Actelsar 40mg Actavis treats idiopathic hypertension (2 blisters x 14 tablets)

Telmisartan is an Angiotensin II (AT) receptor receptor.

Telmisartan antagonistic Angiotensin II with a very high affinity from its link position in the AT receptor group, this receptor is responsible for the known activities of Angiotensin II. Telmisartan does not have any transport owner activities at the AT - Telmisartan receptor receptor selective with the AT. The cohesion is long -term. Telmisartan has no affinity for other receptors, including AT receptors, and other less characteristic AT receptors. It is not known the role of receptors as well as the consequences of excessive stimulation when angiotensin II concentration increases due to telmisartan.

Telmisartan reduces the concentration of Aldosterone Telmisartan does not inhibit blood in humans or blocking bon channels. Telmisartan does not inhibit Angiotensin transfer enzymes (Kininase II). This enzyme also works to describe Bradykinin. So it has no side effects through Bradykinin intermediaries.

In humans, a dose of 80mg Telmisartan almost completely inhibits the hypertension of Angiotensin II. The inhibitory effect is maintained for more than 24 hours and is still effective up to 48 hours.

Pharmacokinetics

absorption

The absorption of Telmisartan is fast despite the change of absorption. Telmisartan's absolute average bioavailability is about 50%.

When Telmisartan is used with food, the area under the plasma concentration curve over time (AUCU-G) of Telmisartan decreases from about 6% (dose of 40mg) to about 19% (dose of 160mg). 3 hours after drinking, the plasma concentration of Telmisartan gets the total hunger or drinking with the same food.

allocation

Telmisartan is largely mounted with plasma proteins (> 99.5%), mainly albumin and alpha -acid glycoprotein. The average integral in stable state (VDSS) is about 500L.

Metabolism

Telmisartan is metabolized by combining with glucuronide of the original compound. Combining without pharmacological activity

Elimination

Telmisartan is characterized by the destruction of pharmacokinetics under the level 2 equation with a half -life of over 20 hours. Plasma (CMAX) and a smaller level, the area below the total curve over time in plasma (AUC) increases not commensurate with the dose.

There is no clinical evidence related to Telmisartan's accumulation at the recommended dose.

Higher concentrations in women in men, without effects related to validity.

After oral and intravenous use), Telmisartan is almost completely excreted through feces, mainly in the form of constant compounds. The total amount of excretion in urine is

Special subjects

Sex influence: The difference in plasma concentrations have been recorded, with CMAX and AUC higher than 3-2 times higher, respectively, in women compared to men.

Older patients: Telmisartan's pharmacokinetics are not different between the elderly and the young people over 65.

Patients with renal impairment: In patients with mild to moderate and severe renal impairment, the doubled plasma concentration has been recorded. However, lower plasma concentrations are recorded in patients with dialysis. Telmisartan is very high with plasma proteins in patients with renal impairment and cannot be removed by dialysis. The sale time is not changed in patients with renal failure.

Patients with liver failure: Pharmacokinetic studies in patients with hepatic impairment shows an absolute increase in bioavailability of nearly 100%. The sale time is not changed in patients with liver failure.

Be cautious when taking drugs

Hepatic failure

Actelsar is not used for biliary obstruction, biliary path disorders or severe liver failure due to Telmisartan is excreted mainly through bile. These patients have the clearance of Telmisartan through the liver, Actelsar should be used in patients with mild and moderate liver failure.

Hypertension caused by kidney artery

Increased risk of severe hypotension and renal failure, when patients have narrowed kidney stenosis or kidney stenosis on one kidney with a single function that is treated with drugs that affect the teenin-ankiotensin-aldosteron system.

kidney failure and kidney transplant

When using Actelsar in patients with renal function, periodically monitoring potassium and serum creatinine concentrations are recommended. There is no experience in using Actelsar in new kidney transplant patients.

Reducing internal volume

Symptomic hypotension, especially after the first data of Actelsar, can occur in patients with decreased volume and or sodium due to strong diuretic, strict salt, diarrhea or vomiting. These conditions should be adjusted before using Actelsar. Reducing volume and or sodium should be adjusted before using Actelsar.

Dual inhibitor Renin-Anotensin-Aldosteron system

As a result of inhibiting the renin-analiotensin-aldosteron system, hypotension, interrupt, hyperkalemia and renal function changes (including acute renal failure) have been reported in sensitive people, especially if combining drugs affecting this system. The double inhibitor of the Renin-Anotensin-Aldosteron system (for example, add an enzyme inhibitor to be transferred to an Angiotensin II receptor resistant drug), therefore, it is not recommended in patients with blood pressure that has been controlled and should be restricted in specific specified cases and closely monitoring kidney function.

Other conditions stimulate the renin-ankiotensin-aldosteron system

In patients where the vascular tone and renal function depend heavily on the activity of the renin-angiotensin-aldosteron system (such as patients with severe congestive heart failure, or kidney disease, including renal artery stenosis), treatment with drugs that affect this system such as Telmisartan will cause hypotension hypertension nitrogen nitrogen, urinary, or nephrotic failure (rare).

primary Aldosteron

Patients with primary Aldosteron intense in general, not responding to antihypertensive drugs operating through inhibition of retin-anideensin-aldosteron systems. Therefore, the use of Telmisartan is not recommended.

Aortic stenosis and mitral stenosis, hypertrophic myocardial disease

As other vasodilators, especially cautious when prescribed patients with aortic stenosis, or mitral valve stenosis or obstruction of myocardial disease.

Hyperbonia

The use of drugs that affects the renin-angiotensin aldosteron system can cause hyperkalemia.

In the elderly, in patients with renal impairment, patients with diabetes, patients use simultaneously with other drugs that increase the concentration of potassium or in patients with recurrent events, increased potassium can cause death.

Before considering using the drugs that affect the renin-angiotensin-aldosteron system, the benefit and risk ratio should be evaluated.

The main risk factors of hyperkalemia are considered:

racial difference

According to the observations of enzyme inhibitors Angiotensin, Telmisartan and other Angiotensin II receptor antagonists seem to be less effective in lowering blood pressure in black people than those who are not black, maybe because of the common low renin in the population of hypertension.

Preventive and other warnings

As with any other hypotension, excessive reduction in patients with ischemic heart disease or cardiovascular disease due to ischemia can lead to myocardial infarction or stroke.

The ability to drive and operate machinery

There are no studies conducted on the effects on the ability to control the train and operate machinery. However, when controlling the train and operating machinery, it should be noted that dizziness or drowsiness can sometimes occur when using blood pressure therapy.

Pregnancy

The use of Angiotensin II receptor antagonistic drugs is not recommended in the first trimester of pregnancy. The use of Angiotensin II receptor is contraindicated in the second and third trimester of pregnancy. There is no enough data from using Telmisartan in pregnant women. Animal studies show reproductive toxicity. Epidemiological evidence about the risk of teratogenicity after exposure to enzyme inhibitors in the first three months of pregnancy has not been concluded, but a small increase in the risk of not being excluded.

While there is no epidemiological data that controls risks to Angiotensin II receptor antagonists, similar risks can exist for this group of drugs. Unless the use is considered essential, the patient intends to become pregnant should be changed to other hypotension therapy that the safety for use during pregnancy has been established. When being diagnosed with pregnancy, Angiotensin II receptor antagonistic should be discontinued immediately, and, if appropriate, should start replacement therapy.

Exposure to Angiotensin II receptor antagonistic therapy in the second and third trimester is known to cause fetal toxicity in people with reduced renal function, amniotic fluid, slow chemistry) and postpartum toxicity (kidney failure, hypotension, hyperkalemia).

If exposed to Angiotensin II receptor antagonists occur from the second trimester of pregnancy, ultrasound tests for kidney and skull function are recommended.

The period of breastfeeding

Infants whose mothers have used Angiotensin II receptor antagonistic drugs should be monitored closely.

Due to not having enough information about the use of Telmisartan during breastfeeding, Telmisartan was not recommended and prioritized for safety alternative therapies that have been better established during breastfeeding, especially in nurturing newborns and premature babies.

Interactive drug

Research on drug interaction is only done in adults. As well as other drugs on the tenin-angiotensin-aldosteron system, Telmisartan can cause hyperkalemia. The risk can be increased when treated in combination with other drugs that cause hyperkalemia (Salt -replacement products containing potassium, potassium diuretics, enzyme inhibitors, Angiotensin II antagonistic drugs, nonsteroidal anti -inflammatory drugs (NSAIDs, including selective inhibitors 2), Heparin, immunosuppressants trimethoprim).

The appearance of hyperkalemia depends on the accompanying risk factors. This risk increases in the above combined treatments. Particularly high risk when combined with potassium diuretics, and when combined with salt replacement products containing potassium. Combined with transferred inhibitors or NSAIDs, for example, lower risk as long as they strictly comply with measures to prevent.

Not recommended coordinates

Potassium diuretic and potassium supplements: Angiotensin II receptor antagonists such as Telmisartan, diuretics that cause potassium loss. Potassium diuretics such as: Spironolactone, Eplerenone , Triamterene or Amiloride, Potassium supplements, or salt -containing salt -containing products can significantly increase potassium in serum. If used simultaneously indicated by the hypokalemia, should be used carefully and regularly monitor serum potassium.

Lithium: Increased serum and toxic lithium concentration may recover the reported in the process of simultaneous use of lithium with angiotensin transferring enamel inhibitors and angiotensin II receptor antagonists, including telmisartan. If the combination use is necessary, carefully monitor the serum lithium concentration is recommended.

Cautions need to be cautious

Non -services NSAIDS non -inflammatory drugs (i.e. acetylsalicylic acid in anti -inflammatory willow, non -specialized C00 and NSAIDs inhibitors) can reduce the effectiveness of hypotension of angiotensin receptor antagonists. In some patients with kidney function damage (such as dehydration, older patients with kidney damage), simultaneous use of Angiotensin II receptor receptor and cyclo-olyena inhibitors can cause worse renal function, may recover more often. Therefore, the combination should be used carefully, especially in the elderly. Patients should be fully rehydrated and should consider monitoring kidney function after starting treatment and periodic treatment.

In a simultaneous study of Telmisartan and Ramipril, it increased by 1.5 times AUC0-24 and CMAX of Ramipril and Ramiprilat. Clinically related in this comment is not known.

Diuretics, thiazid diuretics or diuretic: Pre -treatment with high -dose diuretic drugs such as Furosemid (diuretics) and hydrochlorothiazide (thiazid diuretic) can lead to decreased volume, and risk of hypotension when starting treatment with Telmisartan

Other hypotension drugs: Telmisartan's hypotension effect can be increased by simultaneous use with other hypotension drugs. Based on their pharmacological properties, the following drugs may increase the hypotension effect of all antihypertensive drugs including Telmisartan. Moreover, posture hypotension may be more serious due to alcohol, barbiturates, drugs, or antidepressants.

corticosteroid (systemic line): Reducing the effect of hypotension.