• About
  • Privacy Policy
  • Terms Of Use
  • Contact
Saturday, July 2, 2022
Pharma Info Nepal
  • Home
  • Loksewa
  • License
  • Questions
  • Vacancy
  • Downloads
  • Notice
No Result
View All Result
  • Home
  • Loksewa
  • License
  • Questions
  • Vacancy
  • Downloads
  • Notice
No Result
View All Result
Pharma Info Nepal
No Result
View All Result
Home Medicinal Chemistry

Sulphonamide Mechanism Action | Classification 

Sulphonamide Mechanism Action and Classification in Various Aspect 

Nabin Bista by Nabin Bista
August 25, 2021
in Medicinal Chemistry, Pharmacology, Study Materials
0
Sulphonamide Mechanism Action | Classification 
322
VIEWS
Share on FacebookShare on Twitter

Sulphonamide Mechanism Action | Classification 

 

The term sulphonamides are employed as a generic name for the derivatives of para amino benzene sulphonamide (sulphanilamide). The sulphonamide drugs were the first effective chemotherapeutic agents to be employed systemically for the prevention and treatment of bacterial infections in humans.

The sulphonamides are bacteriostatic antibiotics with a wide spectrum action against most gram-positive bacteria and many gram-negative organisms. Actually it was found to be the metabolic product of Prontosil, which is responsible for antibacterial activity, and this has given the initiation to develop sulphonamides as antibacterial agents.

Antibacterial Sulphonamides
Fig Reference: V Alagarsamy Text Book of Medicinal Chemistry

 

Sulphonamides are total synthetic substances that are produced by relatively simple chemical synthesis. The advent of penicillin and, subsequently of other antibiotics has diminished the usefulness of sulphonamides. Antimicrobial compounds contain sulphonamide (SO2NH2) group. This group (SO2NH) is also present in other compounds, such as antidiabetic agents (e.g. Tolubutamide), diuretics (e.g. chlorthiazide and its congeners, furosemide, and acetazolamide), and anticonvulsants such as sulthiame.

The sulphonamides exists as white powder, mildly acidic in character, and they form water-soluble salts with bases. The pH of sodium salts with some exception, for example, sodium sulphacetamide, is very high when given intramuscular (IM), the marked alkalinity causes damage to the tissues.

Microorganisms that may be susceptible in vitro to sulphonamides include Streptococcus pyogens, Streptococcus pneumoniae, Haemophilus infl uenzae, H. ducreyi, Nocardia, Actinomyces, Calymmatobacterium granulomatis, and Chlamydia trachomatis. The minimal inhibitory concentration ranges from 0.1 μg/ml for C. trachomatis to 4–64 μg/ml for E. coli. Sulphonamides are selective drugs used to treat urinary tract infections, bacterial respiratory infections, and gastrointestinal (GI) infections.

Mechansim of Action of Sulphonamide

Sulphonamides are structure analogues and competitive antagonists of para-amino benzoic acid (PABA). They inhibit dihydropteroate synthetase, the bacterial enzyme responsible for the incorpora- tion of PABA into dihydropteric acid, and it is the intermediate precursor of folic acid. Synergistic effect is obtained by a combination of trimethoprim. The compound trimethoprim is a potent and selective inhibitor of microbial dihydrofolate reductase, the enzyme that reduces dihydrofolate to tetrahydrofolate. The simultaneous administration of sulphonamide and trimethoprim blocks the pathway of cell-wall synthesis sequentially.

Classification of Sulphonamide 

Sulphonamides can be classifi ed in various ways:

On the basis of the site of action

  • Sulphonamides for general infection: Sulphanilamide, Sulphapyridine, Sulphadiazine, Sulphamethoxacine, Sulphamethoxazole.
  • Sulphonamides for urinary tract infections: Sulphaisoxazole, Sulphathiazole.
  • Sulphonamides for intestinal infections: Phthalylsulphathiazole, Succinyl sulphathiazole, Sulphasalazine.
  • Sulphonamides for local infections: Sulpahacetamide, Mafenamide, Silver sulphadiazine.
  • Sulphonamides for dermatitis: Dapsone, Solapsone.
  • Sulphonamides in combination: Trimethoprim with Sulphamethoxazole.

On the basis of the pharmacokinetic properties

  • Poorly absorbed sulphonamides (locally acting sulphonamides)—Sulphasalazine, Phthalylsulphathiazole, Sulphaguanidine, Salicylazo sulphapyridine, Succinyl sulpha thiazole.
  • Rapidly absorbed and rapidly excreted (systemic sulphanamides): Sulphamethoxazole, Sulphaisoxazole, Sulphadiazine, Sulphadimidine, Sulphafurazole, Sulphasomidine, Sulphamethiazole, Sulphacetamide Sulphachlorpyridazine.
  • Topically used sulphonamides: Sulphacetamide, Mafenide, Sulphathiazole, Silver sulphadiazine.

On the basis of the pharamacological activity

  • Antibacterial agents:Sulphadiazine, Sulfi soxazole.
  • Drugs used in dermatitis: Dapsone.

