Gliclazide

• CAT Number: A000219
• CAS Number: 21187-98-4
• Molecular Formula: C15H21N3O3S
• Molecular Weight: 323.41
• Purity: ≥95%
• Synonyms: 21187-98-4; Glimicron; Diamicron; Nordialex; Diaikron
• Target: Potassium Channel
• Solubility: >15.6mg/mL in DMSO
• Storage: -20°C
• InChI: 1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)
• InChIKey: BOVGTQGAOIONJV-UHFFFAOYSA-N
• SMILES: CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2CC3CCCC3C2

Gliclazide is an oral anti-hyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus. It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels.

Reference

1: Vatsavai LK, Kilari EK. Interaction of p-Synephrine on the pharmacodynamic and
pharmacokinetics of gliclazide in animal models. J Ayurveda Integr Med. 2017 Nov
2. pii: S0975-9476(16)30487-9. doi: 10.1016/j.jaim.2017.04.010. [Epub ahead of
print] PubMed PMID: 29103851.

2: Danafar H, Jaberizadeh H, Andalib S. In vitro and in vivo delivery of
gliclazide loaded mPEG-PCL micelles and its kinetic release and solubility study.
Artif Cells Nanomed Biotechnol. 2017 Nov 3:1-12. doi:
10.1080/21691401.2017.1386191. [Epub ahead of print] PubMed PMID: 29099241.

3: Mikov M, Đanić M, Pavlović N, Stanimirov B, Goločorbin-Kon S, Stankov K,
Al-Salami H. Potential Applications of Gliclazide in Treating Type 1 Diabetes
Mellitus: Formulation with Bile Acids and Probiotics. Eur J Drug Metab
Pharmacokinet. 2017 Oct 16. doi: 10.1007/s13318-017-0441-y. [Epub ahead of print]
PubMed PMID: 29039071.

4: Bruni G, Berbenni V, Maggi L, Mustarelli P, Friuli V, Ferrara C, Pardi F,
Castagna F, Girella A, Milanese C, Marini A. Multicomponent crystals of
gliclazide and tromethamine: preparation, physico-chemical, and pharmaceutical
characterization(). Drug Dev Ind Pharm. 2017 Oct 17:1-8. doi:
10.1080/03639045.2017.1386208. [Epub ahead of print] PubMed PMID: 28956461.

5: Zhang YW, Wang X, Ren X, Zhang M. Involvement of Glucose-regulated Protein 78
and Spliced X-box Binding Protein 1 in the Protective Effect of Gliclazide in
Diabetic Nephropathy. Diabetes Res Clin Pract. 2017 May 4. pii:
S0168-8227(16)30699-4. doi: 10.1016/j.diabres.2017.04.019. [Epub ahead of print]
PubMed PMID: 28951332.

6: Żurawska-Płaksej E, Rorbach-Dolata A, Wiglusz K, Piwowar A. The effect of
glycation on bovine serum albumin conformation and ligand binding properties with
regard to gliclazide. Spectrochim Acta A Mol Biomol Spectrosc. 2018 Jan
15;189:625-633. doi: 10.1016/j.saa.2017.08.071. Epub 2017 Sep 6. PubMed PMID:
28888191.

7: Kalra S, Das AK. Epidemiologic Surveillance of Glycemic Response to a Scored,
Breakable, Extended Release, Fixed Dose Combination of Gliclazide and Metformin
in Persons with Type 2 Diabetes. J Assoc Physicians India. 2017 Jun;65(6):38-41.
PubMed PMID: 28782312.

8: Lee JY, Kim G, Lee YH, Lee BW, Cha BS, Nam CM, Kang ES. Comparison of
hepatocellular carcinoma risk between patients treated with glimepiride and
gliclazide. Diabetes Metab. 2017 Aug 1. pii: S1262-3636(17)30471-8. doi:
10.1016/j.diabet.2017.06.007. [Epub ahead of print] PubMed PMID: 28778564.

9: Huang S, O/’Donnell KP, Delpon de Vaux SM, O/’Brien J, Stutzman J, Williams RO
3rd. Processing thermally labile drugs by hot-melt extrusion: The lesson with
gliclazide. Eur J Pharm Biopharm. 2017 Oct;119:56-67. doi:
10.1016/j.ejpb.2017.05.014. Epub 2017 Jun 3. PubMed PMID: 28583588.

10: Golocorbin-Kon S, Calasan J, Milijasevic B, Vukmirovic S, Lalic-Popovic M,
Mikov M, Al-Salami H. High-Loading Dose of Microencapsulated Gliclazide
Formulation Exerted a Hypoglycaemic Effect on Type 1 Diabetic Rats and
Incorporation of a Primary Deconjugated Bile Acid, Diminished the Hypoglycaemic
Antidiabetic Effect. Eur J Drug Metab Pharmacokinet. 2017 May 25. doi:
10.1007/s13318-017-0415-0. [Epub ahead of print] PubMed PMID: 28547295.