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Microsoft word - antibiotics chart 2006 version.doc

THE NEED-TO-KNOW ANTIMICROBIALS Yearly update by Rho Chi University of Washington School of Pharmacy Autumn Quarter, 2006
Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Binds to PBPs to inhibit cell wall synthesis, bactericidal Spectrum (Gm+, Gm-, anaerobes)
Gram +: streptococci, Enterococcus, but NOT S.
aureus
Gram - : only a few (E. coli, Proteus spp, a few
others)…lots of resistance
No below-the-diaphragm anaerobic activity
DOC for which diseases
AOM, ABS, prophylaxis of endocarditis before dental, esophageal, and upper respiratory procedures Absorption, distribution, metabolism, excretion
Absorbed well from GI tract; widely distributed in tissues (especially inflamed tissue); renal excretion PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Diarrhea--common, call MD if excessive, blood in stool or abdominal cramping Allergies
Possible anaphylaxis or rash Drug interactions
Dose (renal/hepatic failure, obesity)
AOM: 90mg/kg/day, div BID x 10 days ABS mild/moderate, w/out recent abx: 1 g TID x 10 days Endocarditis prophylaxis: 2 g po x 1 hr before appt. CrCl 10-50 mL/min: Give q8-12h <10 mL/min: Give q24h Pregnancy, pediatrics issues
Pregnancy B, ok in pediatrics Relative cost
Generic and very inexpensive
Generic name
AMOXICILLIN/CLAVULANIC ACID Proprietary name
Class (generation)
β-lactam/β-lactamase inhibitor combination MOA (bactericidal/bacteriostatic)
Amox: binds to penicillin binding proteins (PBPs) to inhibit protein synthesis (bactericidal) Clavulanic acid: inhibits β-lactamases Spectrum (Gm+, Gm-, anaerobes)
Gram + (S. aureus, Enterococcus, streptococci)
enteric gram -, H.flu, M.cat
anaerobes below the diaphragm
Very similar to amp/sulbactam in activity
DOC for which diseases
Refractory otitis media, acute/severe bacterial sinusitis, dog/cat bites, aspiration CAP Absorption, distribution, metabolism,
Absorption: 75%, excretion
Distribution: inflammation-mediated, gets to most tissues Excretion: Renal PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Common: N/V, antibiotic associated diarrhea Rare: thrombocytopenia Allergies
"Penicillin allergy" rash: 5-10%, anaphylaxis: 0.001% Drug interactions
Allopurinol may increase incidence or rash Dose (renal/hepatic failure, obesity)
Normal Doses: Refractory otitis media: 90mg/kg/day div q12hX10d (Pediatric) Acute/severe bact. Sinusitis & aspiration CAP: augmentin XR 2 tabs po BID X10-14d Dog/cat bites: 875 mg BID X 3-5d (prophylaxis) or 10-14d (infected wound) Renal failure: adjustment may be required Pregnancy, pediatrics issues
Pregnancy cat B, safe in pediatrics Relative cost
Moderately expensive
Generic name
Proprietary name
Omipen, Polycillin Class (generation)
MOA (bactericidal/bacteriostatic)
CIDAL, acid unstable antibiotic that inhibits the biosynthesis of cell wall mucopeptide (peptidoglycan). Most effective when bacteria are growing (subject to the inoculum effect). Spectrum (Gm+, Gm-, anaerobes)
Alone: covers streptococci and Enterococcus, but not
S. aureus
Gm- is ok for a few organisms, but watch out for
resistance. No Pseudomonas coverage.
Anaerobe coverage is poor because of β-lactamases
below the diaphragm
With sulbactam: modest Gm- improvement, but much
better gm+ (including S. aureus) and anaerobe
improvement
DOC for which diseases
Meningitis (for Listeria monocytogenes) Gastroenteritis (for Listeria monocytogenes) Complicated UTI/catheters (alternative choice) Pneumonia (not reliable for H. influenzae) Absorption, distribution, metabolism,
Good GI absorption excretion
Distribution: bound to plasma proteins, diffuses readily into most tissues with inflammation. Excretion: Largely unchanged in the urine PD (time vs. concentration dependent killing)
Time dependent killing Side effects (what, how common, monitoring)
Fever, rash fairly common, diarrhea is a serious problem Allergies
0.7-10% Rash and anaphylaxis. X-sensitivity to all PCN's, and varying X-sensitivity to cephalosporins Drug interactions
Allopurinol (increases frequency of rash) Oral contraceptives (the general warning) Dose (renal/hepatic failure, obesity)
Normal: 250-500 mg po q6h OR 150-200 mg/kg/d IV Max IV dose in adults: 2 gm IV q4h Renal Failure: CrCl >50-90 same, CrCl 10-50: q6-12h, CrCl <10: q12-24h Pregnancy, pediatrics issues
Pregnancy category B, excreted in breast milk, may lead to sensitization Relative cost
Oral 500 mg 35 cents (CHEAP); IV modestly priced
Generic name
AMPICILLIN/SULBACTAM Proprietary name
Class (generation)
Aminopenicillin/β-lactamase inhibitor combination MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs; sulbactam is a β lactamase inhibitor Spectrum (Gm+, Gm-, anaerobes)
G+: streptococci, S. aureus, Enterococcus G-: E. coli, Klebsiella, Proteus, H. influenzae Anaerobes: good for below-diaphragm The sulbactam improves the S. aureus and anaerobic
coverage of ampicillin, but only modestly improves
G- coverage

DOC for which diseases
Intra-abdominal infections With advanced macrolide (azithromycin) for CAP treated on inpatient basis, non ICU (especially if aspiration pneumonia is a concern) Absorption, distribution, metabolism,
excretion
D-to bile, blister, tissue fluids, CSF (inflamed). M-not particularly significant E-75-85% excreted unchanged in urine in 8 hrs. Half-life 1.3 hours. PD (time vs. concentration dependent killing) Time dependent killing
Side effects (what, how common, monitoring) Rash, diarrhea
Allergies
Contraindicated in patients with penicillin and (true) cephalosporin allergies (about 20-40% chance the latter will be allergic to penicillins) Drug interactions
Ampicillin levels can be increased by probenecid. Penicillins may increase methotrexate exposure during concurrent therapy. Monitor MTX levels. Dose (renal/hepatic failure, obesity)
1.5-3 g IV q6h Adjust for renal dysfunction Pregnancy, pediatrics issues
Safe in pediatric and pregnant patients (B) Relative cost
Moderately expensive
Generic name
Proprietary name
Class (generation)
Azalide (advanced-generation macrolide) MOA (bactericidal/bacteriostatic)
Inhibits bacterial growth by suppressing RNA-dependent protein synthesis, bacteriostatic Spectrum (Gm+, Gm-, anaerobes)
Gram pos: S. pneumoniae (lots of resistance, though), other streptococci; not a good staph drug (no MRSA) Gram neg: H. influenzae, M. catarrhalis (not really a good Gram-negative drug) Atypicals (Legionella, Mycoplasma, Chlamydia): good coverage No useful anaerobic activity below diaphragm DOC for which diseases
Penicillin allergic AOM, CAP w/ no previous antibiotics, Chlamydia STD Absorption, distribution, metabolism,
Absorption:good (newest data suggest no reason to avoid excretion
antacids), bioavailability 37% Tissue half-life: 2-4 days Distribution: especially good into lungs PD (time vs. concentration dependent
AUC/MIC correlates best with activity killing)
Side effects (what, how common,
N/V, antibiotic associated diarrhea (rare) monitoring)
Prolong QTc interval (generally minor)
Very well-tolerated drug in general
Allergies
Drug interactions
Digoxin: increases serum levels of digoxin? Dose (renal/hepatic failure, obesity)
Normal Doses: Pen-allergic AOM: 30 mg/kg/day (single dose, or divided over 3-5 days) Pharyngitis: 60 mg/kg/day (divided over 5 days) CAP: 500 mg day 1, then 250 mg day 2-5 (adult) Chlamydia: 1 gm x1 Pregnancy, pediatrics issues
Pregnancy category B, safe in pediatrics Relative cost

Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs. Spectrum (Gm+, Gm-, anaerobes)
Gram (-) including Pseudomonas; no G+, no anaerobes. Not a drug that is commonly used. DOC for which diseases
Useful in patients with a history of severe allergy to penicillin (extremely low rate of cross-allergenicity). Used with metronidazole in secondary peritonitis. Absorption, distribution, metabolism, excretion
Given IV/ IM. Half life approx 1.7 hrs. Distributes throughout body. Mainly excreted in the urine. 12% fecal. PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Pain at injection site, G.I upset, Drug-induced eosinophilia (all somewhat rare) Allergies
Virtually no cross reactivity with other ß-lactams
Drug interactions
Monitor renal function if used with aminoglycosides Dose (renal/hepatic failure, obesity)
1-2 gm IV q6-8h. However, dose adjustments needed for renal dysfunction. The liver plays a minor role in elimination. Pregnancy, pediatrics issues
Pregnancy category B, safety/effectiveness under 9 months not established Relative cost
Expensive- no generic available
Generic name
Proprietary name
Class (generation)
1st generation cephalosporin (IV drug) MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs. Spectrum (Gm+, Gm-, anaerobes)
Mainly gram +, a few enteric GNRs. No anaerobes below the diaphragm. DOC for which diseases
Surgical prophylaxis, occasional skin infections. Absorption, distribution, metabolism,
Distributes into bone well. Does not distribute into excretion
CSF in useful concentrations, even if inflamed. Excreted mainly unchanged in urine. PD (time vs. concentration dependent killing)
Time dependent killing. Side effects (what, how common, monitoring)
Allergies
Cross reactivity possible for those with penicillin allergies (under 5%) Drug interactions
Nothing significant Dose (renal/hepatic failure, obesity)
Decrease dose in renal insufficiency Pregnancy, pediatrics issues
Pregnancy category B Relative cost
Relatively cheap- generic available.
Generic name
Proprietary name
Class (generation)
3rd generation oral cephalosporin MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs. Spectrum (Gm+, Gm-, anaerobes)
Gram (+) cocci like Strep. Might work for S. aureus (not MRSA). Like all cephalosporins it is ineffective for Enterococcus. DOC for which diseases
Some pediatricians favor cefdinir for AOM because of its relatively pleasant taste Absorption, distribution, metabolism,
Absorption independent of food. Half life approx 1.7 excretion
hrs. Distributes into tissue. Excreted renally. PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
GI upset, headache Allergies
Cross reactivity possible for those with penicillin allergies (but chance is <1%) Drug interactions
Antacids may decrease absorption Dose (renal/hepatic failure, obesity)
AOM: 14 mg/kg/day Decrease dose for renal dysfunction Pregnancy, pediatrics issues
Pregnancy category B Relative cost
Moderately expensive- no generic available.
Generic name
Proprietary name
Class (generation)
4th generation cephalosporin MOA (bactericidal/bacteriostatic)
Spectrum (Gm+, Gm-, anaerobes)
Summary: Best of ceftriaxone + best of ceftazidime • Gm+ • lacks anaerobes • Pseudomonas • β lactamase stable DOC for which diseases
• ICU monotherapy, maybe better than imipenem because it lacks anaerobe coverage • In combination with ciprofloxacin for ICU treatment of CAP, 1-2 g IV q 12h x 10 days Absorption, distribution, metabolism,
excretion
D: 20% protein bound, CSF concentrations decent M: Liver metabolism minor E: 85% unchanged in the urine PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
• headache, confusion (rare) • bleeding and bruising (rare, monitor PT) • Mild diarrhea, more common Allergies
Less than 1% cross-reactivity if PCN allergy (rash) Drug interactions
Nothing significant Dose (renal/hepatic failure, obesity)
1-2 gm IV q8-12h Adjust for renal dysfunction Pregnancy, pediatrics issues
Pregnancy category B Relative cost

Generic name
Proprietary name
Class (generation)
3rd generation cephalosporin MOA (bactericidal/bacteriostatic)
Spectrum (Gm+, Gm-, anaerobes)
• Gm- (bacilli), but not Pseudomonas • No below diaphragm anaerobes DOC for which diseases
• Bacterial meningitis for 0-1 month old along with ampicillin, 75 mg/kg q 6h Absorption, distribution, metabolism,
excretion
D: 30-51% protein bound, CSF penetration good M: Liver converts it to active metabolite E: Renal 50-85%, biliary 15-75% PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
• Agranulocytosis (rare) • Steven-Johnson syndrome (rare) • Mild diarrhea, nausea (more common) Allergies
Less than 1% cross-reactivity if PCN allergy (rash) Drug interactions
Nothing significant Dose (renal/hepatic failure, obesity)
1-2 gm IV q8-12h (adults) Adjust for renal dysfunction Pregnancy, pediatrics issues
Pregnancy category B Safe in pediatrics Relative cost

Generic name
CEFPODOXIME PROXETIL Proprietary name
Class (generation)
3rd generation oral cephalosporin MOA (bactericidal/bacteriostatic)
Bactericidal – inhibits cell wall synthesis Spectrum (Gm+, Gm-, anaerobes)
Some Gram + and Gram – bacteria (stable against β-lactamases) NOT: MRSA, Enterococcus, Pseudomonas, Enterobacter DOC for which diseases
Can be used in AOM if recent antibiotic use Can be used in ABS if recent antibiotic use Absorption, distribution, metabolism,
Bioavailability 46% excretion
Minimal metabolism PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Diarrhea, nausea –common Allergies
Watch for penicillin allergy (but cross-allergenicity is probably less than 1%) Drug interactions
Dose (renal/hepatic failure, obesity)
10 mg/kg/day (AOM) 200 mg po bid (ABS) Pregnancy, pediatrics issues
Pregnancy category B Relative cost

Generic name
Proprietary name
Fortaz, Tazicef, Tazidime Class (generation)
Third generation cephalosporin MOA (bactericidal/bacteriostatic)
Spectrum (Gm+, Gm-, anaerobes)
Gm+: limited; don't trust for these Gm-: Pseudomonas, most Enterobacteriaceae Anaerobes: not useful for below-the-diaphragm DOC for which diseases
1. Pseudomonas pneumonia in CF patients 2. Other diseases due to Gram-negative bacteria: life-threatening, susceptible Gram-negative organisms including Pseudomonas and Enterobacteriaceae 3. Gram-negative osteomyelitis, especially due to Pseudomonas 4. Hospital acquired peritonitis (in combination with an antianaerobic drug) 5. Meningitis due to Pseudomonas 6. Nosocomially-acquired UTI Absorption, distribution, metabolism,
A: Parenteral only excretion
D: widely throughout the body including bone, bile, skin, CSF, endometrium, heart, pleural and lymphatic fluids M: minimally metabolized E: 90-96% renal PD (time vs. concentration dependent killing)
Time dependent killing Side effects (what, how common, monitoring)
Hypersensitivity (rash), transient eosinophilia, increased liver function tests Allergies
Hypersensitivity to ceftazidime Drug interactions
Nothing significant Dose (renal/hepatic failure, obesity)
1-2 gm IVq8h Adjust for renal dysfunction Pregnancy, pediatrics issues
Category B; OK to use in pediatrics Relative cost
Moderately expensive
Generic name
Proprietary name
Class (generation)
3rd generation cephalosporin MOA (bactericidal/bacteriostatic)
Binds to PBPs to inhibit cell wall synthesis, bactericidal Spectrum (Gm+, Gm-, anaerobes)
Gram – (no Pseudomonas), Gram +, no below diaphragm anaerobes DOC for which diseases
CAP, inpatient, when Pseudomonas not an issue; bacterial meningitis for 1 mo-50 yrs; necrotizing fasciitis; NVE caused by HACEK group, gonorrhea (urethral, cervical, rectal, pharyngeal, and DGI) Absorption, distribution, metabolism, excretion
100% absorption w/IM or IV administration; widely distributed in tissues including CSF, synovial fluid; minimally metabolized; biliary excretion PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Rash, diarrhea, eosinophilia, increase in LFTs, all uncommon, monitor for severity Allergies
Rash and anaphylaxis uncommon Drug interactions
Dose (renal/hepatic failure, obesity)
CAP, inpatient, when Pseudomonas not an issue: 2 g IV Q24h (+adv. macrolide) Bacterial meningitis for 1 mo-50 yrs: 2 g IV q12h (+vanco+dex) Necrotizing fasciitis: 2 g q12h (+ clindamycin) NVE caused by HACEK group: 2 g IV Q24h x4 wks Gonorrhea (urethral, cervical, rectal, pharyngeal): 125 mg IM x 1 DGI: 1 g IM/IV q24h x 7 days No dose adjustment necessary for renal disease, but possibly for severe hepatic impairment Pregnancy, pediatrics issues
Pregnancy B, safe in pediatrics Relative cost

