More info
Description
Telsartan pills have a pronounced antihypertensive effect and are widely used to control and maintain blood pressure within acceptable values. The tool acts throughout the day, the duration of the effect after its use is observed within 48 hours. The drug begins to act within 3 hours after the initial intake, and only a month after the start of treatment with Telmisartan, the blood pressure drops to the maximum level in both lower and upper values without affecting the pulse rate.
Active ingredients
Telmisartan
Release form
Pills
Composition
Active ingredient: telmisartan. Excipients: meglumine, sodium hydroxide, Povidone K30, Polysorbate 80, mannitol, magnesium stearate.
Pharmacological effect
The mechanism of action of telmisartan is to block the receptor for the hormone angiotensin, which helps to increase blood pressure. Due to the blocking of these receptors, the lumen of the blood vessels expands, the blood pressure decreases. At the same time, patients do not develop a compensatory increase in heart rate in response to a decrease in pressure. In addition, studies have shown that telmisartan has a positive effect on the work of the kidneys, fights ischemia and atherosclerosis, and improves peripheral circulation.
Pharmacokinetics
Telmisartan is rapidly absorbed, the amount absorbed varies. Bioavailability of telmisartan is approximately 50%. When taking telmisartan simultaneously with food, the decrease in AUC (area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). After 3 hours after administration, plasma concentration levels out, regardless of the meal. A slight decrease in AUC does not reduce the therapeutic effect. 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 a significant effect on efficacy. Communication with plasma proteins is more than 99.5%, mainly with albumin and alpha-1 glycoprotein. The volume of distribution is approximately 500 liters.Telmisartan is metabolized by conjugating the parent substance with the glucuronide. Pharmacological activity of the conjugate was not detected. Telmisartan has a biexponential pharmacokinetics with a terminal half-life of> 20 hours. Cmax and - to a lesser extent - AUC increase disproportionately with the dose. Clinically significant cumulation of telmisartan was not detected. After oral administration, Telmisartan is almost completely excreted through the intestine in unchanged form. The total excretion in the urine is less than 2% of the dose. The overall plasma clearance is high (approximately 900 ml / min) compared with the “hepatic” blood flow (approximately 1500 ml / min). Elderly patients. The pharmacokinetics of telmisartan in elderly patients does not change. Patients with renal failure. Patients with renal failure on hemodialysis have lower plasma concentrations. In individuals with renal insufficiency, telmisartan binds more to plasma proteins and is not eliminated during dialysis. In renal failure, the half-life does not change. Patients with liver failure. In patients with hepatic insufficiency, the absolute bioavailability of telmisartan increases to 100%. The half-life for liver failure does not change.
Indications
Hypertension in adults. Reduced cardiovascular morbidity in adults with: severe atherothrombotic cardiovascular diseases (coronary artery disease, stroke, a history of peripheral arteries), type 2 diabetes mellitus with documented target organ damage.
Contraindications
Hypersensitivity to the active substance or auxiliary components of the drug, obstructive diseases of the biliary tract, severe liver dysfunction (Child-Pugh class C), pregnancy, breastfeeding period, age up to 18 years (efficacy and safety not established), simultaneous use with aliskiren in patients with diabetes mellitus or moderate / severe renal failure (GFR <60 ml / min / 1.73 m2).
Precautionary measures
With care: bilateral stenosis of the renal arteries, stenosis of the artery of the single kidney, the state after kidney transplantation (no experience),decrease in BCC due to previous diuretic therapy, restriction of salt intake, dehydration due to diarrhea and vomiting, chronic heart failure (CHF), primary hyper aldosteronism, hyponatremia, hyperkalemia, aortic and / or mitral valve stenosis, hypertrophic obstructive cardiomyopathy (hypertrophic obstructive cardiomyopathy, hypertrophic obstructive stenosis, aortic and / or mitral valve stenosis, hypertrophic obstructive cardiomyopathy) (class A and B on the scale of Child-Pugh) and / or kidney, ischemic heart disease.
Use during pregnancy and lactation
In pregnancy, the use of the drug Telsartan is contraindicated. When planning a pregnancy or when it is confirmed, it is necessary to cancel the drug as early as possible and prescribe another antihypertensive therapy with a known safety profile for use in pregnancy. The use of angiotensin II receptor antagonists, including and telmisartan, in the first trimester of pregnancy is not recommended. The drug is contraindicated in the II-III trimesters of pregnancy, because the use in the II-III trimesters of pregnancy can cause fetotoksicheskie effects (reduced kidney function, lack of water, slowing ossification of the bones of the cranium of the fetus) and neonatal toxic effects (renal insufficiency, hypotension, hyperkalemia). In the case of taking the drug in the II-III trimesters of pregnancy, an ultrasound of the kidneys and bones of the fetus must be performed. The use of Telsartan® during breastfeeding is not recommended, due to the lack of data on the possibility of separating telmisartan with breast milk. If necessary, the use of the drug during this period, breastfeeding should be discontinued.
