International nonproprietary name:
Testosterone propionate buy
1 film-coated tablet contains: Active substance : testosterone propionate buy – 10 mg / 25 mg; Excipients : lactose monohydrate – 162.50 / 113.0 mg, microcrystalline cellulose – 62.50 / 50.0 mg, giproloza (hydroxypropyl) – 7.5 / 6.0 mg, sodium croscarmellose – 5.0 / 4.0 mg colloidal silicon dioxide – 1.25 / 1.0 mg, magnesium stearate – 1.25 / 1.0 mg; Sheath : Opadry yellow (02V38190) – 7,0 / 6,0 mg (hypromellose 2910 – 3.5 / 3.0 mg titanium dioxide (E 171) – 1.733 / 1.485 mg talc – 1.4 / 1.2 mg macrogol 400 – 0.35 / 0.3 mg iron oxide yellow dye (E 172) – 0.018 / 0.015 mg).
Description Tablets dosage 10 mg Round, biconvex beveled edge tablets, film-coated light yellow with an engraving of the symbol at one side of the tablet and «S10» on the other side. The tablets dosage 25 mg Oval biconvex beveled edge tablets, film-coated light -Yellow color of characters engraved on one side of the tablet and «S25» on the other side.
Hypoglycemic agent for oral use – an inhibitor of sodium-glucose transporter type 2
testosterone propionate buy is reversible, highly active, selective and competitive inhibitor of the sodium-glucose transporter type 2 concentration value needed to inhibit 50% of enzyme activity (IC 50 ) equal to 1.3 nM.Selectivity testosterone propionate buya 5000 times the selectivity of the sodium-glucose transporter type 1 is responsible for the absorption of glucose in the intestine. Furthermore, it was found that testosterone propionate buy has high selectivity with respect to other glucose transporters responsible for the homeostasis of glucose in various tissues.
Sodium-glucose transporter type 2 is the main carrier protein responsible for reabsorption of glucose from the glomerular back into the bloodstream. testosterone propionate buy improves glycemic control in patients with type 2 diabetes mellitus (type 2) by reducing the glucose reabsorption in the kidney. The amount of glucose excreted by the kidneys with the help of this mechanism depends on the concentration of glucose in the blood and glomerular filtration rate (GFR). The inhibition of the sodium-glucose transporter type 2 patients with type 2 diabetes and hyperglycemia leads to the excretion of excess glucose by the kidneys.
In clinical studies, it was found that patients with type 2 glucose excretion by the kidneys increased immediately after the first dose testosterone propionate buya; This effect lasted for 24 hours. Increased renal excretion of glucose was maintained until the end of the 4 week treatment period, making use testosterone propionate buya at a dose of 25 mg once a day, on average, about 78 g / day. In patients with type 2 diabetes increase the excretion of glucose by the kidneys resulting in an immediate reduction in plasma glucose concentration.
testosterone propionate buy reduces plasma glucose concentrations in the case of receiving an empty stomach or after a meal.
Insulin-independent mechanism of action testosterone propionate buya helps lower risk of possible development of hypoglycemia.
The effect testosterone propionate buya independent of the functional state of the beta cells of the pancreas and insulin metabolism. It was observed positive effect testosterone propionate buya on surrogate markers of beta cell function, including HOMA index-ß (homeostasis model assessment-B) and the proinsulin to insulin ratio. In addition, extra kidney excretion of glucose causes a loss of calories, which is accompanied by a decrease in the volume of adipose tissue and weight loss.
Glycosuria, observed during the application testosterone propionate buya, accompanied by a slight increase in urine output, which can contribute to a moderate reduction in blood pressure.
In clinical studies, where testosterone propionate buy used as monotherapy; combination therapy with metformin; combination therapy with metformin and a sulfonylurea; metformin combination therapy compared with glimepiride; combination therapy with metformin +/- pioglitazone; as a combination therapy with the inhibitor of dipeptidyl peptidase-4 (DPP-4) +/- metformin other oral hypoglycemic medication; as a combination therapy with insulin it has been proven statistically significant decrease HbAlc glycated hemoglobin and reduced fasting plasma glucose concentration.
