Dianabol review – representative class apparatus pancreatic islet stimulants, selectively inhibits dipeptidyl peptidase-4 (DPP-4) enzyme. Rapid and complete inhibition of DPP-4 (> 90%) activity causes an increase in both basal and stimulated ingestion secretion of glucagon-like peptide type 1 (GLP-1) and gastric inhibitory polypeptide (GIP) from the gut into the systemic circulation throughout the day. increasing levels of GLP-1 and GIP, vildagliptin causes increased sensitivity of pancreatic β-cells to glucose, which leads to an improvement in glucose-insulin secretion. When applying vildagliptin 50-100 mg per day in patients with type 2 diabetes is marked improvement of pancreatic β-cells. The degree of improvement of β-cell function independent of their degree of initial damage; as in patients not suffering from diabetes (with normal levels of plasma glucose) vildagliptin does not stimulate insulin secretion and reduces blood glucose. Increasing levels of endogenous GLP-1, vildagliptin increases sensitivity α-cells to glucose, resulting in improved glucose-regulating glucagon secretion. Reduction of excessive glucagon level during meal, in turn, causes a decrease in insulin resistance. Increasing the ratio of insulin / glucagon amid hyperglycemia due to increased levels of GLP-1 and GIP, causes a decrease in hepatic glucose production in prandial period and after a meal, that lowers the level of glucose in the blood plasma. in addition, on treatment with vildagliptin marked reduction of lipids in blood plasma, however, this effect is not linked to its action on GLP-1 or GIP and the improvement of pancreatic β-cells. it is known that raising GLP-1 can lead to slow gastric emptying, but during treatment with vildagliptin this effect is not observed. in the application of vildagliptin in 5795 patients with type 2 diabetes within 12 to 52 weeks as monotherapy or in combination with metformin, sulfonylurea, a thiazolidinedione, or insulin was a significant prolonged decline in the concentration of glycated hemoglobin (in HbA 1c) and fasting blood glucose. Pharmacokinetics Absorption vildagliptin is rapidly absorbed when administered with an absolute bioavailability of 85%. The therapeutic dosage range to increase the maximum vildagliptin plasma concentration (C max ) and area under the curve “concentration-time» (AUC) practically directly proportional to the increase in dose. After ingestion fasting time to reach C max of vildagliptin in plasma is 1 hour 45 minutes . At the same time taking the drug with food absorption rate decreased slightly: marked decrease in C max by 19% and increasing the time it achieve up to 2 hours 30 minutes. However, the food intake does not affect the degree of absorption and AUC. Distribution Binding to plasma proteins vildagliptin low (9.3%). The drug is distributed equivalently between the plasma and red blood cells. Vildagliptin extravascularly distribution is presumed, the volume of distribution at steady state after intravenous administration (Vss) is 71 liters. Metabolism Biotransformation is the major route of excretion of vildagliptin. The human body is converted 69% of the dose. The major metabolite – LAY151 (57% of dose) and pharmacologically inactive product is cyano Hydrolyze component. About 4% of the dose exposed to the amide hydrolysis. In experimental studies have indicated a positive impact on the DPP-4 hydrolysis of the drug. Vildagliptin is not metabolized with the participation of isoenzyme of cytochrome P 450 . Vildagliptin is not a substrate of P isoenzymes (CYP) 450 , does not inhibit or induce cytochrome isoenzymes CYP 450 . Excretion and elimination After about 85% of the oral dose of the drug excreted by the kidneys and 15% – through the gut, renal excretion of the unchanged vildagliptin is 23%. The half-life following oral administration is approximately 3 hours, regardless of the dose. Gender, body mass index and ethnicity did not affect the pharmacokinetics of vildagliptin. Abnormal liver function in patients with mild to moderate hepatic impairment (6-10 points on the Child-Pugh classification ) after a single dose of the drug bioavailability vildagliptin a decline of 20% and 8%, respectively. In patients with severe hepatic insufficiency (12 points on the classification of Child-Pugh) vildagliptin bioavailability is increased by 22%. Increasing or decreasing the maximum bioavailability of vildagliptin is not greater than 30%, is not clinically significant. The correlation between the severity of liver dysfunction and bioavailability of the drug were found. Impaired renal function in patients with mild, moderate and severe renal impairment, in patients with end-stage renal disease (ESRD) on hemodialysis marked increase in C max at 8-66% and AUC by 32-134%, does not correlate with the severity of the violation, as well as the increase in AUC inactive metabolite LAY151 in 1,6-6,7 times, depending on the severity of the violation. The half-life of vildagliptin is not changed. The use in patients aged ≥65 years maximum increase drug bioavailability by 32% (increase in C max by 18%) in people over 70 years of age is not clinically significant and will not affect the inhibition of DPP-4. The use in patients aged ≤18 years Farmakokinёticheskie vildagliptin especially in children and adolescents under 18 years have not been established.
