Side effects Most patients tolerate sulfonylureas well. However, the two most common side effects of taking sulfonylurea are hypoglycemia and weight gain. All sulfonylureas may cause hypoglycemia, which is usually related to a missed a meal or an excessive dose. Longer-acting sulfonylureas, like glyburide (DiaBeta; Micronase), can cause more hypoglycemia (Kroon & Zhou, 2022a; Sola et al., 2015) than can shorter-acting sulfonylureas, like glipizide (Glucotrol and Glucotrol XL). It is important to recognize specific patient populations that are at risk for hypoglycemia such as patients who are malnourished, debilitated, elderly or those who have an alcohol use disorder or impaired renal, liver, or cardiac function. With sulfonylureas being metabolized in the liver and cleared by the kidneys, sulfonylureas should be used cautiously in patients with impaired Dosing of sulfonylureas The recommended dose for second-generation sulfonylureas is shown in Table 2. Patients who are lean, have CKD, or are frail and older need to start sulfonylureas at the lower end of the dose range and advance slowly. Conversely, younger, more insulin-resistant patients with severe hyperglycemia start on higher doses (White, 2022). Second-generation sulfonylureas tend to be more potent and are administered twice daily in lower
hepatic function or renal insufficiency. Healthcare providers should also be aware that some patients with a sulfa allergy will exhibit hypersensitivity to this class of drugs. Weight gain associated with sulfonylureas may be attributed to two factors: Improved glucose variability and hypoglycemia (Kroon & Zhou, 2022a). As the pancreas begins to release insulin, hypoglycemia begins to develop. This leads to hunger, overeating, and potentially hypoglycemia. Such a sequence of events drives patients to consume additional calories when treating hypoglycemia and subsequently gain weight. Other infrequent side effects that may occur when taking sulfonylureas include nausea, as well as skin reactions such as pruritus, erythema, rash, or exfoliative dermatitis. doses (White, 2022). An example of a low-dose sulfonylurea initiation may consist of glipizide (Glucotrol) 5 mg taken before breakfast, or glimepiride (Amaryl) 1 to 2 mg taken with breakfast. Glucose-lowering effects of sulfonylureas with dose changes are seen quickly, and the titration is performed every week if adequate glycemic management is not attained based on blood glucose monitoring.
Table 2: Noninsulin Antihyperglycemic Agents: Second-Generation Sulfonylureas Sulfonylurea
Available Strengths
Starting Dose
How to Titrate Dose
Dosage Range
Generic Name (Trade Name)
Glimepiride (Amaryl)
• 1 mg • 2 mg • 4 mg
• 1–2 mg/daily.
• 2 mg every 1–2 weeks.
• 1–8 mg/daily (usual maintenance dose is 4 mg/ daily). • IR: 10–40 mg once daily; if >15 mg, take twice daily. • ER: 2.5–20 mg/daily.
Glipizide (Glucotrol and Glucotrol XL)
• IR:
• IR: 5 mg/daily. • ER: 2.5–10 mg/daily.
• IR: 2.5–5 mg every several days. • ER: 2.5 mg every week.
○ 5 mg ○ 10 mg ○ 2.5 mg ○ 5 mg ○ 10 mg
• ER:
Glyburide (Diabeta; Micronase)
• 1.25 mg • 2.5 mg • 5 mg Micronized: ○ 1.5 mg
• 2.5–5 mg/daily. • Micronized: 1.5–3 mg/daily.
• 2.5 mg/1–2 weeks. • Micronized: 1.5 /1–2 weeks.
• 1.25–20 mg/daily or twice daily. • Micronized: 1.5–12 mg/daily (if >6 mg, take twice daily).
○ 3 mg ○ 6 mg
Key points for patients taking a sulfonylurea: ● Take sulfonylureas with food. ● Do not chew extended-release tablets. ● Do not miss your mid-day meal when taking sulfonylurea in the morning, as it will increase the risk of hypoglycemia. ● Sulfonylureas’ may cause hypoglycemia; if prescribed a sulfonylurea, all patients and their families should know the signs and symptoms of hypoglycemia and what to do should it occur. Thiazolidinediones are sometimes referred to as glitazones. This noninsulin antihyperglycemic improves glycemic control by increasing insulin sensitivity by reducing insulin resistance at target cell sites (e.g., skeletal muscle, adipose tissue) with beta-cell preservation properties. The first thiazolidinedione approved by the U.S. Food and Drug Administration (FDA) for use in the U.S. was troglitazone (Rezulin). However, Rezulin was taken off the market in early 2000 because of reports of liver failure, patients needing liver transplants, and deaths. Two other thiazolidinediones were introduced for use in the U.S.:
Self-Assessment Quiz Question #2 How do sulfonylureas work to decrease blood glucose levels?
a. Decrease insulin production. b. Stimulate the release of insulin. c. Decrease the desire to eat carbohydrates. d. Increase insulin sensitivity.
THIAZOLIDINEDIONES
Rosiglitazone (Avandia) and pioglitazone (Actos). Although both thiazolidinediones are like troglitazone (Rezulin), they do not seem to be associated with the same liver toxicity (Capoccia & Odegard, 2022). In 2007, the FDA required that rosiglitazone (Avandia) include a black box warning concerning the potential for increased ischemic cardiovascular risk. By 2010, the FDA reported that only patients who were successfully treated with rosiglitazone (Avandia) or not adequately controlled on other medications could receive the drug. Around 2013, the FDA’s decision to
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Book Code: RPTTX2024
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