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Natural PCN
- PCN-G
- PCN-V: e-withdrawal group (acid stable)
- Mech: B-lactam ring
- Tx: Gram+ Aero,
- N.meningitidis(gram-)
- Actinomycetes, Fusobacterium (anaero)
- Resistant: Staph (PCNase)
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AminoPCN
- Ampicillin: polar group
- Amoxicillin: ^^ + e-withdrawal
- Tx: PCN (Gram+aero,N.meningitidis(gram-)Actinomycetes, Fusobacterium (anaero)) + H. influenza, E.coli, Proteus
- Resist: Klebsiella, Staph (both PCNase)
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UreidoPCN
- Piperacillin: polar (urea+piperazine)
- Tx: PCN/aminoPCN (Gram+aero,N.meningitidis(gram-)Actinomycetes, Fusobacterium (anaero), H.influenzae, E.coli, Proteus) AND many Gram- (Klebsiella, P.auruginosa, N. gonorrhoeaa)
- Resist: Staph (PCNase)
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PCNase-resist PCN
- Nafcillin: bulky
- Oxacillin: ^^+ e-withdrawal
- Dicloxicillin: ^^
- Tx: Staph
- Resist:
MRSA, MRSE
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Beta-Lactamase Inh
- Tazobactam w/ Piperacillin: Pseudomonas
- Clavulanate w/ Ticarcillin: Pseudomonas (not w/Amoxicillin)
- Sulbactam w/ Ampicillin: not Pseudomonas
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Caphalospore
decreased strain on B-lactam ring
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Cephalothin
- 1st Gen Cephalosporin: bulky group
- Target: PBP-3 (hyphal)
- Tx: PCN (Gram+aero, Gram-N.mening, anaero(actinomycetes, fusobacterium) + Staph, some Enterobact (E.coli, Kelbsiella,Proteus)
- Resist: Enterococcus, Haemophilus, Pseudomonas
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Cefazolin
- 1st Gen Cephalosporin: bulky group
- Tx: PCN (Gram+aero, Gram-N.mening, anaero(actinomycetes, fusobacterium) + Staph, some Enterobact (E.coli, Kelbsiella,Proteus)
- Resist: Enterococcus, Haemophilus, Pseudomonas
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Cephalexin
- 1st Gen Cephalosporin: PO absorption
- Tx: PCN (Gram+aero, Gram-N.mening, anaero(actinomycetes, fusobacterium) + Staph, some Enterobact (E.coli, Kelbsiella,Proteus)
- Resist: Enterococcus, Haemophilus, Pseudomonas
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Ceftriaxone
- Advanced Cephalosporin: Oxime
- ^^t1/2
- Tx: (=Cefotaxime) PCN, Staph, most Enterobacteria, Haemophilus
- Resist: Pseudomonas
- S/E: Hepatotoxic with sever liver dysfxn.
- -never given to Neonates!!!
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Cefotaxime
- Advanced Cephalosporin: Oxime
- Tx: (=Ceftriaxone) PCN, Staph, most Enterobacteria, Haemophilus
- Resist: Pseudomonas
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Ceftazidine
- Advanced Cephalosporin:
- R: Propylcarboxy (vs. Pseudomonas)
- Tx: Pseudomonas, Haemophilus, most Enterobacteria
- Resist: Gram+
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Cefepime
- Advanced Cephalosporine
- Zwitterion: en mass porins
- Tx: Pseudomonas, Haemophilus, most Enterobacteria AND Gram+ (same as Ceftazidiime, but Ceftazidime is not effective for Gram+)
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Cefpodoxime
- Advanced Cephalosporin:
- Ph/R group: e-withdrawal
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Ceftaroline
- Advanced Cephalosporine
- Target: PBP2a of MRSA (lose shape)
- Tx: MRSA, VISA, VRSA, PCN/cephalosporine resistant S. pneumoniae
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Carbapenem
- R: steric block of PCNase
- Target: PBP-2 (lose shape) and most others
- -Enters thru differ Porin than PCN/CEPH
- Tx: Life-threatening/polymicrobial infection
- -Enterococcus stasis (need aminoglycoside)
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Imipenem
- Carbapenem, =Meropenem
- (R: steric block of PCNase)
- (Target: PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
- Tx: (Life-threatening/polymicrobial infection-Enterococcus stasis (need aminoglycoside))
- -Gram+cocci, Gram-Rods, Anaerobes
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Meropenem
- Carbapenem, =Imipenem
- (R: steric block of PCNase)
- (Target: PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
- Tx: (Life-threatening/polymicrobial infection-Enterococcus stasis (need aminoglycoside))
- -Gram+cocci, Gram-Rods, Anaerobes
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Ertapenem
- Carbapenem
- (R: steric block of PCNase)
- (Target: PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
- ^^t1/2: once daily (90% protein bound)
- Tx: (Life-threatening/polymicrobial infection)
- -Gram+cocci, Enterobact, Anaerobes
- Resist: Enterococcus, Pseudomonas
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Doripenem
- Gorillazine
- Carbapenem
- (R: steric block of PCNase)
- (Target: PBP-2 (lose shape) and most others-Enters thru differ Porin than PCN/CEPH)
- Tx: (Life-threatening/polymicrobial infection-Enterococcus stasis (need aminoglycoside))
- -greatest activity vs. non-fermenters (Pseudomonas, Nocardia)
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Aztreonam
- Monobactam
- Target: PBP-3 (hyphal)
- R: Propylcarboxy (vs. Pseudomonas)
- No cross rxn w/ PCN allergy
- Tx: Aero Gram-Rods
- Resist: Gram+, Anaerobes
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Vancomycin
- Glycopeptide
- Mech: bind D-Ala-D-Als, block bridging
- Tx: Gram+, Entercoccus with aminoglycoside, MRSA
- Resist: Gram- (too large for porin)
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Fosfomycin
Bind building blocks of peptidoglycans
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Daptomycin
- Lipopeptide
- Form membrane cation channels (Ca-depend)
- IV only (pep broken down)
- Tx: Gram+, MRSA/SE etc.
