PENICILLINS

Drug Classifications

1. Natural penicillins

2. Penicillinase-resistant penicillins

3.Aminopenicillins

4.Extended-spectrum penicillins
 1.Natural Penicillins

- Natural penicillins are beeta lactam antibiotics

-Among the most important antibiotics,natural

penicillins are the preferred drugs in the treatment
of many infectious diseases
 Available agents

Sodium and potassium salts can be administered

1.Penicillin G orally,intravenously or intramuscularly

2. Penicillin V -This is a soluble dosage form

(Pen-Vee-K) - Administered orally

3. Penicillin G -These are repository drug forms

procaine and -Administered Intramuscularly
penicillin G -These insoluble salts allow slow drug absorption from the
benzathine injection site and thus have longer duration of action
 Mechanism of action

- Penicillins are bacteriocidal

- They inhibit bacterial cell wall synthesis like

cephalosporins
 Spectrum of Activity
- Natural penicillins are highly active against
Gram-positive and some gram negative cocci

- Penicillin G is 10-15 times more active than

penicillin V against gram negative organisms
and some anaerobic organisms

-The natural penicillins are hydrolyzed by

beeta lactamase(penicillinases),they are
ineffective against s.aureus and other
organisms that resist penicillin
Structure
 Penicillin G
Therapeutic Uses Precautions and Monitoring effects

- Preferred agent for all -Hypersensitivity reactions are

infections caused by anaphylaxis,urticarial,
penicillin susceptible Scarlatiniform (resembling scarlet
s.pneumoniae organisms fever) or maculopapular (area
including distinguished by spot or colour)
a) pneumonia
b) Arthritis - Anaphylaxis is the life
c) Meningitis threatening reaction that most
d)Peritonitis commonly occur with parenteral
e) Pericarditis administrations.Sign and
f) Osteomyelitis symptoms include severe
h) Mastoiditis hypotension,bronchoconstriction,
nausea,vomiting,abdominal pain
and extreme weekness
 Cont---
Therapeutic uses
-Penicillin G is the preferred
agent for gonococcal
infections, syphilis,anthrax,
actinomycosis, gas gangrene
(tissue necrosis) and listeria
infections
Actinomycosis- Inflammatory lesions of
the lymph nodes draining the mouth by
intraperitoneal or lung abscesses due to
aspiration
Precautions and Monitoring
effects
-Others are GI distress, bone
marrow suppression and
super infection
-With high dose seizures may
occur
(particularly in patients with
renal impairment)
 Cont---
• Scarlet fever- a disease caused by exotoxin released
by streptococcus pyrogens. The term scarlatina may
be used interchangeably with scarlet fever (less
acute form)
• It is characterized by:
• Sore throat
• fever
• Bright tongue with strawberry appearance
• Rash
 Drug Interactions

+ probenecid increases blood levels of natural

penicillins

+ penicillin G procaine and benzathine may

leads to prolonged hypersensitivity reactions
 2.Penicillinase-resistant penicillins

- These penicillins are not hydrolyzed by beeta

Lactamase (Penicillinases)

- These agents include methicillin,nafcilin and

Isoxazolyl penicillins (cloxacillin,dicloxacillin
( Dynapen) and oxacillin)
 Spectrum of activity

- These penicillins resist penicillinases

- They are active against staphylococci that

produces penicillinase enzymes
 Penicillinase-resistant penicillins
Therapeutic uses Precautions and Monitoring
effects
-These are solely in staphylociccal
infections(Impertigo,boils,
osteomyelitis, septic arthritis,
endocarditis, pneumonia)
- Hypersensitivity reactions
- These agents are less potent
than natural penicillins against
- Methicillin may cause
organisms that susceptible to
nephrotoxicity and
natural penicillins
interstitial nephritis
-Nafcillin is excreted by the liver and
thus may be useful in treating
Staphylococcal infections in patients
with renal impairment
 Cont---
Therapeutic uses Precautions and Monitoring
effects

-Oxacillin, cloxacillin and -Oxacillin may be hepatotoxic

dicloxacillin are most valuable
in long term therapy of serious
staphylococcal infections(e.g. - Complete cross-resistance
endoarditis,osteomyelitis) and exists among the penicillinase-
in the treatment of minor resistant penicillins
staphylococcal infections of
the skin and soft tissues
 3.Aminopenicillins
(Broad Spectrum antibiotics)
Therapeutic uses Precautions and Monitoring Effects

-Used to treat gonococcal

infections,upper respiratory
infections,Uncomplicated urinary
tract infections and otitis
-Hypersensitivity reactions
-Ampicillin with sulbactam for may occur
infections resulting from penicillin
resistant organisms -Diarrhea is most common
with ampicillin
- Amoxicillin is less effective than
ampicillin against
shigellosis(bacillary dysendery)
 Cont---
Therapeutic uses Precautions and Monitoring
Effects

- Amoxicillin more effective - Urticarial hypersensitivity

against rash with all penicillins
S.aureus(inflammation and
sepsis on UTI,lungs and -Erythematous,
maculopapular rash occurs
kidneys),
with amoxicillin
Klebsiella(alkylating
spondilities, nosocomial,
pneumonia and UTI) and
Bacteroides fragilis infections
 Spectrum of activity

- Easily destroyed by staphylococcus

penicillinases

-Aminopenicillins hacve a spectrum that is

broader than that of natural and penicillinase
resistant penicillins

- The drugs are amoxicillin and ampicillin

 4.Extented spectrum penicillins

-These agents have the widest antiobacterial

spectrum of all penicillins

- Also called as antipseudomonal penicillins

- The drugs include Carboxy penicillin

(Ticarcillin), Ureidopenicillins (eg.
mezlocillin,piperacillin)
 Spectrum of activity
Microorganisms
Drugs

-P.aeruginosa

1. Ticarcillin -combined with clavulonic acid enhance the activity

against organisms that resist ticarcillin alone

More active than ticarcillin against pseudomonas

2.Pipercillin
organisms

- Tazobactam is a beeta lactamase inhibitor

3. Piperacillin and
- staphylococci,Haemophilus,Bacteroides and
Tazobactam
Enterobacteriaceae
 Extended -Spectrum Penicillins
Therapeutic Uses Precautions and Monitoring effects

- Hypersensitivity reactions
-Mainly used to treat serious infections
caused by gram negative
- Ticarcillin may cause hypokalemia
microorganisms(sepsis,pneumonia,infe
ctions of the abdomen,bone,and soft
- The high sodium content of ticarcillin may
tissue
pose a danger to patients with heart failure
- Piperacillin/tazobactam is effective in
- All inhibit platelet aggregation which may
the treatment of nosocomial pneumonia
result in bleeding