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Actos

Actos
Actos is a hypoglycemic (sugar-lowering) drug. The action of the drug Actos depends on the presence of insulin. It reduces insulin resistance (insulin resistance) of tissues and liver, as a result of which the absorption of glucose by tissues increases and its release from the liver decreases. The drug does not stimulate the production of insulin - by the cells of the pancreas.

Brand: Pioglitazone

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: October 2023
Package Price Per pill Save Order
Actos 45 mg
270 pills - 45 mg
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180 pills - 45 mg
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60 pills - 45 mg $61.95 $1.03 $18.03 Add to cart
30 pills - 45 mg $39.99 $1.33 No Add to cart
Actos 30 mg
360 pills - 30 mg
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270 pills - 30 mg
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Actos 15 mg
360 pills - 15 mg
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$151.99 $0.42 $207.89 Add to cart
270 pills - 15 mg
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60 pills - 15 mg $46.95 $0.78 $13.03 Add to cart
30 pills - 15 mg $29.99 $1.00 No Add to cart

Product description

Pharmacological action of the drug Actos

Packaging of the drug Actos

Actos is an oral antidiabetic agent containing pioglitazone, an active component of the thiazolidinedione group, which has a pronounced hypoglycemic effect in type II diabetes mellitus. The mechanism of action of pioglitazone is dependent on the presence of insulin. Actos is a highly selective gamma receptor agonist that is activated by PPAR-gamma. PPAR-gamma receptors are found in muscle and adipose tissue, as well as in liver tissue; activation of these receptors modulates the transcription of a number of genes that are sensitive to insulin and are involved in the control of glucose and lipid metabolism.

The drug Actos helps to reduce the insulin resistance of peripheral tissues and the liver, as a result of which there is an increase in the consumption of insulin-dependent glucose and a decrease in the release of glucose from the liver.

Unlike sulfonylurea preparations, Actos does not stimulate the production of insulin by the pancreas.

In patients with type 2 diabetes mellitus, when taking Actos, a decrease in insulin resistance is recorded, which leads to a decrease in serum glucose and a decrease in plasma insulin levels, as well as a decrease in glycated hemoglobin. There has been a significant improvement in glycemic control in persons with type 2 diabetes mellitus with combined therapy with Actos and sulfonylurea derivatives, metformin or insulin.

In patients with type 2 diabetes mellitus with concomitant lipid metabolism disorders during therapy with Actos, a decrease in serum triglyceride levels and an increase in high-density lipoprotein levels are recorded without changing the total cholesterol and low-density lipoproteins.

Pharmacokinetics

When taken orally on an empty stomach, the peak levels of pioglitazone are recorded 2 hours later, and the minimum 30 minutes after taking the pill. Eating slightly increases the time to peak pioglitazone levels (up to 3–4 hours), but does not alter the rate of absorption.

After a single dose, the apparent volume of distribution reached 0.63 ± 0.41 l / kg. A significant part of the pioglitazone dose (up to 99%) is bound by serum proteins (most of it is albumin). Certain pioglitazone derivatives also bind significantly to serum proteins. Equilibrium levels of pioglitazone represent about 30-50% of peak serum levels.

The drug is significantly metabolized in the liver, in particular by hydroxylation and oxidation. The derivatives are further converted into conjugates with sulfuric and glucuronic acid. With multiple doses of Actos, there is a significant level of pioglitazone derivatives M-3 and M-4 in serum. The metabolism of the drug is associated with the main isoenzymes of the P450 system.

After oral administration, about 15-30% of the active ingredient is found in the urine. A small part of unchanged pioglitazone is excreted by the urinary system, excretion by the urinary system occurs mainly in the form of metabolites, as well as their conjugates.

A significant part of pioglitazone is excreted by the liver unchanged and in the form of derivatives.

The average elimination half-life of total pioglitazone and pioglitazone reaches 16-24 hours and 3-7 hours, respectively. The clearance indicator is 5–7 l / h.

After a single dose, sufficient therapeutic doses of pioglitazone are noted for 24 hours.

 

Indications for use Actos

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Actos is used in the therapy of patients with non-insulin-dependent diabetes mellitus in the form of monotherapy or in combination with drugs that stimulate the production of insulin (for example, sulfonylurea derivatives), or insulin. The drug should be used only on condition of adherence to a diet and sufficient physical activity (in cases where diet therapy and physical activity do not provide sufficient glycemic control).

Method of administration

The drug Actos is intended for oral administration. Actos tablets are taken 1 time per day, regardless of food. The dose of pills should be selected personally, taking into account the tolerability, effectiveness and concomitant drugs used in complex therapy.

Typically, with pioglitazone monotherapy, 15–30 mg / day is recommended in addition to diet and exercise. If necessary, under the supervision of a specialist, the dose can be increased to 45 mg / day. In case of monotherapy, it is not recommended to prescribe more than 45 mg / day; in case of insufficient glycemic control, it is recommended to prescribe additional drugs that stimulate the secretion of insulin or insulin.