Dosage and administration
Inside, regardless of the meal, 1 time / day. Arterial hypertension. The initial recommended dose is 40 mg 1 time / day. If necessary (in the absence of a therapeutic effect), the dose can be increased to a maximum daily dose of 80 mg 1 time / day. The maximum antihypertensive effect is achieved 4-8 weeks after the start of treatment with telmisartan. Possible combination with hydrochlorothiazide, which has an additive antihypertensive effect. Reduced cardiovascular morbidity. The recommended dose is 80 mg 1 time / day. The effectiveness of telmisartan in lower doses (less than 80 mg / day) for the prevention of cardiovascular morbidity has not been established. In patients with a view to reducing cardiovascular morbidity prior to the initiation of therapy with Telsartan, blood pressure control is recommended. If necessary, antihypertensive therapy should be corrected.Impaired renal function (including in patients on hemodialysis). Experience of use in patients with severe renal insufficiency or receiving treatment with hemodialysis is limited. In these patients, therapy is recommended to start with a lower dose of 20 mg / day. In patients with mild and moderate renal impairment, dose adjustment is not required. Liver dysfunction. For patients with mild or moderate liver dysfunction (class A and B on the Child-Pugh scale, respectively), the recommended dose is 40 mg 1 time / day. Elderly patients. Dose adjustment is not required.
Side effects
The observed cases of side effects did not correlate with the dose, gender, age or race of the patients. The safety of telmisartan in patients using a drug to prevent cardiovascular morbidity was similar to that in patients with arterial hypertension. Classification of the incidence of side effects (WHO): very often (> 1/10), often (1 / 10-1 / 100), rarely (1 / 100-1 / 1000), rarely (1 / 1000-1 / 10 000 ), very rarely (<1/10 000), frequency unknown (cannot be estimated based on available data). Infectious and parasitic diseases: infrequently - urinary tract infections, including cystitis, upper respiratory tract infections, incl. pharyngitis and sinusitis, rarely - sepsis, incl. with a fatal outcome. From the side of blood and lymphatic system: rarely - anemia, rarely - eosinophilia, thrombocytopenia. On the part of the immune system: rarely - anaphylactic reaction, hypersensitivity. On the part of the metabolism: infrequently - hyperkalemia, rarely - hypoglycemia (in patients with diabetes mellitus). Mental Disorders: Infrequently - insomnia, depression, rarely - anxiety. On the part of the nervous system: infrequently - fainting, rarely - drowsiness. On the part of the organ of vision: rarely - visual impairment. On the part of the organ of hearing and labyrinth disturbances: infrequently - vertigo. Since the cardiovascular system: infrequently - bradycardia, excessive decrease in blood pressure, orthostatic hypotension, rarely - tachycardia. On the part of the respiratory system: infrequently - shortness of breath, cough, very rarely - interstitial lung disease. On the part of the digestive system: rarely - bola in the abdomen, diarrhea, dyspepsia, bloating, vomiting, rarely - dryness of the oral mucosa, stomach discomfort. On the part of the liver and biliary tract: rarely - a violation of liver function. On the part of the skin and subcutaneous tissues: infrequently - pruritus, skin rash, rarely - angioedema (includingfatal), eczema, erythema, urticaria, drug skin rash, toxic skin rash. On the part of the musculoskeletal system: infrequently - back pain, muscle spasms, myalgia, rarely - arthralgia, pain in the extremities, pain in the tendons (symptoms of tendinitis). On the part of the urinary system: infrequently - impaired renal function, including acute renal failure. General reactions: infrequently - chest pain, asthenia (weakness), rarely - flu-like symptoms. Laboratory data: infrequently - an increase in the concentration of creatinine in the blood plasma, rarely - a decrease in the concentration of hemoglobin, an increase in the concentration of uric acid, an increase in the activity of liver enzymes, an increase in the activity of CPK. Description of some undesirable reactions Sepsis. According to the results of a single clinical study, an increase in the incidence of sepsis with telmisartan compared with placebo was found. Causal relationship not established. The mechanism is currently unknown. Arterial hypotension. Hypotension is more common in patients with controlled blood pressure who used telmisartan to reduce cardiovascular morbidity and mortality in the setting of standard therapy. Liver function impairment. Liver dysfunction was more common in Japanese. Interstitial lung disease. Cases of interstitial lung disease have been reported, chronologically associated with the use of telmisartan. However, a causal relationship has not been established.
