Indication |
For the treatment of vulvovaginitis caused by Candida albicans. |
Pharmacodynamics |
Sulfanilamide is a sulfonamide antibiotic. The sulfonamides are
synthetic bacteriostatic antibiotics with a wide spectrum against most
gram-positive and many gram-negative organisms. However, many strains of
an individual species may be resistant. Sulfonamides inhibit
multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic
acid in the folic acid metabolism cycle. Bacterial sensitivity is the
same for the various sulfonamides, and resistance to one sulfonamide
indicates resistance to all. Most sulfonamides are readily absorbed
orally. However, parenteral administration is difficult, since the
soluble sulfonamide salts are highly alkaline and irritating to the
tissues. The sulfonamides are widely distributed throughout all tissues.
High levels are achieved in pleural, peritoneal, synovial, and ocular
fluids. Although these drugs are no longer used to treat meningitis, CSF
levels are high in meningeal infections. Their antibacterial action is
inhibited by pus. |
Mechanism of action |
Sulfanilamide is a competitive inhibitor of bacterial enzyme
dihydropteroate synthetase. This enzyme normally uses para-aminobenzoic
acid (PABA) for synthesizing the necessary folic acid. The inhibited
reaction is normally necessary in these organisms for the synthesis of
folic acid. Without it, bacteria cannot replicate. |
Absorption |
Sulfonamides are absorbed through the vaginal mucosa. There are no
pharmacokinetic data available describing how much of an intravaginal
dose reaches the systemic circulation. |
Volume of distribution |
Not Available |
Protein binding |
Not Available |
Metabolism |
Not Available |
Route of elimination |
Not Available |
Half life |
Not Available |
Clearance |
Not Available |
Toxicity |
Oral, mouse LD50 = 3700 mg/kg; Intravenous, mouse LD50 = 621 mg/kg; Oral, rabbit LD50
= 1300 mg/kg. Side effects include itching, burning, skin rash,
redness, swelling, or other sign of irritation not present before use of
this medicine and long-term use of sulfonamides may cause cancer of the
thyroid gland. |