Pharmacodynamics active hormone RAAS is Angiotensin II, which is formed from angiotensin I involving ACE. Angiotensin II binds to specific receptors on cell membranes in various tissues. It buy trenbolone enanthate has a wide range of physiological effects, including in the first place as a direct or indirect involvement in the regulation of blood pressure (BP).
As a potent vasoconstrictor, angiotensin II causes a direct pressor response. In addition, it promotes sodium retention and stimulates aldosterone secretion.
buy trenbolone enanthate – a specific angiotensin II receptor antagonist intended for oral administration. It has an antagonistic effect selectively on the AT receptor subtype 1 , which is responsible for the known effects of angiotensin II. The consequence of the blockade of the AT 1 receptor is to increase the plasma buy trenbolone enanthate concentrations of angiotensin II, which may stimulate the unblocked AT 2 – receptors. It does not any agonist activity expressed in relation to AT 1 – receptors. buy trenbolone enanthate affinity receptor subtype AT 1 approximately 20 000 times higher than that of AT receptor subtype 2 .
In the treatment of patients with buy trenbolone enanthate hypertension observed blood pressure reduction is not accompanied by a change in heart rate. After assigning a single dose into most patients onset of antihypertensive action observed within 2 hours, and the maximum decrease in blood pressure is achieved within 4-6 hours. After ingestion antihypertensive effect persists for more than 24 hours. Repeated use of the drug the maximum reduction in blood pressure, regardless of the dose, usually achieved within 2-4 weeks and maintained at that level during prolonged therapy.
Sudden discontinuation of buy trenbolone enanthate is not accompanied by a sharp increase in blood pressure or other adverse clinical consequences.
Following oral administration of buy trenbolone enanthate absorption occurs rapidly, but the extent of absorption varies widely. The average value of the absolute bioavailability of buy trenbolone enanthate is 23%.
Pharmacokinetic curve is downward multieksponentsialny character (t 1 / 2a <1 h and t 1 / 2β about 9 hours).
In the range of doses studied the kinetics of buy trenbolone enanthate is linear. Repeated use of the drug changes the kinetic parameters were noted. When taking the drug once a day, a slight accumulation. Drug concentrations in the blood plasma in women and men were similar.
buy trenbolone enanthate largely (by 94-97%) binds to serum proteins, mainly albumin. The volume of distribution during the equilibrium state is low (about 17 L). Compared to the liver blood flow (about 30 liters / hour), buy trenbolone enanthate plasma clearance occurs relatively slowly (about 2 liters / hour). The amount of buy trenbolone enanthate which is excreted in the feces, accounting for 70% (on the amount of an oral dose). With urine output of about 30%, mainly in unchanged form.
Pharmacokinetics in specific patient groups Patients elderly Some elderly patients systemic exposure to buy trenbolone enanthate was somewhat more pronounced than in young patients, however, did not show any clinical relevance of this. Patients with renal impairment There was no correlation between the function kidney and systemic exposure to buy trenbolone enanthate was to be expected, given that for the substance renal clearance accounts for only 30% of the total clearance. Therefore, in patients with impaired renal function dose adjustment is required. However, buy trenbolone enanthate has a high degree of binding to plasma proteins, so its removal by hemodialysis is unlikely. Patients with hepatic impairment Approximately 70% of the sucked dose is excreted in the bile, mostly unchanged. buy trenbolone enanthate significant biotransformation is not exposed, and as can be expected, the systemic exposure of buy trenbolone enanthate is not correlated with the degree of liver function. Therefore, in patients with hepatic insufficiency nebiliarnogo origin and without cholestasis does not require dose adjustment valsaforsa.
- Arterial hypertension
- Chronic heart failure (II-IV functional class NYHA classification) in patients receiving standard therapy, including diuretics, digitalis preparations, as well as ACE inhibitors or beta-blockers (not simultaneously).
Use of each of these drugs is not necessary.
Hypersensitivity to any component of the drug.
Pregnancy, lactation, age 18 years (effectiveness and safety have not been established).
Lactose intolerance, galactosemia or malabsorption syndrome glucose / galactose.
Precautions : a bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, with a diet with sodium restriction, for conditions involving reduction in circulating blood volume (including diarrhea, vomiting), hepatic insufficiency on the background of obstruction of the biliary tract, renal insufficiency (creatinine clearance less than 10 ml / min.), hemodialysis.
