Glipizide

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Glipizide
Systematic (IUPAC) name
N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]- 5-methyl-pyrazine-2-carboxamide
Identifiers
CAS number	29094-61-9
ATC code	A10BB07
PubChem	3478
DrugBank	APRD00436
Chemical data
Formula	C₂₁H₂₇N₅O₄S
Mol. mass	445.536 g/mol
Pharmacokinetic data
Bioavailability	100% (regular formulation) 90% (extended release)
Protein binding	98 to 99%
Metabolism	Hepatic hydroxylation
Half life	2 to 5 hours
Excretion	Renal and fecal
Therapeutic considerations
Pregnancy cat.	C (Au, U.S.)
Legal status	POM (UK), ℞-only (U.S.)
Routes	Oral

Glipizide is an oral medium-to-long acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. The structure on the R2 group is a much larger cyclo or aromatic group compared to the 1st generation sulfonylureas. This leads to a once a day dosing that is much less than the first generation, about 100 fold.

Mechanism of action is produced by blocking potassium channels in the Beta cells of the Islets of Langerhans. By partially blocking the potassium channels, you will increase the time the cell spends in the Calcium release stage of cell signaling leading to an increase in calcium. The increase in Calcium will initiate more Insulin release from each Beta cell.

Originally available in 1984, it is marketed by Pfizer under the brand name Glucotrol in the USA, where Pfizer sells Glucotrol in doses of 5 and 10 milligrams and Glucotrol XL (an extended release form of glipizide) in doses of 2.5, 5, and 10 milligrams. Other companies sell generic forms of glipizide, most commonly extended release tablets of 5 and 10 milligrams.

[edit] External links

Glucotrol XL Full U.S. Prescribing Information. Accessed on July 26, 2005.

v • d • e Oral antidiabetic drugs and Insulin analogs (A10)

Biguanides	Metformin

Sulfonylureas	Carbutamide, Chlorpropamide, Glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide

Alpha-glucosidase inhibitors	Acarbose, Miglitol, Voglibose

Thiazolidinediones (TZD)	Pioglitazone, Rivoglitazone^†, Rosiglitazone, Troglitazone^‡

Meglitinides	Nateglinide, Repaglinide, Mitiglinide

Dipeptidyl peptidase-4 (DPP-4) inhibitors	Alogliptin^†, Saxagliptin^†, Sitagliptin, Vildagliptin

Glucagon-like peptide-1 analog	Exenatide, Liraglutide^†, Albiglutide^†

Amylin analog	Pramlintide

Insulin analogs	fast acting (Insulin lispro, Insulin aspart, Insulin glulisine), long acting (Insulin glargine, Insulin detemir), Inhalable insulin (Exubera)

Dual PPAR agonists	Aleglitazar^†, Muraglitazar^§, Tesaglitazar^§

SGLT2 inhibitor	Dapagliflozin^†, Remogliflozin^†, Sergliflozin^†

^†Undergoing clinical trials. ^‡ Withdrawn from market. ^§Development halted.