Amaryl - General Information
Amaryl is the first III generation sulphonyl urea it is a very potent sulphonyl urea with long duration of action.
Pharmacology of Amaryl
Amaryl, like glyburide and glipizide, is a "second-generation" sulfonylurea agents. Amaryl 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.
Amaryl for patients
Patients should be informed of the potential risks and advantages of AMARYL and of alternative modes of therapy. They should also be informed about the importance of adherence to dietary instructions, of a regular exercise program, and of regular testing of blood glucose.
The risks of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be explained to patients and responsible family members. The potential for primary and secondary failure should also be explained.
| Here are some common questions concerning Amaryl and its use in managing diabetes.
What is Amaryl?Amaryl (pronounced AM-a-rill) is a type of diabetes medication called a sulfonylurea (sull-fon-ill-u-REE-ah). Doctors have been prescribing sulfonylureas for more than 40 years.
Amaryl is a sulfonylurea for patients with type 2 diabetes and can be used along with proper diet and exercise when diet and exercise are not enough.
In addition, Amaryl may be used in combination with insulin or metformin (another type of diabetes medication) when diet, exercise, and Amaryl or metformin alone are not enough to lower your blood glucose (sugar) levels. When used in combination with insulin, Amaryl may reduce the amount of insulin needed. Taking Amaryl and metformin or insulin in combination may increase the potential for blood glucose levels to be too low.
How Does Amaryl Work?Amaryl works primarily to correct insulin deficiency. When your body doesn't have enough insulin, it can't carry glucose out of the bloodstream and into the cells. Amaryl helps your body produce extra insulin when it is needed (after meals), so it can carry glucose into your cells to be converted into energy. Amaryl may also make tissues in your muscles and other organs more sensitive to insulin.
How Often is Amaryl Taken?You need to take Amaryl only once a day with the first main meal. It is important to keep getting your prescription refilled and taking Amaryl, unless your doctor gives you other instructions.
Why Did the Doctor Choose Amaryl?Your doctor probably chose Amaryl for several reasons. Amaryl is an effective medication that needs to be taken only once a day, which makes it more convenient for you to fit into your schedule. And, if you inject insulin, Amaryl can reduce the amount of insulin you need.
Does Amaryl Have Any Side Effects?In clinical studies, the most common side effects with Amaryl are blood sugar levels that are too low (0.9% to 1.7%), dizziness (1.7%), weakness (1.6%), headache (1.5%), and nausea (1.1%). As with other drugs similar to Amaryl, there is a possibility of experiencing blood sugar levels that are severely low.
Taking Amaryl and metformin or insulin in combination may increase the potential for blood glucose levels to be too low.
Patients with impaired kidney function should be started on a lower dose because of the increased potential for blood sugar levels to be too low.
How Long Should Amaryl Be Taken?You will need to take Amaryl until your doctor tells you otherwise. Keep getting your prescriptions refilled and taking Amaryl unless your doctor gives you different instructions.
Can Amaryl Be Taken With Other Medications?Many medications can be taken with Amaryl. You should always talk with your doctor about all the prescription and over-the-counter medications and dietary supplements you are taking before starting a new prescription.
Can Amaryl Be Taken During Pregnancy?Amaryl should not be used during pregnancy. Women taking Amaryl who suspect that they are pregnant should contact their doctor immediately.
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),
- 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.
Glimepiride is Contraindicated in Patients with:
- Known hypersensitivity to the drug.
- Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.
Additional information about Amaryl
Amaryl Indication: For concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.
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. Amaryl 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.
Drug Interactions: Cyclosporine The sulfonylurea increases the effect of cyclosporine
Gemfibrozil Gemfibrozil increases the effect and toxicity of rosiglitazone/pioglitazone
Glucosamine Possible hyperglycemia
Ketoconazole Ketoconazole increases the effect of rosiglitazone
Pregabalin Increased risk of edema
Repaglinide Similar mode of action - questionable association
Rifampin Rifampin reduces levels and efficacy of rosiglitazone, rifampin decreases the effect of sulfonylurea
Food Interactions: Even though food reduces product absorption, the manufacturer recommends taking the product with the first meal of the day.
Generic Name: Glimepiride
Synonyms: Glimepirid; Glimepirida; Glimepiridum; Glimepride
Drug Category: Immunosuppressive Agents; Hypoglycemic Agents; Antiarrhythmic Agents; Sulfonylureas
Drug Type: Small Molecule; Approved
Other Brand Names containing Glimepiride: Amarel; Amaryl; Endial; Novo-glimepiride; PMS-glimepiride; Ratio-glimepiride; Sandoz glimepiride;
Absorption: Completely (100%) absorbed following oral administration.
Toxicity (Overdose): Severe hypoglycemic reactions with coma, seizure, or other neurological impairment.
Protein Binding: Over 99.5% bound to plasma protein.
Biotransformation: Hepatic. Following either an intravenous or oral dose, glimepiride is completely metabolized by oxidative biotransformation to a major metabolite, cyclohexyl hydroxymethyl derivative (M1), via the hepatic cytochrome P450 II C9 subsystem. M1 is further metabolized to the carboxyl derivative (M2) by one or several cytosolic enzymes. M1, but not M2, possessed approximately one third of the pharmacologic activity of its parent in an animal model. However, whether the glucose-lowering effect of M1 is clinically significant is not clear.
Half Life: Approximately 5 hours following single dose.
Dosage Forms of Amaryl: Tablet Oral
Chemical IUPAC Name: 3-ethyl-4-methyl-N-[2-[4-[(4-methylcyclohexyl)carbamoylsulfamoyl]phenyl]ethyl]-2-oxo-5H-pyrrole-1-carboxamide
Chemical Formula: C24H34N4O5S
Glimepiride on Wikipedia: http://en.wikipedia.org/wiki/Glimepiride
Organisms Affected: Humans and other mammals