Term
| Beta Lactams (general MOA) |
|
Definition
| Bind to penicillin binding proteins (PBPs, transpeptidases and carboxypeptidases) in cytoplasmic membrane that inhibit cross-linking of cell wall |
|
|
Term
| Gram + Cell Wall (crosslink?) |
|
Definition
| Link via peptide between lys and D-ala |
|
|
Term
| Gram - Cell Wall (crosslink?) |
|
Definition
| Link between diaminopimelic acid (DAP) and D-ala |
|
|
Term
| Beta Lactams (general MOR) |
|
Definition
| Drug inactivation by beta-lactamases, altered PBP, decreased permeability |
|
|
Term
| Penicillin G (indications) |
|
Definition
- aerobic gram + cocci -> strep, non-penicillinase S. aureus, susc. S. pneum
- some gram - cocci -> N. mening., many N. gonorr. are R
- anaerobic gram + and gram - cocci -> mouth flora, actinomyces
-clostridia
- all stages of SYPHILIS |
|
|
Term
| Penicillin G (not used for) |
|
Definition
|
|
Term
| Penicillin G (absorption) |
|
Definition
| acid labile -> NO oral formulation |
|
|
Term
| Penicillin G (good distribution via IV?) |
|
Definition
- well distributed to lung, liver, kidney, muscle, bone
- useful CSF conc. when inflammation present |
|
|
Term
| Penicillin G (poor distribution via IV?) |
|
Definition
| low IC levels, and poor distribution to eye, prostate, brain when inflammation present |
|
|
Term
| Penicillin G (distribution via IM) |
|
Definition
- procaine penicillin G -> repository in serum and tissue for 12 hours
- benzathine penicillin G -> repository in serum and tissue for 15-30 days |
|
|
Term
| Penicillin G (elimination) |
|
Definition
| renual tubular cells primarily |
|
|
Term
|
Definition
| similar to Pen G, less active vs. Haemophilus, Neisseria, enterics |
|
|
Term
| Penicillin V (indications) |
|
Definition
| Mild oral infections (abscesses) , pharyngitis (Strep), skin infections (cellulitis) |
|
|
Term
| Penicillin V (formulation) |
|
Definition
|
|
Term
| Penicillin V (absorption/distribution) |
|
Definition
| low serum levels vs. IV Pen G |
|
|
Term
| Penicillin V (elimination) |
|
Definition
|
|
Term
| Penicillinase-resistant penicillins (new class benefits?) |
|
Definition
| combat penicillinase producing staph |
|
|
Term
| Penicillinase-resistant penicillins (spectrum) |
|
Definition
|
|
Term
| Penicillinase-resistant penicillins (spectrum exceptions) |
|
Definition
| L. monocytogenes, enterococcus spp., MRSA -> R due to low affinity PBP 2a |
|
|
Term
| Penicillinase-resistant penicillins (elimination) |
|
Definition
| Nafcillin (liver) and dicloxacillin (renal) |
|
|
Term
| Penicillinase-resistant penicillins (indications) |
|
Definition
| Nafcillin for severe penicillinase S. aureus (not MRSA) and dicloxacillin for mild staph SSTIs |
|
|
Term
| Aminopenicillins (new class benefits?) |
|
Definition
| increased perm. = enhanced gram - activity |
|
|
Term
| Aminopenicillins (spectrum) |
|
Definition
- gram + -> similar to Pen G; worse against strep but better against L. monocytogenes and enterococci
- gram (-) -> originally active vs. N. gonor., H. flu, E. coli, Salmonella spp., and Shig., but high frequency of beta lactamase makes unreliable |
|
|
Term
| Aminopenicillins (pharmacokinetics/dynamics) |
|
Definition
| Distribution similar to pen G; amox. taken orally; amp. given IV |
|
|
Term
| Aminopenicillins (elimination) |
|
Definition
|
|
Term
| Aminopenicillins (side effect) |
|
Definition
| MACULOPAPULAR RASH in infectious mono cases, CLL patients, and patients taking allopurinol |
