Glimepiride

(BAN, USAN, rINN)
Synonyms: Glimepirid; Glimepirida; Glimépiride; Glimepiridi; Glimepiridum; Glimepiryd; Hoe-490. 1-({p-[2-(3-Ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl]phenyl}sulfonyl)-3-(trans-4-methylcyclohexyl)urea.
Cyrillic synonym: Глимепирид.

💊 Chemical information

Chemical formula: C24H34N4O5S = 490.6.
CAS — 93479-97-1.
ATC — A10BB12.
ATC Vet — QA10BB12.

Pharmacopoeias.

In Eur. and US.

Ph. Eur. 6.2

(Glimepiride). A white to almost white powder. It exhibits polymorphism. Practically insoluble in water; slightly soluble in dichloromethane; soluble in dimethylformamide; very slightly soluble in methyl alcohol.

USP 31

(Glimepiride). A white to almost white powder. Practically insoluble in water; sparingly soluble in dichloromethane; soluble in dimethylformamide; slightly soluble in methyl alcohol. It dissolves in dilute alkali hydroxides and in dilute acids. Store at a temperature not exceeding 25°.

💊 Adverse Effects, Treatment, and Precautions

In some countries hepatic and haematological monitoring is recommended in patients receiving glimepiride; in the UK the BNF considers the practical value of such monitoring unproven.

Fasting.

Glimepiride, given in unchanged doses but with the time of the single daily dose switched from morning to just before breaking fast after sunset, was used in Muslim patients during Ramadan without causing an increased incidence of hypoglycaemic episodes.1 For further advice on the management of diabetes mellitus in fasting Muslim patients during Ramadan see under Precautions of Insulin.
1. The Glimepiride in Ramadan (GLIRA) Study Group. The efficacy and safety of glimepiride in the management of type 2 diabetes in Muslim patients during Ramadan. Diabetes Care 2005; 28: 421–2.

💊 Pharmacokinetics

Glimepiride is completely absorbed from the gastrointestinal tract. Peak plasma concentrations occur in 2 to 3 hours, and it is highly protein bound. The drug is extensively metabolised to two main metabolites, a hydroxy derivative and a carboxy derivative. The half-life after multiple doses is about 9 hours. About 60% of a dose is eliminated in the urine and 40% in the faeces.

💊 Uses and Administration

Glimepiride is a sulfonylurea antidiabetic. It is given orally for the treatment of type 2 diabetes mellitus. Initial doses of 1 to 2 mg daily may be increased if necessary to 4 mg daily for maintenance. The maximum recommended dose is 6 mg in the UK and 8 mg in the USA.
1. Langtry HD, Balfour JA. Glimepiride: a review of its use in the management of type 2 diabetes mellitus. Drugs 1998; 55: 563–84
2. Campbell RK. Glimepiride: role of a new sulfonylurea in the treatment of type 2 diabetes mellitus. Ann Pharmacother 1998; 32: 1044–52
3. McCall AL. Clinical review of glimepiride. Expert Opin Pharmacother 2001; 2: 699–713
4. Massi-Benedetti M. Glimepiride in type 2 diabetes mellitus: a review of the worldwide therapeutic experience. Clin Ther 2003; 25: 799–816
5. Weitgasser R, et al. Effects of glimepiride on HbA(1c) and body weight in type 2 diabetes: results of a 1.5-year follow-up study. Diabetes Res Clin Pract 2003; 61: 13–19
6. Feinbock C, et al. Prospective multicentre trial comparing the efficacy of, and compliance with, glimepiride or acarbose treatment in patients with type 2 diabetes not controlled with diet alone. Diabetes Nutr Metab 2003; 16: 214–21.

💊 Preparations

USP 31: Glimepiride Tablets.

Proprietary Preparations

Arg.: Adiuvan; Amaryl; Endial; Glemaz; Gluceride; Glucopirida; Islopir; Lomet; Next Step; Austral.: Amaryl; Aylide; Diapride; Dimirel; Austria: Amaryl; Belg.: Amarylle; Braz.: Amaryl; Azulix; Bioglic; Diamellitis; Glimepibal; Glimepil; Glimeprid†; Glimeran; Glimesec†; Hipomeril; Canad.: Amaryl; Chile: Amaryl; Glemaz; Glucomet; Cz.: Amarwin; Amaryl; Amyx; ApoGlimep; Eglymad; Glemid; GlimTek; Glymexan; Melyd; Metis; Oltar; Denm.: Amaryl; Fin.: Amaryl; Fr.: Amarel; Ger.: Amaryl; Glimegamma; Glimerid; Gr.: Dialosa; Glimepiron; Glimespes; Glimexin; Gliperin; Mepirid; Penoza; Pharlecon; Saccharofar; Solosa; Sucryl; Tipo II; Toremol; Hong Kong: Amaryl; Diapride; Hung.: Amaryl; Dialosa; Glempid; GlimeWin; Glindia; Gliprex; Limeral; Meglimid; Melyd; Sintecal; India: Amaryl; Betaglim†; Diaglim; Euglim; Glimcip; Glimiprex; Glimitab; Glimulin; Glyree; Glyree M; Karmelitos; Indon.: Amadiab; Amaryl; Anpiride; Glamarol; Glimexal; Gluvas; Mapryl; Metrix; Relide; Irl.: Amaryl; Israel: Amaryl; Ital.: Amaryl; Solosa; Malaysia: Amaryl; Diapride; Glimaryl; Glimin; Glimulin; Miaryl; Mex.: Amaryl; Glupropan; Zukedib; Neth.: Amaryl; Norw.: Amaryl; NZ: Amaryl; Philipp.: Imerid; Norizec; Solosa; Pol.: Amaryl; Amyx; Avaron; Betaglid; Diaril; Glemid; Glibetic; Glibezid; Glidiamid; Glimehexal; Glimesan; Glipid; Limeral; Melyd; Oltar; Pemidal; Symglic; Port.: Amaryl; Diapiride; Glimial; Gludon; Rus.: Amaryl (Амарил); Glemaz (Глемаз); S.Afr.: Amaryl; Glamaryl; Singapore: Amaryl; Diapride; Spain: Amaryl; Roname; Swed.: Amaryl; Switz.: Amaryl; Thai.: Amaryl; Turk.: Amaryl; Diameprid; Glimax; UK: Amaryl; Niddaryl; USA: Amaryl; Venez.: Amaryl; Dimavyl; Glimerid. Multi-ingredient: Cz.: Avaglim; Tandemact; Fr.: Avaglim; Tandemact; Gr.: Avaglim; Hung.: Avaglim; India: Betaglim M†; Exermet GM; Glimiprex MF; Glimulin-MF†; Indon.: Avandaryl; Mex.: Glimetal; Port.: Avaglim; Tandemact; USA: Avandaryl; Duetact.
Published October 27, 2018.