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Gantrisin (Suspension)

Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/676

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Gantrisin (Suspension)
dailymed-instance:dosage
Systemic sulfonamides are contraindicated in infants less than 2 months of age, except in the treatment of congenital toxoplasmosis as adjunctive therapy with pyrimethamine.<br/>Usual Dose for Pediatric Patients Over 2 Months of Age: Initial dose: One half of the 24-hour dose. Maintenance dose: 150 mg/kg/24 hours or 4 gm/M/24 hours���dose to be divided into 4 to 6 doses/24 hours. The maximum dose should not exceed 6 gm/24 hours.
dailymed-instance:descripti...
Gantrisin (sulfisoxazole) is an antibacterial sulfonamide available as a pediatric suspension for oral administration. Each teaspoonful (5 mL) of the pediatric suspension contains the equivalent of approximately 0.5 gm sulfisoxazole in the form of acetyl sulfisoxazole in a vehicle containing 0.3% alcohol, carboxymethylcellulose (sodium), citric acid, methylcellulose, parabens (methyl and propyl), partial invert sugar, sodium citrate, sorbitan monolaurate, sucrose, flavors and water. Acetyl sulfisoxazole, the tasteless form of sulfisoxazole, is N-acetyl sulfisoxazole and must be distinguished from N-acetyl sulfisoxazole, which is a metabolite of sulfisoxazole. Acetyl sulfisoxazole is a white or slightly yellow, crystalline powder that is slightly soluble in alcohol and practically insoluble in water. Acetyl sulfisoxazole has a molecular weight of 309.34 and the following structural formula:
dailymed-instance:clinicalP...
Following oral administration, sulfisoxazole is rapidly and completely absorbed; the small intestine is the major site of absorption, but some of the drug is absorbed from the stomach. Sulfonamides are present in the blood as free, conjugated (acetylated and possibly other forms) and protein-bound forms. The amount present as "free" drug is considered to be the therapeutically active form. Approximately 85% of a dose of sulfisoxazole is bound to plasma proteins, primarily to albumin; 65%to 72% of the unbound portion is in the nonacetylated form. Maximum plasma concentrations of intact sulfisoxazole following a single 2-gm oral dose of sulfisoxazole to healthy adult volunteers ranged from 127 to 211 mcg/mL (mean, 169 mcg/mL) and the time of peak plasma concentration ranged from 1 to 4 hours (mean, 2.5 hours). The elimination half-life of sulfisoxazole ranged from 4.6 to 7.8 hours after oral administration. The elimination of sulfisoxazole has been shown to be slower inelderly subjects (63 to 75 years) with diminished renal function (creatinine clearance, 37 to 68 mL/min).After multiple-dose oral administration of 500 mg qid to healthy volunteers, the average steady-state plasma concentrations of intact sulfisoxazole ranged from 49.9 to 88.8 mcg/mL (mean, 63.4 mcg/mL). Wide variation in blood levels may result following identical doses of a sulfonamide. Blood levels should be measured in patients receiving sulfonamides at the higher recommended doses or being treated for serious infections. Free sulfonamide blood levels of 50 to 150 mcg/mL may be considered therapeutically effective for most infections, with blood levels of 120 to 150 mcg/mL being optimal for serious infections. The maximum sulfonamide level should not exceed 200 mcg/mL, since adverse reactions occur more frequently above this concentration. N-acetyl sulfisoxazole is metabolized to sulfisoxazole by digestive enzymes in the gastrointestinal tract and is absorbed as sulfisoxazole. This enzymatic splitting is presumed to be responsible for slower absorption and lower peak blood concentrations than are attained following administration of an equal oral dose of sulfisoxazole. With continued administration of acetyl sulfisoxazole, blood concentrations approximate those of sulfisoxazole. Following a single 4-gm dose of acetyl sulfisoxazole to healthy volunteers, maximum plasma concentrations of sulfisoxazole ranged from 122 to 282 mcg/mL (mean, 181 mcg/mL) for the pediatric suspension and occurred between 2 and 6 hours postadministration. The half-life of elimination from plasma ranged from 5.4 to 7.4. Sulfisoxazole and its acetylated metabolites are excreted primarily by the kidneys through glomerular filtration. Concentrations of sulfisoxazole are considerably higher in the urine than in the blood. The mean urinary excretion recovery following oral administration of sulfisoxazole is 97% within 48 hours, of which 52% is intact drug, with the remaining as the N-acetylated metabolite. Following administration of acetyl sulfisoxazole pediatric suspension, approximately 58% is excreted in the urine as total drug within 72 hours. Sulfisoxazole is distributed only in extracellular body fluid. It is excreted in human milk. It readily crosses the placental barrier and enters into fetal circulation and also crosses the blood-brain barrier. In healthy subjects, cerebrospinal fluid concentrations of sulfisoxazole vary; in patients with meningitis, however, concentrations of free drug in cerebrospinal fluid as high as 94 mcg/mL have been reported.