-
What is the MOA of beta-lactams?
- bactericidal
- bind to penicillin-binding proteins (PBP)
- inhibit cell wall synthesis
-
What Penicillins are given IV?
- Pen G
- Nafcillin
- Oxacillin
- Ampicillin (also oral)
- Ticarcillin
- Piperacillin
- Unasyn (Amp/sulbactam)
- Timentin (Ticarcillin/clavulanate)
- Zosyn (Pip/tazobactam)
-
What Penicillins are given PO?
- Pen VK
- Dicloxacillin
- Amoxicillin
- Ampicillin (IV also)
- Carbenicillin (only used for UTIs)
- Augmentin (Amox/clavulanate)
-
What Penicillins are given IM?
- benzathine Pen G
- Procaine Pen G
- Pen G benzathing + Pen G procaine
-
What are the natural penicillins?
- Pen G (and all variations)
- Pen VK
-
What are the penicillinase-resistant antistaphylococcal penicillins?
- methicillin
- nafcillin
- oxacillin
- dicloxacillin
-
What are the extended-spectrum aminopenicillins?
-
What are the extended-spectrum antipseudomonal penicillins?
- carbenicillin
- ticarcillin
- piperacillin
-
What are the beta-lactam/beta-lactamase inhibitor combinations?
- Augmentin (amoxicillin clavulanate)
- Unasyn (ampicillin sulbactam)
- Timentin (ticarcillin clavulanate)
- Zosyn (piperacillin tazobactam)
-
How are beta-lactam/beta-lactamase inhibitors formulated?
- amount of beta-lactam changes as dose increases
- amount of beta-lactamase is constant
- 2x250 does not equal 1x500, the inhibitor concentration would be too high = more SE
-
How are Penicillins eliminated?
- renally: glomerular filtration and active tubular secretion
- Oxacillin (renal and bile)
- Navcillin (bile)
-
What type of killing do Penicillins posess?
time-dependent killing
-
What are the SE of Penicillins?
- NVD (infectious and non-infectious D)
- hypersensitivity
- anemia
- decreased platelets
- increased INR
- acute interstitial nephritis (methicillin, nafcillin)
- excess sodium load (ticarcillin worst)
- excess potassium load (Pen G)
- superinfection
-
What pregnancy class are Penicillins?
-
What are the DI of Penicillins?
- oral contraceptives (use condoms for 1 wk after antibiotics)
- warfarin (increased INR d/t loss of gut flora)
-
How are cephalosporins dosed?
-
Which cephalosporins are dosed PO?
- cephalexin
- cefadroxil
- cefaclor
- cefuroxime axetil
- cefprozil
- cefixime
- cefpodoxime proxetil
- ceftibuten
- cefdinir
- cefditoren pivoxil
-
What cephalosporins are 1st generation?
- cefazolin
- cephalexin
- cefadroxil
-
What cephalosporins are 2nd generation?
- cefoxitin
- cefuroxime
- cefotetan
- cefaclor
- cefuroxime axetil
- cefprozil
-
What cephalosporins are 3rd generation?
- cefotaxime
- cefoperazone
- ceftizoxime
- ceftriaxone
- ceftazidime
- cefixime
- cefpodoxime proxetil
- ceftibuten
- cefdinir
- cefditoren pivoxil
-
What cephalosporins are 4th generation?
- cefepime
- ceftaroline fosamil
-
Which cephalosporins are good for anaerobes?
-
Which cephalosporins are good for pseudomonas?
-
Which cephalosporins are good for MRSA, MRSE, and enterococcus
ceftaroline fosamil
-
Which cephalosporin is best for use in neonates?
cefotaxime
-
How are cephalosporins eliminated?
- mostly renal: glomerular filtration and active tubular secretion)
- cefoperazone (bile 70%)
- ceftriaxone (bile 30-40%)
-
How well do cephs penetrate the CNS?
