Endocrine System-Oral Antidiabetic Drugs-Sulfonylureas

Name of the Sulfonylureas Drugs

• Tolbutamide
• Glibenclamide
• Glipizide
• Glimepiride

1.Tolbutamide

Mechanism of Action

Stimulates insulin release from beta cells in the pancreas. Tolbutamide also increases peripheral tissue sensitivity to insulin either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors

Contraindications

Diabetes complicated by pregnancy; diabetic coma; diabetic ketoacidosis; hypersensitivity to tolbutamide, sulfonylureas, or their components; sole therapy for type 1 diabetes mellitus

Adverse Reactions

• CNS: Dizziness, fatigue, headache, malaise, paresthesia, vertigo
• ENDO: Hypoglycemia
• GI: Anorexia, cholestasis, heartburn, nausea, vomiting
• HEME: Agranulocytosis, aplastic anemia, hemolysis, hemolytic anemia, leukopenia, thrombocytopenia
• MS: Muscle weakness
• SKIN: Erythema, photosensitivity, pruritus, rash, urticaria

Nursing Considerations

•  If patient takes 20 units or less of insulin daily, expect a possible transfer from insulin to tolbutamide. If patient takes more than 20 units of insulin daily, expect to reduce insulin dosage as tolbutamide therapy starts.
• Anticipate that patient receiving tolbutamide may need temporary insulin treatment during periods of physiologic stress, such as fever, surgery, systemic infection, or trauma.
• Assess elderly patients for signs of hypoglycemia because they’re more susceptible to drug’s hypoglycemic effect. Anticipate that hypoglycemia may be more difficult to detect.
• Assess patient with thyroid disease for altered blood glucose control because thyroid hormone increases GI absorption of glucose.
• Expect prescriber to stop tolbutamide 2 weeks before pregnant patient delivers her neonate to minimize the risk of prolonged hypoglycemia in neonate.

Patient Teaching

• Advise patient to avoid alcohol while taking tolbutamide.
• Teach patient and family members how to monitor blood glucose level and recognize signs of hypoglycemia and hyperglycemia.
• Instruct patient to treat mild hypoglycemia with fruit juice or other simple sugars.

2.Glibenclamide

Mechanism of Action

Stimulates insulin release from beta cells in the pancreas. Glyburide also increases peripheral tissue sensitivity to insulin either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors.

Pharmacokinetics

• Bioavailability: Variable, depending on oral dosage form
• Protein bound: 99%
• Metabolized extensively in the liver to less-active metabolites
• Half-life: 10 hr (DiaBeta); 4 hr (Glynase, PresTab)
• Excretion: Urine (50%), feces (50%)

Administration

• Know that micronized glyburide is not bioequivalent to regular glyburide
• Check baseline creatinine level for normal renal function before giving first dose.
• Give daily dose at breakfast; for patient receiving drug b.i.d., give second dose at dinner.
• Adjust dosage slowly if patient is taking metformin.

Contraindications

• Hypersensitivity to drug
• Type 1 (insulin-dependent) diabetes
• Severe renal, hepatic, thyroid or other endocrine disease
• Pregnancy or breastfeeding

Precautions:

• Mild to moderate hepatic, renal, or cardiovascular disease; impaired thyroid, pituitary, or adrenal function
• Infection, stress, or dietary changes
• Elderly patients.

Adverse reactions

• CNS: dizziness, drowsiness, headache, weakness
• CV: increased CV mortality risk EENT: visual accommodation changes, blurred vision
• GI: nausea, vomiting, diarrhea, constipation, cramps, heartburn, epigastric distress, anorexia
• Hematologic: aplastic anemia, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia
• Hepatic: cholestatic jaundice, hepatitis
• Metabolic: hyponatremia, hypoglycemia
• Skin: rash, pruritus, urticaria, eczema, erythema, photosensitivity, angioedema
• Other: increased appetite

Patient monitoring

•  Monitor blood glucose level, especially during periods of increased stress.
•  Monitor CBC and renal function test results.
• If patient is ill or has abnormal laboratory findings, monitor electrolyte, ketone, glucose, pH, lactate dehydrogenase, and pyruvate levels.
• Evaluate cardiovascular status.