<br/>Microbiology: The sulfonamides are bacteriostatic agents and the spectrum of activity is similar for all. Sulfonamides inhibit bacterial synthesis of dihydrofolic acid by preventing the condensation of the pteridine with aminobenzoic acid through competitive inhibition of the enzyme dihydropteroate synthetase. Resistant strains have altered dihydropteroate synthetase with reduced affinity for sulfonamides or produce increased quantities of aminobenzoic acid.<br/>Susceptibility Tests:<br/>Diffusion Techniques: Quantitative methods that require measurement of zone diameters give the most precise estimate of the susceptibility of bacteria to antimicrobial agents. One such standard procedurewhich has been recommended for use with disks to test susceptibility of organisms to sulfisoxazole uses the 250- or 300-mcg sulfisoxazole disk. Interpretation involves the correlation of the diameter obtained in the disk test with the minimum inhibitory concentration (MIC) for sulfisoxazole. Reports from the laboratory giving results of the standard single-disk susceptibility test with a 250- or 300-mcg sulfisoxazole disk should be interpreted according to the following criteria: A report of "susceptible" indicates that the pathogen is likely to be inhibited by generally achievable blood levels. A report of "moderately susceptible" suggests that the organism would be susceptible if high dosage is used or if the infection is confined to tissues and fluids in which high antimicrobial levels are attained. A report of "resistant" indicates that achievable concentrations are unlikely to be inhibitory, and other therapy should be selected. Standardized procedures require the use of laboratory control organisms. The 250- or 300-mcg sulfisoxazole disk should give the following zone diameters:<br/>Dilution Techniques: Use a standardized dilution method(broth, agar, microdilution) or equivalent with sulfisoxazole powder. The MIC values obtained should be interpreted according to the following criteria: As with standard diffusion techniques, dilution methods require the use of laboratory control organisms. Dilutions of standard sulfisoxazole powder should provide the following MIC values:
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dailymed-instance:supply
Pediatric Suspension (raspberry flavored), containing acetyl sulfisoxazole equivalent to approximately 0.5 gm sulfisoxazole per teaspoonful (5 mL)���bottles of 16 oz (1 pint) (NDC 0004-1003-28).
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dailymed-instance:overdosag...
The amount of a single dose of sulfisoxazole that is associated with symptoms of overdosage or is likely to be life-threatening has not been reported. Signs and symptoms of overdosage reported with sulfonamides include anorexia, colic, nausea, vomiting, dizziness, headache, drowsiness and unconsciousness. Pyrexia, hematuria and crystalluria may be noted. Blood dyscrasias and jaundice are potential late manifestations of overdosage. General principles of treatment include the immediate discontinuation of the drug; institution of gastric lavage or emesis; forcing oral fluids; and the administration of intravenous fluids if urine output is low and renal function is normal. The patient should be monitored with blood counts and appropriate blood chemistries, including electrolytes. If the patient becomes cyanotic, the possibility of methemoglobinemia should be considered and, if present, the condition should be treated appropriately with intravenous 1% methylene blue. If a significant blood dyscrasia or jaundice occurs, specific therapy should be instituted for these complications. Peritoneal dialysis is not effective and hemodialysis is only moderately effective in eliminating sulfonamides.
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acetyl sulfisoxazole
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Gantrisin (Suspension)
dailymed-instance:adverseRe...
