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Chemotherapy
Chemotherapy
1. Chemo : Chemical
2. Therapy: Treatment to cure disease or
disorder
The term chemotherapy was coined
by Paul Ehrlich ( Father of
Chemotherapy)
Chemotherapy is use of chemicals to
treat disease; more specifically to kill
microorganisms and cancer cells
Magic Bullet Paul Ehrlich
Salvarsan(Arsphenamine) : An arsenical
compound and the first effective treatment
for syphilis ( Treponema pallidum)
Chemotherapy
Antibiotics
Substances that are
of biological origin
Chemotherapeutic agents
Synthetic chemical
Drug Resistance
Drug resistance is the reduction in
effectiveness of a medication or drug to
cure a disease or condition. More
commonly, antimicrobial resistance.
It is the ability of microbes, such as
bacteria, viruses, parasites, or fungi, to
survive in the presence of a chemical drug
that that was previously effective in
killing it or inhibiting its growth.
Kabhi Kabhi lagta
hai….Apunnhi Bhgawan hai
How do they do it ?
Antimicrobial Agents
Sulphonamides
&
Trimethoprim
Fluoroquinolones
Nitrofurantoin
Penicillins Cephalosporins
Antimicrobial Agents
Tetracyclines
Chloramphenicol
Macrolides
Aminoglycosides Clindamycin
History of Sulphonamides(1932) German Pathologist : Gerhard Domagk
Prontosil
● Azo Dye
● Chemically it is ; Sulfonamido-chrysoidine
● It's a Prodrug
Prontosil (Prodrug) Sulphanilamide (Active)
Antimicrobial Agents : Sulphonamides
First antimicrobial agent
effective against Pyogenic
bacterial infection
Mechanism of action
Dihydropteroate synthase
Glutamic acid
Classification
Short acting : Sulfadiazine (4-8 Hours)
Intermediate acting : Sulfamethoxazole ( 8-12 Hours)
Long acting : Sulphadoxine (7 days)
Special Purpose : 1.Sulfacetamide sodium (Eye infection)
2. Mafenide (Skin infection)
3. Silver sulfadiazine ( Skin infection)
4. Sulfasalazine (Rheumatoid arthritis and Ulcerative colitis-IBD)
DAPSONE : Used in leprosy
COTRIMOXAZOLE (1 : 5) : Trimethoprim + Sulfamethoxazole
Combination therapy : Cotrimoxazole
Dihydropteroate synthase
Glutamic acid
Uses
1. Eye infection
2. Skin infection
3. GIT infection
4. Meningitis
5. Urinary tract infection
6. Leprosy
7. Respiratory tract infection
8. Malaria
Side effects
1. Steven Johnson syndrome/Skin rashes
2. Urticaria or Crystalluria
3. Leucopenia (Decrease in WBC count)
4. Folic acid deficiency
5. Aplastic anemia (Damage to bone marrow)
6. Hypersensitivity (Allergy)
7. Hepatitis
8. Kernicterus (Brain damage in newborn)
Antimicrobial Agents : Quinolones
Synthetic antimicrobials active
against Gram negative bacteria
First synthetic quinolone derivative : Nalidixic acid (1960)
Use: Urinary antiseptic
Demerits: Low potency, Low tissue penetration,Restricted
spectrum,Highly susceptible to bacterial resistance
Adverse effects : Headache, Vertigo, Visual disturbance
Fluoroquinolones
● Second generation fluoroquinolones : Norfloxacin, Ciprofloxacin, Ofloxacin, Pefloxacin, Lomefloxacin
● Third generation Fluoroquinolones : Levofloxacin, Moxifloxacin, Gemifloxacin, Prulifloxacin,
Sparfloxacin
● Fourth generation : Trovafloxacin
● High potency
● Expanded spectrum
● Slow development of resistance
● Better penetration
Mechanism of action
DNA gyrase
R.I.P
Fluoroquinolone
Blocks DNA Synthesis
Side effects
Uses
1. Gonorrhoea (N.Gonorrhoeae)
2. Conjunctivitis
3. Typhoid (S.typhi)
4. GIT infection
5. Meningitis
6. Urinary tract infection
7. Respiratory tract infection
8. Pneumonia
9. TB (M.Tuberculosis)
Nausea
Vomiting
Anorexia
Dizziness
Headache
Insomnia
Hypersensitivity
Antimicrobial Agents : Tetracyclines
Broad spectrum antibiotics obtained
from Soil microorganisms.
