Professional Documents
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ANTIBIOTICS
R. Anita Indriyanti
Pharmacological Department
Bandung Islamic University
References :
1. Lippincott’s Illustrated Reviews :
Pharmacology, 2nd ed
(Chapter 28)
Chemical structures
Mechanism of action
DEFINITION
AB are chemical substances obtained from
microbes/microorganisms (bacteria, fungi,
actinomycetes) that able to inhibit or
eradicate the growth of the other
microorganisms.
Antimicrobial all antiinfections
semisynthetic
synthetic
nature antibiotics
IDEAL ANTIBIOTICS CRITERIA
1. Most selective, most effective to infectied
microorganisms
2. More bactericidal effect in the site of
action
3. Antibacterial effect is not interfered by
body fluid, exudate, plasma protein or
enzymes and persist for a long duration
in the blood
4. Minimal toxicity
5. Resistance develops slowly
6. Given by any route
7. Reachable cost
In vitro
1. Primary bacteriostatic effect inhibit the
growth of m.o
Sulfonamide, tetrac, chloramph,
erythromycin (low concentration),
lincomycin, clindamycin and fusidic acid
2. Primary Bactericidal Effects
Eradicate/kill
Pen, cef, aminoglic, erythromycin (high
concentration), cotrimazol. Rifampisin
and vankomycin.
Those classification is not absolute but
relative
SPECTRUM OF AB EFFECTS
1. Narrow spectrum antibiotics (NSAB)
Main effect : sensitive for gram positive
bacteria and bacil
e.g. : Pen. G, Pen. Resistent penicillinase
semisynthetics, bacitracin, macrolides,
lincomycin, vancomycin
2. Broad Spectrum Antibiotics (BSAB)
Main effect : sensitive for gram positive
and gram negative bacteriae
e.g. : Pen. (ampicillin and amoxycillin),
cefalosporins, tetracyclins,
chloramphenicol, trimetroprim and
sulfonamides
Widely used of BSAB an umbrella in
treating the unidentified bacterial
infection
resistance
RESISTANCE and
MECHANISM OF ACTION recall in
microbiology
SIDE EFFECTS
1. ALLERGIC REACTION
2. TOXIC REACTION
Direct effects in unproper dose e.g. :
aminoglycosides
3. SUPERINFECTION : new infection caused
by pathogen microbes or fungi during AB
therapy to primary infection.
SUPERINFECTION : frequent
potentially harmed risk
Causa : Enterobacter, Pseudomonas,
Candida and other fungi. Those agents are
difficult to be eradicated by today available
antibiotics.
AVOIDING SUPERINFECTION
1. Stop the giving antibiotics
2. Treatment according to bacterial
identification and sensitivity test
ANTIBIOTICS HOST
PHARMACOKINETICS
PHARMACODINAMICS
CHARACTERISTIC HOST ASPECTS
OF ANTIBIOTICS BIOCHEMICAL &
PHYSIOLOGICAL &
PATHOLOGICAL
CONDITIONS
DEFINITION OF RATIONAL USE OF
ANTIBIOTICS (WHO)
PROPER INDICATION
PROPER DRUG
PROPER DOSAGE
SE MONITORING
RATIONAL USE OF AB
Define the patient problems specify the
therapeutic objectives
Verify the suitable of your personal
treatment
PROCEDURES Start the treatment
Give information, instruction and warning
Monitoring and stop treatment
Clinical diagnosis
Identification, sensitivity test of
STEPS TO PROCEDURES bacteria
Pharmacodynamics
Pharmacokinetics
Host factors
RATIONAL USE OF ANTIBIOTICS
PREVENTION IN HIGH
SUSCEPTIBILITY TO
GET INFECTION
THERAPY ERADICATING
PROPHYLAXIS
M.O
EMPIRIC THERAPY
IN SURGICAL CONDITIONS
DEFINITIVE THERAPY
It is the most effective, least toxicity
and the narrowest selection
Based on :
* identification of bacteria
* sensitivity test
* interpretation in the content of the
overall clinical picture
* the AB of choice directed to M.O
EMPIRIC AB THERAPY
Giving AB directly without identification
and sensitivity test of bacteria, but……
obtaining specimen for lab. analysis
before giving AB.
Empiric AB therapy based on local
epidemiological data :
- What is the pathogen M.O potentially
infected
- AB given based on susceptibility pattern
- Initiated after obtaining specimen
- Started with AM combination or single
BSAB
SELECTING AB IN EMPIRIC THERAPY
MISUSE of AB :
Treatment of untreatable infection
Therapy of fever of unknown origin
Improper dosage
Inappropiate reliance on AB alone
Lack of adequate bacterial information
STRATEGIC FOR EMPIRIC THERAPY
Empiric therapy :
Coverage by a combination of antibiotics such as
Clindamycin plus gentamycin
Effective against gram positive, gram negatives and anaerobes
Or
A single broad spectrum AB
Such as imipenem/cilastatin
- Laboratory :
ө erroneous report of susceptible
pathogen
AB – COMBINATION
Synergisme (3) :
1) Blockade of sequential steps in
a metabolit sequence
- Trimethoprim - sulfamethoxazol
2) Inhibition of enzymatic inactivation
- Amoxycillin - clavulanat
3) Enhancement - Aminoglycosides
- Penicillins - Aminoglycosides
Antagonism (2) :
1. Inhibition of cidal activity by static
agent
- Tetracyclines – Betalactam AB
► Mixed infection
► Synergism effect
► Risk of developing resistant
organism <
► Increase AB coverage or
► Infection of unknown origin
DISADVANTAGES OF AB COMBINATION
- Increase risk of toxicity
- Increase MDR-pathogens
- Increase cost
- Increase antagonism (bacteriostatic
+ bactericide)