Metformin can help improve glycemic control and ultimately prevent complications that can arise from diabetes. Not only can metformin be used to treat type 2 diabetes, but it can also be used for off-label purposes.
Those with prediabetes and a high fasting plasma glucose FPG may be recommended metformin to prevent the onset of diabetes. Metformin is recommended when blood sugar levels are not managed with diet and exercise alone.
Metformin can also be used as an off-label option to treat gestational diabetes mellitus. This type of diabetes occurs in pregnant women who are predisposed to having diabetes.
However, insulin is usually tried first. Metformin has also been studied to treat polycystic ovary syndrome POCS. This syndrome is characterized by an imbalance of sex hormones which can result in ovarian cysts, menstrual cycle changes, pregnancy issues, acne, and insulin resistance.
Metformin can be prescribed to help decrease insulin resistance, decrease testosterone levels, and improve menstrual cycles as well as fertility. The use of antipsychotic medications, such as olanzapine , risperidone , and clozapine , can lead to weight gain. According to some studies, Metformin has been shown to be effective for treating antipsychotic-induced weight gain.
One review found that metformin helped reduce body mass index BMI , body weight, and insulin resistance compared to placebo in those with antipsychotic-induced weight gain. Based on studies comparing metformin and metformin ER for type 2 diabetes mellitus, metformin ER has been found to be comparable to metformin in effectiveness.
In fact, metformin ER may be superior to regular metformin based on its lower side-effects profile and ease of use. Those with type 2 diabetes mellitus may be more inclined to take a once-daily metformin pill instead of a twice-daily pill. In one randomized, clinical study , metformin ER was found to be more effective than metformin IR when treating patients with type 2 diabetes. Those taking metformin ER experienced better glycemic control and lipid metabolism compared to metformin IR.
Another randomized, double-blind trial found that once-daily metformin ER had similar efficacy and safety to regular metformin. Additionally, the study noted an advantage of once-daily dosing with metformin ER.
Both metformin and metformin ER improved HbA1c levels over 24 weeks in subjects who had never tried any other treatment for their diabetes. Extended-release metformin may be preferred over immediate-release metformin. It has been shown to have better tolerability although it may be more expensive than immediate-release tablets. Metformin is the generic version of Glucophage. Generic metformin is covered by Medicare part D and most insurance plans.
This cost can be reduced by bringing a SingleCare discount card to the pharmacy. Almost all Medicare and insurance plans will cover generic metformin ER. Even with insurance, SingleCare may be able to offer a lower price. Check with your pharmacy to see if you can take advantage of a better discount with SingleCare. Get the SingleCare prescription discount card.
Metformin causes side effects that affect the gastrointestinal GI system. These side effects include diarrhea, nausea, vomiting, gas flatulence , indigestion, and abdominal discomfort or stomach upset. Metformin IR also commonly causes fatigue or lack of energy asthenia as well as headaches. Metformin ER has fewer side effects compared to metformin. The most common side effects associated with metformin ER are diarrhea, nausea, and vomiting.
Metformin ER can also cause constipation in some people. Although metformin ER can cause other GI side effects such as indigestion and flatulence, these side effects do not occur as often compared to regular metformin. Other side effects that can occur with metformin and metformin ER include dizziness, lightheadedness, and taste disturbances.
Use of metformin in patients with hepatic impairment has been associated with some cases of lactic acidosis. Overdose of metformin HCl has occurred, including ingestion of amounts greater than 50 grams. Therefore, hemodialysis may be useful for removal of accumulated drug from patients in whom metformin overdosage is suspected. The chemical name of metformin hydrochloride is N,N-dimethylimidodicarbonimidic diamide hydrochloride.
The structural formula is as shown:. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin is Each mg tablet contains coloring, hypromellose, magnesium stearate, microcrystalline cellulose and polyethylene oxide.
Each 1, mg tablet contains colloidal silicon dioxide, polyvinyl alcohol, crospovidone, glyceryl behenate, polyacrylate dispersion, hypromellose, talc, polyethylene glycol, eudragit, titanium dioxide, simethicone emulsion, polysorbate and coloring. Metformin is a biguanide that improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose.
Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may decrease. Following a single oral dose of 1, mg 2x mg tablets GLUMETZA after a meal, the time to reach maximum plasma metformin concentration Tmax is achieved at approximately hours.
