Hipotel 80 mg tablets № 28

Author Ольга Кияница

2017-05-11

Amount in a package -
Product form Pills
Manufacturer Kusum Pharm Ltd. (Ukraine, Sumi)
Registration certificate UA/13322/01/03
The main medicament Hipotel
morion code 240712

HYPOTEL instructions for use

Composition:

active ingredient: telmisartan; 1 tablet contains telmisartan 20 mg, 40 mg or 80 mg;
auxiliary substances: sodium hydroxide, meglumine, mannitol (B 421), crospovidone, magnesium stearate.

Dosage form.

Pills.

Basic physical and chemical properties:

white or almost white round biconvex tablets.

Pharmacotherapeutic group.

Simple preparations of angiotensin antagonists P. Code ATS C09C A07.

Pharmacological properties.

Pharmacodynamics.

Mechanism of action.

Telmisartan is a specific and selective antagonist of angiotensin II receptors (type AT1). Telmisartan with a very high degree of affinity replaces angiotensin II at its binding sites with the AT 1 subtype receptors responsible for the activity of angiotensin II. Telmisartan does not show any partial agonistic effect on the AT 1 -receptor. Telmisartan selectively binds the AT 1 receptor. Binding is lengthy. Telmisartan does not show affinity with other receptors, including AT2 and other less studied AT receptors. The functional role of these receptors is unknown, as the effect of their possible "overstimulation" by angiotensin II, whose level is enhanced by telmisartan, is unknown. Telmisartan reduces the level of aldosterone in the blood plasma. Telmisartan does not inhibit renin in human blood plasma, it does not block ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (kininase II), an enzyme that also breaks down bradykinin. Therefore, do not expect the potentiation of bradykinin-accompanying side effects.

In humans, telmisartan at a dose of 80 mg almost completely inhibits the increase in blood pressure, which is caused by angiotensin II. The blocking effect persists for 24 hours and remains appreciable up to 48 hours.

Pharmacokinetics.

Suction. The absorption of telmisartan is rapid, although the adsorbed amounts are different. The average absolute bioavailability of telmisartan is about 50%. When telmisartan is taken with food, the area under the plasma concentration-time curve (AUC) for telmisartan varies from about 6% (40 mg) to 19% (160 mg). 3 hours after the administration, the concentration in the blood plasma is the same, irrespective of whether telmisartan is taken on an empty stomach or with food.

Linearity / nonlinearity. It is believed that a slight decrease in AUC does not cause a decrease in therapeutic effectiveness. There is no linear relationship between dose and plasma level. max and to a lesser extent AUC increases disproportionally at doses above 40 mg.

Distribution. Telmisartan is actively associated with plasma proteins (> 99.5%), mainly with albumin and alpha-1 acid glycoprotein. The average value of the volume of distribution (V ss ) is approximately 500 liters.

Metabolism. Telmisartan is metabolized by conjugation to the glucuronide of the parent compound. The pharmacological activity of the conjugate has not been established.

Excretion. Telmisartan is characterized by bi-exponential pharmacokinetics with a terminal half-life of> 20 hours. The maximum concentration in plasma (C max ) and to a lesser extent AUC increase disproportionately to the dose. There is no evidence of a clinically significant cumulation of telmisartan when administered at the recommended doses.Concentrations in blood plasma were higher in women than in men, without a corresponding effect on efficacy.

After ingestion, telmisartan is almost completely excreted with feces, mainly as an unchanged compound. The cumulative renal excretion is <1% of the dose. The total plasma clearance (Cl tot ) is high (approximately 1000 ml / min) compared with hepatic blood flow (about 1500 ml / min).

Special categories of patients.

Children. The results of pharmacokinetic studies in children as a whole correspond to those obtained for adults, and confirm the nonlinearity of telmisartan, in particular for Cmax. Floor. Concentrations in blood plasma C max and AUC in women are approximately 3 and 2 times higher, respectively, than in men.

Patients of advanced age. The pharmacokinetics of telmisartan is not different in elderly people and under the age of 65 years.