- cefuroxime
- cefotaxime
- ceftriaxone
- ceftizoxime
- ceftazidime
-
How protein bound are cephs?
ceftriaxone is concentration dependent: increasing dose increases fraction unbound, so higher doses and longer interval is better
-
What are the SE of cephs?
- hypersensitivity
- increased INR in cephs that have MTT side-chain (cefoperazone)
- NVD
- disulfiram rxn in cephs with MTT side-chain
- HA
- dizziness
- neurotoxicity (high dose in renal impaired)
- bilirubin encephalopathy (ceftriaxone - highly PPB)
-
Which ceph should not be used in neonates?
ceftriaxone displaces bilirubin
-
What are the DI of cephs?
do not administer ceftriaxone with calcium-containing IV fluids in neonates (increased risk of precipitation)
-
Which b-lactam is the only one that is monocyclic instead of bicyclic?
aztreonam
-
How is aztreonam delivered?
IV
-
What type of beta-lactam is aztreonam?
a monobactam
-
How is aztreonam eliminated?
renally
-
What are the SE of aztreonam?
- NVD
- hypersensitivity: not much cross-reactivity with beta-lactams (safe in PCN allergy)
-
Which type of PCN hypersensitivity is IgE mediated?
immediate (< 72h) (type I)
-
Which type of PCN hypersensitivity is not IgE mediated?
late ( > 72h) (type II, III, or IV)
-
What is the risk of cross-reactivity between cephalosporins/carbapenems and penicillin?
about 10%
-
What drugs are carbapenems?
- imipenem/cilastatin (Primaxin)
- meropenem
- ertapenem
- doripenem
-
How are carbapenems delivered?
IV
-
Which carbapenem is used for pediatric menengitis?
meropenem
-
How are carbapenems eliminated?
renally
-
How do carbapenems penetrate the CNS?
- well
- imipenem not used for meningitis d/t risk of neurotoxicity
-
What are the SE of carbapenems?
- NVD
- phlebitis
- HA
- confusion
- seizures (highest with imipenem - no meningitis)
- hypersensitivity (cross reactive with PCN and ceph)
- nephrotoxicity (imipenem worse than meropenem)
-
What pregnancy class are carbapenems?
class B (imipenem is C)
-
What are the DI of carbapenems?
VPA levels reduced by meropenem
-
What drugs are aminoglycosides?
- gentamicin
- tobramycin
- amikacin
- streptomycin (TB only)
- neomycin (hepatic coma, bowel cleansing)
-
What is the MOA of AGs?
- bactericidal
- inhibits protein synthesis by binding 30s subunit of bacterial ribosomes
-
What type of killing do AGs have?
concentration dependent killing
-
How well are AGs absorbed PO?
poorly
-
How well do AGs penetrate the CNS?
poorly
-
How are AGs eliminated?
glomerular filtration
-
What are the SE of the AGs?
- neprhotoxicity (proximal tubule selective)(Black-box Warning)
- ototoxicity (cochlear and vestibular)
- neuromuscular blockade (rare)
- hypersensitivity (rare)
-
What pregnancy class are AGs?
D (teratogenic: ototoxicity)
-
What are the DI of AGs?
- loops (increased otoxicity - increase monitoring)
- neuromuscular blockers
- other nephrotoxic drugs (increase monitoring)
-
What drugs are fluoroquinolones?
- norfloxacin
- ciprofloxacin
- ofloxacin
- levofloxacin
- moxifloxacin
- gemifloxacin
-
-
Which FQs can only be given orally?
-
What is the MOA of the FQs?
- inhibit DNA gyrase (Topo II)
- bactericidal
- some inhibit Topo IV
-
Which FQs inhibit Topo IV?
-
Which FQ are second generation?
- norfloxacin
- ciprofloxacin
- ofloxacillin
-
Which FQ are third generation?
levofloxacin
-
Which FQ are fourth generation?
-
Which FQ have better systemic absorption?
second generation
-
Which FQ have better gram-negative activity?
