Amaryl 4mg medicine Sanofi Treatment of diabetes (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Glimepiride
Ingredient Aventis

Ingredient

Composition information	Content
Glimepiride	4mg

Uses

indicated

Amaryl is indicated as an auxiliary therapy for diet and exercise to reduce blood sugar in patients with type 2 diabetes in adults whose diet and exercise simply cannot control hyperglycemia.

Amaryl can be used with metformin when dieting, exercising, and using Amaryl or Metformin without controlling blood sugar satisfactorily. Amaryl 4mg is also indicated to be used in combination with insulin to reduce blood sugar on patients who cannot control hyperglycemia when dieting and exercise combined with taking blood sugar drugs.

Using combination of Glimepiride and insulin can increase hypoglycemia.

Pharmacokinus

Glimepirid is a substance with oral hypoglycemic activity of the sulfonylurea group.

The drug is used in insulin -indifferent diabetes.

In both healthy people and patients with Type 2 diabetes, Glimepirid reduces blood sugar levels, mainly acting by stimulating insulin release in the pancreatic beta cells. This effect has the advantage based on the improvement of the beta cell's response for physiological glucose stimulation. When the corresponding reduction of blood glucose, the use of low doses of Glimepirid for animals and healthy people can cause release of an amount of insulin than glibenclamide. This information shows the existence of the pancreatic effects of Glimepirir (sensitive insulin and imitating insulin).

Moreover, compared to other sulfonylurea, Glimepirid has less impact on the cardiovascular system. It reduces platelet aggregation (animal and laboratory data) and leads to a significant reduction in the formation of atherosclerotic plaques (animal data).

As well as other sulfonylurea, the effect of the drug is based on an increase in the response of the pancreatic beta cells on physiological glucose stimulants. In addition, Glimepirir seems to have other obvious external effects as in other sulfonylurea.

Insulin release

sulfonylurea regulates insulin secretion by closing ATP sensitive potassium channel on beta cell membranes. Glimepidi closed potassium channel as a beta cell reduction, and by opening calcium channels, increasing the calcium flow into the cell.

That leads to insulin release through cell phenomenon.

Glimepirid is mounted at a high exchange rate with protein on beta cell membrane, this protein combined with ATP sensitive potassium channel is different from the common sulfonylurea connection position.

Glimepidi is often attached and separated from protein faster than glibenclamide. Due to this fast -exchange frequency characteristics of Glimepidi with bonding protein helps to increase the effects of glucose sensitivity and protective beta cells from non -sensitivity and early exhaustion.

Activities outside the pancreas

Pancreatic effects are an example of improving the sensitivity of peripheral tissues for insulin and reducing insulin in the liver.

The effect of increasing insulin sensitivity: Glimepirir increases the normal activity of insulin on the receipt of peripheral glucose (human and animal data).

Imitate insulin: Glimepirir mimic insulin activity on peripheral glucose collection and liver glucose production. The reception of peripheral glucose occurs by the transportation of glucose into muscle cells and fat cells through special transport proteins, located on the cell membrane. The transportation of glucose in these tissues is a limited step in using glucose. Glimepirir increases very quickly the number of molecules of glucose transportation is active on the cell membrane of muscle and fat cells, stimulating glucose collection.

Glimepidi increases the activity of specific phospholipase C with glycosyl phosphatidylinositol, which is correlated with the synthesis of lipids and glycogen synthesis caused by medication in muscle cells and removable fat. Therefore, AMP levels in cells decrease, causing a decrease in the activity of protein kinase A; This makes stimulating glucose metabolism.

Glimepidi inhibits the production of glucose in the liver by increasing the concentration of fructose-2,6 bianphosphate intracellular, in turn this substance inhibits the new sugar.

