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trademark for a preparation of acetohexamide, an oral hypoglycemic agent.
Pregnancy Category: C
Management of type 2 diabetes mellitus as an adjunct to diet.
Lowers blood sugar by stimulating the release of insulin from the pancreas and increasing insulin sensitivity at receptor sites.
May also decrease hepatic glucose production.
Lowering of blood sugar in diabetic patients.
Absorption: Well absorbed following oral administration.
Protein Binding: 65–90% bound to plasma proteins.
Metabolism and Excretion: Mostly metabolized by the liver; some conversion to hydroxyhexamide, which also lowers blood sugar.
Half-life: Acetohexamide—1.3 hr (up to 30 hr in renal impairment); hydroxyhexamide—4.6–6 hr.
Time/action profile (hypoglycemic activity)
|PO||60 min||unknown||12–24 hr|
Contraindicated in: Hypersensitivity; Known severe allergy to sulfonamides (e.g. sulfonylureas, thiazide/loop diuretics; Type 1 diabetes mellitus; Diabetic ketoacidosis; Obstetric / Lactation: Safety not established; insulin recommended during pregnancy.
Use Cautiously in: Geriatric: ↑ sensitivity; dosage ↓ may be required; Renal or hepatic impairment (↑ risk of hypoglycemia); Infection, stress, or changes in diet (may alter blood sugar and requirements for glycemic control); Impaired thyroid, pituitary, or adrenal function (↑ risk of hypoglycemia).
Adverse Reactions/Side Effects
Central nervous system
- dizziness (most frequent)
- headache (most frequent)
- anorexia (most frequent)
- cholestatic jaundice (life-threatening)
- constipation (most frequent)
- diarrhea (most frequent)
- drug-induced hepatitis
- epigastric fullness (most frequent)
- heartburn (most frequent)
- ↑ appetite
- photosensitivity (most frequent)
- hypoglycemia (most frequent)
- syndrome of inappropriate secretion of antidiuretic hormone (SIADH)
- aplastic anemia (life-threatening)
- hemolytic anemia
Drug-Drug interactionIngestion of alcohol may result in disulfiram-like reaction.Effectiveness may be ↓ by concurrent use of calcium channel blockers, cholestyramine, corticosteroids, diazoxide, estrogens, phenytoin, isoniazid, hormonal contraceptives, loop diuretics, phenothiazines, rifampin, sympathomimetics, thiazide diuretics, thyroid hormones, and urinary alkalinizers.beta blockers, chloramphenicol, fluconazole, gemfibrozil, histamine H2 receptor antagonists, methyldopa, MAO inhibitors,NSAIDS, probenecid, salicylates, sulfonamides, tricyclic antidepressants, and urinary acidifiers may ↑ the risk of hypoglycemia.Concurrent use with warfarin may alter the response to both agents (↑ effects of both initially, then ↓ activity; close monitoring recommended during any changes in dosage).Glucosamine may worsen hypoglycemia.Fenugreek, chromium, and coenzyme Q-10 may produce ↑ hypoglycemic effects.
Oral (Adults) 250 mg once daily; dose can be ↑ as needed by 250–500 mg daily every 5–7 days (not to exceed 1.5 g/day; doses >1 g/day should be given as divided doses). Geriatric patients or hepatic insufficiency—dosage ↓ may be required.
Renal ImpairmentOral (Adults) CCr < 50 mL/min—Use not recommended (↑ risk of hypoglycemia).
Availability (generic available)
Tablets: 250 mg, 500 mg
- Observe patient for signs and symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety).
- Assess patient for allergy to sulfonamides.
- Lab Test Considerations: Monitor serum glucose and Hb A1c periodically during therapy to evaluate effectiveness of treatment.
- Monitor CBC periodically throughout therapy. Notify health care professional promptly if ↓ in blood counts occurs.
Overdose is manifested by symptoms of hypoglycemia. Mild hypoglycemia may be treated with administration of oral glucose. Severe hypoglycemia should be treated with IV D50W followed by continuous IV infusion of more dilute dextrose solution at a rate sufficient to keep serum glucose at approximately 100 mg/dL.
- May cause an increase in AST, LDH, BUN, and serum creatinine.
Potential Nursing DiagnosesImbalanced nutrition: more than body requirements (Indications)
Noncompliance (Patient/Family Teaching)
- high alert: Accidental administration of oral hypoglycemic agents to non-diabetic adults and children has resulted in serious harm or death. Before administering, confirm that patient has diabetes.
- high alert: Do not confuse acetohexamide with acetazolamide.
- Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
- To convert from other oral hypoglycemic agents, the initial dose of acetohexamide should be about half the dose of tolbutamide and double the dose of chlorpropamide. A transition period is necessary with chlorpropamide because of the long half-life. Subsequent dose adjustments should be made based on the patient’s response. For patients on an insulin dose of <20 units/day, insulin can be discontinued immediately after starting acetohexamide. Patients taking >20 units/day should convert gradually by receiving an initial dose of acetohexamide of 250 mg and a 25–30% reduction in insulin dose the first day, with gradual insulin dose reduction as tolerated. Hospitalization should be considered during the transition from insulin to acetohexamide.
- Oral: May be administered once in the morning or divided into 2 doses. Administer with meals to ensure best diabetic control and to minimize gastric irritation. Do not administer after last meal of the day.
- Tablets may be crushed and taken with fluids if patient has difficulty swallowing.
- Instruct patient to take medication at same time each day. Take missed doses as soon as remembered unless almost time for next dose. Do not take if unable to eat.
- Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long-term.
- Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water and to notify health care professional.
- Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
- Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness and health care professional notified if significant changes occur.
- May occasionally cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient to notify health care professional promptly if unusual weight gain, swelling of ankles, drowsiness, shortness of breath, muscle cramps, weakness, sore throat, rash, or unusual bleeding or bruising occurs.
- Caution patient to avoid alcohol while on acetohexamide as it may cause a disulfiram-like reaction (facial flushing, breathlessness).
- Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
- Advise patient to inform health care professional of medication regimen before treatment or surgery.
- Insulin is the preferred method of controlling blood sugar during pregnancy. Counsel female patients to use a form of contraception other than hormonal contraceptives and to notify health care professional promptly if pregnancy is planned or suspected.
- Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
- Emphasize the importance of routine follow-up exams.
- Control of blood glucose levels without the appearance of hypoglycemic or hyperglycemic episodes.
a trademark for an antidiabetic (acetoHEXAMIDE).
AcetohexamideA first-generation oral sulfonylurea used to reduce glucose in type 2 diabetics whose diabetes can’t be controlled by diet.
Mechanism of action Triggers release of insulin from the pancreas.
Pharmacokinetics Metabolised in liver to an active analogue; excreted via kidneys.
Adverse effects Hypoglycaemic reactions—e.g., coma, nausea, vomiting, dizziness, cholestatic jaundice, agranulocytosis, aplastic and haemolytic anaemia, hypersensitivity, skin reactions including photosensitivity, rash and itching.
Precautions Hypertension, liver and kidney disease, allergies