ANTIMICROBIAL /

ANTIBIOTICS
Hendrik SB
hendrik-s-b@fkg.unair.ac.id
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What are antibiotics?
 Microbial products 
inhibit or kill other
microbes (MIC &
MBC)

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 Antibiotic requirements
 Not interference the hosts
 Good penetration into the tissue  reaches
the bacteria

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 ANTIBIOTICS

 INHIBIT / KILL MICROORGANISM

 HARMFUL TO MICROORGANISM ENVIRONMENT
 LIMITED TO MICROORGANISM
 NOT TO THE PARASITE

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 ANTIBIOTICS

 MICROBIAL SUBSTANCES
 FUNGI’S PRODUCT
 KILLING / BACTERIOSTATIC OTHER
MICROBIALS
 SEMYSYTHETIC
 FULL SYNTHETIC
 SELECTIVE TOXICITY

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Chloramphenicol Spiramycin
Ciprofloxacin
Garamycin Doxycyclin Streptomycin

Krisdayanti
Amoxicillin
Tetracyclin Cephalosporin Thiamphenicol

Inul

Cloxacillin Azithromycin Colistin

Rifampicin Clindamycin Ampicillin
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 Infects the host
host
a. Immunity Selective toxicity
b. Passive Biologic alteration
immunity
c. Overt 2
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disease

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pathogen drug

Microbes respons
a. Resistance
b. Bacterial destruction

1. Pathogenesis of infection
2. Pharmacokinetic & dinamic in the patient
3. Microbiologic proses of drugs-pathogen interaction 8
What should I do ?

 What’s happen ?
 What is the caused of ?
 How to find the right
therapist for him ?

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 Based on its selective toxicity
properties
 Bacteriostatic activity
 Bactericid activity

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 Based on the spectrum
 Broad spect
 Narrow spect
 Expanded / Extended

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 Structure of Bacteria
 The structure of bacteria is divided into
two, namely:
1. Basic structure
Includes cell wall, plasma membrane, cytoplasm,
ribosomes, DNA, and storage granules
2. Additional structure
Includes capsule, flagellum, pilus, fimbria,
chlorosome, gas vacuole and endospores.

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 BACTERICIDE

 Penicillin (D.S)
 Cephalosporins (D.S)
 Cyclosporine (D.S)
 Vancomycin (D.S – M.S)
 Bacitracin (D.S – M.S)
 Aminoglycoside (S.P)
 Polymyxin (M.S)
 Amphotericin B (M.S)
 Novobiocin (D.S – S.A.N – M.S)

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 BACTERIOSTATIC

 Chloramphenicol (S.P)
 Erythromycin (S.P)
 Lincomycin (S.P)
 Clindamycin (S.P)
 Tetracycline (S.P)

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 MECHANISM OF ACTION ANTIBIOTICS

 ANTIMETABOLITE ACTIVITY
 ALTERATION OF CELL MEMBRANE
PERMEABILITY
 INHIBITION OF CELL WALL SYNTHESIS
 INHIBITION OF PROTEIN SYNTHESIS
 INHIBITION OF NUCLEIC ACID SYNTHESIS

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 ANTIMETABOLITE ACTIVITY

 SULFONAMIDE
 TRIMETHOPRIM
 PARA-AMINOSALICYLIC ACID (PAS)
 SULFONIC ACID

Folic acid → purines and pyrimidines synthesis (precursors of DNA

and RNA), cellular growth and replication
BACTERIOSTATIC EFFECTS
MICROBA NEED FOLIC ACID
BACTERIAL PATHOGEN SYNTHESIS FOLIC ACID FROM
PABA
SULFOMAMID / SULFON COMPETITION with PABA 
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MICROBIAL DISRUPTION
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FOLIC ACID ANTAGONIST
 FOLIC ACID SYNTHESIS INHIBITOR :
 SULFADIAZINE
 SULFAMETHOXAZOLE
 FOLATE REDUCTASE INHIBITORS :
 TRIMETHROPRIM
 PYRIMETHAMINE
 MIX :
 Cotrimoxazole

Pediazole (erythromycin + sulfasoxazole) 

alternative of amoxicillin  acute otitis media
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 ALTERATION OF CELL MEMBRANE
 POLYMYXIN
 POLYENE DERIVATES AND VARIOUS
CHEMOTHERAPIES (ANTISEPTIC’ SURFACE
ACTIVE AGENT)

Permeability Characteristic:
 selective and control the entry and exit of substances from and into
cells  ionophores
 Maintain internal osmotic pressure and excretion of waste products

POLYMYXIN  binding to lipopolysaccharide (LPS) and phospholipids in the

outer membrane of Gram-negative bacteria,  components out PROTEIN,
NUCLEID ACID, NUCLEOTIDE
UNEFFECTIVE FOR GRAM-POSITIVE  PHOSPHATE POOR
RESISTANT ON GRAM-NEGATIVE  PHOSPHATE POOR 20
 INHIBITION OF CELL WALL SYNTHESIS