Generic name
CEFUROXIME AXETIL Proprietary name
Class (generation)
Cephalosporin (oral, second generation) MOA (bactericidal/bacteriostatic)
CIDAL, inhibit mucopeptide synthesis (peptidoglycan) in the bacterial cell wall making it unstable; more effective against rapidly growing bacteria (subject to the inoculum effect) Spectrum (Gm+, Gm-, anaerobes)
Ok Gm+ (not as potent as 1st gen) Better Gm- than 1st gen (not Pseudomonas) Anaerobic coverage not especially good Better β-lactamase resistance than 1st gen, therefore better for resistant strains than 1st gen DOC for which diseases
AOM, ABS (one of a number of options) Absorption, distribution, metabolism,
Absorption: absorbed from GI and rapidly hydrolyzed excretion
in intestinal mucosa and blood, take with food Distribution: widely distributed to most tissues and fluids including CSF (not used for meningitis, though) Metabolism: metabolized to free cefuroxime plus acetaldehyde and acetic acid Excretion: primarily excreted renally PD (time vs. concentration dependent killing)
Time-dependent killing Side effects (what, how common, monitoring)
Anemia, eosinophilia, neutropenia (very rare) Allergies
Cross-sensitivity to penicillins probably on the order of 1-2% Drug interactions
None to speak of Oral contraceptives—the general warning with antibiotics Dose (renal/hepatic failure, obesity)
PO: 250-500 mg q12h Oral suspension for AOM: 30 mg/kg day divided q12h Adjust for renal dysfunction Pregnancy, pediatrics issues
Category B, excreted in breast milk in small quantities Relative cost
Oral moderately priced
Generic name
Proprietary name
Class (generation)
1st generation cephalosporin MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis. Spectrum (Gm+, Gm-, anaerobes)
Better Gm + than Gm -. Gm+: S. aureus (not MRSA); S. pneumoniae Gm-: E.coli; Klebsiella sp; Proteus mirabilis Anaerobic activity: not good DOC for which diseases
Skin infections caused by Gm + organisms Absorption, distribution, metabolism,
Well absorbed from the GI tract and widely distributed excretion
throughout the body and many tissues. Primarily eliminated by kidney excretion. PD (time vs. concentration dependent killing)
Time dependent killing Side effects (what, how common, monitoring)
May cause mild diarrhea. Allergies
Not given to patient with a history of anaphylaxis to penicilin or known cephalosporin hypersensitivity. Probably OK to give to a patient with a history of penicillin rash (cross-allergenicity <5%, if that high) Drug interactions
None of significance Dose (renal/hepatic failure, obesity)
Normal: 250-500mg po q6h Renal failure: increase dosing interval to q12h Pregnancy, pediatrics issues
Pregnancy category B; safe in pediatrics Relative cost
500 mg generic $0.44
Generic name
Proprietary name
Class (generation)
FQ, early 2nd generation, non-respiratory MOA (bactericidal/bacteriostatic)
Binds to DNA gyrase and/or topoisomerase IV to inhibit DNA replication and repair. Bactericidal. Spectrum (Gm+, Gm-, anaerobes)
Gram-, limited Gram +, no anaerobic coverage DOC for which diseases
Acute uncomplicated cystitis (when TMP/SMX resistance 20% and for elderly patients), acute uncomplicated pyelonephritis Absorption, distribution, metabolism, excretion
Bioavailability 70%; widely distributed in most tissues, including synovial and prostatic fluids; eliminated by both renal and nonrenal mechanisms. Half-life 4 hours. PD (time vs. concentration dependent killing)
Concentration-dependent Side effects (what, how common, monitoring)
Nausea, CNS toxicity, tendon toxicity (rare). All uncommon, monitor for severity. Allergies
Rash uncommon, anaphylaxis rare Drug interactions
CYP1A2 inhibitor Dose (renal/hepatic failure, obesity)
Acute uncomplicated cystitis: 250 mg po BID x 3 days for non-elderly, 7-10 days for elderly Acute uncomplicated pyelonephritis: 500 mg po BID x 10-14 days or 200-400 mg IV q12h x 7-14 days CrCl 10-50 mL/min: decrease dose by 50-75% CrCl <10 mL/min: decrease dose by 50% Pregnancy, pediatrics issues
Pregnancy category C, not FDA-approved in pediatrics except for treatment of anthrax and complicated pyelonephritis Relative cost
Generic and relatively inexpensive
Generic name
Proprietary name
Class (generation)
Advanced macrolide MOA (bactericidal/bacteriostatic)
Spectrum (Gm+, Gm-, anaerobes)
Gm+: Group A,B,C, and G streptococci; S. pneumoniae; MSSA Gm-: M. catarrhalis, H. influenzae Atypicals: Mycoplasma, Chlamydophila, Legionella No usable antianaerobic activity DOC for which diseases
Acute exacerbation of chronic bronchitis Acute otitis media (alternative) Community acquired pneumonia (alternative in certain patients) Maxillary sinusitis, acute (alternative) Tonsillitis/pharyngitis H. pylori Absorption, distribution, metabolism,
Bioavailability: 50% excretion
Vd 4 L/kg, protein binding 42-50% Metabolized in liver (active metabolite) Mixed renal and nonrenal elimination, half life 5-7 hr PD (time vs. concentration dependent killing) Time-dependent killing
Side effects (what, how common, monitoring) Common: nausea and vomiting, diarrhea, headache.
Metallic taste is particularly bothersome to patients. Allergies
True allergy to clarithromycin is rare Drug interactions
Inhibitor and substrate of CYP3A4 Dose (renal/hepatic failure, obesity)
Normal:500 mg q12h po or ER 1 gm po qd Renal dosing: CrCl 10-50: 75% of the dose CrCl<10: 50 % of the dose or extend the dosing interval. Pregnancy, pediatrics issues
Category C Can be used in pediatric patients Relative cost
500mg About 5 dollar per tab ER: also about 5 dollar per tab
Generic name
Proprietary name
Class (generation)
Lincosamide (the only one on the US market) MOA (bactericidal/bacteriostatic)
B'static: binds to 50S ribosomal subunit, inhibiting protein synthesis. B'cidal in high concentrations (but still generally viewed as a static drug) Side benefit: appears to decrease toxin synthesis by certain organisms Spectrum (Gm+, Gm-, anaerobes)
Anaerobes (B. fragilis group). Gm (+) cocci [including
streptococci and community-associated-MRSA]. No
aerobic G- activity.
DOC for which diseases
Necrotizing faciitis [in combination with a β-lactam – ceftriaxone or Pen G if GABS]. Also a popular choice for a lung abscess. Absorption, distribution, metabolism,
excretion
T1/2: 1.5-6.5hrs, hepatic metabolism Distribution: High concentrations in bone and urine; no significant levels in CSF, even with inflamed meninges; crosses placenta; enters breast milk Eliminated in feces and bile Excretion: Urine (10%) and feces ( 4%) as active drug and metabolites PD (time vs. concentration dependent killing) Time dependent
Side effects (what, how common, monitoring) Diarrhea (20-30%)
Pseudomembranous colitis due to C. difficile overgrowth (discontinue if significant diarrhea, cramps, or passage of blood and mucus occur) Allergies
No major issues. Drug interactions
Increased duration of neuromuscular blockade from tubocurarine, pancuronium (contraindicated in botulism cases) . Dose (renal/hepatic failure, obesity)
Usual dose: Oral: 150-450 mg q6h (max: 1.8 g/day) IM, IV: 600-900mg q8h (max: 4.8 g/day) Adjustment is recommended in patients with severe hepatic disease. Pregnancy, pediatrics issues
Pregnancy Category B, safe in kids Relative cost
$8.00/600mg IV ($24-$36/day)
Generic name
COLISTIN (POLYMYXIN E), administered as the prodrug COLISTIMETHATE Proprietary name
Coly-Mycin M Parenteral Class (generation)
Polymyxin (a cyclic polypeptide) MOA (bactericidal/bacteriostatic)
Bactericidal. Binds to lipopolysaccharide and alters cell membrane permeability, leading to spillage of cytoplasmic content and cell death Spectrum (Gm+, Gm-, anaerobes)
Many Gram-negative bacilli including P. aeruginosa and Acinetobacter. However, Gram-positive organisms, anaerobes, and a few common Gram-negatives are resistant. DOC for which diseases
None. Useful for serious infections caused by Gram-negative bacilli resistant to everything else. Used in inhaled form in patients with cystic fibrosis. Absorption, distribution, metabolism,
Not absorbed PO. CSF concentrations uncertain (can excretion
be directly instilled). A small fraction of administered colistimethate is hydrolyzed to colistin, which is mostly eliminated nonrenally. Half-lives: colistimethate 2 hours, colistin 4 hours. PD (time vs. concentration dependent killing) Concentration-dependent, limited postantibiotic effect
Side effects (what, how common, monitoring)
Nephrotoxicity (10-15%); neurotoxicity (7%) Allergies
2% incidence of hypersensitivity Drug interactions
Not well studied Dose (renal/hepatic failure, obesity)
Supplied in vials labeled with colistin base activity (150 mg each, equivalent to 400 mg colistimethate sodium). IV Dose: 2.5-5.0 mg/kg/day of colistin base activity, divided 2-4 times a day. Duration depends on indication. Adjust for renal dysfunction. Inhaled dose of colistimethate sodium: 40-60 mg, 2-3 times a day. Better tolerated than inhaled colistin. Pregnancy, pediatrics issues
Relative cost
About $100/day (IV)
Generic name
Proprietary name
Class (generation)
Cyclic lipopeptide MOA (bactericidal/bacteriostatic)
Binds to bacterial membranes and causes rapid
depolarization of membrane potential, leading to
inhibition of protein, DNA, and RNA synthesis and cell
death. Rapidly bactericidal.
Spectrum (Gm+, Gm-, anaerobes)
Vancomycin-like spectrum (includes VRE, MRSA,GISA, PRSP). No useful G- activity, no anaerobic coverage. DOC for which diseases
Approved for skin infections, but not likely to be a big use for this drug, Good use: endocarditis due to VRE Also an for endocarditis due to MRSA and non-MRSA S. aureus Absorption, distribution, metabolism,
excretion
D: thought to have limited tissue penetration; binds to
lung surfactant so must never be used for pulmonary
infections
M: Minimal metabolism
E: Renally excreted
PD (time vs. concentration dependent killing)
Concentration-dependent killing Side effects (what, how common, monitoring)
Increased CPK—monitor for muscle pain or weakness; potential to cause muscle damage still uncertain Allergies
Hypersensitivity reactions possible Drug interactions
HMG-CoA reductase inhibitors—Cubist recommends discontinuing them during daptomycin therapy Dose (renal/hepatic failure, obesity)
Usual dose for skin infections: 4 mg/kg q24h If CrCl < 30: 4 mg/kg q 48 h Endocarditis dose (unapproved) 6 mg/kg q24h Pregnancy, pediatrics issues
Pregnancy: B Pediatrics: Not approved in patients under 18 Relative cost
$135 per 500mg vial
Generic name
Proprietary name
Class (generation)
Penicillinase-resistant penicillin MOA (bactericidal/bacteriostatic)
Bactericidal; inhibits cell wall synthesis Spectrum (Gm+, Gm-, anaerobes)
S. aureus (MSSA), streptococci
NOT ACTIVE FOR MRSA or coagulase-negative
staphylococci

