Pharmacological properties
Pharmacodynamics.
Telmisartan is an oral specific angiotensin II receptor antagonist (type AT1). With high affinity, telmisartan replaces angiotensin II at the sites of its binding to a variety of at1 receptors, through which the action of angiotensin II is mediated. Telmisartan does not exhibit any partial agonist effect on the at1 receptor. Telmisartan selectively binds to the AT1 receptor for a long time, without exerting even a partial agonistic effect on it. The bond is long lasting.
Telmisartan has no affinity for other receptors, including AT2 receptors and other AT receptors. The functional role of these receptors is not clear, as is the effect of their possible stimulation by angiotensin II, the levels of which are increased by telmisartan. Telmisartan reduces plasma aldosterone levels, does not block ion channels and does not reduce plasma renin levels. It does not inhibit angiotensin-converting enzyme (kininase II), an enzyme that also breaks down bradykinin. Therefore, bradykinin-mediated side effects are not expected.
In humans, a dose of 80 mg of telmisartan almost completely inhibits the increase in blood pressure caused by angiotensin II. The inhibitory effect lasts throughout the day and is determined up to 48 hours.
Pharmacokinetics. Telmisartan is rapidly absorbed, but the amount of drug that is absorbed varies. The average bioavailability of telmisartan is about 50%.
When telmisartan is administered with food, the AUC for telmisartan decreases from about 6% (40 mg dose) to about 19% (160 mg dose). 3 hours after administration, the concentration in the blood plasma becomes the same as when using telmisartan without food. It is believed that a slight decrease in AUC does not reduce the therapeutic effectiveness of the drug. There is no linear relationship between dose and plasma levels. Cmax and, to a lesser extent, AUC increase disproportionately at doses above 40 mg.
Telmisartan is highly bound to plasma proteins (more than 99.5%), mainly to albumin and α1-acid glycoprotein. The mean volume of distribution (Vss) at equilibrium is approximately 500 L.
Telmisartan is metabolized by conjugation to the glucuronide of the parent compound, which has no pharmacological activity.
Telmisartan is characterized by a biexponential pharmacokinetic curve with a terminal half-life of more than 20 hours. Cmax in blood plasma and, to a lesser extent, AUC increase disproportionately to the dose. When using telmisartan in recommended doses, no clinically significant accumulation was detected. Plasma concentrations were higher in women than in men, without a corresponding effect on efficacy.
After administration (and intravenous administration), telmisartan is almost completely excreted in the feces, mainly unchanged. Cumulative urinary excretion is less than 1% of the administered dose. The total plasma clearance (CLtot) is high (about 1000 ml/min) compared to blood flow through the liver (about 1500 ml/min).
Special categories of patients
Children. The pharmacokinetics of two doses of telmisartan were assessed as a secondary objective in hypertensive patients (n=57) aged 6 to 18 years after receiving telmisartan at a dose of 1 or 2 mg/kg body weight for 4 weeks of treatment. Pharmacokinetic objectives included determining steady-state telmisartan levels in children and adolescents and examining age-related differences. Although the study was powered to reliably evaluate pharmacokinetics in children under 12 years of age, the results are generally consistent with those obtained in adults and support the nonlinearity of telmisartan, particularly for Cmax.
Floor. Cmax and AUC in women are approximately 3 and 2 times higher, respectively, than in men.
Elderly patients. The pharmacokinetics of telmisartan do not differ between elderly patients and those under 65 years of age.
Patients with impaired renal function. In patients with moderate, moderate and severe renal failure, a 2-fold increase in plasma concentrations was noted. However, low plasma concentrations were detected in patients with renal failure undergoing dialysis. Telmisartan has a high affinity for plasma proteins in patients with renal failure and cannot be eliminated by dialysis. In patients with renal failure, T½ does not change.
Patients with impaired liver function. Pharmacokinetic studies in patients with liver impairment demonstrated an increase in bioavailability to approximately 100%. In patients with liver failure, T½ does not change.
Telmisartan
Telmisartan Telmisartan
Compound
Composition per 1 tablet 40 mg: active ingredient - telmisartan - 40.00 mg. Composition per 1 tablet 80 mg: active ingredient - telmisartan - 80.00 mg.
Pharmacotherapeutic group
Angiotensin II receptor antagonist.
