminoglycosides

clinical pearls
- broadest spectrum
- which 2 used for bowel prep and why
- least ototoxic
- how to use streptomycin
broadest = amikacin

bowel prep to dec bugs in GI
- kanamycin and neomycin PO becuase
not absorbed from GI

least ototoxic = netilmicin

streptomycin (IM only) = adjunct only b/c many bacterial isolates resistant to it when used as monotherapy
aminoglycosides

how are all aminoglycosides elimated
renally
aminoglycosides

spectrum
aerobes
- most gram -
- select gram +

anaerobes
- not effective against most
Beta Lactams
`
β-lactams

broad class that includes the following subclasses
- penicillin derivatives
- cephalosporins
- monobactams
- carbapenems
- β-lactamase inhibitors
β-lactam antibiotics

spectrum/history
at first - mainly only gram +

now - some broad spectrum β-lactam abx with gram - coverage

most widely used class of abx
β-lactam antibiotics

mode of resistance
all have a β-lactam ring

2 modes of resistance
- the bacteria produce enzymes to
hydrolyze the β-lactam ring
- β-lactamase
- penicillinase
- altered Penicillin Binding Proteins
(PBPs) that β-lactams cannot bind
- eg MRSA
common β-lactam antibiotics

classes
Penicillins
- narrow to broad

Cephalosporins
- moderate to broad

Carbapenems
- broadest of the β-lactams

Monobactams
- narrow (gram + aerobes only)

β-lactamase Itrs (not an ABtic)
- have β-lactam ring that
occupies β-lactamase
Penicillins
narrow-spectrum
- β-lactamase sensitive
- Pen V, G
- penicillinase-resistant
- CONDOM drugs
moderate-spectrum
- ampicillin, amoxicillin,
broad-spectrum
- amoxicillin + clanulanic acid
extended-spectrum
- azlocillin
- carbenicillin
- ticarcillin
- mizlocillin
- piperacillin
Penicillins - narrow spectrum

β-lactamase sensitive
penicillin V (Pen-Vee K, Veetids) PO

penicillin G (Pfizerpen) IV, IM, PO

penicillin G procaine (Wycillin) IM

penicillin G benzathine (Bicillin LA) IM
Penicillins - narrow spectrum

penicillinase-resistant

CONDOM drugs
Cloxacillin (Cloxapen) PO

Oxacillin (Prostaphilin, Bactocill)
- PO,IV, IM
- hepatic elimination

Nafcilin (Nafcil, Unipen)
- IV, IM
- hepatic elimination

Dicloxacillin (Dynapen, Dycill) PO

Methicillin (Staphcillin) IV, IM
Penicillins

- moderate spectrum

- broad spectrum
Moderate
- ampicillin (Omnipen, Principen)
PO,IM,IV

- amoxicillin (Amoxil, Trimox) PO

Broad
- amoxicillin+clanulanic acid
(Augmentin) PO
Penicillins

- extended spectrum
azlocillin (Azlin) IM, IV

carbenicillin (Geopen) IM, IV

ticarcillin (Ticar) IM, IV

mezlocillin (Mezlin) IM, IV

piperacillin (Pipracil) IM, IV
penicillins

adverse effects - good enough!
allergic/hypersensitivity
- rash 4-8%
- urticaria (hives)
- anaphylaxis (0.01 - 0.05%)
- occurs in 10-20 minutes; IV>PO

GI: N/V with PO use
what are the only 2 penicillins that are NOT eliminated renally

how are they eliminated?
oxacillin
nafcillin

hepatically
penicillin cross reactivity with other β-lactams
It has previously been accepted that there was up to a 10% cross-sensitivity between penicillin-derivatives, cephalosporins, and carbapenems, due to the sharing of the β-lactam ring

However recent assessments have shown no increased risk for cross- allergy for 2nd generation or later cephalosporins
β-lactamase inhibitors
aren't necessarily antimicrobials

administered with a β lactam

have the β-lactam ring and occupy β-lactamase so it can't find the actual β-lactam antimicrobial

clavulanic acid
tazobactam
sulbactam
β lactam/β lactam inhibitor combos
amoxicillin-clavulanic acid (Augmentin)
- PO

ampicillin-sulbactam (Unasyn)
- IV, IM

piperacillin-tazobactam (Zosyn)
- IV

ticarcillin-clavulanic acid (Timentin)
- IV
Cephalosporins - first generation

players and dosage forms
cefadroxil (Duricef, Ultracef) PO

cefazolin (Ancef, Kefzol) IV

cephalexin (Keflex) PO

cephapirin (Cefadyl) IV, IM

cephradine (Anspor, Velosef) PO, IV
Cephalosporins - spectrum
First-generation
- predominantly active against Gram +

successive generations
- have increased activity against Gram -
bacteria (albeit often with reduced
activity against Gram-positive
organisms)Fourth-generation cephalosporins, however, have true broad spectrum activity.

