Telpres Plus tablets 40 mg + 12.5 mg 98 pcs. (Hydrohlorotyazyd, Telmisartan)
Special Price
$29.75
Regular Price
$35.00
In stock
SKU
newyork930784
Pharmacological action
Pharmacotherapeutic group: Combined antihypertensive (angiotensin II receptor antagonist + diuretic)
ATX:
C.09.DA07 Telmisartan in combination with
diuretics Pharmacodynamics:
Telpres Plus is a combination of telmisartan (an angiotensin II receptor antagonist) and hydrochlorothiazide - a thiazide diuretic. The simultaneous use of these components leads to a more pronounced antihypertensive effect than the use of each of them separately.
Taking Telpres Plus once a day leads to a significant gradual decrease in blood pressure (BP).
Telmisartan
Telmisartan is a specific angiotensin II receptor antagonist (type AT1) that is effective when taken orally. It has a high affinity for the AT 1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from the connection with the receptor, not possessing the action of an agonist in relation to this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, the concentration of which increases with the appointment of telmisartan, has not been studied. It reduces the concentration of aldosterone in the blood, does not inhibit renin in blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, amplification of the side effects caused by bradykinin is not expected.
In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first oral administration of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.
In patients with arterial hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting heart rate (HR).
In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome.
Hydrochlorothiazide
Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides (approximately in equivalent amounts). The diuretic effect of hydrochlorothiazide leads to a decrease in the volume of circulating blood (BCC), an increase in plasma renin activity, an increase in the secretion of aldosterone, followed by an increase in urine potassium and hydrogen carbonates and, as a result, a decrease in potassium in blood plasma. With simultaneous administration with telmisartan, there is a tendency to stop the loss of potassium caused by these diuretics, presumably due to the blockade of the renin-angiotensin-aldosterone system (RAAS). After oral administration, diuresis increases after 2 hours, and the maximum effect is observed after about 4 hours. The diuretic effect of the drug persists for approximately 6-12 hours.
Long-term use of hydrochlorothiazide reduces the risk of complications of cardiovascular disease and mortality from them.
The maximum antihypertensive effect of Telpres Plus is usually achieved 4-8 weeks after the start of treatment.
Pharmacokinetics:
The combined use of telmisartan and hydrochlorothiazide does not affect the pharmacokinetics of each of the components of the drug.
Telmisartan:
Absorption
When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (the area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma is leveled regardless of the meal.
Distribution of
Communication with plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in equilibrium concentration is 500 l.
Metabolism
Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.
Withdrawal
Elimination half-life (T1 / 2) - more than 20 hours. It is excreted through the intestine unchanged, excretion by the kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min) compared with hepatic blood flow (about 1500 ml / min).
Pharmacokinetics in special patient groups
Gender differences
There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared with men without significant impact on effectiveness. Dose adjustment is not required.
Elderly patients
The pharmacokinetics of telmisartan in elderly patients are not different from younger patients. Dose adjustment is not required.
Patients with impaired renal function
In patients with mild to moderate impaired renal function, dose adjustment of telmisartan is not required.
Patients with severe renal impairment and those on hemodialysis are recommended a lower initial dose of 20 mg per day. Telmisartan is not excreted by hemodialysis.
Patients with impaired liver function
Pharmacokinetics studies in patients with hepatic impairment showed an increase in the absolute bioavailability of telmisartan to almost 100%. With liver failure, T1 / 2 does not change. In patients with mild to moderate impaired liver function (class A and B on the Child-Pugh scale), the daily dose should not exceed 40 mg.
Hydrochlorothiazide:
After oral administration of Telpres Plus, the maximum plasma concentrations of hydrochlorothiazide are reached within 1-3 hours. Absolute bioavailability based on total kidney excretion is about 60%. It is bound by blood plasma proteins to 64% hydrochlorothiazide, and the distribution volume is 0.8 В± 0.3 l / kg. Hydrochlorothiazide is not metabolized in the body and excreted by the kidneys almost unchanged. About 60% of the dose taken orally is eliminated within 48 hours. Renal clearance of about 250-300 ml / min. T1L hydrochlorothiazide - 10 - 15 hours. There is a difference in plasma concentrations in men and women. In women, the concentration of telmisartan in plasma is 2-3 times higher than in men, and women have a tendency to increase the concentration of hydrochlorothiazide in the blood plasma is clinically insignificant.