Patients with impaired renal function. In patients with moderate, moderate and severe renal insufficiency, a double increase in plasma concentration was observed. However, in patients with renal failure who underwent dialysis, a low concentration in the blood plasma was observed. Telmisartan has a high affinity for plasma proteins in subjects with renal insufficiency and can not be eliminated by dialysis. In patients with renal failure, the half-life does not change.

Patients with impaired hepatic function. Pharmacokinetic studies in patients with hepatic impairment revealed an increase in absolute bioavailability of about 100%. In patients with hepatic insufficiency, the half-life does not change.

Clinical characteristics.

Indications.

Hypertension.

Treatment of essential hypertension in adults.

Prevention of cardiovascular diseases.

Reducing the incidence of cardiovascular disease in patients with:

  • a manifest atherothrombotic cardiovascular disease (coronary heart disease, stroke or peripheral arterial disease in history);
  • type II diabetes mellitus with a documented lesion of target organs.

Contraindications

  • Hypersensitivity to the components of the drug;
  • pregnant women and women of reproductive age who may be pregnant (see the section on "Use during pregnancy or lactation");
  • obstructive biliary disorders;
  • severe violations of the liver.

The simultaneous use of telmisartan with aliskiren in patients with diabetes mellitus or with impaired renal function (GFR <60 ml / min / 1.73 m 2 ) is contraindicated (see the sections "Dosing and Administration", "Features of use", "Interaction with other medicinal means and other types of interactions ").

Interaction with other drugs and other types of interactions.

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

The combination of telmisartan and aliskiren is contraindicated in patients with diabetes mellitus and renal dysfunction (GFR <60 mL / min / 1.73 m 2 ) and is not recommended for other patients (see "Contraindications", "Features of Use").

Digoxin.

With simultaneous use of telmisartan and digoxin, mean increases in peak concentrations of digoxin in blood plasma (by 49%) and minimal concentrations (by 20%) were noted. At the beginning of the procedure, in the case of dose adjustment and discontinuation of telmisartan, digoxin levels should be monitored to maintain them within the therapeutic range.

As with other drugs that suppress the renin-angiotensin system, telmisartan can provoke hyperkalemia (see section "Features of application"). The risk may increase if treated in combination with other agents that can also provoke hyperkalemia (salt substitutes that contain potassium, potassium-sparing diuretics, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, non-steroidal anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors) , heparin, immunosuppressants (cyclosporine or tacrolimus), and trimethoprim).

Cases of hyperkalemia depend on the associated risk factors. Risk increases in the case of the above therapeutic combinations. Especially high risk in combination with potassium-sparing diuretics and in combination with salt substitutes that contain potassium. Combination with ACE inhibitors or NSAIDs, for example, is less risky, provided that the precautions for use are clearly observed.

Concomitant use is not recommended.

Potassium-sparing diuretics or potassium supplements. Such angiotensin II receptor antagonists, like telmisartan, mitigate the diuretic-induced loss of potassium. Potassium-sparing diuretics, for example spironolactone, eplerenone, triamterene or amiloride, potassium supplements or salt substitutes that contain potassium, can cause a significant increase in potassium concentration in the blood serum. If concomitant use is shown due to documented hypokalemia, they should be taken with caution, often by monitoring the potassium level in the serum.

Lithium. There are cases of reverse growth of lithium serum concentrations and an increase in toxicity with concomitant use of lithium with angiotensin converting enzyme inhibitors and angiotensin II receptor antagonists, including telmisartan. If the appointment of this combination is considered necessary, during the joint application, the level of lithium in the blood serum should be closely monitored.

Concomitant use requires caution.

Non-steroidal anti-inflammatory drugs. NSAIDs (ie, acetylsalicylic acid in anti-inflammatory doses, COX-2 inhibitors and nonselective NSAIDs) can reduce the antihypertensive effect of angiotensin II receptor antagonists.

In some patients with impaired renal function (eg patients with dehydration or elderly patients with impaired renal function), the combined use of angiotensin II receptor antagonists and cyclooxygenase inhibiting agents may lead to further impairment of kidney function, including possible acute renal failure, which is usually reversible. Therefore, this combination should be administered with caution, especially to the elderly. Patients should ensure proper hydration; In addition, after the onset of combination therapy, and also periodically in the future, it is necessary to monitor kidney function.

