Antibiotics

Antibiotics
The word antibiotic comes from the Greek anti meaning 'against' and bios meaning 'life' (a bacterium is a life form). Any chemical or drug used to treat an infectious disease, either by inhibiting or killing the pathogens Antibiotics are also known as antibacterial, and they are drugs used to treat infections caused by bacteria.

History of Antibiotics
Over 2,500 years ago, Chnese medicine used plants with antibiotics properties. Many other cultures, including Egyptians, Greeks and medieval Arabs used moulds and plants to treat infections In 19th scientists observed that a bacillus could inhibit the growth of another Alexander Fleming discovered Penicillin in 1928. Penicillin has antibacterial activity against a wide range of bacteria Alexander Fleming was awarded with the Nobel Prize in Medicine in 1945, shared with another two scientists

History of Antibiotics
Year introduced 1935 1941 1944 1945 1949 Class of drug Sulphonamides Penicillins Aminoglycosides Cephalosporins Chloramphenicol

1950
1952 1956 1957 1959 1962 1968 2000 2003

Tetracyclines
Macrolides/lincosamide s/streptogramins Glycopeptides Rifamycins Nitroimidazoles Quinolones Trimethoprim Oxazolidinones Lipopeptides

Antibiotics Classification
1. According to Source 1. Natural a. Fungi penicillin, griseofulvin b. Bacteria Bacillus sp. (polymixin, bacitracin) ; Actinomycetes (tetracycline, chloramphenicol, streptomycin) 2. Synthetic

Antibiotics Classification
2. According to antimicrobial activity
1. 2. Bactericidal Bacteriostatic
e.g. Penicillins, Cephalosporins, Aminoglycosides, Fluoroquinolones, Nitroimidazoles

e.g. Tetracyclines, Chloramphenicol, Macrolides and lincosamides, Sulfonamides

3. According to bacterial spectrum of activity

1. Narrow spectrum
e.g. Azithromycin, Clarithromycin, Clindamycin, Erythromycin, Vancomycin

2.

Broad spectrum

e.g. Amoxicillin, Imipenem, Levofloxacin, gatifloxacin, Streptomycin, Tetracycline, Chloramphenicol, Ampicillin

Antibiotics Classification
4. According to absorbability from the site of administration and treatment
1. Locally acting 2. Systemic

Antibiotics Classification
5. According to mechanism of action 1. INHIBITION OF CELL WALL SYNTHESIS
e.g. Penicillins, Cephlalosporins

2. INHIBITION OF PROTEIN SYNTHESIS e.g. Aminoglycosides, Tetracyclines, Chloramphenicol, Macrolides and

lincosamides
3. INHIBITION OF NUCLEIC ACID SYNTHESIS

e.g. Fluoroquinolones, Nitroimidazoles

4. INHIBITION OF BACTERIAL GROWTH

e.g. Sulfonamides

Antibiotics Classification

Ideal Qualities of Antibiotic

1. Kill or inhibit the growth of pathogens

2. Cause no damage to the host

3. Cause no allergic reaction to the host 4. Stable when stored in solid or liquid form 5. Remain in specific tissues in the body long enough to be effective 6. Kill the pathogens before they mutate and become resistant to it

Antibiotic Facts
Antibiotics are medicines used to treat infections caused by bacteria only. Most patients are prescribed antibiotics without the doctor knowing the cause of the infection. Colds and coughs are caused by viruses not bacteria, so antibiotics will not help.

Antibiotic Facts
Antibiotics are generally active against multiplying bacteria, but are much less effective against nonreplicating (latent) bacteria.

Antibiotic Facts
Antibiotics can't distinguish between the "good" and the "bad" bacteria
There is a delicate balance of billions of bacteria inside our digestive tract. Also in the large intestine and acidophilus in the small intestine and vagina protect against infection by yeast and other bad bacteria. Also "friendly" bacteria found on the skin protect against bad bacteria, yeast and fungal infections. Continued use of antibiotics, especially broad-spectrum antibiotics, can seriously disrupt the normal ecology of the body and render anyone more susceptible to pathogenic (disease causing) bacteria, yeast, viral and parasitic infection.