Patients with impaired renal function
In patients with impaired renal function, the rate of elimination of hydrochlorothiazide is reduced.
Studies in patients with creatinine clearance (CC) of 90 ml / min showed that T1 / 2 of hydrochlorothiazide is increased. In patients with impaired T1 / 2 renal function, about 34 hours. Buy Telpres Plus tablets 40 mg + 12.5 mg 98 pcs. (Hydrohlorotyazyd, Telmisartan) in newyork free shipping. Fast international shipping USA, AU, EU, UK and others.
Pharmacotherapeutic group: Combined antihypertensive (angiotensin II receptor antagonist + diuretic)
ATX:
C.09.DA07 Telmisartan in combination with
diuretics Pharmacodynamics:
Telpres Plus is a combination of telmisartan (an angiotensin II receptor antagonist) and hydrochlorothiazide - a thiazide diuretic. The simultaneous use of these components leads to a more pronounced antihypertensive effect than the use of each of them separately.
Taking Telpres Plus once a day leads to a significant gradual decrease in blood pressure (BP).
Telmisartan
Telmisartan is a specific angiotensin II receptor antagonist (type AT1) that is effective when taken orally. It has a high affinity for the AT 1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from the connection with the receptor, not possessing the action of an agonist in relation to this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, the concentration of which increases with the appointment of telmisartan, has not been studied. It reduces the concentration of aldosterone in the blood, does not inhibit renin in blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, amplification of the side effects caused by bradykinin is not expected.
In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first oral administration of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.
In patients with arterial hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting heart rate (HR).
In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome.
Hydrochlorothiazide
Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides (approximately in equivalent amounts). The diuretic effect of hydrochlorothiazide leads to a decrease in the volume of circulating blood (BCC), an increase in plasma renin activity, an increase in the secretion of aldosterone, followed by an increase in urine potassium and hydrogen carbonates and, as a result, a decrease in potassium in blood plasma. With simultaneous administration with telmisartan, there is a tendency to stop the loss of potassium caused by these diuretics, presumably due to the blockade of the renin-angiotensin-aldosterone system (RAAS). After oral administration, diuresis increases after 2 hours, and the maximum effect is observed after about 4 hours. The diuretic effect of the drug persists for approximately 6-12 hours.
Long-term use of hydrochlorothiazide reduces the risk of complications of cardiovascular disease and mortality from them.
The maximum antihypertensive effect of Telpres Plus is usually achieved 4-8 weeks after the start of treatment.
Pharmacokinetics:
The combined use of telmisartan and hydrochlorothiazide does not affect the pharmacokinetics of each of the components of the drug.
Telmisartan:
Absorption
When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (the area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma is leveled regardless of the meal.
Distribution of
Communication with plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in equilibrium concentration is 500 l.
Metabolism
Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.
Withdrawal
Elimination half-life (T1 / 2) - more than 20 hours. It is excreted through the intestine unchanged, excretion by the kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min) compared with hepatic blood flow (about 1500 ml / min).
Pharmacokinetics in special patient groups
Gender differences
There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared with men without significant impact on effectiveness. Dose adjustment is not required.
Elderly patients
The pharmacokinetics of telmisartan in elderly patients are not different from younger patients. Dose adjustment is not required.
Patients with impaired renal function
In patients with mild to moderate impaired renal function, dose adjustment of telmisartan is not required.
Patients with severe renal impairment and those on hemodialysis are recommended a lower initial dose of 20 mg per day. Telmisartan is not excreted by hemodialysis.
Patients with impaired liver function
Pharmacokinetics studies in patients with hepatic impairment showed an increase in the absolute bioavailability of telmisartan to almost 100%. With liver failure, T1 / 2 does not change. In patients with mild to moderate impaired liver function (class A and B on the Child-Pugh scale), the daily dose should not exceed 40 mg.
