Amaryl 2mg 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	2mg

Uses

Indications

Amaryl 2 mg is indicated as an auxiliary therapy for dieting and exercise to reduce blood sugar in patients with type 2 diabetes in adults where diet and exercise can not control hyperglycemia.

Amaryl can be used with Metformin when dieting, exercise, and using Amaryl or Metformin without controlling blood sugar satisfactorily.

Amaryl is also indicated in combination with insulin to reduce blood sugar on patients who cannot control hyperglycemia when dieting and exercise in combination with taking blood sugar oral medications. Using combination of Glimepid and insulin can increase hypoglycemia.

Pharmacokological

Glimepirid is a substance with oral hypoglycemic activity of the sulfonylurea group. The drug is used in insulin -induced diabetes.

In both healthy people and patients with TIP 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 pancreatic beta cell's response for physiological glucose stimulation.

When the corresponding reduction of blood glucose, the use of low doses of Glimepirie for animals and healthy people can cause release of an amount of insulin less 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, Glimepidi seems to have other distinct pancreatic effects as in other sulfonylurea.
Insulin release

sulfonylurea regulates insulin secretion by closing ATP sensitive potassium channel on beta cell membranes. Glimepidi closes 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 the insulin: Glimepirir mimicing insulin activity on peripheral glucose and glucose production in the liver.

The receipt 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.

Glimepidi increases very quickly the number of glucose transport molecules that are active on the cellular 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 IIPID and glycogen synthesis caused in muscle cells and detergent fat. Therefore, AMP levels in cells decrease, causing a decrease in the activity of protein kinase A; This makes stimulating glucose metabolism.

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

The effects on platelets and atherosclerosis formation:

Glimepidi reduces platelet aggregation 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. Glimepidi significantly reduces the formation of atherosclerotic plaques in animals.

Heart impact:

Through ATP sensitive potassium channels (see above), sulfonylurea also has an impact on the heart.

Outline

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

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 Glimepirid therapy is used with metformin to improve the metabolic control compared to the single Metformin used in the patient that is not controlled adequately 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 coordination regimen achieved an improvement in metabolic control as using alone 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 8 mg daily or up to 2000 mg of metformin per day) for 24 weeks has been conducted on 285 children with tip 2 diabetes randomly selected (from 8 to 17 years old). Both Glimepirid and Mefformin show a significant reduction in HBA1C compared to the beginning. There is no significant difference observed between the two treatment groups.

Glimepidi does not prove no less than Metformin. Following the Glimepider treatment team, there are no new safety concerns that are noted in patients with 2 children's diabetes compared to adult patients. No safe and long -term data on children's patients.

Dynamic pharmacokinetics

Absorption: After oral, Glimepirir is completely absorbed. Eating does not affect the absorption, the absorption speed only decreases slightly. The maximum concentration of serum (CMAX) is achieved after drinking about 2.5 hours (average 0.3 µg/ml when using 4 mg doses daily) and there is a linear correlation between the dose and CMAX and AUC (the area below the time curve/concentration).

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

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

Biological transformation and elimination: The main semi -cancellation time is mainly, which is meaningful to serum concentration when used in 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 Glimepirid, the final waste 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. There is no meaningful cure.

Mobile 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, Glimepid 3 mg is used in 3 groups of patients with different levels of creatinine (CLCR) (Clcr) (Group I, CLCR = 77.7 ml/min, n = 5 patients), (Group II, CLCR = 27.4 ml/min, N = 3 patients), and (Group III, CLCR = 9.4 ML/N/NO = BN). Glimepirir is well tolerated in all 3 groups.

In patients with low creatinine clearance, there is a tendency to increase Glimepid elimination and the average serum concentration of Glimepidi decreases, mostly think that by a fast Glimepid excretion due to the mound of Glimepirid with low serum protein. The elimination of two metabolites through the kidneys decreases.

Results from a multi -dose standard study conducted 16 patients with insulin -independent diabetes (TIP 2) with kidney failure using the dose of 1 - 8 mg daily for 3 months, showing the same result after taking a daily dose per day.

All patients with clearance of less than 22 ml/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 molasses surgery similar to healthy people.

Animals, Glimepirid are excreted in milk.

Before taking Amaryl 2mg medicine Sanofi treatment of diabetes (3 blisters x 10 tablets)

How to use

amaryl 2 mg oral drug. Amaryl tablets should be taken with a sufficient amount of water (about ½ cup).

Dosage

Amaryl is used by oral to treat insulin -dependent diabetes (type 2 diabetes) in adults.

In principle, the dose of amaryl depends on the desired blood sugar concentration. Glimepirir dose must be used enough to achieve desired metabolic control. The treatment with Amaryl must be started and monitored by a doctor.