Type 2 diabetes:
- as monotherapy in combination with diet and exercise;
- a two-component composition in combination therapy with metformin, a sulfonylurea, or a thiazolidinedione insulin in the case of poor diet, exercise, and of these drugs alone.Contraindications
- Hypersensitivity to vildagliptin or any other components of the preparation.
The efficacy and safety of the drug in children under 18 years of age has not been established.Precautions
dianabol review is not recommended in patients with severe hepatic impairment, including patients with increased activity of liver enzymes (ACAT AlAt or> 2.5 times the upper limit of normal, 2.5x ULN). Since the experience with dianabol review in patients with moderate or severe renal impairment (including end-stage renal failure on hemodialysis) is limited, the drug is not recommended for these patients. As part of dianabol review drug tablets include lactose, the drug is not recommended for use in patients with rare hereditary disorders -. Galactose intolerance, lactase deficiency or malabsorption of glucose-galactose Pregnancy and lactation In experimental studies, when administered at doses 200 times higher than the recommended, the drug did not cause impaired fertility and early embryonic development and teratogenic effects on the fetus. Sufficient data on the use of dianabol review in pregnant women do not have, and therefore the drug should not be used during pregnancy. At disturbances of glucose metabolism in pregnant women have an increased risk razvitiyavrozhdennyh anomalies, as well as the frequency of neonatal morbidity and mortality. Since it is not known whether vildagliptin with breast milk in humans is released, dianabol review should not be used during lactation.Dosing and Administration
dianabol review taken orally with or without food.
The dosage regimen of the drug should be individualized depending on the effectiveness and tolerability.
The recommended dose of the drug in monotherapy or as part of a two-component combination therapy with metformin, a thiazolidinedione or insulin, 50 mg or 100 mg per day. In patients with more severe type 2 diabetes treated with insulin, dianabol review is recommended at a dose of 100 mg / day.
The dose of 50 mg / day should be administered at one time in the morning. The dose of 100 mg / day should be administered 50 mg 2 times a day, morning and evening.
When used as part of a two-component combination therapy with sulfonylurea recommended dose dianabol reviewa is 50 mg 1 time per day in the morning.
When administered in combination with a sulfonylurea effectiveness of drug therapy at a dose of 100 mg / day was similar to that at a dose of 50 mg / day.
in case of insufficient clinical effect in the treatment with the maximum recommended daily dose of 100 mg for better glycemic control possible additional designation of other hypoglycemic drugs: metformin, sulfonylureas, thiazolidinediones or insulin. patients with impaired hepatic or renal function in patients with mild renal impairment and liver does not require drug dosing regimen correction. patients aged ≥65 years elderly patients do not require dianabol reviewa correction mode. Use in patients aged ≤18 years as experience dianabol reviewa application in children and adolescents younger than 18 years is not, it is not recommended to use the drug in these patients.
When using dianabol review as monotherapy or in combination with other drugs, most adverse events were mild, were temporary in nature and did not require discontinuation of therapy. The correlation between the frequency of adverse events (AEs) and the age, sex, ethnicity, duration of use, or dosing regimen has not been identified.