Patient teaching

• Advise patient to take daily dose with breakfast (and second dose, if prescribed, with dinner).
• Teach patient how to self-monitor his glucose level as prescribed; tell him to report significant changes.
• Inform patient that he may need supplemental insulin during times of stress or when he can’t maintain adequate oral intake.
• Teach patient how to recognize signs and symptoms of hypoglycemia and hyperglycemia.
• Instruct patient to keep sugar source available at all times.
• Encourage patient to drink plenty of fluids.
• Stress importance of diet and exercise in helping to control diabetes.
• Advise patient to wear or carry medical identification stating he has diabetes.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient he’ll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

Nursing Considerations

• Use cautiously in patients with glucose 6- phosphate dehydrogenase deficiency because hemolytic anemia may develop. Monitor patient’s CBC closely.
• Give glyburide as single dose before first meal of the day. If patient takes more than 10 mg daily or if severe GI distress occurs, give in 2 divided doses before meals.
• Monitor fasting blood glucose level to determine patient’s response to glyburide. Expect to check glycosylated hemoglobin every 3 to 6 months or as ordered to evaluate long-term blood glucose control.
• When patient switches from insulin to glyburide, check blood glucose level three times daily before meals.
• Be aware that micronized tablets aren’t equal to nonmicronized tablets; they contain smaller particles, which affects drug bioavailability
• Monitor patient with history of allergies to other sulfonamide derivatives closely because he may be allergic to glyburide. If allergic reactions persist or worsen (dyspnea, drop in blood pressure, or shock), expect drug to be discontinued.
• Administer insulin as needed and prescribed during periods of increased stress, such as infection, surgery, and trauma.
• Arrange for diabetic teaching and consultation between patient and dietitian, if appropriate.

3.Glipizide

Mechanism of Action

Stimulates insulin release from beta cells in pancreas. Glipizide also increases peripheral tissue sensitivity to insulin, either by increasing insulin binding to cellular receptors or by increasing number of insulin receptors.

Pharmacokinetics

• Bioavailability: 100% (Glucotrol)
• Protein bound: 99% (Glucotrol)
• Extensively metabolized in liver to inactive metabolites
• Half-life: 2-5 hr (Glucotrol)
• Excretion: Urine (63-90%); feces: (10%)

Administration

• Check baseline creatinine level for normal renal function before giving first dose.
• Give daily dose (extended-release) at breakfast.
• Administer immediate-release tablets 30 minutes before a meal (preferably breakfast). If patient takes two daily doses, give second dose before dinner.

Contraindications

• Hypersensitivity to drug
• Severe renal, hepatic, thyroid, or other endocrine disease
• Uncontrolled infection, serious burns, or trauma
• Diabetic ketoacidosis
• Pregnancy or breastfeeding

Precautions:

• Mild to moderate hepatic, renal, or cardiovascular disease; impaired thyroid, pituitary, or adrenal function
• Elderly patients.

Adverse reactions

• CNS: dizziness, drowsiness, headache, weakness
• CV: increased CV mortality risk
• EENT: blurred vision
• GI: nausea, vomiting, diarrhea, constipation, cramps, heartburn, epigastric distress, anorexia
• Hematologic: aplastic anemia, agranulocytosis, leukopenia, pancytopenia, thrombocytopenia
• Hepatic: cholestatic jaundice, hepatitis
• Metabolic: hyponatremia, hypoglycemia
• Skin: rash, pruritus, erythema, urticaria, eczema, angioedema, photosensitivity
• Other: increased appetite

Patient monitoring

• Monitor blood glucose level, especially during periods of increased stress.
• Evaluate CBC and renal function tests.
• If patient is ill or has abnormal laboratory values, monitor electrolyte, ketone, glucose, pH, lactate dehydrogenase, and pyruvate levels.
• Monitor cardiovascular status.