There is evidence that the combined use of telmisartan and ramipril leads to a 2.5-fold increase in AUCo-24 and Cmax ramipril and ramiprilate. The clinical significance of this observation is unknown.

Diuretics (thiazide or loop diuretics). Preliminary treatment with high doses of such diuretics as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic) can lead to loss of volume and risk of hypotension if treatment with telmisartan is started.

It should be taken into account with concomitant application.

Other antihypertensive drugs. The ability of telmisartan to lower blood pressure can be increased by the concomitant use of other antihypertensive agents.

Based on the pharmacological properties of baclofen and amifostine, these drugs can be expected to enhance the antihypertensive effect of all antihypertensive agents, including telmisartan. In addition, orthostatic hypotension can be worsened by alcohol, barbiturates, drugs and antidepressants.

Corticosteroids (systemic application). Reduction of antihypertensive action.

Features of application.

Liver failure. Hypotheses can not be prescribed to patients with cholestasis, obstructive biliary duct disease and severe hepatic insufficiency (see the "Contraindications" section), since telmisartan is excreted mainly with bile. In such patients, a decrease in the hepatic clearance of telmisartan can be expected. Hypotheses should be administered with caution to patients with moderate to moderate hepatic impairment.

Renovascular hypertension. There is an increased risk of severe arterial hypotension and renal failure if patients with bilateral renal artery stenosis or stenosis of the single kidney artery are treated with drugs that affect the renin-angiotensin-aldosterone system.

Renal failure and kidney transplantation. When Hipotel is prescribed for patients with impaired renal function, periodic monitoring of serum potassium and serum creatinine levels is recommended. There is no experience with telmisartan in patients with recent kidney transplantation.

Decrease intravascular volume of fluid. Symptomatic hypotension, especially after the first dose of Hipotela, may occur in patients with a reduced intravascular volume and / or sodium level that occurs as a result of diuretic therapy, restriction of salt from food, diarrhea, or vomiting. Before receiving Hipotel, it is necessary to adjust such conditions, especially the reduction of intravascular volume and / or sodium level.

Double blockade of the renin-angiotensin-aldosterone system.

The use of telmisartan in combination with aliskiren in patients with diabetes mellitus or with impaired renal function (GFR <60 mL / min / 1.73 m 2 ) is contraindicated (see section "Contraindications").

As a result of inhibition of the renin-angiotensin-aldosterone system, arterial hypotension, syncope, hyperkalemia and changes in renal function (including acute renal failure) were observed in more sensitive patients, especially if the combination therapy included medications that affect this system. Therefore, a double blockade of the renin-angiotensin-aldosterone system (eg, the use of telmisartan with other renin-angiotensin-aldosterone blockers) is not recommended.If the need for simultaneous use is recommended careful monitoring of kidney function.

Other conditions requiring stimulation of an angina-angiotensin-aldosterone system.

In patients whose vascular tone and renal function depend mainly on the activity of the renin-angiotensin-aldosterone system (for example, patients with severe congestive heart failure or severe kidney disease, including renal artery stenosis), telmisartan with other medications affecting renin-angiotensin-aldosterone system, was associated with acute arterial hypotension, hyperazotemia, oliguria, and occasionally with acute renal failure (see "Adverse Reactions" section).

Primary hyperaldosteronism. Patients with primary hyperaldosteronism generally do not respond to antihypertensive drugs, which act by blockade of the renin-angiotensin system. Therefore, the appointment of telmisartan is not recommended.

Stenosis of the aorta and mitral valve, obstructive hypertrophic cardiomyopathy. As with other vasodilators, special care should be taken to prescribe patients who have been diagnosed with aortic stenosis, mitral valve, or obstructive hypertrophic cardiomyopathy.

Diabetic patients who are treated with insulin or antidiabetic drugs.

During treatment with telmisartan, hypoglycemia may develop in such patients. Consideration should be given to the need for appropriate monitoring of blood glucose levels in such patients. If indicated, it may be necessary to adjust the dosage of insulin or anti-diabetic medications.