 PENICILLIN
 CEPHALOSPORINS
 BACITRACIN
 VANCOMYCIN
 CYCLOSERINE

CELL WALL  CONSIST POLYPEPTIDOGLYCAN (GLICOPEPTIDE) 

INHIBIT TRANPEPTIDASE  UNBALANCED OSMOTIC PRESSURE
INSIDE-OUTSIDE  LYSIS

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 INHIBITION OF PROTEIN SYNTHESIS
 AMINOGLYCOSIDE
 MACROLIDE
 LINCOMYCIN
 TETRASCYCLINE
 CLORAMPHENICOL

– Bacterial – 70S (50S/30S)

– Mammalian – 80S (60S/40S)

PROTEIN SYNTHESIS 
In the process that are attacked are :
(1) the formation of the 30S initiation complex (made up of mRNA, the 30S
ribosomal subunit, and formyl-methionyl-transfer RNA),
(2) the formation of the 70S ribosome by the 30S initiation complex and the 50S
ribosome, and 24
(3) the elongation process of assembling amino acids into a polypeptide
 INHIBITION OF NUCLEIC ACID SYNTHESIS

 RIFAMPICIN
 QUINOLONE
 ANTI CANCER & ANTI VIRUS

nucleic acid is a very important in DNA replication

RIFAMPICIN  POLIMERASE-RNA BINDING  INHIBIT RNA & DNA
SYNTHESIS
KUINOLON  INHIBIT DNA GIRASE  CHROMOSOMES ALIGN
LESS SELECTIVITY  toxic >>

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 PRINCIPLE of ANTIBIOTIC
THERAPY
 IDENTIFYING
MICROORGANISMS
 SENSITIVITY TEST
 TARGET OF
INFECTION
 SAFETY & SE
 PX FACTOR
 PRICE
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 FACTORS RELATED TO
PHARMACODYNAMICS &
PHARMACOKINETICS OF ANTIBIOTICS
 AGE
 PREGNANCY
 GENETIC
 PATHOLOGICAL CONDITION

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 DRUGS EXCRETION
 RENAL EX : LIVER EX :
– Tetracyclin •• Sulfamethoxazole
– Vancomycin •• Chloramphenicol
– Norfloxacin
•• Clindamycin
– Trimethoprim
•• Doxycylin
– Penicillin And
Derivates •• Erytrhomycin
– Aminoglycosides •• Metronidazole
– Aztreonam •• Nafcilin
– Cephalosporin
•• Rifampicin
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 PLACENTA
 0 - 30 % :
Oxacillin, Amikacin,Dicloxacillin,Nafcillin, Tobramycin,
Cefazolin, Erythromicin
 30 - 50 % :
Sefamandol, Clindamycin, Gentamicin, Cefalotin,
Streptomycin, Kanamycin
 50 - 100 % :
Chloramphenicol, Sulfonamide, Carbenicillin, Penicillin
G, Tetracyclin, Trimethoprim, Methicillin, Ampicillin

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 FAILURE OF ANTIBIOTIC THERAPY

 LOW DOSAGE
 DURATION OF THERAPY
 MECHANICAL BARRIER: ABSCESS
 WRONG DX/ ETIOLOGY
 PHARMACOKINETICS
 WRONG DRUG CHOICE
 PATIENT FACTORS

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 FREQUENTLY ENCOUNTERED BACTERIA IN
PLAQUE, DENTAL CARIES, GINGIVITIS AND
PERIODONTITIS
BACTERIUM Plaque Dental caries Gingivitis Periodontitis
Streptococcus sanguis ++ ++ ++ +
S. mutans ++ ++ 0 0
S. salivarius 0 0 0 0
Actinomyces viscosis + + ++ +
A. israelii + + ++ ++
Lactobacillus sp. + + 0 0
Propionibacterium acnes 0 + + ++
Bacteroides sp. 0 0 + ++
Selenomonas sputagena 0 0 + ++
Large spirochetes 0 0 0 ++
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ANTIBIOTIC PROPHYLAXIS AIMS
 PROTECT FROM INFECTION  RISK FACTORS
 PREVENT SECONDARY INFECTION
 PREVENT ENDOCARDITIS FROM BACTEREMIA

PRINCIPLES OF PROFILAKSIS
 ANTIBACTERIAL
 MICROORGANISM
 SURGERY
 DURATION OF SURGERY
 IM / IV

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 ADVERSE REACTIONS

 SUPERINFECTION/ SUPRAINFECTION  BROAD

SPECT AM  NARROW
 CHLORAMPHENICOL – COUMARIN  METB.
COUMARIN <
 CHLORAMPHENICOL – PHENOBARBITAL 
METB. CHLORAMF. >
 RIFAMPICIN – COUMARIN  T ½ KUMARIN <
 RIFAMPICIN – STEROID CONTRASEPTION 
METB. STEROID >  UNEFFECTIVE