Streptomyces(Actinomycetes)
species:
Gram positive bacteria
1st Tetracycline compound :
Chlortetracycline(1948)
Source : Streptomyces aureofaciens
Features : Bitter solids, Slightly water soluble,
Unstable in aqueous solution
Ribosomes
70S ribosomes
Larger unit 50S
Smaller unit 30S
80S Ribosomes
Mechanism of action
Tetracycline
Protein synthesis blocked which
leads to death of microorganism
Classification
Short acting :
Oxytetracycline : S. rimosus
Tetracycline : Semisynthetic
Intermediate acting :
Demeclocycline : Streptomyces aureofaciens
Long acting :
Doxycycline : Semisynthetic
Minocycline : semisynthetic
Photosensitivity
And Diabetes
insipidus
Tooth discoloration
(Abnormal tooth colour)
Ototoxicity and renal
toxicity
Uses
1. Plague
2. Cholera
3. Urinary tract infection
4. Sexually transmitted diseases
5. Ulcers
6. Relapsing fever
7. Pneumonia
To be continued……………

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Chemotherapy

  • 2. Chemotherapy 1. Chemo : Chemical 2. Therapy: Treatment to cure disease or disorder The term chemotherapy was coined by Paul Ehrlich ( Father of Chemotherapy) Chemotherapy is use of chemicals to treat disease; more specifically to kill microorganisms and cancer cells
  • 3. Magic Bullet Paul Ehrlich Salvarsan(Arsphenamine) : An arsenical compound and the first effective treatment for syphilis ( Treponema pallidum)
  • 4. Chemotherapy Antibiotics Substances that are of biological origin Chemotherapeutic agents Synthetic chemical
  • 5. Drug Resistance Drug resistance is the reduction in effectiveness of a medication or drug to cure a disease or condition. More commonly, antimicrobial resistance. It is the ability of microbes, such as bacteria, viruses, parasites, or fungi, to survive in the presence of a chemical drug that that was previously effective in killing it or inhibiting its growth. Kabhi Kabhi lagta hai….Apunnhi Bhgawan hai
  • 6. How do they do it ?
  • 9. History of Sulphonamides(1932) German Pathologist : Gerhard Domagk Prontosil ● Azo Dye ● Chemically it is ; Sulfonamido-chrysoidine ● It's a Prodrug
  • 11. Antimicrobial Agents : Sulphonamides First antimicrobial agent effective against Pyogenic bacterial infection
  • 12. Mechanism of action Dihydropteroate synthase Glutamic acid
  • 13. Classification Short acting : Sulfadiazine (4-8 Hours) Intermediate acting : Sulfamethoxazole ( 8-12 Hours) Long acting : Sulphadoxine (7 days) Special Purpose : 1.Sulfacetamide sodium (Eye infection) 2. Mafenide (Skin infection) 3. Silver sulfadiazine ( Skin infection) 4. Sulfasalazine (Rheumatoid arthritis and Ulcerative colitis-IBD) DAPSONE : Used in leprosy COTRIMOXAZOLE (1 : 5) : Trimethoprim + Sulfamethoxazole
  • 14. Combination therapy : Cotrimoxazole Dihydropteroate synthase Glutamic acid
  • 15. Uses 1. Eye infection 2. Skin infection 3. GIT infection 4. Meningitis 5. Urinary tract infection 6. Leprosy 7. Respiratory tract infection 8. Malaria Side effects 1. Steven Johnson syndrome/Skin rashes 2. Urticaria or Crystalluria 3. Leucopenia (Decrease in WBC count) 4. Folic acid deficiency 5. Aplastic anemia (Damage to bone marrow) 6. Hypersensitivity (Allergy) 7. Hepatitis 8. Kernicterus (Brain damage in newborn)
  • 16. Antimicrobial Agents : Quinolones Synthetic antimicrobials active against Gram negative bacteria First synthetic quinolone derivative : Nalidixic acid (1960) Use: Urinary antiseptic Demerits: Low potency, Low tissue penetration,Restricted spectrum,Highly susceptible to bacterial resistance Adverse effects : Headache, Vertigo, Visual disturbance
  • 17. Fluoroquinolones ● Second generation fluoroquinolones : Norfloxacin, Ciprofloxacin, Ofloxacin, Pefloxacin, Lomefloxacin ● Third generation Fluoroquinolones : Levofloxacin, Moxifloxacin, Gemifloxacin, Prulifloxacin, Sparfloxacin ● Fourth generation : Trovafloxacin ● High potency ● Expanded spectrum ● Slow development of resistance ● Better penetration
  • 18. Mechanism of action DNA gyrase R.I.P Fluoroquinolone Blocks DNA Synthesis
  • 19. Side effects Uses 1. Gonorrhoea (N.Gonorrhoeae) 2. Conjunctivitis 3. Typhoid (S.typhi) 4. GIT infection 5. Meningitis 6. Urinary tract infection 7. Respiratory tract infection 8. Pneumonia 9. TB (M.Tuberculosis) Nausea Vomiting Anorexia Dizziness Headache Insomnia Hypersensitivity
  • 20. Antimicrobial Agents : Tetracyclines Broad spectrum antibiotics obtained from Soil microorganisms. Streptomyces(Actinomycetes) species: Gram positive bacteria 1st Tetracycline compound : Chlortetracycline(1948) Source : Streptomyces aureofaciens Features : Bitter solids, Slightly water soluble, Unstable in aqueous solution
  • 21. Ribosomes 70S ribosomes Larger unit 50S Smaller unit 30S 80S Ribosomes
  • 22. Mechanism of action Tetracycline Protein synthesis blocked which leads to death of microorganism
  • 23. Classification Short acting : Oxytetracycline : S. rimosus Tetracycline : Semisynthetic Intermediate acting : Demeclocycline : Streptomyces aureofaciens Long acting : Doxycycline : Semisynthetic Minocycline : semisynthetic Photosensitivity And Diabetes insipidus Tooth discoloration (Abnormal tooth colour) Ototoxicity and renal toxicity
  • 24. Uses 1. Plague 2. Cholera 3. Urinary tract infection 4. Sexually transmitted diseases 5. Ulcers 6. Relapsing fever 7. Pneumonia