Antibiotic Facts
Antibiotics are not completely metabolized in the body and are released as active compounds into the environment
Many antibiotics are stable chemical compounds that are not broken down in the body, but remain active long after being excreted. At present, antibiotics make a considerable contribution to the growing problem of active medical substances circulating in the environment.

Antibiotic Facts
The dosage is a very important factor in antibiotic effectiveness
If the dosage of the antibiotic is not adequate, it will not be effective for treatment of the infection and bacteria are more likely to develop resistance. This is because the bacteria can continue to grow and develop ways to disrupt the antibiotic's effects.

Antibiotic Facts
Antibiotics may interfere with immune system development
Children who are given broad-spectrum antibiotics before two years of age are three times more likely to develop asthma than are children who are not given such antibiotics
Ref- 1. Kozyrskyj AL, Ernst P, Becker AB. Increased risk of childhood asthma from antibiotic use in early life. Chest. 2007 Jun;131(6):1753-9. PubMed 2. Early life exposure to antibiotics and the subsequent development of eczema, wheeze, and allergic sensitization in the first 2 years of life: the KOALA Birth Cohort Study. Pediatrics. 2007 Jan;119(1):e225-31.

Antibiotic Facts
Antibiotics are life-savers
Antibiotics have saved countless lives worldwide. When antibiotics were first used to treat bacterial infection they were hailed as the greatest lifesavers of all time. Before penicillin was discovered, infections were a leading cause of death. In 1900, the three leading causes of death were pneumonia, tuberculosis (TB), and diarrhea and enteritis, which (together with diphtheria) caused one third of all deaths6.

Antibiotic Resistance
When bacteria are exposed to the same antibiotics over and over, the bacteria can change and are no longer affected by the drug

Susceptible bacteria can acquire resistance to antimicrobials by either Genetic Mutation or Accepting antimicrobial resistance Genes from other bacteria.

Antibiotic Resistance
This usually occurs through of several biochemical mechanism. Mutation Destruction or Inactivation Efflux

Antibiotic Resistance Mutation

Mutation is a change in the DNA that sometimes cause a change in the Gene product, which is the target of antimicrobial.

Antibiotic Resistance Destruction or Inactivation

Many bacteria possesses the genes which produce enzyme that chemically degrade or deactivate antimicrobials.

Antibiotic Resistance Efflux

Antibiotic Resistance Conjugation

Conjugation is mediated by a particular kind of circular DNA called plasmid, which is replicated independently of the chromosomes.

Antibiotic Resistance Transformation

During this process genes are transferred from one bacterium to another as DNA.

Antibiotic Resistance Transduction

Bacterial DNA is transferred from one bacterium to another inside a virus that infects bacteria.

Antibiotic Resistance Mechanism

Factors affecting Antibiotic Resistance

1. Administration of antimicrobials when not needed. 2. Lack of /improper adherence to regimens. 3. Dosing that does not maintain adequate drug levels.

Cell Wall Synthesis Inhibitors

Beta Lactams
Penicillins
1. Natural (nature-made) Penicillin G (oral) Penicillin V (IV) 2. Penicillinase Resistant Methicillin Cloxacillin Dicloxacillin Nafcillin Oxacillin 3. Aminopenicillins Amoxicillin Ampicillin 4. Extended Spectrum Azlocillin Carbenicillin Mezlocillin Piperacillin Ticarcillin

Polypeptides
Vancomycin Bacitracin Fosfomycin Daptomycin

Cephalosporins
1. First Generation Cefazolin Cephalexin 2. Second Generation Cefaclor Cefamandole Cefoxitin 3. Third Generation Cefotaxime Ceftazidime Ceftriaxone 4. Fourth Generation Cefepine Cefpirone

Carbapenems
Imipenem + cilastatin Ertapenem Meropenem

Monobactams
Aztreonam