SULPHONAMIDES

• Sulphonamides are derivatives of Para amino

benzene sulfonamide, the antibacterial
component of azo dye (prontosil)
• Synergism Trimethoprim
• Antagonists
• 1) PABA is the most prominent sulfonamide antagonist.
Certain local anesthetics such as procaine (esters of
PABA) antagonize these drugs.
• 2) Nicotinamide, folic acid and choline and their
precursors.
• 3) Gelatin, albumin, peptone and serum proteins
antagonize sulphanimides action by binding with them.
• 4) Products of cell and tissue death, especially pus.
• Classification of Sulfonamides
(a).Systemically acting sulphonamides
Short acting sulphonamides / Agents
absorbed rapidly and excreted rapidly
(duration of t1/2 <12 hrs)
• Sulphadiazine 60 mg/kg repeat every 6 hrs.
• Sulphamerazine
• (b) Intermediate acting sulphanamides (duration 12-24 hr)
Sulfamethoxazole (50-60 mg/kg 25-30 mg every 12 hrs)
Sulphadimidine 110 mg/kg
• (c) Long-acting sulphonamides (duration 24-48 hrs)
Sulphadimethoxine
• (d) Ultra-long acting sulphonamides (duration >48 hrs)
• Sulphadoxine: it has long half-lifr that is 7-9 days. It is used
in combination with pyrimethamine for the prophylaxis and
treatment of malaria caused by chloraquine-resistant
strains of plasmodium falciparum
Sulphamethopyrazine
• Locally acting sulphonamides
(a) Gut acting sulphonamides
Sulphasalazine: used in the therapy of
ulcerative colitis and regional enteritis
Sulphaguanidine – 264 mg/kg and 55 mg SID
Pthalylsulfathiazole – oral 150-200 mg/kg BID
Pthalyl sulfacetamide – oral 100-250 mg/kg BID
b) Sulphonamides employed for topical us
Sulfacetamide: used in ophthalmic infections
Silver sulphadiazine: burns
• Trimethoprim is most often compounded with
Sulfamethoxazole, the resulting combination
is called co–trimoxazole, which shows greater
antimicrobial activity than equivalent
quantities of either drug used alone
(Synergism)
• Sulphadiazine + Trimethoprim:
• Parenteral solution:
sulfadiazine – 400 mg
trimethoprim – 80 mg 1–5 ml/30 kg once in day.
• Oral: Bolus: Sulfadiazine – 1 G
Trimethaprim – 0.2 G 30 mg/kg.
• Sulfadoxin + Trimethoprim (33%)
Parenteral: A solution containing 200 mg
sulfadoxine and 40 mg trimethoprine
• Toxicity
1. Crystalluria
2. Reversible hypersensitivity
In dogs: Kerato conjunctivitis sicca, Bone marrow
suppression, Cutaneous allergic reactions.
• Hypoprothrombinaemia: prolonged administration may
lead to vitamin K deficiency due to inhibition of enzyme
vitamin K epoxide reductase.
• Keratoconjunctivitis sicca (dry eyes): occurs with
sulphasalazine, sulphadiazine and sulphamethoxazole in
dogs
• Aplasticanaemia and thrombocytopenia
• Points to be remembered with sulfonamide
therapy
• 1. Most of the sulfonamides are bacteriostatic, so these should be used
in early stages of infection.
• 2. Sulfonamides are competitive inhibitor of PABA so PABA and other
B –complex vitamins should not be administered along with sulfonamides.
• 3. Sulfonamides are extensively bound to serum albumin, and also their
activity is impaired in the presence of pus, tissue debris, so
sulfonamides should not be given in pyemia and extensive cellular
damage condition.
• 4. Preferably sulfonamides should be used in combination with
trimethoprim.