Glucotrol - General Information
An oral hypoglycemic agent which is rapidly absorbed and completely metabolized. [PubChem]
Pharmacology of Glucotrol
Glucotrol, a second-generation sulfonylurea, is used with diet to lower blood glucose in patients with diabetes mellitus type II. The primary mode of action of glipizide in experimental animals appears to be the stimulation of insulin secretion from the beta cells of pancreatic islet tissue and is thus dependent on functioning beta cells in the pancreatic islets. In humans glipizide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. In man, stimulation of insulin secretion by glipizide in response to a meal is undoubtedly of major importance. Fasting insulin levels are not elevated even on long-term glipizide administration, but the postprandial insulin response continues to be enhanced after at least 6 months of treatment. Some patients fail to respond initially, or gradually lose their responsiveness to sulfonylurea drugs, including glipizide.
Glucotrol for patients
Glipizide is a sulfonylurea used in patients with diabetes mellitus to lower blood sugar. Notify your physician if you are pregnant or nursing. Do not change the dose or stop taking glipizide without talking with your physician. Immediate-release glipizide tablets should be taken on an empty stomach, 30 minutes before a meal. Extended-release glipizide tablets may be taken with food. Do not break, crush, or chew extended-release glipizide tablets. Patients taking extended release glipizide tablets may notice something that looks like a tablet in their stool. This is the leftover tablet after the medicine has been absorbed and is normal. Avoid drinking alcohol while taking this medication. Alcohol may cause flushing, weakness, dizziness, a tingling sensation and headache. Avoid taking aspirin with this medication. Notify your physician if you develop unexplained fever, sore throat, yellowing of the skin or eyes, dark urine, or skin rash. Notify your physician if you develop fatigue, nausea, confusion, agitation, excessive hunger, profuse sweating, numbness or tingling of lips, tongue or extremities (may indicate low blood sugar), or if you develop excessive thirst or urination, or glucose or ketones in the urine or blood (may indicate high blood sugar).
Immediate and Extended Release Tablets
The hypoglycemic action of sulfonylureas may be potentiated by certain drugs including nonsteroidal anti-inflammatory agents, some azoles and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, and beta adrenergic blocking agents. When such drugs are administered to a patient receiving glipizide, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving glipizide, the patient should be observed closely for loss of control. In vitro binding studies with human serum proteins indicate that glipizide binds differently than tolbutamide and does not interact with salicylate or dicumarol. However, caution must be exercised in extrapolating these findings to the clinical situation and in the use of glipizide with these drugs.
Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving glipizide, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving glipizide, the patient should be observed closely for hypoglycemia.
A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical, or vaginal preparations of miconazole is not known. The effect of concomitant administration of fluconazole and glipizide has been demonstrated in a placebo-controlled crossover study in normal volunteers. All subjects received glipizide alone and following treatment with 100 mg of fluconazole as a single daily oral dose for seven days. The mean percentage increase in the glipizide AUC after fluconazole administration was 56.9% (range: 35 to 81).
Immediate and Extended Release Tablets
Glipizide is contraindicated in patients with:
1. Known hypersensitivity to the drug.
2. Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.
Additional information about Glucotrol
Glucotrol Indication: For use as an adjunct to diet for the control of hyperglycemia and its associated symptomatology in patients with non-insulin-dependent diabetes mellitus (NIDDM; type II), formerly known as maturity-onset diabetes, after an adequate trial of dietary therapy has proved unsatisfactory.
Mechanism Of Action: Sulfonylureas likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.
Drug Interactions: Not Available
Food Interactions: Avoid alcohol.
Avoid sugar and sugary food.
Take 30-60 minutes before breakfast.
Generic Name: Glipizide
Synonyms: Glipizida [Inn-Spanish]; Glipizidum [Inn-Latin]; Glydiazinamide
Drug Category: Hypoglycemic Agents
Drug Type: Small Molecule; Approved
Absorption: Gastrointestinal absorption is uniform, rapid, and essentially complete.
Toxicity (Overdose): The acute oral toxicity was extremely low in all species tested (LD50 greater than 4 g/kg). Overdosage of sulfonylureas including glipizide can produce hypoglycemia.
Protein Binding: 98-99%, primarily to albumin.
Biotransformation: Hepatic. The major metabolites of glipizide are products of aromatic hydroxylation and have no hypoglycemic activity. A minor metabolite which accounts for less than 2% of a dose, an acetylaminoethyl benzine derivatives, is reported to have 1/10 to 1/3 as much hypoglycemic activity as the parent compound.
Half Life: 2-5 hours
Dosage Forms of Glucotrol: Tablet, extended release Oral
Chemical IUPAC Name: N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-5-methylpyrazine-2-carboxamide
Chemical Formula: C21H27N5O4S
Glipizide on Wikipedia: https://en.wikipedia.org/wiki/Glipizide
Organisms Affected: Humans and other mammals