Hydrochlorothiazide:
After oral administration of Telpres Plus, the maximum plasma concentrations of hydrochlorothiazide are reached within 1-3 hours. Absolute bioavailability based on total kidney excretion is about 60%. It is bound by blood plasma proteins to 64% hydrochlorothiazide, and the distribution volume is 0.8 В± 0.3 l / kg. Hydrochlorothiazide is not metabolized in the body and excreted by the kidneys almost unchanged. About 60% of the dose taken orally is eliminated within 48 hours. Renal clearance of about 250-300 ml / min. T1L hydrochlorothiazide - 10 - 15 hours. There is a difference in plasma concentrations in men and women. In women, the concentration of telmisartan in plasma is 2-3 times higher than in men, and women have a tendency to increase the concentration of hydrochlorothiazide in the blood plasma is clinically insignificant.
Patients with impaired renal function
In patients with impaired renal function, the rate of elimination of hydrochlorothiazide is reduced.
Studies in patients with creatinine clearance (CC) of 90 ml / min showed that T1 / 2 of hydrochlorothiazide is increased. In patients with impaired T1 / 2 renal function, about 34 hours. Buy Telpres Plus tablets 40 mg + 12.5 mg 98 pcs. (Hydrohlorotyazyd, Telmisartan) in newyork free shipping. Fast international shipping USA, AU, EU, UK and others.
Pharmacological action
Pharmacotherapeutic group: Combined antihypertensive (angiotensin II receptor antagonist + diuretic)
ATX:
C.09.DA07 Telmisartan in combination with
diuretics Pharmacodynamics:
Telpres Plus is a combination of telmisartan (an angiotensin II receptor antagonist) and hydrochlorothiazide - a thiazide diuretic. The simultaneous use of these components leads to a more pronounced antihypertensive effect than the use of each of them separately.
Taking Telpres Plus once a day leads to a significant gradual decrease in blood pressure (BP).
Telmisartan
Telmisartan is a specific angiotensin II receptor antagonist (type AT1) that is effective when taken orally. It has a high affinity for the AT 1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from the connection with the receptor, not possessing the action of an agonist in relation to this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, the concentration of which increases with the appointment of telmisartan, has not been studied. It reduces the concentration of aldosterone in the blood, does not inhibit renin in blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, amplification of the side effects caused by bradykinin is not expected.
In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first oral administration of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.
In patients with arterial hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting heart rate (HR).
In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome.
Hydrochlorothiazide
Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides (approximately in equivalent amounts). The diuretic effect of hydrochlorothiazide leads to a decrease in the volume of circulating blood (BCC), an increase in plasma renin activity, an increase in the secretion of aldosterone, followed by an increase in urine potassium and hydrogen carbonates and, as a result, a decrease in potassium in blood plasma. With simultaneous administration with telmisartan, there is a tendency to stop the loss of potassium caused by these diuretics, presumably due to the blockade of the renin-angiotensin-aldosterone system (RAAS). After oral administration, diuresis increases after 2 hours, and the maximum effect is observed after about 4 hours. The diuretic effect of the drug persists for approximately 6-12 hours.
Long-term use of hydrochlorothiazide reduces the risk of complications of cardiovascular disease and mortality from them.
The maximum antihypertensive effect of Telpres Plus is usually achieved 4-8 weeks after the start of treatment.
Pharmacokinetics:
The combined use of telmisartan and hydrochlorothiazide does not affect the pharmacokinetics of each of the components of the drug.
Telmisartan:
Absorption
When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (the area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma is leveled regardless of the meal.
Distribution of
Communication with plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in equilibrium concentration is 500 l.
Metabolism
Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.
Withdrawal
Elimination half-life (T1 / 2) - more than 20 hours. It is excreted through the intestine unchanged, excretion by the kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min) compared with hepatic blood flow (about 1500 ml / min).
Pharmacokinetics in special patient groups
Gender differences
There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared with men without significant impact on effectiveness. Dose adjustment is not required.