ATX code
C09CA07
pharmachologic effect
Telmisartan is a specific angiotensin II receptor antagonist (ARA II) (AT1 type), 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 connection with the receptor, without having an agonist effect on this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. The connection is long-term. It has no affinity for other receptors, including AT2 receptors and other, less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation by angiotensin II, the concentration of which increases under the influence of telmisartan, have not been studied. Telmisartan reduces the concentration of aldosterone in the blood plasma, does not reduce the activity of renin in the blood plasma and does not block ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (ACE, kininase II), which also catalyzes the degradation of bradykinin. This avoids side effects associated with bradykinin (for example, dry cough). Arterial hypertension: Telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II in patients. The onset of antihypertensive action is observed within 3 hours after the first dose of telmisartan. The effect of the drug lasts for 24 hours and remains significant for up to 48 hours. A pronounced antihypertensive effect usually develops after 4-8 weeks of regular use of telmisartan. In patients with arterial hypertension, telmisartan reduces both systolic and diastolic blood pressure (BP) without affecting heart rate (HR). In case of abrupt withdrawal of telmisartan, blood pressure gradually (within several days) returns to initial values without the development of withdrawal syndrome. In comparative clinical studies, it was shown that the antihypertensive effect of telmisartan is comparable to the antihypertensive effect of drugs of other classes (amlodipine, atenolol, enalapril, hydrochlorothiazide and lisinopril). The incidence of dry cough was significantly lower in patients receiving telmisartan compared to those receiving ACE inhibitors. In patients aged 55 years or older with a history of coronary artery disease, stroke, transient ischemic attack, peripheral arterial disease, or complications of type 2 diabetes mellitus (eg, retinopathy, left ventricular hypertrophy, macro- or microalbuminuria) who are at risk for cardiovascular disease -vascular complications. Telmisartan had an effect similar to that of ramipril in reducing the primary composite endpoint of cardiovascular mortality, nonfatal myocardial infarction, nonfatal stroke, or hospitalization due to chronic heart failure. Telmisartan was as effective as ramipril in reducing the secondary endpoints of cardiovascular mortality, nonfatal myocardial infarction, or nonfatal stroke. The effectiveness of reducing the risk of cardiovascular mortality with doses of telmisartan less than 80 mg has not been studied. Dry cough and angioedema were less frequently described with telmisartan compared with ramipril, while arterial hypotension occurred more frequently with telmisartan. The safety and effectiveness of telmisartan in children and adolescents under 18 years of age have not been established.
Indications for use
Reduce cardiovascular morbidity and mortality in patients aged 55 years and older at high risk of cardiovascular disease.
Contraindications
- Hypersensitivity to the active substance or to the auxiliary components of the drug, - pregnancy and breastfeeding, - obstructive diseases of the biliary tract, - severe liver dysfunction (class C according to the Child-Pugh classification), - simultaneous use with aliskiren or aliskiren-containing drugs in patients with diabetes mellitus and/or moderate or severe renal impairment (glomerular filtration rate (GFR) less than 60 ml/min/1.73 m2 body surface area), - simultaneous use with angiotensin-converting enzyme inhibitors in patients with diabetic nephropathy, - lactase deficiency, lactose intolerance, glucose-galactose malabsorption, age up to 18 years (efficacy and safety have not been established).
Method of administration and dosage
Inside, regardless of the time of meal. Arterial hypertension: The initial recommended dose is 1 tablet (40 mg) of Telmisartan once a day. In some patients, taking telmisartan 20 mg per day may be effective. A 20 mg dose can be obtained by splitting a 40 mg tablet in half according to the score. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telmisartan can be increased to 80 mg once a day. Alternatively, the drug can be taken in combination with thiazide diuretics, for example, hydrochlorothiazide, which, when used together with telmisartan, had additional antihypertensive effects. If it is necessary to increase the dose, it should be taken into account that the maximum antihypertensive effect usually develops 4-8 weeks after the start of treatment (see section “Pharmacodynamics”). Reduction of cardiovascular morbidity and mortality: The recommended dose is 1 tablet of Telmisartan 80 mg once daily. Regular monitoring of blood pressure and, if necessary, dose adjustment of drugs that lower blood pressure are recommended. Special groups of patients For patients with mild to moderate renal impairment, no dose adjustment is required. Experience with telmisartan in patients with severe renal impairment or patients on hemodialysis is limited. A lower initial dose of 20 mg per day is recommended for these patients (see section "Special Instructions"). Liver failure In patients with mild to moderate liver dysfunction (Child-Pugh class A and B, respectively), the daily dose of Telmisartan should not exceed 40 mg. In patients with severe liver dysfunction (class C according to the Child-Pugh classification), the use of the drug is contraindicated (see section “Contraindications”). For elderly patients, no dose adjustment is required.