The effects on platelets and atherosclerosis formation: Glimepirir reduces plateletal collection in the laboratory and on humans. This effect may be due to the results of the selective inhibition of cyclo-oxygenase enzymes responsible for forming thromboxan A, an important endogenous platelet aggregation. Glimepirid significantly reduces the formation of atherosclerotic plaques in animals. This mechanism is being clarified.

Heart effects: Through ATP sensitive potassium channels (see above), sulfonylurea also has an impact on the heart. Compared to conventional sulfonylurea, Glimepirid also has less impact on the cardiovascular system (animal data). This can be explained the specific nature of interaction with protein associated with ATP sensitive potassium channel.

General

On healthy people, the minimum oral dose is about 0.6mg. The effect of Glimepiride depends on the dose and can be repeated. Physiological response when physical activity in time, reducing insulin secretion, still present when using Glimepid.

There is no significant difference in effect when the drug is used 30 minutes before meals or right before meals. In patients with diabetes, it is possible to achieve good metabolic control for 24 hours with a single dose of the day.

Although on a healthy person, Glimepidi's hydroxy metabolites reduce blood sugar at a slight but meaningful level, but this is only a small part of the total effect of the drug.

Treatment in combination with metformin

In one study, the Glimepidi therapy was shared with metformin to improve the metabolic control compared to the single Metformin on the patient that was not controlled satisfactorily with the maximum Metformin dose.

Treatment in combination with insulin

Data on treatment in combination with insulin is limited. On patients are not controlled satisfactorily with the maximum Glimepid doses, may start using a combination therapy with insulin. In two studies, the coordinated regimen achieved an improvement in metabolic control as the unique insulin; However, in the average dose combination of insulin is usually lower.

Clinical effects/clinical research

A clinical study with a control group (Glimepirir used up to 8mg daily or up to 2,000mg of metformin per day) for 24 weeks has been conducted on 285 children with type 2 diabetes chosen randomly (from 8 to 17 years old). Both Glimepirid and Metformin show a significant reduction in HBA1C compared to the beginning. There is no significant difference observed between the two treatment groups. Glimepirir does not prove no less than Metformin. Monitoring the Glimepirid treatment team, there are no new safety concerns that are noted in patients with type 2 children compared to adult patients. No safe and long -term data on children's patients.

Pharmacokinetics

absorption

After drinking, Glimepirir is completely absorbed. Eating does not affect the absorption, the absorption speed only decreases slightly. Maximum concentration in serum (CMAX) is achieved after taking about 2.5 hours (on average 0.3mg/ml when using 4mg doses per day) and there is a linear correlation between the dose and CMAX and score (area under the time curve/concentration).

Distribution

Glimepirid has a very small distribution (about 8.8 liters) approximately equal to the albumin distribution, highly attached to protein (> 99%), and low clearance (about 48ml/min).

In animals, Glimepirir is excreted in milk. Glimepirir passes through the placenta. The rate of drugs passing through a low blood barrier.

Biological transformation and elimination

Mainly average half -life, which is significant for serum concentration when used in multiple doses, at about 5 to 8 hours. After high doses, the half -life is slightly longer.

After taking a single dose of Glimepirid marked radioactive, 58% of radioactive activity is recovered in urine, and 35% in feces. No substances are not detected in the urine. Two metabolites - probably due to metabolism in the liver - detected in urine and feces: hydroxy derivatives and carboxy derivatives. After taking Glimepirir, the last waste sale time of these metabolites, in the order of 3 to 6 hours and 5 to 6 hours.

Comparison when taking the only dose and taking many doses of the day does not see the significant difference of pharmacokinetics, and the variation in each individual is very low. No meaningful drug accumulation.

