Tikrit university

College of pharmacy
Pharmacognosy III 5th lec.

Antibiotics

Antibiotic: Chemical produced by a microorganism that kills or inhibits the

growth of another microorganism.

Antimicrobial agent: Chemical that kills or inhibits the growth of microorganisms

History of antibiotic development

1928 :Alexander Fleming noted mould of the genus penicilium contaminating one
of his cultures

preventing the growth of bacteria.

1935: Domagk ,sulphonamide –synthetic dye

1941: clinical trials of penicilin- Florey and Chain

Mechanisms of action

antibiotics act by disrupting various molecular targets within bacteria and cel
surface, preventing growth or initating kiling.

3 broad mechanisms:

•Disrupt bacterial cell envelope

•Block production of new proteins

•Inhibit DNA replication

Bacteriostatic drugs arrest the growth and replication of bacteria at serum (or
urine) levels achievable in the patient, thus limiting the spread of infection until the
body’s immune system attacks, immobilizes, and eliminates the pathogen.

Bactericidal drugs kill bacteria at drug serum levels achievable in the patient.
Because of their more aggressive antimicrobial action, bactericidal agents are often
the drugs of choice in seriously ill patients.

Acquired resistance to Antimicrobial drugs. Mechanisms:

1) Microbes may elaborate drug-metabolizing enzymes (ie penicillinase).

2) Microbes may cease active uptake of certain drugs

3) Microbial drug receptors may undergo change resulting in decreased antibiotic

binding and action.

4) Microbes may synthesize 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 effect
macrolide spectrum

Selection of the most appropriate antimicrobial agent requires knowing

1) the organism’s identity

2) the organism’s susceptibility to a particular agent,

3) the site of the infection

4) patient factors

5) the safety of the agent

6) the cost of therapy

COMBINATIONS OF ANTIMICROBIAL DRUGS

It is therapeutically advisable to treat patients with a single agent that is most

specific to the infecting organism. This strategy reduces the possibility of
superinfection, decreases the emergence of resistant organisms and minimizes
toxicity. However, situations in which combinations of drugs are employed do
exist. For example, the treatment of tuberculosis benefits from drug combinations.
A. Advantages of drug combinations Certain combinations of antibiotics, such as
β-lactams and aminoglycosides, show synergism; that is, the combination is more
effective than either of the drugs used separately. Because such synergism among
antimicrobial agents is rare, multiple drugs used in combination are only indicated
in special situations—for example, when an infection is of unknown origin

B. Disadvantages of drug combinations A number of antibiotics act only when

organisms are multiplying. Thus, coadministration of an agent that causes
bacteriostasis plus a second agent that is bactericidal may result in the first drug
interfering with the action of the second. For example, bacteriostatic tetracycline
drugs may interfere with the bactericidal effect of penicillins and cephalosporins.