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Glucophage, Glucophage XR Review Article

 

type 2 diabetesConsidered as the first drug of choice in the treatment of type 2 diabetes and classed in the biguanide type of medication Glucophage( Metformin) is an oral anti-diabetic drug use mostly for overweight and obese people and those with normal kidney function. Glucophage SR (slow release) or XR (extended release) was introduced in 2004, in 500 mg and 750 mg strengths, mainly to counteract the most common gastrointestinal side effects, as well as to increase patient compliance by reducing pill burden.

Used also as a treatment for polycystic ovary syndrome its efficacy on gestational diabetes has also been noted although safety concerns still hinder its widespread use in this setting. It’s also known as Glyburide (USAN) and has been investigated for other diseases where insulin resistance may be an important factor.

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According to the American Diabetes Association (ADA), approximately 20.8 million Americans have diabetes mellitus, but only two thirds have been diagnosed. This is of major concern since diabetes, if not managed properly can lead to several complications, such as retinopathy, peripheral neuropathy, kidney failure and cardiovascular problems. In fact, the ADA further stated that diabetes is the leading cause of blindness among adults; almost 82,000 leg amputations are caused by this disease; it is also a major contributor to the development end-stage renal disease; and almost 50% of diabetic patients die of heart problems.

Diabetes and Glucose

Diabetes is a metabolic disorder characterized by high blood glucose levels. This may either be due to poor insulin secretion, decreased glucose usage of the body, or there is an increased glucose production (due to glucagon activity). Decreased glucose usage may be due to increased resistance of the cells of the body to insulin, therefore glucose is not used.

There are several signs and symptoms of diabetes. Of these, polyuria (excess urination), polyphagia (excess hunger) and polydipsia (excess thirst) are the most significant indication of diabetes. Other symptoms include glucosuria, (presence of glucose in the urine), dry mouth, blurring of vision, weakness, drowsiness, weight loss and in severe cases, coma.

Laboratory analysis is done to confirm a possible diagnosis of diabetes. In particular, Blood Glucose tests and Urinalysis are the primary tests done. Urinalysis conveying glucose in the urine is an indication of the disease. As for blood glucose analysis, four tests can be done, either of which can confirm a diabetic case.

Blood Glucose Test and Values for Diabetes
Tests: Fasting Plasma Glucose
Values: >126 mg/dL

Tests: 2 Hour Postload Glucose
Values: >200 mg/dL

Tests: Random Plasma Glucose
Values: >200 mg/dL

Tests: Hemoglobin A1c
Values: 6.5%

Type 2 Diabetes Mellitus

Type 2 Diabetes or Non Insulin Dependent Diabetes Mellitus is a specific type of diabetes in which there is decreased insulin sensitivity (increased resistance of cells to insulin) combined with decreased insulin secretion. Because of this combination, the patient has excess body weight or even obese. Type 2 diabetes is the most common type of diabetes, accounting for 90% of diabetic cases. The onset of this disease is usually in adulthood, around the age of 30.

Though there are several medications for diabetes, there is no absolute cure for it. Medications used for this disease are called Oral Hypoglycemic Agents or OHAs. These drugs are aimed at lowering glucose levels, which eventually leads to the prevention or reduction of cardiovascular complications. Glucophage is an OHA recommended for patients with type 2 diabetes.

Glucophage

structural formulaGlucophage (Metformin) is a drug belonging to the class of biguanides.

Being a hypoglycemic agent, Glucophage is used for the management of diabetes. Specifically, Glucophage is used for Diabetes Type 2.

Mechanism of Action

Glucophage, belonging to the biguanide drug class, acts as an insulin sensitizer. According to the study of Hundal and colleagues (1992), they found that Glucophage increases the uptake of glucose of skeletal muscle cells or myoctes, thereby lowering blood glucose levels. This finding was supported by Galuska and colleagues (1994). Aside from that, according to the studies of Stumvoll and colleagues (1995), Schafer (1983) and Hundal and colleagues (2000), Glucophage acts by another mechanism, which is suppression of glucose production.

