Synonyms
6-Chloro-2-sodio-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
Molecular Formula
C7H5ClN3NaO4S2
Smiles
C1=C2C(=CC(=C1Cl)S(=O)(=O)N)S(=O)(=O)[N-]C=N2.[Na+]
General Description
Chlorothiazide Sodium is the sodium salt of chlorothiazide, the first synthetically developed thiazide diuretic approved for clinical use. It is the parent compound of the thiazide diuretic class and contains a sulfonamide group and a chloro substituent on the benzothiadiazine ring system.
Mechanism of Action
Chlorothiazide Sodium inhibits the sodium-chloride cotransporter (NCC/SLC12A3) in the distal convoluted tubule of the kidney, reducing sodium and chloride reabsorption. This increases urinary sodium, chloride, and water excretion, and secondarily promotes potassium loss through increased distal tubular sodium delivery.
Application
Indicated for the treatment of hypertension and edema. Chlorothiazide Sodium is the first thiazide diuretic, inhibiting sodium-chloride reabsorption in the distal convoluted tubule to promote natriuresis and diuresis. It is the prototypical agent of the entire thiazide diuretic class used worldwide.
Chlorothiazide sodium mucoadhesive sustained-release pellets were developed using extrusion-spheronization technique to overcome the drug's poor and variable oral bioavailability caused by site-specific absorption in the upper gastrointestinal tract and carrier-mediated saturable transport. The formulation was optimized using a 32 full factorial design with HPMC K15M and polycarbophil as independent variables. The optimized pellets achieved sustained drug release over 12 hours and over 90 percent mucoadhesion after 8 hours in vivo. Pharmacokinetic studies in rats demonstrated a 2.93-fold improvement in bioavailability compared to conventional chlorothiazide formulations. FTIR and PXRD analyses confirmed the stability of chlorothiazide in the pellet formulation, confirming the feasibility of this mucoadhesive sustained-release approach for enhancing therapeutic outcomes.
Fig. 2 Preparation and characterization of Chlorothiazide Sodium mucoadhesive controlled-release pellets. (Borkhataria C.; et al. 2025)
References
- Borkhataria C, et al. Development and optimization of mucoadhesive sustained-release chlorothiazide pellets for improved bioavailability: A response surface methodology based approach. Journal of Drug Delivery Science and Technology, 2025, 108: 106951.
Why is Chlorothiazide Sodium the founding compound for thiazide diuretics?
Chlorothiazide is the first and structurally simplest thiazide diuretic, making it the essential reference for studying pharmacophore requirements and structure-activity relationships of the entire class.
What storage conditions are required?
Must be stored under -20℃ in a tightly sealed container, protected from light and moisture.
What purity grade is available?
Supplied as a high-purity grade suitable for R&D and pharmaceutical manufacturing.
Can packaging be customized?
Order quantities and packaging formats are customizable upon request for R&D and production needs.