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Penicillin

By : abdelmnaem elgelia
Classification:
 Cell wall synthesis inhibitors
Beta-lactams (penicillins, cephalosporins,

aztreonam, imipenem)
Poly-peptides (bacitracin, vancomycin)

 Protein synthesis inhibitors


Aminoglycosides

Tetracyclins

Macrolides

Chloramphenicol

Clindamycin

 Folate antagonists
Sulfonamides

Trimethoprim

 Quinolones
BACTERIAL CELL WALL
 Gram-negative (e.g. E.coli, Salmonella)
Few peptidoglycan

layers(Lipopolysaccheride)

 Gram-positive (e.g. Staphylococci,


Listeria)
Many peptidoglycan layers(Lipoteichoic

acid)
ØPenicillin binds to cell
wall ofMechanism of 
bacteria , Prevention
from developing a cross link
action
in peptidoglycans , and lyses
it .
ØPenicillins inactivate the
transpeptidase , in order to
destroy the cell wall
ØActivation of autolysins
enzymes
ØAffect more on growing
bacteria
ØPenicillin resistance
Resistance to Penicillins
1)Production of β -lactamases
2)
3)The occurrence of modified penicillin-
binding sites
4)
5)Decreased permeability to the drug
Penicillins 
classification
– Narrow spectrum – penicillinase sensitive

– Narrow spectrum – penicillinase resistant

– Broad spectrum penicillins

– Extended­spectrum penicillins
Narrow spectrum – penicillinase (= β ­
lactamase) sensitive
• Benzylpenicillin

– Naturally occuring

– Poor oral availability (sensitive to stomach 

acid)

– given by injection

– Active against gram­positive bacteria

• Phenoxymethylpenicillin

– Better oral availability (acid resistant)
Narrow spectrum – penicillinase (= 
β ­lactamase) resistant
• Methicillin

– Semisynthetic

– Poor oral availability (only parenteral)

– Active against gram­pos bacteria

– Mostly used for Staphylococcus aureus

• Oxacillin

– Good oral availability

• Cloxacillin
Broad spectrum – penicillinase (= β ­
lactamase) sensitive(= Aminopenicillins)
• Ampicillin

– Semisynthetic

– Good oral availability

– Active against gram­pos and gram­neg 

bacteria

– Active against enterobacteria

• Amoxicillin

– Excellent oral availability
Extended spectrum – penicillinase (= β ­
lactamase) sensitive (= 
Carboxypenicillins)
• Carbenicillin
– Semisynthetic
– Poor oral availability
– Active against gram­pos and gram­neg bacteria
– Active against Pseudomonas aeruginosa,        
Klebsiella

• Ticarcillin

• Mezlocillin

• Pipercillin
PHARMACOKINETIC:

Absorbtion orally
Distrubution
BBB
Placenta
Renal execretion
Metabolizetion
Therapeutic use
Treatment of: 
Gram +
cocci___________________Staph
, strepto >>>> abcess
Gram _
cocci__________________nisseria
>>>> meningitis
Gram +
bacilli_________________anthrax
, tetanus , gas gangrene
spirochetes >>>> syphilis
actinomycese >>>> actinomycosis
Gram –
bacilli__________________UTI ,
H . Pylori , typhoid fever
üimpairment of platelet aggregation.

üirritative responses to penicillin at site 

of injection

üphlebitis or thrombophlebitis

ünausea, with or without vomiting

üIntrathecal injection of penicillin G 

may produce arachnoiditis
PROBENECID
 Probenecid is an oral drug used for reducing
blood uric acid levels in patients with
hyperuricemia (high uric acid)
 Probenecid prevents attacks of gout by
reducing uric acid levels in the blood.
 It does this by preventing the reabsorption of
uric acid by the kidney and increasing its
excretion from the body in the urine.
 Probenecid also blocks excretion by the
kidney of penicillin and related antibiotics
and is used for increasing the levels of the
antibiotics in the blood and increasing
their effectiveness when treating
PRESCRIBED FOR:

Probenecid is used for the treatment 

of hyperuricemia associated with 

gout. It also is used for increasing 

blood levels of penicillin­type 

antibiotics (for example, ampicillin 

and amoxicillin).
SIDE EFFECTS:
Common side effects of probenecid include 
headache, dizziness, nausea, vomiting, skin 
rash, sore gums, and fever. 
Probenecid may cause a flare of gout and 
kidney stones, and it is not started during an 
acute attack of gout.
Serious but rare side effects include reduced 
red blood cell counts (anemia), liver damage 
and severe allergic reactions.