DOC for which diseases
Impetigo (especially bullous) Ecthyma In general, a reasonable choice for a skin infection due to S. aureus or S. pyogenes Absorption, distribution, metabolism,
A: Oral - 60-80% excretion
D: volume of dist: 0.16 L/kg M: Hepatic E: Mainly by the liver PD (time vs. concentration dependent killing)
Time-dependent killing Side effects (what, how common, monitoring)
Diarrhea (don't expect a lot) Rash Allergies
Hypersensitivity reaction possible Drug interactions
Dose (renal/hepatic failure, obesity)
No specific adjustment necessary in renal failure Pregnancy, pediatrics issues
Pregnancy: B Pediatric: OK Relative cost
500 mg generic = $1.20
Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bacteriostatic, binds to bacterial ribosome Spectrum (Gm+, Gm-, anaerobes)
Gram (+) and Gram (-) (resistance is a problem with tetracyclines) Atypical pathogens (for CAP) DOC for which diseases
Possible for CAP (healthy, no recent antibiotics) Possible for cat bite in penicillin-allergic patient Absorption, distribution, metabolism,
A: oral, almost complete excretion
D: wide M/E: feces 30%, urine 23% PD (time vs. concentration dependent killing)
Concentration-dependent killing Side effects (what, how common, monitoring)
Nausea—a common problem with this drug "Bad taste" Diarrhea Less phototoxicity than with tetracycline Allergies
Drug interactions
Increases activity of warfarin Cations (aluminum, iron, magnesium) decrease absorption of doxycycline Dose (renal/hepatic failure, obesity)
100 mg po q12h No specific adjustments necessary in renal failure Pregnancy, pediatrics issues
Pregnancy: D Not in children under 8 Relative cost

Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs. Excellent β-lactamase stability (typical of a carbapenem). Spectrum (Gm+, Gm-, anaerobes)
More active than imipenem against Enterobacteriaceae,
but not clinically useful for P. aeruginosa. A bit less
active than imipenem against gram-positive aerobic
organisms and anaerobes. Poor activity against
Enterococcus
, Stenotrophomonas, and Acinetobacter.