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 ANTIMICROBIAL
RESISTANCE
 THE CAPACITY OF BACTERIA TO WITHSTAND THE
EFFECTS OF ANTIBIOTICS OR BIOCIDES THAT ARE
INTENDED TO KILL OR CONTROL

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 HOW ANTIBIOTIC
RESISTANCE HAPPENS
– RESISTANCE GENES  SPONTAN
– RESISTANCE GENES TRANSFER  PLASMID &
EPISOM
• TRANSFORMATION
• TRANSDUCTION
• KONJUGATION
– RESTING PHASE G0
– CROSS RESISTANCE

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MECHANISMS OF ANTIMICROBIAL
RESISTANCE

 ENZYMES PRODUCTION  betalactamase

 INACTIVATION AM  resting
 NEW PATHWAY
 LIMITING UPTAKE  barrier
 MODIFICATION DRUG TARGET  receptor <<

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Antibiotic Consumption

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 SPECIFIC ATTACHMENTS OF BACTERIA TO
HOST CELL OR TISSUE SURFACES
Bacterial ligand for Host cell or tissue
Bacterium attachment receptor Attachment site
Amino terminus of
Streptococcus pyogenes Protein F fibronectin Pharyngeal epithelium
Streptococcus mutans Glycosyl transferase Salivary glycoprotein Pellicle of tooth
Buccal epithelium of
Streptococcus salivarius Lipoteichoic acid Unknown tongue
N-acetylhexosamine-
Streptococcus pneumoniae Cell-bound protein galactose disaccharide Mucosal epithelium
Amino terminus of
Staphylococcus aureus Cell-bound protein fibronectin Mucosal epithelium
N-methylphenyl- alanine Glucosamine-galactose Urethral/cervical
Neisseria gonorrhoeae pili carbohydrate epithelium
Species-specific
carbohydrate(s) (e.g.
Enterotoxigenic E. coli Type-1 fimbriae mannose) Intestinal epithelium
Uropathogenic E. coli Type 1 fimbriae Complex carbohydrate Urethral epithelium
Globobiose linked to
Uropathogenic E. coli P-pili (pap) ceramide lipid Upper urinary tract
Fimbriae ("filamentous Galactose on sulfated
Bordetella pertussis hemagglutinin") glycolipids Respiratory epithelium
N-methylphenylalanine Fucose and mannose
Vibrio cholerae pili carbohydrate Intestinal epithelium
Peptide in outer
Treponema pallidum membrane Surface protein (fibronectin) Mucosal epithelium

Mycoplasma Membrane protein Sialic acid Respiratory epithelium

Conjunctival or urethral
Chlamydia Unknown Sialic acid epithelium 39
 KOMBINASI ANTIMIKROBA

 PENGOBATAN INFEKSI CAMPURAN

 PENGOBATAN AWAL PD INFEKSI BERAT
 ETIOLOGI BLM JELAS
 MENDAPATKAN EFEK SINERGI
 MEMPERLAMBAT RESISTENSI

KOMBINASI TETAP
AS. KLAVUNAMAT-AMOKSISILIN
SULBAKTAM-AMPISILIN

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 ANTIBIOTIC COMBINATIONS

 BACTERICIDAL – BACTERICIDAL

SYNERGY
 BACTERIOSTATIC - BACTERIOSTATIC

ADDITIVE
 BACTERICIDAL – BACTERICIDAL

ANTAGONIS

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 DRUGS INTERACTION
https://reference.medscape.com/drug-interactionchecker

 TETRACYCLINE, FLUOROQUINOLONE –
ANTACIDS (Fe2+, CA2+, Zn, Sulf  CHELATION -
decrease drug absorption
 TETRACYCLINE – COUMARIN (A.C)  abs.VIT. K
<
 BETA-LACTAMS (except Sefolosporin) –
PROBENESID  T ½ >

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 DRUGS INTERACTION
https://reference.medscape.com/drug-interactionchecker

 Liver P 450 : Statins, Cyclosporine, Benzodiazepines,

Theophylline, Anticonvulsants, oral hypoglycemics
– Increasing Concentration of:
• Macrolides (Erythromycin)
• Azoles (Fluconazole, Itraconazole)
• Ciprofloxacin
– Decreased Concentration of:
• Rifampin, rifabutin
 Oral Contraceptives
– Effectiveness  : rifampin & nafcillin +/- others

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 CONCLUSION
Using antibiotics responsibly:
1. Right indication
1. Prophylaxis
2. Therapeutic
1. Empiric: epidemiology data
2. Selected: >>>effective, safety, narrow
spectrum
2. Right drug
3. Right dose
4. Right time
5. Aware to “AE” 44
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