Recent studies have been made which proposes the exact mechanism of action of Glucophage – via activation of AMPK or AMP-activated protein kinase. AMPK is an enzyme that has several metabolic roles, the important of which are increased muscular glucose uptake (Goodyear, 2000; Fryer et al., 2002) and inhibition of hepatic glucose production by insulin-like effects (Lochhead, et al., 2000) and inhibition of fatty acid synthase (Foretz, et al., 1998). Glucophage stimulates AMPK which overall leads to a decrease in blood glucose levels.

Safety and Efficacy

Glucophage is a widely used drug for the management of Type 2 diabetes. Its importance as a mainstay treatment for diabetes has been stated by several health organization. The World Health Organization has included it as an essential antidiabetic drug; the International Diabetes Federation’ Global Guideline for type 2 Diabetes (2005) and The National Collaborating Centre for Chronic Conditions’ Type 2 Diabetes National Clinical Guideline both have stated that Glucophage is the drug of choice as the first line agent, and the drug of choice for diabetic patients who are obese. Most patients with type 2 diabetes are obese – and Glucophage is an effective drug due to the fact that it does not cause weight gain.

Several studies have been made regarding the safety and efficacy of Glucophage. Studies made by Hermann and Melander (1992), Schafer (1983) and Lucis (1983) have all proven the clinical effectiveness of Glucophage. In a study by DeFronzo and colleagues (1995), they compared Glucophage against glyburide (a sulfonylurea) and Glucophage with glyburide (combination therapy). They concluded that whether as a monotherapy or a combination therapy, Glucophage is well tolerated and with very good glycemic control. In a systematic review made by Bolen and colleagues (2007), they compared the effectiveness and safety of different OHAs available today. They concluded that though there are several new classes of drugs used for diabetes such as thiazolidinediones, α-glucosidase inhibitors and meglitinides, the older classes of drugs like biguanides (Glucophage) has superior glucose controls.

Prevention of the serious complications of diabetes is another area that should be assessed to prove the efficacy of Glucophage. In a study called United Kingdom Prospective Diabetes Study, it was found that the risk of myocardial infarction, as well as mortality associated with diabetes with the use of Glucophage was reduced by as much as 39% and 36%, respectively. A 10 year follow-up, post trial monitoring study was later done on the participants of this study. The aim in the new study made by Holman and colleagues (2008) was to determine if the improved glucose control can last upon continued use and determine any possible long term vascular effects. It was found that the risk reductions after 10 years persisted with myocardial infaction (33%) and mortality associated with diabetes (27%). These results were further strengthened by a systematic review made by Selvin and colleagues (2008). In their study, they concluded that Glucophage had the highest risk reduction among other OHAs. The results of these studies are very significant – showing that long term use of Glucophage is effective for the management of diabetes.

Sadly, Glucophage is associated with the highest risk for gastrointestinal side effects in general. However, the risk of lactic acidosis compared to other OHAs, was proven to be just the same.

Glucophage and Cancers

After years of use as an antidiabetic agent, research is now focusing on the possible use of Glucophage in the treatment and prevention of cancer. It may sound as a weird approach, since essentially it means reduction of glucose, which results to a weaker body that is fighting a very serious disease. However, it makes a big sense. In a research paper made by Martin-Castillo and colleagues, they explained that tumor cells are highly proliferating cells with high metabolism rates. Thus, inhibiting some of its metabolic functions is essential for weakening the tumor cells. A group of Russian researchers led by Dilman in the 1970s were the first to achieve a metabolic rehabilitation with the use of phenformin (another drug belonging to the biguanides). Metabolic rehabilitation was characterized by reduction of cancer relapses and multiple neoplasias.

In a study made Evans and colleagues (2005), they have proposed a concrete possible mechanism for the action of Glucophage in cancer, aside from metabolic control. Glucophage as mentioned activates AMPK. The upstream regulator of AMPK is a protein kinase LKB1 (Lizcano et al., 2004), which is a potent tumor suppressing agent (Hawley, et al., 2003). Thus, the use of Glucophage eventually leads to an increased LKB1 activity, leading to tumor suppression. Evans and colleagues have concluded that Glucophage may be use to decrease the risk of cancer in diabetic patients.