Patient teaching

• Advise patient to take daily dose of extended-release tablets with breakfast or immediate-release tablet 30 minutes before breakfast (and second dose, if prescribed, before dinner).
• Advise patient to monitor blood glucose level as instructed by prescriber.
• Tell patient he may need supplemental insulin during times of stress or when he can’t maintain adequate oral intake
• Teach patient how to recognize signs and symptoms of hypoglycemia and hyperglycemia.
• Stress importance of diet and exercise to help control diabetes.
• Instruct patient to wear or carry medical identification describing his condition.
• Advise patient to keep sugar source at hand at all times in case of hypoglycemia.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient he’ll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

Nursing Considerations

• Use cautiously in patients with glucose 6- phosphate dehydrogenase deficiency because hemolytic anemia may develop. Monitor patient’s CBC closely.
• To improve blood glucose control, give drug in divided doses instead of once daily.
• Check blood glucose level at least three times daily for a patient switching from insulin to glipizide. Patients who take more than 40 units of insulin daily may need hospitalization during transition.• If patient gradually loses responsiveness to glipizide, expect to give a second antidiabetic to maintain blood glucose control
• Monitor fasting blood glucose level to determine response to drug. Expect to check glycosylated hemoglobin every 3 to 6 months or as ordered to evaluate longterm blood glucose control.
• Expect to switch patient to insulin therapy, as prescribed, during physical stress, such as infection, surgery, or trauma.

4.Glimepiride

Mechanism of Action

Stimulates insulin release from beta cells in pancreas. Glimepiride also increases peripheral tissue sensitivity to insulin, either by enhancing insulin binding to cellular receptors or by increasing the number of insulin receptors.

Pharmacokinetics

• Bioavailability: 100%
• Protein bound: 99.5%
• Metabolized extensively by hepatic P450 enzyme CYP2C9 to less-active metabolites
• Half-life: 5-9 hr
• Total body clearance: 47.8 mL/min
• Excretion: Urine (60%); feces (40%)

Administration

• Check baseline creatinine level for normal renal function before giving first dose.
• Give with first meal of day

Contraindications

• Hypersensitivity to drug
• Diabetic coma or ketoacidosis
• Severe renal, hepatic, or endocrine disease
• Pregnancy or breastfeeding

Precautions:

• Mild to moderate hepatic or renal disease; cardiovascular disease; impaired thyroid, pituitary, or adrenal function
• Elderly patients.

Adverse reactions

• CNS: dizziness, drowsiness, headache, weakness
• CV: increased CV mortality risk
• EENT: blurred vision
• GI: nausea, vomiting, diarrhea, constipation, cramps, heartburn, epigastric distress, anorexia
• Hematologic: aplastic anemia, leukopenia, pancytopenia, thrombocytopenia, agranulocytosis
• Hepatic: cholestatic jaundice, hepatitis
• Metabolic: hyponatremia, hypoglycemia
• Skin: rash, erythema, maculopapular eruptions, urticaria, eczema, angioedema, photosensitivity
• Other: increased appetite

Patient monitoring

•  Monitor CBC with white cell differential, electrolyte levels, and blood chemistry results.
• Monitor blood glucose level regularly. Assess glycosylated hemoglobin level every 3 to 6 months.
• Evaluate kidney and liver function test results frequently, especially in patients with impairments.
• Assess neurologic status. Report cognitive or sensory impairment.

Patient teaching

• Instruct patient to self-monitor his blood glucose level as prescribed.
• Teach patient how to recognize signs and symptoms of hypoglycemia and hyperglycemia.
• Stress importance of diet and exercise to help control diabetes.
• Instruct patient to wear or carry medical identification describing his condition.
• Advise patient to keep sugar source readily available at all times in case of hypoglycemia.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient he will undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

Nursing Considerations

• Monitor fasting blood glucose level to determine response to glimepiride. Expect to check glycosylated hemoglobin level every 3 to 6 months to evaluate long-term blood glucose control.
• Arrange for dietary consultation and diabetic teaching, if appropriate. Ask dietitian to discuss amount of alcohol patient can consume without risking hypoglycemia.
• Expect to switch patient to insulin therapy, as prescribed, during physical stress, such as infection, surgery, and trauma
• Monitor patient with a history of allergies to other sulfonamide derivatives closely because he may be allergic to glimepiride. If allergic reactions persist or worsen (dyspnea, drop in blood pressure, or shock), expect drug to be discontinued.

REFERENCES

1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
5. Nursebro.com, Search – Nursebro

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