Fourth-generation cephalosporins have true broad spectrum activity
Cephalosporins - a/e
β-lactam...

plus some have a disulfiram-like reaction
- Antabuse
Cephalosporins - monitoring
serum concentrations not necessary

monitory for response
what is the only cephalosporine that is NOT renally eliminated
cefoperazone (Cefobid) IV

hepatic
cephalosporins

second generation
cefaclor - Ceclor PO
cefmatazole -Zefazone IV
cefonicid - Monocid IV
cefotetan - Cefotan IV, IM
cefoxitin - Mefoxin IV
cefprozil - Cefzil PO
cefuroxime - Ceftin, Zanacef IV, IM
cefamondole - Mandole IV
loracarbef - Lorabid PO
third generation cephalosproins
cefixime - Suprax PO
cefdinir - Omnicef PO
cefoperazone - Cefobid IV
cefotaxime - Claforan IV
cefpodoxime - Vantin PO
cefazidime - Fortaz, Tazicef IV, IM
cefibuten - Cedax PO
cefizoxime - Cefizox IV
ceftriaxone - Rocephin IV, IM
4th gen cephalosporins
cefepime - Maxipime IV, IM
linezolin
Zyvox IV, PO 600mg q12h
renally eliminated
active against
- enterococci, staphylococci,
streptococci, enterococcus faecium
(including VRE) (not E faecalis)
adverse effects:
- myelosuppression
- anemia, leukopenia, panncytopenia,
thrombocytopenia
- a weak MAO inhibitor
quinupristin-dalfopristin
Synercid IV 7.5mg/kg q8h
HEPATIC
combo synergistic against GRAM +
active against:
- staph and stretococci, enterococcus
faecium (including VRE) not E faecalis
adverse effects:
- common thrombophlebitis and severe
injection site reations
- some say central venous catheter only
- hyperbilirubinemia in 25%
- arthralgias and myalgias are common
vancomycin
Vanocin IV, PO 500mg q6h or 1g q12IV
125-2250 mg PO q6h
renally eliminated
active against:
- most gram + including the following:
- staphylococci (including MRSA)
- streptococi, enterococci, clostridium
(including C difficile)
- synergistic w/aminogoycoside against
enterococci
vancomycin

a/e
monitoring
adverse effects:
- nephrotoxicity, ototoxicity
- thrombophlebitis common requiring
frequent IV site rotation

monitoring
- trough concentrations (5-10mcg/ml) in
pts with renal impairment
- peak concentrations not routinely
monitored unless serious infection and
poor response (20-40mcg/ml)
Fluoroquinolones

spectrum
broad spectrum

Gram + (many staph strains)
strep becoming increasingly resistant
newer agents superior gram + coverage
limited enterococcal activity
inactive against MRSA

Gram - activity is extensive

anaerobic coverage is poor
fluorquinolones

a/e
GI: n/dyspepsia
CNS: ha/dizziness/insomnia
CV: QT prolongaton
Endocrine: hypo or hyperglycemia
GU: crystalluria
fluoroquinolones - newer

the players
sparfloxicin (Zagam) PO 200mg q24h

gatifloxacin (Tequin) IV, PO 400mg q24

clinafloxiain (apparently very new)

moxifloxacin (Avelox)
fluoroquinolones - older

the players
ciprofloxacin (Cipro)
- IV 400, PO 500 mg q12h
ofloxacin (Floxin)
- PO, IV 100-400mg/d
levofloxacin (Levaquin)
- PO, IV 500mg q24h
lomefloxacin (Maxaquin)
- PO 400mg qd
norfloxacin (Noroxin)
- PO 400mg bid
sparfloxacin (Zagam)
- Po 200 mg q24h
flurorquinolones