- Resist: Gram- (too large)
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Colistin
- Polypeptide AB
- Mech: bind LPS/Plipids
- Tx: Gram-
- Resist: very common
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Fluoroquinolones
- Fluoroquinolone: inh Type II topoisomerase
- Tx: Gram-Rods, Gram+Cocci, Mycobacterium, intracellulars
- -Protatitis, Mycobacteriosis
- -inh DNA Gyrase (Gram-)
- -inh Topoiso IV (Gram+)
- S/E: GI, CNS (delerium), Abnl Glc homeo (no DM)
- -Arthropathy (no kids)
- -Prolonged QT
- Rx:
- -Levofloxacin:
- -Moxifloxacin: ^anaerobic
- -Gemifloxacin:
- -Ciprofloxacin: ^aerobic (no effect on S.aureus, S.pneum)
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Metronidazole
- Nitroimidazole: Tinidazole also
- Mech: ^^Free Redicals damage DNA (NO2 group reduced by ferredoxin)
- Tx: Anarobes (not Actinomycetes), Protozoa
- Resist: Actinomycetes, Aerobes
- S/E: Seizure, Encephalopathy, neuropathy, Red urine, gynecomastia, Antabuse Rxn
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Rifampin
- Rifamycin
- Mech: binds RNA Polymerase
- ^oral available, not given alone
- -Osteomyelitis, Endocarditis
- S/E:
- -Induce CYP3A: decr contracept,warfarin,Azoles
- -levels decr by AlOH3(antiacid), Azoles
- -Orange/red urine/contacts
- -rash, hepato/nephrotox, flu-like
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Rifabutin
- Rifamycin
- Mech: inh RNA Pol
- well absorbed
- Tx: M.avium, resistant MTb
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Rifaximin
- Rifamycin
- Mech: inh RNA Pol
- poorly absorbed: Zwitterion!
- Tx: C. diff
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Aminoglycosides
- Mech: bind 30S ribos: cause misread^^polar cation
- only with severe infection
- Tx: Gram- Aerobic Rods, Enterococcus (w/ cell wall inh)
- S/E:
- Nephrotox: absorb in prox. tubule, accum in lysos
- Ototoxic: choclea (outerHC), vest (type1 HC)
- NMJ Block: decrease ACh release
- Rx:
- Gentamicin
- Tobramycin
- Amikacin
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Tetracyclines
- Mech: bind 30S ribos
- Tx: Rickettsiae,
mycoplasma, chlamydiae - S/E: no preg!!! (hepatotox to mom, interfere w/ fetal teeth/bones: stain)
- -esoph ulcers, diarrh, benign intracranial HT, vertigo
- Interaction: forms complexes with cations
- -decr abs w/ milk/antacid,iron, cimetidine (h2-block)
- -decr t1/2 w/ EtOH/anti-epilectics
- Rx:
- Tetracycline
- Doxycycline
- Minocycline
- Tigecycline
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Macrolides & Axalides
- Mech: bind 50S chromos
- Tx: Mycoplasma, Gram+/-, protozoa, spirochetes, intracellulars
- Resist: Enterobacteria
- S/E: GI upset, cholestatic hepatitis,
- -Hearing loss (transient)
- -Prolonged QT
- Rx:
- Macrolides: Erythromycin, Clarithromycin
- Azalide: Azythromycin
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Clindamycin
- Mech: bind 50S ribosfavorite of dentist/Sx
- Tx: Viridans strep, Aero Gram+cocci,
- -Anaero: Fusobacteria, B.fragilis,Prevotella,Peptostrep
- S/E: AB Colitis: C. diff overgrowth (pseudomem)
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Linezolid
- Mech: bind 50S ribos
- Tx: Gram+Cocci, MRSA, MRSE, VRE, PCN-resistant S.pneum.
- S/E: BM suppression
(thrombocytopenia) - -Mito Tox: Lactic Acidosis
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Sulfonamides
- Mech: inh Folic Acid syn: replace PABA on pterydine synthase
- Same as Trimethoprim:
- Tx: Bacteria, Parasites, Fungi
- Ristant: Anaerobes
- S/E:
- -GI upset
- -Steven-Johnson
- -Hypouricemia
- -leukopenia
- -thrombocytopenia (also seen w/ Linezolid)
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Trimethoprim
- Mech: inh Folic Acid syn: last step (dihydropteroic-x-> FA)
- Same as Sulfonamides:
- Tx: Bacteria, Parasites, Fungi
- Ristant: Anaerobes
- S/E:
- -GI upset
- -Steven-Johnson
- -Hypouricemia
- -leukopenia
- -thrombocytopenia (also seen w/ Linezolid)
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