Natural Penicillin

Parenteral Administration

For G+ non-resistant staph and strep

G-: N Meningitidis

A. Israelii, T. Pallidum

Natural Penicillin

Better oral absorbsion than Penicillin G (stable under acidic conditions)

Less active than Penicillin G against most microbes- used for minor infections.

Natural Penicillin 

Depot Injection- slow release

Adult: Glut or Thigh

Children: Thigh

Strep. Pyogenes

Penicillin G Benzathine

Natural Penicillin for Depot

Adult: Glut or Thigh

Children: Thigh

Streptococcal pharyngitis, rheumatic fever, syphilis

Penicillinase Resistant Penicillins (Anti-Staphylococcal Penicillins)

No need for adjustment in renal dysfunction- just hepatic.

No longer used clinically

Can cause Interstitial Nephritis (Type IV hypersensitivity)

Penicillinase Resistant Penicillins- Anti staphylococcal Penicillins

Not effective against G-

One of the most resistant to breakdown by beta-lactamases

No need for adjustment in renal failure- only hepatic

IV adminstration

Penicillinase Resistant Penicillins- Anti-staphylococcal penicillins

Not effective against G- 

No need for adjustment in renal failure- only hepatic

Oral or IV adminstration

Extended Spectrum Penicillins (Aminopenicillins)

Greater activity towards G- than Penicillin G

Oral of IV adminstration

Extened Spectrum (HELPSS ME)

Extened Spectrum Penicillins (Aminopenicillins)

Food does not interfere with absorbsion

Oral administration only

Better against G- than Penicillin G

Extened Spectrum (HELPSS ME)

Antipseudomonal Penicillin - Carboxypenicillin

Treatment of Serious infections by G- aerobic bacilli and mixed aerobic-anaerobic infections (Pseudomonal infections)

Major use is combo with AG for pseudomonal infections (Septicemia and UTI's)

Toxic: Sodium for CHF, and prolong bleeding time

Antipseudomonal Penicillins - Ureidopenicillins

Broader spectrum of activity than ticarcillin (better against G- bacilli)

Used in combo with AG

CAP, Nosocomial Pneumonia, Septicemia, Nosocomial UTI, Gynecologic and Obstetric infections, Intra-Abdominal infections

Costs Less than ticarcillin and less effect on bleeding time, less sodium

Monobactam (monocyclic beta lactam ring)

Highly resistant to b-lactamases from G-

Only active against G- rod (Bacilli)

Pts allergic to pens or cephs -> not react to azetreonam

Imipenem=rapidly broken down in renal tubule-> cilastatin inhibits the dehydropeptidases-> inc. conc in kidney

Resistant to breakdown by most beta-lactamases

Eliminated by renal excretion-adjust dose in RF

Inhibits 90% of clinically important bacteria-> reserved for serious hospital aquired infections

Potent beta-lactamase inducer and can cause siezures

B-Lactamase inhibitors 

Good against Amber Class A, not Class C (G- Bacilli)

First Generation Cephalosporin

Good activity against G+ but modest against G-

Drug of Choice for Surgical Prophylaxis

Parenteral Administration

PECK=Gram negative that has good activity against

Alternative agent for Staph and Strep in pts with allergies to Pen's

2nd Generation Cephalosporin

Increased activity against G- from first gen.

Activity against anaerobe B. fragilis*

Not effective against Pseudomonas aeruginosa

3rd Generation Cephalosporin

Can penetrate CNS to treat meningitis

Much more acive against G- than second generation

Less Active against G+ than first generation

Useful against G- Bacilli resistant to other cephalosporins, pens and AG's

Can treat Lyme Dx from B. burgdorferi

3rd Generation Cephalosporin

Much more acive against G- than second generation

Less Active against G+ than first generation

Useful against G- Bacilli resistant to other cephalosporins, pens and AG's

First line for N. gonnorrhoeae

3rd Generation Cephalosporin

Can penetrate CNS to treat meningitis

Much more acive against G- than second generation

Less Active against G+ than first generation

Useful against G- Bacilli resistant to other cephalosporins, pens and AG's

3rd Generation Cephalosporin

Much more acive against G- than second generation

Can penetrate CNS to treat meningitis

Less Active against G+ than first generation

Useful against G- Bacilli resistant to other cephalosporins, pens and AG's

4th Generation Cephalosporin

resistant against deactivation by plasmid and chromosomal b-lactamases

Useful against enterobacter infections

Useful against penicillin resistant Streptococci

Penetrates well into the CNS and is used to treat meningitis.

Chloramphenicol- Broad Spectrum- Binds reversibly to 50s rib. subunit

Oral- includes active drug and pro-drug

Parenteral- chlorampheniol succinate broken dn in body

Reaches thearaputic levels in CNS- meningitis

not first line due to many toxic effects (can also inhibit protein syn in mammalian cells)

No adjustment in renal failure- hepatic gluc conj.

Resistance caused by bacterial enzyme acetyl transferase- prevents drug from binding to ribosome

Bone Marrow Toxicity (bone marrow suppression, aplastic anemia)

Gray Baby Syndrome

Tetracycline Antibiotic- bind 30s rib. su.

Take with water and not within 1-2 hours of lying down- esophageal ulceration

Bind calcium-decrease absorbsion- dont give with dairy products

Tet(AE) and Tet(K) pump produces resistance

SE: GI, B+T, RD, sunlight sens

SE: GI, B+T, RD, sunlight sens

Tetracycline Antibiotic - inhibit 30s rib su. 

IV admin

No dosing change in RF

Not pumped out by Tet(AE) or Tet(k) or Tet(M) efflux pmp.

Skin and skin structure infections/intra-abdominal infections

Macrolide Antibiotic- reversibly inhibit 50s rib su. 

Widely dist. but not in brain and csf.

Base has poor oral absorbsion- esters (stearate, estolate, and ethylsuccinate) increase oral absorbsion and acid stability

Tox: liver-Estolate form can cause chol. hepatitis.  GI upset.  Inhibit CYP.

Antag. with Chloraphenicol (binding sites too close)

First line for Chlamydial Infections

Aminoglycoside Antibiotic- reversibly inhibit the 30s ribosomal subunit

Poor Oral Absorbsion- Prefer IV or IM

Not readily enter cells, eye, or CNS

Not effective against Anaerobic Bacteria or Abcess (Acidic)

Adjust dose in renal faliure