Pharmacokinetics in men and women are similar, as well as in young patients and elderly patients (over 65 years old). In an open label study, taking a simple dose in 15 patients with renal failure, Glimepirid 3mg is used in 3 groups of patients with different levels of Creatinine (CLCR) level (Group I, CLCR = 77.7ml/min, n = 5BN), (Group II, CLCR = 27.4ml/min, N = 3BN), and (Group III, CLCR = 9.4ml/minute, CLCR/minute n = 7bn). Glimepirir is well tolerated in all 3 groups. In patients with low creatinine clearance, there is a tendency to increase the elimination of Glimepirid and the average serum concentration of Glimepidi decreases, mostly think that by a rapid Glimepiride excretion due to the cohesion of Glimepirid with low serum protein. The elimination of two metabolites through the renal decline.

Results from a multi -dose standard study conducted 16 patients with insulin -induced diabetes (type 2 diabetes) with renal failure using the dose of 1 - 8mg daily for 3 months, it shows that it is like the observation results after taking a dose daily. All patients with lower clearance of more than 22ml/minute are well controlled with a mode of only 1 mg daily. In general, the risk of accumulation does not increase in these patients.

It is unknown whether Glimepirid can be differentiated. Pharmacokinetics in 5 patients without diabetes after pipe surgery is similar to healthy people.

In animals, Glimepirir is excreted in milk.

Before taking Amaryl 4mg medicine Sanofi Treatment of diabetes (3 blisters x 10 tablets)

How to use

Should take Amaryl tablets with a sufficient amount of water (about 1/2 cup).

Dosage

amaryl is used by oral to treat insulin -dependent diabetes (tube 2 diabetes) in adults. In principle, the dose of amaryl 4mg depends on the desired blood sugar concentration. Glimepirir dose must be used enough to achieve desired metabolic control. The treatment with amaryl 4mg must be started and monitored by a doctor. Amaryl 4mg should be taken at the right time and at the right dose.

Initial dose and maintenance dose are determined based on regular glucose test results in blood and urine. The monitoring of blood glucose and urine also to detect cases of primary or secondary treatment failure.

Initial dose and dose adjustment

Initially used dose is 1mg of Amaryl 4mg once a day. If necessary, the dose may be increased. When increasing the right dose, it is based on regular hemorrhage monitoring, and should increase slowly, about 1-2 weeks away, and take step by step as follows: 1mg, 2mg, 3mg, 4mg, and in some finite cases are 8mg.

Dosage in patients with diabetes is well controlled

The common dose used in patients with diabetes well controlled is 1 to 4mg of amaryl daily. Only a few patients have to take the dose over 6mg.

Dosage distribution

The time to take the medicine and the dose distribution is decided by the doctor, taking into account the current lifestyle of the patient. Normally, only one dose of amaryl is sufficient every day.

This dose needs to be taken right before breakfast, or if not for breakfast, drink right before the first meal of the day. It is important not to skip meals after drinking amaryl.

Secondary dose adjustment

When diabetes control is improved, the sensitivity to insulin increases, so the demand for Glimepirid can decrease when continued treatment. To avoid excessive hypoglycemia (hypoglycemia), it is necessary to consider reducing the dose or stop using amaryl at the right time.

It is also necessary to consider adjusting the dose every time the patient's weight or lifestyle changes, or there are other factors that increase the causes of hypoglycemia or high blood sugar levels (hyperglycemia).

Treatment time

Treatment with amaryl is usually a long -term treatment. Change from other oral diabetes to amaryl: There is no accurate dosage correlation between amaryl and other anti -lowering drugs. When using Amaryl to replace those drugs, the initial dose should be 1mg/day, even patients who are taking oral hypoglycemic drugs with maximum doses. When increasing the dose of amaryl should follow the instructions in the "initial dose and adjust the dose" above. The activity and impact time of hypoglycemic drugs should be considered before. It may be necessary to suspend treatment to avoid force effects that can increase the risk of hypoglycemia.

Used in combination with Metformin

When it is impossible to control the blood sugar levels fully with the maximum daily dose of Amaryl or anti -diabetes drugs containing Metformin alone, can use these two drugs. In that case, the dosage used remains unchanged. Start treatment with additional drugs in low doses, depending on the desired blood sugar level, then gradually increase to the maximum daily dose. It is advisable to start coordinating treatment under tight medical supervision.

