1. Penicillin G (IV form), Penicillin V (oral)

2. Prototype B-lactam antibiotics

3.MOA: bind PBPs, block transpeptidase cross-linking of cell wal, activate autolytic enzymes

4. Use: bactericidal for gram positives, gram negative cocci, and spirochetes

5. Not penicillinase resistant

6. Toxicity: Hypersensitivity reactions, hemolytic anemia

1. Methicillin, Nafcillin, Dicloxacillin

2. MOA: smae as penicillin, narrow spectrum, penicillinase resistant due to bulkier R group

3. Clinical use: S. aureus (except MRSA because of altered PBP target site)

Toxicity: Hypersensitivity, methicillin causes interstitial nephritis

4. Nafcillin- not absorbed orally

"Use Naf (Nafcillin) for Staph"

1. Clavulanic acid

2. Sulbactam

3. Tazobactam

4. Work against 2e cephalosporinases and ESBL but not BUSH 1

1. chromosomally mediated and inducible

2. gram - bacteria

3. Treat with carbapenems

1. Resistant to oxyimino-cephalosporins and monobactams

2. Klebsiella and E. coli- resistant to cephalosporins

3. Susceptible to imipenem

1. inhibited by tazobactam, clav acid, etc.

2. blocked by suicide inhibitors

1. food interferes with ampicillin, not amoxicillin (AmOxicillin has greater Oral bioavailability)

2. MOA same as penicillin, Wider spectrum, Penicillinase sensitive

3. Can combine with clavulanic acid to enhance spectrum

Clinical Use: Extended spectrum penicillin- certain gram-positive bacteria (less than other penicillins) and gram-negative rods (H. influenzae, E. coli, L. monocytogenes, P. mirabilis, Salmonella, enterococci)

4. Toxicity: Hypersensitivity, ampicillin rash, pseudomembranous colitis

AMPed up penicillin

Ampicillin/Amoxicillin HELPS kill enterococci

1. Ticarcillin, Carbenicillin, Piperacillin

2. Same MOA as penicillin, extended spectrum

3. Clinical use: Pseudomonas spp and gram-negative rods

4. susceptible to penicillinase so use with clavulanic acid

5. Toxicity: Hypersensitivity reactions

TCP: Takes Care of Pseudomonas

1. B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases, Bactericidal

2. Toxicity: Hypersensitivity reactions- cross hypersensitivity with penicillin in 5-10% of patients; increased nephrotoxicity of aminoglycosides; disulfiram-like reaction with ethanol in cephalosporins with methylthiotetrazole group e.g. cefamandole

1. Cefazolin- IM or IV

2. Cephalexin, cephradine- oral

3. Gram-positive cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae

PEcK

1. Cefoxitin/Cefotetan- IV/IM

2. cefachlor- oral

3. cefuroxime enters CSF

4. Gram-positive cocci, Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp, Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens

HEN PEcKS

1. Ceftriaxone (long 1/2 life)/Cefotaxime/Ceftriaxone

2. Serious gram-negative infections resistant to other B-lactams, meningitis (most penetrate BBB)

3. Ceftaxidime for pseudomonas

4. Ceftriaxone for gonorrhoea

5. Resistance: failure to reach PBPs, beta lactamase, variant PBPs, B lactamase induction

1. Cefepime- zwitterion

2. Increased activity against psedomonas and gram-positive organisms

1. Imieneum is a broad-spectrum, B-lactamase resistant carbapenem always administered with cilastatin which inhibits renal dihydropeptidase I to decrease its inactivation in the renal tubules

2. Clinical use: gram-positive cocci, gram-negative rods, and anaerobes

3. DOC for enterobacter

4. Toxicity: GI distress, skin rash, CNS toxicity (seizures) at high plasma levels- significant side effects limit use to life-threatening infections or after other drugs have failed

5. Meropenem has a reduced risk of seizures and is stable to dihydropeptidase I

lacks activity v. E. faecium, MRSA, coag - staph, P. maltophilia and cepacia, C. difficile

With imipenem "the kill is LASTIN with ciLASTIN"

1.Monobactam resistant to B-lactamses

2. MOA- inhibits cell wall synthesis by binding PBP (like penicillin)- works synergistically with aminoglycosids

3. no cross allergicity with penicillins or cephalosporins

4. Use: Gram-negative rods- Klebsiella spp, Pseudomonas spp, Serratia spp; for penicillin allergic patients and those with renal impairment who cannot tolerate aminoglycosides

5. NO ACTIVITY AGAINST GRAM + OR ANAEROBES

6. Toxicity: usually nontoxic; occasional GI upset

1. MOA- inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors. Bactericidal

2. Resistance occurs with amino acid change of D-ala D-ala to D-ala D-lac

3. Use: serious gram-positive multidrug resistant organisms including S. aureus and C. difficile

4. Toxicity: Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing (Red man syndrome- prevent with antihistamines and slow infusion rate)

Well tolerated in general- does NOT have many problems

1. Polymyxin B, Polymyxin E

2. MOA- bind to cell membranes of bacteria and disrupt their osmotic properties- cationic, basic proteins that act like detergents

3. Clinical use- resistant gram-negative infections

4. Toxicity- neurotoxic, acute renal tubular necrosis

MYXins MIX up membranes