Telmisartan

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Clinical Pharmacology

Pharmacotherapeutic group: Angiotensin II receptor antagonist

ATH:

C.09.C.A.07 Telmisartan

Pharmacodynamics:

Telmisartan is a specific angiotensin II receptor antagonist (type AT1), effective when taken orally. It has a high affinity for the AT1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from its association with the receptor, not having the action of an agonist on this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible over-stimulation with angiotensin II, the concentration of which increases with the administration of telmisartan, has not been studied. Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block the ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (kininase II) (an enzyme that also destroys bradykinin). Therefore, an increase in side effects caused by bradykinin is not expected.

In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of the antihypertensive effect is noted within 3 hours after the first intake of telmisartan inside. The effect of the drug lasts for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.

In patients with hypertension, telmisartan reduces systolic and diastolic blood pressure (BP), without affecting the heart rate (HR).

In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to the original level without the development of the "cancellation" syndrome.

Pharmacokinetics:

Suction

When ingestion is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (the area under the concentration-time curve) ranges from 6% (at the 40 mg dose) to 19% (at the 160 mg dose). After 3 hours after ingestion, plasma concentration levels off regardless of food intake.

Distribution

Communication with plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution at an equilibrium concentration is 500 l.

Metabolism

Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.

Removal

The half-life (T1 / 2) is more than 20 hours. Excreted through the intestine unchanged, the excretion of the kidneys - less than 2% of the dose. The overall plasma clearance is high (900 ml / min) compared with "hepatic blood flow" (about 1500 ml / min).

Pharmacokinetics in Special Patient Groups

Gender Differences

There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared to men without significant effect on efficacy. Dose adjustment is not required.

Elderly patients

The pharmacokinetics of telmisartan in elderly patients does not differ from pharmacokinetics in younger patients. Dose adjustment is not required.

Patients with impaired renal function

In patients with mild and moderate renal dysfunction, dose adjustment of telmisartan is not required.

Patients with severe renal insufficiency and patients on hemodialysis are recommended a lower initial dose of 20 mg per day.

Telmisartan is not excreted by hemodialysis.

Patients with impaired liver function

Pharmacokinetic studies in patients with hepatic insufficiency showed an increase in the absolute bioavailability of telmisartan to almost 100%.

When liver failure T1 / 2 does not change.In patients with mild and moderate liver dysfunction (class A and B on the Child-Pugh scale), the daily dose of the drug should not exceed 40 mg.

Indications

- Arterial hypertension;

- Reducing cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular disease.

Composition

Each 40 mg tablet contains:active substance: Telmisartan - 40.00 mg;

excipients: sodium hydroxide - 3.40 mg, povidon-K25 - 10.80 mg, meglumin - 12.00 mg, mannitol - 163.80 mg, magnesium stearate - 4.00 mg, crospovidone - 6.00 mg

Telmisartan is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Telpres			pills
Telmisartan-SZ			pills
			pills
Micardis	Boehringer Ingelheim	Austria	pills

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Dosage and Administration

Orally, regardless of the meal.

Arterial hypertension

The initial recommended dose of Telpres is 1 tab. (40 mg) once a day. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telpres can be increased to 80 mg once a day. When deciding whether to increase the dose should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment.

Reduced cardiovascular morbidity and mortality

The recommended dose is 1 tablet of Telpres 80 mg 1 time per day.

In the initial period of treatment, it is recommended to monitor the level of blood pressure (BP), may require correction of antihypertensive therapy.

Renal dysfunction

Patients with severe impaired renal function and patients on hemodialysis have limited experience. In these patients, the recommended starting dose is 20 mg per day. Patients with mild and moderate renal impairment do not require dose adjustment.

Liver dysfunction

In patients with mild and moderate liver dysfunction (class A and B on the Child-Pugh scale, respectively) the daily dose of Telpres should not exceed 40 mg.

Elderly patients

Elderly patients do not require dose adjustment.

Adverse reactions

In general, the incidence of adverse reactions noted for telmisartan is comparable to that for placebo. The observed cases of side effects did not correlate with the gender, age, or race of the patients. Classification of the frequency of adverse reactions of the World Health Organization (WHO): very often (> 1/10); often (from> 1/100 to 1/1000 to 1/10 000 to

Infectious and parasitic diseases:

infrequently: upper respiratory tract infections, including pharyngitis and sinusitis, urinary tract infections (including cystitis);

unknown frequency: sepsis, including sepsis with a fatal outcome.

