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![Cotrimoxazole
[TRIMETHOPRIM-SULFAMETHOXAZOLE]
• Introduction
• Sulfamethoxazole is a close congener of sulfisoxazole
• A pyrimidine inhibitor of dihydrofolate reductase, it is
an antibacterial related to PYRIMETHAMINE
• Trimethoprim in combination with sulfamethoxazole
constitutes an important advance in the development
of clinically effective antimicrobial agents
• Popularly this combination is various names such as
cotrimoxazole , Bactrim , Septran](https://image.slidesharecdn.com/sulphonamaidesshyam-160811035233/75/Sulphonamaides-and-cotrimoxazole-11-2048.jpg)
![Spectrum
• G + VE
• S. pneumoniae [susceptible, there
has been a disturbing increase in
resistance ]
• Staphylococcus aureus
• Staphylococcus epidermidis
• S. pyogenes
• S. viridans
• MRSA
• G –VE
• E. coli
• Proteus mirabilis
• Proteus morganii
• Proteus rettgeri
• Enterobacter spp
• Salmonella
• Shigella
• Pseudomonas pseudomallei
• Serratia
• Klebsiella spp.
• Brucella abortus
• Pasteurella haemolytica
• Yersinia pseudotuberculosis
• Yersinia enterocolitica](https://image.slidesharecdn.com/sulphonamaidesshyam-160811035233/75/Sulphonamaides-and-cotrimoxazole-16-2048.jpg)
![Available doses
• BACTRIM -TAB [S-400mg T-80 mg] APHL
-TAB [S-100mg T-20mg]
-TAB [S-200mg T-40mg]
• SEPTRAN -TAB [S-400mg T-80 mg] GSK
-TAB [S-100mg T-20mg]
-TAB [S-200mg T-40mg]](https://image.slidesharecdn.com/sulphonamaidesshyam-160811035233/75/Sulphonamaides-and-cotrimoxazole-22-2048.jpg)
Uploaded byNarasimha Kumar G V
Sulphonamaides and cotrimoxazole
Sulfonamides and cotrimoxazole are classes of antibiotics that work by inhibiting the enzyme dihydropteroate synthase, interrupting the biosynthesis of nucleic acids. Cotrimoxazole is a combination of trimethoprim and sulfamethoxazole that have synergistic antibacterial effects through sequential blockade in bacterial folate metabolism. It has broad spectrum activity against both gram-positive and gram-negative bacteria. Common adverse effects include hypersensitivity reactions. The drugs are well absorbed orally and have a volume of distribution that allows penetration into tissues and body fluids.
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Sulphonamaides and cotrimoxazole
- 1. SULFONAMIDES & COTRIMOXAZOLE G Vijay NarasimhaKumar Asst. Professor, Dept. of. Pharmacology Sri Padmavathi School of Pharmacy
- 2. INTRODUCTION • These area class of anti- biotics which acts by inhibition/ interrupting the synthesis of nucleic acids • Although they interfere in the bio-synthesis of nucleic acids they are not genotoxic due to it`s specificity of target Prontosil rubrum Sulphanilamide
- 3. Mechanism of action PABA+ Pteridine Dihydropteroate Unique target sulfon amide s Dihydropteroate synthase
- 4. Chemical properties NH2 SO 2 NH2 Antibacterial activity Solubility character
- 5. CLASIFICATION Based upon durationof action:- Short acting (Sulfadiazine) Intermediate acting (Sulfamethaxozole) Long acting (Sulfamethopyrazine) Based on chemical properties:- Sulfanilamide derivatives (Sulfadiazine) Sulfones (DAPSONE) Miscellaneous (Sulfacetamide)
- 6. Pharmacokinetics Absorption:- Better absorptionorally and also taken through IV route Distribution:- Large volume of distribution Can cross all barriers Highly protein bound Phenytoin toxicity Metabolism:- Metabolism in liver by N-Acetyl trasferase enzyme Excretion:- Through kidney by urine
- 7. Resistance Alterations in theDHPS enzyme & PABA binding site Production of PABA by Bacterial strains Cell membrane permeability of Sulfonamides
- 8. Anti microbial spectrum •G-ve entero bactor sps affect intestine • Sulfadiazine used as *Silver ointment used to treat infection of open wound & burns • Sulfasalazine is not absorbed orally due to this used as suppositories • Genrally given in combination therapy Pyrimithamine + Trimethoprim Protozoal infection Sulfamethaxozole + Trimethoprim Bacterial infection Sulfasalazine SulfaPyridine N-Acetyl salicylic acid Metabolism
- 9. Adverse effects Hypersensitivityreactions Kernicterus Metabolism of sulfonamides Hapten Host tissue protine Immunogenic but not antigenic Antigenic A L Bilirubin A L BilirubinS.A Serum Bilirubin CNSKernicterus
