Meyersiliptin 50 meyer - BPC supports diet, blood sugar control (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Sitagliptin

Ingredient

Composition information	Content
Sitagliptin	50mg

Uses

indicated

Meyersiliptin is used in the following cases:

Use as a supportive therapy for diet and physical exercise to improve blood sugar control in patients with type 2 diabetes.

Meyersiliptin belongs to a group of hypoglycemic drugs, called DapeIlidyl peptidase 4 (DPP-4) inhibitors that improve blood sugar in patients with type 2 diabetes by increasing the concentration of active invoretin hormones. Incretin hormones include glugacon-like peptid-1 (GLP-1) and Glucose-Dependent insulinotropic polypeptide (GIP), released from the intestine throughout the day, and increase the concentration of meals. These invoretin hormones are components of the endogenous system participating in physiological regulating the state of HELVIEP Glucose.

When the blood glucose levels in the blood are normal or high, GLP-1 and GIP increase the synthesis and release of insulin from the pancreatic beta cells through intracellular signal transmission links to the loop. It has been proven that the treatment with GLP-1 or DPP-4 inhibitors on animals tested with type 2 diabetes have improved the response of beta cells for glucose, stimulates synthesis and releases insulin. The absorption and use of glucose at tissue increases when higher insulin levels.

In addition, GLP-1 reduces glucagon secretion from pancreatic alpha cells. The decrease in glucagon concentration with higher blood insulin levels leads to reduced glucose production in the liver, leading to a decrease in blood glucose levels. These effects of GLP-1 and GIP depend on glucose, so when the blood glucose levels are low, the stimulation of insulin release increases. Moreover, GLP-1 does not impair the normal response of Glucagon for low blood sugar condition.

The activity of GLP-1 and GIP is limited by the DPP-4 enzyme, this enzyme quickly hydrolyses the hormones into non-active substances. Sitagliptin prevents DPP-4 hydrolyzed hormones, thus increasing the concentration of active forms of GLP-1 and Gip in plasma. By increasing the concentration of active insectin hormones, sitagliptin increases insulin release and reduces glucagon levels in a way that depends on glucose.

In patients with type 2 diabetes with hyperglycemia, changes in insulin and glucagon concentration leads to a decrease in A1C hemoglobin levels (HBA1C) and glucose concentration at hunger and after eating. The mechanism depends on this glucose of sitagliptin different from the mechanism of action of hypoglycemia sulfamids; Hypotension sulfamides increase insulin secretion even when glucose concentration is low and can lead to hypoglycemia in patients with type 2 diabetes and in normal objects.

Sitagliptin is a strong, selective inhibitor on the DPP-4 enzyme and does not inhibit related enzymes near DPP-8 or DPP-9 at treatment concentrations.

Pharmacokinetics

absorption

In healthy subjects taking 1 dose of 100mg, Sitagliptin is quickly absorbed to reach the peak concentration in plasma (TMAX) after 1-4 hours after taking the drug. The AUC of Sitagliptin in plasma increases, corresponding to the dose, in a healthy volunteer when taking a single dose of 100mg, the average AUC of Sitagliptin in plasma is 8.52 MCM/hour, CMAX is 950 nm, absolute bioavailability of sitagliptin is about 87%. Due to taking medicine during a high -fat meal that does not affect the impact on the pharmacokinetics of sitagliptin used at the same time, it is possible to use the Sitagliptin with or not with food.

Distribution

The average distribution volume is in a sustainable state after taking a single dose of Sitagliptin 100mg of intravenous lines in healthy objects approximately 198 liters. Sitagliptin ratio is inversely connected to plasma proteins (38%).

Metabolism

Sitagliptin is excreted mainly in urine in the form of unchanged and a small part in the form of metabolic. About 79% Sitagliptin is discharged in urine in the form of unchanged.

After taking 1 dose of sitagliptin marked [MC], about 16% of radioactive substances are the metabolites of sitagliptin. These six metabolites are detected at mark concentration and are thought to be unrelated to the plasma inhibition activity of sitagliptin. In vitro studies have shown the enzyme mainly responsible for the limited metabolism of sitagliptin is CYP3A4, with the contribution of CYP2C8.

In vitro research data shows that the sitagliptin is not an isoenzym inhibitor CYP CYP3A4, 2C8, 2C9, 2D6, 1A2, 2C19 or 2B6, and is not the touch substance of CYP3A4 and CYP1A2.