Used in combination with insulin

When the maximum daily amearl is not controlled with the daily dosage, can be used with insulin at the same time. In this case, the dose of Amaryl is currently unchanged. Start insulin treatment in low doses, then gradually increase step by step depending on the desired blood sugar level. Should start coordination treatment under tight medical supervision.

Should monitor long -term effectiveness by measuring HBA1C concentration, for example every 3-6 months.

Can use short -term amaryl in the temporary stages of loss of control on patients well controlled with diet and exercise.

Special population

kidney failure

There is little current information about using amaryl in patients with renal impairment. Patients with renal failure may be more sensitive to the hypoglycemic effect of Amaryl.

In case of impaired renal function, the Amaryl dose should be responded to a blood sugar when hungry, the initial dose is only 1mg/1 time per day. The dose may increase, if the concentration of blood glucose is still high. If the creatinine clearance coefficient is below 22ml/min, usually only use 1 mg/1 time daily, no need to increase.

What to do when overdose? Overdose with severe reactions is a case of medical emergency and forced to be treated immediately and hospitalized.

Mild hypoglycemia can usually be treated with oral carbohydrates. May need to adjust the dose, eating and physical activity. More severe attacks, convulsions or nerve damage must be treated with glucagon (intramuscularly or subcutaneous or intravenous injection, for example from 0.5 to 1mg of glucagon) or hypertonic glucose solution (intravenous, for example in adults, transmitting 40ml of 20%sugar solution). If you have to take great life -threatening doses, you need to detoxify (for example by gastrointestinal lavage, using activated carbon).

It is necessary to use prolonged carbohydrate and monitor because hypoglycemia may recur after seeming clinical recovery. The patient's blood sugar concentration should be closely monitored for at least 24 hours. In severe cases with prolonged hypoglycemia, or the risk of hypoglycemia returned, continuing to monitor blood sugar in a few days.

What to do when you forget the dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Do not use double the prescribed dose.

Side Effects

Nutrition and metabolic disorders

Hypoglycemia: As a result of the hypoglycemia of Amaryl, hypoglycemia may occur and may also last.

The possible symptoms of hypoglycemia include headache, hunger, nausea, vomiting, sluggishness, drowsiness, sleep disorders, restlessness, struggling, poor concentration, agitation and reactions, depression, confusion, hard or unable to speak, visual disorders, limb tremor, abnormalities, sensitivity disorders, self -sufficient, self -sufficient, self -reliance Shallow, slow heart rate. In addition, there may be signs of sympathetic regulation such as sweating, cold and moist skin, fear, fast heartbeat, hypertension, suspense, angina, and arrhythmia. The clinical disease of severe hypoglycemia may be like a stroke. Symptoms of hypoglycemia almost always disappear when treating hypoglycemia.

Eyes: temporary vision can be reduced, especially when starting treatment, due to changes in blood sugar levels.

Gastrointestinal tract: Sometimes gastrointestinal symptoms may occur such as nausea, vomiting, irritation or bloating in the epigastrium, abdominal pain, and diarrhea .

In a rare number of cases, the concentration of liver enzymes may increase. Some special cases may impair liver function (with bile and jaundice) and hepatitis, leading to liver failure that can progress life -threatening liver failure but can be regression if stopped using amaryl.

Blood: may occur seriously blood changes. Platelets may occur in some cases, in particular, there are cases of leukopenia, anemia hemolytic or red blood cells, granulocytes, granulocytes and full -stream anemia (due to bone marrow inhibition).

There have been recorded after circulation cases of severe platelets for less than 10,000 cells and thrombocytopenic reduction (unknown frequency).