- 10. Steven Jonson syndrome(separation of epidermal layers) Non immune haemolytic anaemia in G-6-PDH deficiency patients Immune complex NecrosisEpithelial cells NADPH G-6-PDH Not available Folate NO Glutathione reductase (Anti- oxident) Energy source for RBC
- 11. Cotrimoxazole [TRIMETHOPRIM-SULFAMETHOXAZOLE] • Introduction • Sulfamethoxazoleis a close congener of sulfisoxazole • A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE • Trimethoprim in combination with sulfamethoxazole constitutes an important advance in the development of clinically effective antimicrobial agents • Popularly this combination is various names such as cotrimoxazole , Bactrim , Septran
- 12. Composition • Cotrimoxazole isan combination of trimethoprim and sulphamethoxazole in the ratio of 1:5 • The reason for selecting these drugs is they have an equal t1/2 of approximately 10 hours • Their mechanism of action help in sequential blockade in the pathway of an obligate enzymatic reaction in bacteria
- 13. Mechanism of action Stepsin folate metabolism blocked by sulfonamides and trimethoprim
- 14. Antibacterial Spectrum andEfficacy • Antibacterial spectrum of trimethoprim is similar to that of sulfamethoxazole • Resistance can develop easily when the individual drugs are used alone • A synergistic interaction between the components of the preparation is apparent even when microorganisms are resistant to sulfonamide with or without moderate resistance to trimethoprim activity.
- 15. However, amaximal degree of synergism occurs when microorganisms are sensitive to both components. The activity of trimethoprim-sulfamethoxazole in vitro depends on the medium in which it is determined; e.g., low concentrations of thymidine almost completely abolish the antibacterial
- 16. Spectrum • G +VE • S. pneumoniae [susceptible, there has been a disturbing increase in resistance ] • Staphylococcus aureus • Staphylococcus epidermidis • S. pyogenes • S. viridans • MRSA • G –VE • E. coli • Proteus mirabilis • Proteus morganii • Proteus rettgeri • Enterobacter spp • Salmonella • Shigella • Pseudomonas pseudomallei • Serratia • Klebsiella spp. • Brucella abortus • Pasteurella haemolytica • Yersinia pseudotuberculosis • Yersinia enterocolitica
- 17. Bacterial Resistance • Resistanceoften is due to the acquisition of a plasmid that codes for an altered dihydrofolate reductase
- 18. Pharmacokinetics • Absorption ;Orally and intravenously well absorbed sulfamethoxazole and trimethoprim are closely but not perfectly matched to achieve a constant ratio of 20:1 in their concentrations in blood and tissues. • The ratio in blood is often greater than 20:1, and that in tissues is frequently less. • After a single oral dose of the combined preparation, trimethoprim is absorbed more rapidly than sulfamethoxazole. • The concurrent administration of the drugs appears to slow the absorption of sulfamethoxazole. • Peak blood concentrations of trimethoprim usually occur by 2 hours in most patients, whereas peak concentrations of sulfamethoxazole occur by 4 hours after a single oral dose. • The half-lives of trimethoprim and sulfamethoxazole are approximately 11 and 10 hours, respectively
- 19. Pharmacokinetics • Distribution ;Distributed well in all body fluids Trimethoprim is distributed and concentrated rapidly in tissues, and about 40% is bound to plasma protein in the presence of sulfamethoxazole. • The volume of distribution of trimethoprim is almost nine times that of sulfamethoxazole. • The drug readily enters cerebrospinal fluid and sputum, About 65% of sulfamethoxazole is bound to plasma protein • Metabolism ; By liver • Execration ; About 60% of administered trimethoprim and from 25% to 50% of administered sulfamethoxazole are excreted in the urine in 24 hours
- 20. Adverse reactions • Similarto that of sulphonamides Therapeutic uses • Uncomplicated lower urinary tract infections • Bacterial Respiratory Tract Infections • Infection by Pneumocystis jiroveci • In G-VE rods infection's • Gastrointestinal Infections • MRSA infections –skin and soft tissue infections
- 21. Contraindications' • Contraindicated topatients with hypersensitivity • Sever renal or hepatic insufficiency • Infants less than 4 weeks • Megaloblastic anemia pregnancy and lactating mother's
- 22. Available doses • BACTRIM-TAB [S-400mg T-80 mg] APHL -TAB [S-100mg T-20mg] -TAB [S-200mg T-40mg] • SEPTRAN -TAB [S-400mg T-80 mg] GSK -TAB [S-100mg T-20mg] -TAB [S-200mg T-40mg]