Pharmacokinetics testosterone propionate buya been comprehensively studied in healthy volunteers and patients with diabetes 2. Suction testosterone propionate buy after intake of rapidly absorbed, the maximum concentration testosterone propionate buya in plasma (C max ) was achieved after 1.5 hours. Then concentration testosterone propionate buya plasma decreased in two stages. After receiving testosterone propionate buya average value of the area under the curve “concentration-time» (AUC) in the period of sustained plasma concentration was 4,740 nmol • h / L and the value of C max – 687 nmol / l . Pharmacokinetics testosterone propionate buya in healthy volunteers and in patients with type 2 diabetes was generally similar. food intake has no clinically meaningful effect on the pharmacokinetics testosterone propionate buya. distribution The volume of distribution during the stable plasma concentration was approximately 73.8 liters. After oral administration in healthy volunteers testosterone propionate buya labeled [ 14 C] binding to plasma proteins is 86%. Metabolism The main pathway testosterone propionate buya a person – glucuronidation with uridine-5′-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 and UGT1A9. The most frequently reported are the three metabolites testosterone propionate buya glucuronic conjugate (2-0, 3-0 and 6-0 glucuronide). The systemic impact of each metabolite is low (less than 10% of the total impact of testosterone propionate buya). Elimination half-life was approximately 12.4 hours. In the case of testosterone propionate buya once daily sustained plasma concentration is reached after the fifth dose. After oral administration testosterone propionate buya labeled [ 14 C] in healthy volunteers excreted about 96% of the dose (41% through the intestines and kidneys 54%). A large part of the intestine labeled drug is excreted unchanged. Kidney in unchanged output is only half of the labeled product. Pharmacokinetics in special patient populationsRenal impairment In patients with renal insufficiency, mild, moderate and severe degrees of severity (30 <GFR <90 mL / min / 1.73 m 2 ) and patients with AUC values of end-stage renal failure testosterone propionate buya increased, respectively, by approximately 18%, 20%, 66% and 48% as compared to patients with normal renal function. In patients with renal failure and moderate severity in patients with end stage renal failure testosterone propionate buya maximum concentration in the plasma it was similar to the corresponding values in patients with normal renal function. In patients with renal insufficiency mild to severe testosterone propionate buya maximum concentration in the plasma was about 20% higher than in patients with normal renal function. These population pharmacokinetic analysis showed that total clearance testosterone propionate buya decreased with decreasing GFR, which led to increased exposure to the drug. Disturbances of liver function in patients with impaired hepatic function mild, moderate and severe degrees of severity (according to the classification of Child-Pugh) AUC values testosterone propionate buya increased respectively, about 23%, 47% and 75% and the values of Cmax, respectively, by approximately 4%, 23% and 48% (compared with patients with normal liver function). body mass index, gender, race and age has no clinically meaningful effect on the pharmacokinetics testosterone propionate buya. children pharmacokinetic studies have not been conducted testosterone propionate buya children.
Type 2 Diabetes:
- as monotherapy in patients with inadequate glycemic control on diet only and exercise background, whom metformin is considered inappropriate in view of intolerance;
- as a combination therapy with other hypoglycemic agents, including insulin therapy when used in conjunction with diet and exercise does not provide the desired glycemic control.
- Hypersensitivity to any component of the drug;
- Type 1 diabetes;
- Diabetic ketoacidosis;
- Rare hereditary disorders (lactase deficiency, lactose intolerance, glucose-galactose malabsorption);
- Renal failure with GFR <45 mL / min per 1.73 m 2 (due to inefficiency);
- Pregnancy and breast-feeding;
- Age older than 85 years;
- Use in combination with analogues of glucagon-like peptide 1 (due to lack of efficacy and safety data);
- Children under the age of 18 years (due to lack of efficacy and safety data).
- Patients at risk of developing hypovolemia (use of antihypertensive drugs cases of arterial hypotension in history);
- In diseases of the gastrointestinal tract, resulting in loss of fluid;
- Age older than 75 years;
- Use in combination with sulfonylureas or insulin;
- Infections of the genitourinary system.
Use during pregnancy and during breastfeeding
Application testosterone propionate buya during pregnancy is contraindicated because of the lack of efficacy and safety data.
The data obtained in preclinical studies in animals suggest testosterone propionate buya penetration into breast milk. It is not excluded a risk of exposure to newborns and children through breastfeeding. Application testosterone propionate buya during breastfeeding is contraindicated. If necessary, use testosterone propionate buya during breast-feeding, breast-feeding should be discontinued.
Dosing and Administration
Monotherapy or combination therapy
recommended starting dose is 10 mg (one dose of 10 mg tablet) 1 time per day, orally.
In case the daily dose of 10 mg did not provide adequate glycemic control, the dose may be increased to 25 mg (1 tablet dosage 25 1 mg once a day). The maximum daily dose is 25 mg.
The drug DZHARDINS may be taken with or without food at any time of the day. Responding to the admission of reception of one or more drug doses If you forget a dose, the patient should take the drug as soon as it is to remember it. Do not take a double dose in one day. Special patient groups in renal insufficiency with a GFR of 45 to 90 mL / min / 1.73 m 2 dose adjustment is required. patients with renal insufficiency with a GFR less than 45 mL / min / 1.73 m 2 to use the drug not recommended due to inefficiency. Patients with impaired hepatic function dose adjustment is required.
