3. antibiotic (protein synthesis inhibitors)

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BY BY Dr. Dr. SAMINATHAN KAYAROHANAM SAMINATHAN KAYAROHANAM M.PHARM, M.B.A, PhD M.PHARM, M.B.A, PhD ANTIBIOTIC (PROTEIN SYNTHESIS INHIBITORS) 1 3

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BYBY

Dr. Dr. SAMINATHAN KAYAROHANAMSAMINATHAN KAYAROHANAM

M.PHARM, M.B.A, PhDM.PHARM, M.B.A, PhD

ANTIBIOTIC (PROTEIN SYNTHESIS

INHIBITORS)

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NUM CONTENT SLIDE 1 INTRODUCTION TO PROTEIN SYNTHESIS 42 PROKARYOTIC AND EUKARYOTIC RIBOSOMES 5 3 GENERAL MECHANISM OF ANTIBIOTIC 6 4 CLASSIFICATION OF PROTEIN SYNTHESIS INHIBITORS 7 5 THERAPEUTIC APPLICATIONS OF TETRACYCLINES 8 6 THERAPEUTIC APPLICATIONS OF MACROLIDES 9 7 THERAPEUTIC APPLICATIONS OF LINEZOLID AND ADMINISTRATION

MACROLIDE ANTIBIOTICS10

8 PROTEIN SYNTHESIS IN RIBOSOMES 119 GENERAL MECHANISM OF PROTEIN SYNTHESIS INHIBITORS 12,13

10 MECHANISM OF TETRACYCLINES 14 11 MECHANISM OF AMINOGLYCOSIDES 15 12 MECHANISM OF ERYTHROMYCIN AND CLINDAMYCIN 1613 MECHANISM OF CHLORAMPHENICOL 1714 MECHANISM OF LINEZOLID 1815 PHARMACOKINETICS OF SOME PROTEIN SYNTHESIS INHIBITORS AND

ADVERSE EFFECTS OF TETRACYCLINE19

16 SOME ADVERSE EFFECTS OF MACROLIDE AND AMINOGLYCOSIDES ANTIBIOTICS

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17 DRUG INTRACTION OF PROTEIN SYNTHESIS INHIBITOR 21

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LEARNING OUTCOME

1. Able to understand the protein synthesis of prokaryotic and eukaryotic.

2. List the common protein synthesis inhibitor drug classification.

3. Abele to demonstrate the general mechanism of common protein synthesis inhibitor.

4. Able to describe the common protein synthesis inhibitor adverse effects.

5. Able to understand the therapeutic application of protein synthesis inhibitor.

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1. INTRODUCTION TO PROTEIN SYNTHESIS A protein synthesis inhibitor is a substance that stops or slows the growth or proliferation of bacterial cells by disrupting the processes to the generation of new proteins by targeting the bacterial ribosome.

Protein synthesis inhibitors usually act at the ribosome level, taking advantage of the major differences between prokaryotic and eukaryotic ribosome structures.

Protein synthesis inhibitors work at different stages of prokaryotic mRNA translation into proteins like initiation, elongation (including aminoacyl tRNA entry, proofreading, peptidyl transfer, and ribosomal translocation), and termination.

Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

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2. PROKARYOTIC AND EUKARYOTIC RIBOSOMES

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3. GENERAL MECHANISM OF ANTIBIOTIC

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4. CLASSIFICATION OF PROTEIN SYNTHESIS INHIBITORS1

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5.THERAPEUTIC APPLICATIONS OF TETRACYCLINES

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6. THERAPEUTIC APPLICATIONS OF MACROLIDES

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7. THERAPEUTIC APPLICATIONS OF LINEZOLID AND ADMINISTRATION MACROLIDE ANTIBIOTICS

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8.PROTEIN SYNTHESIS IN RIBOSOMES

Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

9.GENERAL MECHANISM OF PROTEIN SYNTHESIS INHIBITORS

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9.GENERAL MECHANISM OF PROTEIN SYNTHESIS INHIBITORS

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Tetracyclines binds reversibly to the 30S subunit of the bacterial ribosome, thereby blocking access of the amino acyl-tRNA to the mRNA-ribosome complex at the acceptor site.

By this mechanism, bacterial protein synthesis is inhibited

10. MECHANISM OF TETRACYCLINES

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11. MECHANISM OF AMINOGLYCOSIDES

•Susceptible gram-negative organisms allow aminoglycosides to diffuse through porin channels in their outer membranes.

•oxygen-dependent system that transports the drug across the cytoplasmic membrane.

•The antibiotic then binds to the 30S ribosomal subunit prior to ribosome formation.

•There, it interferes with assembly of the functional ribosomal apparatus and/or can cause the 30S subunit of the completed ribosome to misread the genetic code.

Dr.K.Saminathan.M.Pharm, M.B.A, Ph.D

The macrolides bind irreversibly to a site on the 50S subunit of the bacterial ribosome, thus inhibiting the translocation steps of protein synthesis.

They may also interfere at other steps, such as transpeptidation.

Generally considered to be bacteriostatic, they may be bactericidal at higher doses.

Their binding site is either identical or in close proximity to that for clindamycin and chloramphenicol.

12.MECHANISM OF ERYTHROMYCIN AND CLINDAMYCIN

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Chloramphenicol binds to the bacterial 50S ribosomal subunit and inhibits protein synthesis at the peptidyl transferase reaction.

Because of the similarity of mammalian mitochondrial ribosomes to those of bacteria, protein synthesis in these organelles may be inhibited at high circulating chloramphenicol levels, producing bone marrow toxicity.

13. MECHANISM OF CHLORAMPHENICOL

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The linezolid inhibits bacterial protein synthesis by inhibiting the formation of the 70S initiation complex.

Linezolid binds to a site on the 50S subunit near the interface with the 30S subunit

14. MECHANISM OF LINEZOLID

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15.PHARMACOKINETICS OF SOME PROTEIN SYNTHESIS INHIBITORS AND ADVERSE EFFECTS OF TETRACYCLINE.

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16.SOME ADVERSE EFFECTS OF MACROLIDE AND AMINOGLYCOSIDES ANTIBIOTICS

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17.DRUG INTRACTION OF PROTEIN SYNTHESIS INHIBITOR

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TETRACYCLINE DISCOLORED TEETH

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ACNE TREATMENT

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TETRACYCLINE ACNE TREATMENT

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AMINOGLYCOSIDES ANTIBIOTICS

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