Elderly patients
The pharmacokinetics of telmisartan in elderly patients are not different from younger patients. Dose adjustment is not required.
Patients with impaired renal function
In patients with mild to moderate impaired renal function, dose adjustment of telmisartan is not required.
Patients with severe renal impairment and those on hemodialysis are recommended a lower initial dose of 20 mg per day. Telmisartan is not excreted by hemodialysis.
Patients with impaired liver function
Pharmacokinetics studies in patients with hepatic impairment showed an increase in the absolute bioavailability of telmisartan to almost 100%. With liver failure, T1 / 2 does not change. In patients with mild to moderate impaired liver function (class A and B on the Child-Pugh scale), the daily dose should not exceed 40 mg.
Hydrochlorothiazide:
After oral administration of Telpres Plus, the maximum plasma concentrations of hydrochlorothiazide are reached within 1-3 hours. Absolute bioavailability based on total kidney excretion is about 60%. It is bound by blood plasma proteins to 64% hydrochlorothiazide, and the distribution volume is 0.8 В± 0.3 l / kg. Hydrochlorothiazide is not metabolized in the body and excreted by the kidneys almost unchanged. About 60% of the dose taken orally is eliminated within 48 hours. Renal clearance of about 250-300 ml / min. T1L hydrochlorothiazide - 10 - 15 hours. There is a difference in plasma concentrations in men and women. In women, the concentration of telmisartan in plasma is 2-3 times higher than in men, and women have a tendency to increase the concentration of hydrochlorothiazide in the blood plasma is clinically insignificant.
Patients with impaired renal function
In patients with impaired renal function, the rate of elimination of hydrochlorothiazide is reduced.
Studies in patients with creatinine clearance (CC) of 90 ml / min showed that T1 / 2 of hydrochlorothiazide is increased. In patients with impaired T1 / 2 renal function, about 34 hours.
Indications
Arterial hypertension (in the case of inefficiency of telmisartan or hydrochlorothiazide in monotherapy).
Contraindications
- Hypersensitivity to the active substances or auxiliary components of the drug or other sulfonamide derivatives
- Pregnancy
- Breastfeeding period
- Obstructive biliary tract disease
- Severe class) Severe dysfunction impaired renal function (CC less than 30 ml / min)
- Refractory hypokalemia, hypercalcemia
- Concomitant use with aliskiren in patients with diabetes mellitus and / or usheniem renal function (glomerular filtration rate of less than 60 ml / min / 1.73 m2)
- Simultaneous use of ACE in patients with diabetic nephropathy
inhibitors - lactase deficiency, lactose intolerance,
glucose-galactose malabsorption syndrome - Age under 18 years (efficacy and safety not established).
Caution:
- Bilateral renal artery stenosis or stenosis of a single kidney artery (see Special instructions)
- Hepatic function impairment (Class A and B according to the Child-Pugh classification) (see Special instructions)
- Decreased BCC due to previous diuretic therapy, restrictions on the intake of salt, diarrhea or vomiting
- Hyperkalemia
- Condition after kidney transplantation (no experience with application)
- Chronic heart failure III-IV functional class (FC) according to the classification of the New York Cardiology Association
- Hypercalcemia
- Hypercholesterolemia - Hypercholesterolemia heart
- Progressive liver disease (risk of hepatic coma)
- Aortic and mitral valve stenosis
- Idiopathic hypertrophic subaortic stenosis (hypertrophic Skye obstructive cardiomyopathy)
- Diabetes
- Primary aldosteronism
- Gout
Composition
Each tablet 12.5 mg + 80 mg contains:
active ingredients: hydrochlorothiazide - 12.50 mg, telmisartan - 80.00 mg excipients: mannitol - 327.70 mg, povidone-K25 - 21.60 mg , crospovidone - 40.0 mg, magnesium stearate - 8.50 mg, meglumine - 24.00 mg, sodium hydroxide - 6.70 mg, lactose monohydrate - 49.84 mg, microcrystalline cellulose - 32.00 mg, hypromellose - 3.00 mg, sodium carboxymethyl starch, type A - 2.00 mg, iron red oxide (E 172) - 0.17 mg.