2nd generation
-
Which FQ is used for UTIs and GI infections only?
norfloxacin
-
Which FQ are better for gram-positive, atypical, and/or anaerobic activity?
4th generation
-
How do serum concentrations compare between IV and PO FQ?
they are equal except for ciprofloxacin (80% PO)
-
What type of elimination do FQ have?
- renal
- moxifloxacin (hepatic)
-
What type of killing to FQ have?
concentration-dependent killing
-
What are the SE of the FQ?
- NVD (including infectious D)
- dizziness
- HA
- somnolence
- confusion
- seizures (rare)
- rash (gemifloxacin - limit to 7d)
- photosensitivity
- crystalluria
- cartilage malformations
- tendonitis/rupture
- QT prolongation
- dysglycemia (esp with diabetes)
-
What pregnancy class are FQ?
- class C
- no nursing or pediatric patients either
-
What are the DI of FQ?
- CYP1A2 inhibition (cipro, oflox, norflox) affects R isomer of warfarin (least active)
- decreased absorption with multivalent cations (separate by at least 4h)
- decreased absorption with calcium and dairy (separate by at least 2h)
- antiarrhythmics (qt prolongation)
- sulfonylureas (dysglycemia)
-
What type of drug is vancomycin?
glycopeptide
-
How is vancomycin delivered?
-
What is vancomycin's MOA?
- inhibits bacterial cell wall synthesis
- bacteriostatic and bactericidal
-
How well does vanco penetrate the CNS?
erratically
-
How is vanco eliminated?
- IV: glomerular filtration
- PO: feces
-
What type of killing does vanco exhibit?
time-dependent killing
-
What is the goal trough level for vanco?
10-20 mcg/ml
-
What are the SE of vanco?
- red man's syndrome
- nephrotoxicity
- ototoxicity
-
What pregnancy class is vanco?
class C
-
What are the DI of vanco?
other nephrotoxic or ototoxic drugs
-
Which drugs are macrolides?
- azithromycin
- clarithromycin
- erythromycin
-
What is the MOA for macrolides?
- inhibit protein synthesis
- bind 50s ribosomal subunit
- bacteriostatic
-
How are macrolides delivered?
-
Which macrolide can only be given PO?
clarithromycin
-
What infections are the macrolides the DOC for?
- CAP
- MAC (clarith)
- H. Pylori (Clarith)
-
How is azithromycin distributed?
gets into tissues very well, so low serum concentration (not good for bacteremia)
-
How well do macrolides penetrate the CNS?
not well
-
How are the macrolides metabolized?
Erythromycin is metabolized by 3A4
-
What are the SE of macrolides?
- NVD (take with meals)
- rash
- HA
- QT prolongation
- cholestatic hepatitis
-
What pregnancy class are the macrolides?
class B (clarith is C)
-
What are the DI of macrolides?
- inhibit 1A2 and 3A4 (eryth and clarith)
- antiarrhythmics
-
What kind of drug is telithromycin?
a ketolide
-
What is the MOA of telithromycin?
- inhibit protein synthesis
- bind 50s ribosomal subunit
- bacteriostatic
-
How is telithromycin delivered?
PO
-
What are the SE of telithromycin?
- diarrhea
- hepatotoxicity
- QT prolongation
-
What pregnancy class is telithromycin?
class C
-
What is the black-box warning associated with telithromycin?
respiratory failure in pts with myasthenia gravis
-
What are the DI of telithromycin?
substrate and inhibits 3A4
-
What is the MOA of the TCNs?
- inhibit protein synthesis
- bind 30 ribosomal subunit
- bacteriostatic
-
What are the names of the TCNs?
- tetracycline
- demeclocycline
- doxycycline
- minocycline
-
How are the TCNs delivered?
-
Which TCN can be delivered IV?
doxycycline
-
What are TCNs used for?
