Tolbutamide

What is Tolbutamide

Tolbutamide is a ‘first-generation’ oral sulfonylurea antidiabetic agent used as an adjunct to diet to control blood glucose in patients with type 2 diabetes mellitus (DM).

Tolbutamide is the shortest-acting and least potent sulfonylurea; its duration of action is 6 to 12 hours.

Since it is extensively metabolized to inactive metabolites, tolbutamide may be useful in the treatment of elderly patients or patients with renal disease.

Brand Name

  • Orinase
  • Tol-Tab

Side Effects

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

Monitoring Parameters

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

Contraindications

  • breast-feeding
  • children
  • diabetic ketoacidosis
  • fever
  • G6PD deficiency
  • geriatric
  • hepatic disease
  • infection
  • neonates
  • obstetric delivery
  • pregnancy
  • renal disease
  • renal failure
  • renal impairment
  • sulfonamide hypersensitivity
  • sulfonylurea hypersensitivity
  • surgery
  • trauma
  • type 1 diabetes mellitus
  • uremia

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
  • Alpelisib
  • 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
  • Bosentan
  • Brexpiprazole
  • Brimonidine; Timolol
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Bumetanide
  • Canagliflozin; Metformin
  • Candesartan
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Cannabidiol
  • 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
  • Conjugated Estrogens
  • Conjugated Estrogens; Bazedoxifene
  • Conjugated Estrogens; Medroxyprogesterone
  • Corticosteroids
  • Cyclosporine
  • Daclatasvir
  • Danazol
  • Dapagliflozin; Metformin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Demeclocycline
  • Desloratadine; Pseudoephedrine
  • 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
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • 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
  • Fluvoxamine
  • 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; Methyldopa
  • 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
  • Imatinib
  • Indapamide
  • Indinavir
  • Insulin Glargine; Lixisenatide
  • Irbesartan
  • Isocarboxazid
  • Isoproterenol
  • Itraconazole
  • Ivacaftor
  • Ivosidenib
  • Ketoconazole
  • Labetalol
  • Lanreotide
  • Ledipasvir; Sofosbuvir
  • Leflunomide
  • Levobetaxolol
  • Levobunolol
  • Linagliptin; Metformin
  • Linezolid
  • Lisdexamfetamine
  • Lisinopril
  • Lithium
  • Lixisenatide
  • Lomefloxacin
  • Lopinavir; Ritonavir
  • Loratadine; Pseudoephedrine
  • Lorcaserin
  • Losartan
  • Lovastatin; Niacin
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • 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
  • Methyldopa
  • 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
  • Nitisinone
  • Nonsteroidal antiinflammatory drugs
  • Norepinephrine
  • Octreotide
  • Olanzapine
  • Olmesartan
  • Omadacycline
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oritavancin
  • 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
  • Rucaparib
  • Sacubitril; Valsartan
  • Salsalate
  • Saquinavir
  • Sarecycline
  • Segesterone Acetate; Ethinyl Estradiol
  • Selegiline
  • Sodium Iodide
  • Sofosbuvir
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Somatropin, rh-GH
  • Sotalol
  • Sparfloxacin
  • St. John’s Wort, Hypericum perforatum
  • Sulfacetamide
  • Sulfacetamide; Sulfur
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Sulfinpyrazone
  • Sulfonamides
  • Sympathomimetics
  • Tacrolimus
  • Tazarotene
  • Tegaserod
  • Telmisartan
  • Teniposide
  • Testolactone
  • Testosterone
  • Tetracycline
  • Tetracyclines
  • Tezacaftor; Ivacaftor
  • Thiazide diuretics
  • Thyroid hormones
  • Timolol
  • Tipranavir
  • tobacco
  • Torsemide
  • Trandolapril
  • Trandolapril; Verapamil
  • Tranylcypromine
  • Tretinoin, ATRA
  • Triamterene
  • Trimethoprim
  • Trovafloxacin, Alatrofloxacin
  • Valproic Acid, Divalproex Sodium
  • Valsartan
  • Vemurafenib
  • Verteporfin
  • Voriconazole
  • Warfarin
  • Zafirlukast
  • Ziprasidone
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