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Antibiotics

Definition Mode of action Examples

Dr.Sami Albaba MSC.Muhammad Hashem

Definition of Antibiotic
A substance of biological, synthetic origin of low molecular weight. produced by a fungus or bacterium as secondary metabolites that inhibits or stop growth of other microorganisms in vitro and in vivo selectively, when it used in low concentration.

Characteristics of Antibiotics
It must be able to reach the part of the human body where the infection is occurring.

Characteristics of Antibiotics
It should not cause the development of resistant forms of parasites.

Characteristics of Antibiotics
It should not produce undesirable side effects in the host such as allergic reaction, nerve damage or irritation of the kidneys and gastrointestinal tract.

Antibiotic Therapy
Before giving any Antibiotics to patient you should know: Identify infecting organism Evaluate drug sensitivity Target site of infection Drug safety/side effect profile Patient factors Cost

Classification of Antibiotics
Bacteriostatic Bactericidal

Classification of Antibiotics
Chemical Structure Spectrum of Activity Mechanism of Action

Mechanism of Action

Inhibitors of Cell Wall Synthesis

Protein Synthesis Inhibitors


Human Ribosome
80S
40S 60S

Bacterial Ribosome
70S
30S 50S

Inhibitors of Metabolism
Sulfonamides Trimethoprim Interfere with the production of folic acid coenzymes that are required for purine and pyrimidine synthesis

Major groups of Antibiotics


Beta-lactam antibiotics .1 1. Penicillins 2. Cephalosporins 3. Carbapenems 4. Monobactams

1. Beta-lactam antibiotics Toxicity Problem

The main toxicity problem with these antibiotics is an allergic reaction that occurs because of formation of beta-lactam/serum protein conjugate that elicits an inflammatory immune response.

1. Beta-lactam antibiotics Mode of Action

The beta-lactam antibiotics inhibit the last step in peptidoglycan synthesis

1. Beta-lactam antibiotics Spectrum


Some are effective against both Grampositive and Gramnegative bacteria whereas others are more effective against Gram-positive than Gram-negative bacteria or vice versa.

1. Beta-lactam antibiotics Example 1.


( Natural penicillins and cephalosporins )

Penicillin G, Cephalothin Biological source Penicillium notatum Cephalosporium species Spectrum (effective against) Gram-positive bacteria Mode of action Inhibits steps in cell wall (peptidoglycan) synthesis.

1. Beta-lactam antibiotics Example 2.


( Semisynthetic penicillin)

Ampicillin, Amoxycillin Spectrum (effective against) Gram-positive and Gram-negative bacteria Mode of action Inhibits steps in cell wall (peptidoglycan) synthesis.

1. Beta-lactam antibiotics Example 3. (Clavulanic Acid )


Clavamox(Aug) is clavulanic acid plus amoxycillin Biological source Streptomyces clavuligerus Spectrum (effective against) Gram-positive and Gram-negative bacteria Mode of action Suicide inhibitor of beta-lactamases

1. Beta-lactam antibiotics Example 5. ( Carbapenems, Carboxypenems )


Imipenem: most broad-spectrum antibacterial drug. Biological source Streptomyces cattleya Spectrum (effective against) Gram-positive and Gram-negative bacteria, and ESBL Mode of action Inhibits steps in cell wall (peptidoglycan) synthesis. Cost: Expensive (example:Tenam)

Example 4. (Monobactams )
Aztreonam: only monobactam available structure. Biological source Chromobacter violaceum Spectrum (effective against) Gram-positive and Gram-negative bacteria Mode of action Inhibits steps in cell wall (peptidoglycan) synthesis and murein assembly.

First generation Cephalosporins


Agent: cefazolin, cephalexin, cefadroxil, cephalothin Good for gram positive, moderate for some enteric gram negative, and poor for enterococci. Second generation Cephalosporins Agent: Cefuroxime, cefdinir, cefotetan, cefaclor, cefoxitin Good for some enteric gram negative, modertae for gram positive, and poor for enterococci. Third generation Cephalosporins Agent: Ceftriaxone, cefotaxime, ceftazidime, cefpodoxime, cefixime. Good for gram positive & negative, poor for MSSA, and poor for enterococci and MRSA.

Fourth generation Cephalosporins Agent: cefepime. Good for MSSA, gram positive & gram negative, moderate for Acinetobacter, and poor for enterococci & MRSA.

Beta-Lactamase inhibitor
Agent: Ampicillin/sulbactam, Amoxicillin/clavulanate, Ticarcillin/clavulanate, Piperacillin/tazobactam.
Good for gram positive & negative, enterococci, and betalactamase except ESBL(Extended Spectrum Beta Lactamase) in this case we use only Carbapenems.

