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| Targets |
Sulfadiazine sodium acts as a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase (DHPS). This enzyme is essential for the proper processing of para-aminobenzoic acid (PABA), which is required for folic acid synthesis in bacteria. By inhibiting DHPS, sulfadiazine blocks the conversion of pteridine and PABA to dihydropteroate, an intermediate in folate biosynthesis. This inhibits the production of folic acid necessary for bacterial growth and multiplication. The compound shows broad-spectrum activity against gram-positive bacteria, gram-negative bacteria, and Chlamydia. Sulfadiazine sodium is classified as a folate synthesis inhibitor.
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| ln Vitro |
Sulfadiazine sodium exhibits broad-spectrum antibacterial activity against a range of gram-positive and gram-negative bacteria. Its mechanism of action is bacteriostatic rather than bactericidal, as it inhibits bacterial growth by blocking folic acid synthesis. The compound’s activity is assessed using standard broth dilution or agar diffusion methods to determine minimum inhibitory concentrations (MICs) against various bacterial strains. In vitro studies have confirmed its efficacy against organisms such as Escherichia coli, Staphylococcus aureus, and Streptococcus species. The presence of PABA in the medium can antagonize sulfadiazine’s activity, as PABA competes with the drug for binding to DHPS.
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| ln Vivo |
This study assessed the efficacy of pyrimethamine and sodium sulfadiazine in treating mice infected with various atypical Toxoplasma gondii during an acute infection. A total of seven strains of Toxoplasma gondii were injected into Swiss mice. Treatment for the infected mice involved giving them 10-640 mg/kg of sodium sulfadiazine, 3-200 mg/kg of pyrimethamine, or a less potent combination of the two medications every day. The relationship between genotype and sensitivity to sodium and/or pyrimethamine was assessed using descriptive analysis. Treatment with salt or pyrimethamine decreased the sensitivity of the TgCTBr4 and TgCTBr17 strains (genotype 108). Similar sensitivity to PYR was seen in TgCTBr1 and TgCTBr25 strains (genotype 206), but not in response to salt treatment. The only strain that responds well to treatment with both medications is the TgCTBr9 strain (genotype 11) [1].
Sulfadiazine sodium is used in vivo to treat systemic infections in both humans and animals. It is effective against urinary tract infections, respiratory tract infections, toxoplasmosis, and other susceptible infections. In veterinary medicine, it is used to treat infections in domestic animals, including respiratory and urinary tract infections, mastitis, uterine sarcoiditis, and peritonitis. The compound also exhibits antimalarial activity and may be utilized in the study of toxoplasmosis. Its efficacy depends on the susceptibility of the infecting organism and the ability to achieve adequate drug concentrations at the site of infection. |
| Enzyme Assay |
Sulfadiazine sodium is a competitive inhibitor of dihydropteroate synthetase (DHPS), and in vitro enzyme assays are used to characterize this interaction. These assays typically involve incubating the enzyme with its substrate (pteridine and PABA) in the presence of varying concentrations of sulfadiazine. The reaction product, dihydropteroate, is measured spectrophotometrically or by other analytical methods. The inhibition constant (Ki) is calculated from enzyme kinetics data. These assays demonstrate that sulfadiazine competitively inhibits DHPS by mimicking PABA, thereby blocking the enzyme’s active site and preventing folic acid synthesis.
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| Cell Assay |
Sulfadiazine sodium is tested in vitro using standard microbiological susceptibility assays. Broth microdilution or agar dilution methods are employed to determine the minimum inhibitory concentration (MIC) against bacterial isolates. Susceptibility testing follows guidelines such as those from the Clinical and Laboratory Standards Institute (CLSI). Bacterial cultures are grown in appropriate media, and serial dilutions of sulfadiazine sodium are added. After incubation, the MIC is determined as the lowest concentration that inhibits visible bacterial growth. Cytotoxicity assays in mammalian cell lines may also be performed to assess the compound’s selectivity and safety profile.
