Scribd
Upload
124 views

Sulphonamides PDF

Sulphonamides are a group of synthetic antibacterial drugs that were first discovered in 1935. They work by inhibiting the bacterial enzyme involved in folic acid synthesis. Common sulphonamides include sulfadiazine and sulfamethoxazole. They are often used in combination with trimethoprim to treat various bacterial infections in humans, livestock and poultry. Adverse effects can include crystalluria and hypersensitivity reactions.

Uploaded by

Abhinav Gupta
Copyright
© © All Rights Reserved
Available Formats
Download as PDF, TXT or read online on Scribd
124 views

Sulphonamides PDF

Sulphonamides are a group of synthetic antibacterial drugs that were first discovered in 1935. They work by inhibiting the bacterial enzyme involved in folic acid synthesis. Common sulphonamides include sulfadiazine and sulfamethoxazole. They are often used in combination with trimethoprim to treat various bacterial infections in humans, livestock and poultry. Adverse effects can include crystalluria and hypersensitivity reactions.

Uploaded by

Abhinav Gupta
Copyright
© © All Rights Reserved
Available Formats
Download as PDF, TXT or read online on Scribd
You are on page 1/ 11

Sulphonamides

• Sulphonamides are a group of synthetic organic chemicals with


chemotherapeutic agent.
• First chemotherapeutic agent used systematically for prevention and
treatment of various disease.
• Antibacterial activity of sulphonamide was first discovered by
Grehard Domagk in 1935, developed from the produrg Prontosil
dye.
• It is a bacteriostatic, broad spectrum drug that inhibit folic acid
synthesis.
 Source and chemistry:
• Sulphonamides posses a common chemical nucleus, which is closely
related to PABA ( essential member of vitamin-B complex).
• Sulphonamides are about twice or more soluble in alkaline PH as
compared with the acidic or neutral PH.
• In acidic urine, sulphonamides may form becoz of their decrease
solubility.
• A free amino group in N4 position is essential for antibacterial
activity.
• Therefore, combination of two or more sulphonamides is occasionally
used to increase solubility and efficacy (additive effect) and to
decrease toxicity (less crystallization in urine).
 Classification:
(1)Systemically acting sulphonamides:
(a) Short acting (duration < 12 hrs.)
sulphadiazine, sulphafurazole, sulphamirazine, sulphathiazole,
sulphachlorpyridine, sulphanilamide
(b) Intermediate acting (12-24 hrs.)
sulphadimidine, sulphamoxole, sulphamethoxazole,
sulphaphenazole
(c) Long acting sulphonamides (duration 24-48 hrs.)
sulphamethoxine, sulphaethoxypyridazine, sulphabromomethazine,
sulphamethoxypyridazine
(d) Ultra long acting (> 48 hrs.)
sulphadoxine, sulphamethopyrazine
(2) Locally acting sulphonamides:
(a) Gut acting sulphonamides (enteric poor soluble):
sulphaguanidine, sulphaquinoxaline, sulphasalazine,
succinyl sulphathiazole, phthalyl sulphacetamide,
phthalyl sulphathiazole
(b) Highly soluble (urinary):
sulphasoxazole, sulphasomidine
(c) Topically acting:
mefenide, sulphacetamide, silver sulphadiazine
 Mechanism of action:
• Folic acid essential for synthesis of nucleic acid.
• Bacteria synthesize their own folic acid from PABA with the help of
enzyme folic acid synthetase.
• Sulphonamides are structurally similar to PABA and competitively
inhibit the enzyme folic acid synthetase.
• Cause folic acid deficiency and thereby inhibition of bacterial growth
as well as injury to the bacterial cell.
• Mammalian cell are not affected becoz they required performed folic
acid supplied from diet and cannot synthesize folic acid themselves.
• Sulphonamides are more effective in acute stage of infection bacteria
multiply at a much faster rate utilizing larger amount of PABA and
host immune system is also active.
 Pharmacokinetic:
Absorption:
• Rapidly absorbed from GIT, except gut acting sulpha. Drug.
• In general dogs, cats and birds absorb sulphonamides rapidly, pigs
takes some time and cattle require much longer time.
Distribution:
• Diffuse well into body tissue and fluids.
Metabolism:
• Sulphonamides are primarily metabolized by acetylation at N4 by
non-microsomal enzyme in liver except sulphapyridine derivatives
( sulphadiazine, sulphamerazine and sulphadimidine).
• Acetylation of sulphonamide reduce their solubility in acidic urine
thus promoting crystallization.
• In cattle sulphonamides are more toxic due to extensive acetylation.
Excretion:
• Alkalinisation of urine favours ionisation of sulphonamide and its
rapid elimination.
• It also excrete in tears, faeces, bile and sweat, but gut acting are
poorly absorbed from the G.I tract and are primarily elimination in the
faeces.

 Triple sulpha: The combination (( sulphadiazine, sulphamerazine


and sulphadimidine) in form of triple sulpha has added antibacterial
action with minimized risk of crystalluria.
• The crystallization can be prevented by alkalizing the urine,
increasing water intake and reducing the dose rate or by using triple
sulpha.
• Sulphonamides and chlortetracycline act as growth promoter prevent
clostridial ET.
 Toxicity:
• Acute effect:
(a) Renal toxicity: Crystalluria, hematuria, obstruction of ureter and
bladder.
(b) Hypersensitivity reaction: Skin rashes due to anaphylactic shock.
(c) Other effects: Vomiting, nausea, anorexia and diarrrhoea.
• Chronic effect:
(a) Hematological alteration
(b) Hepatic degeneration
(c) Jaundice
(d) Drop in egg production in poultry.
 Clinical use: Colibacillosis, pasteurellosis, footrot and coccidiosis.
• In poultry prevention and treatment of coccidiosis, pullorum and fowl
typhoid disease.
Potentiated Sulphonamides

• Sulphonamides in combination with trimethoprim, which potentiates


the antibacterial action of sulphonamides.
 Trimethoprim: Diaminopyrimidine derivatives.
• Bacteriostatic drug, selectively inhibit bacterial dihydrofolate
reductase enzyme.
• In combination with sulphonamide results in potentiation of
antibacterial action by sequential blockade.
• Readily absorbed after oral administration except in ruminants
trapped and undergo microbial degradation .
• Widely distributed, metabolized in liver and excretion by urine
glomerular filtration and tubular secretion.
• Common combinations:
Trimethoprim + sulphamethoxazole (cotrimoxazole)
Trimethoprim + sulphadiazine (cotriazine)
Trimethoprim + sulphadoxine

 Side effects:
• Swelling at the site of injection.
• Anemia
• Keratoconjuctivitis (reduced lacrimal secretion)

 Clinical uses:
• Urinary tract infection
• Salmonellosis and brucellosis
• Cattle – Salmonellosis, diarrhea and pneumonia
• Poultry – E.coli.

You might also like