Index of drugs

Treatment of essential hypertension. The combined drug 40 / 12.5 mg and 80 / 12.5 mg are indicated for use in adults whose blood pressure is not adequately controlled after using telmisartan alone. The 80/25 mg combination is indicated for adults whose blood pressure is not adequately controlled with the telmisartan / hydrochlorothiazide 80 mg / 12.5 mg combination or in adults who have previously been stabilized with telmisartan and hydrochlorothiazide given separately.

1 tabl contains a combination of telmisartan and hydrochlorothiazide 40 mg + 12.5 mg, 80 mg + 12.5 mg or 80 mg + 25 mg, respectively. The product contains lactose and sorbitol.

A hypotensive preparation containing two antihypertensive agents with complementary mechanisms of action: an angiotensin II receptor antagonist (telmisartan) and a thiazide diuretic (hydrochlorothiazide). Telmisartan is a selective angiotensin II receptor (type AT antagonist)₁) 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. Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides. The diuretic action of hydrochlorothiazide reduces plasma volume, increases plasma renin activity, increases aldosterone secretion, increases urinary potassium and bicarbonate loss, decreases in potassium in the blood. Co-administration of telmisartan causes the blockade of the renin-angiotensin-aldosterone system to stop the potassium loss associated with the action of diuretics. Co-administration of telmisartan and hydrochlorothiazide does not affect the pharmacokinetics of any of these active substances. After oral administration, telmisartan is rapidly absorbed from the gastrointestinal tract, reaching C_max during 0.5-1.5 hours. The average absolute bioavailability is about 50%. It is highly bound to plasma proteins (> 99.5%). It is metabolized (in about 11%) to pharmacologically inactive acylglucuronide and excreted in faeces in> 97%. T_0,5 is> 20 h. The bioavailability of hydrochlorothiazide after oral administration is 60%. Achieve_max 1-3 h after administration. It binds 68% of plasma proteins. It is not metabolized, it is almost completely excreted unchanged in the urine. T_0,5 is 10-15 hours.

Hypersensitivity to the components of the preparation. Hypersensitivity to other sulfonamide derivatives. Bile stasis and biliary obstruction. Severe hepatic failure. Severe renal failure (creatinine clearance <30 ml / min). Resistance to hypokalemia, hypercalcemia. Co-administration with aliskiren in patients with diabetes or renal impairment (GFR <60 ml / min / 1.73 m²). II and III trimester of pregnancy.

Caution should be exercised in patients with impaired hepatic function or progressive liver disease, as minor alterations in fluid and electrolyte balance may precipitate hepatic coma. There are no clinical data on the use of telmisartan in patients with hepatic impairment. 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. There are no data on the use of the preparation in patients after a recent kidney transplantation.Caution for use in patients with mild to moderate renal insufficiency - monitoring of potassium, creatinine and uric acid levels is recommended; In patients with impaired renal function, there may be azotemia associated with the administered thiazide diuretic. 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. In patients whose vascular tone and renal function depend mainly on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure or kidney disease, including renal artery stenosis), administration of drugs such as telmisartan affecting on this system, it was associated with a sharp reduction in blood pressure, hyperazotemia, oliguria and rarely with acute renal failure. 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. Patients with primary aldosteronism usually do not respond to treatment with antihypertensive drugs acting through the inhibition of the renin-angiotensin system - the use of the preparation in these cases is not recommended. Angiotensin II receptor antagonists are less effective in the treatment of hypertension in the black population. Special care should be taken in patients with aortic or bifurcular stenosis or hypertrophic narrowing cardiomyopathy. As with other antihypertensive agents, excessive hypotension in patients with ischemic cardiomyopathy or coronary heart disease may result in a heart attack or stroke. Caution for patients with diabetes mellitus, as thiazide therapy may impair Glucose tolerance - glucose monitoring should be monitored, or a dose adjustment of insulin or oral antidiabetic agents may be required. Hydrochlorothiazide may accelerate the onset of diabetes mellitus in patients with latent diabetes; may cause increased cholesterol and triglycerides in the blood; may cause hyperuricemia and trigger a gout attack; may cause or exacerbate the symptoms of systemic lupus erythematosus; may cause hypomagnesaemia, hyponatremia and hypochloraic alkalosis; may cause slight and transient hypercalcaemia - a significant hypercalcemia may indicate an unrecognized hyperparathyroidism (thiazides should be discontinued before performing parathyroid function tests). Hydrochlorothiazide may cause specific reactions (usually resolving within hours or weeks of the start of treatment with the drug) leading to acute transient myopia and acute angle-closure glaucoma; since untreated acute angle-closure glaucoma may lead to permanent loss of vision, treatment is primarily based on the withdrawal of hydrochlorothiazide as soon as possible; if intraocular pressure can not be controlled, immediate surgical or surgical treatment should be considered (risk factors for developing acute angle-closure glare may include a history of sulfonamide or penicillin allergy). Regular monitoring of electrolytes in the blood should be performed during treatment with the product. Although hypokalemia may occur with thiazide diuretics, concomitant therapy with telmisartan may reduce the hypokalaemia induced by diuretics. The risk of hypokalaemia (due to the presence of hydrochlorothiazide) is higher in patients with liver cirrhosis, in patients who experience rapid diuresis or in patients who take an inadequate amount of electrolytes or are treated with either corticosteroids or ACTH.Risk factors associated with the occurrence of hyperkalemia (due to the presence of telmisartan) include renal failure, heart failure and diabetes, as well as the use of preparations that increase the concentration of potassium in the blood. Hypersensitivity reactions to hydrochlorothiazide may occur in or with allergy or bronchial asthma, but are more likely in patients with history. Hydrochlorothiazide may cause photosensitivity reaction - in this case, it is recommended to stop the drug; if it is necessary to restart the diuretic therapy, it is recommended to protect the body against sunlight or artificial UV radiation. The safety and efficacy of the preparation in children and adolescents <18 years have not been established. Due to the lactose and sorbitol content, the preparation should not be used in patients with hereditary fructose intolerance and / or rare congenital galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.

