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Pronunciation |
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(sul
fi SOKS a
zole) |
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U.S. Brand
Names |
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Gantrisin® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Novo-Soxazole; Sulfizole® |
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Synonyms |
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Sulfisoxazole Acetyl; Sulphafurazole |
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Pharmacological Index |
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Antibiotic, Sulfonamide Derivative |
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Use |
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Treatment of urinary tract infections, otitis media, Chlamydia;
nocardiosis; treatment of acute pelvic inflammatory disease in prepubertal
children; often used in combination with trimethoprim |
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Pregnancy Risk
Factor |
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B/D (at term) |
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Contraindications |
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Hypersensitivity to any sulfa drug or any component, porphyria, pregnancy
during 3rd trimester, infants <2 months of age (sulfas compete with bilirubin
for protein binding sites), patients with urinary obstruction, sunscreens
containing PABA |
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Warnings/Precautions |
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Use with caution in patients with G-6-PD deficiency (hemolysis may occur),
hepatic or renal impairment; dosage modification required in patients with renal
impairment; risk of crystalluria should be considered in patients with impaired
renal function |
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Adverse
Reactions |
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>10%:
Central nervous system: Fever, dizziness, headache
Dermatologic: Itching, rash, photosensitivity
Gastrointestinal: Anorexia, nausea, vomiting, diarrhea
1% to 10%:
Dermatologic: Lyell's syndrome, Stevens-Johnson syndrome
Hematologic: Granulocytopenia, leukopenia, thrombocytopenia, aplastic anemia,
hemolytic anemia
Hepatic: Hepatitis
<1%: Vasculitis, thyroid function disturbance, crystalluria, jaundice,
hematuria, acute nephropathy, interstitial nephritis, serum sickness-like
reactions |
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Overdosage/Toxicology |
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Symptoms of overdose include drowsiness, dizziness, anorexia, abdominal pain,
nausea, vomiting, hemolytic anemia, acidosis, jaundice, fever, agranulocytosis;
doses of as little as 2-5 g/day may produce toxicity; the aniline radical is
responsible for hematologic toxicity
High volume diuresis may aid in elimination and prevention of renal failure
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Drug
Interactions |
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Decreased effect with PABA or PABA metabolites of drugs (ie, procaine,
proparacaine, tetracaine); cyclosporine levels may be decreased
Increased effect/toxicity of oral anticoagulants, oral hypoglycemic agents,
hydantoins, uricosuric agents, methotrexate when administered with sulfonamides
Increased toxicity of sulfonamides with diuretics, indomethacin, methenamine,
probenecid, and salicylates |
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Stability |
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Protect from light |
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Mechanism of
Action |
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Interferes with bacterial growth by inhibiting bacterial folic acid synthesis
through competitive antagonism of PABA |
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Pharmacodynamics/Kinetics |
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Absorption: Sulfisoxazole acetyl is hydrolyzed in the GI tract to
sulfisoxazole which is readily absorbed
Distribution: Crosses the placenta; excreted into breast milk
Ratio of CSF to blood level (%): Normal meninges: 50-80; Inflamed meninges:
80+
Protein binding: 85% to 88%
Metabolized: In the liver by acetylation and glucuronide conjugation to
inactive compounds
Half-life: 4-7 hours, prolonged with renal impairment
Time to peak serum concentration: Within 2-3 hours
Elimination: Primarily in urine (95% within 24 hours), 40% to 60% as
unchanged drug |
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Usual Dosage |
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Not for use in patients <2 months of age:
Pelvic inflammatory disease: 100 mg/kg/day in divided doses every 6 hours;
used in combination with ceftriaxone
Chlamydia trachomatis: 100 mg/kg/day in divided doses every 6 hours
Adults: Oral: Initial: 2-4 g, then 4-8 g/day in divided doses every 4-6 hours
Pelvic inflammatory disease: 500 mg every 6 hours for 21 days; used in
combination with ceftriaxone
Chlamydia trachomatis: 500 mg every 6 hours for 10 days
Dosing interval in renal impairment:
Clcr 10-50 mL/minute: Administer every 8-12 hours
Clcr <10 mL/minute: Administer every 12-24 hours
Hemodialysis: >50% removed by hemodialysis
Children and Adults: Ophthalmic:
Solution: Instill 1-2 drops to affected eye every 2-3 hours
Ointment: Apply small amount to affected eye 1-3 times/day and at bedtime
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Dietary
Considerations |
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Should be administered with a glass of water on an empty stomach; interferes
with folate absorption |
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Monitoring
Parameters |
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CBC, urinalysis, renal function tests, temperature |
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Test
Interactions |
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False-positive protein in urine; false-positive urine glucose with
Clinitest® |
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Mental Health: Effects
on Mental Status |
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Dizziness is common; sulfonamides reported to cause restlessness,
irritability, depression, euphoria, disorientation, panic, hallucinations, and
delusions |
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Mental Health:
Effects on Psychiatric
Treatment |
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Photosensitivity is common; use caution with concurrent psychotropics; may
cause leukopenia; caution with clozapine and carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take as directed, at regular intervals around-the-clock. Take 1 hour before
or 2 hours after meals with a full glass of water. Take full course of therapy
even if you are feeling better. Avoid aspirin or aspirin-containing products and
avoid large quantities of vitamin C. It is very important to maintain adequate
hydration (2-3 L/day of fluids unless instructed to restrict fluid intake) to
prevent kidney damage. You may experience dizziness or headache (use caution
when driving or engaging in tasks requiring alertness until response to drug is
known); photosensitivity (use sunscreen, wear protective clothing and eyewear,
and avoid direct sunlight); nausea, vomiting, or loss of appetite (small
frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help).
Diabetics: Drug may cause false tests with Clinitest®
urine glucose monitoring; use of glucose oxidase methods
(Clinistix®) or serum glucose monitoring is preferable.
Report persistent nausea, vomiting, diarrhea, or abdominal pain; skin rash;
persistent or severe sore throat, mouth sores, fever, or vaginal itching or
discharge; unusual bruising or bleeding; blackened stool; fatigue; or difficulty
breathing. Pregnancy precautions: Inform prescriber if you are pregnant.
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Nursing
Implications |
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Maintain adequate fluid intake |
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Dosage Forms |
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Solution, ophthalmic, as diolamine: 4% [40 mg/mL] (15 mL)
Suspension, oral, pediatric, as acetyl (raspberry flavor): 500 mg/5 mL (480
mL)
Tablet: 500 mg |
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References |
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Boisvert A, Barbeau G, and Belanger PM,
"Pharmacokinetics of Sulfisoxazole in Young and Elderly Subjects,"
Gerontology, 1984, 30(2):125-31.
Kaplan SA, Weinfold RE, Abruzzo CW, et al,
"Pharmacokinetic Profile of Sulfisoxazole Following IM, IV, and PO Administration to Man,"
J Pharm Sci, 1972, 61:773.
Liston TE and Harbison R,
"Sulfisoxazole Chemoprophylaxis for Frequent Otitis Media," Pediatrics,
1983, 71:524-30.
Thoene DE and Johnson CE, "Pharmacotherapy of Otitis Media,"
Pharmacotherapy, 1991, 11(3):212-21.
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