GLIPIZIDE

GLIPIZIDE
(glip'i-zide)
Glucotrol, Glucotrol XL
Classifications: hormone; antidiabetic agent; sulfonylurea;
Therapeutic: antidiabetic
; sulfonylurea
Prototype: Glyburide
Pregnancy Category: C

Availability

5 mg, 10 mg tablets; 5 mg, 10 mg sustained release tablets

Action

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.

Therapeutic Effect

It lowers blood glucose level by stimulating pancreatic beta cells.

Uses

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.

Contraindications

Hypersensitivity to sulfonylureas; diabetic ketoacidosis; pregnancy (category C), lactation. Safe use in children is not established.

Cautious Use

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 2.5–5 mg/d 30 min before breakfast, may increase by 2.5–5 mg q1–2wk; >15 mg/d in divided doses 30 min before morning and evening meal (max: 40 mg/d); 5–10 mg sustained release tablets once/d

Administration

Oral
  • 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: Nausea, diarrhea, constipation, gastralgia, cholestatic jaundice (rare). Metabolic: Hepatic porphyria, hypoglycemia. 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. CV: Tachycardia. Special Senses: Visual disturbances.

Interactions

Drug: Alcohol produces disulfiram-like reaction in some patients; oral anticoagulants, chloramphenicol, clofibrate, phenylbutazone, mao inhibitors, salicylates, 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.

Pharmacokinetics

Absorption: Readily from GI tract. Onset: 15–30 min. Peak: 1–2 h. Duration: Up to 24 h. Metabolism: Metabolized extensively in liver. Elimination: Mainly in urine with some excretion via bile in feces. Half-Life: 3–5 h.

Nursing Implications

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: 30–40 h) must be observed for hypoglycemic responses (see Appendix F) for 1–2 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 5–7 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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