which two are eliminated hepatically
the rest of course are eliminated by which route?
moxifloxacin
norfloxacin

rest-renally eliminated
fluoroquinolones

monitoring

pt education
serum concentrations not monitored

only patient resonse

pt ed:
- avoid in children and pregnant or nursing women
- do NOT take antacids, multivitamis or other Ca, Mg, or Fe supplements for at least 2 h after each dose
Macrolides aka erythromycins

coverage
principally against gram + including penicillin resistant streptococci
Macrolides

adverse events
stimulate GI motility - pain, cramp, n/v/d
clarithromycin the least GI stimulating

erythormycin lactobionate causes thrombophlebitis
- dilute in 250ml and infuse over 30-60m
macrolides

the players

plus a ketolide
azithromycin (Zithromax)
- PO, IV 250mg/d hepatic

clarithromycin (Biaxin and Biaxin XL)
- 250mg bid Renal

erythomycin (various)
- Po 250-500 mg q6h hepatic
- IV 500-1000mg q6h hepatic

telithromycin (Ketek)
- PO 800mg/d hepatic
- 5d for bronchitis
- 7-10 for CAP
Macrolides aka erythromycins

coverage
principally against gram + including penicillin resistant streptococci
Macrolides

adverse events
stimulate GI motility - pain, cramp, n/v/d
clarithromycin the least GI stimulating

erythormycin lactobionate causes thrombophlebitis
- dilute in 250ml and infuse over 30-60m
macrolides

the players

plus a ketolide
azithromycin (Zithromax)
- PO, IV 250mg/d hepatic

clarithromycin (Biaxin and Biaxin XL)
- 250mg bid Renal

erythomycin (various)
- Po 250-500 mg q6h hepatic
- IV 500-1000mg q6h hepatic

telithromycin (Ketek)
- PO 800mg/d hepatic
- 5d for bronchitis
- 7-10 for CAP
tetracyclines

drugs of choice for the following
respiratory infections
- atypical pneumonia

Genital infections

systemic infections

other infections
- MRSA when vanc or others not approp
- H pylori w/bismuth subsalicilate and
either metronidazole or clarithromycin

malaria prophylaxis in mefloquine-resistant cases
tetracyclines

adverse events
photosensitivity reactions
- less with doxy and mino
CId during pregnancy
- bone growth and tooth discoloration

minocycline
- vestibular effects
- skin and membrane pigmentation
- lupus-like syndrom
tetracyclines

pearls
milk, antacids, Fe, Ca, Mg, Al
- decrease tetracycline absorption
- take several hours aprart

take several hours before or after food
tetracyclines

the players
demeclocycline (Declomycin)
-PO 300-1000mg/d renal

doxycycline (Vibramycin, others)
- PO 100-200mg q12h HEPATIC

minocycline (Minocin)
- PO, IV 100-200mg q12h HEPATIC

tetracycline (Achromycin V, Xumycin, Tetracyn, others)
- PO, IV, IM 1-2g/d renal
sulfonamides

spectrum
utility decreased due to resistence

Gram + coverage
- staph (MSSA and MRSA)
- strep
- not enterococci

Gram - coverage
- enterobacter, E coli, ...salmon, shig
sulfonamides

a/e
hypersensitivity rxns
- cross reactive with
- other sulfonamides
- diuretics (thiazides)
- sulfonylureas

rash, utricaria, stevens-Johnson synd
sulfonamindes

players
sulfamethoxazole/trimethoprim IV, PO
- Bactrim, Septra tablets HEPATIC
- 80 mg trim / 400 mg sulfa
- DS 160 trim / 800 sulfa
- susp 40 trim/200 sulfa per 5 mL

sulfamethizole (Urobiotic) PO renal
sulfisoxazole (Gantrisin) IV, PO renal
Bactrim indications
Oral and parenteral:
UTIs due to susceptible strains
Shigellosis enteritis:
Pneumocystis carinii pneumonia (PCP):

