Glucotrol, Glucotrol XL
Classifications: hormone; antidiabetic agent; sulfonylurea; Therapeutic: antidiabetic; sulfonylurea
Pregnancy Category: C
5 mg, 10 mg tablets; 5 mg, 10 mg sustained release tablets
Second-generation sulfonylurea hypoglycemic agent. Potency is enhanced by as much as 200-fold over first-generation agents.
Directly stimulates functioning pancreatic beta cells to secrete insulin, leading to an acute drop in blood glucose. Indirect
action leads to altered numbers and sensitivity of peripheral insulin receptors, resulting in increased insulin binding. It
also causes inhibition of hepatic glucose production and reduction in serum glucagon levels.
It lowers blood glucose level by stimulating pancreatic beta cells.
Adjunct to diet for control of hyperglycemia in patient with type 2 diabetes mellitus after dietary control alone has failed;
also used to treat transient loss of control in patient usually controlled well on diet.
Hypersensitivity to sulfonylureas; diabetic ketoacidosis; pregnancy (category C), lactation. Safe use in children is not established.
Impaired renal and hepatic function; thyroid disease; older adults; debilitated, malnourished patients; patients with adrenal
or pituitary insufficiency.
Route & Dosage
|Control of Hyperglycemia
Adult: PO 2.55 mg/d 30 min before breakfast, may increase by 2.55 mg q12wk; >15 mg/d in divided doses 30 min before
morning and evening meal (max: 40 mg/d); 510 mg sustained release tablets once/d
- Give once-daily dosing 30 min before the first meal of the day.
- Ensure that sustained release form of drug is not chewed or crushed. It must be swallowed whole.
- Store in tightly closed, light-resistant container at 15°30° C (59°86° F).
Adverse Effects (≥1%)GI:
, gastralgia, cholestatic jaundice
(rare). Metabolic: Hepatic
. Skin: Erythema
, morbilliform or maculopapular rash, pruritus, urticaria, eczema
(transient). Body as a Whole:
Hypersensitivity (fatigue, drowsiness, hunger, GI distress with heartburn, abdominal pain, anorexia). CNS:
Transient drowsiness, headache, anxiety, ataxia, confusion; seizures, coma
Tachycardia. Special Senses:
-like reaction in some patients; oral anticoagulants, chloramphenicol, clofibrate, phenylbutazone, mao inhibitors
, probenecid, sulfonamides
may potentiate hypoglycemic actions; thiazides
may antagonize hypoglycemic effects; cimetidine
may increase glipizide levels, causing hypoglycemia
. Herbal: Ginseng, garlic
may increase hypoglycemic effects.
Readily from GI tract. Onset:
1530 min. Peak:
12 h. Duration:
Up to 24 h. Metabolism:
Metabolized extensively in liver. Elimination:
Mainly in urine with some excretion via bile in feces. Half-Life:
Assessment & Drug Effects
- Observe response to the initial dose and establish maintenance regimen cautiously in older adult or debilitated patients;
early signs of hypoglycemia are easily overlooked.
- Lab tests: monitor periodically during long-term therapy: Liver function tests, serum electrolytes, and serum osmolarity.
- Note: Severe drug-induced skin rashes and pruritus may necessitate discontinuation of drug use. Symptoms usually subside rapidly
when drug is withdrawn.
- Check urine for sugar and ketone bodies at least 3 times daily during insulin withdrawal and transfer to glipizide. Contact
physician if tests are abnormal.
- Note: Patients transferred from a sulfonylurea with a long half-life (e.g., chlorpropamide, half-life: 3040 h) must be observed
for hypoglycemic responses (see Appendix F) for 12 wk because of potential overlapping of drug effect.
- Note: The first signs of hypoglycemia may be hard to detect in patients receiving concurrent beta blockers or older adults.
Patient & Family Education
- Overdose treatment: Treat mild hypoglycemia (reaction without loss of consciousness or neurologic symptoms) with PO glucose
and adjustment of dosage and meal pattern; monitor closely for at least 57 d to assure reestablishment of safe control.
Severe hypoglycemia requires emergency hospitalization to permit treatment to maintain a blood glucose level above 100 mg/dL.
- Note: Glipizide therapy accompanies (does NOT substitute for) continued control of diet and (if patient is obese) a weight-loss program.
- Test fasting and postprandial blood glucose frequently.
- Exercise is an important part of the total control program.
- When a drug that affects the hypoglycemic action of sulfonylureas (see DRUG INTERACTIONS) is withdrawn or added to the glipizide regimen, be alert to the added danger of loss of control. Urine and blood glucose
tests and test for ketone bodies should be carefully monitored.