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Glimetal 2mg 1000mg 16 Tabs, Glimepiride, Metformin

Glimetal 2mg 1000mg 16 Tabs, Glimepiride, Metformin
Model:7501101615856
Current Reviews:0
Price:$31.00

Glimetal 2mg 1000mg 16 Tabs, Glimepiride, Metformin

INDICATIONS: Glimetal * is indicated for the treatment of type 2 diabetes mellitus associated with changes in lifestyle:

Type 2 diabetes newly diagnosed with resistance to properly track changes in lifestyle.

Type 2 diabetic, obese, overweight or normal weight, failure to diet and no tendency to ketosis.

Type 2 Diabetic on therapy with diet and sulfonylureas fault prone to weight gain .

Obese type 2 diabetic, overweight or normal weight with diet and sulfonylureas, lipid disorder secondary to diabetes.

Type 2 diabetic diet and low secondary failure to sulfonylureas or biguanides.

Diabetic type 1 ( insulin dependent) on diet and insulin, to reduce the dose of the latter, never to be replaced.

Pharmacokinetics HUMAN: Glimepiride is completely absorbed from the GI tract yielding bioavailability of 100 % and being significant from the first hour. Metformin is partly absorbed in a period of 1 to 3 hours , with bioavailability of 50 to 60% . Co-administration of both drugs with food produces important kinetic effects that are reflected in the clinic.

With Glimepiride Cmax of 352 ± 222 average ng / ml and 591 ± 232 ng / ml was obtained with a single dose of 4 or 8 mg, respectively, in a Tmax of 2.5 hours.  For multiple doses, administered for 10 days, numbers of 309 ± 134 Cmax ng / mL (4 mg) and 578 ± 265 ng / ml were reported (8 mg) in a Tmax of 2.8 hours. With metformin area under the concentration-time curve (AUC) achieved was 10.83 mcg per ml / h . After single oral administration of 1 g of metformin type 2 diabetes, peak plasma levels were 3.25 mcg / ml and dropped to less than 0.1 mcg / ml at 24 hours post-administration.

Glimepiride binds to plasma proteins in 99.5 %, whereas metformin does almost zero and as a part of it is distributed in erythrocytes.

Glimepiride is extensively metabolized by the liver, yielding 2 metabolites. Cytochrome C450 II C9 is involved with the formation of cyclohexyl hydroxymethyl derivative (active) and this is then biotransformed by cytosolic enzymes to the carboxy metabolite (inactive). Metformin is not biotransformed instead.

63% of glimepiride is excreted renally (mostly as metabolites) and the remaining with bile (also almost entirely as metabolites). Metformin is excreted unchanged in 90 % by the kidney (tubular secretion), probably a small amount is removed by saliva.

The half-life (t ½ ) of elimination of glimepiride is 5-9 hours and their cyclohexyl hydroxymethyl metabolites of carboxyl metabolite 3 hours and 5 hours. The t ½ of the plasma elimination of a single dose metformin is 1.5 to 6.2 hours, and multiple dose was increased to 19.8 hours. Moreover, the t ½ of blood clearance is 17.6 hours , which suggests that metformin is distributed by erythrocytes.

Metformin is removed effectively by hemodialysis (see Manifestations and management of overdose or accidental ingestion).

The fixed combination of these two drugs in Glimetal * provides for different mechanisms of action , the following positive effects: It increases the number of insulin receptors, which encourages a recovery in the ability of " insulin - receptor " link, which leads to a reduction of hyperinsulinemia and insulin resistance .

By action of glimepiride, the sensitivity of beta cells to glucose stimulus is increased, thus favoring the synthesis and secretion of endogenous insulin. Metformin does not act on pancreas, not increase the level of insulin, reduces gluconeogenesis and hepatic glucose production while favors better glucose utilization peripherally.

Glimepiride modifies platelet aggregation suppression pathway of arachidonic acid metabolism (that is a cyclooxygenase inhibitor but not lipoxygenase).  As thromboxane A2, an endogenous activator of platelets, is a product of this pathway, glimepiride has Annex benefit in diabetes mellitus, to reduce microvascular complications associated with hypersensitivity and increased platelet function.

