Acetohexamide

Acetohexamide Brand Name

Dymelor

What is Acetohexamide

NOTE: This drug is discontinued in the U.S.

Acetohexamide was a first-generation oral sulfonylurea.

It was used, as an adjunct to diet and exercise, to lower blood glucose in patients with type 2 diabetes mellitus.

Similar hypoglycemic efficacy occurs with equipotent dosage of sulfonylureas. Sulfonylurea antidiabetic agents exhibit similar hypoglycemic mechanisms, although there are quantitative differences in their individual pharmacokinetic properties.

The duration of action of acetohexamide is about 12 to 18 hours.

Acetohexamide is metabolized to a more potent active metabolite which is primarily renally eliminated; the active metabolite accounts for the prolonged effects of acetohexamide relative to the parent drug’s short half-life.

Acetohexamide is contraindicated for use in patients with significant renal impairment.

In addition, acetohexamide exhibits uricosuric activity, which made the drug potentially useful for diabetic patients with gout.

Acetohexamide was FDA approved in 1964.

The drug was removed from marketing in the U.S. in the 1990’s.

Indications

  • type 2 diabetes mellitus

For treatment of type 2 diabetes mellitus not controlled by diet and exercise alone

Side Effects

  1. agranulocytosis
  2. angioedema
  3. aplastic anemia
  4. arthralgia
  5. blurred vision
  6. cholestasis
  7. dizziness
  8. elevated hepatic enzymes
  9. erythema
  10. erythema multiforme
  11. exfoliative dermatitis
  12. fatigue
  13. flushing
  14. headache
  15. hemolysis
  16. hemolytic anemia
  17. hepatic failure
  18. hepatitis
  19. hypoglycemia
  20. hyponatremia
  21. jaundice
  22. leukopenia
  23. maculopapular rash
  24. myalgia
  25. nausea
  26. pancytopenia
  27. photosensitivity
  28. porphyria
  29. pruritus
  30. pyrosis (heartburn)
  31. secondary failure
  32. SIADH
  33. thrombocytopenia
  34. urticaria
  35. vasculitis
  36. weakness
  37. weight gain

Monitoring Parameters

  • blood glucose
  • glucose-6-phosphate dehydrogenase (G6PD) activity
  • glycosylated hemoglobin A1c (HbA1c)

Contraindications

  • breast-feeding
  • children
  • diabetic ketoacidosis
  • fever
  • geriatric
  • hepatic disease
  • infection
  • neonates
  • obstetric delivery
  • porphyria
  • pregnancy
  • renal disease
  • renal failure
  • renal impairment
  • sulfonamide hypersensitivity
  • sulfonylurea hypersensitivity
  • surgery
  • thyroid disease
  • trauma
  • type 1 diabetes mellitus