Overdose
Data on overdose is limited. Symptoms: marked reduction in blood pressure, tachycardia, bradycardia. Cases of the development of vertigo, increased serum creatinine concentration and acute renal failure are described. Treatment: symptomatic therapy. Tactics of treatment depends on the time elapsed after taking the drug, and the severity of symptoms. Recommended gastric lavage, the use of activated carbon. The serum electrolyte content and serum creatinine concentration should be regularly monitored. With a pronounced decrease in blood pressure, it is necessary to transfer the patient to a supine position with their legs elevated, then measures should be taken to maintain the functions of the cardiovascular and respiratory systems, the BCC (administration of 0.9% sodium chloride solution in / in) and control of daily diuresis. Hemodialysis is ineffective.
Interaction with other drugs
Telsartan, like other drugs acting on the RAAS, can cause hyperkalemia. The risk of developing hyperkalemia increases with simultaneous use with other drugs that cause hyperkalemia, including with potassium-sparing diuretics, potassium preparations, potassium-containing dietary supplements and other drugs and substances that can increase serum potassium (eg, heparin), ACE inhibitors, angiotensin II receptor antagonists, NSAIDs, including selective COX-2 inhibitors, immunosuppressive drugs (cyclosporine or tacrolimus) and trimethoprim. The frequency of development of hyperkalemia depends on the presence of risk factors. With the simultaneous use of potassium-sparing diuretics and potassium-containing salt substitutes, the risk of developing hyperkalemia is particularly high. Simultaneous use with ACE inhibitors or NSAIDs is accompanied by a lower risk of developing hyperkalemia, provided that careful precautions are taken. The data obtained in clinical studies indicate an increase in the incidence of adverse events such as hypotension, hyperkalemia and decreased kidney function (including the development of renal failure) with a double blockade of RAAS due to the simultaneous use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren compared to only one drug that affects the RAAS. Simultaneous use with aliskiren in patients with diabetes mellitus or moderate / severe renal insufficiency (GFR <60 ml / min / 1.73 m2) is contraindicated. Simultaneous use is not recommended Calis-saving diuretics, potassium preparations or potassium-containing salt substitutes. Angiotensin II receptor antagonists, such as telmisartan, reduce potassium loss caused by diuretics. Potassium-sparing diuretics, such as spironolactone, eplerenone, triamterene or amiloride, potassium supplements or potassium-containing salt substitutes, can cause a significant increase in the serum potassium content. If their simultaneous use is necessary due to the presence of proven hypokalemia, treatment should be carried out with caution under frequent monitoring of the serum potassium content. Lithium.With simultaneous use of lithium preparations with ACE inhibitors, a reversible increase in plasma concentration of lithium was observed with the development of toxic effects. Similar changes in rare cases were noted with the use of angiotensin II receptor antagonists. If necessary, the simultaneous use of lithium preparations and angiotensin II receptor antagonists, incl. telmisartan, it is recommended to control the content of lithium in the blood plasma. Simultaneous use with caution PNVP, including selective COX-2 inhibitors, acetylsalicylic acid and non-selective NSAIDs. In patients with impaired renal function (for example, in patients with dehydration or elderly patients) with simultaneous use, further deterioration in renal function is possible, including the development of reversible acute renal failure. Use this combination with caution, especially in elderly patients. Therefore, before using telmisartan, it is recommended to evaluate the function of the kidneys, as well as correct the disturbances of water and electrolyte balance, in the future it is advisable to monitor the function of the kidneys. NSAIDs reduce the hypotensive effect of telmisartan. Ramipril Simultaneous use with ramipril leads to an increase in AUC0-24 and Cmax of ramipril and ramiprilat 2.5 times. The clinical significance of this effect has not been established. Diuretics (thiazide and "loop"). Prior diuretic therapy in high doses, incl. furosemide ("loopback" diuretic) and hydrochlorothiazide (thiazide diuretic), can lead to a decrease in bcc and an increased risk of arterial hypotension at the beginning of telmisartan therapy. Given the pharmacological properties, potentiation of the antihypertensive effect is possible with simultaneous use with baclofen and amifostine. Ethanol, barbiturates, anesthetics and antidepressants can contribute to the development of orthostatic hypotension. GCS reduces the antihypertensive effect of telmisartan. When taking telmisartan with digoxin, there is a median increase in the maximum and residual concentration of digoxin in the blood plasma (49% and 20%, respectively).At the beginning, with correction and discontinuation of telmisartan, it is necessary to control the concentration of digoxin in order to maintain it within the therapeutic range.
