Professional Documents
Culture Documents
Definition
Chemotherapeutic agents
Drugs that act against diseases
Antimicrobial agents
Drugs that treat infections
Antibiotics
Antimicrobial agents produced naturally by organisms
Semisynthetics
Chemically altered antibiotics that are more effective
than naturally occurring ones
Synthetics
Antimicrobials that are completely synthesized in a
lab
1928 Fleming
discovered
penicillin,
produced by
Penicillium.
1940 Howard
Florey and
Ernst Chain
performed first
clinical trials of
penicillin.
Features of Antimicrobial
Drugs toxicity
Selective
Antibiotics cause greater harm
(kerugian) to microorganisms than to
human host
Toxicity of drug is expressed as
therapeutic index
Lowest dose toxic to patient divided by dose
typically used for treatment
High therapeutic index = less toxic to patient
Narrow therapeutic index = more toxic, monitor
closely
Features of Antimicrobial
Drugs
Antimicrobial action
Bacteriostatic drugs
Inhibit bacterial growth
rely on host immunity
Bacteriocidal drugs
Kill bacteria
Most useful in situations when host defenses
cannot control pathogen
Classification of antibacterial
agents:
bactericidal
bacteriostatic
-lactam agents
Aminoglycosides
Co-trimoxazole
Vancomycin
Erythromycin
Tetracycline
Chloramphenicol
Sulfonamide
Trimethroprim
Features of Antimicrobial
Drugs
Spectrum of activity
Antimicrobials vary (rubah) with respect
to range(jarak) of organisms controlled
Narrow (sedikit) spectrum
Work on narrow range of organisms
Gram-positive only OR Gram-negative only
Advantage (untung) : effects pathogen only
Disadvantage: requires identification of pathogen
Broad spectrum
Advantage: Work on broad range of organisms
Disadvantage : disruption of normal flora
Features of Antimicrobial
Drugs
Effects of combinations of
antimicrobial drugs
Combination sometimes used to treat
infections
Synergistic: whole is > sum
Antagonistic: whole is < sum
Effects of Combinations of
Drugs
Features of Antimicrobial
Drugs
Tissue distribution, metabolism and
excretion
Drugs differ(berbda) in how they are
distributed, metabolized and excreted
Half-life: Rate of elimination of drug from
body
Time it takes for the body to eliminate one
half the original dose in serum
Half-life dictates frequency of dosage
Features of Antimicrobial
Drugs
Adverse effects
Allergic reactions
Toxic effects
Suppression of normal flora
Antimicrobial resistance
Inhibition of cell
wall synthesis
Penicillins
Cephalosporins
Vancomycin
Bacitracin
Isoniazid
Ethambutol
Echinocandins
(antifungal)
Inhibition of pathogens
attachment to, or
recognition of, host
Arildone
Pleconaril
Inhibition of
protein synthesis
Aminoglycosides
Tetracyclines
Chloramphenicol
Macrolides
Human
cell membrane
Inhibition of DNA
or RNA synthesis
Actinomycin
Nucleotide
analogs
Quinolones
Rifampin
Disruption of
cytoplasmic membrane
Polymyxins
Polyenes (antifungal)
Inhibition of general
metabolic pathway
Sulfonamides
Trimethoprim
Dapsone
-lactam ring
Penicillin G (natural)
Cephalothin (semisynthetic)
Aztreonam (semisynthetic)
Cephalosporin
Monobactam
Methicillin (semisynthetic)
Penicillins
Growth
New NAM-NAM
cross-links
inhibited by
penicillin
Previously formed
cross-links remain
unchanged
Bacitracin
Blocks secretion of NAG and NAM from
cytoplasm