* Thiazolidine and beta lactam ring. Side chain determines properties and spectrum of activity

* Inhibits transpeptidase

* Bacteriocidal

* Microbes make beta-lactamase, breaks open beta lactam ring.

* Procaine-complexed suspension for IM. Local anesthetic that helps numb pain of injection

*Available w benzathine as Bicillin C-R

* Ester form and can cause allergic reaction

* Aqueous for IM/IV

* Procaine

*Benzathine

* Bicillin LA, longer lastering, suspension for IM

* 90% eliminated by tubular secretion, things that compete for secretion site ie. uric acid and probenecid increases PCN levels

* Dosed in Units 1 unit-.6 uG

* Given as an IM or IV

* Distributes to CNS only if the meninges are inflammed

* Grand daddy of PCN

* phenoxymethyl PCN

* Acid stable form for oral use

* Dose in mgs.

* Food interferes with absorption of most PCNs so give 1hr before or after eating

* Less active than "G" in some organisms

Dicloxacillin oral

Oxacillin parenteral

Nafcillin parenteral

Eliminated by biliary and renal excretion

*Have an amino group

* provide more activity against gram - bacteria

* Still susceptible to PCNase

* Ampicillin and Amoxicillin

* oral or IV

* Available with Subactum or unasyn for IM IV to prevent beta lactamase activity.

* beta lactamase resistor

* preferable to ampicillin for peritonitis due to Bacteroides fragilis.

*Parenteral

* Tablets, oral suspension, prediatric drop

* Better oral absorption and longer half live than ampicillin

* Available with Clavulanate (beta lactamase inhibitor) (Augmentin brand name)

* Before dental work if high risk (prosthetic heart valve, cyanotic heart disease)

* Otitis media

* Forperitonitis orally AFTER IV thrapy to finish off infection

Antipseudomonas PCNs

* Against pseudomona and some Proteus

* susceptible to PCNases

*Marketed with beta lactam inhibitor and parenteral

* Ticarcillin+CLavulanate

* Piperacillin+ Tazobactam (piperacillin sometimes given by itself)

* Hypersensitivity fomr metabolites acting as haptens. IgE mediated.

* Diarrhea common to all antibiotics

* Superinfection, especially with C. difficile

* Seizures if penetrat BBB by blocking GABA inhibitor receptor

* Jarisch-Herxheimer Reaction in 70-90% w 2 degree syphyllis.Self limiting, looks like allergic rxn

* Beta lactam and dihydrothiazine ring with side chain that has same function as PCNs

* Can resist many beta lactamases, greater spectrum of activity

* General 1-4, increasing in activity against gram Neg

Cephalosporins

Gen 1

* Resist Staph PCNase

Cefazolin IV

Cephalexin Oral

Cefadroxil Oral

Good G+ and the PEcK gram-

Cephalosporins

Gen 2

* Less G+, HNPEcK Gram -

* Cefalcor oral every 8 hf. Associated w serum sickness

Cefuroxime- 12 h

Cefoxitin- cephamycin. Acitve vs. Bacteroides fragilis, IV.IM

* Cefotetan- IV.IM. Methylthiotetrazole side chain antagonizes vit K> hypoprothrombinemia. Give w K

Cephalosporins

Gen 3: Ceftriaxone

Much less G+ more G-

* Ceftriazone-IV/IM highly protein bound, can displace bilirubin. Not to <3 mo old.

* Can use in those <3 mo for a single dose for gonorrhoeae conjunctivitis

* good against meningitis, 50-50 bile, renal, do not use w Ca++ precipitates form in lung and kidney.

* Sludge in children. nausea anorexia, epigastric pain, coli. Reversible when discountinues

* Cefotaxime IV IM Parent and metabolit active> increase specturm

* Cefpodoxime

* Cefdinir excreted mostly unchanged. Binds Fe, decrease absorption, red feces with high Fe intake

* Ceftazidime IV IM neurologic SE, increase risk if you are epileptic

Cephalosporins

4th Generation

* For gram - rods

*Save them as last resort

* Cefepime: IV IM Good CNS penetration. Neuro side effects: disorientation, m yclonus, EFG, increased risk if epileptic. Mainly renal excretion

* Cefditoren- pro RX, hydrolyzed by esterases during absorption

* Ceftaroline- IV proRx given every12 h for community acquired bacterial pneumonia and complicated skin and skin sturcture infection, MRSA

* Side effects; Nausea, Diarrhea, rash

* Hypersensitivity: Risk of cross allergy w PCN greatest for 1st gen.

* Risk and avoid if you have documented type IgE to PCN

* Immune mediated hemolytic anemia risk

* Broad spectrum beta lactams. G+/G- microbes, reserved for resistent

Impipenem only on needing with Cilastatin

Meropenem

Ertapenem

Doripenem

* Note, most "statins' mean lower cholesterol. This DOESNT

* Imipenem metabolized by dehydropeptidase with a toxic metabolite. Cilastatin inhibits this.

* Cause nausea and vmitting side effects

* Increase rick of infection with C. diff, seizures

* Meropenem- few seizures, not metabolized by dehydropeptidase

* Ertapenem- once a day dosing

* Doripenem- injection for complicated intra-abdominal infections andUTIs, newest

* Cardiopenem needing cilastatin with it.

* IV/IM

* Resistant infectoins causing:

1. UTIs
2. Lower RTIs
3. Bone, joint, skin
4. intra abdominal and gynecological infection
5. bacterial septicemia