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

Initial dose and dose adjustment:

The initial dose is usually 1 mg of amaryl once a day. When increasing the right dose, it is based on regular hemorrhage monitoring, and should be increased slowly, which is about 1-2 weeks away, and step by step as follows: 1 mg - 2 mg - 3 mg - 4 mg, and in some finite cases is 8 mg.

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

Dosage distribution: The time of taking the drug 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 eaten breakfast, drink right before the first meal of the day. It is important not to skip meals after taking Amaryl.

Secondary dose adjustment: When diabetes control is improved, the sensitivity to insulin increases; Therefore, the demand for Glimepirid can decrease when continuing treatment. To avoid excessive hypoglycemia (hypoglycemia), it is necessary to consider reducing the dose or stopping 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: Amaryl treatment is usually a long -term treatment.

Change from other oral diabetes to amaryl:

There is no accurate dosage correlation between Amaryl and other anti -hypoglycemic drugs.

Should consider the activity and impact time of hypoglycemic drugs used earlier. It may be necessary to suspend treatment to avoid force effects that can increase the risk of hypoglycemia.

Use 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 for lone, can share these two drugs. Start treatment with additional drugs with low doses, depending on the desired blood sugar level, then gradually increase until the maximum daily dose.

Used in combination with insulin:

When it is impossible to control adequate blood sugar with the maximum daily dosage of Amaryl, can be used with insulin. Start insulin treatment in low doses, then gradually increase step by step according to the desired blood sugar level.

Should monitor long -term effectiveness by measuring HBA1C concentration, for example every 3-8 months.

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

Patients with renal failure:

There is little current information about using amaryl in patients with renal failure.

Patients with renal failure may be more sensitive to the hypoglycemic effect of Amaryl.

In case of impaired renal function, the dosage of Amaryl should respond to the blood sugar when hungry, the initial dose is only 1 mg/time per day.

The dose may increase, if the concentration of blood glucose is still high. If the creatinine clearance coefficient is below 22 ml/min, usually only 1 mg/1 time per day, no need to increase.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

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.

Sites with coma, convulsions or nervous damage must be treated with glucagon (intramuscularly or subcutaneous or intravenous injection, for example from 0.5 to 1 mg of glucagon) or superior glucose solution (venous, for example in adults, 40 ml of 20%sugar solution). If you take the big doses of life -threatening, detoxifying (for example by gastrointestinal lavage, using activated carbon).

It is necessary to use prolonged carbohydrates and monitor because hypoglycemia may recur after seeming clinical recovery.

Patient blood sugar concentration should be closely monitored for at least 24 hours. In severe cases with prolonged hypoglycemia, or the risk of slipping back into hypoglycemia, blood sugar monitoring may last for a few days.

What to do when forgetting a dose? If you forget to take the medicine, do not arbitrarily increase the dose then to compensate.

Measures to deal with such negligence (especially when forgetting to take medicine or skip meals) or in case of not being able to use the drug on time prescribed, it is necessary to be discussed in front of the doctor and the patient. Doctors need to be notified immediately if taken too high dose, or excess a dose.

Side Effects

When using 2 mg amaryl, you may experience unwanted effects (ADR).

Based on experience with Amaryl and what is known to other sulfonylurea, must consider the following adverse 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, streaming, poor concentration, agitation and reaction, depression, confusion, hard or unable to speak, visual disorders, limb tremor, abnormalities, sensory disorders, self -sufficient, self -sufficient, self -consciousness Agriculture, slow heart rate.

In addition, there may be signs of sympathetic regulation such as sweating, cold and moist skin, fear, fast heartbeat, hypertension, nervousness, angina, and arrhythmia. The clinical disease of severe hypoglycemia may be like a mutant. 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: Occasionally gastrointestinal symptoms such as nausea, vomiting, irritation or bloating in the epigastrium, abdominal pain, and diarrhea. In rare cases, the concentration of liver enzymes may increase. Some special cases may impair liver function (with cholestasis and jaundice) and hepatitis, leading to liver failure may progress life -threatening liver failure but may be regressed if they stop using amaryl.

Blood: may occur seriously blood changes. Platelets may occur in a rare number of cases, in particular, there are cases of leukopenia, hemolytic anemia or red blood cells, granulocytes, losy of leukocytes and anemia of the whole stream (due to bone marrow inhibition). It has been recorded after the circulation of cases of severe platelets reducing the number of platelets less than 100,000 cells/µl and the platelet hemorrhage board (unknown frequency).

Other undesirable effects: Sometimes allergic or allergic reactions may occur, for example in the form of itching, urticaria or rash (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, sodium concentration may occur in serum, vascular inflammation (allergic vasculitis) and skin hyperactive to sunlight. The doctor should be consulted 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 hypoglycemia, blood change, allergic reactions or severe allergies or liver failure) in some cases become life -threatening, it is necessary to immediately report to the doctor whenever sudden or severe reactions occur, and should not continue to use drugs without a doctor's guidance.

