Iscept-P

Glyburide:

• Iscept-P (Glyburide) reviews

Iscept-P (Glyburide) is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Iscept-P (Glyburide) has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Iscept-P (Glyburide) appears to be completely metabolized, likely in the liver. Although its metabolites exert a small hypoglycemic effect, their contribution to glyburide’s hypoglycemic effect is thought to be clinically unimportant. Iscept-P (Glyburide) metabolites are excreted in urine and feces in approximately equal proportions. The half-life of Iscept-P (Glyburide) appears to be unaffected in those with a creatinine clearance of greater than 29 ml/min/1.73m2.

Indication: Indicated as an adjunct to diet to lower the blood glucose in patients with NIDDM whose hyperglycemia cannot be satisfactorily controlled by diet alone.

Iscept-P (Glyburide), a second-generation sulfonylurea antidiabetic agent, lowers blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glibenclamide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, Iscept-P (Glyburide) produces a mild diuresis by enhancement of renal free water clearance. Iscept-P (Glyburide) is twice as potent as the related second-generation agent glipizide.

Metformin:

• Iscept-P (Metformin) reviews

Iscept-P (Metformin) is a biguanide antihyperglycemic agent used for treating non-insulin-dependent diabetes mellitus (NIDDM). It improves glycemic control by decreasing hepatic glucose production, decreasing glucose absorption and increasing insulin-mediated glucose uptake. Iscept-P (Metformin) is the only oral antihyperglycemic agent that is not associated with weight gain. Iscept-P (Metformin) may induce weight loss and is the drug of choice for obese NIDDM patients. When used alone, Iscept-P (Metformin) does not cause hypoglycemia; however, it may potentiate the hypoglycemic effects of sulfonylureas and insulin. Its main side effects are dyspepsia, nausea and diarrhea. Dose titration and/or use of smaller divided doses may decrease side effects. Iscept-P (Metformin) should be avoided in those with severely compromised renal function (creatinine clearance < 30 ml/min), acute/decompensated heart failure, severe liver disease and for 48 hours after the use of iodinated contrast dyes due to the risk of lactic acidosis. Lower doses should be used in the elderly and those with decreased renal function. Iscept-P (Metformin) decreases fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Iscept-P (Metformin) may also have a positive effect on lipid levels.

Indication: For use as an adjunct to diet and exercise in adult patients (18 years and older) with NIDDM. May also be used for the management of metabolic and reproductive abnormalities associated with polycystic ovary syndrome (PCOS).

Iscept-P (Metformin) is an oral antihyperglycemic agent that improves glucose tolerance in patients with NIDDM, lowering both basal and postprandial plasma glucose. Iscept-P (Metformin) is not chemically or pharmacologically related to any other class of oral antihyperglycemic agents. Unlike sulfonylureas, Iscept-P (Metformin) does not produce hypoglycemia in either patients with NIDDM or healthy subjects and does not cause hyperinsulinemia. Iscept-P (Metformin) does not affect insulin secretion.

Pioglitazone:

• Pharmacological action
• Pharmacokinetics
• Why is Iscept-P prescribed?
• Dosage and administration
• Iscept-P (Pioglitazone) side effects, adverse reactions
• Iscept-P contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Iscept-P drug interactions
• Iscept-P in case of emergency / overdose
• Iscept-P (Pioglitazone) reviews

Pharmacological action

Iscept-P is an oral hypoglycemic agent, series of thiazolidinedione derivatives. Powerful and selective agonist of gamma-receptors, peroxisome proliferator-activated (PPAR-gamma). PPAR-gamma receptors are found in adipose and muscle tissues and liver. Activation of nuclear receptor PPAR-gamma modulates the transcription of several genes that are sensitive to insulin, involved in controlling glucose and lipid metabolism. This medicine reduces insulin resistance in peripheral tissues and liver, as a result of this is increased flow of glucose and insulin reduced glucose production in the liver. Unlike sulfonylureas, Iscept-P (Pioglitazone) does not stimulate insulin secretion by beta cells of the pancreas.

In diabetes mellitus type 2 (insulin-dependent) decrease in insulin resistance under the action of Iscept-P (Pioglitazone) reduces blood glucose levels, reduce insulin levels in plasma and hemoglobin A1c (glycated hemoglobin, HbA1c).

In diabetes mellitus type 2 (insulin-dependent) with lipid disorders during treatment with Iscept-P (Pioglitazone) there is a decrease in triglycerides and increase HDL. The level of LDL and total cholesterol in these patients does not change.

Pharmacokinetics

After oral administration Iscept-P (Pioglitazone) is found in fasting plasma after 30 minutes. C_max in plasma is reached after 2 hours. At ingestion there was a slight increase of C_max to 3-4 hours, but the extent of absorption was not changed.