|
|
Term
| Aminopenicillins (indications) |
|
Definition
- Amp. IV used for serious enterococcus and L. monocytogenes; for enterococcus, given with aminoglycoside for synergy
- Amox. PO used for sinusitis, otitis, bronchitis, mild CA pneumonia |
|
|
Term
| Carboxy/ureidopenicillins (new class benefits?) |
|
Definition
| developed for better gram - activity (i.e. Pseudomonas) |
|
|
Term
| Carboxy/ureidopenicillins (main drugs used) |
|
Definition
- Ticarcillin is only carboxy used and in conjunction with beta lactamase inhibitor
- Ureidos have lower sodium load and mezlocillin and piperacillin are main drugs used |
|
|
Term
| Carboxy/ureidopenicillins (Piperacillin spectrum) |
|
Definition
- aerobic gram + -> similar to amp vs. enterococci
- aerobic gram (-) -> better than other penicillins; good vs. Neisseria, Haemophilus, many enterobacteriaciae and most active penicillin vs. Pseudomonas
- anaerobes -> beta lactamase production makes pip inferior to drugs like clindamycin or metronidazole |
|
|
Term
| Carboxy/ureidopenicillins (Piperacillin absorption) |
|
Definition
|
|
Term
| Carboxy/ureidopenicillins (Piperacillin synergy) |
|
Definition
| Synergy seen w/ aminoglycosides vs. Pseudomonas, enterococcus, and enterobacteriaciae |
|
|
Term
| Carboxy/ureidopenicillins (Piperacillin distribution) |
|
Definition
| Distribution similar other penicillins |
|
|
Term
| Carboxy/ureidopenicillins (Piperacillin elimination) |
|
Definition
| Excreted via glomerular filtration and tubular secretion |
|
|
Term
| Carboxy/ureidopenicillins (Piperacillin indications) |
|
Definition
| Major indication is for serious gram - infections |
|
|
Term
| General penicillins (side effects) |
|
Definition
- Pen G -> anaphylaxis/early urticaria, hemolytic anemia, serum sickness, DTH/contact dermatitis, acute hyperkalemia, SEIZURES
- Amp -> skin rash, fever, late urticaria, diarrhea, enterocolitis
- Meth -> INTERSTITIAL NEPHRITIS
- Ticarcillin -> platelet dysfunction, sodium overload
- INCREASE IN TRANSAMINASE -> nafcillin, oxacillin
- Neutropenia -> PenG, nafcillin, oxacillin, piperacillin |
|
|
Term
| Beta-lactamase inhibitors (drugs in use) |
|
Definition
| clavulanic acid, sulbactam, tazobactam |
|
|
Term
| Beta-lactamase inhibitors (spectrum) |
|
Definition
| inhibits s. aureus, most gram - (plasmid mediated), and anaerobic penicillinases |
|
|
Term
| Beta-lactamase inhibitors (ineffective against?) |
|
Definition
| chromosomal beta lactamases of enterobacter, citrobacter, serratia, and PSEUDOMONAS due to consititutive expression; orgs using diff. resistance mech |
|
|
Term
| Penicillin + Beta-lactamase inhibitors (Ticarcillin/clavulanate = Timentin indication) |
|
Definition
| polymicrobial infections and Stenotrophomonas maltophila |
|
|
Term
| Penicillin + Beta-lactamase inhibitors (Amoxicillin/clavulanate = Augmentin indication) |
|
Definition
| oral combo only; EXCELLENT FOR HUMAN AND ANIMAL BITES; otitis, sinusitis, lower RT inf, UTI, SSTI |
|
|
Term
| Penicillin + Beta-lactamase inhibitors (Ampicillin/sulbactam = Unasyn indication) |
|
Definition
| Similar to Timentin but no intrinsic Pseudomonas |
|
|
Term
| Penicillin + Beta-lactamase inhibitors (Piperacillin/tazobacta = Zosyn indication) |
|
Definition
| polymicrobial infections and Stenotrophomonas maltophila; greater potency than Timentin bc piperacillin more active than ticarcillin |
|
|
Term
| Cefazolin (1st gen ceph; spectrum) |
|
Definition
