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Acetohexamide

Published: July 26, 2026Updated: August 24, 2026

Acetohexamide is a first-generation sulfonylurea medication used to treat type 2 diabetes mellitus by stimulating the pancreas to release more insulin, helping to lower blood glucose levels.

Quick summary

Acetohexamide is an oral sulfonylurea that helps control blood sugar in type 2 diabetes by stimulating insulin release from the pancreas.

Medically reviewed by WellAlly Editorial TeamLast reviewed August 24, 2026Editorial policy

Key facts at a glance

ATC
A10BB31
RxNorm
173
Generic
Acetohexamide
Class
atc-a10
Brands
—
Availability
rx
Lactation
unknown
Routes
oral
Forms
tablet
Regions
US, EU, CN, JP
Monitoring
—

This page is for informational purposes only.

Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.

Dosage and administration

adult (standard)tablet
Usual dose
500mg twice daily
Maximum
consult physician
Frequency
every 12 hours
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard
pediatric (standard)tablet
Usual dose
250mg twice daily
Maximum
consult physician
Frequency
every 12 hours
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard
geriatric (standard)tablet
Usual dose
400mg daily
Maximum
consult physician
Frequency
once daily
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard

Overdose information

Important overdose information
Toxic dose: Single dose that may cause serious toxicity
Chronic overdose: cumulative doses exceeding 2000mg daily over extended periods may lead to persistent hypoglycemia
Immediate actions
administer intravenous dextrose, consider activated charcoal if presentation within 1-2 hours
Antidote
Dextrose (glucose) and Octreotide(highly effective when promptly administered to restore blood glucose levels)
Poison Control: 1-800-222-1222

Special Populations

8 groups
✗

pregnancy

first trimester
unsafe
FDA Category
C
Dose Adjustment

avoid if possible

Key Recommendations

avoid use during pregnancy unless benefits outweigh risks; insulin is preferred

Monitor

regular fetal monitoring

Use of this medication in this population requires careful consideration of risks and benefits.

✗

pregnancy

second trimester
unsafe
FDA Category
C
Dose Adjustment

avoid if possible

Key Recommendations

avoid use during pregnancy; insulin therapy recommended

Monitor

regular fetal monitoring and glucose control assessment

Use of this medication in this population requires careful consideration of risks and benefits.

✗

pregnancy

third trimester
unsafe
FDA Category
C
Dose Adjustment

avoid if possible

Key Recommendations

discontinue before delivery; insulin is preferred for glycemic control

Monitor

fetal monitoring and assessment of glycemic control

Use of this medication in this population requires careful consideration of risks and benefits.

✗

lactation

not recommended
unsafe
FDA Category
C
Dose Adjustment

avoid

Key Recommendations

do not breastfeed while taking acetohexamide; consider alternative antidiabetic therapy

Monitor

monitor infant for signs of hypoglycemia

Use of this medication in this population requires careful consideration of risks and benefits.

⚠

geriatric

elderly
caution
FDA Category
N
Dose Adjustment

start with lowest effective dose

Key Recommendations

use with caution; increased risk of hypoglycemia in elderly; start low and titrate slowly

Monitor

frequent blood glucose monitoring

Use with caution and monitor for adverse effects.

✗

pediatric_age

children adolescents
contraindicated
FDA Category
N
Dose Adjustment

not recommended

Key Recommendations

not indicated for use in pediatric patients; insulin therapy preferred

Monitor

not applicable

Use of this medication in this population requires careful consideration of risks and benefits.

⚠

renal_impairment

mild to moderate
caution
FDA Category
N
Dose Adjustment

dose reduction may be required

Key Recommendations

use with caution; may require dose adjustment based on renal function; increased risk of hypoglycemia

Monitor

monitor renal function and blood glucose closely

Use with caution and monitor for adverse effects.

⚠

hepatic_impairment

mild to moderate
caution
FDA Category
N
Dose Adjustment

dose reduction may be required

Key Recommendations

use with caution; drug metabolized in liver; may require dose adjustment

Monitor

monitor liver function and blood glucose

Use with caution and monitor for adverse effects.

Statistics and clinical data

prescribingFDA
2023

Commonly prescribed since

Value:1970s

General prescribing information

drug_classWHO
2023

Drug class

Value:Sulfonylurea (First-generation)

Drug class information

usageMedical guidelines
2023

Common uses

Value:Type 2 Diabetes Mellitus treatment

Common therapeutic uses

mechanismPharmacology references
2023

Mechanism of action

Value:Stimulates insulin secretion from pancreatic beta cells

Pharmacological action

Acetohexamide is used to treat type 2 diabetes in adults when diet control and exercise have not provided adequate blood sugar control. It may be used as monotherapy or in combination with other diabetes medications.

As a sulfonylurea, acetohexamide stimulates insulin release from pancreatic beta cells by binding to specific receptors on these cells. This increased insulin production helps lower blood glucose levels.

Acetohexamide can cause hypoglycemia, especially in elderly patients, those with kidney or liver impairment, and when combined with other diabetes medications. Patients should take it as prescribed, typically 30 minutes before a meal. This medication is rarely prescribed today due to the availability of safer, more effective alternatives.

Contraindications

Conditions and patient states where this medication should be avoided or used with caution.

Do not use (1)

ABSOLUTEhypersensitivity

Known allergy to this medication or its components

Use caution (1)

RELATIVEpregnancy

Consult healthcare provider for benefits vs risks assessment

Official drug label

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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.

Medical Disclaimer

This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.

If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.

Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy