Telmisartan 40 A.T An Thien treats hypertension (3 blisters x 10 tablets)

ATC code: C09CA076

Telmisartan is a specific antagonist of Angiotensin II receptor (AT1) in the smooth and adrenal smooth muscle.

In the renin-ankiotensin system, angiotensin II is made up of angiotensin I thanks to the catalyst of the enzyme transferring angiotensin (ACE). Angiotensin II is a vascular contraction, stimulating synthetic adrenal skin and releasing aldosterone, stimulating heart. Aldosterone reduces sodium excretion and increases potassium excretion in the kidneys.

Telmisartan blocks selectively the attachment of angiotensin II into the AT1 receptor in the blood vessel and adrenal glands, causing vasodilation and reducing the effects of Aldosterone.

AT2 receptors are also found in many tissues, but it is unclear whether this receptor has nothing to do with cardiovascular stability.

Telmisartan has a strong affinity for AT1 receptor, 3,000 times higher than the AT2 receptor.

Unlike angiotensin enzyme inhibitors - a group of drugs that are widely used to treat hypertension, Angiotensin II receptor antagonists do not inhibit bradykinin chemistry, so they do not cause persistent dry cough - an unwanted effect when treated with ACE inhibitors. Therefore, Angiotensin II receptor antagonists are used for people who have to stop using ACE inhibitors because they persist.

In humans, the dose of 80 mg Telmisartan inhibits almost completely hypertension due to angiotensin II. Inhibiting effects (hypotension) are maintained for 24 hours and still measures 48 hours after drinking. After taking the first dose, the effect of reducing blood pressure manifests itself slowly within the first 3 hours.

Normally, the maximum reduction of arterial blood pressure reaches 4-8 weeks after the beginning of treatment. The effect lasts for long -term treatment. In hypertension people, Telmisartan reduces systolic and diastolic blood pressure without changing the heart frequency. Telmisartan's anti -hypertension effect is equivalent to other anti -hypertension drugs.

When stopping treatment of Telmisartan suddenly, the blood pressure again gradually again for a few days as not yet treated, but there is no strong increase in the phenomenon.

Dynamic pharmacokinetics

absorption

Telmisartan is quickly absorbed, although the absorption has changed. Absolute bioavailability when drinking is 50%. When taken with food area under the curve of plasma concentrations over time (AUC) Telmisartan may decrease from 6% at 40 mg to 19% for 160 mg dose. Telmisartan's plasma concentrations are hungry and drink at the same time with food after 3 hours is equivalent. AUC decreases less, so it has little effect on treatment effects.

Elimination

Gender difference in plasma concentrations, plasma peak concentrations (CMAX) increased by about 3 times and AUC increased by about 2 times in women compared to men but did not affect the effectiveness of treatment.

distribution

Telmisartan binds to plasma proteins (> 99.5%), mainly with albumin and alpha 1 glycoprotein. The average distribution volume is in a stable state of about 500 1.

transformation

Telmisartan metabolizes by the reaction combined with glucuronid, metabolites have no pharmacological effects.

Telmisartan is eliminated according to the second -level dynamic equation. The maximum concentration in plasma and the area below the plasma concentration curve over time increases is not commensurate with the dose.

There is no clinical evidence of Telmisartan accumulation.

After taking Telmisartan eliminated almost entirely through the stool, most of the form of unchanged. The total amount of secretion through urine is less than 2% of the dose. Total clearance in plasma (about 1000 ml/min) compared to the blood flow through the liver (1500 ml/min).

on special subjects

Children:

pharmacokinetics of two doses of Telmisartan is considered a secondary target in hypertension patients (n = 57) from 6 to

Mobile pharmacological goals include determining the stability of Telmisartan in children and adolescents, and investigating age -related differences.

Despite being too small to evaluate the pharmacokinetic significance of children under 12 years old, the results are generally suitable for adult findings and confirm the non -linear nature of Telmisartan, especially for CMAX.

Sex:

cmax and auc in women are about 3 and 2 times higher than men.

Elderly:

Telmisartan pharmacokinetics are not different between the elderly and the young people over 65.

kidney failure:

In patients with mild to medium and severe renal impairment, observing the doubling of the drug concentration in plasma.

However, lower plasma concentrations have been observed in patients with dialysis treatment for dialysis. Telmisartan is highly linked to plasma proteins in patients with renal impairment and does not pass the filter during hemorrhage. The sale time does not change in patients with renal failure.

Hepatic failure:

Dynamic pharmacokinetics research in patients with hepatic impairment shows an absolute increase in bioavailability of nearly 100%. The sale time does not change in patients with liver failure.

Notify the physician the unwanted effects when using the drug.

Caution when using

Hepatic failure:

Because telmisartan is eliminated mostly through bile, Telmisartan is not used for biliary core, bile congestion or severe liver failure. It can be seen that Telmisartan clearance through the liver decreases in these patients. Drugs can only be used to be careful for patients with mild to medium liver failure.

Hypertension due to kidney artery:

There is an excessive risk of hypotension and renal failure when the patient has narrowed kidney stenosis on both sides or the kidney stenosis to the only kidney is still functioning to be treated with drugs that affect the renin-angiotensin-aldosterone system.

kidney failure and kidney transplantation:

When using Telmisartan for patients with renal function, periodic monitoring of potassium and serum creatinine.

No experience using Telmisartan for new kidney transplant patients.

Intravascular volume decline:

Symptomatic hypotension, especially after the first dose, can occur in patients with reduced intravascular volume and/or sodium reduction due to excessive diuretic therapy, too strict salt abstinence, diarrhea or vomiting. Such conditions should be overcome before using telmisartan.

Double Renin-Anotensin-Aldosterone System:

When using the concomitant medication (ACEI) with Angiotensin II or Aliskiren receptor antagonists, increases the risk of hypotension, hypokalemia and reduced kidney function (including acute renal failure). Do not use Telmisartan simultaneously with enzyme inhibitors or Aliskiren. In the case of really needed use, it is necessary to closely monitor blood pressure, electrolytes and kidney function.

Other conditions that stimulate the Renin-Angio-Tensin-Ordosterone system:

In patients with renal and vascular functions depend largely on the operation of the renin-angiotensin-aldosterone system (for example, patients with severe congestive heart failure or basic kidney disease, including kidney artery stenosis), coordination with other drugs that affect the renin-angiotensin-irtosterone system will cause acute hypotension, hyperemia, or rarely cause acute impairment. Review nsnseine

Increasing primary Aldosterone:

Patients with raw raw hyperplasia often do not respond to anti-hypertension drugs through inhibiting the Renin-Anotensin system. Therefore, it is not recommended to use Telmisartan.

Aortic valve stenosis and mitral valve, hypertrophic myocardial disease:

As well as for other vasodilators, special attention should be paid to patients with aortic valve stenosis or leaf valve, or hypertrophic cardiomyopathy.

Patients with diabetes are treated with insulin or diabetes drugs:

In these patients, hypoglycemia can occur under Telmisartan treatment. Therefore, in patients with diabetes, it is necessary to consider monitoring blood sugar, may need to adjust insulin dose or oral hypoglycemic drugs.

Hyperbonemia:

The use of drugs that affect the renin-angioten-sin-irtosterone system can cause hyperkalemia.

People over 70 years old, patients with renal impairment, diabetes, patients are treated simultaneously with many other drugs that may increase the concentration of potassium and/or other patients with other diseases, increased potassium can be fatal.

Before using simultaneously drugs that affect the renin-angiotensin-aldosterone system, should evaluate the ratio between harmful risks and treatment benefits.

Other caution:

Observing the enzyme inhibitors, Telmisartan and other Angiotensin receptor antagonists show that the effect of lowering blood pressure is noticeable in black skin patients in other skin -colored people. Maybe because in the body of human hypertension black has a lower amount of renin).

Like all medications for hypertension, excessive decrease in blood pressure in patients with myocardial ischemia or ischemic heart disease can lead to myocardial infarction or a stroke.

Use drugs for pregnant and lactating women

Pregnant women

Do not recommend the use of Angiotensin II receptor antagonistic drugs in the first 3 months of pregnancy and contraindicated use in the middle 3 months and the last 3 months of pregnancy.

There is no adequate data on use on pregnant women. Animal studies show that there is toxicity on reproduction.

Epidemiological evidence is related to the risk of teratogenicity when using an angiotensin transferred enzyme inhibitors, but it does not rule out a small risk. This risk exists similarly in the Angiotensin II receptor antagonistic group.

Unless necessary, women planning to get pregnant, so they are changed to treatment that has been proven to be safe during pregnancy. When diagnosis is pregnant, it is necessary to stop the drug immediately and use other appropriate replacement therapy.

Using Angiotensin II receptor antagonistic drugs in the last 3 months and the last 3 months of pregnancy leads to fetal toxicity (impaired renal function, less amniotic fluid, slow chemistry) and on newborn babies (kidney failure, hypotension, hyperkalemia).

If the Angiotensin II receptor is used for more than 3 months between pregnancy, it is necessary to have an ultrasound to check for kidney function and fetal skull.

Infants whose mothers use Angiotensin II receptor drugs should be carefully monitored the risk of hypotension.

breastfeeding women

There is no adequate information about the use of Telmisartan in nursing women, so it is not recommended to use in breastfeeding women. Should use other replacement therapy safer, especially for mothers with newborn or premature babies.

fertility

In preclinical studies, there is no observation of Telmisartan's influence on fertility in both men and women.

The effect of the drug on the ability to drive and operate machinery

Side effects of the drug such as dizziness, drowsiness, headache, fatigue, visual disorders can affect the ability to drive and operate machinery.

Drug interaction

Digoxin:

Using telmisartan with digoxin increases the peak concentration of Digoxin in serum (49%) and bottom concentration (20%). When starting the dose, adjusting the dose or stopping Telmisartan, it is necessary to monitor the concentration of digoxin to ensure the concentration is within the therapy range.

As well as other-acting drugs on the renin-ankiotensin-aldosterone system, Telmisartan may increase potassium. The risk of hyperkalemia increases when combined with other drugs that can cause other potassium hyperactics such as replacement salts containing potassium, potassium-saving diuretic, enzyme inhibitors, other Angiotensin II receptor anti-receptor drugs, NSAIDS nonsteroidal anti-inflammatory drugs (including COX-2 selective inhibitors), Heparin, Cyclosporin, Tacrolimus, Trimethoprim. Particularly high risks in case of combination with potassium -saving dtered or alternative salts containing potassium.

There is no recommendation to combine Telmisartan with the following drugs:

Potassium -saving diuretic: The combination of Telmisartan and potassium -saving drugs such as Spironolactone, Eplerenone, Triamterene, or Amiloride, potassium salts can significantly increase potassium potassium. If used at the same time, serum potassium must be monitored.

Lithi: The increase in lithium and toxic lithium recovery has been reported during simultaneous use of lithium with Telmisartan. If used in combination in case of necessity, careful monitoring of serum lithium concentration.

When used in combination must be cautious with the following drugs:

Steroid anti -inflammatory drugs: