Teveten pills 600 mg 14 pcs
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Active ingredients
Eprosartan
Release form
Pills
Composition
Active ingredient: Eprosartan (Eprosartan) Active ingredient concentration (mg): 600
Pharmacological effect
An antihypertensive agent, a synthetic angiotensin ii receptor antagonist, a non-biphenyl tetrazole derivative, eprosartan binds selectively to the at1 receptors located in the vessels, heart, kidney, and adrenal cortex, forms a strong bond with them, followed by slow dissociation. many tissues (including vascular smooth muscle, adrenal glands, kidneys, heart) and causes vasoconstriction, sodium retention and release of aldosterone, target organ damage - hyper rofiyu sosudov.eprosartan infarction and prevents the development of or reduces the effects of angiotensin ii. inhibits the activity of raas. has vasodilating, hypotensive and indirectly - diuretic effect. reduces arterial vasoconstriction, ops, pressure in the pulmonary circulation, reabsorption of fluid and sodium ions in the proximal segment of the renal tubules, aldosterone secretion. with prolonged use, it inhibits the proliferative effect of angiotensin ii on vascular smooth muscle cells and myocardium. Eprosartan does not affect the concentration of Tg, total cholesterol (xc) or xc-lpnp in the blood, determined by an empty stomach, in patients with arterial hypertension. in addition, eprosartan does not affect the concentration of glucose in the blood on an empty stomach. It increases the renal blood flow and glomerular filtration rate, reduces the excretion of albumin (nephroprotective effect), while maintaining renal self-regulation, regardless of the severity of renal insufficiency. does not inhibit the isoenzymes cyp1a, 2a6, 2c9 / 8, 2c19, 2d6, 2e, and 3a in vitro. The hypotensive effect after taking a single dose lasts for 24 hours; The cue effect appears when taken regularly - after 2-3 weeks without changing the heart rate.
Pharmacokinetics
After ingestion of a single dose of 300 mg, bioavailability is approximately 13%. When taking eprosartan simultaneously with food, a clinically insignificant decrease in absorption (less than 25%), Cmax in the blood plasma and AUC values are observed. Cmax is reached in 1-2 hours.Plasma protein binding is 98% and is constant in the range of therapeutic concentrations. It is excreted in breast milk. Vd - 13 liters, total clearance - 130 ml / min. Virtually no accumulation. T1 / 2 is 5-9 hours. It is mainly eliminated unchanged through the intestines (90%), kidneys (7%). A small part (less than 2%) is excreted by the kidneys in the form of glucuronides. 20% of the concentration in the urine is the acylglucuronide of eprosartan, 80% is unchanged eprosartan. In the elderly, the values of Сmax and AUC increase on average by 2 times, which does not require correction of the dosage regimen. In case of chronic renal failure of moderate severity (CC from 30 to 59 ml / min), AUC and Cmax values are 30%, and in severe cases (CC from 5 to 29 ml / min) - 50% higher than in healthy people. When liver failure after oral administration of a single dose of AUC (but not Cmax) increases by almost 40% compared with healthy people. It is practically not displayed in hemodialysis (clearance is less than 1 l / h).
Indications
Arterial hypertension.
Contraindications
Hypersensitivity to the drug; pregnancy; lactation period; age up to 18 years (efficacy and safety not established); hemodynamically significant bilateral renal artery stenosis and arterial stenosis of a single kidney. Lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (the product contains lactose monohydrate).
Precautionary measures
During the treatment of hypertension, care must be taken when driving motor vehicles and engaging in potentially hazardous activities that require increased concentration and psychomotor speed, due to the fact that dizziness and weakness may occur.
Use during pregnancy and lactation
Contraindicated use during pregnancy and lactation (breastfeeding).
Dosage and administration
Inside, regardless of the meal. The recommended daily dose is 1 tablet of Tevetin 1 time a day in the morning. The maximum reduction in blood pressure (BP) in most patients is achieved after 2-3 weeks of treatment. The maximum daily dose is 1200 mg. Dose adjustment is not required for elderly patients and patients with impaired liver function. For patients with moderate renal failure (QA less than 60 ml / min.), The daily dose should not exceed 600 mg. The duration of use of the drug is not limited.
Side effects
From the side of the central nervous system: very often - headache, often - dizziness, asthenia. Since the cardiovascular system: infrequently - a pronounced decrease in blood pressure. On the part of the skin and subcutaneous fat: often - allergic skin reactions (eg, skin rash, itching), rarely - angioedema (including the face, lips, tongue, pharynx). On the part of the digestive system: often - non-specific complaints of the gastrointestinal tract (for example, nausea, diarrhea, vomiting). On the part of the immune system: infrequently - hypersensitivity. On the part of the urogenital system: impaired renal function, including acute renal failure, especially in patients at risk (for example, with renal artery stenosis).
Overdose
There is only limited data on overdose. The drug is well tolerated when taken orally. The effectiveness of daily doses up to 1200 mg is shown when taken for 8 weeks and there are no reports of a clear dependence of the frequency of adverse effects on the dose. Symptoms: a pronounced decrease in blood pressure is possible. Treatment: symptomatic therapy.
Interaction with other drugs
Eprosartan can be used in combination with thiazide diuretics (including hydrochlorothiazide) and slow calcium channel blockers (including long-acting nifedipine) without expecting a clinically significant undesirable interaction, and the hypotensive effect is mutually reinforced. use of eprosartan with potassium-sparing diuretics, nutritional supplements containing potassium, salt substitutes containing potassium, and other drugs that increase the level of potassium in blood serum ( for example, heparin) may increase the level of potassium in the serum. During treatment with drugs that affect the RAAS, hyperkalemia may develop, especially in patients with renal and / or liver failure. The antihypertensive effect of eprosartan can be potentiated by other antihypertensive drugs. There are cases of a reversible increase in serum lithium concentration and the development of toxic reactions while taking lithium preparations with ACE inhibitors.The possibility of a similar effect after taking eprosartan cannot be ruled out (with this combination, it is recommended to control the concentration of lithium in the blood plasma). When eprosartan is used simultaneously with NSAIDs, there is a likelihood of kidney function deterioration, including the risk of developing acute renal failure, and an increase in serum potassium in patients with already existing renal dysfunction (these combinations should be used with caution, especially in elderly patients; control fun kidney Keying).
special instructions
It is not recommended to use for the treatment of patients with primary hyper aldosteronism. It is used with caution in severe chronic heart failure (functional class IV of the NYHA classification); reducing bcc and / or excessive removal of sodium chloride from the body (including as a result of vomiting, diarrhea, taking high doses of diuretics); in patients on hemodialysis or with CC less than 30 ml / min; with aortic and mitral valve stenosis, as well as with hypertrophic cardiomyopathy. Use with extreme caution in patients with impaired liver function and ischemic heart disease, due to insufficient clinical experience with these categories of patients. There is no data on the use of eprosartan in patients with end-stage renal deficiency and recent kidney transplantation.