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Amaryl Review Article

 

Diabetes type 2Amaryl (generic name: glimepiride) is a sulfonylurea anti-diabetic drug that is medium to long acting. It is very potent as the first third-generation sulfonylurea. This drug is oral blood sugar-lowering and belongs to the sulfonylurea class of medications which are used for managing diabetes. Lowering of blood sugar is due to the release of insulin through pancreatic beta cells drug stimulation and by drug induced increase in activity of intracellular insulin receptors. Glimepiride is related to other sulfonylureas such as glipizide (Glucotrol), glyburide (Micronase; Diabeta), tolazamide (Tolinase), and tolbutamide (Orinase). Its contraindications include pregnancy and hypersensitivity sulfonylureas while side effects may include leukopenia, occasional allergic reactions, hemolytic anemia, gastrointestinal disturbance, and thrombocytopenia (rarely). Moreover, the risk of hypoglycemia is raised in the first weeks of treatment. In December of 1995, Glimepiride was approved by the FDA.

AMARYL Ė DIABETES INNOVATIVE TREATMENT

Supposing yourself to be healthy, strong-minded and energetic with an adequate nutritional diet, the concept of Diabetes and its undesirability might never bother you. Take an overall attention to statistic below then consider again whether you should be even more careful than you thought you have already been or not. Continue reading...

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Diabetes in the U.S.A. National Health and Nutrition Examination Surveyē 25.8 million People at all ages get affectedby Diabetes every year.

ē In the United States of modern healthcare system, elders affected by Diabetes took 26.9% (65 years old and over) (2010)

ē The diagnosed adultsí new cases reached 1.9 million (2010)

ē From 2005 to 2008, 20% people had pre-diabetes symptoms and 50% adults (from 20 to 65 years old) affected.

(National Institute of Diabetes and Digestive and Kidney Diseases, 2011)

Diabetes derives from various reasons depending on specific type of Diabetes. There have been 3 types Diabetes studied: Type 1 Diabetes (insulin dependent diabetes mellitus Ė IDDM) resulted by endocrine systemís decline of Pancreas in producing Insulin (β-cellís function); type 2 Diabetes (non-insulin dependent diabetes mellitus Ė NIDDM) caused by various factors (aging, obesity, unhealthy dietary, and family history or genetic factor), which take a proportion of over 90% diabetes diagnosed cases and can be affected by all ages; type 3 and others deriving form genetic origins which take a slight account of all 3 types.

Rate of new cases of type 1 and 2 diabetes among youthIs Diabetes dangerous?

Diabetes appears to be likely unharmful since diabetes patients still have full access to normal daily lifeís activities without demonstrating specific illness symptoms, causing a dangerous underestimation to Diabetes. Patients whose levels of blood glucose are high receiving no appropriate medication accompanied with healthy dietary can measurably be in risk of hazardous Diabetesís complications: cardiovascular diseases (heart failure, heart stroke, hypertension) (68% heart diseases were reported to be diabetes-related, National Institute of Diabetes and Digestive and Kidney Diseases, 2011), eye and dental-related problems, kidney diseases, non-traumatic lower-limb amputations (amputations causing by the un-healable wounds) and other various complications which may result in immune systemís erosion.

Such threatening circumstance has led to an urgency of controlling bloodís glucose levels, which conventionally and effectively performed by Insulin, a specific prescriptive therapy for type 2 Diabetes patients. This medication yet has not satisfied the scientists and Diabetes experts due to the expanding requirement for more efficacies in more rapid action time with accurate improvement and fewer side effects, which apparently was considered to be impossible, until Amaryl appeared and subsequently regarded as innovative type 1 and type 2 Diabetes patientsí rescuer.