| pen'ase + S. aureus (not MRSA), streptococci |
|
|
Term
| Cefazolin (1st gen ceph; formulation) |
|
Definition
|
|
Term
| Cefazolin (1st gen ceph; elimination) |
|
Definition
| kidneys (same as most cephs except ceftriaxone and cefoperazone) |
|
|
Term
| Cefazolin (1st gen ceph; distribution) |
|
Definition
| excellent to tissue and fluid compartments except CSF |
|
|
Term
| Cefazolin (1st gen ceph; indications) |
|
Definition
| SSTIs (but inferior to Naf for serious Staph aureus), first choice for SURGICAL PROPHYLAXIS (except bowel or appendix) |
|
|
Term
| Cephalexin (1st gen ceph; spectrum) |
|
Definition
| pen'ase + S. aureus (not MRSA), streptococci |
|
|
Term
| Cephalexin (1st gen ceph; formulation) |
|
Definition
|
|
Term
| Cephalexin (1st gen ceph; elimination) |
|
Definition
| kidneys (same as most cephs except ceftriaxone and cefoperazone) |
|
|
Term
| Cephalexin (1st gen ceph; distribution) |
|
Definition
| excellent to tissue and fluid compartments except CSF |
|
|
Term
| Cephalexin (1st gen ceph; indications) |
|
Definition
| used for minor infections: strep pharyngitis, cellulitis, furuncles; poor choice for animal bites due to lack of Pasturella activity |
|
|
Term
| Cefuroxime (2nd gen ceph; gram + spectrum) |
|
Definition
| activity against streptococci, less s. aureus activity than 1st gen |
|
|
Term
| Cefuroxime (2nd gen ceph; gram - spectrum) |
|
Definition
| more resistance to beta-lactamases of some gram -'s, thus useful against: beta lactamase + and - H. flu, N. gon, M. catarrhalis, E. coli, P. mirabilis, Klebsiella spp., citrobacter spp., and morganella |
|
|
Term
| Cefuroxime (2nd gen ceph; formulation) |
|
Definition
|
|
Term
| Cefuroxime (2nd gen ceph; elimination) |
|
Definition
|
|
Term
| Cefuroxime (2nd gen ceph; distribution) |
|
Definition
| Good tissue and fluid distribution including CSF but slower sterilization of CSF than 3rd gen |
|
|
Term
| Cefuroxime (2nd gen ceph; indication) |
|
Definition
| community-acquired pneumonia (not nosocomial), epiglottitis, complicated sinusitis, bacteremia, soft-tissue infection, UTI |
|
|
Term
| Cefaclor (2nd gen ceph; spectrum) |
|
Definition
| between 1st gen and cefuroxim |
|
|
Term
| Cefaclor (2nd gen ceph; formulation) |
|
Definition
|
|
Term
| Cefaclor (2nd gen ceph; elimination) |
|
Definition
|
|
Term
| Cefaclor (2nd gen ceph; indication) |
|
Definition
| primarily minor RT infection |
|
|
Term
| Cefoxitin (2nd gen ceph; gram - spectrum) |
|
Definition
| less active than cefuroxime vs H. influenzae, but it is hightly effective vs E. coli, Klebsiella, and Proteus; not active vs Pseudomonas |
|
|
Term
| Cefoxitin (2nd gen ceph; gram + spectrum) |
|
Definition
| less active than 1st gen and true 2nd gen |
|
|
Term
| Cefoxitin (2nd gen ceph; anaerobic spectrum) |
|
Definition
| cephamycins (cefoxitin) are only ones with significant activity against gram negative gut anaerobes (e.g. Bacteroides fragilis) |
|
|
Term
| Cefoxitin (2nd gen ceph; elimination) |
|
Definition
|
|
Term
| Cefoxitin (2nd gen ceph; distribution) |
|
Definition
| Wide distribution except prostate, vitreous humor. CSF concentrations inadequate |
|
|
Term
| Cefoxitin (2nd gen ceph; indications) |
|
Definition
| Intra-abd/pelvic, infected decubitus ulcers, mixed aerobic-anaerobic soft tissue infections, PID (+ doxy), superior to cephazolin prophylaxis in colorectal surgery or appendectomy |
|
|
Term
| Ceftriaxone (3rd gen ceph; gram + spectrum) |
|