DOC for which diseases
Not DOC for anything, but a useful alternative for mild-to-moderate intraabdominal infection, and also CAP Absorption, distribution, metabolism,
Parenteral only. 85-95% protein bound, Vd 8L at excretion
steady state. Renal excretion 80% of total drug (40% unchanged, 40% ring-opened form). Elimination half-life 4 hours, prolonged in renal insufficiency. PD (time vs. concentration dependent killing) Time-dependent (like all β-lactams)
Side effects (what, how common, monitoring)
Typical of a β-lactam (GI, dermatologic). Seizures not a problem (as they were initially with imipenem). May cause LFT and hematologic abnormalities (rare). Allergies
Avoid in patients with history of penicillin-induced anaphylaxis Drug interactions
None significant Dose (renal/hepatic failure, obesity)
1 gm IV/IM q24h. Decrease to 500 mg IV/IM q24h if CrCl less than 30. Duration of treatment depends on specific infection. Pediatric (3 mon-12 years): 15 mg/kg IV/IM bid, maximum 1 gram/day. Pregnancy, pediatrics issues
Relative cost
$40-50 per gram depending on the institution
Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bacteriostatic. Inhibits bacterial growth by suppressing RNA-dependent protein synthesis. Spectrum (Gm+, Gm-, anaerobes)
Gm+ aerobes and atypicals (Mycoplasma, Chlamydophila, Legionella) No good for MRSA Poor for most Gram-negatives, no good for anaerobes DOC for which diseases
Atypical pneumonia; diphtheria; pertussis; Alternative to amoxicillin for preventing bacterial endocarditis Absorption, distribution, metabolism, excretion
Absorbed well from the fasting GI tract, distributed readily into most tissues except brain and CSF, excreted primarily in bile. PD (time vs. concentration dependent killing)
Time-dependent killing Side effects (what, how common, monitoring)
N/V/D, abdominal cramps (due to hemiketal metabolites formed in the gut); may prolong QTc interval (questionable significance) Allergies
Drug interactions
CYP 3A4 inhibitor.
Increases blood levels of benzodiazepines,
carbamazepine, cyclosporine, ergot alkaloids,
lovastatin, simvastatin, tacrolimus, pimozide
Dose (renal/hepatic failure, obesity)
Normal: 250-500mg po (or IV) q6h Possibly adjust dose for CrCl <10 Orally available as salt form and esters (be careful with doses) Pregnancy, pediatrics issues
Pregnancy category B Pediatrics: safe Relative cost
Generally inexpensive
Generic name
Proprietary name
Class (generation)
Antimycobacterial agent MOA (bactericidal/bacteriostatic)
Spectrum (Gm+, Gm-, anaerobes)
Mycobacterium spp. DOC for which diseases
Initial treatment of active TB (to cover resistance) Removed from therapy as soon as susceptibility to INH and RIF are confirmed Absorption, distribution, metabolism,
Poor CNS penetration regardless of inflammation excretion
Renal elimination PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Most frequent toxicity: optic neuritis (dose-related). May result in changes in red-green color perception. Allergies
Drug interactions
No significant interactions Dose (renal/hepatic failure, obesity)
Must adjust dose in renal dysfunction Pregnancy, pediatrics issues
CDC says "safe" in pregnancy Relative cost

Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal, inhibits protein synthesis by binding with 30S ribosomal subunit. Spectrum (Gm+, Gm-, anaerobes)
Aerobic gram-negative bacilli, Pseudomonas aeruginosa. Synergistic with cell-wall active drugs for G+ organisms. No anaerobic coverage. DOC for which diseases
HAP (w/antipseudomonal β-lactam) Absorption, distribution, metabolism,
Poor oral absorption excretion
Vd = 0.26 L/kg; does not cross blood-brain barrier Relatively low concentrations in lung secretions Renally eliminated, T1/2 = 2-3 hours PD (time vs. concentration dependent killing)
Concentration dependent killing Side effects (what, how common, monitoring)
Nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade at high concentrations Allergies
Drug interactions
Increased nephrotoxicity with amphotericin B, cisplatin, cyclosporine, NSAIDs, vancomycin, radiographic contrast. Increased ototoxicity with cisplatin and loop diuretics. Increased apnea or respiratory paralysis with neuromuscular blocking agents. Dose (renal/hepatic failure, obesity)
2 mg/kg load, then 1.7 mg/kg IV q8h Sarubbi-Hull dosing nomogram is very useful Peak = 5-8 mcg/ml (10-12 for pneumonia, <3 for G+) Trough = <1 mcg/ml Renal failure: adjust dose based on CrCl Obesity: Dose based on IBW + 0.4(TBW-IBW) Pregnancy, pediatrics issues
Pregnancy Category D, may be used in pediatrics, Breastfeeding: infant risk minimal Relative cost

Generic name
IMIPENEM/CILASTATIN Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal, interferes with last stage of bacterial cell
wall synthesis.
Excellent β-lactamase resistance.
Spectrum (Gm+, Gm-, anaerobes)
Very broad spectrum: most gram positive, gram negative (including Pseudomonas), and anaerobes. Not Coag(-) staph or MRSA. DOC for which diseases
Hospital acquired infections: high severity intraabdominal infections, hospital-acquired pneumonia Absorption, distribution, metabolism,
Not absorbed by GI tract. Given IV or IM. Hydrolyzed excretion
by dihydropeptidases present in brush border of renal proximal tubule to a toxic metabolite; therefore given with cilastatin, an inhibitor of these enzymes, to prevent breakdown. 70% excreted in urine as active drug. Half-life 1 hour. PD (time vs. concentration dependent killing)
Time-dependent killing Side effects (what, how common, monitoring)
N/V if infused too quickly. Increased potential for seizures if recommended doses exceeded in patients with CrCl less than 20 ml/min. Allergies
Incidence of hypersensitivity is low. Potential for cross-reactivity with other β-lactams is about 50% for immediate hypersensitivity, 10% or less for accelerated hypersensitivity Drug interactions
Dose (renal/hepatic failure, obesity)
500 mg q6h IV – adjust for renal failure. CrCl>50-90: 250-500 mg q6-8h CrCl 10-50: 250 mg q6-12h CrCl<10: 125-250 mg q12h Pregnancy, pediatrics issues
Pregnancy category C, well tolerated in adults and children. Safety and efficacy of IM product not established in children under 12. Relative cost
500 mg Primaxin: $33.10. One of the more expensive antimicrobials.
Generic name
Proprietary name
INH (abbreviation for isonicotinic acid hydrazide) Class (generation)
Antituberculous agent, first line MOA (bactericidal/bacteriostatic)
Bactericidal, mechanism unknown--possibly via inhibition of mycolic acid synthesis resulting in disruption of the cell wall Spectrum (Gm+, Gm-, anaerobes)
Mycobacterium tuberculosis DOC for which diseases
Absorption, distribution, metabolism, excretion
A-Rapid and complete; slowed with food D-distributes widely to all body tissues and fluids, CYP 2E1 inhibitor
including CSF; crosses placenta; enters breast milk MAO inhibitor (weak)
M-mostly hepatic by acetylation E-Half-life: Fast acetylators:30-100 minutes Slow acetylators: 2-5 hours 75-95% excreted in urine; also in feces and saliva PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Hepatitis (monitor LFT baseline, 1, 3, and 6 months). Avoid ethanol. Peripheral neuropathy (give pyridoxine 25-50 mg qd). Allergies
Drug interactions
Metabolic enzyme inhibitor (CYP2C19, CYP3A4).
Significance uncertain, don't fret too much about
this.

Dose (renal/hepatic failure, obesity)
5 mg/kg/day (max 300 mg qd). Duration depends on clinical situation. Pregnancy, pediatrics issues
Pregnancy category C. Enters breast milk, compatible with lactation Relative cost
Cheap: 300 mg tablets, 30/$9.84
Generic name

Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Inhibits DNA gyrase and/or topoisomerase IV in susceptible organisms thereby inhibits relaxation of DNA and promote breakage. Bactericidal. Spectrum (Gm+, Gm-, anaerobes)
Very good coverage of almost all Gram negatives; borderline for Pseudomonas. Decent Streptococcus coverage and non-resistant S. aureus. Active vs. Enterococcus if in the urine. Poor anaerobic coverage, not reliable for MRSA. DOC for which diseases
CAP/HAP; UTI in elderly and where E. coli is >20% TMP/SMX resistant; bacterial sinusitis if exposed to antibiotics one month prior Absorption, distribution, metabolism,
Oral: bioavailability=99% excretion
Distribution: Vd:1.25L/kg, CSF conc. about 15% of serum levels, high concentrations in prostate, lung, gynecological tissues, sinus, saliva Metabolism: minimal Excretion: primarily urine as unchanged drug, half-life 6-8 hours PD (time vs. concentration dependent killing) Concentration dependent (AUC/MIC correlates best)
Side effects (what, how common, monitoring) Gastrointestinal: diarrhea, nausea
Neurologic: confusion, headache Cardiovascular: QTc prolongation (rare) Endocrine: hypoglycemia (in diabetic patients, rare) Musculoskeletal: rupture of tendon (rare) Acute interstitial nephritis (rare) Allergies
Skin rashes occur now and then (generally uncommon) Drug interactions
Avoid use of metal cations (e.g. aluminum, magnesium) Dose (renal/hepatic failure, obesity)
Normal: 500 mg IV/PO qd (UTI: 250 mg PO qd) CrCl between 10-50: 500 mg x1, then 250 mg q24-48h CrCl <10: 500 mg x1 then 250 mg q48h Depending on the situation, 750 mg levofloxacin qd x5 days can be used (CAP, ABS) Pregnancy, pediatrics issues
Not approved for pediatric use; pregnancy category C Relative cost
Moderately priced
Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Inhibits bacterial growth by preventing formation of 70s initiation complex, which inhibits protein synthesis, Bacteriostatic. Spectrum (Gm+, Gm-, anaerobes)
Gram +: yes, including MRSA, PNSP, and VRE Gram -: not useful Anaerobes: some, not especially useful here DOC for which diseases
VRE In addition, linezolid is looking better and better for certain MRSA infections, especially pneumonia Absorption, distribution, metabolism,
Absorption: very good excretion
Metabolism: 2 major metabolites Excretion: mostly in urine ( 80%) PD (time vs. concentration dependent
Time-dependent killing killing)
Side effects (what, how common,
N/V, diarrhea, headache monitoring)
Reversible thrombocytopenia, anemia, neutropenia (the blood dyscrasias mainly occur in patients who receive >2 weeks of treatment) Allergies
Drug interactions
Weakly and reversibly inhibits monoamine oxidase (MAO); may interact with dietary tyramine and SSRIs (possible serotonin syndrome) Adrenergic agents: risk of hypertension Dose (renal/hepatic failure, obesity)
600 mg PO (or IV) BID X10-14d (adult) 10 mg/kg q8h (pediatric) Renal failure: no adjustment necessary Pregnancy, pediatrics issues
Pregnancy category C, safe in pediatrics Relative cost

Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
CIDAL, inhibition of cell wall synthesis; readily penetrates the cell wall of most Gm+ and Gm- bacteria to reach PBP targets Spectrum (Gm+, Gm-, anaerobes)
Good Gm+, good Gm-, Good anaerobic coverage No MRSA coverage, Pseudomonas YES In general, a bit more potent than imipenem for Gm- but a bit less potent than imipenem for Gm+ DOC for which diseases
HAP (empiric) Severe diverticulitis, perirectal abscess, peritonitis Sinusitis (hospitalized + intubation-related) Malignant otitis externa BOTTOM LINE: can be used for anything imipenem can be used for Absorption, distribution, metabolism,
Penetrates well into most tissues including CSF excretion
Largely eliminated unchanged in the urine Half-life 1 hour PD (time vs. concentration dependent killing) Time-dependent
Side effects (what, how common, monitoring)
Rash, thrombocytopenia, nausea/vomiting, diarrhea, headache (all less than imipenem) Allergies
Have occurred in patients with hypersensitivities to β lactam antibiotics (the pattern is assumed to be like imipenem) Drug interactions
Probenecid (inhibits renal excretion of meropenem) Oral contraceptives (the usual antibiotic-OC risk) Dose (renal/hepatic failure, obesity)
Normal dose is 0.5-1.0 gm IV q8h 2 gm IV q8h for meningitis Adjust in renal insufficiency Pregnancy, pediatrics issues
Pregnancy category B Lactation: unknown if excreted in breast milk (probably isn't) Relative cost
Comparable to imipenem
Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal; causes disruption of DNA helix and strand breakage leading to inhibition of protein synthesis and cell death Spectrum (Gm+, Gm-, anaerobes)
Anaerobes, protozoa, H. pylori. No activity against
aerobic bacteria.

DOC for which diseases
Trichomoniasis, C. difficile colitis, bacterial vaginosis, anaerobic infections Absorption, distribution, metabolism,
excretion
D-distributes to saliva, bile, seminal fluid, breast milk, bone, liver, lung and vaginal secretions, crosses placenta, and BBB. M-30-60% hepatic E-Half-life: 6-8 hr 20-40% excreted unchanged in urine; 6-15% in feces PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Nausea, vomiting, metallic taste Disulfiram reaction (alcohol) Allergies
Drug interactions
2C9 inhibitor--potential interactions with warfarin and phenytoin Dose (renal/hepatic failure, obesity)
500 mg PO tid x 10-14 days (C. difficile colitis) 2 g PO x 1 (Trichomonas) 500 mg po bid x 7 days (bacterial vaginosis) 500 mg IV q8h (serious anaerobic infection) Dose reduction recommended if CrCl <10 Pregnancy, pediatrics issues
Safe in pregnancy (B) Relative cost

Generic name
Proprietary name
Class (generation)
3rd generation fluoroquinolone MOA (bactericidal/bacteriostatic)
Bactericidal – inhibits topoisomerase II (DNA gyrase) and topoisomerase IV Attacking dual targets with roughly equal affinity may give moxifloxacin an advantage over levofloxacin in terms of causing resistance Bulky C-7 group helps to avoid bacterial efflux Spectrum (Gm+, Gm-, anaerobes)
Excellent gram-positive coverage Not as great gram-negative coverage Anaerobe coverage is good (unproven though) DOC for which diseases
Can be used in ABS if recent antibiotic use CAP patients with co-morbid conditions Absorption, distribution, metabolism,
90% bioavailability excretion
Absorbed in the gut Widely distributed throughout body Mainly eliminated by the liver (conjugation) PD (time vs. concentration dependent killing)
Concentration-dependent (AUC/MIC correlates best) Side effects (what, how common, monitoring)
Can prolong the QT interval (usually insignificant); has other typical FQ side effects; overall well tolerated Allergies
Drug interactions
Dose (renal/hepatic failure, obesity)
400 mg PO qd (no adjustment in renal insufficiency) Pregnancy, pediatrics issues
Pregnancy category C Not approved in pediatric patients Relative cost
More expensive compared to ciprofloxacin and levofloxacin
Generic name
Proprietary name
Class (generation)
Penicillinase-resistant penicillin MOA (bactericidal/bacteriostatic)
CIDAL. Penicillinase-resistant inhibitor of biosynthesis of mucopeptide (peptidoglycan). Most effective when bacteria are growing (subject to the inoculum effect) Spectrum (Gm+, Gm-, anaerobes)
Ok Gm+, but really no Gm- or anaerobic coverage (NO
MRSA)

DOC for which diseases
Osteomyelitis (MSSA) Brain abscess Mastoiditis (outpatient) Staphylococcal endocarditis (MSSA) Anything S. aureus that is MSSA Cellulitis, erysipelas Toxic shock syndrome Absorption, distribution, metabolism,
Distributes to most tissues readily where there is excretion
inflammation
Excretion: metabolized. NO ADJUSTMENT FOR
RENAL DYSFUNCTION.

PD (time vs. concentration dependent killing)
Time-dependent killing Side effects (what, how common, monitoring)
Fever, rash, neutropenia (monitor WBC); all relatively rare Allergies
Patients who are truly penicillin-allergic should be assumed nafcillin-allergic Drug interactions
Decreases the anticoagulant effect of warfarin (mechanism unclear; CYP3A induction suggested, although CYP3A catalyzes only a minor R-warfarin metabolic pathway) Dose (renal/hepatic failure, obesity)
Normal: 1-2 gm q4h IV, IM Renal failure: no reduction generally needed Hepatic failure: adjust empirically if dysfunction is severe Pregnancy, pediatrics issues
Pregnancy category B Excreted into breast milk in small quantities (not clinically significant) Relative cost

Generic name
Proprietary name
Macrobid, Macrodantin Class (generation)
Synthetic nitrofuran MOA (bactericidal/bacteriostatic)
Bactericidal at high conc, bacteriostatic at low conc. Inhibition of bacterial acetylcoenzyme A and subsequent disruption of the carbohydrate metabolism. Spectrum (Gm+, Gm-, anaerobes)
Gm+: S. aureus, Enterococcus
Gm-: E. coli; be careful, many Gram-negatives are
relatively resistant, e.g. Proteus, Enterobacter
,
Klebsiella

Anaerobes: no useful activity
DOC for which diseases
Alternative therapy for UTI (x7days) Occasionally used for longterm prophylaxis Absorption, distribution, metabolism,
Increased absorption with meal; highly protein bound excretion
and distributed throughout tissues; readily metabolized
in tissues, renally excreted. USE ONLY FOR
URINARY TRACT INFECTION!

