In its unaltered active state, sulfadiazine is quickly absorbed and nearly totally eliminated in the urine [1].

Absorption, Distribution and Excretion
Well absorbed following oral administration.
Sulfacytine...is rapidly absorded following oral administration. More than 90% is excreted by kidneys almost entirely in the free, active form. ...86% is bound to serum proteins. ...The drug crosses the placenta & is excreted in milk...
By comparison to sulfisoxazole urine levels, 1 g/day of sulfacytine appears to be appropriate therapeutic dose & produces urine concn at least 10 times highest min inhibitory concentration found for sensitive microorganisms.
Sulfacytine is highly soluble in urine within the normal acidic pH range.
Thirty-four subjects were divided into 3 groups of 12, 12, and 10 respectively. The first group received 250 mg /sulfacytine/ 4 times a day, the second, 500 mg 4 times a day, and the third group received placebo. The renal function was not altered during the 84 days of the trial. Creatinine clearance, urea nitrogen, urinalysis, and phenosulfophthalein excretion tests were performed to evaluate kidney function.
For more Absorption, Distribution and Excretion (Complete) data for SULFACYTINE (11 total), please visit the HSDB record page.

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Metabolism / Metabolites
Sulfonamides undergo metabolic alterations to varying extent in tissues, especially in liver. Both acetylation & oxidation occur. ... In nearly all species, major metabolic derivative is N4-acetylated sulfonamide. /Sulfonamides/
Although the liver is the major site of metabolism, sulfonamides may also be metabolized in other body tissues. Most sulfonamides are metabolized mainly by N4-acetylation. The degree of acetylation, which is a function of time, varies from less than 5% for sulfamethizole to up to 40% for sulfadiazine. The N4-acetyl metabolites, which do not possess antibacterial activity, have greater affinity for plasma albumin than does the nonacetylated drug and are usually less soluble than the parent sulfonamide, particularly in acidic urine. Like acetyl derivatives, glucuronide derivatives do not possess antibacterial activity; however, glucuronide derivatives are water soluble, appear to resemble the nonacetylated sulfonamide in plasma binding capacity, and have not been associated with adverse effects. /Sulfonamides/

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Biological Half-Life
Sulfacytine has a biological half-life of approximately 4 hrs...

Interactions
These medications /coumarin- or indandione-derivative anticoagulants; hydantoin anticonvulsants or oral antidiabetic agents/ may be displaced from protein binding sites and/or their metabolism may be inhibited by some sulfonamides, resulting in increased or prolonged effects and/or toxicity; dosage adjustments may be necessary during and after sulfonamide therapy. /Sulfonamides/
Concurrent use of bone marrow depressants with sulfonamides may increase the leukopenic and/or thrombocytopenic effects; if concurrent use is required, close observation for myelotoxic effects should be considered. /Sulfonamides/
Concurrent long-term use of sulfonamides /with estrogen-containing, oral contraceptives/ may result in increased incidence of breakthrough bleeding and pregnancy. /Sulfonamides/
Concurrent use /of cyclosporine/ with sulfonamides may increase the metabolism of cyclosporine, resulting in decreased plasma concentration and potential transplant rejection, and additive nephrotoxicity; plasma cyclosporine concentrations and renal function should be monitored. /Sulfonamides/
For more Interactions (Complete) data for SULFACYTINE (13 total), please visit the HSDB record page.

[1]. J Hughes, et al. Sulfacytine: A New Sulfonamide. Double-blind Comparison With Sulfisoxazole in Acute Uncomplicated Urinary Tract Infections. J Urol. 1975 Dec;114(6):912-4.

Therapeutic Uses
Anti-Infective Agents /SRP: Antibacterial/
Sulfacytine is used to treat acute urinary tract infections caused by susceptible strains of Escherichia coli, the Klebsiella-Enterobacter group, Staphylococcus aureus, Proteus mirabilis, & less frequently, Proteus vulgaris.
Sulfonamides are indicated in the treatment of chancroid caused by Hemophilus ducreyi. However, other agents such as erythromycin and ceftriaxone, are considered to be first line agents. /Sulfonamides; Included in US product labeling/
Sulfonamides are indicated in the treatment of endocervical and urethral infections caused by Chlamydia trachomatis. However, other agents, such as doxycycline and azithromycin, are considered to be first line agents. /Sulfonamides; Included in US product labeling/
For more Therapeutic Uses (Complete) data for SULFACYTINE (15 total), please visit the HSDB record page.

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Drug Warnings
The number of conditions for which the sulfonamides are therapeutically useful and constitute drugs of first choice has been reduced sharply by the development of more effective antimicrobial agents and by the gradual increase in the resistance of a number of bacterial species to this class of drugs. /Sulfonamides/
Although the risk of crystalluria apparently is minimal, fluid intake should be increased when this drug is prescribed. Sulfacytine should be used with caution in patients with impaired renal function.
...Because no well-controlled clinical studies exist.../sulfacytine/ should not be used during pregnancy unless the expected benefits outweigh the possible adverse effects of the drug.
Sulfacytine is contraindicated in individuals allergic to sulfonamides.
For more Drug Warnings (Complete) data for SULFACYTINE (26 total), please visit the HSDB record page.

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Pharmacodynamics
Sulfacytine is a short-acting sulfonamide. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus.

C12H14N4O3S

294.329

294.079

17784-12-2

5322

Crystals from butyl alcohol, methanol
Crystalline

1.45g/cm3

496.8ºC at 760mmHg

166.5-168ºC

254.2ºC

5.25E-10mmHg at 25°C

1.664

2.381

2

4

4

20

527

0

CCN1C=CC(=NC1=O)NS(=O)(=O)C2=CC=C(C=C2)N

SIBQAECNSSQUOD-UHFFFAOYSA-N

InChI=1S/C12H14N4O3S/c1-2-16-8-7-11(14-12(16)17)15-20(18,19)10-5-3-9(13)4-6-10/h3-8H,2,13H2,1H3,(H,14,15,17)

4-amino-N-(1-ethyl-2-oxopyrimidin-4-yl)benzenesulfonamide

CI 636; CI-636; CI636

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~125 mg/mL (~424.69 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)