Definition
| potent vs S. pneumoniae, S. pyogenes and other streptococci, modest vs S. aureus; not active vs MRSA, enterococcus, Listeria |
|
|
Term
| Ceftriaxone (3rd gen ceph; gram - spectrum) |
|
Definition
| highly potent vs Neisseria spp., H. influenzae, E. coli, P. mirabilis, Klebsiella, and other Enterobacteriaceae that don’t make ESBLs |
|
|
Term
| Ceftriaxone (3rd gen ceph; anaerobic spectrum) |
|
Definition
| not effective vs B. fragilis |
|
|
Term
| Ceftriaxone (3rd gen ceph; elimination) |
|
Definition
|
|
Term
| Ceftriaxone (3rd gen ceph; distribution) |
|
Definition
| wide; NOTE that parenteral 3rd gen’s achieve useful CSF concentrations |
|
|
Term
| Ceftriaxone (3rd gen ceph; indications) |
|
Definition
| severe nosocomial infections due to gram neg rods (pneumonia, wounds, complicated UTI, septic arthritis); BACTERIAL MENINGITIS; single IM injection for gonorrhea; often useful for once daily therapy on outpatient basis (e.g. late therapy of Lyme disease; OFTEN EMPIRIC THERAPY UNTIL CULTURE RESULTS COME BACK |
|
|
Term
| Cefixime (3rd gen ceph; spectrum) |
|
Definition
| similar to ceftriaxone but poorer activity vs. S. aureus |
|
|
Term
| Cefixime (3rd gen ceph; formulation) |
|
Definition
|
|
Term
| Cefixime (3rd gen ceph; elimination) |
|
Definition
|
|
Term
| Cefixime (3rd gen ceph; absorption) |
|
Definition
| slowly, peak levels not comparable to IV |
|
|
Term
| Cefixime (3rd gen ceph; indications) |
|
Definition
| single oral dose therapy of GONORRHEA including penicillinase-producing strains; 2ND LINE for UTIs, sinusitis, otitis |
|
|
Term
| Ceftazidime (3rd gen ceph; spectrum) |
|
Definition
| poor anti-staph activity, but EXCELLENT anti-PSEUDOMONAS activity and other gram-negatives; more active vs Pseudomonas than cefoperazone |
|
|
Term
| Ceftazidime (3rd gen ceph; elimination) |
|
Definition
|
|
Term
| Ceftazidime (3rd gen ceph; distribution) |
|
Definition
|
|
Term
| Ceftazidime (3rd gen ceph; indications) |
|
Definition
| documented serious Pseudomonas infections or empiric treatment of febrile neutropenic patients who have an increased likelihood of Pseudomonas -> often in conjunction with aminoglycoside |
|
|
Term
| cefepime (4th gen ceph; gram + spectrum) |
|
Definition
| excellent Staph, Strep, but not Listeria, or MRSA |
|
|
Term
| cefepime (4th gen ceph; gram - spectrum) |
|
Definition
| excellent vs Neisseria spp., H. influenzae, E. coli, P. mirabilis, Klebsiella, and other Enterobacteriaceae; similar activity to ceftazidime against Pseudomonas; 70-80% of ceftazidime resistant Pseudomonas remain sensitive to cefepime |
|
|
Term
| cefepime (4th gen ceph; anaerobic spectrum) |
|
Definition
| not active vs gram neg gut anaerobes |
|
|
Term
| cefepime (4th gen ceph; elimination) |
|
Definition
|
|
Term
| cefepime (4th gen ceph; distribution) |
|
Definition
| similar to other cephalosporins; achieves good CSF levels |
|
|
Term
| cefepime (4th gen ceph; indications) |
|
Definition
| Not fully established; similar to ceftazidime indications; should be targeted to nosocomial infections where increased frequency of gram negative infections are anticipated |
|
|
Term
| ceftaraline (5th gen ceph; gram + spectrum) |
|
Definition
| Excellent activity and active against MRSA |
|
|
Term
| ceftaraline (5th gen ceph; gram - spectrum) |
|
Definition
| Haemophilus influenzae, Escherichia coli, Salmonella spp., Citrobacter freundii, Morganella morganii, Proteus mirabilis, and Klebsiella pneumoniae. NOT PSEUDOMONAS AERUGINOSA |
