Glipizide

Trade Names:
Glucotrol
- Tablets 5 mg
- Tablets 10 mg

Trade Names:
Glucotrol XL
- Tablets, extended release 5 mg
- Tablets, extended release 10 mg

Pharmacology

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Decreases blood glucose by stimulating insulin release from pancreas and by increasing tissue sensitivity to insulin.

Pharmacokinetics

Absorption

Bioavailability is 100% (immediate-release); 90% (extended-release). T _max is 1 to 3 h (immediate-release); 6 to 12 h (extended-release). Food delays absorption by about 40 min.

Distribution

The mean apparent Vd is about 10 L. Protein binding is 98% to 99%.

Metabolism

Hepatic.

Elimination

Mean t _½ is 2 to 5 h. Mean total Cl is about 3 L/h. About 80% is excreted in urine and 10% in feces as metabolites.

Onset

30 min.

Duration

24 h.

Indications and Usage

Adjunct to diet to lower blood glucose in patients with non-insulin-dependent diabetes mellitus (type 2) whose hyperglycemia cannot be controlled by diet alone.

Contraindications

Hypersensitivity to sulfonylureas; diabetes complicated by ketoacidosis, with or without coma; sole therapy of insulin-dependent (type 1) diabetes mellitus; diabetes when complicated by pregnancy.

Dosage and Administration

PO 5 mg/day 30 min before breakfast. Adjust dose in 2.5 to 5 mg/day increments based on blood glucose response. Divided doses may be given (single daily dose max, 15 mg; total daily dose max, 40 mg).

PO 2.5 mg/day initially.

Storage/Stability

Store in tightly closed container at room temperature.

Drug Interactions

Produces disulfiram-like reactions (eg, facial flushing, headache, breathlessness).

Hypoglycemic effects may be increased.

May decrease hypoglycemic effect.

Absorption is delayed when taken with food. Give drug about 30 min before meal.

Laboratory Test Interactions

Mild-to-moderate elevations in BUN and creatinine.

Adverse Reactions

Cardiovascular

May have increased risk of CV mortality when compared with patients treated with diet alone.

CNS

Dizziness; vertigo.

Dermatologic

Allergic skin reactions; eczema; pruritus; erythema; urticaria; morbilliform or maculopapular eruptions; lichenoid reactions; photosensitivity.

EENT

Tinnitus.

GI

GI disturbances (eg, nausea, epigastric fullness, heartburn); diarrhea.

Genitourinary

Mild diuresis; elevated BUN and creatinine.

Hepatic

Cholestatic jaundice; elevated LFT results.

Hematologic

Leukopenia; thrombocytopenia; aplastic anemia; agranulocytosis; hemolytic anemia; pancytopenia; hepatic porphyria.

Metabolic

Hypoglycemia.

Miscellaneous

Disulfiram-like reaction; weakness; paresthesia; fatigue; malaise.

Precautions

Pregnancy

Category C . Insulin is recommended to maintain blood glucose levels during pregnancy. Prolonged severe neonatal hypoglycemia can occur if sulfonylureas are administered at time of delivery.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Elderly and debilitated patients are particularly susceptible to hypoglycemic action. Hypoglycemia may be difficult to recognize in elderly.

Renal Function

Use drug with caution and monitor renal function frequently.

Hepatic Function

Use drug with caution and monitor liver function frequently.

Overdosage

Symptoms

Prolonged hypoglycemia, tingling of lips and tongue, hunger, nausea, lethargy, yawning, confusion, agitation, nervousness, tachycardia, sweating, tremor, convulsions, stupor, coma.

Patient Information

• Remind patient to take medication on empty stomach 30 min before meals.
• Teach patient to self-monitor blood glucose.
• Emphasize importance of following diabetic diet.
• Inform patient that this drug is not substitute for exercise and diet control and that patient should follow prescribed regimens.
• Instruct patient to inform health care provider that they are taking this drug.
• Advise patient to carry identification stating that patient is diabetic.
• Inform patient to contact health care provider if symptoms of hypoglycemia occur (eg, fatigue, excessive hunger, profuse sweating, numbness of extremities).
• Tell patient to notify health care provider if symptoms of hyperglycemia occur (eg, excessive thirst or urination, urinary glucose or ketones).
• Instruct patient to report these symptoms to health care provider: nausea, vomiting, diarrhea, heartburn, sore throat, rash, unusual bruising or bleeding or other physical complaints.
• Advise patient not to take any medication (including OTC) or alcohol without consulting health care provider.

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