2.. PRINCIPLES OF ANTIMICROBIAL THERAPY

PRINCIPLES OF ANTIMICROBIAL
THERAPY
DR. KASHYAP DAHAL
SENIOR RESIDENT
CHEMOTHERAPY
The use of chemicals against invading
organisms.
The term is used for both treatment of cancer

and treatment of infection.
ANTIBIOTIC
A chemical that is produced by one
microorganism and has the ability to harm
other microbes.
SELECTIVE TOXICITY
The ability of a drug to injure a target cell or
organism without injuring other cells or
organisms that are in intimate contact .
• Minimum inhibitory concentration(MIC): The
lowest concentration of antibiotic that
inhibits bacterial growth.
• Minimum bactericidal concentration(MBC):
The lowest concentration of antimicrobial
agent that results in a 99.9 percent
decline in colony count after overnight
broth dilution incubations effects.
CLASSIFICATION OF ANTIMICROBIAL
DRUGS BY SUSCEPTIBLE ORGANISMS
• Antibacterial
• Antiviral drugs
• Antifungal
• Antiparasitic
CLASSIFICATION BY MECHANISM OF
ACTION
1. Bacterial cell wall synthesis inhibitor
2. Disruption of cell membrane function
3. Protein synthesis inhibitor
4. Nucleic acids synthesis inhibitor
5. Antimetabolites formation
6. Inhibitors of viral enzymes.
RESISTANCE
Acquired resistance to Antimicrobial drugs.
➢Drug-metabolizing enzymes (ie penicillinase).
➢Cease active uptake of certain drugs
➢Drug receptors may undergo change resulting
in decreased antibiotic binding and action.
➢Synthesis of compounds that antagonize drug
actions.
DELAYING THE EMERGENCE OF
RESISTANCE
1. Use antimicrobial agents only when needed.
2. Use narrow-spectrum antibiotics whenever

possible.
3. Newer antibiotics should be reserved for

situations in which older drugs are dangerous
or no longer effective
SELECTION OF ANTIBIOTICS
➢The identity of the infecting organism.
➢Drug sensitivity of the infecting organism.
➢Host factors
ANTIBIOTIC COMBINATIONS
• Additive response : The antimicrobial effect of
the combination is equal to the sum of the
effects of the two drugs alone.
• Potentiative interaction : The effect of the

combination is GREATER than the sum of the
effects of the individual agents.
• Antagonistic response : The combination of
two antimicrobials may be less effective than
one of the agents by itself (i.e. combination of
a bacteriostatic with a bactericidal drug)
DISADVANTAGES OF ANTIMICROBIAL
COMBINATIONS
➢ Increased risk of toxic and allergic reactions.
➢ Possible antagonism of antimicrobial effects.
➢ Increased risk of suprainfection

PENICILLINS
➢ Mechanism of action : Inhibit cell wall
synthesis
➢ Penicillinases (Beta-lactamases) :Enzymes

that cleave the beta-lactam ring and thereby
render penicillin and other beta-lactam
antibiotics inactive.
CLASSIFICATION
➢ Narrow-spectrum (penicillinase sensitive)
➢ Narrow-spectrum that are penicillinase resistant

(antistaphylococcal)
➢ Broad-spectrum penicillins (aminopenicillins)
➢ Extended-spectrum penicillins (antipseudomonal)

• PENICILLIN ALLERGY: Most common cause of
drug allergy (1-10%).
• Cross-sensitivity :5-10% of patients allergic to

penicillins are also allergic to cephalosporins.
• Skin tests for penicillin allergy: Skin tests are
employed to assess the currents risk of a
severe reaction.
NOT RELIABLE
• For many infections VANCOMYCIN AND
ERYTHROMYCIN are effective and safe. In
cases with allergic reaction to penicillin.
• PENICILLINASE-RESISTANT PENICILLINS
(Antistaphylococcal): Methicillin,Nafcillin.
• BROAD-SPECTRUM PENICILLINS •
(Aminopenicillins) : Ampicillin (Bordetella
pertussis, E.coli, Salmonella, Shigella)
• EXTENDED-SPECTRUM PENICILLINS •
(Antipseudomonal ): Ticarcillin
CEPHALOSPORINS
• Mechanism of action :disruption of cell wall
synthesis and consequent lysis of the cell.
CLASSIFICATION
• First generation :highly active against gram
positive bacteria (staphylococci)
• Second-generation : enhanced activity against
gram-negative bacteria
• Third-generation : more active against gram
negative aerobes (important activity against
Pseudomonas Aeruginosa).
• Fourth generation : highly resistant to
betalactamases. Broad spectrum antibiotics.
• Fifth generation: For MRSA
Other inhibitors of cell wall synthesis
• IMIPENEM : highly active against gram-
positive and gram-negative cocci .
• It is also the most effective beta-lactam

antibiotic against anaerobic bacteria.
VANCOMYCIN
• Principal indications : antibiotic-associated
pseudomembranous colitis (Clostridium
difficile)
• Infection with methicillin-resistant

Staphylococcus aureus.
BACTERIOSTATIC INHIBITORS OF
PROTEIN SYNTHESIS
• TETRACYCLINES
• MACROLIDES
• CLINDAMYCIN
• CHLORAMPHENICOL
• AMINOGLYCOSIDES:disruption of bacterial
protein synthesis.
• Antimicrobial spectrum : aerobic gram-
negative bacilli (E.Coli,Klebsiella
pneumoniae,Proteus Mirabilis,Pseudomonas
Aeruginosa).
• The drugs are inactive against most gram-
positive bacteria.T
• The drugs are ineffective against anaerobes.
SULFONAMIDES AND TRIMETHOPRIM
SULFONAMIDES: Inhibit synthesis of of folic
acid
• Antimicrobial spectrum :broad antibiotics
TRIMETHOPRIM: Inhibit dihydrofolate

reductase
ANTITUBERCULUS DRUGS
ISONIAZID (Administer pyridoxine)
RIFAMPIN
PYRAZINAMIDE
ETHAMBUTOL
FLUOROQUINOLONES
• CIPROFLOXACIN
• Mechanism of action : Inhibits DNA replication
by acting on DNA gyrase
METRONIDAZOLE:
Iinhibition of nucleic acids synthesis.
Therapeutic uses: The drug is active against
obligate anaerobes
It is used in combination against Helicobacter
Pylori.
ANTIFUNGALS
ANTIVIRAL
THANKYOU

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PRINCIPLES OF ANTIMICROBIAL

The term is used for both treatment of cancer

2. Use narrow-spectrum antibiotics whenever

3. Newer antibiotics should be reserved for

➢Drug sensitivity of the infecting organism.

• Potentiative interaction : The effect of the

➢ Possible antagonism of antimicrobial effects.

➢ Increased risk of suprainfection

➢ Penicillinases (Beta-lactamases) :Enzymes

➢ Narrow-spectrum that are penicillinase resistant

➢ Broad-spectrum penicillins (aminopenicillins)

➢ Extended-spectrum penicillins (antipseudomonal)

• Cross-sensitivity :5-10% of patients allergic to

• It is also the most effective beta-lactam

• Infection with methicillin-resistant

TRIMETHOPRIM: Inhibit dihydrofolate

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