- DOC for Rickettsial infections, chlamydia, and Lyme disease
- Acne vulgaris
- CAP pts on antiarrhythmics
-
How are TCNs eliminated?
renal and hepatic
-
Which TCN can be used in renal impairment?
doxycycline
-
What are the SE of TCNs?
- discoloration of bone/teeth
- NVD
- esophogeal ulceration
- photosensitivity
- hepatotoxicity
- renal toxicity
- vertigo (minocycline)
- hypersensitivity (rare)
-
What are the DI of TCNs?
- food
- multivalent cations (except minocycline and doxycycline)
-
What type of drug is tigecycline?
a glycylcycline
-
What is the MOA of tigecycline?
- inhibit protein synthesis
- bind 30s ribosomal subunit
-
How is tigecycline delivered?
IV
-
What pregnancy class is tigecycline?
D
-
What are the SE of tigecycline?
- NVD
- inj site reactions
- discoloration of teeth in peds
- hypersensitivity if allergic to TCNs
-
Which drugs are sulfonamides?
- sulfasalazine
- sulfadiazine
- sulfisoxazole
-
How are sulfonamides delivered?
PO
-
What is the MOA for sulfonamides?
- antagonize PABA synthesis
- bacteriostatic
-
What is the use for sulfonamides?
uncomplicated UTI
-
What are the SE of sulfonamides?
- hypersensitivity
- photosensitivity
- bone marrow suppression
- kernicterus
-
What pregnancy class are sulfonamides?
class B (except D in 3rd trimester)
-
What are the DI of sulfonamides?
significant increase in INR d/t 2C9 inhibition (S isomer of warfarin) (monitor q 2-3d)
-
What is the MOA of trimethoprim?
- inhibits the enzyme dihydrofolate reductase (DHFR)
- bacteriostatic
-
What is trimethoprim used for?
UTIs
-
How is bactrim dosed?
weight-based dosing based on trimethoprim component
-
What is the absorption of bactrim?
give tmp/smx as a ratio of 1:5 to achieve serum concentrations of 1:20 (synergism)
-
What are the SE of bactrim?
- bone marrow suppression
- hypersensitivity
- kernicterus
-
What pregnancy class is bactrim?
class C (D in 3rd trimester)
-
What are the DI of bactrim?
2C9 inhibition - increase INR (warfarin S isomer) (monitor q 2-3d)
-
What drugs are lincosamides?
-
What is the MOA for lincosamides?
- inhibit protein synthesis
- bacteriostatic
-
What are lincosamides used for?
gram-positive or anaerobic skin infections or pneumonia
-
What are the SE for lincosamides?
black-box warning for clindamycin causing colitis (C. diff associated diarrhea - CDAD) (treat with metronidazole)
-
What pregnancy class are lincosamides?
class B
-
What is the MOA of metronidazole?
- toxic to bacterial DNA and RNA
- bactericidal
-
What is metronidazole used for?
- anaerobes
- protozoa
- CDAD (C.diff associated diarrhea)
-
What type of killing does metronidazole have?
concentration-dependent killing
-
What are the SE of metronidazole?
- furry tongue
- metallic taste
- urine discoloration (red-brown)
- peripheral neuropathy
- carcinogenic (Black-box warning)
-
What pregnancy class is metronidazole?
class B (D in first trimester)
-
What are the DI of metronidazole?
- alcohol (disulfuram rxn)
- 2C9 inhibitor increases INR
-
What is the MOA of tinidazole?
- toxic to bacterial DNA and RNA
- bactericidal
-
How is tinidazole delivered?
PO with food
-
What is tinidazole used for?
-
What are the SE of tinidazole?
- NVA
- bitter taste
- carcinogenic (black-box)
-
What pregnancy class is tinidazole?
class C
-
What are the DI of tinidazole?
- alcohol - disulfuram rxns
- 3A4 substrate
-
What is the MOA of rifampin?
- inhibits DNA-dependent RNA polymerase
- bactericidal
-
What is rifampin used for?
