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| Systematic (IUPAC) name | |
|---|---|
| N-(hexahydrocyclopenta[c]pyrrol-2(1H)-ylcarbamoyl)-4-methylbenzenesulfonamide | |
| Identifiers | |
| CAS number | 21187-98-4 |
| ATC code | A10BB09 |
| PubChem | 3475 |
| DrugBank | APRD00460 |
| Chemical data | |
| Formula | C15H21N3O3S |
| Mol. mass | 323.412 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
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Gliclazide is an oral hypoglycemic (anti-diabetic drug) and is classified as a sulfonylurea. It is marketed as Diamicron and Dianorm in India. The modified-release formulation of Diamicron is marketed as Remicron MR, Diabeton MR, Diamicron 30mg, Diamicron LM 30mg, Diamicron MR 30 mg, Diamicron Uno 30mg, Dianormax MR, Diaprel MR and Uni Diamicron.
Its classification has been ambiguous as literature uses it as both a first-generation [1] and second-generation[2] sulfonylurea.
Contents |
Form and Composition
Each tablet contains 80 mg of gliclazide.
Not marketed in the United States and Philippines. In the Philippines, it is marketed under the brandname of Glubitor-OD 30mg or 80mg.
Indication
Control of hyperglycemia in gliclazide responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity onset or adult type which cannot be controlled by proper dietary management and exercise, or when insulin therapy is not appropriate.
Dosage
40 to 320 mg depending on response, once or twice daily before food, no more than 160 mg at a time. for diabetes pateint
Properties
Hypoglycemic sulfonylurea, restoring first peak of insulin secretion, increasing insulin sensitivity. Glycemia-independent hemovascular effects, antioxidant effect. No active circulating metabolites.
Contraindications
type 1 diabetes, hypersensitivity to sulfonylureas, severe renal or hepatic failure, pregnancy and lactation, miconazole coprescription.
Metabolism
Gliclazide undergoes extensive metabolism to several inactive metabolites in humans, mainly methylhydroxygliclazide and carboxygliclazide. CYP2C9 is involved in the formation of hydroxygliclazde in human liver microsomes and in a panel of recombinant human P450sin vitro[3][4]. But the pharmacokinetics of gliclazide MR are affected mainly by CYP2C19 genetic polymorphism instead of CYP2C9 genetic polymorphism.[5][6]
Interactions
Hyperglycemic action may be caused by danazol, chlorpromazine, glucocorticoids, progestogens, β-2 agonists. Its hypoglycemic action may be potentiated by phenylbutazone, alcohol, fluconazole, β-blockers, possibly ACE inhibitors. Park et al.have found that rifampin increases gliclazide metabolism in humans in vivo.[7]
Adverse effects
Hypoglycemia, gastrointestinal disturbance (reported), skin reactions (rare), hematological disorders (rare), hepatic enzyme rises (exceptional).
Overdosage
Possible severe hypoglycemia requiring urgent IV glucose and monitoring.
References
- ^ Ballagi-Pordány G, Köszeghy A, Koltai MZ, Aranyi Z, Pogátsa G (January 1990). "Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compounds". Diabetes Res. Clin. Pract. 8 (2): 109–14. doi:. PMID 2106423.
- ^ Shimoyama T, Yamaguchi S, Takahashi K, et al (2006). "Gliclazide protects 3T3L1 adipocytes against insulin resistance induced by hydrogen peroxide with restoration of GLUT4 translocation". Metabolism - Clinical and Experimental 55 (6): 722-30. PMID 16713429.
- ^ Rieutord A, Stupans I, Shenfield GM, Gross AS. Gliclazide hydroxylation by rat liver microsomes. Xenobiotica 1995; 25: 1345–54.
- ^ Identification of the human cytochromes P450 catalysing the rate-limiting pathways of gliclazide elimination. Elliot DJ, Suharjono, Lewis BC, Gillam EM, Birkett DJ, Gross AS, Miners JO. Br J Clin Pharmacol. 2007 Oct;64(4):450-7.
- ^ Influence of CYP2C9 and CYP2C19 genetic polymorphisms on pharmacokinetics of gliclazide MR in Chinese subjects.Zhang Y, Si D, Chen X, Lin N, Guo Y, Zhou H, Zhong D.Br J Clin Pharmacol. 2007 Jul;64(1):67-74. [1]
- ^ Effects of St John's wort and CYP2C9 genotype on the pharmacokinetics and pharmacodynamics of gliclazide. Xu H, Williams KM, Liauw WS, Murray M, Day RO, McLachlan AJ. Br J Pharmacol. 2008 Apr;153(7):1579-86.
- ^ Park JY, Kim KA, Park PW, Park CW, Shin JG. Effect of rifampin on the pharmacokinetics and pharmacodynamics of gliclazide. Clin Pharmacol Ther 2003; 74: 334–40.
External links
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