pharmacokinetic

Absorption
Acid resistant penicillin
absorbed orally
Affected by meal
Better taken 1h before, 2h
after meal
Distributionall over body
Pass BBB
o very little (normal)
o very easy (inflamed)
pass placenta easily but
not teratogenic
bound to plasma protein
Metabolized by bacterial
enzyme
penicillinase penicillin
acid react with protein
(inactive + hapten)
major determinant for
allergic reaction
Excretion
Kidney active renal
tubular excretion
probenecid inhibit it
readjust dose in patient
with impaired renal
function
bile enterohepatic

Antibacterial activity
Bactericidal
Mechanism
Bind to specific penicillin binding
protein (PBP)
transpeptidase responsible
for cell wall synthesis (cross link
of peptidoglycan)
Activate autolysin enzyme
lysis of cell wall
Bacteria imbibe water rupture
& death of microbe
Resistance
Natural absence of
peptidoglycan mycoplasma
Plasmid mediated
o Production of -lactamase
enzyme
o Alteration in PBP
o permeability
Spectrum
a. Narrow
o Gram +ve cocci
o Gram ve cocci
o Gram +ve bacilli
o Anaerobes
o Spirochete
o Actinomycete
b. Broad
o Similar to narrow
o Gram ve bacilli
c. Extended
o Similar to broad

uses
Treatment
a. Gram +ve cocci
i. Pharyngitis streptococcal
ii. Abscess staphylococcal
iii. Lobar pneumonia
pneumococcal
b. Gram ve cocci
neisseria
i. Gonorrhea
ii. Meningococcal meningitis
c. Gram +ve bacilli
i. Anthrax
ii. Diphtheria
iii. Tetanus
iv. Gas gangrene

Adverse effect
1) Allergy
Urticaria, angioedema &
anaphylactic shock,
avoided by
previous history
Dermal sensitivity test
Never use again
TTT of shock adrenaline,
antihistamine, cortisol
2) Jarisch Herxheimer
Reaction
Only 1st injection in
spirochete, syphilis due
to liberation of toxin
TTT by cotisol continue
penicillin therapy

d. Spirochete syphilis
3) Diarrhea
e. Actinomycosis +
pseudomonas
f. Gram ve bacilli
i. Thyphoid fever
ii. UTI
iii. H. influenza
iv. H. pylori peptic ulcer
Prophylaxis
1. Gonorrheal neonatal
ophtalmia
Benzyl penicillin eye drop
2. Pharyngitis in rheumatic
fever
Benzathin penicillin
3. Bacterial endocarditis in

4) CNS irritation
5) Na+ or K+ salt dangerous
in renal or cardiac problem
Benzathin penicillin
pain, tenderness at site of
injection,
thrombophlebitis
Methicillin nephritis
Caboxy penicillin
platelet dysfunction
Ampicillin rashes

o Klebsilla pneumonia
o Proteus
o Pseudomonas aeruginosa

rheumatic fever or
prothetic cardiac valve
Procain penicillin before
dental procedure

patient with infective

monoclonus, leukemia,
taking allopurinol
immune reaction

Penicillin inhibitors
Penicillin Inhibitors
Clavulanic
Sulbactam
Tazobactam

Mechanism
Bound with the B-lactamase enzyme
irreversible inhibition suicide
substrate

Action
Very weak or no
antibacterial activity

Preparation
Clavulanic + Amoxicillin Augmentin
orally

Protect from inactivation

by bacteria producing blactamase

Clavulanic + Ticarcillin Timentine IV

Sulbactam + Ampicillin Unasym
orally, IV, IM
Tazobactam + Piperacillin Tazocin - IV