2. Glycopeptides
Another group of peptidoglycan synthesis inhibitors is the glycopeptides, exemplified by vancomycin and teichoplanin.

2. Glycopeptides
Vancomycin Biological source Streptomyces orientales Spectrum (effective against) Gram-positive bacteria, especially Staphylococcus aureus, MSSA, MRSA, enterococci, and poor for gram negative. Mode of action Inhibits steps in murein (peptidoglycan) biosynthesis

3. Aminoglycosides
Members of this group contain sugars and consists of streptomycin, dihydrostreptomycin, neomycin, gentamicin, kanamycin, tobramycin and amikacin.

3. Aminoglycosides
Example 1.
Gentamicin Biological source Micromonospora species Spectrum (effective against) Gram-positive and Gram-negative bacteria esp. Pseudomonas, poor for anaerobes. Mode of action Inhibit translation (protein synthesis)

3. Aminoglycosides
Example 2 Streptomycin Biological source Streptomyces griseus Spectrum (effective against) Gram-positive and Gram-negative bacteria Mode of action Inhibit translation (protein synthesis)

4. Tetracyclines
Tetracyclines consist of eight members, and may be considered as a group of antibiotics, obtained as byproducts from the metabolism of various species of Streptomyces .

4. Tetracyclines
Example 1.( Natural ) Tetracycline (Bacteriostatic) Biological source Streptomyces species Spectrum (effective against) Gram-positive and Gram-negative bacteria, Rickettsias, enterococci, VRE, MRSA, poor for pseudomonas, and proteus. Mode of action Inhibit translation (protein synthesis)

4. Tetracyclines
Example 2. (Semisynthetic tetracycline) Doxycycline Spectrum (effective against) Gram-positive and Gram-negative bacteria, Rickettsias , Borellia Mode of action Inhibit translation (protein synthesis)

5. Macrolides
Macrolides are an ill-defined group representing those antibiotics that have large ring structures containing oxygen.

5. Macrolides
Example Erythromycin Biological source Streptomyces erythreus Spectrum (effective against) H.influenza, Moraxella, H.pylori, Mycobacterium, streptococcus, poor for staph,and enteric gram negtaive. Mode of action Inhibits translation (protein synthesis)

6. Lincosamides
Lincosamides are a family of antibiotics that bind to bacterial 50S ribosomal subunit. They differ considerably from macrolides in structure.

6. Lincosamides
Example Clindamycin Biological source Streptomyces lincolnensis Spectrum (effective against) Gram-positive and anaerobes Gram-negative bacteria. Mode of action Inhibits translation (protein synthesis)

7. Fluoroquinolones
Floroquinolones are a family of antibiotics that interferes with DNA replication. Floroquinolones are bactericidal antibiotics.

Nalidixic acid Ciprofloxacin Norfloxacin Levofloxacin Ofloxacin Good for enteric gram negative, poor for Staph & S.pneumoniae.

8. Rifampin
Rifampin (or Rifampicin) is an antibiotic that inhibits bacterial RNA polymerase by binding to its -subunit. Rifampin is a bactericidal antibiotic.

9. Polypeptides
Example 1 Polymyxin Biological source Bacillus polymyxa Spectrum (effective against) Gram-negative bacteria Mode of action Damages cytoplasmic membranes

9. Polypeptides
Example 2 Bacitracin Biological source Bacillus subtilis Spectrum (effective against) Gram-positive bacteria Mode of action Inhibits steps in murein (peptidoglycan) biosynthesis.

10. Polyenes
Example 1. Amphotericin Biological source Streptomyces nodosus Spectrum (effective against)

Fungi
Mode of action Inactivate membranes containing sterols

10. Polyenes
Example 2. Nystatin Biological source Streptomyces noursei Spectrum (effective against)

Fungi (Candida)
Mode of action Inactivate membranes containing sterols

11. Rifamycins
Examples Rifampicin Biological source Streptomyces mediterranei Spectrum (effective against) Gram-positive and Gram-negative bacteria, Mycobacterium tuberculosis Mode of action Inhibits transcription (eubacterial RNA polymerase)

12. Phenols
Example Chloramphenicol (Bacteriostatic) Biological source Streptomyces venezuelae Spectrum (effective against) Gram-positive and Gram-negative bacteria Mode of action Inhibits translation (protein synthesis)

13. Nitrofurans
Agent: Nitrofurantoin Especial treatment for UTI (E.coli & Klebsiella) Poor for Pseudomonas, Proteus, and some group of gram positive.

Clinical Microbiology
Gram Positive Cocci Gram Positive Bacilli Gram Negative Cocci Gram Negative Bacilli Anaerobes Spirochetes Mycobacteria

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