Worst Pills, Best Pills

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Drug Profile

Do NOT stop taking this or any drug without the advice of your physician. Some drugs can cause severe adverse effects when they are stopped suddenly.

Do Not Use [what does this mean?]
Generic drug name: acetohexamide (a set oh HEX a mide)
Brand name(s): DYMELOR
GENERIC: not available FAMILY: Sulfonylureas
Find the drug label by searching at DailyMed.

Do Not Use [what does this mean?]
Generic drug name: chlorpropamide (klor PROE pa mide)
Brand name(s): DIABINESE, GLUCAMIDE
GENERIC: not available FAMILY: Sulfonylureas
Find the drug label by searching at DailyMed.

Alternative Treatment [top]

Safety Warnings For This Drug [top]

Risk of Low Blood Sugar (Hypoglycemia) With Individual Sulfonylureas in Older People

A study has been published assessing the risk of serious hypoglycemia in diabetics over age 65 taking one of the sulfonylurea drugs.[1] The new sulfonylurea drug glimepiride was not included in the study.

Serious hypoglycemia was more than four times more frequent in those using glyburide or chlorpropamide than in users of tolbutamine. Serious hypoglycemia occurred twice as often among users of glyburide compared to those taking glipizide. Compared to tolbutamide, those taking glipizide experienced serious hypoglycemia 2.5 times more often in the study.

Listed below are the drugs taken by diabetics in the study, from glyburide, which caused the most reactions, to tolbutamide, which caused the fewest.

Frequency of Serious Hypoglycemic Reactions with Sulfonylureas
  1. glyburide
  2. chlorpropamide
  3. acetohexamide
  4. tolazamide
  5. glipizide
  6. tolbutamide

Facts About This Drug [top]

Acetohexamide

Acetohexamide was approved for use in the United States in 1964. We strongly recommend that you do not use it because it takes a long time to be eliminated from the body and is more likely than other diabetes pills to cause serious adverse effects associated with low blood sugar. The drug is particularly dangerous in people with impaired kidney function,1 which many people older than 60 have even though they have blood test results showing normal kidney function.

This drug...

Acetohexamide

Acetohexamide was approved for use in the United States in 1964. We strongly recommend that you do not use it because it takes a long time to be eliminated from the body and is more likely than other diabetes pills to cause serious adverse effects associated with low blood sugar. The drug is particularly dangerous in people with impaired kidney function,1 which many people older than 60 have even though they have blood test results showing normal kidney function.

This drug is no longer officially marketed in the U.S., either because it was withdrawn for safety reasons or its manufacturers discontinued its production.[2]

Chlorpropamide

Chlorpropamide is a member of the sulfonylurea family of antidiabetic drugs and has been on the U.S. market since 1959.

Problems were recognized with chlorpropamide at the time of its original FDA approval in this country. The Medical Letter on Drugs and Therapeutics, a publication we frequently cite because it is a consistent source of objective drug information, reviewed chlorpropamide in March 1959 and concluded: “Whatever the incidence, the toxicity of Diabinese is clearly much greater than that of Orinase and it seems highly inadvisable to substitute Diabinese for Orinase. The convenience of taking Diabinese only once daily is hardly worth the added risk.”[3]

In 1978, we raised concerns about the safety of chlorpropamide and other diabetes drugs in the book titled Off Diabetes Pills published by the Health Research Group.[4] We have listed chlorpropamide as a Do Not Use drug ever since publication of the 1988 edition of Worst Pills, Best Pills because it was more likely than other diabetic drugs to cause low blood sugar in the elderly. This recommendation was based on a 1985 World Health Organization publication.[5]

A new warning was added in May 2002 to the professional product labeling or package insert for chlorpropamide concerning its use in the elderly. The new warning cites increased risks of low blood sugar (hypoglycemia), low blood sodium levels (hyponatremia) or both in patients aged 65 and older. The text of the warning reads:

Geriatric Use

The safety and effectiveness of Diabinese in patients aged 65 and over has not been properly evaluated in clinical studies. Adverse event reporting suggests that elderly patients may be more prone to developing hypoglycemia and/or hyponatremia when using Diabinese. Although the underlying mechanisms are unknown, abnormal renal (kidney) function, drug interaction, and poor nutrition appear to contribute to these events.

Chlorpropamide also is the only oral diabetes drug that causes an adverse effect known as the syndrome of inappropriate secretion of antidiuretic hormone (SIADH), one cause of hyponatremia.[6]

The drug also may increase cardiovascular risks and mortality relative to a placebo.[7],[8]

last reviewed June 30, 2021