Other undesirable effects

Sometimes allergic or allergic reactions may occur, for example in the form of rashes, urticaria or rashes (skin redness, measles rash or papules), if reaction on persistent skin should stop taking the drug. Those reactions may be mild but can also become worse and accompanied by shortness of breath, hypotension, sometimes leading to shock. If the urticaria, must immediately notify the doctor.

In special cases, there may be a decrease in serum sodium levels, blood vessels blood (allergic vasculitis) and skin hyperactive skin.

Should consult your doctor if you notice any side effects stated in this tutorial or any unwanted effects or other expected changes.

Because some adultery effects (for example, severe blood sugar, changes in blood, allergic reactions or severe allergies or liver failure) in some cases becomes life -threatening, it is necessary to immediately report to the doctor whenever sudden or severe reactions occur, and should not continue to use the drug without a doctor's instructions.

In addition to the adverse effects of Amaryl mentioned above, the following complications have been reported to the sulfonylurea:

Porphyrin metabolic disorders manifest late on the skin.

Porphyrin metabolic disorders in the liver.

Disulfiram reaction.

Inappropriate anti -diuretic hormone secretion (ADH).

suggest that these sulfonylurea may increase the peripheral reaction of ADH and/or increase ADH release.

Warnings

Contraindicated

Amaryl is not suitable for the treatment of diabetes dependent on insulin (tube 1) (for example, treating patients with diabetes with a history of acidic infection), acidosis caused by diabetes, coma or coma due to diabetes.

Do not use amaryl in patients with allergies to Glimepid, with other sulfonylurea, with other sulfamids, or with any excipients of the drug.

The experience has not been collected in the use of amaryl in patients with severe hepatic impairment and the patient is fertilized. In patients with severe renal impairment or severe liver failure, they should be changed to insulin, especially to achieve optimal metabolic control.

Be cautious when using

to achieve optimal blood sugar control, a proper diet, exercise regularly and properly, and if necessary, weight loss, is as important as regular drinking amaryl.

Clinical signs of hyperglycemia are urinating, thirsty, dry mouth and dry skin.

At the beginning of treatment, the patient must be reported in advance about the effects and risks of Amaryl and the role of combining with diet and exercise, in addition to emphasizing the importance of proper cooperation.

In the first weeks of treatment, the risk of hypoglycemia may increase and need to be monitored especially carefully. Factors that facilitate hypoglycemia include:

Patients who lack goodwill or (common in elderly patients) lack of cooperation.

Poor nutrition, erratic time or skip meals.

Imbalance between physical movement and carbohydrate collection.

Change of diet.

Drinking alcohol, especially when at the same time as to eat.

Renal failure.

Severe liver function.

Use amaryl overdose.

Some of the hormonal disorders in the endocrine system affects carbohydrate metabolism or hypoglycemia due to the regulatory mechanism, such as some thyroid dysfunction and the boundary or adrenal insufficiency).

simultaneously used with some other drugs.

Must tell the doctor about these factors and hypoglycemia, as they need to be carefully monitored. If there are risk factors for hypoglycemia, Amaryl dose should be adjusted or all therapy. Hypoglycemia symptoms reflect the body's adrenergic regulation may be lighter or not occur in the case of hypoglycemia that slowly takes place on the elderly, and in patients there are several types of neurological diseases (plant neuropathy) or on patients being treated with beta, clonidine, reserpine, guanethidine, or other sympathetic inhibitors.

Hypoglycemia can always be instantly controlled by using sugar, in the form of glucose, sugar or soft drinks with sugar. Patients should always carry at least 20g of glucose for this purpose (food or drink with artificial sweetness - like dieted foods that have no effect on hypoglycemia).

Patients may need the help of others to avoid complications. For other sulfonylurea, it is known that although the initial measures are successful, hypoglycemia may recur. Therefore, it is necessary to continue monitoring closely. In addition, heavy hypoglycemia needs to be treated immediately and monitored by a doctor, and in some cases, hospitalized.