- Tx and prophylaxis of TB
- Tx of asymptomatic carriers of N. meningitidis
- in combo with PCN or vanco for endocarditis or osteomyelitis (synergy)
-
What are the SE of rifampin?
- flu-like syndrome
- reddish-orange excretions
-
What pregnancy class is rifampin?
class C
-
What are the DI of rifampin?
1A2, 2C9, 2C10, 3A4 inducer
-
What is the MOA of rifaximin?
- inhibits DNA-dependent RNA polymerase
- bactericidal
- non-systemic
-
What is rifaximin used for?
traveler's diarrhea (E. coli)
-
What pregnancy class is rifaximin?
class C
-
What are the DI of rifaximin?
none clinically
-
What is the MOA of nitrofurantoin?
- inhibits acetyl CoA to inhibit carb metabolism
- also inhibits cell wall synthesis
- bacteriostatic at low dose
- bactericidal at high dose
-
What is nitrofurantoin used for?
UTIs
-
What are the SE of nitrofurantoin?
- discolors urine brown
- pulmonary toxicity
-
What pregnancy class is nitrofurantoin?
class B
-
What is the MOA of chloramphenicol?
- inhibits protein synthesis
- bacteriostatic
-
What is chloramphenicol used for?
serious infections for which potentially dangerous drugs are ineffective or contraindicated when caused by susceptible strains, especially meningitis or brain abscess
-
How well does chloramphenicol penetrate the CNS?
very well
-
What are the goals for chloramphenicol concentrations?
- peak: 15-25 mcg/ml
- trough: 5-15 mcg/ml
- monitor CBC q 2-3d
-
What are the SE of chloramphenicol?
- bone marrow suppression (black box)
- monitor q 2-3d
-
What drugs are the streptogramins?
quinupristin/dalfopristin (synercid)
-
What is the MOA of synercid?
inhibit protein synthesis
-
How is synercid delivered?
IV
-
What is synercid used for?
- serious gram-positive aerobic infections
- reserved for vanco-resistant
-
What are the SE of synercid?
infusion-site rxns
-
What pregnancy class is synercid?
class B
-
What are the DI of synercid?
3A4 inhibitor
-
What drug is an oxazolidinone?
linezolid
-
What is the MOA of linezolid?
- inhibit protein synthesis
- bacteriostatic
-
What kind of killing does linezolid have?
time-dependent killing
-
How is linezolid delivered?
-
What is linezolid used for?
serious gram-positive aerobic infections only
-
What are the SE of linezolid?
thrombocytopenia (rare) (monitor CBC weekly if on longer than 2 wks)
-
What pregnancy class is linezolid?
class C
-
What are the DI of linezolid?
inhibits MAO
-
What kind of drug is daptomycin?
a cyclic lipopeptide
-
What is the MOA of daptomycin?
inhibits DNA/RNA/protein synthesis
-
What type of killing does daptomycin have?
concentration-dependent killing
-
How is daptomycin delivered?
IV
-
What is daptomycin used for?
- gram-positive aerobes including MRSA and VRE
- skin infections
- bacteremia (not pneumonia)
-
What is an advantage of daptomycin?
low resistance potential
-
What are the SE of daptomycin?
can increase CPK at high doses (monitor weekly)
-
What pregnancy class is daptomycin?
class B
-
What are the DI of daptomycin?
consider d/c statins while on daptomycin to decrease risk of myopathy
-
What should patients be counseled on for antibiotics?
- what the medication is and what it is for
- how to take it
- when to expect symptom improvement
- need for compliance
- SE
- DI (esp. OC)
-
How should antibiotic efficacy be monitored?
- sx resolution
- temp
- WBC
- compliance
- serum drug concentrations
- other tests (x-rays, TEE, lumbar puncture, bone scan, etc)
-
how should antibiotic safety be monitored?
- SE
- DI
- CI
- serum drug concentrations
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