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Active ingredient: Glimepiride - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Immunosuppressive Agents
  • Hypoglycemic Agents
  • Antiarrhythmic Agents
  • Sulfonylureas

Dosage Forms

  • Oral tablets with various strengths

Brands / Synonyms

Amarel; Amaryl; Avandaryl; Duetact; Endial; Glimepirid; Glimepirida [Spanish]; Glimepiride [Usan:Ban:Inn]; Glimepiridum [Latin]; Glimepride

Indications

For concomitant use with insulin for the treatment of noninsulin-dependent (Type II) diabetes mellitus; For the treatment of hyperglycemia that cannot be controlled by diet and exercise in conjunction with an oral hypoglycemic agent

Pharmacology

Glimepiride, like glyburide and glipizide, is a "second-generation" sulfonylurea agents. Glimepiride is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin.

Mechanism of Action

The mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Glimepiride likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin.

Absorption

completely (100%) absorbed

Toxicity

Severe hypoglycemic reactions with coma, seizure, or other neurological impairment, LD50=mg/kg(in mice)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Glimepiride is Contraindicated in Patients with:

1. Known hypersensitivity to the drug.

2. Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.

Drug Interactions

Many other medicines may increase or decrease the effects of glimepiride or affect your condition. Before taking
glimepiride, tell your doctor if you are taking any of the following medicines:
, aspirin or another salicylate such as magnesium/choline salicylate (Trilisate), salsalate (Disalcid, others),
choline salicylate (Arthropan), magnesium salicylate (Magan), or bismuth subsalicylate (Pepto-Bismol);
, a nonsteroidal anti-inflammatory drug (NSAID) such as ibuprofen (Motrin, Advil, Nuprin, others), ketoprofen
(Orudis, Orudis KT, Oruvail), diclofenac (Voltaren, Cataflam), etodolac (Lodine), indomethacin (Indocin),
nabumetone (Relafen), oxaprozin (Daypro), and naproxen (Anaprox, Naprosyn, Aleve);
, a sulfa-based drug such as sulfamethoxazole-trimethoprim (Bactrim, Septra), sulfisoxazole (Gantrisin),
or sulfasalazine (Azulfidine);
, a monoamine oxidase inhibitor (MAOI) such as isocarboxazid (Marplan), tranylcypromine (Parnate), or phenelzine (Nardil);
, a beta-blocker such as propranolol (Inderal), atenolol (Tenormin), acebutolol (Sectral), metoprolol (Lopressor),
and others;
, a diuretic (water pill) such as hydrochlorothiazide (HCTZ, Hydrodiuril), chlorothiazide (Diuril), and others;
, a steroid medicine such as prednisone (Deltasone, Orasone, others), methylprednisolone (Medrol, others), prednisolone
(Prelone, Pediapred, others), and others;
, a phenothiazine such as chlorpromazine (Thorazine), fluphenazine (Prolixin, Permitil), prochlorperazine (Compazine),
promethazine (Phenergan), and others;
, phenytoin (Dilantin);
, isoniazid (Nydrazid);
, rifampin (Rifadin, Rifamate); or
, over-the-counter cough, cold, allergy, or weight loss medications.

You may require a dosage adjustment or special monitoring if you are taking any of the medicines listed above.

Drugs other than those listed here may also interact with glimepiride or affect your condition. Talk to your doctor
and pharmacist before taking any prescription or over-the-counter medicines, including herbal products.

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