Several studies have already been made that there is indeed a risk reduction for cancer among diabetic patients who are on Glucophage therapy. Studies made by Evans et al., (2005), Bowker et al., (2006) and Landman et al., (2010) have all found that Glucophage reduces the occurrence of cancer.

Adverse Effects

Gastrointestinal intolerance, specifically lactic acidosis is the most serious side effect of the biguanides drug class. It is a rare yet often fatal complication, especially when the patient is renally impaired. Lactic acidosis is associated with daily doses of 3g; avoiding such dose reduces the chance of incurring this side effect (Sweetman, 2009).

Precautions

It is important to measure the renal function of patients taking Glucophage due to the possible risk of severe renal impairment.

Interactions

There are fewer drug interactions with biguanides such as Glucophage than sulfonylureas. Concomitant use of alcohol, as well as antiviral drugs while on Glucophage therapy may result to lactic acidosis; cimetidine may increase plasma metformin concentrations. Before undergoing examinations that require the use of iodinated contrast media, Glucophage should temporarily be stopped to avoid possible renal impairment due to the interaction of the two (Sweetman, 2009).

Dosage

According to the Global Guideline for Type 2 Diabetes, the starting dose of Glucophage is slowly titrated over the early weeks of treatment to minimize possible gastrointestinal intolerance side effect. The recommended starting dose is 500mg at breakfast for the first week, titrated slowly up to a maximum of 2g daily divided in three doses (Sweetman, 2009).

Bibliography

American Diabetes Association, 2007, Diabetes facts and figures, retrieved from
http://www.diabetes.org/diabetes-statistics.jsp

Bolen, S., Feldman, L., Vassy, J., et al., 2007, Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus

Bowker, S. L., Majumdar, S. R., Veugelers, P., and Johnson, J.A., 2006, Increased cancer-related mortality for patients with type 2 diabetes who use sulfonylureas or insulin, Diabetes Care. 29:254-258.

Clinical Guidelines Task Force, International Diabetes Federation, 2005, Global guideline for type 2 diabetes

DeFronzo, R. A., Goodman, A. M., et al., 1995, Efficacy of metformin in patients with non-insulin-dependent diabetes mellitus

Evans, J. M. M., Donnely, L. A., Emslie-Smith, A. M., Alessi, D. R., and Morris, A. D., 2005, Metformin and reduced risk of cancer in diabetic patients

Foretz, M., Carling, D., Guichard, C., Ferre, P., and Foufelle, F., 1998, AMP-activated protein kinase inhibits the glucose-activated expression of fatty acid synthase gene in rat hepatocytes, J.
Biol. Chem. 273:14767–14771

Fryer, L. G. D.,Parbu-Patel, A., and Carling, D., 2002, The anti-diabetic drugs rosiglitazone and metformin stimulate AMP-activated protein kinase through distinct signaling pathways

Goodyear, L. J., 2000, AMP-activated protein kinase: a critical signaling intermediary for exercise-stimulated glucose transport?, Exerc. Sport Sci. Rev. 28:113-116

Hawley, S. A., Boudeau, J., Reid, J. L., et al., 2003, Complexes between the LKB1 tumor suppressor, STRAD alpha/beta and MO25 alpha/beta are upstream kinases in the AMP-activated
protein kinase cascade. J Biol. 2(4):28

Hermann, L. S., and Melander, A., 1992, Biguanides: basic aspects and clinical uses, International textbook of diabetes mellitus, London: John Wiley 773-795

Holman, R. R., Paul, S. K., Bethel, M. A., Matthews, D. R., and Neil, A. W., 2008, 10-year follow-up of intensive glucose control in type 2 diabetes

Hundal, R. S., et al., 2000, Mechanism by which metformin reduces glucose production in type 2 diabetes, Diabetes. 49:2063-2069

Landman, G. W., Kleefstra, N., van Hateren, K. J., Groenier, K. H., Gans, R. O., Bilo, H. J., 2010, Metformin associated with lower cancer mortality in type 2 diabetes, (ZODIAC-16). Diabetes Care. 33:322-326.


 

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