Levistel 80 Tada Pharma tablets treat hypertension, heart failure (4 blisters x 7 tablets)

Telmisartan is an oral medication, Angiotensin II receptor.

Telmisartan antagonistic Angiotensin II with strong affinity at the position of cohesion on the AT1 receptor, receptor is responsible for all the known activities of Angiotensin II. There is no Telmisartan's operating activity at the AT1 receptor. This cohesion is sustainable and prolonged.

Telmisartan does not show affinity for other receptors, including AT2 and other less characteristic AT receptors. It is not known the role of these receptors as well as the consequences of the excessive stimulation of them when the angiotensin II concentration increases due to telmisartan. Telmisartan reduces the amount of aldosterone in the blood.

Telmisartan does not inhibit plasma renin and no ion channels. Telmisartan does not inhibit the enzyme Angiotensin (Kinase II), yeast has the effect of breaking Bradykinin. So there are no side effects caused by Bradykldnin.

On the human body, the dose of 80 mg Telmisartan has an almost complete inhibition effect that causes hypertension of angiotensin II. This inhibitory effect is maintained in 24 hours and is still effective until 48 hours.

After the first dose of Telmisartan, the hypotension effect will gradually and clearly within 3 hours. Hypotension effects maximum after 4 weeks of treatment and is maintained during long -term treatment.

24 -hour continuous blood pressure measurement (ABPM) shows that the lowering effect is maintained stably during 24 hours after taking the drug and even the last 4 hours before the next dose. This is confirmed by the percentage/peak ratio of over 80% with a dose of 40 and 80 mg Telmisartan in clinical studies that are controlled to placebo.

There is a clear tendency for the relationship between the dose and the time for the systolic blood pressure to return to the original level. In this respect, data related to diastolic blood pressure is not constant.

In patients with high blood pressure, Telmisartan works to reduce both systolic and diastolic blood pressure without affecting the heart rate. Telmisartan's lowering effects can be compared with other groups of high blood pressure treatments of other groups (seen through clinical trials comparing telmisartan with amlodipine, atenolol, enalapril, hydrochlorothiazid, losartan and lisinopril).

If stopped with Telmisartan, blood pressure will gradually return to the original value before treatment within a few days without the phenomenon of hypertension. Treatment with Telmisartan has also been clinically proven to reduce the statistical statistically of the left ventricular weight and the left ventricle index in patients with hypertension with left ventricular hypertrophy.

Efficiency of Telmisartan on reduced mortality and disability caused by cardiovascular disease.

Through clinical trials directly compare two antihypertensive drugs, the rate of dry cough in patients treated with Telmisartan is lower than that of patients using angiotensin transferring enzymes inhibitors.

pharmacokinetics

Telmisartan is quickly absorbed, although the absorption amount changes. Telmisartan's absolute bioavailability is about 50%.

When taken with food, the area under the plasma concentration curve over time (AUC) of Telmisartan may decrease from 6% (at 40 mg) to about 19% (at a dose of 160 mg). The plasma concentration of Telmisartan is hungry or with food after 3 hours is similar.

AUC is small, so it does not reduce the effectiveness of treatment.

Gender difference to plasma concentrations, peak concentration in blood (CMAX) increases about 3 times and AUC increases about 2 times in women compared to men, but does not affect efficiency.

Telmisartan is highly connected to plasma proteins (> 99.5%), mainly with albumin and Alpha-1 acid Glycoprotein. Average distribution volume in a stable state of about 500L.

Telmisartan metabolizes by the reaction with glucuronide. Metabolic substances have no pharmacological effects.

Telmisartan is destroyed by dynamic according to the level 2 equation, the last disposal time is over 20 hours. Maximum concentration in plasma and area under the curve of plasma concentrations over time (AUC) increases not commensurate with the dose. There is no clinically related evidence of Telmisartan's accumulation.

After drinking (and intravenous injection), Telmisartan eliminates almost entirely through feces, mostly in the form of unchanged. The total amount of secretion through urine is less than 2% of the dose. The total clearance of the plasma is high (about 900 ml/min) compared to the blood flow through the liver (about 1500 ml/min).

Older people

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

Patients with renal failure

Lower plasma concentrations in patients with kidney failure are treating dialysis. Telmisartan combines with high plasma proteins on patients with renal impairment and does not pass the membrane during blood accumulation. The sale time does not change in patients with renal failure.

Patients with liver failure

Having been dynamic research in patients with hepatic impairment shows that there is an bioavailability of nearly 100%. Sell ​​waste time does not change in patients with liver failure.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Precautions for use

There is a risk of strong hypotension and renal failure when the patient has narrowed kidney stenosis on both sides or one side treated with drugs that influence the Rennin Angiotensin-Aldosteron system.

kidney failure and kidney transplant

Periodically monitor potassium and blood creatinine concentrations when Telmisartan is used in patients with renal failure. There is no experience using Telmisartan in new kidney transplant patients.