The incidence of angioedema during therapy with dianabol review was ≥1 / 10,000, <1/1000 (gradation “rarely”) was similar to that in the control group. Most often angioedema observed in the appointment of the drug in combination with inhibitors of angiotensin enzyme pre torque. In most cases of angioedema have been moderate and disappeared during the continuation of vildagliptin therapy. The therapy dianabol review rarely observed in human liver (including hepatitis), asymptomatic. In most cases, these disorders and abnormalities in liver function of normal resolved spontaneously without complications after the cessation of drug therapy. When using dianabol review 50 mg 1 or 2 times per day rate increase in liver enzymes (AlAt or ACAT ≥3h ULN) was 0.2% and 0.3%, respectively (compared to 0.2% in the control group). Increase in liver enzymes in most cases were asymptomatic, did not progress and was not accompanied by changes or cholestatic jaundice. To evaluate the incidence of adverse events, the following criteria: very common (≥1 / 10); commonly (≥1 / 100, <1/10), occasionally (≥1 / 1000, <1/100), rare (≥1 / 10,000, <1/1 000), very rare (≤1 / 10,000 ) including individual messages. When using dianabol review monotherapy: When applying dianabol review 50 mg of 1 or 2 times a day, frequency of discontinuation due to adverse reactions (0.2% or 0.1%, respectively) is not higher than that in the placebo group (0.6%) or a comparator product (0.5%). In monotherapy dianabol review 50 mg of 1 or 2 times a day, the incidence of hypoglycemia without increasing the severity of the condition was 0.5% (2 persons of 409) or 0.3% (4 out of 1082), which is comparable to the reference formulation and placebo (0.2 %). When used as monotherapy dianabol review were observed increase of patient body weight. On the part of the central nervous system: often – dizziness;sometimes – headache. From the digestive system: sometimes – constipation; the part of the body as a whole: . sometimes – peripheral edema, long-term clinical studies of up to 2 years did not show any additional safety profile deviation or unforeseen risks when using vildagliptin as monotherapy . When using dianabol review 50 mg of 1 or 2 times a day in combination with metformin: When applying dianabol review 50 mg / day in combination with metformin frequency of discontinuation due to adverse reactions was 0.4% (Group vildagliptin (50 2 mg twice a day) + metformin versus placebo + metformin treatment discontinuations were noted due to adverse reactions). When applying dianabol review 50 mg 1 or 2 times a day in combination with metformin hypoglycemia was observed in 0.9% and 0.5%, respectively (placebo metformin + – 0.4%). In the group of dianabol review were observed of severe hypoglycemia. Combined vildagliptin therapy + metformin did not affect the patients body weight. On the part of the central and peripheral nervous system . Often – tremor, dizziness, headache, long-term clinical studies of up revealed no 2 years no additional variations safety profile or unanticipated risks when applied vildagliptin in combination with metformin. in applying dianabol review 50 mg / day in combination with sulfonylureas when applying dianabol review 50 mg / day in combination with glimepiride frequency of discontinuation due to adverse reactions was 0.6% (compared to 0% in the placebo + glimepiride). The incidence of hypoglycemia in patients receiving dianabol review 50 mg / day together with glimepiride amounted to 1.2% (versus 0.6% for placebo + glimepiride). Under Gadvus not observed the development of severe hypoglycemia. In the application of dianabol review at the recommended dose (50 mg / day) in combination with glimepiride were observed increase of patient body weight. On the part of the central nervous system: often – tremor, dizziness, headache. On the part of the body in general: often – asthenia. When using dianabol review 50 mg of 1 or 2 times a day in combination with derivatives thiazolidinedione When applying dianabol review 50 mg / day in combination with pioglitazone frequency of discontinuation due to adverse reactions was 0.7% (Group vildagliptin (50 mg two times a day) + pioglitazone placebo + pioglitazone discontinuations of therapy is not mentioned in connection with the development of adverse events). When using dianabol review 50 mg / day in combination with pioglitazone 45 mg hypoglycemia not He noted; group vildagliptin (50 mg two times a day) + pioglitazone (45 mg) of hypoglycemia was observed in 0.6% of cases and patients receiving placebo + pioglitazone 45 mg, – 1.9% of cases. In the group of dianabol review were observed of severe hypoglycemia. The mean increase in body weight compared to placebo treated patients dianabol review 50 mg 1 or 2 times per day with pioglitazone was + or + 0.1 kg 1.3 kg, respectively. When adding dianabol review 50 mg 1 or 2 times per day for pioglitazone in a dose of 45 mg / day incidence of peripheral edema was 8.2% and 7%, respectively (compared to 2.5% on pioglitazone monotherapy). However for initial combination therapy vildagliptin 50 mg 1 or 2 times per day with a dose of pioglitazone 45 mg / day and peripheral edema were observed in 3.5% or 6.1% of patients, respectively (compared to 9.3% on pioglitazone monotherapy . 30 mg / day), cardio-vascular system: . frequently – peripheral edema On the part of the body as a whole: often – increase in body weight. When using dianabol review 50 mg 2 times a day in combination with insulin: P ri appointment drug in combination with insulin are not observed increased risk of hypoglycemia as compared to insulin + placebo combination. The mean increase in body weight compared to placebo treated patients dianabol review 50 mg 2 times a day with insulin, was 0.9 kg . On the part of the central nervous system: often – headache; From the digestive system: . frequently – nausea, flatulence, gastroesophageal reflux disease, metabolic disorders and nutrition: . frequently – hypoglycemia Post-marketing research: During postmarketing studies the following adverse reactions were vyyaleny: urticaria (frequency unknown).
dianabol review is well tolerated when administered at a dose of 200 mg / day.
In applying the drug in a dose of 400 mg / day may experience muscle pain, rarely -Easy and transient paraesthesia, fever, edema and a transient increase in lipase concentrations (above the upper limit of normal 2 times). With increasing doses dianabol reviewa to 600 mg / day may develop swelling of limbs with paresthesias, and increased creatine phosphokinase concentrations, alanine, C-reactive protein and myoglobin. All symptoms of overdose and changes in laboratory parameters disappear after discontinuation of the drug. Elimination of the drug from the body by hemodialysis is unlikely. However, the main metabolite of the hydrolysis of vildagliptin (LAY151) can be removed from the body by hemodialysis.
The interaction with other drugs
dianabol review has a low potential for drug interactions.
As dianabol review is not a substrate of cytochrome P (CYP) 450 , and does not inhibit or induce these enzymes dianabol reviewa interaction with drugs that are substrates, inhibitors or inducers of P ( CYP) 450 , it is unlikely.With simultaneous use of vildagliptin also affects the rate of metabolism of drugs that are substrates for enzymes: CYP1A2, CYP2C8, CYP2C9, CYP2C19 , CYP2D6, CYP2E1 and CYP3A4 / 5.
The clinical significance of the interaction dianabol reviewa with the drugs most commonly used in the treatment of type 2 diabetes (glibenclamide , pioglitazone, metformin), or has a narrow therapeutic range (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin) is not established.
Cautions Disturbances of liver function Since the rare cases when the use of vildagliptin was an increase in transaminases (usually without clinical manifestations), before the appointment dianabol reviewa, as well as regularly during the first year of treatment (1 every 3 months), it is recommended to determine the biochemical parameters of liver function. If the patient revealed elevated aminotransferases, this result should be confirmed by repeated research, and thereafter to conduct regular measurements of biochemical parameters of liver function, as long as they are not normalized. If the excess of AST or AlAt in Sx ULN confirmed by re-examination, the drug should be repealed. With the development of jaundice or other signs of liver function abnormalities during treatment dianabol reviewa drug therapy should be discontinued immediately. After the normalization of liver function indicators drug treatment can not renew. If necessary, insulin therapy dianabol review is used only in combination with insulin. The drug should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Effects on ability to drive vehicles and / or work with mechanisms Influence dianabol reviewa on the ability to drive vehicles or operate machinery has not been established. With the development of vertigo on the background of treatment patients should not drive vehicles or operate machinery.
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