The use of telmisartan in the first trimester of pregnancy is not recommended (there is a risk of teratogenic effects). The use of telmisartan 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. Thiazides penetrate the placental barrier. Hydrochlorothiazide in the second and third trimester may lead to decreased fetal-placental perfusion and may cause abnormalities in the fetus and newborn, such as jaundice, electrolyte imbalance and thrombocytopenia. Hydrochlorothiazide should not be used in pregnancy edema, gestational hypertension and preeclampsia due to the risk of decreased plasma volume and placental ischemia, without a beneficial effect on the course of the disease. Hydrochlorothiazide should not be used in idiopathic hypertension in pregnant women except in rare situations where alternative treatment is not possible. Thiazides are excreted in breast milk and can inhibit lactation. The preparation is not recommended during breast-feeding. When using the product during breastfeeding, the lowest possible doses should be used.

Common: dizziness. Uncommon: hypokalemia, anxiety, fainting, paresthesia, dizziness, tachycardia, tachycardia, arrhythmias, hypotension, orthostatic hypotension, dyspnoea, diarrhea, dry mouth, flatulence, back pain, muscle spasms, muscle pain, erectile dysfunction, chest pain, increase in uric acid in the blood. Rare: bronchitis, pharyngitis, sinusitis, exacerbation or activation of systemic lupus erythematosus, increased uric acid in the blood, hyponatremia, depression, insomnia, sleep disorders, blurred vision, respiratory distress syndrome (including pneumonia and edema lung), abdominal pain, constipation, dyspepsia, vomiting, gastritis, liver dysfunction, angioneurotic edema (also fatal), erythema, pruritus, rash, hyperhidrosis, urticaria, joint pain, muscle cramps, limb pain, flu-like symptoms , pain, increase in blood creatinine, increase in creatine phosphokinase in the blood, increased activity of liver enzymes. In addition, there may be adverse reactions to individual components, even if not observed in the clinical trials of the combined preparation. Telmisartan: uncommon: urinary tract infections (including cystitis), upper respiratory tract infection, anemia, hyperkalemia, bradycardia, cough, renal dysfunction (including acute renal failure), weakness; rarely: sepsis (including fatal outcome), eosinophilia, thrombocytopenia, hypersensitivity reactions, anaphylactic reaction, hypoglycaemia (in patients with diabetes), drowsiness, stomach disorders, eczema, eruptions, toxic excrescence, osteoarthritis, tendon pain , reduction in hemoglobin; very rare: interstitial lung disease.Hydrochlorothiazide: salivary gland inflammation, aplastic anemia, hemolytic anemia, bone marrow failure, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, hypersensitivity reactions, anaphylactic reaction, improper diabetes control, anorexia, decreased appetite, electrolyte imbalance, hypercholesterolemia, hyperglycemia, hypovolemia, anxiety, dizziness, vision in yellow, acute angle glaucoma, necrotizing vasculitis, pancreatitis, abdominal pain, jaundice, cholestatic jaundice, lupus-like syndrome, photosensitivity reactions, vasculitis of the skin, toxic necrotic decay of the epidermis, weakness, interstitial nephritis, renal dysfunction, glycosuria, fever, increased triglycerides.

Orally. Adults: 1 tabl. once a day. A dose adjustment of each component of the preparation is recommended before using a fixed dose of the combined preparation. If this is considered clinically appropriate, a direct change from monotherapy to combination therapy may be considered. The 40/12.5 mg dose can be given to patients whose blood pressure is not adequately controlled with telmisartan 40 mg. The 80/12.5 mg dose may be given to patients whose blood pressure is not adequately controlled after the administration of 80 mg telmisartan. The 80/25 mg dose can be given to patients whose blood pressure is not adequately controlled after taking the 80 / 12.5 mg combination, or in patients who have previously been stabilized with telmisartan and hydrochlorothiazide alone.Special groups of patients. Patients with mild or moderate hepatic impairment should not exceed 40/12.5 mg once daily. Elderly patients do not need to adjust their dose.Way of giving. The tablets should be taken once a day, with liquid, can be taken regardless of the meal.