Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Actos
Active ingredient: Pioglitazone
Available dosage forms: 15, 30 mg
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Pioglitazone general information
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For the Vitamin to eventually become active, it must undergo a number of processes within the body. Without insulin, the body can’t utilize glucose, which is a significant blood glucose. A superior carbohydrate, superior fiber diet will decrease the need for insulin. A diet full of sugar and white flour may lead to diabetes. Another portion of the vitamin D originates from food. Vitamin D behaves in this type of way in the body it is classified as a hormone.
The systemic kind of lupus can affect multiple regions of the human body and cause a wide selection of unspecific symptoms, which range from mild to severe. In the absence of the correct cure, discoid lupus may get systemic over the plan of time. With the right treatment, the vast majority of patients diagnosed with lupus can live healthful and active lives. After the prosperous pituitary surgery the elevated rates of ACTH drop two times lower when compared to the typical level.
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Mode of action PIOGLITAZONE (pioglitazone)
Oral hypoglycemic means derivative thiazolidinedione series. Potent, selective agonist of gamma – receptors, peroxisome proliferator-activated (PPAR – gamma). PPAR – gamma receptors are found in the fat, muscle and liver tissues. Activation of the nuclear receptor PPAR – gamma modulates transcription of several genes that are sensitive to insulin involved in the control of glucose and lipid metabolism. Reduces insulin resistance in peripheral tissues and liver, resulting in an increase insulin-dependent glucose consumption and a decrease in glucose production in the liver. Unlike sulfonylureas, pioglitazone did not stimulate secretion of insulin beta – pancreatic cells.
In diabetes mellitus type 2 (insulin-dependent) decrease insulin resistance under the action of pioglitazone leads to a decrease in blood glucose concentration, lower insulin levels in plasma and hemoglobin A 1c (glycated hemoglobin, HbA 1c ).
In diabetes mellitus type 2 (insulin-dependent) with impaired lipid metabolism during treatment with pioglitazone there is a decrease in triglycerides and increase HDL levels. At this level of LDL and total cholesterol levels in these patients is not changed.
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Description of pioglitazone. The active substance is pioglitazone. pioglitazone. Medications and active substance pioglitazone. Which drugs are used pioglitazone. Pioglitazone chemical composition. indications of pioglitazone. side effects of pioglitazone. pioglitazone instructions
Pharmacokinetics PIOGLITAZONE (pioglitazone)
Once inside the empty stomach pioglitazone detected in plasma within 30 minutes. C max plasma achieved in 2 hours When eating there was a slight increase in the time to reach C max 3 -. 4 hours, but the extent of absorption was not changed.
After a single dose of an apparent V d pioglitazone averaged 0.63 & plusmn; 0.41 l / kg. Binding to human serum proteins, mainly albumin is greater than 99%; binding of other serum proteins less pronounced. Metabolites pioglitazone M – III and M – IV in substantially bind serum albumin – more than 98%.
Pioglitazone is extensively metabolized in the liver by hydroxylation and oxidation. Metabolites M – II, M – IV (hydroxy – derivatives of pioglitazone) and M – III (keto – derivatives pioglitazone) exhibit pharmacological activity in models of type 2 diabetes in the animals. The metabolites also partly converted into conjugates of glucuronic or sulfuric acid.
The metabolism of pioglitazone in the liver occurs with the participation of isoenzymes CYP2C8 and CYP3A4.
T 1/2 unchanged pioglitazone is 3 – 7 hours, total pioglitazone (pioglitazone and active metabolites) – 16 – 24 hours. Clearance pioglitazone is 5 – 7 l / h.
After oral administration of about 15 – 30% of the dose is found in the urine of pioglitazone. Kidneys displayed negligible amount of pioglitazone, mainly in the form of metabolites and conjugates. It is believed that when administered most of the dose is excreted in the bile in unchanged form and in the form of metabolites and excreted in the feces.
concentrations in serum and pioglitazone active metabolites remain at a high level at 24 hours following a single administration of a daily dose.