Amaryl Ė Diabetes treatment pioneer

Amarylís molecular mechanism:

Amaryl belongs to the group of Sulfonylureas, a hypoglycemic (responsible for reducing bloodís glucose levels) chemical compound which has proved to be significantly effective for type 1 and 2 Diabetes treatment due to its direct actions on β-cellís. β-cellís Insulin secretion is an accurate circulative process, started by an increase glucose blood level bringing about subsequent biochemical reactions, see on this image below:

Amarylís molecular mechanism

Amarylís molecular mechanism

Amaryl molecular mechanism of treating Diabetes lays on its action of stimulatingPancreaticβ-cellís Insulin secretion. Amaryl closes the ATP-dependent potassium channel of β-cell (KATP) (step 2), which stimulates the whole Insulin producing process in order of: closing KATP channel (leading to a reduction of potassium efflux) β-cellís plasma membraneí depolarization  increasing Ca2+ influx by the opening of voltage sensitive Ca2+ channel  increasing Insulin secretion (G?nter M?ller, 2000). The final result of increasing Insulin Secretion presumably triggered by some Ca2+-dependent protein kinase enzymes (enzymes modifying proteins by adding phosphate group into their structures - phosphorylation) as protein kinase II Ė CaMKII, associating in regulating the Insulin granulesí activity of the Pancreatic β-cell(G?nter M?ller, 2000).

Amarylís statistic:

Research on various criteria have been made to intensively study about Amarylís efficacy and interactions to Diabetes patients, including in vitro, animal experiments and clinical surveys as well. United States and Europeís trial in 6500 Diabetes patients announced a number of 4200 patients under Glimepirideís (generic name of Amaryl) treatment controlled were remedied, in Japan, the statistic was 718/983 people treated by Glimepiride with appropriate dose varied from 0.5-8 mg/day orally (Schneider J., 1996) (Langtry H.D. and Balfour J.A, 1998). A noticeable action of Amaryl has been discovered not so long after the efficacy of stimulating the Insulin secretion of β-cell announced: Amaryl has efficiently used for NIDDM due to its parallel efficacies on increasing Insulin production of the Pancreas and decreasing the activity of Insulin-dependent blood glucose, which means decreased the sensitivity of blood glucose to Insulin efflux and subsequently improved the bodyís tolerance on fluctuant level of Insulin (50-70% NIDDM patients receiving Amaryl reported a decrease of Insulin-dependent blood glucose, compared with using Insulin Glargine only and using Glibenclamide (the second generation Diabetes drug) (G?nter M?ller, 2000). Specific surveys have been made on Diabetes patients to whom diet therapy showed no improvement stated good results of using Amaryl as a well-tolerated Insulin-mimetic after 1-year treatment (Langtry H.D. and Balfour J.A, 1998). Adverse effects of using Amaryl most commonly happen as headache, dizziness and hypoglycemia (low blood glucose level) but they rarely occur (under 2%) (Schneider J., 1996)

Conclusion

Amaryl is considered to be an effective Insulin-mimetic medication for both type 1 (IDDM) and type 2 (NIDDM) patients due to its direct actions to internal Insulin-related activities and process in safe mechanisms. Patients suffering from renal diseases, cardiovascular diseases and/or under ineffective diet therapy also report good results in using Amaryl accompanied with conventional Insulin Glargine and other clinical treatments.

REFERENCES

G?nter M?ller, The Molecular Mechanism of the Insulin-mimetic/sensitizing Activity of the Anti-diabetic Sulfonylurea Drug Amaryl, Molecular Medicine, 2000, 6(11): 907Ė933,

J. Schneider, An Overview of the Safety and Tolerance of Glimepiride, ThiemeeJournals, Hormone and Metabolic research, 1996 Sep;28(9):413-8.

Langtry H.D.; Balfour J.A., Glimepiride: A Review of its Use in the Management of Type 2 Diabetes Mellitus, Drugs, Volume 55, Number 4, April 1998, pp. 563-584(22)

U.S. Department of Health and Human Services, NATIONAL INSTITUTES OF HEALTH, National Diabetes Statistics, 2011


 

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