Elimination

After healthy subjects take 1 dose of sitagliptin [14C], about 100%of radioactive substances are discharged in feces (13%) or urine (87%) within 1 week of taking the drug. The sale time is measured after taking 1 dose of Sitagliptin 100mg, approximately 12.4 hours and the renal clearance is about 350 ml/min.

Sitagliptin is excreted mainly through the kidney with the active excretion through the renal tubules. Sitagliptin is a substrate for Human Organic Anion Transporter-3: Human Organic Anion-3: Active 3), which is a substance that can be involved in the elimination of the kidney sitagliptin, has not yet determined the clinical relevance of activated-3 in the transport of sitagliptin. Sitagliptin is also the substrate of p-glycoprotein, which can also participate in the elimination of sitagliptin through the kidney. However, cyclosporine, a p-glycoprotein inhibitor does not reduce the sitagliptin clearance.

The characteristics in patients

Sitagliptin pharmacokinetics are generally similar in healthy subjects and in patients with type 2 diabetes.

kidney failure

Patients with mild renal impairment do not increase plasma sitagliptin levels of clinical significance compared to healthy objects. The AUC of plasma sitagliptin has increased by about 2 times in medium renal impairment patients, and increased by about 4 times in patients with severe renal impairment and in end -stage patients who are being hemoglobin, when compared to healthy and normal subjects.

Sitagliptin is eliminated moderately through hemolysis (13.5% after 3-4 hours of hemolysis, starting the fertilizer after taking the drug for 4 hours). To achieve sitagliptin concentration in plasma similar to patients with normal renal function, should take lower doses in patients with average and severe renal impairment, as well as in patients with the final stage of kidney disease, bloody diseases need hemolysis.

Hepatic failure

No dose adjustment in patients with mild and medium liver failure (Child-Pough score 9). However, because sitagliptin is mainly eliminated through the kidneys, it is predicted that the severe liver failure does not work on the pharmacokinetics of the sitagliptin.

Elderly

No need to adjust the dose by age. Age does not cause clinical significance to the pharmacokinetics of sitagliptin based on a pharmacokinetic analysis according to population from phase I and phase II data. The elderly (65-80 years old) has a 19% higher level of plasma sitagliptin levels than young people.

Children

There is no study of sitagliptin conducted in children.

Other patient characteristics

No need to adjust the dose by gender, race or body block (BMI). These characteristics do not cause clinical significance to the pharmacokinetics of Sitagliptin based on a synthetic analysis from pharmacokinetic data phase I and according to a population pharmacokinetic analysis from phase I and phase II.

Before taking Meyersiliptin 50 meyer - BPC supports diet, blood sugar control (3 blisters x 10 tablets)

How to use

Meyersiliptin 50 Used orally, can be taken or not with food.

Dosage

Sitagliptin dose recommends 100mg, once a day when used for monomers or combined with metformin, hypoglycemia, PPARIton (such as thiazolidinediones), or Metformin and sulfamid hypoglycemia or can use Metformin and PPARI (hungry or full abdominal division).

When using Meyersiliptin 50 combined with hypoglycemia sulfamid, it is possible to consider using lower -dose hypoglycemia sulfamid to reduce the risk of hypoglycemia due to hypoglycemia sulfamid.

Dosage on special subjects:

Patients with liver failure

No need to adjust the dose for patients with mild to moderate liver failure. Safety and effectiveness of drugs in patients with severe liver failure.

Patients with renal failure

For patients with mild renal impairment (creatinine clearance coefficient [CICR]> 50 ml/min, almost equivalent to serum creatinine

For patients with medium renal impairment (ClCr> 30 to 1.7 to 1.5 to

For patients with severe renal impairment (CLCR 3.0 mg/dl in men and> 2.5 mg/dl in women), or have end -stage kidney disease that requires hemolysis or peritoneal fertilizer: Sitagliptin dose is 25 mg once a day. Sitagliptin can be used at any time, not related to the time of hemolysis.

Elderly

No need to adjust the dose, need to be cautious when choosing the dose because the kidney function can decrease.

Children

Not yet determined the safety and effectiveness of sitagliptin in children and adolescents under 18 years old.

Because there is a dose correction based on kidney function, it is recommended that kidney function should be assessed before the beginning of the treatment and then periodically check.

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

In a study of the dose of 800mg Sitagliptin. The QTC range increased very little and unrelated to clinical.

Inexperienced use of doses higher than 800 mg in humans. In phase I studies on dosage doses in the day, clinical adverse adverse reactions are found related to the dose when using sitagliptin to the dose of 600 mg/day for 10 days and 400 mg/day to 28 days.

