penicillins 2 Flashcards
how to increase penicillin activity against gram neg bacterua
- increase hydrophilicity
how to increase penicillin stability for oral formulation
- electron w drawing R group
how to increase resistance to penicillinase
- steric shields aka bulky R groups
- excellent against gram pos especially strep and staph
- ineffective against gram neg
- susceptible to penicillina
pen G
- slightly less active but can be given orally
- given in form of potassium salt
- higher levels if given on empty stomah
- indicated for mild-moderate infections of upper respiratory tract, scarlet fever (strep, pneumococcal), mild staph skin or soft tissue infections and mild to moderate infections of oropharynx and gum tissues
pen V
what does pen G cover according to antibiotic map
- Enerococcus faecalis
- S. pneumonia
- Strep pyogenes
- N. menigitidis (sorta)
Natural penicillins are active against Neisseria gonorrhea and staph areus and coagulase neg staph…so why aren’t they indicated for use?
- bc high resistance potential
natural penicillins also very effective against spirochete:
- treponema pallidum aka syphilis
penicillinase resistant penicillins (think CONDOMS) indicated for staph MSSA and strep producing penicillinase
- Cloxacillin
- Oxacillin*(second best in US, but no oral)
- Nafcillin* (no oral)
- Diloxicillin* (best in US)
- Oxacliin again
- Methiillin (not available in US)
Naficillin covers is a penicillinase resistant antibiotic that is active against
- S. pneumonia
- strep pyogenes
- MSSA staph aureus (major use)
- broad spectrum penicillins
- amide bond and no resonance
- added hydrophilic groups to increase gram neg activity
- no bulky ortho groups so inactivation of beta lactamase likely
- EWG make it acid resistant so higher oral absorptiom
- Aminopenicillins
aminopeniillins
- Amoxicillin (oral only)
- Ampicillin (Oral, IV, IM)
ampicillin/amoxicillin (aminopenicillins) coverage according to map
- Enterococcus faecalis (+)
- S. pneumonia (+)
- S. pyogenese (+)
- Proteus Mirabilis (-)
- H ingluenzae (-)
- N. meninigitidis (-)
antipseudomonal penicillins aka extended spectrum antibiotics
- carboxypenicillins (carbenillin)
- Ureidopenicillins (pippercillin)
piperacillin
- ureidopenicillin (extended spectrum)
- activity against klebsiella, enterococcus and increased anaerobic coverage
- highest activity against P. aerginosa
- slightly decreased activity against gram pos compared to natural penicillins and ampicillin
- susceptible to beta lactamase
- IC or IM