Dosing and Administration
Take the pill inside, not liquid, regardless of the meal. When hypertension The recommended dose is 80 mg 1 time per day. Antigipertendozy preparation is required. Valsafors can be administered jointly with other antihypertensive agents. In chronic heart failure. The recommended starting dose is 40 mg 2 times a day. Possibly a gradual increase in the dose to 80 mg 2 times daily, if tolerated – 160 mg 2 times a day. The maximum daily dose – 320 mg, divided into 2 doses. In patients concurrently treated with diuretics, and in patients with chronic heart failure requires regular monitoring of renal function, blood pressure. When clinical signs of hypotension, the dose should be reduced.
On the part of the central nervous system: often – headache, dizziness, including postural, vertigo; rarely – insomnia; sometimes – syncope (when used after myocardial infarction). The respiratory system:often – cough, infections of the upper respiratory tract, pharyngitis, rhinitis, sinusitis. Since the cardiovascular system: often – pronounced reduction in blood pressure and orthostatic hypotension; sometimes (when used after myocardial infarction) – heart failure. On the part of the gastrointestinal tract: often – nausea, diarrhea, abdominal pain. For the skin and subcutaneous fat: seldom – skin rash. On the part of the musculoskeletal system: often – back pain, myalgia, arthralgia. From the urogenital system: rarely – decreased libido; very rarely – renal dysfunction. Allergic reactions: seldom – angioedema, skin rash, itching, hypersensitivity reactions including serum sickness, and vasculitis. From the laboratory parameters: rare – decrease in hemoglobin concentration and hematocrit, neutropenia, thrombocytopenia, hypercreatininemia, hyperbilirubinemia, increased activity of “liver” transaminases, increases in serum urea nitrogen; . often – hyperkalemia Other: often – general weakness; Infrequent – edema, asthenia, fatigue.
Symptoms: . Marked reduction of blood pressure treatment: if the drug was passed recently, induce vomiting. In marked decrease in blood pressure – intravenous infusion of normal saline. It is unlikely that buy trenbolone enanthate can be derived from the body by hemodialysis.
Interaction with other drugs
Clinically significant interactions with such drugs as: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, and glibenclamide have been identified.
As buy trenbolone enanthate is not exposed to any significant metabolism, for it is unlikely clinically significant interactions with other drugs on the level of metabolism that are due to inhibition or induction of cytochrome P450. Despite the fact that buy trenbolone enanthate largely bound to plasma proteins does not reveal any significant interaction of diclofenac, furosemide, and warfarin. The simultaneous use of potassium-sparing diuretics (e.g., spironolactone, triamterene, amiloride), potassium salts or formulations containing potassium, may lead to increased concentration of potassium in blood serum. If such a combination treatment considered necessary, caution should be exercised.
The deficit in the sodium the body and / or reduced blood volume (CBV)
in patients with severe deficiency in sodium the body and / or reduced BCC, for example, receiving high doses of diuretics, in rare cases, early treatment Valsaforsom may occur symptomatic hypotension.
Before treatment should carry out the correction contents in the body of sodium and / or blood volume, for example, by reducing the dose of a diuretic. In the case of arterial hypotension, the patient must be placed on the back, and, if necessary, to an intravenous infusion of saline. After the blood pressure has stabilized, the treatment can be continued. Renal artery stenosis Given that other drugs that affect the renin-aldosterone system (RAAS) can cause increased levels of urea and serum creatinine in patients with bilateral or unilateral renal artery stenosis , as a precaution we recommend a systematic monitoring of these indicators. renal function impairment Patients with impaired renal function does not require adjustment of dosage. However, when expressed violations (when creatinine clearance less than 10 ml / min.) Is recommended to be careful. Abnormal liver function in patients with hepatic impairment is not required correction dose. buy trenbolone enanthate is derived mainly unchanged in the bile, but in patients with biliary tract obstruction clearance of buy trenbolone enanthate reduced. In appointing the drug to these patients should be particularly careful. Congestive heart failure due to inhibition of the RAAS in patients sensitive to changes in renal function. In patients with severe chronic heart failure treatment with ACE inhibitors and angiotensin receptor antagonists may be associated with oliguria and / or increase of azotemia and (rarely) with acute renal failure and / or death. Therefore, an evaluation of the degree of impairment of renal function in patients with heart failure.
Effects on ability to drive a car and operate machinery .
In appointing valsaforsa, as well as other antihypertensive agents, it is advisable to use caution when driving and control mechanisms that require attention and speed of psychomotor reactions.