Release form
Tablets 40 mg and 80 mg. 5, 7, 10 or 20 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil. 10, 20, 28, 30, 40, 50 or 100 tablets in polyethylene terephthalate jars for medicines, sealed with screw-on lids with first opening control or a “push-turn” system made of polypropylene or polyethylene or polypropylene jars for medicines, sealed with lids pull-on with tamper-evident control made of polyethylene or polypropylene jars for medicines, sealed with tamper-evident pull-on lids made of high-density polyethylene. One can or 1, 2, 3, 4, 5, 8 or 10 blister packs along with instructions for use are placed in a cardboard package (pack).
Terms of release from pharmacies
Dispensed by prescription.
Application
Telmisartan-teva should be taken orally once a day with a sufficient amount of liquid, regardless of food intake.
Treatment of hypertension. The recommended dose is 40 mg/day. For some patients, a dose of 20 mg/day will be sufficient. If the blood pressure level does not decrease to the desired levels, then the dose can be increased to a maximum of 80 mg 1 time per day. Telmisartan-Teva can be prescribed in combination with thiazide diuretics, such as hydrochlorothiazide, which exhibit additional blood pressure lowering effects when administered together with telmisartan. When deciding whether to increase the dose, it should be borne in mind that the maximum hypotensive effect occurs 4–8 weeks from the start of treatment.
Prevention of cardiovascular diseases. The recommended dose is 80 mg 1 time per day. It is unknown whether the 80 mg dose of telmisartan is effective in reducing cardiovascular morbidity.
At the beginning of treatment with telmisartan, in order to reduce the risk of cardiovascular diseases, careful monitoring of blood pressure is recommended. It may be necessary to appropriately adjust the regimen of drugs that lower blood pressure.
Renal dysfunction. In patients with mild or moderate renal failure, there is no need for dose adjustment. There is limited experience with use in patients with renal failure or hemodialysis. For these patients, the recommended low starting dose is 20 mg.
Liver dysfunction. For patients with mild to moderate liver dysfunction, the dose should not exceed 40 mg/day. The drug is contraindicated in patients with severe liver dysfunction.
Elderly patients. No dose adjustment is required.
Instructions for use TELSARTAN®
Telsartan®, like other drugs acting on the RAAS, can cause hyperkalemia. The risk of developing hyperkalemia increases when used simultaneously with other drugs that cause hyperkalemia, incl. with potassium-sparing diuretics, potassium supplements, potassium-containing nutritional supplements and other drugs and substances that can increase potassium levels in the blood serum (for example, heparin), ACE inhibitors, angiotensin II receptor antagonists, NSAIDs, including selective COX-2 inhibitors, immunosuppressive drugs (cyclosporine or tacrolimus) and trimethoprim. The incidence 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 especially high. Concomitant use with ACE inhibitors or NSAIDs is accompanied by a lower risk of hyperkalemia, provided careful precautions are taken.
Data obtained from clinical studies indicate an increased incidence of adverse events such as hypotension, hyperkalemia and decreased renal function (including the development of renal failure) with dual blockade of the RAAS due to the simultaneous use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren compared with the use of only one drug that affects the RAAS.
Concomitant use with aliskiren in patients with diabetes mellitus or moderate/severe renal failure (GFR <60 ml/min/1.73 m2) is contraindicated.
Concomitant use is not recommended
Potassium-sparing diuretics, potassium supplements, 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 may cause a significant increase in serum potassium levels. If their simultaneous use is necessary due to the presence of proven hypokalemia, treatment should be carried out with caution and frequent monitoring of serum potassium levels.
Lithium
With the simultaneous use of lithium preparations with ACE inhibitors, a reversible increase in the concentration of lithium in the blood plasma was observed with the development of toxic effects. Similar changes have been observed in rare cases with the use of angiotensin II receptor antagonists. If necessary, simultaneous use of lithium preparations and angiotensin II receptor antagonists, incl. telmisartan, monitoring of lithium levels in the blood plasma is recommended.
Concomitant use with caution
NSAIDs, incl. selective COX-2 inhibitors, acetylsalicylic acid and non-selective NSAIDs
In patients with impaired renal function (eg, dehydrated or elderly patients), concomitant use may result in further deterioration of renal function, including the development of reversible acute renal failure. This combination should be used with caution, especially in elderly patients. Therefore, before using telmisartan, it is recommended to evaluate renal function, as well as correct water and electrolyte imbalances; In the future, it is advisable to monitor renal function. NSAIDs reduce the hypotensive effect of telmisartan.