Both meals prolonged metformin T max by approximately 3 hours but C max was not affected. In a two-way, single-dose, crossover study in healthy volunteers, the 1, mg tablet was found to be similar to two mg tablets under fed conditions based on equivalent C max and AUCs for the two formulations. Metformin is negligibly bound to plasma proteins. Metformin partitions into erythrocytes, most likely as a function of time. Intravenous, single-dose studies in healthy subjects demonstrate that metformin is excreted unchanged in the urine and does not undergo hepatic metabolism no metabolites have been identified in humans , nor biliary excretion.
Renal clearance is approximately 3. In blood, the elimination half-life is approximately From these data, it appears that the change in metformin pharmacokinetics with aging is primarily accounted for by a change in renal function. In controlled clinical studies in patients with type 2 diabetes, the antihyperglycemic effect of.
The gender differences for Cmax are unlikely to be clinically important. The differences between the Asian and Caucasian groups are unlikely to be clinically important. However, such studies have been performed on metformin HCl tablets. Cationic drugs that are eliminated by renal tubular secretion may increase the accumulation of. Carbonic anhydrase inhibitors may cause metabolic acidosis: [see Warnings and Precautions 5. These doses are approximately 2, 4, and 8 times in males, and 3, 7, 12, and 16 times in females of the maximum recommended human daily dose of 2, mg based on body surface area comparisons.
No evidence of carcinogenicity with metformin was found in either male or female rats. A carcinogenicity study was also performed in Tg. AC transgenic mice at doses up to 2, mg applied dermally.
No evidence of carcinogenicity was observed in male or female mice. Genotoxicity assessments in the Ames test, gene mutation test mouse lymphoma cells , chromosomal aberrations test human lymphocytes and in vivo mouse micronucleus tests were negative. Patients who were enrolled on monotherapy or combination antidiabetic therapy underwent a 6-week washout. Patients randomized to immediate-release metformin initiated mg twice daily for 1 week followed by mg with breakfast and 1, mg with dinner for the second week.
The 3-week treatment period was followed by an additional week period at the randomized dose. The results are presented in Table 5. Mean baseline body weight was Mean change in body weight from baseline to week 24 was Use of insulin and oral hypoglycemic agents other than the study drugs were prohibited. The results are presented in Table 6. Mean change in body weight from baseline to week 24 was 0.
Explain the risks of lactic acidosis, its symptoms, and conditions that predispose to its development. Advise patients to discontinue GLUMETZA immediately and to promptly notify their healthcare provider if unexplained hyperventilation, myalgias, malaise, unusual somnolence or other nonspecific symptoms occur.
Instruct patients to inform their doctor that they are taking GLUMETZA prior to any surgical or radiological procedure, as temporary discontinuation may be required [see Warnings and Precautions 5. Explain to patients receiving concomitant therapy the risks of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development [see Warnings and Precautions 5. Inform patients that GLUMETZA must be swallowed whole and not crushed, cut, or chewed, and that the inactive ingredients may occasionally be eliminated in the feces as a soft mass that may resemble the original tablet.
Manufactured by: Bausch Health Companies Inc. Patent Numbers: 6,,; 6,,; 7,, and 8,, Glumetza is a trademark of Salix Pharmaceuticals, Inc.
Lactic acidosis. Metformin hydrochloride, the medicine in GLUMETZA, can cause a rare, but serious side effect called lactic acidosis a buildup of lactic acid in the blood that can cause death. Lactic acidosis is a medical emergency and must be treated in the hospital. Your doctor may need to stop.
Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. Know the medicines you take. Keep a list of them to show your doctor and pharmacist. In May , Depomed licensed manufacturing and marketing rights for its proprietary formulation of metformin extended release mg dose to Biovail Corporation for the US including Puerto Rico and Canada.
Under the terms of the agreement, Biovail will pay DepoMed a 25 million dollars milestone fee upon approval of the mg dosage and also customary royalties on the net sales in the US and Canada. Biovail also agreed to acquire approximately 2. Biovail has subsequently developed a mg dose of metformin extended release [metformin XR] using its proprietary Smartcoat delivery technology allowing a graduated release of the active drug from the tablet.
In April , Depomed and Biovail amended their original license agreement of May Under the terms of the amended agreement, Depomed will receive royalties on sales of Biovail's mg tablet in the US and Canada. In turn, Biovail acquired access to Depomed's clinical data for the metformin mg tablet that will be used to accelerate regulatory filings for Biovail's mg tablet and establish equivalence between the two dosages.
Biovail is seeking marketing partners for metformin extended release Glumetza in the US. The company anticipates signing an agreement for the US during the second half of Depomed has an agreement with LG Life Sciences for the commercialisation and distribution of metformin extended release in Korea.
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