Introdution to

Antimicrobials agent
Dr.Mohammad Jadaan
Antimicrobials Agents
A chemical substance produce by microorganism (natural
products) which has the capacity to inhibit the growth of
bacteria, fungi, viruses or protozoa. It has a high
chemotherapeutical index to reduce the active process in
organism in a diluted solution.
Classification of antibiotics
1. Based on chemical structures
2. Based on the sources
3. Based on mechanism of action
4. Based on spectrum of action / activity
5. Based on modes of action
Based on chemical structures
1. Groups of sulfonamides: Sulfamethoxazole, sulfadiazine
2. Groups of Penicillin: Penicillin G (Benzylpenicillin),
Penicillin V,Ampicillin, amoxicillin, nafcillin
3. Groups of cephalosporins: cefalotin, cefazolin,
cefamandole, cefuroxime, cefotaxime, ceftriaxone.
4. Groups of aminoglycosides: streptomycin, neomycin,
kanamycin, gentamycin, tobramycin
5. Groups of chloramphenicol: chloramphenicol,
tiamphenicol
6. Groups of tetracyclines: chlortetracycline, oxytetracycline,
doxycycline, minocycline HCl
7. Groups of macrolides: erythromycin, roxithromycin, spiramycin,
azithromycin
8. Groups of polyenes: amphotericin B, nystatin
9. Groups of Lincomycins: lincomycin, clindamycin
10. Groups of polymixins: Polymyxin B, Polymyxin E
11. Groups of sulfon: dafsone
12. Other groups: vancomycin, cycloxerine, bacitracin,
metronidazole
13. Groups of quinolones: nalidixic acid, norfloxacin,
ciprofloxacin, offloxacin
Based on mechanism of action
A. Inhibition of cell wall synthesis leads to the death of
the bacteria lysis (bactericidal effect) penicillin,
cycloserine, vancomycin, bacitracin, cefottaxime,
ceftriaxone.
B. Disruption of cell membrane function, polymyxin
(polymyxin B, polymyxin E), polyenes, nystatin
C. Inhibition of protein synthesis: this antibiotics inhibit
one of the reactions in the process of transcription
➢Inhibition of translation process of microbes
➢Inhibit ribosome on the 30 S subunit(streptomycin,
tetracylines, netilmicin, kanamycin)
➢Inhibit ribosom on the 50 S subunit (chloramphenicol,
clyndamycin, lincomycin)
➢Inhibits the transcription process of microbes (Rifampin,
actinomycin)
D. Inhibits spesific metabolic reaction
➢Inhibits the enzymatic reactions (sulfonamides, INH, PAS,
trimethoprim)
 Based on spectrum of action
❖Broad spectrum: Effective to Gram +, Gram - bacteria,
mycoplasmas, chlamydiae, rickettsiae, sometimes
protozoa (chloramphenicol, tetracyclines)
❖Narrow spectrum: Effective to Gram + / Gram -
bacteria only
(penicillins, cephalosporins, erythromycins, polymyxins)
Mechanisms of resistance
❖Bacteria produce enzymes that destroy the active drugs such
as beta-lactamases which will destroy betalactams antibiotics.
❖Natural resistance :
➢genetic - chromosomal resistance and extrachromosomal
resistance
➢non genetic
❖Genetic resistance happen because of genetic changes
❖Non genetic resistance happen because of antibiotics come
into contact with bacteria which have active metabolism.
Some approaches to solve resistance problems
1. Administration of antibiotics prescription only if the clinical
signs and tests indicated that certain bacteria are the most
probable caused of infection
2. Bacteriologic diagnosis must be sought and susceptibility tests
must be determined
3. Avoid the usage of antibiotics which have been known
resistance in one population
4. Reduce the usage of topical antibiotics, use antiseptics
instead.
5. Limit the period of consuming antibiotics
6.Reduce the usage of prophylactic antibiotics
7.Use narrow spectrum antibiotics
8.Always follow directions for use of antibiotics
9.Prescrible antibiotics based on clinical situation and not on
patient’s will or pharmaceutical advertisements.
❖Rational drug: drugs given after accurate diagnosis. It will be
effective with minimal side effects.
Factors involve in the usage of AB rationally,
effectively and safely.
1. Accurate diagnosis
2. Accurate choices of antibiotics
3. Deliver accurate dose
4. Accurate dosing interval
5. Accurate examinations of patophysiologic conditions of the
patient
❖Factors involve in choosing antibiotics
➢Disease factors
➢Drug factors
➢Recipient factors
Factors involve in choosing antibiotics
1.Disease factors
➢Selective for etiologic bacteria susceptibility test
➢Types and doses depend on location of infection
➢Enough penetrating potentials to cross :
➢blood-brain barrier in
➢abscess walls
Drugs factors Ideal antibiotics :
➢Have a narrow spectrum, affect only to etiologic bacteria
➢Have a bactericidal effect, unless none is sensitive,
bacteriostatic drugs can be delivered
 Ideal antibiotics
➢Effective even in the presence of body fluids exudate, protein
or enzymes.
➢Ability to reach the infected tissue, enough drug
concentration during the span of a dosing interval in blood /
infected area.
➢Do not caused resistance
➢Have a minimal toxic effects for the patient
➢Safe for pregnancy and pediatric patients
➢Low costs
Factors involve in choosing antibiotics
2.Patient factors :
I. Age
II. Genetics
III. Pregnancy
IV. Accompanying diseases
❖Antibiotic prophylaxis: An antibiotic is used to anticipate
infection from certain bacteria which are sensitive to the drug.
❖Goal: To minimize the surgical wound infection, by treating
with antibiotic in lethal concentration for microorganisms at
the beginning of surgery until it finished (done).
Side effects of antibiotics
Allergic reaction : Is a respond in sensitive individual due to the
abnormality in his immune system (Penicillin, Sulfonamides,
Streptomycin)
❖Mild symptoms are skin rashes and itching.
❖Severe symptoms are anaphylactic shock.
Toxic reaction : Can happen in individual depend on the doses
of drugs in the body Hearingdisorder because of gentamycin
❖Manifestation can occur :
➢Temporary and permanently
➢After a prolonged used / acute respond
Antiviral Agents
1. Inhibit viruses coverage
2. Inhibit DNA and RNA synthesis in the viruses
3. Inhibit protein synthesis in the viruses
4. Inhibit specific enzymes activities in the viruses
5. Inhibit the growth of viruses
6. Promote immunity system of the body
Antifungal Agents
❑Fungal infection occur less frequently than bacterial or viral
infections.
Three major groups of antifungal agents :
1. Groups of polyenes :
➢Amphotericin B
➢Nystatin
2. Groups of Azole Imidazoles : Ketoconazole, Miconazole,
Clotrimazole ,Fluconazole, Itraconazole
3.Groups of Alilamin:
➢Terbinafin
➢Naftitin
❖Other antifungal agents :
➢Griseofulvin
➢Flucytosine