Glimepiride closes potassium channels (K +) ATP -dependent beta-cell via a protein binding. The membrane is depolarized and provides the signal to the calcium channels (Ca2 +) -dependent voltage to open and allowing the inflow of calcium ions.

The increase in the intracellular calcium concentration triggered insulin secretion.

Moreover, the increase in cytosol calcium activates a second type potassium channel , the potassium channel dependent calcium (Ca2 + ) which opens and causes repolarization this promotes the closure of calcium channels, that is restart the cycle.

Although the mechanism of action of metformin is not fully clarified, increases insulin binding to its receptors and it potentiates the action at the cellular level.

The consistent and metformin direct glucose transport effect is reinforced at the level of skeletal muscle, by increasing intracellular glucose transport. As skeletal muscles are qualitatively the major users of glucose and the most sensitive of the peripheral tissues to insulin, the authors suggest that the hypoglycemic action of Metformin is mediated via increased glucose utilization by skeletal muscle.

With glimepiride administration for prolonged periods sustained declines in peripheral glucose are achieved, resulting in an improvement in the function of pancreatic beta cells and the utilization of glucose by adipose tissue, liver and muscle, which is reinforced by the action of metformin especially at the muscle tissue through the anaerobic pathway by inhibiting oxidative enzymes.

High levels of cholesterol, triglycerides and low density lipoproteins (LDL ), secondary to metabolic disorder, are reduced by action of metformin, which also increases fibrinolytic activity and decreases platelet adhesiveness and these effects contribute to reducing the risks of so frequent cardiovascular complications observed in diabetic patients.

Metformin decreases glucose absorption in the intestine, as well as stimulates the satiety center, which leads to the decrease in body weight in diabetic patients with overweight and helps keep the weight of normal weight diabetic. Coupled with these actions, reduces hypertriglyceridemia by decreasing the risk factor of atherosclerosis.

Hypersensitivity to glimepiride and / or metformin and other sulfonylureas or biguanides. Diabetic ketosis. Hypoglycemic states. Liver and / or kidney failure severe.  Intake of alcoholic beverages.  Type 1 Diabetes as a substitute for insulin.  Surgical interventions.  All those pathologies that course or cause a state of hypoxia or hypermetabolic states such as advanced age, cardiovascular, cardiopulmonary , serious infections (bacteremia, septicemia, pulmonary disease), trauma, fever, dehydration and adrenal insufficiency, or pregnancy.

Radiologic studies using IV contrast media It is recommended to discontinue the medication 48 hours prior to the radiological study and resume administration 48 hours after you've finished, to prevent lactic acidosis.

PRECAUTIONS: Save the attachment to diet, exercise and drug intake are essential to ensure the effectiveness of Glimetal * in controlling diabetes and avoid hypoglycemia boxes.

Metformin is a biguanide with lowest inducing lactic acidosis (0.24 per 10,000 patients) index and can be avoided if one has in mind the maximum dose per day and contraindications . In the presence of this table should be discontinued administration and apply corrective therapeutic measures.

Obese patients, elderly or splenic pituitary renal failure, liver or should be monitored closely to avoid hypoglycemia is presented.

If planned surgery, discontinuation of Glimetal * the day of surgery and institute insulin therapy, when the patient is able to re-employ buccal and there is no postoperative contraindication management Glimetal restarts * adjusting the dose to metabolic conditions and dietary plan. Patients with sensitive or inflamed gastroduodenal mucosa, initiating therapy with low dose and increasing it every 2 to 3 weeks , always giving the medication with food or immediately after them.

Monitor levels of vitamin B12 per year (9% of patients treated with metformin had decreased values)

RESTRICTIONS OF USE DURING PREGNANCY AND LACTATION: Use of Glimetal is contraindicated during pregnancy and lactation.

ADVERSE REACTIONS: Glimetal * is a well tolerated drug, the side effects are directly related to the dose , are transient and respond to dose reduction or stopping the medication. However, there are reports that as with other oral hypoglycemic agents, some due to hypersensitivity side effects can be severe.

Gastrointestinal reactions: These are the most frequently observed in the clinic and are nausea, vomiting, bloating, heartburn, anorexia, diarrhea , bitter or metallic taste, which is often correct to split the daily dose into two doses.

Rarely, cholestatic jaundice may occur in this case should suspend Glimetal *.

Metabolic reactions: Hypoglycemia and lactic acidosis. Selecting the patient and be aware of the contraindications, precautions, and the maximum dose in 24 hours, triggering avoid these side effects.

Lactic acidosis induced metformin is generally to avoid pre-existing risk factors (renal failure, liver disease, alcoholism, intercurrent infection or heart failure) that determine Preventing adequate tissue perfusion or reduced elimination of lactate.

Dermatological reactions: pruritus, erythema, urticaria and maculopapular lesions.

They are all so transient and small in magnitude , often disappear during therapy Glimetal * general.  In rare cases it is necessary to discontinue the drug.

Hematologic reactions: Most common are decreased platelet aggregation and increased clotting time, which in patients with cardiocirculatory disorders are desired to help to reduce cardiovascular risk.

Sporadic reports of leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, aplastic anemia and pancytopenia, mainly for its sulfonilureico component. It has been sporadically reported reduced absorption of vitamin B12 in diabetic patients treated with metformin for periods longer than 2 years, which can cause megaloblastic anemia.

Therefore, it is recommended in patients who are treated for prolonged periods determination of serum vitamin B12 and blood count.

Cardiac reactions: Insulin and sulfonylureas can cause hypoglycemia, facilitate release of catecholamines, which in turn can trigger arrhythmias and angina crisis.

DRUG INTERACTIONS AND OTHER GENDER: Drug interactions that occur with Glimetal *, are not unique to this combination, since they are shared by other sulfonylureas and biguanides.

Drugs that potentiate the hypoglycemic action: thioctic acid, nonsteroidal anti-adrenergic blockers, biguanides, bezafibrate, clofibrate, chloramphenicol, cyclophosphamide, anabolic steroids, fenfluramine, cyclophosphamide, fluconazole, phenylbutazone, fluoroquinolones, gemfibrozil, insulin, MAO inhibitors, itraconazole, ACE inhibitors, miconazole, parenteral pentoxifylline (high dose), probenecid, hypoglycemic sulfonylureas, sulfamethoxazole, sulfathiazole, sulfisoxazole, sulfadiazine, sulfonamide, sulfinpyrazone, salicylates and tetracyclines.

Medications that decrease the hypoglycemic action: Nicotinic acid ( high dose ) , acetazolamide, calcium channel inhibitors, barbiturates, steroids, clonidine, estrogen, phenothiazine and its derivatives, glucagon, progestins, thyroid hormones, isoniazid, laxatives (high dose), rifampicin, sympathomimetics, thiazides and other saluretics.

Other drug interactions: Cationic drugs compete with metformin renal tubular secretion (cimetidine, ranitidine, amiloride, digoxin, morphine, quinine, quinidine, triamterene, trimethoprim, and vancomycin ) increasing the concentration of metformin.

Inhibitors of histamine H2 can strengthen or weaken the hypoglycaemic effect.

The consumption of alcohol or drugs with sulfonilureicos biguanide can cause reaction disulfirámica regardless of which may enhance or decrease the hypoglycemic effect of them.

The effect of anticoagulants and fibrinolytics are enhanced by metformin.

Interactions Food: Food does not alter the absorption Glimetal *, so may be administered before, with or after food, for the pharmacological characteristics of Glimetal * best carried out with food or immediately after eating.

CHANGES IN RESULTS OF LABORATORY TESTS sulfonylureas such as glimepiride at the beginning of therapy may transiently elevate creatinine, alkaline phosphatase, SGOT and SGPT.

Metformin increases the coagulation time and platelet aggregation decreases.

PRECAUTIONS IN RELATION TO EFFECTS Carcinogenesis, Mutagenesis , Impairment of Fertility Studies , aimed at finding abnormalities in animals showed no effects or changes in these areas.

DOSAGE AND ADMINISTRATION: Oral.

We recommend monitoring the response through the determination of glycated hemoglobin (HbA1c), as this is a better indicator of long-term glycemic control than FPG or postprandial, it should also be noted on the patient 's behavior to follow if miss a dose (resolving never forget that increasing the dose in the next shot) as well as to the omission of one of your meals or changes in the amount of exercise you get used to perform.

* Does not substitute Glimetal lifestyle change, therefore, it must always accompany drug administration.