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

Porphyrin metabolic disorders are late on the skin; There are suggestions that these sulfonylurea may increase the peripheral reaction of ADH and/or increase ADH release.

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Amaryl 2mg drug is contraindicated in the following cases:

Amaryl is not suitable for the treatment of diabetes dependent on insulin (type 1) (e.g. treatment of diabetes patients with a history of keton acidosis), keton acidosis caused by diabetes, coma or diabetes due to diabetes. Do not use amaryl in patients with allergies to Glimepid, with other sulfonylurea, with other sulfamide, or with any excipients of the drug.

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

Caution when using

to achieve optimal blood sugar control, a proper diet, regular and proper exercise, and if necessary, weight loss, is as important as regular drinking amaryl. The clinical signs of hyperglycemia are urinating, thirsty, dry mouth and dry skin.

When starting to treat, the patient must be notified of the effects and risks of Amaryl and the role of combining with diet and exercise; In addition, it must emphasize the importance of appropriate 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;

Change the diet;

renal function;

severe liver failure;

Use amaryl overdose.

Some of the hormonal disorders affect carbohydrate metabolism or hypoglycemia due to the regulatory mechanism (for example, some thyroid dysfunction and the front of the yen or adrenal insufficiency).

Also used with some other drugs (see "interaction").

Must tell the doctor about those factors and hypoglycemia, because they need to be monitored carefully.

If there are risk factors for hypoglycemia, the amaryl dose should be adjusted or all therapy. This is also applied every time you get sick during treatment or the patient's lifestyle changes.

Symptoms of hypoglycemia reflect the body's adrenergic regulation (see "undesirable effects") may be lighter or not occur in the case of hypoglycemia that takes place slowly above the elderly, and in patients there are some types of neurological diseases (plant neuropathy) or on patients being treated with beta, clonidine, reserpine, guanethidine, or other sympathetic drugs.

Hypoglycemia almost always can be instantly controlled by using sugar, in the form of glucose, sugar or soft drinks with sugar. Patients should always bring at least 20 g of glucose for this purpose (food or drink with artificial sweetness (such as dietary 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 an accident after an accident, sick on holidays), the patient must notify the doctor about his diabetes and the previous treatment.

In some limited stress situations (for example trauma, surgery, bacterial 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.

The ability to drive and operate machinery

The patient's concentration and reaction ability may decrease 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 the 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.

Pregnancy

To avoid the risk of harming babies, 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.

Breastfeeding period

Glimepidi in breast milk can cause damage to breastfeeding. Therefore, women breastfeeding are not used amaryl and need to switch to insulin or stop breastfeeding.

Medicinal interaction

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

Giimepirid is metabolized by CYLOCHROME P450 2C9 (CYP2C9). It should be noted when Glìimepirid is simultaneously used with induction substances (such as rifampicin) or inhibitors (such as fluconazol) of CYP2C9.

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

Enhancing hypoglycemia: In some cases, hypoglycemia may occur when taking one of the following drugs: insulin and other anti-diabetic drugs, enzyme inhibitors, allopurinol, steroids and male sex hormones, chloramphenicols, coumarin conductors, cyclophosphamide, diSo-Pipluramine, fenfluramine, fenfluramine, fenfluramine, fenfluramine, fenfluramine Fenylamidol, fibrate, fluoxetine, guanethidine, ifosfamide, Mao inhibitors, miconazole, para-aminosalicylic acid, pentoxifylline (high-dose injection), phenylbutazone, azapropazone, Oxyphenbutazone, Probenecid, Quinolone, Salicylate, Salicylate, Sal blackecid Sulfinpyrazone, sulfonamide, Tetracycline, Tritoquine, Trofosfamide.

Reducing hypoglycemia: There may be an increase in blood sugar levels when taking one of the drugs such as acetazolamide, barbiturate, corticosteroid, diazoxide, diuretics, epinephrine (adrenaline) and other sympathetic drugs, glucagon, laxative drugs (after prolonged use), Nicotinic acid (high dose), estrogen and progestrogens, progestrogen Phenothiazine, phenytoin, rifampicin, thyroid hormone.

H2, clonidine and reserpine receptor resistant drugs can lead to increased or lower hypoglycemic effects.

Beta blockers reduce glucose tolerance. In patients with diabetes, this can make it difficult to control metabolism. In addition, the chena drug 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 regulating 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 effects of cooumarin derivatives 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 no more than 30 ° C. Leave the medicine out of the reach of children.

Expiry date: 36 months from the date of manufacture. Do not use overdue drugs stated on the packaging.

Manufacturer: PT Aventis Pharma.

Other drugs

Disclaimer

Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.