|
|
Term
| ceftaraline (5th gen ceph; resistance issues) |
|
Definition
| Vulnerable to AmpC ß-lactamases, ESBLs, and some classical penicillinases |
|
|
Term
| ceftaraline (5th gen ceph; elimination) |
|
Definition
|
|
Term
| ceftaraline (5th gen ceph; indications) |
|
Definition
| community-acquired pneumonia and complicated skin and skin structure infections including MRSA |
|
|
Term
| cephalosporin (adverse reactions, hypersensitivities) |
|
Definition
Rash, urticaria, pruritis (1-3%)
Anaphylaxis or angioedema (Rare); serum sickness w/ cefaclor
Eosinophilia (1-7%)
Cross reaction with pen allergy (1-7%) |
|
|
Term
| cephalosporin (adverse reactions, hematologic) |
|
Definition
Neutropenia (<1%)
Thrombocytosis (2-5%)
+ Coombs’ test (hemolysis rare) (1-5%) |
|
|
Term
| cephalosporin (adverse reactions, coagulopathies) |
|
Definition
Hypoprothrombinemia– related to N-methylthiotetrazole (MTT) side chain
- Cefamandole, cefoperazone, cefotetan, moxalactam, cefmetazole, cefmenoxime
- Weekly vitamin k recommended when these are used
decreased platelet aggregation– moxalactam |
|
|
Term
| cephalosporin (adverse reactions, GI) |
|
Definition
Mild increase in transaminases (1-7%)
Diarrhea (2-5%)
BILIARY SLUDGE (ceftriaxone-associated 20%); occasionally symptomatic; more common in high dose (>2 g/day) |
|
|
Term
| Only cephalosporins active against Pseudomonas? |
|
Definition
|
|
Term
| When ceph gens have good CSF levels? |
|
Definition
|
|
Term
| Which cephs are good against enterococcus? |
|
Definition
|
|
Term
| Which ceph(s) are good against MRSA? |
|
Definition
|
|
Term
| Each increase in gen of cephs usually decrease Gram + effectiveness, what is the exception? |
|
Definition
| cefepime (it maintains gram + coverage) |
|
|
Term
|
Definition
| monobactam (monocyclic Beta lactam) |
|
|
Term
|
Definition
| no activity vs. gram + or anaerobes; Active vs aerobic gram neg including Pseudomonas; not hydrolyzed by most plasmid and chromosomal beta-lactamases |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| no major reactions; DOES NOT CROSS REACT WITH PEN OR CEPH ALLERGIC PATIENTS |
|
|
Term
|
Definition
| Serious nosocomial gram-neg. infections |
|
|
Term
| Carbapenems (gram + spectrum) |
|
Definition
| Gram pos.– includes S. aureus, streptococci, Enterococcus faecalis (not faecium), Listeria, Bacillus spp.; not MRSA |
|
|
Term
| Carbapenems (gram - spectrum) |
|
Definition
| covers most including Pseudomonas (except ertapenem) |
|
|
Term
| Carbapenems (anaerobic spectrum) |
|
Definition
|
|
Term
| Carbapenems (mech. of resistance) |
|
Definition
| loss or mutation of outer membrane porin causing decreased permeability; carbapenemases increasing threat (a beta-lactamase) |
|
|
Term
|
Definition
|
|
Term
|
Definition
| kidneys; cilastatin inhibits dehydropeptidase-1 to prevent renal degradation of drug |
|
|
Term
|
Definition
| wide; low conc. In biliary tract; not for meningitis |
|
|
Term
|
Definition
Cross allergy with other beta lactams
SEIZURES 1.5% most serious side effect |
|
|
Term
| Carbapenems (mero- vs. dori-) |
|
Definition
| meropenem less likely to cause seizures; doripenem most active in vitro vs Pseudomonas |
|
|
Term
| Carbapenems (indications) |
|
Definition
| Febrile neutropenia, mixed infections (abd/pelvis); SHOULD NOT BE USED ALONE for serious Pseudomonas infection due to emergence of resistance during treatment |
|
|