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In combination with other oral antidiabetic drugs, including metformin or sulfonylurea derivatives, Actos is prescribed at a dose of 15–30 mg / day. The total daily dose of pioglitazone is given in one dose. At the beginning of therapy with Actos tablets, the dose of sulfonylurea derivatives or other hypoglycemic agents can be left unchanged, however, careful monitoring of glucose indicators and a decrease in the dose of hypoglycemic agents with the development of hypoglycemia is necessary. It should be borne in mind that combined therapy with sulfonylureas without changing their dose is more often accompanied by the development of hypoglycemia (in comparison with combined therapy with metformin and pioglitazone).

In combination with insulin, Actos is prescribed at a dose of 15-30 mg / day. The total daily dose of pioglitazone is given in one dose. At the beginning of therapy with Actos, the dose of insulin can be left unchanged, however, careful monitoring of glucose values ​​and a decrease in the dose of insulin preparations by 10-25% when glucose values ​​are less than 100 mg / dL, further changes in the dose of insulin are carried out depending on the level of glucose in serum ...

In combination therapy regimens for type 2 diabetes mellitus, it is not recommended to prescribe more than 30 mg / day of pioglitazone.

The combined use of Actos with other thiazolidinedione derivatives has not been studied.

Patients with impaired renal filtration do not require dose adjustment of Actos tablets.

Contraindications

Actos is not used in the therapy of patients with intolerance to the active or auxiliary components of the tablets.

Actos is contraindicated in type 1 diabetes mellitus.

Actos tablets are not prescribed for diabetic ketoacidosis.

The use of Actos tablets is contraindicated in case of heart failure of the third or fourth degree according to the international classification.

The drug Actos is not used in pediatrics.

Pregnancy

The use of the drug Actos is contraindicated during pregnancy and lactation. In the case of planning or the onset of pregnancy during therapy with Actos, it is recommended to contact a specialist who will select the optimal therapy regimen.

Women of reproductive age who take COCs or other estrogen-containing contraceptives should take into account that Actos reduces the effectiveness of oral contraceptives and use additional contraceptives.

Drug interactiontogether

Actos, when used, can reduce the effectiveness of contraceptive drugs containing estrogens.

Actos has no effect on the pharmacokinetics of digoxin, metformin, indirect anticoagulants and glipizide when used together.

The effect of Actos on erythromycin, calcium channel blockers, astemizole, statins, triazolam, itraconazole, tacrolimus and trimetrexate has not been studied.

In vitro, ketoconazole reduces the metabolism of pioglitazone, but the clinical significance of this effect is unknown. Caution should be exercised when using Actos in combination with ketoconazole.

Overdose

Reception of excessive doses of the drug Actos was not accompanied by the development of clinical effects (subject to monotherapy with pioglitazone). In case of an overdose of pioglitazone taken in combination with sulfonylurea preparations, hypoglycemia may occur.

There is no specific antidote. In case of an overdose, which is accompanied by hypoglycemia, the appointment of therapy aimed at normalizing carbohydrate metabolism is indicated.


Side effect

From the endocrine system: hypoglycemia (2% - when combined with a sulfonylurea drug, 8-15% - when combined with insulin).

From the side of the hematopoietic system: 1-1.6% - anemia (with monotherapy and combination therapy); a decrease in hemoglobin (2-4%) and hematocrit, which are observed mainly 4-12 weeks after the start of treatment and remain relatively constant (not associated with any clinically significant hematological effects and are most often due to an increase in plasma volume).

From the side of metabolism: edema (4.8% - with monotherapy, 15.3% - with a combination with insulin); 5% - increase in body weight; rarely - increased activity of CPK.

On the part of the digestive system: about 0.25% - an increase in ALT activity> 3 times from VGN; rarely - hepatitis.

From the side of the organ of vision: very rarely - the development or progression of diabetic edema of the macula, accompanied by a decrease in visual acuity. A direct relationship between the development of macular edema and pioglitazone administration has not been established. Physicians should consider the possibility of developing macular edema if patients complain of decreased visual acuity.

Cardio-vascular system: A study in US placebo-controlled trials, the frequency of serious cardiovascular side effects associated with the increase in BCC, was not different in patients treated with only Actos® and Actos® in combination with a sulfonylurea, metformin, or placebo. In a clinical study with concomitant administration of drug Actos® insulin and a small number of patients who had a history of heart disease, congestive heart failure cases are marked. Patients with heart failure III and IV NYHA functional class classification have not participated in the clinical studies on the use of the drug, however Actos® is contraindicated for this group of patients.

According to post-marketing data, when using the drug Actos® , cases of congestive heart failure have been registered in patients, regardless of the indication of previously existing heart disease.