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| Animal Protocol |
In vivo animal experiments with sulfadiazine sodium are conducted in various animal models of bacterial infection. Rodent models of urinary tract infection, pneumonia, or systemic bacterial infection are commonly used. Animals are infected with a pathogenic bacterial strain, and sulfadiazine sodium is administered via injection or oral gavage at varying doses. Efficacy endpoints include survival rates, bacterial load in tissues (e.g., kidneys, lungs, blood), and clinical signs of infection. Pharmacodynamic parameters such as the ratio of area under the curve (AUC) to MIC are calculated to optimize dosing regimens. Toxicity and tolerability are also assessed in these studies.
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| ADME/Pharmacokinetics |
Sulfadiazine sodium is well absorbed after oral administration and distributes widely throughout body tissues and fluids, including cerebrospinal fluid. The drug is metabolized in the liver, primarily by acetylation, and excreted in the urine. The sodium salt form is highly water-soluble (50 mg/mL), making it suitable for intravenous or intramuscular administration. In veterinary species, the pharmacokinetic profile varies depending on the species and formulation. The drug’s elimination half-life is influenced by renal function, as it is primarily excreted unchanged and as metabolites via the kidneys. Dosage adjustments may be necessary in patients with impaired renal function to avoid accumulation and toxicity.
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| Toxicity/Toxicokinetics |
The most common adverse effects of sulfadiazine sodium are hypersensitivity reactions, including skin rashes and, rarely, Stevens-Johnson syndrome. Hematological effects such as agranulocytosis, hemolytic anemia, and thrombocytopenia have been reported. Renal toxicity, including crystalluria and interstitial nephritis, can occur due to precipitation of the drug and its metabolites in the urine, particularly at high doses or with inadequate fluid intake. Gastrointestinal disturbances such as nausea, vomiting, and diarrhea may also occur. The compound is contraindicated in patients with known sulfonamide hypersensitivity, porphyria, or severe renal impairment. Toxicological studies have shown that sulfadiazine is generally well-tolerated at therapeutic doses.
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| References |
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| Additional Infomation |
Sulfadiazine sodium is the sodium salt form of sulfadiazine, a moderately potent antibacterial synthetic sulfonamide derivative. See also: sulfadiazine (with active moiety); pyrimethamine; sulfadiazine sodium (component); sulfadiazine sodium; trimethoprim (component).
Sulfadiazine sodium is classified as a sulfonamide antibiotic and is available for both human and veterinary use. In veterinary medicine, it is used to treat systemic infections in domestic animals. The compound is on the WHO Model List of Essential Medicines. It is often used in combination with other agents, such as pyrimethamine, for the treatment of toxoplasmosis. The sodium salt formulation enhances aqueous solubility, allowing for parenteral administration. Drug resistance can develop through mutations in the DHPS gene or by increased production of PABA. Monitoring of susceptibility patterns is important for guiding therapy. Sulfadiazine sodium has a well-established safety and efficacy profile from decades of clinical use. |
| Molecular Formula |
C10H9N4NAO2S
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|---|---|
| Molecular Weight |
272.2588
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| Exact Mass |
272.034
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| CAS # |
547-32-0
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| Related CAS # |
Sulfadiazine;68-35-9;Sulfadiazine-d4;1020719-78-1
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| PubChem CID |
15899898
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| Appearance |
White to off-white solid powder
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| Density |
1.496g/cm3
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| Boiling Point |
512.6ºC at 760 mmHg
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| Flash Point |
263.8ºC
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| LogP |
2.38
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
332
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JLDCNMJPBBKAHH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H9N4O2S.Na/c11-8-2-4-9(5-3-8)17(15,16)14-10-12-6-1-7-13-10;/h1-7H,11H2;/q-1;+1
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| Chemical Name |
sodium;(4-aminophenyl)sulfonyl-pyrimidin-2-ylazanide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~459.12 mM)
H2O : ~100 mg/mL (~367.30 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6730 mL | 18.3648 mL | 36.7296 mL | |
| 5 mM | 0.7346 mL | 3.6730 mL | 7.3459 mL | |
| 10 mM | 0.3673 mL | 1.8365 mL | 3.6730 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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