Apo-Pioglitazone

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Apo-Pioglitazone uses


Pharmacological action

Apo-Pioglitazone is an oral hypoglycemic agent, series of thiazolidinedione derivatives. Powerful and selective agonist of gamma-receptors, peroxisome proliferator-activated. 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, Apo-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 Apo-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 Apo-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 Apo-Pioglitazone is found in fasting plasma after 30 minutes. Cmax in plasma is reached after 2 hours. At ingestion there was a slight increase of Cmax 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 Apo-Pioglitazone M-III and M-IV also significantly associated with serum albumin is more than 98%.

Apo-Pioglitazone is extensively metabolized in the liver by hydroxylation and oxidation. Metabolites M-II, M-IV (hydroxy derivatives of Apo-Pioglitazone) and M-III (keto derivative of Apo-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 Apo-Pioglitazone in the liver occurs with the participation of isoenzymes CYP2C8 and CYP3A4.

T1/2 of unchanged Apo-Pioglitazone is 3-7 hours, total Apo-Pioglitazone (pioglitazone and active metabolites) is 16-24 hours. The clearance of Apo-Pioglitazone is 5-7 L / h.

After oral administration about 15-30% of the dose of Apo-Pioglitazone is found in urine. Kidneys displayed a negligible amount of Apo-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 Apo-Pioglitazone and active metabolites in serum remained at a high level 24 h after a single daily dose.

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Why is Apo-Pioglitazone prescribed?

Type 2 diabetes.

Dosage and administration

Apo-Pioglitazone 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.

Apo-Pioglitazone side effects, adverse reactions

Metabolism: a possible development of hypoglycaemia.

Hematopoietic system: possible anemia, decreased hemoglobin and hematocrit.

Digestive system: rarely - increased ALT.

Apo-Pioglitazone contraindications

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

Using during pregnancy and breastfeeding

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

In experimental studies in animals showed that Apo-Pioglitazone has no teratogenic effects and adverse effects on fertility.

Category of the fetus by FDA - C.

Special instructions

Apo-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 should define indicators of liver function tests. In the case of jaundice Apo-Pioglitazone should be discontinued.

Apo-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 Apo-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 Apo-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 Apo-Pioglitazone is not mutagenic.

The use of Apo-Pioglitazone in children is not recommended.

Apo-Pioglitazone 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 Apo-Pioglitazone and oral contraceptives may decrease contraceptive efficacy.

Ketoconazole inhibits the metabolism of Apo-Pioglitazone in the liver in vitro.

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

Apo-Pioglitazone in case of emergency / overdose

Treatment: symptomatic therapy.

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References

  1. Dailymed."ACTOS (PIOGLITAZONE HYDROCHLORIDE) TABLET [LAKE ERIE MEDICAL & SURGICAL SUPPLY DBA QUALITY CARE PRODUCTS LLC]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  2. "Pioglitazone". https://pubchem.ncbi.nlm.nih.gov/co... (accessed August 28, 2018).
  3. "Pioglitazone". http://www.drugbank.ca/drugs/DB0113... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Apo-Pioglitazone?

Depending on the reaction of the Apo-Pioglitazone after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Apo-Pioglitazone not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is Apo-Pioglitazone addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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Review

sdrugs.com conducted a study on Apo-Pioglitazone, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Apo-Pioglitazone consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

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The information was verified by Dr. Rachana Salvi, MD Pharmacology

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