Intravascular volume exhaustion

Symptomatic hypotension may occur, especially after the first dose in patients with intravascular volume reduction and/or sodium reduction due to treatment with strong diuretics, diets that limit salt, diarrhea or vomiting. It is necessary to treat the patient before using Telmisartan.

Other pathologies stimulate the renin-angiotensin-aldosteron system

In patients with renal and vascular functions prioritize depending on the activity of the Renin - Angiotensin - Aldosterone system (for example, patients with severe congestive heart failure or renal disease include kidney stenosis), treatment in combination with other drugs that affect the renin -angiotensin -aldosterone system will cause acute blood pressure, rare nitrogen nitrogen.

Increased primary Aldosterol

In general, patients with primary aldosterone increases will not respond to antihypertensive drugs that act on the inhibition of the Renin - Angiotensin system. Therefore, Telmisartan should not be used in these patients.

Security of mitral valve and aortic valve, hypertrophic heart muscle disease

As other vasodilators, special attention should be paid to patients with aortic valve stenosis or mitral valve or congested heart muscle.

Hemorrhage

When treated with drugs that affect the Renin - Angiotensin - Aldosteron system can cause hyperkalemia, especially in patients with renal impairment and/or heart failure. Monitoring the amount of blood potassium in patients is at risk of recommended.

The use in combination with potassium -keeping, potassium supplements, replacement salts containing potassium or other drugs may increase blood potassium levels (for example, heparin, etc.), which can increase serum potassium so attention should be paid when using these drugs with telmisartan.

Hepatic failure

Telmisartan is excreted mainly through bile. The removal is impaired in patients with bile or liver impairment. Caution should be used in these patients.

Other notes

Through studies on angiotensin transferring enzymes show that Telmisartan and other Angiotensin antagonists have a significant lowering effect in darker people in other black -colored people. Maybe because the body of the black high blood pressure has a lower amount of renin.

Like all antihypertensive drugs, excessive decrease in blood pressure in patients with cardiovascular disease due to ischemia can lead to myocardial infarction or stroke.

The ability to drive and operate machinery

There is no research on the effect of the drug on the ability to drive and what makes the machine perform. However, when driving or operating machinery, it is important to pay attention to the feeling of dizziness or drowsiness can sometimes occur during the treatment of high blood pressure.

Pregnancy

do not recommend Angiotensin II anti -receptor drugs in the first 3 months of pregnancy. Contraindicated to use Angiotensin II receptor drugs in the middle and late pregnancy.

Breastfeeding period

Because there is no credibility on the use of Telmisartan during breastfeeding, it is not recommended to use Telmisartan and should prioritize drugs with safety data that have been determined in this period, especially for infants and children with shortage.

Medicinal interaction

Telmisartan may increase the effect of other hypotension drugs. Other interactions are not significant clinical significance.

There is no clinical significant interaction when using Telmisartan simultaneously with digoxin, warfarin, hydrochlorothiazid, glibenclamid, ibuprofen, paracetamol, simvastatin and amlodipine. Digoxin bottom concentration is found to increase by 20% (in a single case increasing by 39%) should consider monitoring digoxin levels in plasma.

Increased plasma and recovery lithium concentration has been recorded when shared with lithium with angiotensin transfer enzymes inhibitors. In some cases, it has also been reported when used with Angiotensin II receptor antagonist. Therefore, lithium concentration should be monitored when using two drugs.

Potassium or potassium supplements

Angiotensin II receptor antagonists like Telmisartan, reduced to cause potassium loss of diuretics. Potassium diuretics (for example, Spirinolacton), eplerenon, triamteren or amilorid, potassium supplements, or salt containing potassium can lead to significant increase in blood potassium. If used simultaneously due to the defined hypokalemia, it should be used carefully and often monitor blood potassium.

Non -steroid anti -inflammatory drugs (NSAID)

Simultaneously used with NSAID drugs (such as acetylsalicylic acid at doses for anti-inflammatory effects, COX-2 inhibitors and non-selective NSAID drugs) can reduce the effect of lowering the blood pressure of Angiotension II receptor anti-receptor drugs.

In some patients with renal function (patients with dehydration or elderly people with reduced renal function), the synonyms of Angiotension II receptor antagonistic drugs and cycloxygenase inhibitors can lead to more renal failure including acute renal failure, often recovered.

Therefore, this combination should be careful, especially in the elderly. Patients should be fully rehydrated and monitor kidney function from the beginning of combination and periodic treatment.

The anti -hypertension effect of Telmisartan drugs is reduced by the inhibition of vasodilic prostaglandin that has been reported during treatment in combination with nonsteroidal anti -inflammatory drugs.

In a combination of Telmisartan and Ramipril, which led to increased 2.5 times AUC0-24 and CMAX of Ramipril and Ramiprilat. Unknown clinical involvement of this observation.

corticosteroids (using the whole body)

Reducing the hypotension effect of Temisartan.