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Sulfamethoxazole
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(sul fa meth OKS a zole)

U.S. Brand Names
Gantanol®; Urobak®

Generic Available

Yes: Tablet


Canadian Brand Names
Apo®-Sulfamethoxazole

Pharmacological Index

Antibiotic, Sulfonamide Derivative


Use

Treatment of urinary tract infections, nocardiosis, toxoplasmosis, acute otitis media, and acute exacerbations of chronic bronchitis due to susceptible organisms


Pregnancy Risk Factor

B/D (at term)


Contraindications

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


Warnings/Precautions

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


Adverse Reactions

>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


Overdosage/Toxicology

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


Drug Interactions

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


Stability

Protect from light


Mechanism of Action

Interferes with bacterial growth by inhibiting bacterial folic acid synthesis through competitive antagonism of PABA


Pharmacodynamics/Kinetics

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


Usual Dosage

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%)


Dietary Considerations

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


Monitoring Parameters

Monitor urine output


Test Interactions

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)


Mental Health: Effects on Mental Status

Dizziness is common; sulfonamides reported to cause restlessness, irritability, depression, euphoria, disorientation, panic, hallucinations, and delusions


Mental Health: Effects on Psychiatric Treatment

Photosensitivity is common; use caution with concurrent psychotropics; may cause leukopenia; caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

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.


Nursing Implications

Maintain adequate hydration


Dosage Forms

Suspension, oral (cherry flavor): 500 mg/5 mL (480 mL)

Tablet: 500 mg


References

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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