In patients with diabetes mellitus with cardiovascular risk (patients with diabetes mellitus with concomitant diseases of the coronary arteries) the risk of developing a myocardial infarction with a fatal outcome and sudden cardiovascular death may be higher when treated with antihypertensive drugs such as angiotensin II receptor antagonists and ACE inhibitors. In patients with diabetes mellitus, the course of concomitant diseases of the coronary arteries can be asymptomatic, and therefore they can be undiagnosed. Patients with diabetes should be carefully screened, for example, by stress testing to identify and treat concomitant diseases of the coronary arteries before prescribing the drug.

Hyperkalemia. During the entire intake of medications that affect the renin-angiotensin-aldosterone system, hyperkalemia may occur.

In elderly people, in patients with renal insufficiency, diabetes, in patients who are in parallel treated with other drugs that can lead to increased potassium levels and / or in patients with concomitant diseases, hyperkalemia can lead to death.

Before considering the question of the concomitant use of drugs that suppress the renin-angiotensin system, it is necessary to weigh the ratio of benefit and risk. The following are the main risk factors for the development of hyperkalemia, which need to be addressed.

  • Diabetes mellitus, renal failure, age (over 70 years).
  • Combination therapy with one or more other drugs affecting renin-angiotensin system, and / or potassium supplements. For drugs or therapeutic groups of drugs that can cause hyperkalemia belong salt substitutes containing potassium, potassium-sparing diuretics, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, nonsteroidal antiinflammatory drugs (NSAIDs, including selective COX-2 inhibitors), heparin, immunosuppressants ( cyclosporin or tacrolimus), and trimethoprim.
  • Concomitant diseases, especially dehydration, acute cardiac decompensation, metabolic acidosis, impaired renal function, a sharp deterioration in renal condition (e.g., infectious disease), cell lysis (e.g., acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk must be carefully control serum potassium concentration (cm. 'Interaction with other drugs and other types of interactions "section).

Ethnic differences. As with all other angiotensin II receptor antagonists, telmisartan is apparently less effective in lowering blood pressure in patients with blacks than in other races. Perhaps this is due to the higher prevalence of low renin states in the black race patients suffering from hypertension.

Other. As with any other antihypertensive agents, a significant reduction in blood pressure in patients with ischemic cardiomyopathy or ischemic cardiovascular disease could result in a myocardial infarction or stroke.

Use during pregnancy or lactation.

Pregnancy.

angiotensin II receptor antagonists should not be used for pregnant women or women who might be pregnant (see. "Contraindications"). If confirmed pregnancy during treatment with this drug, its use should be discontinued immediately and begin an alternative treatment if necessary.

Reported fatal cases of fetus and newborn, oligohydramnios, hypotension in the fetus and newborn, renal failure, hyperkalemia, hypoplasia of the skull, limb contractures / cerebral, craniofacial deformities / pulmonary dysplasia, possibly caused by oligohydramnios pregnant patients who used angiotensin receptor antagonists II or III in II trimester of pregnancy.

Patients who prepared the angiotensin II receptor antagonists and are planning a pregnancy should go on antihypertensive drugs, which have established safety profile for use during pregnancy.

Lactation.

Due to lack of information on the use of telmisartan lactation Hipotel not recommended for use. Preference is given to alternative treatment with a well-studied safety profile, especially when feeding a newborn or premature baby.

Fertility.

Preclinical studies revealed no effect of telmisartan on the fertility of men and women.

Ability to influence the reaction rate when driving or operating other machinery.

While driving and mechanical devices necessary to consider the possibility of dizziness or hypersomnia during antihypertensive therapy, including Hipotel drug.

Dosing and dose.

Treatment of hypertension.

The usual effective dose is 40 mg per day. Some patients may be sufficient daily dose of 20 mg. If desired blood pressure is not achieved, telmisartan dose can be increased to 80 mg 1 time per day. Alternatively telmisartan can be administered in combination with a thiazide diuretic, such as hydrochlorothiazide, which makes a further reduction of blood pressure when used with telmisartan. When considering an increase in dose, you must take into account that the maximum antihypertensive effect is generally achieved after 4-8 weeks of starting treatment.

