Tsiklamid
Tsiklamid - General Information
A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide. [PubChem]
Pharmacology of Tsiklamid
Tsiklamid 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. The pancreas must produce insulin for this medication to work. Tsiklamid has one-third the potency of chlorpropamide, and twice the potency of tolbutamide; however, similar hypoglycemic efficacy occurs with equipotent dosage of sulfonylureas.
Tsiklamid for patients
Tsiklamid Interactions
Tsiklamid Contraindications
Contraindicated in kidney disease, liver disease, and thyroid disease.
Additional information about Tsiklamid
Tsiklamid Indication: Used in the management of diabetes mellitus type 2 (adult-onset).
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 voltage-gated Ca2+ channels. The rise in intracellular calcium leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of (pro)insulin.
Drug Interactions: Acebutolol The beta-blocker decreases the symptoms of hypoglycemia
Atenolol The beta-blocker decreases the symptoms of hypoglycemia
Betaxolol The beta-blocker decreases the symptoms of hypoglycemia
Bisoprolol The beta-blocker decreases the symptoms of hypoglycemia
Carteolol The beta-blocker decreases the symptoms of hypoglycemia
Carvedilol The beta-blocker decreases the symptoms of hypoglycemia
Esmolol The beta-blocker decreases the symptoms of hypoglycemia
Labetalol The beta-blocker decreases the symptoms of hypoglycemia
Metoprolol The beta-blocker decreases the symptoms of hypoglycemia
Nadolol The beta-blocker decreases the symptoms of hypoglycemia
Pindolol The beta-blocker decreases the symptoms of hypoglycemia
Propranolol The beta-blocker decreases the symptoms of hypoglycemia
Sotalol The beta-blocker decreases the symptoms of hypoglycemia
Timolol The beta-blocker decreases the symptoms of hypoglycemia
Aspirin The salicylate increases the effect of sulfonylurea
Salicyclic acid The salicylate increases the effect of sulfonylurea
Chloramphenicol The agent increases the effect of sulfonylurea
Clofibrate The agent increases the effect of sulfonylurea
Dicumarol The agent increases the effect of sulfonylurea
Diazoxide Diazoxide / sulfonylurea:Antagonism of action
Isocarboxazid The MAO inhibitor increases the effect of the hypoglycemic agent
Phenelzine The MAO inhibitor increases the effect of the hypoglycemic agent
Tranylcypromine The MAO inhibitor increases the effect of the hypoglycemic agent
Phenylbutazone Increases the effect of the hypoglycemic agent
Repaglinide Similar mode of action - questionable association
Rifampin Rifampin decreases the effect of sulfonylurea
Sulfadiazine Sulfonamide/Sulfonylurea - possible hypoglycemia
Sulfamethizole Sulfonamide/Sulfonylurea - possible hypoglycemia
Sulfamethoxazole Sulfonamide/Sulfonylurea - possible hypoglycemia
Sulfapyridine Sulfonamide/Sulfonylurea - possible hypoglycemia
Sulfasalazine Sulfonamide/Sulfonylurea - possible hypoglycemia
Sulfisoxazole Sulfonamide/Sulfonylurea - possible hypoglycemia
Bevantolol The beta-blocker decreases the symptoms of hypoglycemia
Dicumarol The agent increases the effect of sulfonylurea
Glucosamine Possible hyperglycemia
Practolol The beta-blocker decreases the symptoms of hypoglycemia
Sulfacytine Sulfonamide/sulfonylurea: possible hypoglycemia
Sulfadoxine Sulfonamide/sulfonylurea: possible hypoglycemia
Food Interactions: Take without regard to meals.
Avoid alcohol.
Generic Name: Acetohexamide
Synonyms: Acetohexamid
Drug Category: Hypoglycemic Agents; Sulfonylureas
Drug Type: Small Molecule; Approved
Other Brand Names containing Acetohexamide: Cyclamide; Dimelin; Dimelor; Dymelor; Gamadiabet; Hypoglicil; Metaglucina; Minoral; Ordimel; Tsiklamid;
Absorption: Rapidly absorbed from the GI tract.
Toxicity (Overdose): 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.
Protein Binding: 90%
Biotransformation: Extensively metabolized in the liver to the active metabolite hydroxyhexamide, which exhibits greater hypoglycemic potency than acetohexamide. Hydroxyhexamide is believed to be responsible for prolonged hypoglycemic effects.
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.
Dosage Forms of Tsiklamid: Not Available
Chemical IUPAC Name: 3-(4-acetylphenyl)sulfonyl-1-cyclohexylurea
Chemical Formula: C15H20N2O4S
Acetohexamide on Wikipedia: https://en.wikipedia.org/wiki/Acetohexamide
Organisms Affected: Humans and other mammals
