Glipizide

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: CP-28720; Glipitsidi; Glipizid; Glipizida; Glipizidas; Glipizidum; Glydiazinamide; K-4024
USAN: Glipizide
INN: Glipizide [pINN (en)]
INN: Glipizida [pINN (es)]
INN: Glipizide [pINN (fr)]
INN: Glipizidum [pINN (la)]
INN: Глипизид [pINN (ru)]
Chemical name: 1-Cyclohexyl-3-{4-[2-(5-methylpyrazine-2-carboxamido)ethyl]benzenesulphonyl}urea
Molecular formula: C21H27N5O4S =445.5
CAS: 29094-61-9
ATC code: A10BB07
Read code: y02Xb

Pharmacopoeias. In China, Europe, and US.

European Pharmacopoeia, 6th ed. (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.

The United States Pharmacopeia 31, 2008 (Glipizide). Store in airtight containers. Protect from light.

Adverse Effects, Treatment, and Precautions

As for sulfonylureas in general.

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

Interactions

As for sulfonylureas in general.

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. No such effect was seen with aluminium hydroxide

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 plasma-insulin concentrations and a lesser reduction in plasma-glucose concentrations. There is, however, some evidence that glycae-mic control and insulin sensitivity can be improved by the use of a modified-release rather than a conventional formulation of glipizide.

Preparations

British Pharmacopoeia 2008: Glipizide Tablets

The United States Pharmacopeia 31, 2008: Glipizide and Metformin Hydrochloride Tablets Glipizide Tablets.

Proprietary Preparations

Argentina: Minodiab

Australia: Melizide Minidiab

Austria: Glibenese Minidiab

Belgium: Glibenese Minidiab

Brazil: Minidiab

Chile: Minidiab Xiprine

Czech Republic: Antidiabf Glucotrol † Mediab Minidiab

Denmark: Glibenese Minidiab

Finland: Apamid † Glibenese Melizid Minidiab

France: Glibenese Minidiab Ozidia

Greece: Glibenese Minodiab

Hong Kong: Diase Glucotrol Minidiab Sunglucon

Hungary: Minidiab

India: Diaglip Glez Glide Glucolip Glynase Glyzip

Indonesia: Aldiab Glucotrol Glyzid

Ireland: Glibenese

Israel: Gluco-Rite

Italy: Minidiab

Malaysia: Dibizicle † Dipazide Glix Melizide Minidiab

Mexico: Glupitel Luditec Minodiab Pigloss Singloben

The Netherlands: Glibenesej

Norway: Apamid Minidiab

New Zealand: Glipid Minidiab

Philippines: Glix Minidiab

Poland: Antidiab Glibenese

Portugal: Minidiab

Russia: Glibenese Minidiab †

South Africa: Minidiab

Singapore Beapizide Diactin Diasef Melizide Minidiab

Spain: Glibenese Minodiab

Sweden: Apamid † Glipiscandl Minidiab

Switzerland: Glibenese

Thailand: Apamid † Depizide Diase Dipazide Gipzide Glipimed Glizide Glucodiab Glygen GP-Zide Melizide Minibit Minidiab Namedia Pezide

Turkey: Glucotrol Minidiab

UK: Glibenese Minodiab

USA: Glucotrol

Venezuela: Minidiab.

Multi-ingredient

India: Diaglip M Metaglez

USA: Metaglip.

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