Prevention of cardiovascular disease.

The recommended dose is 80 mg once a day. telmisartan Efficiency at doses less than 80 mg in the prevention of cardiovascular disease is unknown.

Starting telmisartan therapy for the prevention of cardiovascular disease, it is recommended to carry out a blood pressure monitor and, if necessary, adjust the dose of drugs that reduce blood pressure.

Special patient groups

Impaired renal function. Experience in treating patients with renal insufficiency or in patients on hemodialysis is limited. Such patients it is recommended to begin treatment with low doses of 20 mg (cm. "Application Features" section). For patients with mild renal insufficiency and moderate doses does not require correction. The simultaneous use of telmisartan with aliskiren patients with diabetes or impaired renal function (GFR <60 mL / min / 1.73 m 2 ) is contraindicated (cm. "Contraindications").

Abnormal liver function. Hipotel contraindicated in patients with severe hepatic impairment.

For patients with mild to moderate hepatic impairment daily dose should not exceed 40 mg 1 time per day (cm. "Application Features" section).

Elderly patients. There is no need for dose adjustment for elderly patients.

Mode of application.

Hipotel take one time a day orally with a sufficient quantity of liquid, together with or without food.

The tablets stored in a sealed blister to protect against moisture. Tablets must be removed from the blister immediately before use.

Children.

Hipotel contraindicated in children due to the limited information on the safety and efficacy of the drug for these patients.

Overdose.

Limited information on human overdosing.

Symptoms. The most significant manifestations of telmisartan overdose were hypotension and tachycardia; also reported bradycardia, dizziness, increase in serum creatinine, and acute renal failure.

Therapy. Telmisartan is not displayed by hemodialysis. Patients should be closely monitored and receive symptomatic and supportive therapy. Treatment time depends on the drug and the severity of symptoms. Recommended actions include vomiting and / or gastric lavage. Activated carbon can be used in the treatment of overdose. You must frequently check the level of electrolytes, and serum creatinine. In the event of hypotension the patient should be put on the back and provide assistance aimed at rapid replenishment volume of fluid and salt in the body.

Adverse reactions.

Infections and infestations: upper respiratory infections, including pharyngitis and sinusitis; urinary tract infections, including cystitis; sepsis, including fatal.

From the blood system and lymphatic system: anemia, thrombocytopenia, eosinophilia.

Immune system: hypersensitivity, anaphylactic reaction. Violations metabolism: hyperkalemia, hypoglycemia (in diabetic patients). Psychiatric disorders: depression, insomnia, anxiety.

From the nervous system: syncope, somnolence.

On the part of the organs of vision: visual disturbances.

On the part of ear, the vestibular apparatus: vertigo.

Of the heart: bradycardia, tachycardia.

On the part of the vessels: hypotension, orthostatic hypotension.

The respiratory system, organs, thoracic and mediastinal disorders: dyspnea, cough, interstitial lung disease.

On the part of the digestive tract: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting, stomach discomfort, dry mouth.

On the part of the hepatobiliary system: abnormal liver function / liver disorder. Skin and subcutaneous tissue: sweating, itching, rash, erythema, angioneurotic edema (including fatal), medicamentosa dermatitis, chronic dermatitis, eczema, urticaria.

On the part of the musculoskeletal system and connective tissue disorders: myalgia, back pain (eg sciatica), muscle cramps, arthralgia, pain in extremity, pain in the tendons (tendonitis like symptoms).

From the urinary system: renal function, including acute renal failure.

General disorders: chest pain, asthenia (weakness), influenza-like symptoms. Laboratory data: increased creatinine levels, increased uric acid in the blood, elevated liver enzymes, increased levels of creatine phosphokinase (CPK) in the blood, reduced hemoglobin.

Shelf life.

2 years.

Storage conditions.

Store at a temperature not higher than 25 ° C in its original packaging. Keep out of the reach of children.

Packaging.

10 tablets in a blister; 3 blisters in a carton box.
14 tablets in a blister; 2 or 4 or 6 blister packs in a cardboard box.

Category vacation.

On prescription.


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