Handling

In case of overdose, the common supportive measures should be applied, such as removing substances that have not been absorbed from the digestive tract, clinically monitoring (including electrocardiogram), and supportive treatment, if necessary.

Sitagliptin can be moderately separated. In clinical research, about 13.5% of the dose is removed after 3-4 hours of hemolysis. It is possible to consider the prolonged blood decomposition if it is clinically suitable, it is still unknown whether the peritoneal can be able to separate the sitagliptin or not.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

Serious reactions include pancreatitis and sensitive reaction that has been reported. Lowering blood glucose has been reported when coordinated with Suifonlure (4.7% - 13.8%) and insulin (9.6%).

Common, 1/100

Metabolism and nutrition: Hypoglycemia.

Nervous system: headache.

Nervous system: Dizziness.

The immune system: Sensitive reactions like anaphylaxis. Improving kidney function, acute renal failure.

Warnings

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

contraindicated

Meyersiliptin is contraindicated in the following cases:

Hypersensitivity to sitagliptin or any other ingredient of the drug.

Be cautious when using

general: Sitagliptin should not be used in patients with type 1 diabetes or to treat diabetes infected with ceton - acid.

Acute pancreatitis has been reported on the user of Sitagliptin in combination with metformin. When taking drugs for people with a history of pancreatitis, caution and closely monitoring. Must monitor the manifestations of pancreatitis such as nausea, vomiting, anorexia, severe severe abdominal pain. If suspected pancreatitis must stop using sitagliptin. Pancreatitis usually occurs within the first 30 days of treatment.

Used in patients with renal failure: Sitagliptin is eliminated through the kidneys. In order to achieve the plasma sitagliptin levels similar to patients with normal renal function, the drug should be reduced in patients with medium and severe renal impairment, as well as in patients with end -stage renal disease (ESRD), hemolysis or peritoneal fertilizer.

During stress (fever, bacterial infection, surgery) may lose blood glucose, suspend sitagliptin and use insulin to control. Applying therapy with sitagliptin again when the stage of increased blood glucose is over.

Hypersensitivity reactions: including anaphylactic reaction, angioedema and skin peeling diseases including Stevens - Johnson syndrome. These reactions began to appear in the first 3 months after starting treatment with sitagliptin, with several reports that occurred after the first dose. If there is a suspected hypersensitivity reaction, sitagliptin must be discontinued, assessing other potential causes and starting alternative therapies for diabetes.

Used in the elderly: In clinical studies the safety and effectiveness of sitagliptin in the elderly (> 65 years) similar to younger patients (

The ability to drive and operate machinery

has not conducted studies on the impact of sitagliptin on the ability to drive and operate machinery. However, it is thought that sitagliptin does not affect the ability to drive and operate machinery.

Pregnancy

Avoid using drugs during pregnancy.

Lactation period

Sitagliptin is excreted in milk on experimental animals, still unknown whether sitagliptin is excreted in human milk or not. However, sitagliptin should not be used for breastfeeding women unless they have carefully considered the benefits and risks.

Drug interaction

The effect of other drugs on sitagliptin

CYP3A4 and 2C8 inhibitors or touches do not affect the metabolism of sitagliptin.

Metformin: Take the dose 2 times daily 1,000 mg of metformin along with 50mg of sitagliptin does not change the pharmacokinetic significance of sitagliptin in patients with type 2 diabetes.

Cyclosporin: Sitagliptin has no significant interaction with cyclosporin and other p-glycoprotein inhibitors.

The effect of sitagliptin on other drugs

Digoxin: Sitagliptin increases the concentration of digoxin in plasma. After 0.25 mg of Digoxin inject with 100 mg of sitagliptin per day for 10 days, Digoxin's AUG increased by 11% and 18% CMAX. It is not recommended to adjust the Digoxin dose. However, patients at risk of Digoxin poisoning should be monitored when using sitagliptin and digoxin simultaneously.

In In vitro study shows that sitagliptin does not inhibit or CYP450. In clinical studies, sitagliptin does not cause clinical significance to the pharmacokinetics of the following drugs: metformin, glyburide, simvastatin, rosiglitazone, warfarin, or oral contraceptive pill. Based on Vivo data, there is a light interaction with substrates such as CYP3A4, CYP2C8, CYP2C9 and organic cation (OCT) transportation. Sitagliptin can be a light inhibitor P - Glycoprotein in in vivo.

Storage

Store in a dry place, avoid light, temperatures below 30 ° C.

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