When being treated by another doctor (for example, when admitted to the hospital after an accident, sick on holidays, the patient must notify the doctor about his diabetes and treated before).

In some limited stress situations (e.g. trauma, surgery, fever infection), blood sugar control may be more difficult, and need to be temporarily changed to insulin.

While treating with amaryl, it is necessary to regularly check the blood glucose concentration in the urine and in the urine, as well as check the ratio of hemoglobin glycosylat - usually every 3 - 6 months to more accurate assessment of long -term blood sugar control.

To avoid the risk of harming the baby, do not use amaryl during pregnancy, it is necessary to change to insulin. Patients who intend to get pregnant should notify the doctor for treatment, and change to insulin.

Glimepirir in breast milk can cause damage to breastfeeding. Therefore, breastfeeding women must not use amaryl and need to change to insulin or stop breastfeeding. The patient's ability to concentrate and react may be impaired due to lowering or hyperglycemia, or for example, due to vision loss, especially when starting or after changing treatment or when Amaryl is not taken regularly. This is a risk in situations where these possibilities are particularly important (for example, driving or operating machine).

advise patients to be cautious to avoid hypoglycemia while driving. This is especially important in patients who have decreased or not identified alarm symptoms of hypoglycemia or often have hypoglycemia. In these cases, it is necessary to consider whether patients can drive or operate the machine.

Interactive drug

Patients who use or stop taking some other drugs while being treated with amaryl may have changes in blood sugar control effects.

Glimepirir is metabolized by Cytochrome P450 249 (CYP2C9). It should be noted when Glimepirid is used simultaneously with induction substances (VD Rifampicin) or CYP2C9's inhibitors (VD fluconazol).

Based on experience with Amaryl and what is known to other sulfonylurea, must consider the following interactions:

Enhancing hypoglycemia, and so in some cases, hypoglycemia may occur when taking one of the following drugs: insulin and other anti-diabetic drugs, transferring inhibitors, allopurinol, assimilated steroids and male sex hormones, chloramphenicols, Coupharin, cyclophosphamide, diso -pide, diclophosphamide Fenfluramine, fenylamidol, fibrate, fluoxetine, guanethidine, ifosfamide, Mao inhibitors, miconazole, para-aminosalicylic acid, pentoxifylline, phenylbutazone, azapropazone, oxyphenbutazone, proobenecid, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone, quinolone Salicylate, sulfinpyrazone, sulfonamide, tetracycline, tritoquine, trofosfamide.

Reduce hypoglycemia, and thus increased blood sugar concentration when using one of the following drugs: acetazolamide, barbiturate, corticosteroid, diazoxide , diuretics, epinephrine (Adrenaline) and other sympathetic drugs, glucagon, laxative drugs (after prolonged use), nicotinic acid (high dose) (high dose) (high dose). Estrogen and progestogen, phenothiazine , phenytoin, rifampicin, thyroid hormone.

H2, clonidine and reserpine receptor antagonists can lead to enhancement or decrease in hypoglycemia.

Beta blockers reduce glucose tolerance. In patients with diabetes, this can make it difficult to control metabolism. In addition, beta blockers can increase the trend of hypoglycemia (due to decreased regulating effects).

Under the influence of sympathetic inhibitors such as beta, clonidine, guanethidine and reserpine, adrenergic regulatory signs for hypoglycemia may decrease or not occur.

Drinking alcohol or alcoholism can strengthen or weaken the hypoglycemic effects of Amaryl in an unpredictable way. The effect of cooumarin conductors may be stronger or weak.

Bile acid -mounted drugs: Coleselam binds to Glimepides and reduces Glimepidi absorption from the stomach. No observations of interactions when using Glimepirir minimum before 4 hours use Coleselam. Therefore, Glimepidi should be used before 4 hours to use Coleselam.

Storage

Store in a cool dry place, avoid light, at a temperature not exceeding 30 ° C.

Leave the medicine out of the reach of children.

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