Protein binding of human serum, mainly to albumin greater than 99%; binding to other serum proteins less pronounced. The metabolites of Iscept-P (Pioglitazone) M-III and M-IV also significantly associated with serum albumin is more than 98%.

Iscept-P (Pioglitazone) is extensively metabolized in the liver by hydroxylation and oxidation. Metabolites M-II, M-IV (hydroxy derivatives of Iscept-P (Pioglitazone)) and M-III (keto derivative of Iscept-P (Pioglitazone)) exhibit pharmacological activity in models of type 2 diabetes in animals. Metabolites also partly converted into conjugates glucuronic or sulfuric acids.

The metabolism of Iscept-P (Pioglitazone) in the liver occurs with the participation of isoenzymes CYP2C8 and CYP3A4.

T_1/2 of unchanged Iscept-P (Pioglitazone) is 3-7 hours, total Iscept-P (Pioglitazone) (pioglitazone and active metabolites) is 16-24 hours. The clearance of Iscept-P (Pioglitazone) is 5-7 L / h.

After oral administration about 15-30% of the dose of Iscept-P (Pioglitazone) is found in urine. Kidneys displayed a negligible amount of Iscept-P (Pioglitazone), mainly in the form of metabolites and their conjugates.

It is believed that the ingestion of large doses is excreted in bile as unchanged and as metabolites and excreted in the feces.

The concentrations of Iscept-P (Pioglitazone) and active metabolites in serum remained at a high level 24 h after a single daily dose.

Why is Iscept-P prescribed?

Type 2 diabetes (insulin independent).

Dosage and administration

Iscept-P is taken orally in dose 30 mg 1 time / day. The duration of treatment is determined individually.

The maximum dose in combination therapy is 30 mg / day.

Iscept-P (Pioglitazone) side effects, adverse reactions

Metabolism: a possible development of hypoglycaemia (mild to severe).

Hematopoietic system: possible anemia, decreased hemoglobin and hematocrit.

Digestive system: rarely - increased ALT.

Iscept-P contraindications

Diabetes mellitus type 1 (insulin-dependent), diabetic ketoacidosis, pregnancy, lactation, hypersensitivity to Iscept-P (Pioglitazone).

Using during pregnancy and breastfeeding

Iscept-P is contraindicated during pregnancy and lactation. In patients with insulin resistance and anovulatory cycles in pre menopausal period the treatment with thiazolidinediones, including Iscept-P (Pioglitazone), can cause ovulation. This increases the risk of pregnancy if you do not use adequate contraception.

In experimental studies in animals showed that Iscept-P (Pioglitazone) has no teratogenic effects and adverse effects on fertility.

Category of the fetus by FDA - C.

Special instructions

Iscept-P (Pioglitazone) should not be used in the presence of clinical presentations of liver disease in the active phase or an increase in ALT is 2.5 times above ULN.

During treatment for suspected development of liver dysfunction (nausea, vomiting, abdominal pain, fatigue, lack of appetite, dark urine) should define indicators of liver function tests. In the case of jaundice Iscept-P (Pioglitazone) should be discontinued.

Iscept-P (Pioglitazone) should be used with caution in patients with edema.

Anemia, decreased hemoglobin and hematocrit decrease may be associated with increased plasma volume and do not show any clinically significant hematological effects.

If necessary to usee Iscept-P (Pioglitazone) simultaneously with ketoconazole should be more regular follow-up blood glucose levels.

There have been rare cases of a temporary increase in the activity level of CPK during treatment with this drug, which had no clinical consequences. The relationship of these reactions from taking Iscept-P (Pioglitazone) is unknown.

The average values of bilirubin, AST, ALT, ALP and GGT decreased in the survey at the end of treatment by this medicine compared with those of before treatment.

Before treatment and during the first year of treatment (every 2 months) and then periodically monitor the activity of ALT should be.

Experimental studies have shown that Iscept-P (Pioglitazone) is not mutagenic.

The use of Iscept-P (Pioglitazone) in children is not recommended.

Iscept-P drug interactions

In another thiazolidinedione derivative simultaneously observed with oral contraceptives decrease the concentration of ethinyl estradiol and norethindrone in plasma by approximately 30%. Therefore, while the use of Iscept-P (Pioglitazone) and oral contraceptives may decrease contraceptive efficacy.

Ketoconazole inhibits the metabolism of Iscept-P (Pioglitazone) in the liver in vitro.

Sulfonamides derivatives, metformin and insulin potentiate (relatively) hypoglycemia.

Iscept-P in case of emergency / overdose

Treatment: symptomatic therapy.