On the basis of the duration of action

  • Extra long-acting sulphonamides (half-life greater than 50 h): Sulphasalazine, Sulphaclomide, Sulphalene.
  • Long-acting sulphonamides (half-life greater than 24 h):Sulphadoxine, Sulphadimethoxine, Sulphamethoxy pyridazine, Sulphamethoxydiazine, Sulphaphenazole, Sulphamethoxine.
  • Intermediate-acting sulphonamides (half-life between 10–24 h): Sulphasomizole, Sulphamethoxazole.
  • Short-acting sulphonamides (half-life less than 20 h): Sulphamethiazole, sulphaisoxazole.
  • Injectables (soluble sulpha drugs): Sulphafurazole, Sulphadiazine, Sulphamethoxine.

On the basis of the chemical structure

  • N-substituted sulphonamide:Sulphadiazine, Sulphacetamide, Sulphadimidine.
  • N-4 substituted sulphonamides (prodrugs): Prontosil.
  • Both N-1 and N-4 substituted sulphonamides: Succinyl sulphathiazole, Phthalylsulphathiazole.
  • Miscellaneous: Mefenide sodium.

 



  • Microsomal Enzyme Induction 
  • SAR of Morphine (Structure Activity Relationship of Morphine)

Follow us on Facebook : Pharma Info Nepal


 

Tags: Medicinal ChemistryPharmacologyStudy MaterialsSulphonamide
Previous Post

FDA Approves First COVID-19 Vaccine Pfizer-BioNTech

Next Post

Vacancy Annoucement Procurement and Supply Chain Officer fhi 

Nabin Bista

Nabin Bista

Hello, Thank You for visiting my blog I am Nabin Bista, Dedicated and self motivated young Pharmacist from Nepal. Blogging is my passion. I am studying B Pharmacy at Institute of Medicine - IOM. If you want me to write about any posts that you found confusing/difficult, please mention in the comments below.

Related Posts

A Guide to Stability Storage

A Guide to Stability Storage

May 18, 2022
Provision and Process for Registration, Manufacturing & Importation of any Drug in Nepal

Provision and Process for Registration, Manufacturing & Importation of any Drug in Nepal

February 6, 2022
General Pharmacology Important MCQs

General Pharmacology Important MCQs

December 21, 2021
10 Poisonous Plants in Nepal 

10 Poisonous Plants in Nepal 

October 19, 2021
Load More
Next Post
Vacancy Annoucement Procurement and Supply Chain Officer fhi 

Vacancy Annoucement Procurement and Supply Chain Officer fhi 

Discussion about this post

Recommended

Nursing Loksewa Aayog Vacancy Announcement 

Nursing Loksewa Aayog Vacancy Announcement 

1 year ago
Vacancy Announcement Loksewa Aayog Pharmacy Officer 

Vacancy Announcement Loksewa Aayog Pharmacy Officer 

8 months ago

Don't Miss

List of B Pharm Colleges in Nepal

List of B Pharm Colleges in Nepal

June 3, 2022
Vacancy Announcement for Technical Editorial International Consultant Pharmacist 

Vacancy Announcement for Technical Editorial International Consultant Pharmacist 

May 26, 2022
Nepal Pharmacy Council 19th Name Registration Exam Application Form Notice

Nepal Pharmacy Council 19th Name Registration Exam Application Form Notice

May 20, 2022
A Guide to Stability Storage

A Guide to Stability Storage

May 18, 2022

About Pharma Info Nepal

Pharma Info Nepal (Nabin’s Blog) was initiated in 2019 with the aim of providing relevant and accurate information for pharmacy, nursing and other health professionals. Since then it is conveying health related educational and informational updates of Nepal. It serves as a source for learning materials on diverse topics relating to medicine intended basically for pharmacy and nursing students. It covers job opportunities, question collections for pharmacy license, nursing license as well as various competitive exams.

Our readers rely on us for the well referenced and latest updates collected from the reliable sites.

Follow us

  • Facebook
  • Twitter
  • LinkedIn
  • YouTube
  • Instagram

Information Reader

Contents (text, image, graphics, documents and other materials) published on this portal are collected from other relevant sources with the sole purpose of sharing information. Contents and features are subject to change and all rights reserved to Pharma info Nepal. The information presented on this web portal and its official social media handles have no affiliation to any organization that author is involved with either professionally or personally.

If you have found anything displayed incorrectly or have further suggestions on improving our effort, please do not hesitate to reach out at pharmainfonepal1@gmail.com !
We hope you find Pharma info Nepal a helpful site. Thanks !!!

Categories

  • B Pharmacy
  • Colleges
  • D Pharmacy
  • Downloads
  • License
  • Loksewa
  • M Pharmacy
  • Medicinal Chemistry
  • Notice
  • Nursing
  • Pharmacognosy
  • Pharmacology
  • Questions
  • Scholarship
  • Study Materials
  • Syllabus
  • Updates
  • Vacancy

DOWNLOADS

Pharmacy Book 

Pharmacy Act and Guidelines

About Pharma Info Nepal

About Admin

  • About
  • Privacy Policy
  • Terms Of Use
  • Contact

© 2021 Nabin's Blog

No Result
View All Result
  • Home
  • Loksewa
  • License
  • Questions
  • Vacancy
  • Downloads
  • Notice

© 2021 Nabin's Blog

error: