Presented by: Sheetal Singh M.

sc(Bio-Chem) III Sem Suresh Gyan Vihar University, Jaipur

INTRODUCTION CHARACTERISTICS ANTIBIOTICS RESISTANCE CLASSIFICATION ANTIFUNGAL DRUGS ANTI VIRAL DRUGS

A substance of low molecular weight produced by microorganism as secondary metabolites that inhibit or stop the growth of other micro-organism in vitro and in vivo selectively, when it is used in low concentration.

It must be able to reach the part of the human body where the infection is occurring. It should not cause the development of resistant forms of parasites

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

It should be given orally without inactivation by stomach acid, or by injection (parenterally) without binding to the blood proteins.

Finally, it should have a high level of solubility in the body fluids and be possible to achieve concentrations in the tissue or blood, which are sufficiently high to inhibit or kill the infectious agent.

Bacteria either have pre- existing resistance to drugs or develop resistance. The internal or acquired resistant are identical and can be explained by following reasons Inactivation or modification of drug by bacterial enzyme. Formation of impermeable barrier so that drug can not reach the desired region of action. Changing the target itself so drug cant bind or have an effect on it. DNA transfer of drug resistance from one organism to other by transformation ,transduction or bacterial conjugation. Development of altered metabolic pathway which commit the effect of the drug to be bypassed.

1) 2) 3) 4)

5)

Antimicrobials are classified in several ways.

1. 2.

3.
a) b) c) d)

On basis of spectrum of study. On basis of effect on bacteria. On basis of mode of action Cell wall synthesis inhibitor Protein synthesis inhibitor Nucleic acid inhibitor Other metabolic functions inhibitor

Depending on the range of bacterial species susceptible to these agents, antibacterials are classified as : 1. Broad-spectrum
2.

Narrow- Spectrum Extended -spectrum

3.

Because of differences in the mechanisms by which antibiotics affect bacteria, the clinical use of antibacterials may have very different effects on bacterial agents, leading to an endpoint of either inactivation or actual death of the bacteria.

Bactericidal drugs Bacteriostatic drugs

Different antibiotics have different modes of action, owing to the nature of their structure and degree of affinity to certain target sites within bacterial cells.

-lactam inhibitors
penicillin Penicillin G Penicillin V Oxacillin Cloxacillin cephalosporin carbapenem s PARENETRA Imipenem L Meropenem Cefazolin Cefmetazole Ceftizoxime monobacta ms Aztreonam

other antibiotics
Bacitracin Vancomycin

Dicloxacillin Cefepime

ORAL Cefadroxil Cefaclor

Antimicrobial drug selectively interfere with synthesis of the bacterial cell wall.
The cell wall is made by polymer called peptidoglycan that consist of a glycan unit joined to each other by peptide cross links.

Synthesis occurs in three steps: 1) Occurs in cytoplasm. 2) Inner surface of cytoplasmic membrane. 3) Occurs in peri-plasmic space(in gram negative bacteria).

Protein synthesis is an essential process necessary for multiplication and survival of all bacterial cells. Several types of antibacterial agent s target bacterial protein synthesis by binding either to 30S or 50S subunits of intracellular ribosomes. The result is disruption of normal cellular metabolism of bacteria and leads to death or inhibition of its growth .EXAMPLESAminoglycosides, chloramphenicol, tetracyclines, macrolides, etc.

Some chemotherapeutic agents affect the synthesis of DNA or RNA or can bind to them so that message can not be read and they can block the growth of cell.
INHIBITORS OF FOLATE SYNTHESIS 4th generation trovafloxacin Sulfadiazine, Silver Sulfadiazine, Sulfamethoxazole Mefinide

FLUOROQUINOLONES 1st 2nd 3rd generatio generati n on Ciproflo xacin Gatiflox acin

generation

Nalidixic acid

norfloxac lavoflox in acin

Quinolones inhibit DNA gyrase (also called as topoisomerase) This enzyme introduces negative superhelical turns into duplex DNA using the energy of ATP. Fluoroquinolones enters the bacterium and inhibiyt replication of bacterial DNA by interfering with action of DNA gyrase .

Some antibiotics act on selected cellular processes that are essential for survival of bacterial pathogen. SULFONAMIDES and TIRIMETHOPRIM disrupts folic acid pathway , which is essential step for bacteria to produce precusors important for DNA synthesis.

An antifungal agent is a drug that selectively eliminates fungal pathogens from a host with minimal toxicity to the host. Infectious disease caused by fungi is called MYCOSIS.

CLASSIFICATION Drugs for systemic mycosis Amphotericin B Flucytosine Fluconazole Drugs for sub-cutaneous mycosis Econazol Griseofluvin Nystatin

Different classes of drug target plasma membrane, sterol biosynthesis , DNA biosynthesis and -glucan biosynthesis.

Fungal membranes and sterol biosynthetic enzymes are different enough from ours that these agents kill fungi and not us.

Virus are intracellular parasites that lack independent metabolism and can replicate only within living host cell. Amantadine and - globulin inhibit penetration of cell by virus. Acyclovir is very selective as it remain inactive until phosphorylated by enzymes that are synthesized by virus. Antiretroviral drugs suppress the replication of HIV . Protease inhibitors ,in HIV m-RNA are translated into inert proteins.

 Dixon B .2006 . Sullfas true

significance. Microle 1(11):500-501

Pharmacological module Microbiology Michael J Pelczar