Antibiotics 1

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Chemotherapeutic Agents

Prepared by

Dr. Sibbala Subramanyam,


Assistant professor
Dept. of Pharmaceutical Chemistry,
College of Health Sciences
Haramaya University

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Chemotherapy
The use of drugs to treat a disease

Paul Ehrlich introduced the term


chemotherapy in 1907
Alexander Fleming
The world's first antibiotic substance
benzylpenicillin (Penicillin G) from the mould
Penicillium notatum in 1928, for which he secured
the Nobel Prize in Physiology or Medicine in 1945

‘” Antibiotics are defined as chemical substances produced by


various species of microorganisms such as bacteria and fungi,
which in low concentrations destroy, kill or inhibit the growth of
other species of microorganisms.”

Greek words anti = against ; bios = life


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CLASSIFICATION OF Antibotics

Antibiotics s are classified in several ways, including:


 1 Based on source
 2.Spectrum of activity
 3.Mode of action
 4.Chemical nature
 5.Mechanisam of action
 6.Based on pharmacological action

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Classification of Antibiotics
Based on mode
of Action

Bacteriostatic Bactericidal

Based on their
spectrum of
action

Narrow
Broad-spectrum
Spectrum
2.Based on spectrum of activity
Narrow Spectrum: have limited activity and are primarily only useful
against particular species of microorganisms.
bacitracin are only effective against Gram-positive bacteria,
Polymixins -only effective against Gram negative bacteria.
Broad spectrum antibacterials are active against both Gram-
positive and Gram-negative organisms. Examples include:
tetracyclines, fluoroquinolones, Ampicillin,
Chloramphenicol,sulfonamides.
3. Mode of action(Type of Action)
Bacteriostatic - Antimicrobial agents that reversibly inhibit
growth of bacteria are called as bacteriostatic
(Tetracyclines, Chloramphenicol, Erythromycin, Sulphonamides)
Bactericidal – these drugs kills the microorganisam
(Penicillin, vancomycin, Isoniazide, Aminoglycosides)
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4.Chemical Classification of Antibiotics
 Beta lactam antiobiotics: Penicillins and
cephalosporins( cephalexin)
 Fluoroquinolones: Levofloxacin, Norfloxacin
 Aminoglycosides: Gentamicin, Kanamycin,streptomycin
 Macrolides: Erythromycin, Azithromycin
 Tetracyclines: Tetracycline, chlortetracycline
 Nitrobenzene derivative: Chloramphenicol
 Lincosamide antibiotics: Lincosamide,Clindamycin
 Polypeptide antibiotics :Polymixin-B,Bacitracin,polyenes
 Polyenes :Nystatin,Amphotericin-B
 Glycopeptideantibiotiics: Vancomycin
Streptogramins -DalfoPristin
2,4-diaminopyrimidine- . Quinu Pristine
Trimethoprim,pyrimethamine
Oxazolidine-2-one - Linezolid 8
1. Drugs Inhibiting of cell wall synthesis-( Bactericidal)
 By inhibiting cell wall of bacteria------pencillins, cephalosporins, vancomycin( bacteria)
Isoniazide(mycobacteria), Caspofungin,micafungin (fungi)

2. Drugs inhibiting cell membrane function: ( Bactericidal)


 Polymyxin, Polyenes
3. Drugs inhibiting nucleic acid synthesis(bactericidal)
Drugs inhibiting RNA synthesis- Rifampicin
Drugs inhibiting DNA synthesis- Metronidazole, Fluroquinolones
4.Drugs inhibiting folic acid synthesis: (Bacteriostatic)
Sulfonamides,PAS, Dapsone Trimethoprim, Pyrimethamine
5 Drugs inhibits Mycolic acid synthesis -- Isoniazide, Pyrazinamide, Ethionamide
6. Drugs inhibiting celldivision or mitosis: ( AntiMiitotic drugs)
Vincristine, Griseofulvin
7.Drugs inhibiting Protein synthesis:Bactriostatic except
( aminoglycosides( bactericidal)
By blocking to 30Sribsomes: -Aminoglycosides, Tertacyclines
By blocking to 50 S ribosome: Chloramphenicol,Clindamycin,Erythromycin,linezolid,
CLASSIFICATION OF ANTIBACTERIAL AGENTS
Cont…..

Polymixin B, Nystatin,
Amphotericin
 Based on pharmacological activity

1 ANTI-TB Antibiotic--- - Isoniazide (INH),Rifampicin


2 ANTI-Fungal antibiotic– Griseofulvin and
Polyenes( natamycin,amphotericin –B)
3 ANTI-Cancer Antibitics –Vinca alkaloides-
Vincristine,Vinblastine
4 -Anti-malarial antibiotics-Pyrimethamine,Trimethoprim
5- Anti-leprotic antibiotics- Dapsone, Rifampicin
Adverse effects of antibiotics
S. Antibiotic Adverse effect
No
1 Aminoglycosides Ototoxicity, Nephrotoxicity
2 Tetracyclins Teeth Discoluration, Liverfailure
3 Chlormphenicol Gray baby syndrome and
Bonemarrow depression
4 Isoniazide Nephrotoxicity, Hepatotoxicity
5 Sulphonamides Steven Johnson syndrome, kernicterus

6 Pencillin & cephalosporins Hypersensitivity

7 Vancomycin Neurotoxicity,Redmansyndrome
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Antibiotic resistance
Antibiotic resistance is the ability of bacteria to
resist the effects of an antibiotic.
Antibiotic resistance occurs when bacteria
change in a way that reduces the effectiveness of
drugs The bacteria survive and continue to
multiply, causing more harm.
MECHANISMS OF ANTIBACTERIAL RESISTANCE

1.Inhibition of drug uptake or blocking the


entry
2. Produce enzymes that destroy the chemical
structures of drugs
Ex- Bactria produce beta lactamse enzymes .it
inactvates Beta lactam antibiotics
3.Alter or modified the target molecule.
4. Active efflux of the drug from cell
b -lactamase against penicillins and
cephalosporins
 Acetyltransferase against
chloramfenicol
 Phosphorilase, acetylase and
adenylase againstaminoglycosides
PREVENTION OF ANTIBIOTIC RESISTANCE

Don’t take antibiotics for a viral infection like a cold


or the flu.
Do not save any antibiotics for the next time you get
sick. Discard any leftover medication once you have
completed your prescribed course of treatment
Take an antibiotic exactly as the healthcare provider
tells you. Do not skip doses.
Never pressure your doctor to prescribe an
antibiotic.
Contraindications of antibiotics during
pregnancy
The following drugs should not be given during pregnancy
for treatment of bacterial infection

S A F E T Y P M & CM
S- Sulfonamides
A- Amino glycosides ( streptomycin,Kanamycin)
F- Fluroquinolones- Ciprofloxacin
E- Macrolides– Erythromycin
T- Tetracyclines
Y- ClindmY cin
P- Primaquine only ( not chlorquine)
M- Mebendazole, Misoprostol
C-chloramphenicol
M-Metronidazole
Contraindications of antibiotics during pregnancy
• S A F ET YPM &
CM
• Safe during pregnancy
S- Sulfonamides • PCM
A- Amino glycosides • Penicillin
( streptomycin,Kanamycin)
F- Fluroquinolones- Ciprofloxacin • Cephalosporons
E- Macrolides– Erythromycin • Macroliodes
T- Tetracyclines
Y- ClindmY cin
P- Primaquine only ( not
chlorquine)
M- Mebendazole, Misoprostol
C-chloramphenicol

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