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Pronunciation |
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(sul
fa meth OKS a
zole) |
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U.S. Brand
Names |
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Gantanol®;
Urobak® |
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Generic
Available |
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Yes: Tablet |
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Canadian Brand
Names |
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Apo®-Sulfamethoxazole |
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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, nocardiosis, toxoplasmosis, acute
otitis media, and acute exacerbations of chronic bronchitis due to susceptible
organisms |
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Pregnancy Risk
Factor |
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B/D (at term) |
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Contraindications |
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Porphyria, hypersensitivity to any sulfa drug or any component, pregnancy
during 3rd trimester, children <2 months of age unless indicated for the
treatment of congenital toxoplasmosis, sunscreens containing
PABA |
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Warnings/Precautions |
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Maintain adequate fluid intake to prevent crystalluria; use with caution in
patients with renal or hepatic impairment, and patients with G-6-PD deficiency;
should not be used for group A beta-hemolytic streptococcal
infections |
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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;
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: Oral: 90%
Distribution: Crosses the placenta; readily enters the CSF
Protein binding: 70%
Metabolism: Primarily in the liver, with 10% to 20% as the N-acetylated form
in the plasma
Half-life: 9-12 hours, prolonged with renal impairment
Time to peak serum concentration: Within 3-4 hours
Elimination: Unchanged drug (20%) and its metabolites are excreted in urine
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Usual Dosage |
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Oral:
Adults: Initial: 2 g, then 1 g 2-3 times/day; maximum: 3 g/24 hours
Dosing adjustment/interval in renal impairment:
Clcr 10-50 mL/minute: Administer every 12-24 hours
Clcr <10 mL/minute: Administer every 24 hours
Hemodialysis: Moderately dialyzable (20% to 50%) |
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Dietary
Considerations |
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Should be administered 1 hour before or 2 hours after a meal on an empty
stomach; avoid large quantities of vitamin C or acidifying agents (cranberry
juice) to prevent crystalluria; presence of food delays but does not reduce
absorption |
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Monitoring
Parameters |
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Monitor urine output |
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Test
Interactions |
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May interfere with Jaffé alkaline picrate reaction
assay for creatinine resulting in over-estimations of ~10% in the range of
normal values; decreased effect with PABA or PABA metabolites of drugs (ie,
procaine, proparacaine, tetracaine) |
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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 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).
Report skin rash, persistent diarrhea, persistent or severe sore throat, fever,
vaginal itching or discharge, unusual bruising or bleeding, fatigue, persistent
headache or abdominal pain, blackened stool, or difficulty breathing.
Pregnancy precautions: Inform prescriber if you are
pregnant. |
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Nursing
Implications |
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Maintain adequate hydration |
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Dosage Forms |
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Suspension, oral (cherry flavor): 500 mg/5 mL (480 mL)
Tablet: 500 mg |
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References |
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Ljungberg B and Nilsson-Ehle I,
"Pharmacokinetics of Antimicrobial Agents in the Elderly," Rev Infect
Dis, 1987, 9(2):250-64.
Varoquaux O, Lajoie D, Gobert C, et al,
"Pharmacokinetics of the Trimethoprim-Sulfamethoxazole Combination in the Elderly,"
Br J Clin Pharmacol, 1985, 20:575-81.
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