Glipizide

(BAN, USAN, pINN)
Glipizide Chemical formula
Synonyms: CP-28720; Glipitsidi; Glipizid; Glipizida; Glipizidas; Glipizidum; Glipizyd; Glydiazinamide; K-4024. 1Cyclohexyl-3-{4-[2-(5-methylpyrazine-2-carboxamido)ethyl]benzenesulphonyl}urea.
Cyrillic synonym: Глипизид.

💊 Chemical information

Chemical formula: C21H27N5O4S = 445.5.
CAS — 29094-61-9.
ATC — A10BB07.
ATC Vet — QA10BB07.

Pharmacopoeias.

In Chin., Eur., and US.

Ph. Eur. 6.2

(Glipizide). A white or almost white crystalline powder. Practically insoluble in water and in alcohol; very slightly soluble in acetone and in dichloromethane. It dissolves in dilute solutions of alkali hydroxides.

USP 31

(Glipizide). Store in airtight containers. Protect from light.

💊 Adverse Effects, Treatment, and Precautions

Porphyria.

Glipizide has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.

💊 Interactions

Antacids.

Magnesium hydroxide and sodium bicarbonate have been reported to increase the rate of absorption, although not the total amount absorbed, of a dose of glipizide in healthy subjects.1,2 No such effect was seen with aluminium hydroxide.2
1. Kivisto KT, Neuvonen PJ. Enhancement of absorption and effect of glipizide by magnesium hydroxide. Clin Pharmacol Ther 1991; 49: 39–43
2. Kivisto KT, Neuvonen PJ. Differential effects of sodium bicarbonate and aluminium hydroxide on the absorption and activity of glipizide. Eur J Clin Pharmacol 1991; 40: 383–6.

💊 Pharmacokinetics

Glipizide is readily absorbed from the gastrointestinal tract with peak plasma concentrations occurring 1 to 3 hours after a single dose. It is extensively bound to plasma proteins and has a half-life of about 2 to 4 hours. It is metabolised mainly in the liver and excreted chiefly in the urine, largely as inactive metabolites.

💊 Uses and Administration

Glipizide is a sulfonylurea antidiabetic. It is given orally in the treatment of type 2 diabetes mellitus and has a duration of action of up to 24 hours. The usual initial dose is 2.5 to 5 mg daily given as a single dose about 30 minutes before breakfast. Dosage may be adjusted at intervals of several days by amounts of 2.5 to 5 mg daily, to a maximum of 20 mg daily. Doses up to 40 mg daily have been used, but see below. Doses larger than 15 mg daily are given in two divided doses before meals. Modified-release formulations of glipizide are available in some countries; one such preparation (Glucotrol XL; Pfizer, USA) is given in doses of 5 to 10 mg daily as a single dose with breakfast.

Administration.

Although glipizide may be given in doses up to a maximum of 40 mg daily, evidence for the benefits of high doses is scanty. A small study in patients with type 2 diabetes mellitus found that not only did increases in glipizide doses to more than 10 mg daily produce little or no benefit, but that the higher doses were associated with reduced rises in plasmainsulin concentrations and a lesser reduction in plasma-glucose concentrations.1 There is, however, some evidence that glycaemic control and insulin sensitivity can be improved by the use of a modified-release rather than a conventional formulation of glipizide.2,3
1. Stenman S, et al. What is the benefit of increasing the sulfonylurea dose? Ann Intern Med 1993; 118: 169–72
2. Berelowitz M, et al. Comparative efficacy of once-daily controlled-release formulation of glipizide and immediate-release glipizide in patients with NIDDM. Diabetes Care 1994; 17: 1460–4
3. Leaf E, King JO. Patient outcomes after formulary conversion from immediate-release to extended-release glipizide tablets. Am J Health-Syst Pharm 1999; 56: 454–6.

💊 Preparations

BP 2008: Glipizide Tablets; USP 31: Glipizide and Metformin Hydrochloride Tablets; Glipizide Tablets.

Proprietary Preparations

Arg.: Minodiab; Austral.: Melizide; Minidiab; Austria: Glibenese; Minidiab; Belg.: Glibenese; Minidiab; Braz.: Glipgen†; Minidiab; Chile: Minidiab; Xiprine; Cz.: Antidiab†; Glucotrol†; Mediab†; Minidiab; Denm.: Glibenese; Mindiab; Fin.: Apamid†; Glibenese; Melizid; Mindiab; Fr.: Glibenese; Minidiab; Ozidia; Gr.: Glibenese; Minodiab†; Hong Kong: Diasef; Glucotrol; Minidiab; Sunglucon; Hung.: Minidiab; India: Diaglip; Glez; Glide; Glipicontin†; Glucolip; Glynase; Glyzip; Indon.: Aldiab; Glucotrol; Glyzid; Irl.: Glibenese; Israel: Gluco-Rite; Ital.: Minidiab; Malaysia: Dibizide†; Dipazide; Glix; Melizide; Minidiab; Mex.: Glupitel†; Luditec; Minodiab; Pigloss; Singloben; Neth.: Glibenese†; Norw.: Apamid; Mindiab; NZ: Glipid†; Minidiab; Philipp.: Glix; Minidiab; Pol.: Antidiab; Glibenese; Port.: Minidiab; Rus.: Glibenese (Глибенез); Minidiab (Минидиаб)†; S.Afr.: Minidiab; Singapore: Beapizide; Diactin; Diasef; Melizide; Minidiab; Spain: Glibenese†; Minodiab; Swed.: Apamid†; Glipiscand†; Mindiab; Switz.: Glibenese; Thai.: Apamid†; Depizide; Diasef; Dipazide; Gipzide; Glipimed; Glizide; Glucodiab; Glygen; GP-Zide; Melizide; Minibit; Minidiab; Namedia; Pezide; Turk.: Glucotrol; Minidiab; UK: Glibenese; Minodiab; USA: Glucotrol; Venez.: Minidiab. Multi-ingredient: India: Diaglip M; Metaglez; USA: Metaglip.
Published October 29, 2018.