Dosage and administration
Inside, regardless of the meal time.
The drug Telpres Plus must be taken once a day.
- Telpres Plus 12.5 / 40 mg may be prescribed to patients in whom the use of telmisartan preparations in a dosage of 40 mg or hydrochlorothiazide does not lead to adequate control of blood pressure.
- Telpres Plus 12.5 / 80 mg may be prescribed to patients in which the use of telmisartan preparations in a dosage of 80 mg or Telpres Plus 12.5 / 40 mg does not lead to adequate control of blood pressure.
- Telpres Plus 25/80 mg can be prescribed to patients in whom the use of telmisartan preparations in a dosage of 80 mg or Telpres Plus 12.5 / 80 mg drug does not lead to adequate control of blood pressure, or to patients whose condition has previously been stabilized by telmisartan or hydrochlorothiazide with separate application.
In patients with severe arterial hypertension, the maximum daily dose of telmisartan is 160 mg in combination with hydrochlorothiazide in a daily dose of 12.5-25 mg.
Impaired renal function
Limited experience with Telpres Plus in patients with mild to moderate renal impairment does not require dose changes in these cases. In such patients, renal function should be monitored (with CC less than 30 ml / min, see section Contraindications).
Impaired liver function
In patients with mild to moderate impaired liver function (Child-Pugh Class A and B), the daily dose of Telpres Plus should not exceed 12.5 / 40 mg per day (see Pharmacokinetics section).
Elderly patients
Dosage regimen does not require changes.
Overdose
Information on overdose is limited. Possible symptoms of an overdose are composed of symptoms from the individual components of the drug. Telmisartan - the most significant - a marked decrease in blood pressure and tachycardia, bradycardia, dizziness, increased serum creatinine concentration and acute renal failure can also be observed.
Hydrochlorothiazide - a violation of the water-electrolyte balance of the blood (hypokalemia, hypochloremia), a decrease in BCC, which can lead to muscle spasms and / or increase disorders of the cardiovascular system: arrhythmias caused by the simultaneous use of cardiac glycosides or some antiarrhythmic drugs.
Treatment: symptomatic therapy, hemodialysis is ineffective. The degree of removal of hydrochlorothiazide during hemodialysis has not been established. Regular monitoring of serum electrolytes and creatinine is required. Hemodialysis is not effective.
Storage conditions
At a temperature not exceeding 25 ° C, in the original packaging.
Keep out of the reach of children!
Shelf life
2 years.
Active ingredient
Hydrochlorothiazide, Telmisartan
pharmacy terms
pharmacy leave for
lekarstvennaja form
tablets
Telpres Plus tablets 40 mg + 12.5 mg 98 pcs. (Hydrohlorotyazyd, Telmisartan) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Telpres Plus tablets 40 mg + 12.5 mg 98 pcs. - Sale. PayPal accept. Free shipping florida. Fast international shipping.
Pharmacotherapeutic group: Combined antihypertensive (angiotensin II receptor antagonist + diuretic)
ATX:
C.09.DA07 Telmisartan in combination with
diuretics Pharmacodynamics:
Telpres Plus is a combination of telmisartan (an angiotensin II receptor antagonist) and hydrochlorothiazide - a thiazide diuretic. The simultaneous use of these components leads to a more pronounced antihypertensive effect than the use of each of them separately.
Taking Telpres Plus once a day leads to a significant gradual decrease in blood pressure (BP).
Telmisartan
Telmisartan is a specific angiotensin II receptor antagonist (type AT1) that is effective when taken orally. It has a high affinity for the AT 1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from the connection with the receptor, not possessing the action of an agonist in relation to this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, the concentration of which increases with the appointment of telmisartan, has not been studied. It reduces the concentration of aldosterone in the blood, does not inhibit renin in blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, amplification of the side effects caused by bradykinin is not expected.
In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first oral administration of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.
In patients with arterial hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting heart rate (HR).
In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome.
