GLIP-i-zide

Therapeutic Classification: antidiabetics

Pharmacologic Classification: sulfonylureas

• PO: Type 2 diabetes mellitus (as adjunct to diet and exercise).

• Lowers blood sugar by stimulating the release of insulin from the pancreas and increasing the sensitivity to insulin at receptor sites.
• May also decrease hepatic glucose production.

• Lowering of blood sugar in diabetic patients.

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 99%.

Metabolism/Excretion: Mostly metabolized by the liver.

Half-life: 2.1–2.6 hr.

(hypoglycemic activity)

Contraindicated in:

• Hypersensitivity
• Hypersensitivity to sulfonamides (cross-sensitivity may occur)
• Insulin-dependent diabetics
• Diabetic coma or ketoacidosis.

Use Cautiously in:

• Severe cardiovascular or hepatic disease
• Glucose 6-phosphate dehydrogenase deficiency (↑ risk of hemolytic anemia)
• Severe renal impairment (↑ risk of hypoglycemia)
• Infection, stress, or changes in diet may alter requirements for control of blood sugar
• Impaired thyroid, pituitary, or adrenal function
• Malnutrition, high fever, prolonged nausea, or vomiting
• OB: Crosses the placenta and ↑ risk of neonatal hypoglycemia; should be discontinued 2 wk before delivery; insulin recommended during pregnancy
• Lactation: May ↑ risk of hypoglycemia in infant; use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Geri: Appears on Beers list. ↑ risk of prolonged hypoglycemia in older adults. Avoid use as first- or second-line monotherapy or as add-on treatment in older adults unless there are significant barriers to the use of safer and more effective agents. If a sulfonylurea must be used, this is the preferred agent.

Derm: photosensitivity, rash.

Endo: hypoglycemia.

F and E: hyponatremia.

GI: constipation, cramps, diarrhea, dyspepsia, hepatitis, nausea, vomiting.

Hemat: agranulocytosis, APLASTIC ANEMIA, hemolytic anemia, leukopenia, pancytopenia, thrombocytopenia.

Metab: ↑appetite.

Neuro: dizziness, drowsiness, headache, weakness.

Drug-Drug:

• Ingestion of alcohol may result in disulfiram-like reaction.
• Effectiveness may be ↓ by concurrent use of diuretics, corticosteroids, atypical antipsychotics, danazol, phenothiazines, oral contraceptives, estrogens, progestins, glucagon, protease inhibitors, somatropin, thyroid preparations, phenytoin, niacin, sympathomimetics, calcium channel blockers and isoniazid.
• Alcohol, ACE inhibitors, angiotensin II receptor blockers, chloramphenicol, fibric acid derivatives, fluoxetine, disopyramide, fluoroquinolones, MAO inhibitors, NSAIDs (except diclofenac), pentoxifylline, probenecid, salicylates, voriconazole, H₂ receptor antagonists, sulfonamides, and warfarin may ↑ risk of hypoglycemia.
• Concurrent use with warfarin may alter the response to both agents (↑ effects of both initially, then ↓ activity); close monitoring recommended during any changes in dose.
• Beta-adrenergic blockers may mask the signs and symptoms of hypoglycemia.
• May ↑cyclosporine levels.
• Colesevelam may ↓ effects; administer glipizide 4 hr before colesevelam

• PO (Adults): 5 mg/day initially, ↑ as needed (range 2.5–40 mg/day); extended-release dose form is given once daily. Doses >15 mg/day may be given as 2 divided doses of regular-release product (not extended-release).
• PO (Geriatric Patients): 2.5 mg/day initially.

(Generic available)

• Immediate-release tablets: 5 mg; 10 mg;
• Extended-release tablets: 2.5 mg; 5 mg; 10 mg;
• In combination with: metformin.

• Observe for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety). Patients on concurrent beta-blocker therapy may have very subtle signs and symptoms of hypoglycemia.
• Assess patient for allergy to sulfonamides.

• Monitor serum glucose and glycosylated hemoglobin (A_1C) periodically during therapy to evaluate effectiveness of treatment.
  • Monitor CBC periodically during therapy. Report ↓ in blood counts promptly.
  • May cause an ↑ in AST, LDH, BUN, and serum creatinine.

• Overdose is manifested by symptoms of hypoglycemia. Mild hypoglycemia may be treated with administration of oral glucose. Treat severe hypoglycemia with IV D50W followed by continuous IV infusion of more dilute dextrose solution at a rate sufficient to keep serum glucose at approximately 100 mg/dL.

• High Alert:Accidental administration of oral hypoglycemic agents to non-diabetic adults and children has resulted in serious harm or death. Before administering, confirm that patient has Type 2 diabetes.
• High Alert:Do not confuse glipizide with glyburide.
• Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
  • To convert from other oral hypoglycemic agents, gradual conversion is not required. For insulin dose of less than 20 units/day, change to glipizide can be made without gradual dose adjustment. Patients taking 20 or more units/day should convert gradually by receiving glipizide and a 25–30% reduction in insulin dose every day or every 2nd day with gradual insulin dose reduction as tolerated. Monitor serum or glucose and ketones at least 3 times/day during conversion.
• PO: Administer 30 min before a meal. DNC: Swallow extended-release tablets whole; do not crush, break or chew.

• Instruct patient to take medication at same time each day. Take missed doses as soon as remembered unless almost time for next dose. Do not take if unable to eat.
• Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
• Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to drink a glass of orange juice or ingest 2–3 tsp of sugar, honey, or corn syrup dissolved in water or an appropriate number of glucose tablets and notify health care professional.
• Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
• Concurrent use of alcohol may cause a disulfiram-like reaction (abdominal cramps, nausea, flushing, headaches, and hypoglycemia).
• Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
• May occasionally cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
• Caution patient to avoid other medications, especially aspirin and alcohol, while on this therapy without consulting health care professional.
• Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
• Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
• Advise patient to notify health care professional promptly if unusual weight gain, swelling of ankles, drowsiness, shortness of breath, muscle cramps, weakness, sore throat, rash, or unusual bleeding or bruising occurs.
• Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
• May cause fetal harm. Insulin is the recommended method of controlling blood sugar during pregnancy. Counsel female patients to use a form of contraception other than oral contraceptives and to notify health care professional promptly if pregnancy is planned or suspected or if breastfeeding. Discontinue glipizide at least 2 wk before expected delivery. Neonates of women with gestational diabetes who are treated with sulfonylureas during pregnancy may be at increased risk for respiratory distress and hypoglycemia (jitters, cyanosis, apnea, hypothermia, excessive sleepiness, poor feeding, seizures).
• Emphasize the importance of routine follow-up exams.

• Control of blood glucose levels without the appearance of hypoglycemic or hyperglycemic episodes.

Glucotrol, Glucotrol XL