Instruction for use: Telmisartan

The trade name of Telmisartan: Micardis, Pritor, Telmesteine-Richter, Tezeo, Telsap, Telmesteine, Telmista, Telsartan

Latin name of substance Telmisartan

Telmisartanum (genus. Telmisartani)

Chemical name

4 '- [[4-Methyl-6- (1-methyl-2-benzimidazolyl) -2-propyl-1-benzimidazolyl] methyl] -2-biphenylcarboxylic acid

Gross formula

C₃₃H₃₀N₄O₂

Pharmacological group of substance Telmisartan

Angiotensin II receptor antagonists (AT1 subtype)

The nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

CAS code

144701-48-4

Characteristics of the substance Telmisartan

White or colorless crystalline powder odorless, practically insoluble in water and at a pH of 3 to 9 partially soluble in strong acids (with the exception of hydrochloric acid), soluble in strong alkalis.

Pharmacology

Pharmacological action - antihypertensive.

It blocks the receptors of angiotensin II (subtype AT1). Dosocependently inhibits the pressor effect of angiotensin II, lowers the level of aldosterone in plasma, increases diuresis, excretion of sodium and chlorides. Has nephroprotective effect, reduces albuminuria. At 10% reduces renal blood flow, without worsening the glomerular filtration. In high doses reduces the severity of myocardial hypertrophy. In patients with arterial hypertension lowers both the SAD and DAD, without changing the heart rate.

Well absorbed from the digestive tract. Absolute bioavailability is 40-60% (due to the effect of "first passage" through the liver). After taking a single dose of 80 mg Cmax is achieved within 1 hour. Intensively binds to plasma proteins, mainly with albumin and acid alpha-1-glycoprotein. Relatively uniformly distributed in the body (highly lipophilic and easily penetrates tissues), the volume of distribution is 500 liters. Metabolised in the liver by conjugation with glucuronic acid, forming a stable inactive acylglucuronide, which is rapidly excreted in the bile: about 85% of unchanged telmisartan and 11% of glucuronide are found in faeces; Renal excretion does not exceed 2%. Output is slow, T1 / 2 is about 21 hours for men and 31 hours for women. Hypotension develops 3 hours after ingestion, persists for more than 24 hours and stabilizes for 4-8 weeks of course use. If you stop taking BP gradually (within a few days) returns to the initial values without the development of "ricochet" hypertension.

Application of the substance Telmisartan

arterial hypertension.

Contraindications

Hypersensitivity, obstruction of the biliary tract, severe violations of the liver and kidneys, pregnancy, breast-feeding.

Restrictions

Children and adolescence (safety and efficacy in children and adolescents are not defined).

Application of pregnancy and breastfeeding

Contraindicated in pregnancy. Before the planned pregnancy, it is recommended to replace the drug with another antihypertensive drug in advance.

The action category for fetus by FDA is D.

For the duration of treatment, breastfeeding should be stopped.

Side effects of the substance Telmisartan

From the nervous system and sensory organs: ≥ 1% - headache, dizziness.

On the part of the digestive system: ≥ 1% - nausea, indigestion, abdominal pain, diarrhea.

On the part of the respiratory system: ≥ 1% - cough, pharyngitis, influenza-like symptoms, lowering of tolerance to upper respiratory tract infections.

Other: ≥ 1% - chest and lower back pain, myalgia, urinary tract infections, lowering hemoglobin, increasing uric acid level.

Interaction

Hydrochlorothiazide enhances (mutually) the hypotensive effect. With the simultaneous appointment of ACE inhibitors, potassium-sparing diuretics and other drugs that can raise the level of potassium in the plasma, and potassium-containing food additives, especially in patients with renal insufficiency, the risk of developing hyperkalemia increases. Increases the concentration of lithium and digoxin in the blood.

Overdose

Symptoms: hypotension.

Treatment: symptomatic and supportive therapy. Hemodialysis is ineffective.

Routes of administration

Inside.

Precautions for the substance Telmisartan

Be wary appoint patients with symptomatic renovascular hypertension caused by bilateral stenosis of the renal arteries or stenosis of the renal artery of the only functioning kidney (increases the risk of severe hypotension and renal failure). Patients with moderate renal dysfunction require regular monitoring of the level of creatinine and electrolytes (potassium) in plasma. Caution should be exercised in appointing patients with reduced BCC and / or sodium deficiency (with diuretics, limited intake of salt, diarrhea, vomiting), aortic stasis and mitral valve, with obstructive hypertrophic cardiomyopathy, mild liver dysfunction, severe heart failure (constant Monitoring the level of potassium and serum creatinine), with IHD (possibly the development of acute coronary syndrome and myocardial infarction), peptic ulcer of the stomach or duodenum tadii exacerbation or others. diseases of the intestine (likely occurrence of gastrointestinal bleeding). It is not recommended for primary aldosteronism, congenital fructose intolerance (1 tablet 80 mg contains 338 mg sorbitol). Care should be taken to drivers of vehicles and people whose profession is associated with increased concentration of attention. With the simultaneous administration of digoxin or lithium preparations, monitoring of their serum content is required.