Glimetal * is not a substitute for insulin, but it can be associated to lower doses and / or daily applications, always coupled with a comprehensive plan for lifestyle change.

The suggested dose for initiation of therapy Glimetal * in diabetic type 2 (non- insulin dependent) is the lowest dose (1 mg of glimepiride and metformin 500 mg) and make gradual adjustments to determine the minimum effective dose with which get control of blood glucose in each patient.

Glimetal * preferably should be administered with breakfast or the first main day intake. If required 2 or more tablets a day will be split into two or three doses with food.

To set the maintenance dose adjustments increases or decreases in dose are performed every 15 days and will be based on the results of laboratory tests and tolerance.

After obtaining metabolic control, effectiveness must be evaluated with measurements of glycated hemoglobin (HbA1c) every 3 months.

Use of sulfonylurea insulin allows a reduction of up to 30% in the daily insulin dose necessary to achieve the desired glycemic.

The combination of metformin and insulin allows the best use of the latter with subsequent dose reduction up to 25%, so in the combined metformin plus sulfonylurea and insulin therapy, insulin requirements will be lower than when it is combined with either drug separately and recommended to start with lower doses of insulin (4 U less).

Type 2 diabetic with renal impairment: Reduce by 50% the normal daily dose Glimetal * and in the same proportion will increase or decrease every 15 days, prior determination of glucose and assessment of renal function.

Hepatic impairment: Since glimepiride is extensively metabolized in the liver, it is suggested in patients with mild start to the dose of ½ tablet a day and be increased carefully under strict glycemic control.  In patients with severe impairment avoided.

Geriatrics: There seems no need for a particular behavior in these patients, except for those with adverse that constrain states of hypoxia, and that metformin does not respond well to these changes, and may favor the presence of lactic acidosis.

Substitution of other oral antidiabetic: If the patient is being controlled with a sulfonylurea than chlorpropamide, suspend 24 hours and initiating therapy with Glimetal *, if chlorpropamide, suspend and wait 48 hours before giving Glimetal *.

The maximum dose per day is:

Maximum daily dose

Glimepiride 1 mg to 500 mg

6 tablets metformin

Glimepiride 2 mg to 1,000 mg

3 tablets metformin

Glimepiride 4 mg to 1,000 mg

1 ½ to 2 tablets metformin

MANIFESTATIONS AND MANAGEMENT OF OVERDOSE OR ACCIDENTAL INGESTION: Overdose causes hypoglycemia in diabetic patients and / or lactic acidosis.

Accidental ingestion by non-diabetic person, depending on the dose, can produce hypoglycemia of variable intensity is in direct proportion to the dose ingested.

Hypoglycemia is characterized by hunger, anxiety, profuse sweating, tremors, irritability, restlessness, confusional state, dizziness, palpitations, pallor, paresthesia and hyperesthesia of lips, nose, fingers, nausea, vomiting, seizures and other neurological disorders, I can reach up coma.  Confirm hypoglycemia by standard laboratory methods or test strips. In mild cases of hypoglycemia (no loss of consciousness or neurological symptoms), administered orally, if no vomiting, food or drinks rich in glucose.

In moderate to severe cases intravenously administered a glucose solution quick 50 % glucose solution followed by 5 or 10 % by continuous infusion at a rate that maintains the blood glucose level of 100 mg / ml. It requires close monitoring for 48 hours after blood levels normalized to avoid relapse.

Lactic acidosis and lactic acidosis: The condition is characterized by nausea, vomiting, abdominal discomfort, bloating, heartburn, anorexia, myalgia, lactoacidemia above 5 mmol / l and serum creatinine elevation, in which case , discontinue medication, therapy institute intensive symptomatic and close monitoring. Hemodialysis effectively removes metformin and can correct lactic acidosis induced by metformin.

The franc has clinical symptoms and warning signs and also hyperventilation , hypothermia, cardiovascular collapse , coma , decreased blood pH (7.2 or less), lactate level of 5 mmol / l or greater, creatinemia, and elevated lactate / pyruvate ratio.

Given this picture, hospitalization, discontinue the drug, establishing intensive therapy to correct the acidosis and if you have the necessary equipment to dialyze the patient.



   
   
   
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