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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) |
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antimicrobial classes
penicillins |
penicillins
- natural - 2 - aminopenicillins - 3 - penicillinase resistant penicillins - 5 - carboxypenicillins - 2 - ureidopenicillins - 3 - combos with beta lactams - 4 |
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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 |
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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) |
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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 |
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aminoglycosides
how are all aminoglycosides elimated |
renally
|
|
aminoglycosides
spectrum |
aerobes
- most gram - - select gram + anaerobes - not effective against most |
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Beta Lactams
|
`
|
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β-lactams
broad class that includes the following subclasses |
- penicillin derivatives
- cephalosporins - monobactams - carbapenems - β-lactamase inhibitors |
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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 |
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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 |
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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 |
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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 |
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Penicillins
- extended spectrum |
azlocillin (Azlin) IM, IV
carbenicillin (Geopen) IM, IV ticarcillin (Ticar) IM, IV mezlocillin (Mezlin) IM, IV piperacillin (Pipracil) IM, IV |
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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 |
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what are the only 2 penicillins that are NOT eliminated renally
how are they eliminated? |
oxacillin
nafcillin hepatically |
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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 |
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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 |
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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 |
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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 |
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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 |
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Cephalosporins - a/e
|
β-lactam...
plus some have a disulfiram-like reaction - Antabuse |
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Cephalosporins - monitoring
|
serum concentrations not necessary
monitory for response |
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what is the only cephalosporine that is NOT renally eliminated
|
cefoperazone (Cefobid) IV
hepatic |
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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 |
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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 |
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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 |
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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 |
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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) |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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.
|
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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 |
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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 |
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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. |
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other "Penems"
|
Merrem IV Renal
- 500-2000 mg q8h - similar to imipenem but metabolized differently - no need for cilastin - dec CNS toxicity Ertapenem (Invanz) |
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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 |
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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 |
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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 |
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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 |