SULFISOXAZOLE
(sul-fi-sox'a-zole)
Gantrisin
Classifications: antiinfective; sulfonamide
Pregnancy Category: B (D if near term)

Availability

500 mg tablets

Actions

Short-acting derivative of sulfanilamide. Bacteriostatic action believed to be by competitive inhibition of p-aminobenzoic acid (PABA), thereby interfering with folic acid biosynthesis required for bacterial growth.

Therapeutic Effects

Exhibits broad antimicrobial spectrum against both gram-positive and gram-negative organisms.

Uses

Acute, recurrent, and chronic urinary tract infections and chancroid; adjunctive therapy in trachoma, chloroquine-resistant strains of malaria, acute otitis media due to Haemophilus influenzae, and meningococcal and H. influenzae meningitis. Ophthalmic preparations used in treatment of conjunctivitis, corneal ulcer, and other superficial eye infections and as adjunct to systemic sulfonamide therapy for trachoma. Topical vaginal preparation used for H. vaginalis vaginitis.

Contraindications

History of hypersensitivity to sulfonamides, salicylates, or chemically related drugs; use in treatment of group A beta-hemolytic streptococcal infections; infants <2 mo of age (except in treatment of congenital toxoplasmosis); porphyria; advanced kidney or liver disease; intestinal and urinary obstruction; pregnancy (category B, category D if near term), lactation.

Cautious Use

Impaired kidney or liver function; severe allergy; bronchial asthma; blood dyscrasias; patients with G6PD deficiency.

Route & Dosage

Infection by Susceptible Organisms
Adult: PO 2–4 g initially, followed by 4–8 g/d in 4–6 divided doses Vaginal 1 applicator full 1–2 times/d
Child: PO >2 mo, 75 mg/kg initially, followed by 150 mg/kg/d in 4–6 divided doses (max: 6 g/d)

Administration

Oral

Adverse Effects (1%)

CNS: Headache, peripheral neuritis, peripheral neuropathy, tinnitus, hearing loss, vertigo, insomnia, drowsiness, mental depression, acute psychosis, ataxia, convulsions, kernicterus (newborns). GI: Nausea, vomiting, diarrhea, abdominal pains, hepatitis, jaundice, pancreatitis, stomatitis. Hematologic: Acute hemolytic anemia (especially in patients with G6PD deficiency), aplastic anemia, methemoglobinemia, agranulocytosis, thrombocytopenia, leukopenia, eosinophilia, hypoprothrombinemia. Body as a Whole: Headache, fever, chills, arthralgia, malaise, allergic myocarditis, serum sickness, anaphylactoid reactions, lymphadenopathy, local reaction following IM injection, fixed drug eruptions, diuresis, overgrowth of nonsusceptible organisms, LE phenomenon. Skin: Pruritus, urticaria, rash, erythema multiforme including Stevens-Johnson syndrome exfoliative, dermatitis, alopecia, photosensitivity, vascular lesions. Urogenital: Crystalluria, hematuria, proteinuria, anuria, toxic nephrosis, reduction in sperm count. Metabolic: Goiter, hypoglycemia. Special Senses: Conjunctivitis, conjunctival or scleral infection, retardation of corneal healing (ophthalmic ointment).

Diagnostic Test Interference

Sulfonamides may interfere with BSP retention and PSP excretion tests and may affect results of thyroid function tests (I-131 may be decreased for about 7 d). Large doses of sulfonamides reportedly may produce false-positive urine glucose determinations with copper reduction methods (e.g., Benedict's and Clinitest). SULFONAMIDES may produce false-positive results for urinary protein (with sulfosalicylic acid test) and may interfere with urine urobilinogen determinations using Ehrlich's reagent or Urobilistix. Follow-up cultures are unreliable unless PABA is added to culture medium.

Interactions

Drug: paba-containing local anesthetics may antagonize sulfa's effects; oral anticoagulants potentiate hypoprothrombinemia; may potentiate sulfonylurea-induced hypoglycemia; may decrease concentrations of cyclosporine; may increase levels of phenytoin.

Pharmacokinetics

Absorption: Readily absorbed from GI tract. Peak: 2–4 h. Distribution: Distributed in extracellular space; crosses blood–brain barrier and placenta; detected in breast milk. Metabolism: Metabolized in liver. Elimination: 95% excreted in urine in 24 h. Half-Life: 4.6–7.8 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug