Treatment of spontaneous hypertension in adults. Reduction in cardiovascular morbidity in patients with overt atherosclerosis (ischemic heart disease, stroke or peripheral arterial disease) or type 2 diabetes with documented target organ damage.
Selective angiotensin II receptor antagonist (AT type1) with high affinity. Selectively binds to the AT receptor1by blocking the effects of angiotensin II. It has no agonist activity towards the AT receptor1, does not bind and does not block other AT receptor subtypes. Telmisartan reduces the amount of aldosterone in the blood. It does not inhibit the activity of renin plasma and does not block ion channels. It is not an ACE inhibitor (kinase II), so it does not increase the effects of bradykinin-dependent effects. After oral administration, telmisartan is rapidly, but to a different degree absorbed from the gastrointestinal tract. The average absolute bioavailability is about 50%. It is highly bound to plasma proteins (> 99.5%). It is metabolized in the process of coupling to glucuronide derivatives, which do not have pharmacological activity. The drug is almost completely excreted unchanged in the faeces, urinary excretion accounts for less than 1% of the administered dose. T0,5 is> 20 h.
Contraindications:
Hypersensitivity to the components of the preparation. Disorders in the outflow of bile. Severe liver dysfunction. Co-administration of telmisartan and aliskiren is contraindicated in patients with diabetes mellitus or renal impairment (GFR <60 ml / min / 1.73 m2). II and III trimester of pregnancy.
Precautions:
It may be used in patients with mild or moderate hepatic impairment only with caution. There was an increased risk of severe hypotension and renal failure when administering drugs that affect the renin-angiotensin-aldosterone system (RAA) in patients with bilateral renal artery stenosis or renal artery stenosis for one active kidney. In patients with impaired renal function, periodic monitoring of potassium and creatinine in the blood is recommended. There are no data on the use of telmisartan in patients who have recently had a kidney transplant. Symptomatic hypotension, especially after the first dose, may occur in patients with decreased intravascular volume and / or reduced sodium concentration as a result of intense diuretic therapy and / or reduced salt intake, diarrhea or vomiting - these disorders should be compensated before administration. Due to the risk of hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure), dual RAA blocking is not recommended (eg, by the combined use of an angiotensin II receptor antagonist with an ACE inhibitor or aliskiren); if the use of the RAA double block is absolutely necessary, it should only be carried out under the supervision of a specialist. At the same time, angiotensin II receptor antagonists and ACE inhibitors should not be used in patients with diabetic nephropathy. In patients whose vascular tone and renal function depend mainly on RAA activity (eg patients with severe congestive heart failure or kidney disease, including renal artery stenosis), the administration of drugs such as telmisartan affecting the system has been associated with with a sharp reduction in blood pressure, hyperazotemnia, oliguria and rarely with acute renal failure. Patients with primary aldosteronism generally do not respond to treatment with antihypertensive drugs acting through the inhibition of the renin-angiotensin system - the use of telmisartan in these patients is not recommended. Special care should be taken in patients with aortic or bifurcular stenosis or hypertrophic narrowing cardiomyopathy.Excessive reduction in blood pressure in patients with ischemic cardiomyopathy or atherosclerosis may result in a heart attack or stroke. Due to the risk of hypoglycaemia, in patients with diabetes taking insulin or oral antidiabetic agents, monitoring of blood Glucose should be monitored frequently during treatment with telmisartan; it may also be necessary to adjust the dose of insulin or antidiabetic medicines. In patients at risk for hyperkalemia, the benefit-risk ratio should be assessed before deciding on the use of telmisartan. The main risk factors for hyperkalemia are: diabetes, renal failure, age (> 70 years), concomitant use of potassium supplements, potassium chloride substitutes or medicines that can increase blood potassium levels (such as potassium-sparing diuretics, ACE inhibitors) , angiotensin II receptor antagonists, non-steroidal anti-inflammatory drugs, Heparin, trimethoprim, immunosuppressive drugs - cyclosporine or tacrolimus), co-morbidities, in particular such as dehydration, acute decompensated heart failure, metabolic acidosis, deterioration of renal function, sudden deterioration of renal function (e.g. in the course of infectious diseases), cell disintegration (eg in acute limb ischemia, striated muscle decay, extensive trauma). In patients at risk for hyperkalemia, blood potassium levels should be monitored in great detail. Angiotensin II receptor antagonists are less effective in the treatment of hypertension in the black population. The safety and efficacy of the medicine in children and adolescents <18 years has not been established. Due to the lactose content, the drug should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of the preparation in the first trimester of pregnancy is not recommended (there is a risk of teratogenic effect). Use in the second and third trimester of pregnancy is contraindicated. Telmisartan used in the second and third trimester of pregnancy is toxic to fetal development (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and newborn (renal failure, hypotension, hyperkalemia) - when exposure to the drug occurred from the second trimester of pregnancy, it is recommended an ultrasound examination of the fetus skull and kidneys; children whose mothers took the drug during pregnancy should be closely monitored for hypotension. The drug is not recommended during breast-feeding.
Side effects:
Uncommon: urinary tract infections (including cystitis), upper respiratory tract infection (including pharyngitis and sinusitis), anemia, hyperkalemia, insomnia, depression, syncope, diarrheal headache, bradycardia, hypotension, orthostatic hypotension, dyspnoea, cough, abdominal pain, diarrhea, indigestion, bloating, vomiting, pruritus, excessive sweating, rash, back pain (eg sciatica), muscle cramps, muscle pain, kidney problems (including acute renal failure), pain in the chest, weakness, increased plasma creatinine. Rare: sepsis (including fatal outcome), eosinophilia, thrombocytopenia, hypersensitivity reactions, anaphylactic reaction, hypoglycaemia (in patients with diabetes), anxiety, drowsiness, visual disturbances, tachycardia, dry mouth, gastritis, abnormal liver function and liver disorders (in most cases, in Japanese people who are more susceptible to this side effect), angioneurotic edema (also leading to death), erythema, urticaria, drug eruption, toxic skin damage, joint pain, limb pain, tendon pain (symptoms imitating tendinitis), flu-like symptoms, decreased hemoglobin, increased blood uric acid, increased liver enzymes, increased creatine phosphokinase in the blood. Very rare: interstitial lung disease (no causal relationship has been established).
Dosage:
Orally.Spontaneous hypertension: the usual effective dose is 40 mg once a day. In some patients, improvement may occur after 20 mg. In the absence of a satisfactory antihypertensive effect, the dose of telmisartan may be increased to 80 mg once a day.Telmisartan can be used in combination with thiazide diuretics such as hydrochlorothiazide. In the event that a dose increase is considered, it must be taken into account that the maximum pressure-lowering effect is achieved 4-8 weeks after the start of treatment.Prevention of cardiovascular diseasesThe recommended dose is 80 mg once a day. It has not been determined whether doses lower than 80 mg of telmisartan are effective in reducing the incidence of cardiovascular problems. Close blood pressure monitoring is recommended when initiating telmisartan to reduce cardiovascular morbidity and if necessary to adjust the dose of blood-pressure medication.Special groups of patients. Dosage adjustment is not necessary in the elderly and in patients with mild to moderate renal impairment. In patients with severe renal failure or undergoing hemodialysis, it is recommended to start treatment with a 20 mg dose. For mild to moderate hepatic impairment, the dose should not exceed 40 mg once daily.Way of giving. The drug should be taken once a day, with liquid. Can be taken regardless of meals.