PD (time vs. concentration dependent killing) Concentration-dependent killing
Side effects (what, how common, monitoring) N/V, pulmonary fibrosis, peripheral neuropathy,
pseudotumor cerebri, intrahepatic cholestasis, hepatitis, and hemolytic anemia in G6PD deficiency. When given long-term, monitor for pulmonary, hepatic, and neurologic toxicity. These toxicities aren't necessarily common, but nevertheless physicians like to avoid them by choosing other agents. Allergies
Drug interactions
Antacids can decrease the absorption of nitrofurantoin Dose (renal/hepatic failure, obesity)
Macrodantin: 100 mg q6h x 7 days
Macrobid: 100 mg bid x7 days
Longterm UTI prophylaxis: 50-100 mg po qd
Contraindicated in renal failure (CrCl <50)

Pregnancy, pediatrics issues
Pregnancy category B (but not for use in G6PD-deficient mothers) Relative cost
Macrodantin:100mg generic $1.21 Macrobid: 100mg generic $2.26
Generic name
Proprietary name
Class (generation)
Natural penicillin (susceptible to penicillinase) MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs. Spectrum (Gm+, Gm-, anaerobes)
Gram +: good for Streptococcus pyogenes (GABS) but not active against Staphylococcus (neither MSSA nor MRSA). PNSP prevalence about 40% in the US. Gram -: useful for nonpenicillinase-producing species of Neisseria Usually effective for above-diaphragm anaerobes but not for below-diaphragm anaerobes DOC for which diseases
Acute pharyngitis
ARF prophylaxis
Syphilis, neurosyphilis

Absorption, distribution, metabolism,
excretion
65% protein bound Crosses BBB if meninges are inflamed >80% excreted unchanged via kidneys Half-life: 30 minutes PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Diarrhea, serum sickness (rare) Allergies
Immediate allergy: anaphylaxis (rare) Accelerated: urticarial rash Late: maculopapular rash Drug interactions
Probenecid inhibits tubular secretion of penicillin which results in increased blood levels Dose (renal/hepatic failure, obesity)
Acute pharyngitis: Bicillin LA 0.6 or 1.2 million units x1, depending on patient weight Neurosyphilis: Pen G 3-4 MU IV q4h x10-14d Dose reduction in renal failure Pregnancy, pediatrics issues
Safe in pregnancy and pediatrics Relative cost
Pen G: 5MU about $5-6
Generic name
Proprietary name
Class (generation)
Natural penicillin (susceptible to penicillinase) MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis by binding to PBPs. Spectrum (Gm+, Gm-, anaerobes)
Gram +: good for Streptococcus pyogenes (GABS) but not active against Staphylococcus (neither MSSA nor MRSA). PNSP prevalence about 40% in the US. DOC for which diseases
Acute pharyngitis Absorption, distribution, metabolism,
excretion
65% protein bound >80% excreted unchanged via kidneys Half-life: 30 minutes PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Diarrhea, serum sickness (rare) Allergies
Immediate allergy: anaphylaxis (rare) Accelerated: urticarial rash Late: maculopapular rash Drug interactions
Probenecid inhibits tubular secretion of penicillin which results in increased blood levels Dose (renal/hepatic failure, obesity)
Acute pharyngitis: 250 mg PO bid or tid (25-50
mg/kg/day) x10d
Pregnancy, pediatrics issues
Safe in pregnancy and pediatrics Relative cost

Generic name
PIPERACILLIN/TAZOBACTAM Proprietary name
ß-lactam/ß-lactamase inhibitor MOA (bactericidal/bacteriostatic)
Bactericidal. Inhibits cell wall synthesis. Tazobactam is a β-lactamase inhibitor that inhibits some ß-lactamases (such as Bush class 2b enzymes, or the ESBLs) but NOT class 1 enzymes (from SPICE organisms) Spectrum (Gm+, Gm-, anaerobes)
Broad: gram (+) and (-) including Pseudomonas, plus anaerobes DOC for which diseases
CAP: with cipro for ICU pts at risk for Pseudomonas
HAP: combined with gentamicin
Secondary peritonitis (all by itself)
Osteomyelitis in diabetes
Absorption, distribution, metabolism,
Widely distributed throughout body excretion
Excreted mostly unchanged via kidneys Half-life of piperacillin: 1 hour PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
Drug fever, rash, diarrhea Allergies
Immediate allergy: anaphylaxis (rare) Accelerated: urticarial rash Late: maculopapular rash Drug interactions
Nothing significant Dose (renal/hepatic failure, obesity)
"Standard" dose: 3.375 g IV q6h (can also use 4.5 g
q8h). This dose is not reliable for Pseudomonas,
however, so be careful.
Reduce dose in renal failure
IMPORTANT: 16-18 grams/day of piperacillin
must be used whenever Pseudomonas
is a concern
(i.e. 3.375 g IV q4h or 4.5 gm IV q6h)

Pregnancy, pediatrics issues
Relative cost
$50 per day (standard dose)
Generic name
Proprietary name
PZA (abbreviation) Class (generation)
Antituberculous agent MOA (bactericidal/bacteriostatic)
Bactericidal in acid pH of macrophages Spectrum (Gm+, Gm-, anaerobes)
Mycobacterium tuberculosis
DOC for which diseases
Active TB, first line (only used in combination with other drugs) Absorption, distribution, metabolism,
A: almost completely absorbed from GI tract excretion
D: 5-10% protein bound, Vd 0.75-1.65 L/kg, distributes into CSF well M: 15-30% E: Renal 70% Half-life: 9 hours PD (time vs. concentration dependent killing)
Side effects (what, how common, monitoring)
N/V, Hyperuricemia, arthralgia (40%), severe liver
injury
Monitor LFTs, serum uric acid levels
Allergies
Not commonly reported Drug interactions
Not well defined Dose (renal/hepatic failure, obesity)
TB: 25-30 mg/kg/day Renal dosing: consider decreasing dose by 50% if CrCl less than 10 Pregnancy, pediatrics issues
Pregnancy category C, safe in pediatrics Relative cost

Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal drug Binds to bacterial DNA-dependent RNA polymerase Spectrum (Gm+, Gm-, anaerobes)
M. tuberculosis
Excellent for S. aureus (including MRSA) and S.
epidermidis
but only in combination with another
drug

DOC for which diseases
First line for TB PVE Chemoprophylaxis for N. meningitidis meningitis Absorption, distribution, metabolism,
A: 90-95% GI absorbed, delayed by food excretion
D: 60-90% protein bound, rapidly distributed into tissues, penetrate abscesses and CSF (if inflamed) Vd: 0.9 L/kg M: Liver 60-80%, enterohepatic circulation E: Renal 15-30%, Bile, Feces 60% PD (time vs. concentration dependent killing) Not established
Side effects (what, how common, monitoring)
GI upset is common, colors body fluids orange; routinely causes hyperbilirubinemia (usually transient); hemolytic anemia, renal failure, thrombocytopenia (1%) especially in patients who receive intermittent therapy (get baseline CBC, liver enzymes, SCr) Allergies
Drug interactions
Makes oral contraceptives unreliable
Potent inducer of CYP 1A2, 2C9, 2C19, 3A4

Dose (renal/hepatic failure, obesity)
TB dose: 10 mg/kg/day (maximum 600 mg qd) Meningococcus prophylaxis: 600 mg PO bid x2 days PVE: 300 mg PO q8h Adjunct drug for S. aureus: 300 mg PO q8-12h Renal: consider a dosage change if CrCl <50 Hepatic: decrease dose if severe dysfunction Pregnancy, pediatrics issues
Pregnancy category C, ok in pediatrics Relative cost

Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bacteriostatic; binds to 2 sites on 23S ribosome (macrolides bind to only one); also avoids drug efflux Spectrum (Gm+, Gm-, anaerobes)
G+: especially good for drug resistant S. pneumoniae, S
pyogenes

G-: M cat and H flu
Unreliable for MRSA
Not good for anaerobes
SUMMARY: the "best" of azithro plus the "best" of
clarithro rolled into one drug, with the added
advantage of covering drug-resistant S. pneumoniae

DOC for which diseases
Indicated for CAP, AECB, sinusitis Absorption, distribution, metabolism,
A: oral 57% bioavailability, unaffected by food excretion
D: 60-70% protein bound, penetrates lung tissues well, Vd=2.9 L/kg M: 37% in liver (50% CYP metabolized) E: 75% feces, Renal 12-14%. Half-life 10 hours. PD (time vs. concentration dependent killing) Concentration dependent, prolonged post antibiotic
Side effects (what, how common, monitoring)
Diarrhea (10%), nausea (7%), headache (5%), dizziness
(4%), vomiting (3%)
Liver dysfunction (rare)
Visual disturbances can be serious
Allergies
Hypersensitivity to ketolide or macrolide antibiotics Drug interactions
Competitive inhibitor of CYP 3A4 and 2D6 Dose (renal/hepatic failure, obesity)
Usual: 800 mg PO qd x5 days (7-10 days for CAP) Renal dosing: 400 mg PO qd if CrCl <30 Pregnancy, pediatrics issues
Pregnancy category C Pediatrics safety not yet established (no suspension form available) Relative cost
Expensive, overpriced (at least initially)
Generic name
Proprietary name
Class (generation)
Glycylcycline (derived from minocycline) MOA (bactericidal/bacteriostatic)
Bacteriostatic: inhibits protein translation by binding to the 30S ribosomal subunit Spectrum (Gm+, Gm-, anaerobes)
Most Gm+ (including MRSA, VRE, PNSP)
Many Gm- (not Proteus spp. or Pseudomonas)
Anaerobes: pretty good below-the-diaphragm
Tigecycline is not affected by the 2 major tetracycline
resistance mechanisms: ribosomal protection and efflux
DOC for which diseases
Alternative treatment for complicated skin and skin
structure infections as well as intraabdominal infections
Absorption, distribution, metabolism,
Metabolism / Excretion: not extensively metabolized. excretion
59% of the dose is eliminated by biliary/fecal excretion, and 33% is excreted in urine. Approximately 22% of the total dose is excreted as unchanged tigecycline in urine. Half-life LONG: 30-36 hours. PD (time vs. concentration dependent killing)
Concentration-dependent (AUC/MIC) Side effects (what, how common, monitoring)
Significant nausea, vomiting and diarrhea.

Tooth discoloration: the use of tigecycline during tooth
development (last half of pregnancy, infancy, and
childhood until the age of 8 years) may cause
permanent discoloration of the teeth (yellow-gray-
brown).
Allergies
Drug interactions
May decrease warfarin clearance (significance unclear) Dose (renal/hepatic failure, obesity)
100 mg IV x1, then 50 mg IV q12 hours (x10-14 days) NO adjustment in renal dysfunction In severe hepatic impairment, the initial dose of tigecycline should be 100 mg, then 25 gm IV q12h Pregnancy, pediatrics issues
Pregnancy Category D; safety in pediatrics has not been established Relative cost
About $90/day (similar to linezolid)
Generic name
TRIMETHOPRIM/SULFAMETHOXAZOLE (TMP/SMX) Proprietary name
Class (generation)
Sulfonamide plus DHFR inhibitor MOA (bactericidal/bacteriostatic)
Bacteriostatic: SMX inhibits dihydropteroate synthetase, TMP inhibits dihydrofolate reductase Spectrum (Gm+, Gm-, anaerobes)
Gm+: good for CA-MRSA, but usually does not work for PNSP and does not cover Enterococcus, S. epidermidis, or GABS Gm-: generally effective for enteric GNR, H. influenzae; does not cover Pseudomonas Anaerobes: inactive DOC for which diseases
UTI (unless E. coli resistance is >20%) SBP prophylaxis PCP in AIDS patients Absorption, distribution, metabolism,
Absorption: 90-100% excretion
Vd: TMP 2.0 L/kg; SMX 360 mL/kg; penetrates CSF Half-life: 10-12 hr (each component) Metabolism: extensive liver metabolism Renal excretion: SMX 10-30%; TMP 50-75% PD (time- or concentration-dependent
killing)
Side effects (what, how common,
10% of patients: N/V/GI upset; skin problems (rash, monitoring)
urticaria, photosensitivity); hyperkalemia Less common: Stevens-Johnson syndrome, toxic epidermal necrolysis. Can cause blood dyscrasias, especially in AIDS patients. Commonly suspected cause of aseptic meningitis. Allergies
Sulfonamide allergy is common Drug interactions
SMX is a CYP2C9 inhibitor Dose (renal/hepatic failure, obesity)
UTI: 1 DS tablet BID PCP: 5 mg/kg q6-8h (based on TMP component) Reduce dose by 50% if CrCl <50 ml/min Pregnancy, pediatrics issues
Pregnancy category C but do not use near term; safe for use in pediatrics but do not use in children < 2 months old due to possibility of kernicterus Relative cost
Very inexpensive
Generic name
Proprietary name
Class (generation)
MOA (bactericidal/bacteriostatic)
Bactericidal: inhibits cell wall synthesis by binding to D-ala-D-ala dipeptides Spectrum (Gm+, Gm-, anaerobes)
Gm+: active against most genera (should be combined with an aminoglycoside to treat E. faecalis) No Gm- activity Anaerobic activity: C. difficile (oral only) DOC for which diseases
MRSA infections Bacterial meningitis (combined with ceftriaxone) Vascular catheter infections due to S. epidermidis Endocarditis (second line) Antibiotic-associated diarrhea (second line) Absorption, distribution, metabolism,
A: not orally absorbed excretion
D: wide, including CSF if meninges are inflamed; Vd 0.7 L/kg M: not metabolized E: excreted unchanged in the urine (half-life 6 hours) PD (time vs. concentration dependent killing) Time-dependent killing
Side effects (what, how common, monitoring) Rapid infusion can cause "red man syndrome" (flushed
skin, edema) Neutropenia (rare) Rash (rare) Ototoxicity and nephrotoxicity (rare) Allergies
Not a particular issue with this drug Drug interactions
Increased frequency of nephrotoxicity with aminoglycosides Dose (renal/hepatic failure, obesity)
Normal dose: 1 gm IV q12h Obesity: daily dose correlates with actual body weight Renal dysfunction: increase dosing interval as CrCl decreases Pregnancy, pediatrics issues
Pregnancy category C, safe to use in pediatrics Relative cost
Somewhat expensive

Source: http://students.washington.edu/rhochi/antibiotics.pdf

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Microsoft word - aml17 may 08 adult - very latest - without track changes4.doc

WORKING PARTIES ON LEUKAEMIA IN ADULTS AND CHILDREN TRIAL IN ACUTE MYELOID LEUKAEMIA OR HIGH RISK MYELODYS PLASTIC SYNDROME 17 PROTOCOL FOR PATIENTS AGED 18 to 60 (Trial Reference ISRCTN55675535) Through the use of a risk based approach AML17 will evaluate several relevant therapeutic questions in acute myeloid leukaemia (AML) as defined by WHO, and high risk Myelodysplastic Syndrome. The trial is open to all patients aged 18 to 60 years, and also to patients aged 60 years or over for whom intensive therapy is considered appropriate. At least 2800 patients will be recruited. For patients who do not have the Acute Promyelocytic Leukaemia (APL) subtype, an induction randomisation will compare two courses of the standard ADE with ADE or DA each in combination with one of two doses of the immunoconjugate Mylotarg in course 1 (five options). Consolidation will compare one course with two courses (MACE/Midac versus MACE).