Violations of the blood and lymphatic system:

infrequently: anemia;

rarely: thrombocytopenia;

unknown frequency: eosinophilia.

Mental disorders:

infrequently: depression; rarely: anxiety.

Nervous system disorders:

infrequently: insomnia, syncope, vertigo; rarely: fainting.

Violations by the organ of vision:

rarely: visual impairment.

Heart disorders:

infrequently: bradycardia; seldom: tachycardia.

Vascular disorders:

infrequently: pronounced decrease in blood pressure *, orthostatic hypotension;

* Frequently observed in patients with controlled blood pressure who received treatment with telmisartan to reduce the risk of cardiovascular mortality in addition to standard treatment.

Disorders of the respiratory system, organs of the chest and mediastinum:

infrequently: shortness of breath, cough.

Disorders of the gastrointestinal tract:

infrequently: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting;

rarely: indigestion, discomfort, dryness of the oral mucosa, abnormal liver function / liver disease.

Immune system disorders:

rarely: hypersensitivity, angioedema (including fatal); unknown frequency: anaphylactic reaction.

Violations of the skin and subcutaneous tissue

infrequently: hyperhidrosis, pruritus, rash;

rarely: erythema, drug rash, toxic skin rash, eczema, unknown frequency: urticaria.

Disorders of the musculoskeletal system and connective tissue: infrequently: myalgia, back pain (eg, sciatica), muscle cramps;

rarely: arthralgia, pain in the limbs;

unknown frequency: pain in the tendon area (tendinitis-like symptoms).

Kidney and urinary tract disorders:

infrequently: renal failure, including acute renal failure.

Disorders from the side of nutrition and metabolism:

infrequently: hyperkalemia.

Common disorders:

infrequently: chest pain, asthenia (weakness);

rarely: flu-like state.

Impact on the results of laboratory parameters and instrumental studies:

infrequently: increased concentration of creatinine in the blood;

rarely: increased uric acid concentration in the blood, “liver” enzymes, serum creatine phosphokinase activity, decreased hemoglobin, hypoglycemia (in patients with diabetes mellitus).

Contraindications

- Hypersensitivity to the active substance or auxiliary components of the drug;

- Pregnancy;

- The period of breastfeeding;

- Obstructive diseases of the biliary tract;

- Severe abnormal liver function (class C on the Child-Pugh scale);

- Simultaneous use of the drug Telpres with aliskiren in patients with diabetes and / or impaired renal function (glomerular filtration rate less than 60 ml / min / 1.73 m2);

- Simultaneous use of ACE inhibitors in patients with diabetic nephropathy;

- Age up to 18 years (efficacy and safety have not been established).

Carefully:

- Bilateral renal artery stenosis or single kidney artery stenosis;

- Violations of the liver and / or kidneys (see section "Special instructions");

- Condition after kidney transplantation (no experience);

- Decreased circulating blood volume (BCC) due to previous diuretic therapy, restriction of salt, diarrhea or vomiting;

- Hyponatremia;

- Hyperkalemia;

- Chronic heart failure;

- Coronary heart disease;

- Aortic and mitral valve stenosis;

- Idiopathic hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy);

- Primary aldosteronism (efficacy and safety have not been established);

- Simultaneous use with ACE inhibitors or aliskiren;

- Simultaneous use with potassium preparations, potassium-sparing diuretics;

- Diabetes.

Drug interactions

Telmisartan may increase the antihypertensive effect of other antihypertensive drugs. Other types of interactions of clinical significance have not been identified. Combined use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interaction.

Double blockade of the renin-angiotensin-aldosterone system (RAAS).

Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes or renal failure (GFR less than 60 ml / min / 1.73 m2 of body surface area) and is not recommended for other patients. Simultaneous use of telmisartan and inhibitors of AG1F is contraindicated in patients with diabetic nephropathy.

Data from clinical studies have shown that double blockade of the RAAS due to the combined use of ACE inhibitors, ARA II or aliskiren is associated with an increased incidence of adverse events, such as arterial hypotension, hyperkalemia and impaired renal function (including acute renal failure) compared to using only one drug acting on the RAAS.