Oral:
Pneumocystis carinii pneumonia prophylaxis: in immunosuppressed pts
Acute otitis media in children:
Acute exacerbations of chronic bronchitis in adults:
Travelers' diarrhea in adults:
clindamycin

spectrum

dosing

a/e
covers aerobic gram + but not gram -
covers anaerobic gram -

Cleocin IV, PO
- 300mg q6h PO
- 600-900mg q8h IV

GI with all forms - n,v,d,pain, tenesmus
IV - thrombophlebitis
IM - sterile absesses
clindamycin

indications
Reserve for serious infections only

Reserve its use for patients allergic to penicillin or other patients for whom a penicillin is inappropriate. Before selecting clindamycin, consider the nature of the infection and the suitability of less toxic alternatives (eg, erythromycin) because of the risk of colitis
clindamycin BB warning
Because clindamycin therapy has been associated with severe colitis, which may end fatally, reserve it for serious infections for which less toxic antimicrobial agents are inappropriate. Do not use clindamycin in patients with nonbacterial infections, such as most upper respiratory tract infections.
imipenem-cilastin

dosing
spectrum
s/e
Primaxin IV, IM Renal
- around 500mg q6h

cilastin prevents renal metab of imipenem and has no abx activity itself

very broad-spectrum

GI - n/v/d (including c.diff)
staining of teeth
seizures
imipenem-cliastin

indications
Infections resistant to other antibiotics (eg, cephalosporins, penicillins, aminoglycosides) have responded to treatment with imipenem.
imipenem-cilastin

IM indications:
Treatment of serious infections of mild-to-moderate severity where IM therapy is appropriate. Not intended for severe or life-threatening infections, including bacterial sepsis or endocarditis, or in major physiological impairments (eg, shock).
Gynecologic infections
Lower respiratory tract infections
Intra-abdominal infections
Skin and skin structure infections
imipenem-cilastin

IV indications
Treatment of serious infections
Polymicrobic infections
Urinary tract infections (complicated and uncomplicated)
Intra-abdominal infections
Gynecologic infections
Bacterial septicemia
Bone and joint infections
Skin and skin structure infections
Endocarditis
Lower respiratory tract infections
warning for all antibiotics

regarding C. difficile
Clostridium difficile–associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents and may range in severity from mild diarrhea to fatal colitis.

Treatment with antibacterial agents alters the normal flora of the colon, leading to overgrowth of C. difficile.
other "Penems"
Merrem IV Renal
- 500-2000 mg q8h
- similar to imipenem but metabolized
differently - no need for cilastin
- dec CNS toxicity

Ertapenem (Invanz)
generally penems are reserved for what
moderate to severe infections in hospital-treated patients

IV, IM administration

very broad spectrum - "big guns"
chloramphenicol

indications
Chloromycetin IV
Serious infections:
chloramphenicol must be used only in those serious infections for which less potentially dangerous drugs are ineffective or contraindicated.

typhoid fever

Cystic fibrosis
chloramphenicol BB warning

big gun - basically last line unless certain serious condition (the plague, rat bite...)
- Serious and fatal blood dyscrasias (aplastic anemia, hypoplastic anemia, thrombocytopenia, and granulocytopenia) after both short-term and prolonged therapy
- must not be used when less potentially dangerous agents will be effective
- It must not be used in the treatment of trivial infections or where it is not indicated, as in colds, influenza, infections of the throat
daptomycin - name, route

indications

good enough
Cubicin IV

Staphylococcus aureus bloodstream infections

Complicated skin and skin structure infections (cSSSIs)

not indicated for the treatment of pneumonia
metronidazole
Flagyl oral, IV, topical, vaginal
-po 250, 375, 500, 750ER

ER labeled for bacterial vaginosis only
metronidazole

indications IV
Endocarditis
Intra-abdominal infections
Skin and skin structure infection
Gynecologic infection
Bacterial septicemia
Bone and joint infections
(CNS) infections
Lower respiratory tract infections
Anaerobic infections
metronidazole

off label IV
Off-label uses:
Pelvic inflammatory disease
metronidazole

indications PO
Symptomatic trichomoniasis
Asymptomatic trichomoniasis
Treatment of asymptomatic consorts
Amebiasis
Anaerobic bacterial infections
Intra-abdominal infections
Skin and skin structure infections
Gynecologic infections:
Bacterial septicemia
Bone and joint infection
CNS infections
Endocarditis
Lower respiratory tract infections
metronidazole

off label PO
Hepatic encephalopathy
Crohn's disease:
Diarrhea associated with C difficile
Helicobacter pylori
Recurrent and persistent urethritis
Bacterial vaginosis
Pelvic inflammatory disease:
Prophylaxis after sexual assault:
Gardnerella vaginalis and giardiasis