Indications PIOGLITAZONE (pioglitazone)
Diabetes mellitus type 2 (non-insulin dependent).
Dosage PIOGLITAZONE (pioglitazone)
It is taken at a dose of 30 mg 1 time / day. Duration of treatment is determined individually.
The maximum dose in combination therapy is 30 mg / day.
Side effects PIOGLITAZONE (pioglitazone)
From a metabolism: may develop hypoglycaemia (mild to severe).
From the hematopoietic system: may be anemia, decrease in hemoglobin and hematocrit.
From the digestive system: , rarely – increased ALT.
Contraindications PIOGLITAZONE (pioglitazone)
Diabetes mellitus type 1 (insulin-dependent), diabetic ketoacidosis, pregnancy, lactation, hypersensitivity to pioglitazone.
Application of pregnancy and breastfeeding PIOGLITAZONE (pioglitazone)
Pioglitazone is contraindicated during pregnancy and lactation.
In patients with insulin resistance and anovulatory cycle in premenopauznom period of treatment with thiazolidinediones, including pioglitazone may cause ovulation. This increases the risk of pregnancy if you do not use adequate contraception.
The experimental research on animals have shown that pioglitazone has no teratogenic effects and the negative impact on fertility.
Cautions PIOGLITAZONE (pioglitazone)
Do not use pioglitazone in the presence of clinical manifestations of liver disease in the active phase or by increasing the activity of ALT 2.5 times above the ULN. When moderately elevated liver enzymes (ALT less than 2.5 times the ULN) prior to or during treatment with pioglitazone patients should be evaluated to determine the reasons for increasing rates. At moderately elevated liver enzymes should be cautious to start or continue treatment. In this case, we recommend more frequent monitoring of clinical research and the level of liver enzymes.
In the case of increasing the activity of transaminases in the serum (ALT> 2.5 times the ULN) monitoring liver function should be performed more often and as long as the level does not return to normal or to indicators that observed before treatment. If ALT activity 3 times the ULN, then re-test to determine the activity of ALT should be performed as quickly as possible. If ALT activity remained at 3 times> ULN pioglitazone should be discontinued.
In the period of treatment in cases of suspected development of liver dysfunction (cause nausea, vomiting, abdominal pain, fatigue, lack of appetite, dark urine) should define indicators of liver function tests. The issue of continued therapy with pioglitazone should be taken on the basis of clinical data based on laboratory parameters. In case of jaundice, pioglitazone should be discontinued.
Caution should be used pioglitazone in patients with edema.
The development of anemia, decrease in hemoglobin and hematocrit decrease may be associated with an increase in plasma volume and do not show what – or clinically significant hematological effects.
If necessary, the simultaneous application of ketoconazole should be more regularly monitoring blood glucose levels.
There have been rare cases of temporary increase in the level of CPK during treatment with pioglitazone, it did not have any clinical consequences. The relationship of these reactions taking pioglitazone is unknown.
The average values of bilirubin, AST, ALT, GGT and alkaline phosphatase decreased during the examination at the end of treatment with pioglitazone, compared with those before treatment.
Before the start of treatment and during the first year of treatment (every 2 months), and then periodically monitor the activity of ALT should be.
The experimental research is shown that pioglitazone has no mutagenicity.
The use of pioglitazone in children is not recommended.
Drug Interactions PIOGLITAZONE (pioglitazone)
When using another thiazolidinedione derivative simultaneously with oral contraceptives was observed decrease in the concentration of ethinyl estradiol and norethindrone plasma by approximately 30%. Therefore, while the use of pioglitazone and oral contraceptives may decrease the effectiveness of birth control.
pioglitazone Ketoconazole inhibits in vitro metabolism in liver.
Application for violations of liver function PIOGLITAZONE (pioglitazone)
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Application for violations of renal function PIOGLITAZONE (pioglitazone)
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Overdose PIOGLITAZONE (pioglitazone)
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