Description

Simple

Clinical

Overview

A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide. Acetohexamide has been discontinued in the US market.

Pharmacology

Indication

Used in the management of diabetes mellitus type 2 (adult-onset).

Pharmacodynamic

Acetohexamide is an intermediate-acting, first-generation oral sulfonylurea. It lowers blood sugar by stimulating the pancreatic beta cells to secrete insulin and by helping the body use insulin efficiently. Due to its primary action on the pancreatic beta cells, the drug is only effective when ther... Read more

Mechanism of action

Sulfonylureas such as acetohexamide bind to an ATP-dependent K+ channel on the cell membrane of pancreatic beta cells. This inhibits a tonic, hyperpolarizing outflux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization opens volt... Read more

Absorption

Rapidly absorbed from the GI tract.

Protein binding

90%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Elimination half-life of the parent compound is 1.3 hours and the elimination half-life of the active metabolite is approximately 5-6 hours.

Route of elimination

Information currently not available.

Toxicity

Oral, rat LD50: 5 gm/kg; Oral, mouse LD50: >2500 mg/kg. Symptoms of an acetohexamide overdose include hunger, nausea, anxiety, cold sweats, weakness, drowsiness, unconsciousness, and coma.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

Interactions

Type in a drug name to check for interaction with Acetohexamide
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
Acetohexamide may increase the anticoagulant activities of (R)-warfarin.
(S)-Warfarin
Acetohexamide may increase the anticoagulant activities of (S)-Warfarin.
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Acetohexamide is combined with 2,4-thiazolidinedione.
3,5-diiodothyropropionic acid
The therapeutic efficacy of Acetohexamide can be decreased when used in combination with 3,5-diiodothyropropionic acid.
3,5-Diiodotyrosine
The therapeutic efficacy of Acetohexamide can be decreased when used in combination with 3,5-Diiodotyrosine.
4-hydroxycoumarin
The therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Acetohexamide.
4-methylumbelliferyl beta-D-glucoside
The therapeutic efficacy of Acetohexamide can be increased when used in combination with 4-methylumbelliferyl beta-D-glucoside.
5-(2-methylpiperazine-1-sulfonyl)isoquinoline
The therapeutic efficacy of Acetohexamide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Acetohexamide.
Abaloparatide
The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Abaloparatide.
Abatacept
The metabolism of Acetohexamide can be increased when combined with Abatacept.
Abiraterone
The metabolism of Acetohexamide can be decreased when combined with Abiraterone.
Acarbose
The risk or severity of hypoglycemia can be increased when Acarbose is combined with Acetohexamide.
Acebutolol
The therapeutic efficacy of Acetohexamide can be increased when used in combination with Acebutolol.
Aceclofenac
The protein binding of Acetohexamide can be decreased when combined with Aceclofenac.
Acemetacin
The protein binding of Acetohexamide can be decreased when combined with Acemetacin.
Acenocoumarol
The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Acetohexamide.
Acepromazine
The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Acepromazine.
Aceprometazine
The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Aceprometazine.
Acetazolamide
The therapeutic efficacy of Acetohexamide can be increased when used in combination with Acetazolamide.