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SULPHONAMIDES
SUBMITTED TO:
Ms. Neelam Painuly
Associate Professor
Sopr.Neelam@dbuu.ac.in
Sopr,DBUU, Dehradun
SUBMITTED BY:
Vijaya Laxmi
Student, M.pharm (Pharmacology)
Vijaya2562002@gmail.com
Sopr, Dbuu, Dehradun
1. Introduction and History
2. Classification
3. Mechanism of action and Drug resistance
4. Pharmacokinetics
5. Adverse effect
6. Therapeutic uses
7. References
INDEX
• These are a class of Anti-biotic. As an AMA, it is the first antimicrobial agent.It works well to treat infections caused
by pyrogenic bacteria.
• Structurally and Chemically related to Para aminobenzoic acid (PABA)
• Against numerous gram positive and gram negative bacteria, these are mostly bacteriostatic agents.
History:-
• Gerhard Domagk discovered the first sulphonamide in 1935.Ater 4 year he received Novel prize.
• One of the dyes included by Domagk to cure experimental streptococcal infection in mice was proven to be quite
effective: protosil (sulphonamido-chrysodine).
• Afterwards an infant was cured of staphylococcal septicaemia by prontosil.
Introduction
CLASSIFICATION
Systemic – acting agents Long – acting agents Others
Sulphasalazine
Acts both locally and
systemically
Sulphacetamide
silver sulphadiazine
Mefenide
Systemic- acting (4-8 h) :-
Sulphadiazine
Intermediate-acting (8- 12h) :-
Sulphamethaoxazole
Long- acting (≥7days) :- Sulphadoxine
• Para-aminobenzoic acid, or PABA, is
necessary for the growth and
proliferation of numerous bacteria and
is a precursor to folic acid. PABA and
sulfonamides share a structural
similarity.
• Folate synthase enzyme is
competitively inhibited, which stops
folic acid from forming.
• These have the effect of being
bacteriostatic.
Para-aminobenzoic acid (PABA)
Dihydrofolic acid (DHFA)
Tetrahydrofolic acid (THFA)
Folate synthetase
Dihdrofolate reductase
Sulphonamides
Inhibit
Mechanism of action
• Decreased affinity of folate synthetase.
• Drug efflux caused by bacteria.
• Creation of a different metabolic route for the production of
folate.
Pharmacokinetics:-
• Absorption –The gut absorbs all systemic-acting sulphonamides efficiently.
They are attached to plasma proteins, especially those found in albumin.
• Distribution- They are found in practically every bodily tissue, including the CSF. They pass through the
placenta and enter the fetal circulation..
Bacterial Resistance to Sulphonamides
• Excretion- partially eliminated unaltered and partially as metabolic products
• Quickly absorbed orally and eliminated through the urine.
• Between 20 and 40 percent of plasma protein binding is acetylated.(Crystalluria is likely because
acetylated derivatives are less soluble in urine.)
• Its penetration into the brain and CSF is good.
Sulphamethaoxazole
• Slow to absorb orally and excrete in the urine (mid duration of action)
• Which are relatively insoluble _ Crystalluria can occur.
Sulphadiazine
Sulphadoxine, Sulphamethopyrazine
• Slow renal excretion and high binding of plasma proteins
• It is used topically for ocular infection.
• Highly soluble compound.
Mefenide
• This isn't your normal sulphonamide. It is limited to topical usage and inhibits both gram-positive
and gram-negative bacterial growth.
Adverse effect
• On urinary system
• On haemopoietic system – Bone marrow depression, Aplastic anaemia.
• On gastrointestinal tract – Vomiting, diarrhea, nausea.
• Hypersensitivity reaction – Skin rashes, anaphylaxis, steven Johnson.
Sulphacetamide sod.
1. Sulphamethaoxazole in combination with trimethoprim is used in the treatment of P. jiroveci infection
in patients with AIDS.
2. Rheumatic feverInflammatory bowel disease
3. Opthalmic infection.
Indication-Typhoid and paratyphoid feverAcute and chronic urinary tract infection.Bacillary
dysenteryDermatitis.
Therapeutic Uses
Contraindication
In Pregnancy- Use of Sulphonamides in the first trimester of pregnancy might be associated with Congenital
malformations.
• Since sulphonamides displace bilirubin from protein-binding sites in newborns, it is not recommended to use
them in infants younger than two months.
References
• Text book of Pharmacology for medical graduates by V
Shanbhag Tara and Shenoy Smita , Fourth edition , page no.
375-377
• Text book of Essential of pharmacology by Tripathi KD ,
Seven edition ,new delhi , page no. 704-706.
• https://www.slideshare.net/raselmahbub1/sulfonamide

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Sulphonamides, mechanisms and their uses

  • 1. SULPHONAMIDES SUBMITTED TO: Ms. Neelam Painuly Associate Professor Sopr.Neelam@dbuu.ac.in Sopr,DBUU, Dehradun SUBMITTED BY: Vijaya Laxmi Student, M.pharm (Pharmacology) Vijaya2562002@gmail.com Sopr, Dbuu, Dehradun
  • 2. 1. Introduction and History 2. Classification 3. Mechanism of action and Drug resistance 4. Pharmacokinetics 5. Adverse effect 6. Therapeutic uses 7. References INDEX
  • 3. • These are a class of Anti-biotic. As an AMA, it is the first antimicrobial agent.It works well to treat infections caused by pyrogenic bacteria. • Structurally and Chemically related to Para aminobenzoic acid (PABA) • Against numerous gram positive and gram negative bacteria, these are mostly bacteriostatic agents. History:- • Gerhard Domagk discovered the first sulphonamide in 1935.Ater 4 year he received Novel prize. • One of the dyes included by Domagk to cure experimental streptococcal infection in mice was proven to be quite effective: protosil (sulphonamido-chrysodine). • Afterwards an infant was cured of staphylococcal septicaemia by prontosil. Introduction
  • 4. CLASSIFICATION Systemic – acting agents Long – acting agents Others Sulphasalazine Acts both locally and systemically Sulphacetamide silver sulphadiazine Mefenide Systemic- acting (4-8 h) :- Sulphadiazine Intermediate-acting (8- 12h) :- Sulphamethaoxazole Long- acting (≥7days) :- Sulphadoxine
  • 5. • Para-aminobenzoic acid, or PABA, is necessary for the growth and proliferation of numerous bacteria and is a precursor to folic acid. PABA and sulfonamides share a structural similarity. • Folate synthase enzyme is competitively inhibited, which stops folic acid from forming. • These have the effect of being bacteriostatic. Para-aminobenzoic acid (PABA) Dihydrofolic acid (DHFA) Tetrahydrofolic acid (THFA) Folate synthetase Dihdrofolate reductase Sulphonamides Inhibit Mechanism of action
  • 6. • Decreased affinity of folate synthetase. • Drug efflux caused by bacteria. • Creation of a different metabolic route for the production of folate. Pharmacokinetics:- • Absorption –The gut absorbs all systemic-acting sulphonamides efficiently. They are attached to plasma proteins, especially those found in albumin. • Distribution- They are found in practically every bodily tissue, including the CSF. They pass through the placenta and enter the fetal circulation.. Bacterial Resistance to Sulphonamides • Excretion- partially eliminated unaltered and partially as metabolic products
  • 7. • Quickly absorbed orally and eliminated through the urine. • Between 20 and 40 percent of plasma protein binding is acetylated.(Crystalluria is likely because acetylated derivatives are less soluble in urine.) • Its penetration into the brain and CSF is good. Sulphamethaoxazole • Slow to absorb orally and excrete in the urine (mid duration of action) • Which are relatively insoluble _ Crystalluria can occur. Sulphadiazine Sulphadoxine, Sulphamethopyrazine • Slow renal excretion and high binding of plasma proteins
  • 8. • It is used topically for ocular infection. • Highly soluble compound. Mefenide • This isn't your normal sulphonamide. It is limited to topical usage and inhibits both gram-positive and gram-negative bacterial growth. Adverse effect • On urinary system • On haemopoietic system – Bone marrow depression, Aplastic anaemia. • On gastrointestinal tract – Vomiting, diarrhea, nausea. • Hypersensitivity reaction – Skin rashes, anaphylaxis, steven Johnson. Sulphacetamide sod.
  • 9. 1. Sulphamethaoxazole in combination with trimethoprim is used in the treatment of P. jiroveci infection in patients with AIDS. 2. Rheumatic feverInflammatory bowel disease 3. Opthalmic infection. Indication-Typhoid and paratyphoid feverAcute and chronic urinary tract infection.Bacillary dysenteryDermatitis. Therapeutic Uses Contraindication In Pregnancy- Use of Sulphonamides in the first trimester of pregnancy might be associated with Congenital malformations. • Since sulphonamides displace bilirubin from protein-binding sites in newborns, it is not recommended to use them in infants younger than two months.
  • 10. References • Text book of Pharmacology for medical graduates by V Shanbhag Tara and Shenoy Smita , Fourth edition , page no. 375-377 • Text book of Essential of pharmacology by Tripathi KD , Seven edition ,new delhi , page no. 704-706. • https://www.slideshare.net/raselmahbub1/sulfonamide