Natural Penicillin Flashcards
Now the organism used to produce penicillin are ?
Penicillium chrysogenum
Organism where penicillin is derived
Penicillium notatum
MOA of penicillin
Bactericidal
Inhibit bacterial cell wall synthesis, 3rd stage
4 important steps in MOA of penicillin ?
- Bind to PBP
- Inhibit transpeptidase (helps in cross linkage)
- No peptidoglycan produced
- Autolysin ( supposedly remodel cell wall) will now act and kill the bacteria
Mechanism of bacterial resistance in penicillin?
Production of Beta lactamases
Altered PBP - decreased entry of drug into organism
Transpepetidase alteration
Pharmacokinetics of Penicillin?
- absrptn in git
- blood ( plasma protein)
- distribution in tissues
- metabolism
- excretion
Poor absptn by oral ( gastric acidity)
All natural penicillin only by parenteral route. IV suitable. IM painful. X displace albumin. Widely distributed. Enters CSF only when meningits. Placentae ok. Metabolised in liver. Active tubular secretion.
How to prolong DOA of penicillin?
Probenecid or benzathine added.
Poorly water soluble compounds.
Preparations of natural penicillin ?
✅Penicillin G ( benzyl penicillin) ✅Procaine Penicillin G ✅Fortified Procaine Penicillin G ( 0.3 MU procaine penicillin G + 0.1 MU penicillin G ) ✅Benzathine Penicillin G
Antibacterial spectrum of Penicillin
Cocci- gram positive & negative
Bacilli- gram positve
Spirochetes
PENICILLIN G
Duration of Action
Dosage
Uses
PENICILLIN G
4~6 hours
0.2~2MU/every 4~12 H IM/IV
▶ Confirmed case of Meningococcal meningitis
▶ Enterococcal endocarditis ( with IV gentamicin, for 6 weeks)
▶ Sensitive pneumococcal organism - 20~24MU/day for 7-10days
▶Anthrax - 8~10 days
▶ Gas gangrene -1~2weeks
▶ Leptospirosis -7 days
▶Neurosyphilis
▶Rat bite fever
PROCAINE PENICILLIN G
Duration of Action
Dosage
Uses
PROCAINE PENICILLIN G 6~12hours 0.6~1.2MU/every 12 H IV/IM ▶ Streptococcal pharyngitis, sinusitis, rheumatic fever, otitis media - 10 days ▶Carrier of C. Diphtheria - 10 days ▶ Early syphilis & latent syphilis
FORTIFIED PROCAINE PENICILLIN G
Duration of Action
Dosage
Uses
FORTIFIED PROCAINE PENICILLIN G 12~24 hours 2MU/day ▶ Sensitive Gonococcal infections -14 days ▶Actinomycosis (+sulphadiazine) for 6 weeks
BENZATHINE PENICILLIN G
Duration of Action
Dosage
Uses
BENZATHINE PENICILLIN G 1~3 weeks 0.6~2.4MU/month ▶Streptococcal pharyngitis, sinusitis, otitis media - single dose ▶All stages of syphilis ▶Prophylaxis of rheumatic fever
Syphilis stages and how penicllin helps
1⃣ Early & latent syphilis
Procaine penicillin
Benzathine penicillin
2⃣ Late syphilis
Benzathine penicillin
3⃣Neurosyphilis/cardiosyphilis
Penicillin G
Benzathine penicillin
Limitations of penicillin G
Acid labile
Short DOA
Susceptible to penicillinase enzymes
Narrow antibac specturm