The overall incidence of adverse events in patients treated with testosterone propionate buy or placebo in clinical trials was similar. The most common adverse reaction was hypoglycemia, have been reported with the use of testosterone propionate buya in combination with a sulfonylurea or insulin (see. The description of the individual adverse reactions).
Adverse reactions observed in patients treated with testosterone propionate buy in placebo-controlled trials are presented below in Table (adverse reactions were classified organs and systems in accordance with preferred in MedDRA terms) with their absolute frequency. Frequency categories are defined as follows: very common ( > 1/10), frequent (from > ; 1/100 to <1/10), infrequent (from > 1/1000 to <1/100), rare (from > 1 / 10,000 to <1/1000) or very rare (<1/10000); allocated as adverse reactions, the frequency of which is unknown (can not be estimated on the basis of available data).
|Classification of organs
|Infectious and parasitic
|Vaginal candidiasis, vulvovaginitis,
balanitis and other genital infections
Urinary tract infections
|Violations by the exchange of
substances and power
application with derivatives of
sulfonylurea or insulin)
|Violations of the kidney
and urinary tract
Description of individual adverse reactions Hypoglycaemia The frequency of hypoglycaemia depended from that used concomitant hypoglycemic therapy. Light hypoglycemia (blood glucose 3.0 – 3.8 mmol / L (54-70 mg / dL)) The incidence of mild hypoglycemia was similar in patients treated with testosterone propionate buy or placebo as monotherapy as well as in the case of adding testosterone propionate buya to metformin in the case of adding testosterone propionate buya to pioglitazone (± metformin). If testosterone propionate buya destination in combination with metformin and a sulfonylurea incidence of hypoglycemia was higher (10 mg: 10.3%; 25 mg: 7.4%) than with placebo administered in the same combination (5.3%). Weight hypoglycemia (blood glucose less than 3 mmol / l (54mg / dl)) The incidence of severe hypoglycemia was similar in patients treated with placebo and testosterone propionate buy monotherapy. If testosterone propionate buya destination in combination with metformin and a sulfonylurea incidence of hypoglycemia was higher (10 mg: 5.8%; 25 mg: 4.1%) than with placebo administered in the same combination (3.1%). Increased urination frequency pollakiuria (assessed symptoms such as pollakiuria, polyuria, nocturia) was higher in the case of testosterone propionate buya (10 mg 3.4% 25 mg 3.2%) than in the placebo application (1 %). The frequency of nocturia was similar in the group of patients who received testosterone propionate buy and in the group of patients treated with placebo (less than 1%). The intensity of these side effects were mild or moderate. Urinary tract infection incidence of urinary tract infections was similar in the case of testosterone propionate buya 25 mg and placebo (7.6%), but higher in the case of testosterone propionate buya 10 mg (9.3%). As in the case of urinary tract infection the use of placebo in patients receiving testosterone propionate buya were more common in patients with chronic and recurrent urinary tract infections in history. The intensity of urinary tract infections was similar in patients receiving placebo and testosterone propionate buy. Urinary tract infections were more frequent in women. Genital Infection Incidence of adverse events such as a vaginal candidiasis, vulvovaginal, balanitis and other genital infections was higher in the case of testosterone propionate buya (10 mg: 4.1%, 25 mg: 3, 7%) than with placebo (0.9%). Genital infections were more common in women. Genital infections intensity was weak or moderate. Hypovolaemia frequency of hypovolemia (expressed which lower blood pressure, orthostatic hypotension, dehydration, syncope) was similar in the case of testosterone propionate buya (10 mg: 0.5% at 25 mg:. 0 , 3%) and placebo (0.3%). In patients older than 75 years, the incidence of hypovolemia was similar in patients treated testosterone propionate buy 10 mg (2.3%) and placebo (2.1%), but higher in patients receiving testosterone propionate buy 25 mg (4.4% ).
During controlled clinical studies, single doses testosterone propionate buya, up to 800 mg (32 times the maximum daily dose) in healthy volunteers and multiple doses up to 100 mg (4 times the maximum daily dose) in patients with diabetes 2 were well tolerated. The observed increase in urine volume is not dependent on the dose and had no clinical significance. Experience of using a dose exceeding 800 mg, no.Treatment In case of overdose, it is recommended removal of unabsorbed drug from the gastrointestinal tract, clinical monitoring implementation and carrying out symptomatic treatment.
The interaction with other drugs Evaluation in vitro drug interactions testosterone propionate buy not inhibit not inactivate or induce isozymes CYP450. The main route of metabolism in humans is testosterone propionate buya glucuronidation with uridine-5′-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 and UGT1A9. testosterone propionate buy does not inhibit UGT1A1. Drug interactions testosterone propionate buya and drugs that are substrates of CYP450 isoenzymes and UGT1A1 are considered unlikely. testosterone propionate buy is a substrate for P-glycoprotein (P-gp) and protein that determines the resistance of breast cancer (BCRP). at therapeutic doses, but did not inhibit these proteins. Based on the data obtained in the in vitro studies, it is believed that the ability testosterone propionate buya in interactions with drugs that are substrates for P-glycoprotein (P-gp), is unlikely. testosterone propionate buy is a substrate for the organic anion transporter: OATZ, OATR1V1 and OATR1VZ, but is not a substrate for the organic anion transporter 1 (OAT1), and organic cationic transporter 2 (OST2). However, drug interactions testosterone propionate buya with drugs that are substrates for the above-described carrier proteins are considered to be unlikely. Evaluation of drug interactions in vivo pharmacokinetics testosterone propionate buya not altered in healthy volunteers in the event of a joint application with metformin, glimepiride, pioglitazone, sitagliptin, linagliptinom, warfarin, verapamil, ramipril, simvastatin, torasemide and hydrochlorothiazide. In a joint application testosterone propionate buya with gemfibrozil, rifampicin and probenecid was an increase in the AUC testosterone propionate buya 59%, 35% and 53%, respectively, but these changes were not considered clinically significant. testosterone propionate buy has no clinically meaningful effect on the pharmacokinetics of metformin, glimepiride, pioglitazone, sitagliptin , linagliptina, warfarin.digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide and oral contraceptive preparations. Diuretics testosterone propionate buy may potentiate the diuretic effect of thiazide and “loop” diuretics, which in turn may increase the risk of dehydration and hypotension. Insulin and drugs that increase its secretion of insulin and drugs enhancing secretion such as sulfonylureas, may increase the risk of hypoglycemia.Therefore, while the use testosterone propionate buya with insulin and drugs that increase the secretion of it, may need to reduce their dose to avoid the risk of hypoglycemia.
The drug DZHARDINS not recommended for use in patients with type 1 diabetes and for the treatment of diabetic ketoacidosis.
The maximum daily dose of the drug DZHARDINS contains 113 mg of lactose, and the drug should not be used in patients with these rare genetic disorders such as lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
Clinical studies have shown that treatment testosterone propionate buyom does not lead to an increase in cardiovascular risk. Application testosterone propionate buya 25 mg does not lead to a lengthening of the QT interval.
With the combined use of the drug DZHARDINS with sulfonylureas or insulin may need to reduce the dose of sulfonylurea derivatives / insulin due to the risk of hypoglycemia. Not studied combination of hypoglycemic agents testosterone propionate buy has not been studied in combination with analogs of glucagon-like peptide 1 (GLP-1). Monitoring the renal Efficiency DZHARDINS drug depends on renal function. It is therefore recommended to monitor renal function prior to appointment and periodically during treatment (at least once a year), as well as to the purpose of concomitant therapy, which may adversely affect renal function. Patients with renal impairment (GFR less than 45 ml \ min). the drug is not recommended. Elderly patients aged 75 years or more have an increased risk of dehydration. In such patients, treated with testosterone propionate buy more often (compared to patients treated with placebo) observed adverse reactions caused by hypovolemia. Experience with testosterone propionate buya in patients older than 85 years is limited, therefore it is not recommended to prescribe a drug DZHARDINS patients older than 85 years. Use in patients at risk for hypovolemia According to the mechanism of action of the drug DZHARDINS intake can lead to a moderate reduction in blood pressure. Therefore, the drug should be used with caution in those cases where the blood pressure decrease is not desirable, for example, in patients with cardiovascular diseases; patients taking antihypertensive drugs (cases of arterial hypotension in history), and in patients older than 75 years. In the event that a patient receiving the drug DZHARDINS.developing conditions that can lead to fluid loss (e.g., diseases of the gastrointestinal tract), should be carefully monitored condition of the patient, blood pressure, and also to control electrolyte balance and hematocrit. It may require temporary until rehydration, discontinuation of the drug. Urinary tract infection incidence of side effects such as urinary tract infections, was comparable when using testosterone propionate buya 25 mg and placebo, and higher with testosterone propionate buya 10 mg. Complicated urinary tract infections (such as pyelonephritis and urosepsis) have been reported with similar frequency in patients receiving placebo and testosterone propionate buy. In the case of complicated urinary tract infections must be testosterone propionate buyom temporary cessation of therapy. Laboratory analysis of urine According to the mechanism of action in patients taking the drug DZHARDINS determined glucose in the urine.
Effects on ability to drive vehicles and mechanisms of
clinical studies on the effect of testosterone propionate buya on ability to drive and use machinery has not been. Patients should use caution when driving and mechanisms as well as the application of DZHARDINS preparation (especially in combination with a sulfonylurea and / or insulin) may develop hypoglycaemia. steroids side effects