Interactions

  • Acebutolol
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Dichloralphenazone; Isometheptene
  • Acetaminophen; Guaifenesin; Phenylephrine
  • Acetaminophen; Pseudoephedrine
  • Acitretin
  • Acrivastine; Pseudoephedrine
  • Aliskiren; Valsartan
  • Alogliptin; Metformin
  • Aminolevulinic Acid
  • Amiodarone
  • Amlodipine; Benazepril
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amphetamine
  • Amphetamine; Dextroamphetamine
  • Amprenavir
  • Androgens
  • Angiotensin II receptor antagonists
  • Angiotensin-converting enzyme inhibitors
  • Aripiprazole
  • Articaine; Epinephrine
  • Asenapine
  • Aspirin, ASA
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Dipyridamole
  • Aspirin, ASA; Omeprazole
  • Aspirin, ASA; Oxycodone
  • Aspirin, ASA; Pravastatin
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atenolol
  • Atenolol; Chlorthalidone
  • atypical antipsychotic
  • Azilsartan
  • Azilsartan; Chlorthalidone
  • Benazepril
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Bendroflumethiazide; Nadolol
  • Benzphetamine
  • Beta-blockers
  • Betaxolol
  • Bexarotene
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bisoprolol
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Bortezomib
  • Brexpiprazole
  • Brimonidine; Timolol
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Bumetanide
  • Canagliflozin; Metformin
  • Candesartan
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Captopril
  • Captopril; Hydrochlorothiazide, HCTZ
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Guaifenesin; Phenylephrine
  • Carbetapentane; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pseudoephedrine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Carbonic anhydrase inhibitors
  • Cariprazine
  • Carteolol
  • Carvedilol
  • Cetirizine; Pseudoephedrine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chlophedianol; Guaifenesin; Phenylephrine
  • Chloramphenicol
  • Chloroquine
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorthalidone; Clonidine
  • Choline Salicylate; Magnesium Salicylate
  • Chromium
  • Cimetidine
  • Cisapride
  • Clarithromycin
  • Clindamycin; Tretinoin
  • Clonidine
  • Clozapine
  • Codeine; Phenylephrine; Promethazine
  • Colchicine; Probenecid
  • Colesevelam
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  • Demeclocycline
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  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmethylphenidate
  • Dextroamphetamine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Guaifenesin; Phenylephrine
  • Dextromethorphan; Guaifenesin; Pseudoephedrine
  • Diazoxide
  • Dienogest; Estradiol valerate
  • Diethylpropion
  • Diethylstilbestrol, DES
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Phenylephrine
  • Disopyramide
  • Dobutamine
  • Dopamine
  • Dorzolamide; Timolol
  • Doxycycline
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enalapril, Enalaprilat
  • Enalapril; Felodipine
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Ephedrine
  • Epinephrine
  • Eprosartan
  • Eprosartan; Hydrochlorothiazide, HCTZ
  • Eravacycline
  • Ertugliflozin; Metformin
  • Esmolol
  • Esterified Estrogens
  • Esterified Estrogens; Methyltestosterone
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Estradiol; Levonorgestrel
  • Estradiol; Norethindrone
  • Estradiol; Norgestimate
  • Estradiol; Progesterone
  • Estramustine
  • Estrogens
  • Estropipate
  • Ethanol
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Ethotoin
  • Exenatide
  • Fenofibrate
  • Fenofibric Acid
  • Fexofenadine; Pseudoephedrine
  • Fluconazole
  • Fluocinolone; Hydroquinone; Tretinoin
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluoxymesterone
  • Fosamprenavir
  • Fosinopril
  • Fosinopril; Hydrochlorothiazide, HCTZ
  • Fosphenytoin
  • Furosemide
  • Garlic, Allium sativum
  • Gemfibrozil
  • Glecaprevir; Pibrentasvir
  • Glimepiride; Rosiglitazone
  • Glipizide; Metformin
  • Glyburide; Metformin
  • Green Tea
  • Griseofulvin
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guaifenesin; Phenylephrine
  • Guaifenesin; Pseudoephedrine
  • Halobetasol; Tazarotene
  • Hydantoins
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Telmisartan
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrochlorothiazide, HCTZ; Valsartan
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydroxychloroquine
  • Ibuprofen; Pseudoephedrine
  • Iloperidone
  • Indapamide
  • Indinavir
  • Insulin Glargine; Lixisenatide
  • Irbesartan
  • Isocarboxazid
  • Isoproterenol
  • Itraconazole
  • Ketoconazole
  • Labetalol
  • Lanreotide
  • Ledipasvir; Sofosbuvir
  • Levobetaxolol
  • Levobunolol
  • Linagliptin; Metformin
  • Linezolid
  • Lisdexamfetamine
  • Lisinopril
  • Lithium
  • Lixisenatide
  • Lomefloxacin
  • Lopinavir; Ritonavir
  • Loratadine; Pseudoephedrine
  • Lorcaserin
  • Losartan
  • Lovastatin; Niacin
  • Lumateperone
  • Lurasidone
  • Magnesium Salicylate
  • Mecasermin rinfabate
  • Mecasermin, Recombinant, rh-IGF-1
  • Mepivacaine; Levonordefrin
  • Mequinol; Tretinoin
  • Mestranol; Norethindrone
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methamphetamine
  • Methotrexate
  • Methoxsalen
  • Methylphenidate
  • Methyltestosterone
  • Metoprolol
  • Metreleptin
  • Metyrapone
  • Miconazole
  • Midodrine
  • Minocycline
  • Moexipril
  • Monoamine oxidase inhibitors
  • Nadolol
  • Nandrolone Decanoate
  • Naproxen; Pseudoephedrine
  • Nebivolol
  • Nebivolol; Valsartan
  • Nelfinavir
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicotine
  • Nitazoxanide
  • Nonsteroidal antiinflammatory drugs
  • Norepinephrine
  • Octreotide
  • Olanzapine
  • Olmesartan
  • Omadacycline
  • Ombitasvir; Paritaprevir; Ritonavir
  • Orlistat
  • Oxandrolone
  • Oxymetholone
  • Paliperidone
  • Pasireotide
  • Pegvisomant
  • Pemoline
  • Penbutolol
  • Pentamidine
  • Pentoxifylline
  • Perindopril
  • Perindopril; Amlodipine
  • Phendimetrazine
  • Phenelzine
  • Phenothiazines
  • Phentermine
  • Phentermine; Topiramate
  • Phenylephrine
  • Phenylephrine; Promethazine
  • Phenytoin
  • Photosensitizing agents (topical)
  • Pindolol
  • Porfimer
  • Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
  • Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
  • Prilocaine; Epinephrine
  • Probenecid
  • Progestins
  • Propranolol
  • Protease inhibitors
  • Pseudoephedrine
  • Quetiapine
  • Quinapril
  • Quinolones
  • Racepinephrine
  • Ramipril
  • Ranitidine
  • Reserpine
  • Rifamycins
  • Risperidone
  • Ritodrine
  • Ritonavir
  • Rosiglitazone
  • Sacubitril; Valsartan
  • Salsalate
  • Saquinavir
  • Sarecycline
  • Segesterone Acetate; Ethinyl Estradiol
  • Selegiline
  • Sofosbuvir
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Somatropin, rh-GH
  • Sotalol
  • Sparfloxacin
  • Sulfacetamide
  • Sulfacetamide; Sulfur
  • Sulfinpyrazone
  • Sulfonamides
  • Sympathomimetics
  • Tacrolimus
  • Tazarotene
  • Tegaserod
  • Telmisartan
  • Testolactone
  • Testosterone
  • Tetracycline
  • Tetracyclines
  • Thiazide diuretics
  • Thyroid hormones
  • Timolol
  • Tipranavir
  • tobacco
  • Torsemide
  • Trandolapril
  • Trandolapril; Verapamil
  • Tranylcypromine
  • Tretinoin, ATRA
  • Triamterene
  • Trovafloxacin, Alatrofloxacin
  • Valsartan
  • Verteporfin
  • Voriconazole
  • Warfarin
  • Ziprasidone
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