The risk of developing hyperkalemia may increase when used in conjunction with other drugs that can cause hyperkalemia (potassium-containing dietary supplements and salt substitutes containing potassium and potassium-sparing diuretics (spironolactone, eplerenone, triamterene, or amiloride), nonsteroidal anti-inflammatory drugs (NPVV). 2 (COX)), heparin, immunosuppressants (cyclosporine, tacrolimus, trimethoprim)). If necessary, against the background of documented hypokalemia, the combined use of drugs should be carried out with caution and regularly monitor the content of potassium in the blood plasma.

Digoxin

When co-administration of telmisartan with digoxin, an increase in the mean Cmax of digoxin in the blood plasma by 49% and a minimum concentration by 20% was noted. At the beginning of treatment, when selecting a dose and stopping treatment with telmisartan, the concentration of digoxin in the blood plasma should be carefully controlled to maintain it within the therapeutic range.

Potassium-sparing diuretics or potassium-containing dietary supplements

Angiotensin II receptor antagonists, such as telmisartan, reduce the potassium loss caused by diuretics. Potassium-sparing diuretics, for example, spironolactone, eplerenone, triamterene or amiloride, potassium-containing dietary supplements or salt substitutes can lead to a significant increase in plasma potassium. If concomitant use is indicated, since there is documented hypokalemia, they should be used with caution and against the background of regular monitoring of potassium in the blood plasma.

Lithium preparations

When lithium preparations were taken together with ACE and APAII inhibitors, including telmisartan, there was a reversible increase in the concentration of lithium in the blood plasma and its toxic effect. If you need to use this combination of drugs is recommended to carefully monitor the concentration of lithium in the blood plasma.

Nonsteroidal anti-inflammatory drugs (NSAIDs)

NSAIDs (including acetylsalicylic acid in doses used for anti-inflammatory treatment, COX-2 inhibitors and non-selective NSAIDs) can weaken the antihypertensive effect of APAII. In some patients with impaired renal function (for example, patients with dehydration, elderly patients with impaired renal function), the combined use of APAII and cyclooxygenase-2 depressant drugs can lead to further deterioration of renal function, including the development of acute renal failure, which, as a rule, reversible. Therefore, the joint use of drugs should be carried out with caution, especially in elderly patients. Adequate fluid intake should be ensured, in addition, at the beginning of the joint use and periodically in the future, indicators of renal function should be monitored.

Diuretics (thiazide or loop diuretics)

Prior treatment with high doses of diuretics, such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic), can lead to hypovolemia and risk of developing hypotension at the beginning of treatment with telmisartan.

Other antihypertensive drugs

The effect of telmisartan may be enhanced by the combined use of other antihypertensive drugs. Based on the pharmacological properties of baclofen and amifostine, it can be assumed that they will enhance the therapeutic effect of all antihypertensive drugs, including telmisartan. In addition, orthostatic hypotension may increase with alcohol, barbiturates, narcotic drugs, or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the effect of telmisartan.

Pregnancy and Lactation

Drugs acting directly on the RAAS can cause serious damage and death of the developing fetus, so when planning or determining whether the drug is pregnant, the drug should be immediately canceled and, if necessary, an alternative antihypertensive therapy is prescribed, having an established safety profile when used during pregnancy. Use of the drug during pregnancy is contraindicated.

In preclinical studies of telmisartan, no teratogenic effects have been identified, but fetotoxicity has been established.It is known that exposure to angiotensin II receptor antagonists during the second and third trimesters of pregnancy causes fetotoxicity in a person (reduced kidney function, oligohydramnion, delayed cranial ossification), as well as neonatal toxicity (renal failure, hypotension, hyperkalemia). Patients planning a pregnancy should be given alternative therapy. If treatment with angiotensin II receptor antagonists occurred during the second trimester of pregnancy, it is recommended that ultrasound test the kidney function and the condition of the fetal skull.

Newborns whose mothers received angiotensin II receptor antagonists should be carefully monitored for hypotension.

Therapy with Telpres is contraindicated during breastfeeding. Studies of the effect on human fertility have not been conducted.

Special instructions

Liver function disorders

The use of the drug Telpres is contraindicated in patients with cholestasis, obstruction of the biliary tract or severe liver dysfunction (Child-Pugh class C) (see section "Contraindications"), since telmisartan is mainly excreted in the bile. It is believed that these patients have reduced hepatic clearance of telmisartan. In patients with mild or moderate liver function abnormalities (class A and B according to the Child-Pugh classification), Telpres should be used with caution (see section "With caution").

Renovascular hypertension

When treating drugs acting on the RAAS, in patients with bilateral arterial stenosis or arterial stenosis of a single functioning kidney, the risk of severe arterial hypotension and renal failure increases.

Impaired renal function and kidney transplantation

When using the drug Telpres in patients with impaired renal function, periodic monitoring of the content of potassium and creatinine in blood plasma is recommended. The experience of the clinical use of the drug Telpres in patients who recently underwent kidney transplantation is absent.

Decreased circulating blood volume

Symptomatic arterial hypotension, especially after the first dose of Telpres, may occur in patients with reduced BCC and / or sodium in the blood plasma on the background of previous treatment with diuretics, limitation of salt, diarrhea or vomiting. Such conditions (lack of liquid and / or sodium) should be eliminated before the start of Telpres administration.

Double blockade of the renin-angiotensin-aldosterone system

Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal failure (glomerular filtration rate less than 60 ml / min / 1.73 m2) (see section "Contraindications").

Simultaneous use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section "Contraindications").

As a result of inhibition of the RAAS, arterial hypotension, syncope, hyperkalemia and impaired renal function (including acute renal failure) in susceptible patients were noted, especially when several drugs were used together, also acting on this system. Therefore, a double blockade of RAAS (for example, against the background of receiving telmisartan with other RAAS antagonists) is not recommended.

In cases of dependence of the vascular tone and kidney function, mainly on the activity of the RAAS (for example, in patients with chronic heart failure or kidney disease, including stenosis of the renal arteries, or stenosis of the artery of a single kidney), the administration of drugs affecting this system can accompanied by the development of acute arterial hypotension, hyperazotemia, oliguria and, in rare cases, acute renal failure.

Primary aldosteronism

In patients with primary aldosteronism, treatment with antihypertensive drugs, which are mediated by inhibition of the RAAS, is generally ineffective.

Aortic stenosis and mitral valve, hypertrophic obstructive cardiomyopathy

Care must be taken when using Telpres (as well as other vasodilators) in patients with aortic or mitral stenosis, as well as hypertrophic obstructive cardiomyopathy.

Hyperkalemia

Taking medicines acting on the RAAS can cause hyperkalemia. In elderly patients, patients with renal insufficiency or diabetes mellitus, patients also taking medications that increase the plasma content of potassium, and / or patients with concomitant diseases, hyperkalemia can be fatal.

When deciding on the concomitant use of drugs acting on the RAAS, it is necessary to evaluate the risk-benefit ratio.

The main risk factors for the development of hyperkalemia that should be considered are:

- diabetes, renal failure, age (patients older than 70 years);

- combination with one or more drugs acting on the RAAS and / or potassium-containing food additives. Drugs or therapeutic classes of drugs that can cause hyperkalemia are salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, nonsteroidal anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors, heparin un synthesis), heparin IO, synthesis, anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors, heparin-ios, anti-inflammatory drugs (NSAIDs, including COX-2 inhibitors, heparin-ios), anesthetic anti-inflammatory drugs (NSAIDs, selective COX-2 inhibitors, heparin-i anti-inflammatory drugs). (cyclosporine or tacrolimus) and trimethoprim;

- intercurrent diseases, especially dehydration, acute heart failure, metabolic acidosis, impaired renal function, cytolysis syndrome (for example, acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk are advised to carefully monitor the potassium content in the blood plasma (see the section "Interaction with other drugs).

Ethnic differences

ACE inhibitors, telmisartan, and other APAII seem to be less effective at lowering blood pressure in patients of the Negroid race than in other races, possibly due to a greater propensity to decrease renin activity in the population of these patients.

Other

As with other antihypertensive drugs, an excessive reduction in blood pressure in patients with ischemic cardiomyopathy or ischemic heart disease can lead to myocardial infarction or stroke.

Impact on the ability to drive trans. Wed and fur .:

Special clinical studies of the effect of the drug on the ability to drive and mechanisms were not conducted. When driving and working with mechanisms that require increased concentration of attention, caution should be exercised, since dizziness and drowsiness can rarely occur while taking telmisartan.

Overdosage

Information regarding overdose is limited.

Symptoms: the most significant - marked reduction in blood pressure and tachycardia, bradycardia, dizziness, increased serum creatinine concentration and acute renal failure can also be observed.

Treatment: symptomatic and supportive. The proposed measures include: induction of vomiting and / or gastric lavage, ingestion of activated carbon, replenishment of lack of fluid and salt. Continuous monitoring of electrolyte and creatinine in serum. Hemodialysis is not effective.