special instructions
Liver dysfunction. Telsartan should not be used in patients with cholestasis, obstruction of the biliary tract or severe liver dysfunction, because Telmisartan is primarily excreted in the bile through the intestines. The drug Telsartan® should be used with caution in patients with mild or moderate liver dysfunction (class A and B on the Child-Pugh scale). Violation of the kidney function. When using the drug Telsartan in patients with renal insufficiency, it is recommended to control the serum potassium content and creatinine concentration. There is no experience with recent kidney transplantation. Hypovolemia. In patients with hypovolemia and / or hyponatremia, due to intensive diuretic therapy, restriction of salt intake, diarrhea or vomiting, symptomatic hypotension may develop, especially after taking the first dose of telsartan. Before starting therapy, water and electrolyte balance disorders should be corrected. Renovascular hypertension. When using angiotensin II receptor antagonists in patients with bilateral renal artery stenosis or stenosis of a single functioning kidney, the risk of severe arterial hypotension and renal failure is increased. Double RAAS blockade. Cases of increased risk of arterial hypotension, hyperkalemia, and decreased renal function (up to the development of acute renal failure) have been reported with the simultaneous use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren. Therefore, double blocking of RAAS using a combination of ACE inhibitors, angiotensin II receptor antagonists, or aliskiren is not recommended. When absolutely necessary, therapy with the use of double blockade of RAAS should be carried out under the supervision of a specialist and careful monitoring of the function of the kidneys, electrolytes and blood pressure. ACE inhibitors and angiotensin II receptor antagonists should not be used simultaneously in patients with diabetic nephropathy. Other conditions accompanied by the activation of RAAS.In patients whose vascular tone and renal function is determined by RAAS activity (for example, patients with chronic heart failure or kidney disease, including stenosis of two renal arteries or stenosis of a single kidney artery), the use of drugs that affect the RAAS can be accompanied by the development of arterial hypotension, hyperazotemia, oliguria and, in rare cases, acute renal failure. Primary hyper aldosteronism. Patients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect the RAAS, so these patients are not recommended to use Telsartan. Stenosis of the aortic and / or mitral valves, GOKMP. Telsartan should be used with caution in patients with hemodynamically significant stenosis of aortic and / or mitral valves or with GOKMP. Patients with diabetes mellitus who receive insulin or hypoglycemic agents for oral administration. When telmisartan is used in these patients, hypoglycemia may develop. It is recommended to regularly monitor the concentration of blood glucose and, if necessary, to correct the dose of hypoglycemic agents. The use of drugs that affect the RAAS can cause hyperkalemia. Before the simultaneous use of drugs that affect the RAAS should assess the ratio of benefit / risk. Risk factors for hyperkalemia: renal failure, elderly patients (over 70 years old), diabetes mellitus, simultaneous use of drugs that affect the RAAS (for example, ACE inhibitors, angiotensin II receptor antagonists) and / or potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), as well as preparations of potassium or potassium-containing substitutes for edible salt, as well as NSAIDs (including selective COX-2 inhibitors), heparin, immunosuppressive drugs (cyclosporine or tacrolimus) and trimethoprim, soput solid states (reduced BCC, heart failure in the decompensation stage, metabolic acidosis, deterioration of kidney function, sudden progression of kidney disease (eg, infectious diseases), conditions accompanied by tissue ischemia / necrosis (eg, acute limb ischemia, rhabdomyolysis, extensive trauma)) In patients at high risk, use with caution and regularly monitor the content of potassium in the blood serum. Ethnic features.Telmisartan (as well as other drugs that affect the RAAS) has a less pronounced antihypertensive effect in patients of the Negroid race compared to other races, possibly due to a higher incidence of hyporinemia in patients with arterial hypertension. As with the treatment of any antihypertensive drugs, an excessive decrease in blood pressure in patients with coronary artery disease or cerebrovascular diseases can lead to the development of myocardial infarction or stroke. The effect on the ability to drive vehicles and mechanisms. Against the background of the use of the drug Telsartan, patients should be careful when driving vehicles and other technical devices in connection with the possibility of dizziness, drowsiness and other side effects that are characteristic of drugs used to treat hypertension.