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Presented by,
Dr Noor Jahan
Objective
At the end of lecture students will be able to,
Classify penicillins
Explain mechanism of penicillin
Enlist penicillins
Give indications of penicillins
Describe mechanism of resistance
Explain adverse effects and drug interactions
of penicillin
CHEMOTHERAPY
Classification According to Site of Action
1- Synthesis of bacterial cell wall
2- Protein synthesis
3- Nucleic acid metabolism
4- Permeability of cytoplasmic membrane
cell damage
1- Synthesis of bacterial cell wall:
a- Cycloserine: Formation of di-d-alanine
b- Fosfomycin: Formation of N-acetyl
cysteine
c- Vancomycin , Teicloplanin & Bacitracin:
Elongation of peptidoglycan
d- β-Lactam antibiotics: last step of cell wall
synthesis. [Transpeptidase
enzyme responsible for cross linking of
bacteria
eg.:Aminoglycoside , Tetracycline
c- Binding with 50S ribosomal subunit of
bacteria
eg.:Chloramphenicol , Erythromycin ,
Lincosamides
3- Nucleic acid metabolism:
a- Folate antagonists:
- Compete with PABA :eg.: Sulphonamides
- Dihydrofolate reductase enz.: eg.:
Trimethoprime & Pyrimethamine
b- DNA:
-Antiviral & anticancer –Griseofulvine
-Metronidazole & Chloroquine
-Quinolones [ DNA gyrase enz.]
c- RNA eg.: Rifampicine [ RNA polymerase
enz.].
4- Permeability of cytoplasmic
membrane cell damage:
eg.: Amphotericin & Nystatin (antifungal), Daptomycin &
Polymyxin [Colomycin (colistin)].
Colistin is a polycationic peptide and has
both hydrophilic and lipophilic moieties.
These cationic regions interact with the bacterial outer
multidrug-resistant Pseudomonas
aeruginosa, Klebsiella pneumoniae, and Acinetobacter.
Classification According to
Mechanism of Action
1- Bactericidal: β-lactam antibiotics,
Polymixines, Quinolones, Aminoglycosides ,
Rifampicin
2- Bacteriostatic: Sulphonamides ,
Chloramphenicol , Tetracyclines
1-Vancomycin (Vancocin)
2-Teicloplanin
3-Bacitracin
4- Fosfomycin
5-Cycloserine
Empirical Treatment is a medical treatment
not derived from the scientific method, but
derived from observation, survey or common
use.
In the medical profession, the term is also used
cure of a disease.
Penicillins
food allergies
If the prick test does not show any reactions,
allergies
The RAST (radioallergosorbent test) is a
blood test to determine the level of the IgE
antibody in the system
A newer blood test, the ImmunoCap has been
antibiotics
A history of any type of allergy.
Penicillin G
Penicillin V
Ampicillin
Amoxicillin
Nafcillin
Oxacillin
Ticarcillin
Piperacillin
Structure of Penicillin
Mechanism of Action
• Penicillins are dipeptide analogs of D-ala-D-
ala.
• Radiolabelled Penicillin G binds to several
bid
Piperacillin (IV): 3–4 g q4–6h
Augmentin
AUGMENTIN is an oral antibacterial combination consisting
of amoxicillin and the beta-lactamase inhibitor, clavulanate
potassium (the potassium salt of clavulanic acid).
Augmentin 250, for example, contains 250 mg of
amoxicillin and 125 mg of clavulanic acid. (375mg Tab).
Film-coated tablet contains amoxicillin trihydrate
equivalent to 500 mg amoxicillin and potassium clavulanate
equivalent to 125 mg of clavulanic acid. (625mg Tab).
Tablets 875mg amoxicillin plus 125mg potassium
clavulanate (1000mg Tab).
Suspensions of amoxicillin/clavulanic acid are available for
use in children.
Augmentin Dosage
Adults and children ≥ 40 kg
One 250 mg/125 mg dose taken three times
such as:
◦ dental infections
◦ infected animal bites
◦ infected human bites (including uncomplicated "clenched-fist" or
"reverse-bite" injuries)
Ampiclox 500mg capsules
Ampiclox 500mg Capsules is Indicated for the
prophylaxix or treatment of bacterial infections
It is also appropriate for the treatment of respiratory
tract infections: Bronchitis, pneumonia, empyema, lung
abscess and infections associated with cystic fibrosis.
Ear, nose and throat infections: Tonsillitis, sinusitis,
pharyngitis, otitis media and quinsy. Pelvic infections:
Septic abortion, salpingitis, puerperpal pyrexia and
caesarian section prophylaxis.
Urinary tract infections: Cystitis and pyelonephritis.
Skin and soft tissue infections: Abscesses, boils,
carbuncles and post-operative wound infections.
Gastro- intestinal infections, Septicaemia, endocarditis
and orthopaedic infection.
Ampiclox 500mg capsules
Ingredient
Each gelatin capsules contains the equivalent
tract, including infections of the ears, nose and throat:
Acute otitis media, acute sinusitis and bacterial
pharyngitis; Infections of the lower respiratory tract:
Acute exacerbation of chronic bronchitis, community-
acquired pneumonia; Infections of the lower urinary
tract: Cystitis; Prophylaxis of endocarditis in patients at
risk i.e. surgery in the oral cavity or upper airways.
Amoxil
In haemolytic streptococcal infections the duration of therapy should
be 6-10 days in order to achieve eradication of the organism.
Adult dosage (including elderly patients): Standard dosage: The
usual dosage covers a range from 750 mg to 3g amoxicillin daily in
divided doses. In some areas 1500 mg amoxicillin daily in divided
doses are recommended as the upper usual dose. Special dosage
recommendation: Acute exacerbation of chronic bronchitis in
adults: 2 x 1 g per day.
Children's dosage (under 40 kg): The daily dosage for children is
40 - 90 mg/kg/day in two to three divided doses (not exceeding 3
g/day) depending on the indication, the severity of the disease and
the susceptibility of the pathogen. Children weighing more than 40
kg should be given the usual adult dosage.
Difference of Penicillin and
Amoxicillin
Amoxicillin does not have to be taken as long as
penicillin. It does the job in a shorter period of
time.
A study published June 2007 in the journal
(continuous infusion)
5. Prophylaxis for scarlet fever - recent
local epidemics of scarlet fever
Streptococci have occurred in U.S.
Benzathine Pen G
Penicillins Advantages:
Bactericidal against sensitive strains
Relatively nontoxic
Have excellent tissue penetration
Efficacious in the treatment of infections
Relatively inexpensive in comparison with
other antibiotics
Newer penicillins are resistant to stomach
synthetically
Penicillins Disadvantages:
Acid lability - most of these drugs are destroyed
by gastric acid
Short duaration of action - because of this short
half-life, the penicillins must be administered at
short intervals, usually every 4 hours
Lack of activity against most Gram-negative
organisms
Drug hypersensivity - about 10% of population
has allergy
Many patients experience GI upset
Painful if given intramuscularly
Thank you