The listing that follows includes adverse reactions both that have been reported with Gantrisin and some which have not been reported with this specific drug; however, the pharmacologic similarities among the sulfonamides require that each of the reactions be considered with the administration of Gantrisin. Allergic/Dermatologic: Anaphylaxis, erythema multiforme (Stevens-Johnson syndrome), toxic epidermal necrolysis, exfoliative dermatitis, angioedema, arteritis and vasculitis, allergic myocarditis, serum sickness, rash, urticaria, pruritus, photosensitivity, and conjunctival and scleral injection, generalized allergic reactions and generalized skin eruptions. In addition, periarteritis nodosa and systemic lupus erythematosus have been reported . Cardiovascular: Tachycardia, palpitations, syncope, cyanosis. Endocrine: The sulfonamides bear certain chemical similarities to some goitrogens, diuretics (acetazolamide and thiazides) and oral hypoglycemia agents. Cross-sensitivity may exist with these agents. Development of goiter, diuresis and hypoglycemia have occurred rarely in patients receiving sulfonamides. Gastrointestinal: Hepatitis, hepatocellular necrosis, jaundice, pseudomembranous colitis, nausea, emesis, anorexia, abdominal pain, diarrhea, gastrointestinal hemorrhage, melena, flatulence, glossitis, stomatitis, salivary gland enlargement, pancreatitis. Onset of pseudomembranous colitis symptoms may occur during or after treatment with sulfisoxazole . Sulfisoxazole has been reported to cause increased elevations of liver-associated enzymes in patients with hepatitis. Genitourinary: Crystalluria, hematuria, BUN and creatinine elevations, nephritis and toxic nephrosis with oliguria and anuria. Acute renal failure and urinary retention have also been reported. The frequency of renal complications, commonly associated with some sulfonamides, is lower in patients receiving the more soluble sulfonamides such as sulfisoxazole. Hematologic: Leukopenia, agranulocytosis, aplastic anemia, thrombocytopenia, purpura, hemolyticanemia, anemia, eosinophilia, clotting disorders including hypoprothrombinemia, and hypofibrinogenemia, sulfhemoglobinemia, methemoglobinemia. Musculoskeletal: Arthralgia, myalgia. Neurologic: Headache, dizziness, peripheral neuritis, paresthesia, convulsions, tinnitus, vertigo, ataxia, intracranial hypertension. Psychiatric: Psychosis, hallucination, disorientation, depression, anxiety, apathy. Respiratory: Cough, shortness of breath, pulmonary infiltrates . Vascular: Angioedema, arteritis, vasculitis. Miscellaneous: Edema (including periorbital), pyrexia, drowsiness, weakness, fatigue, lassitude, rigors, flushing, hearing loss, insomnia, pneumonitis, chills.
dailymed-instance:indicatio...
Acute, recurrent or chronic urinary tract infections (primarily pyelonephritis, pyelitis and cystitis) due to susceptible organisms (usually Escherichia coli, Klebsiella-Enterobacter, staphylococcus, Proteus mirabilis and, less frequently, Proteus vulgaris) in the absence of obstructive uropathy or foreign bodies. Meningococcal meningitis where the organism has been demonstrated to be susceptible. Haemophilus influenzae meningitis as adjunctive therapy with parenteral streptomycin. Meningococcal meningitis prophylaxis when sulfonamide-sensitive group A strains are known to prevail in family groups or larger closed populations. (The prophylactic usefulness of sulfonamides when group B or C infections are prevalent has not been proven and in closed population groups may be harmful.) Acute otitis media due to Haemophilus influenzae when used concomitantly with adequate doses of penicillin or erythromycin (see appropriate labeling for prescribing information). Trachoma. Inclusion conjunctivitis. Nocardiosis. Chancroid. Toxoplasmosis as adjunctive therapy with pyrimethamine. Malaria due to chloroquine-resistant strains of Plasmodium falciparum, when used as adjunctive therapy. Currently, the increasing frequency of resistant organisms is a limitation of the usefulness of antibacterial agents including the sulfonamides, especially in the treatment of chronic and recurrent urinary tract infections. Important Note: In vitro sulfonamide susceptibility tests are not always reliable. The test must be carefully coordinated with bacteriologic and clinical response. When the patient is already taking sulfonamides, follow-up cultures should have aminobenzoic acid added to the culture media.
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dailymed-instance:name
Gantrisin