Hydrochlorothiazide
Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides (approximately in equivalent amounts). The diuretic effect of hydrochlorothiazide leads to a decrease in the volume of circulating blood (BCC), an increase in plasma renin activity, an increase in the secretion of aldosterone, followed by an increase in urine potassium and hydrogen carbonates and, as a result, a decrease in potassium in blood plasma. With simultaneous administration with telmisartan, there is a tendency to stop the loss of potassium caused by these diuretics, presumably due to the blockade of the renin-angiotensin-aldosterone system (RAAS). After oral administration, diuresis increases after 2 hours, and the maximum effect is observed after about 4 hours. The diuretic effect of the drug persists for approximately 6-12 hours.
Long-term use of hydrochlorothiazide reduces the risk of complications of cardiovascular disease and mortality from them.
The maximum antihypertensive effect of Telpres Plus is usually achieved 4-8 weeks after the start of treatment.
Pharmacokinetics:
The combined use of telmisartan and hydrochlorothiazide does not affect the pharmacokinetics of each of the components of the drug.
Telmisartan:
Absorption
When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (the area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma is leveled regardless of the meal.
Distribution of
Communication with plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in equilibrium concentration is 500 l.
Metabolism
Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.
Withdrawal
Elimination half-life (T1 / 2) - more than 20 hours. It is excreted through the intestine unchanged, excretion by the kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min) compared with hepatic blood flow (about 1500 ml / min).
Pharmacokinetics in special patient groups
Gender differences
There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared with men without significant impact on effectiveness. Dose adjustment is not required.
Elderly patients
The pharmacokinetics of telmisartan in elderly patients are not different from younger patients. Dose adjustment is not required.
Patients with impaired renal function
In patients with mild to moderate impaired renal function, dose adjustment of telmisartan is not required.
Patients with severe renal impairment and those on hemodialysis are recommended a lower initial dose of 20 mg per day. Telmisartan is not excreted by hemodialysis.
Patients with impaired liver function
Pharmacokinetics studies in patients with hepatic impairment showed an increase in the absolute bioavailability of telmisartan to almost 100%. With liver failure, T1 / 2 does not change. In patients with mild to moderate impaired liver function (class A and B on the Child-Pugh scale), the daily dose should not exceed 40 mg.
Hydrochlorothiazide:
After oral administration of Telpres Plus, the maximum plasma concentrations of hydrochlorothiazide are reached within 1-3 hours. Absolute bioavailability based on total kidney excretion is about 60%. It is bound by blood plasma proteins to 64% hydrochlorothiazide, and the distribution volume is 0.8 В± 0.3 l / kg. Hydrochlorothiazide is not metabolized in the body and excreted by the kidneys almost unchanged. About 60% of the dose taken orally is eliminated within 48 hours. Renal clearance of about 250-300 ml / min. T1L hydrochlorothiazide - 10 - 15 hours. There is a difference in plasma concentrations in men and women. In women, the concentration of telmisartan in plasma is 2-3 times higher than in men, and women have a tendency to increase the concentration of hydrochlorothiazide in the blood plasma is clinically insignificant.
Patients with impaired renal function
In patients with impaired renal function, the rate of elimination of hydrochlorothiazide is reduced.
Studies in patients with creatinine clearance (CC) of 90 ml / min showed that T1 / 2 of hydrochlorothiazide is increased. In patients with impaired T1 / 2 renal function, about 34 hours.
Indications
Arterial hypertension (in the case of inefficiency of telmisartan or hydrochlorothiazide in monotherapy).
Contraindications
- Hypersensitivity to the active substances or auxiliary components of the drug or other sulfonamide derivatives
- Pregnancy
- Breastfeeding period
- Obstructive biliary tract disease
- Severe class) Severe dysfunction impaired renal function (CC less than 30 ml / min)
- Refractory hypokalemia, hypercalcemia
- Concomitant use with aliskiren in patients with diabetes mellitus and / or usheniem renal function (glomerular filtration rate of less than 60 ml / min / 1.73 m2)
- Simultaneous use of ACE in patients with diabetic nephropathy
inhibitors - lactase deficiency, lactose intolerance,
glucose-galactose malabsorption syndrome - Age under 18 years (efficacy and safety not established).
Caution:
- Bilateral renal artery stenosis or stenosis of a single kidney artery (see Special instructions)
- Hepatic function impairment (Class A and B according to the Child-Pugh classification) (see Special instructions)
- Decreased BCC due to previous diuretic therapy, restrictions on the intake of salt, diarrhea or vomiting
- Hyperkalemia
- Condition after kidney transplantation (no experience with application)
- Chronic heart failure III-IV functional class (FC) according to the classification of the New York Cardiology Association
- Hypercalcemia
- Hypercholesterolemia - Hypercholesterolemia heart
- Progressive liver disease (risk of hepatic coma)
- Aortic and mitral valve stenosis
- Idiopathic hypertrophic subaortic stenosis (hypertrophic Skye obstructive cardiomyopathy)
- Diabetes
- Primary aldosteronism
- Gout
Composition
Each tablet 12.5 mg + 80 mg contains:
active ingredients: hydrochlorothiazide - 12.50 mg, telmisartan - 80.00 mg excipients: mannitol - 327.70 mg, povidone-K25 - 21.60 mg , crospovidone - 40.0 mg, magnesium stearate - 8.50 mg, meglumine - 24.00 mg, sodium hydroxide - 6.70 mg, lactose monohydrate - 49.84 mg, microcrystalline cellulose - 32.00 mg, hypromellose - 3.00 mg, sodium carboxymethyl starch, type A - 2.00 mg, iron red oxide (E 172) - 0.17 mg.
Dosage and administration
Inside, regardless of the meal time.
The drug Telpres Plus must be taken once a day.
- Telpres Plus 12.5 / 40 mg may be prescribed to patients in whom the use of telmisartan preparations in a dosage of 40 mg or hydrochlorothiazide does not lead to adequate control of blood pressure.
- Telpres Plus 12.5 / 80 mg may be prescribed to patients in which the use of telmisartan preparations in a dosage of 80 mg or Telpres Plus 12.5 / 40 mg does not lead to adequate control of blood pressure.
- Telpres Plus 25/80 mg can be prescribed to patients in whom the use of telmisartan preparations in a dosage of 80 mg or Telpres Plus 12.5 / 80 mg drug does not lead to adequate control of blood pressure, or to patients whose condition has previously been stabilized by telmisartan or hydrochlorothiazide with separate application.
In patients with severe arterial hypertension, the maximum daily dose of telmisartan is 160 mg in combination with hydrochlorothiazide in a daily dose of 12.5-25 mg.
Impaired renal function
Limited experience with Telpres Plus in patients with mild to moderate renal impairment does not require dose changes in these cases. In such patients, renal function should be monitored (with CC less than 30 ml / min, see section Contraindications).
Impaired liver function
In patients with mild to moderate impaired liver function (Child-Pugh Class A and B), the daily dose of Telpres Plus should not exceed 12.5 / 40 mg per day (see Pharmacokinetics section).
Elderly patients
Dosage regimen does not require changes.
Overdose
Information on overdose is limited. Possible symptoms of an overdose are composed of symptoms from the individual components of the drug. Telmisartan - the most significant - a marked decrease in blood pressure and tachycardia, bradycardia, dizziness, increased serum creatinine concentration and acute renal failure can also be observed.
Hydrochlorothiazide - a violation of the water-electrolyte balance of the blood (hypokalemia, hypochloremia), a decrease in BCC, which can lead to muscle spasms and / or increase disorders of the cardiovascular system: arrhythmias caused by the simultaneous use of cardiac glycosides or some antiarrhythmic drugs.
Treatment: symptomatic therapy, hemodialysis is ineffective. The degree of removal of hydrochlorothiazide during hemodialysis has not been established. Regular monitoring of serum electrolytes and creatinine is required. Hemodialysis is not effective.
Storage conditions
At a temperature not exceeding 25 ° C, in the original packaging.
Keep out of the reach of children!
Shelf life
2 years.
Active ingredient
Hydrochlorothiazide, Telmisartan
pharmacy terms
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tablets
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