Ramipril
Concomitant use with ramipril leads to an increase in AUC0-24 and Cmax of ramipril and ramiprilat by 2.5 times. The clinical significance of this effect has not been established.
Diuretics (thiazide and loop)
Previous therapy with diuretics in high doses, incl. furosemide (“loop” diuretic) and hydrochlorothiazide (thiazide diuretic), can lead to a decrease in blood volume and an increased risk of arterial hypotension at the beginning of therapy with telmisartan.
Concomitant use requiring attention
Telmisartan enhances the effect of other antihypertensive drugs.
Considering the pharmacological properties, it is possible to potentiate the antihypertensive effect when used simultaneously with baclofen and amifostine.
Ethanol, barbiturates, anesthetics and antidepressants
may contribute to the development of orthostatic hypotension.
GKS
reduce the antihypertensive effect of telmisartan.
When taking telmisartan with digoxin
There is a median increase in the maximum and residual concentrations of digoxin in the blood plasma (49% and 20%, respectively). During initiation, adjustment, and discontinuation of telmisartan, digoxin concentrations must be monitored to maintain them within the therapeutic range.
Contraindications
Hypersensitivity to the active substance or any of the excipients of the drug.
Pregnant women or women planning to become pregnant (see Use during pregnancy or lactation). Obstructive diseases of the bile ducts. Severe liver dysfunction. Children under 18 years of age. The simultaneous use of telmisartan and aliskiren-containing drugs is contraindicated in patients with diabetes mellitus or impaired renal function (glomerular filtration rate 60 ml/min/1.73 m2) (see INTERACTIONS and PHARMACOLOGICAL PROPERTIES).
Side effects
Serious adverse events, including anaphylactic reactions and angioedema, are possible in isolated cases, and acute renal failure has also been observed.
Infectious diseases and infestations: infectious diseases of the upper respiratory tract (including pharyngitis and sinusitis), infectious diseases of the urinary tract (including cystitis), sepsis (including fatal ones)1.
Disorders of the blood and lymphatic system: anemia, thrombocytopenia, eosinophilia.
Immune system disorders: hypersensitivity, anaphylactic reactions.
Metabolism disorders: hyperkalemia, hypoglycemia (in patients with diabetes mellitus).
Mental disorders: depression, insomnia, anxiety.
Neurological disorders: fainting, drowsiness.
Visual disorders: visual impairment.
Disorders of the hearing and vestibular apparatus: vertigo.
Cardiovascular system disorders: bradycardia, tachycardia, arterial hypotension2, orthostatic hypotension.
Disorders of the respiratory system, chest and mediastinal organs: shortness of breath, cough, interstitial lung disease.
Cases of interstitial lung disease have been reported transiently with telmisartan during post-marketing surveillance. However, a causal relationship has not been established.
Digestive system disorders: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting, stomach discomfort, dry mouth, dysgeusia.
Hepatobiliary system disorders: liver dysfunction/liver function disorders. Patients of Japanese nationality have been reported to be more susceptible to these adverse reactions.
Skin and subcutaneous tissue disorders: hyperhidrosis, itching, rash, erythema, angioedema (including fatal), drug-induced dermatitis, toxic dermatitis, eczema, urticaria.
Musculoskeletal and connective tissue disorders: myalgia, back pain (eg sciatica), muscle cramps, arthralgia, limb pain, tendon pain (tendinitis-like symptoms).
Disorders of the urinary system: renal dysfunction, including acute renal failure.
General disorders: chest pain, asthenia (weakness), flu-like symptoms.
Laboratory indicators: increased level of creatinine in the blood, increased level of uric acid in the blood, increased level of liver enzymes, increased level of CPK in the blood, decreased level of hemoglobin.
Description of selected adverse reactions
Sepsis. It was reported that patients receiving telmisartan had a higher incidence of sepsis compared to those receiving placebo. This could be either an accident or a sign of a process, the essence of which is still unknown.
Hypotension. This adverse reaction was noted frequently in patients with controlled blood pressure who were treated with telmisartan to reduce cardiovascular disease in addition to standard therapy.
Liver dysfunction/liver disorders. According to post-marketing data, the majority of cases of liver dysfunction/hepatic disorders were observed in patients of Japanese nationality. Patients of Japanese nationality are more susceptible to these adverse reactions.
Interstitial lung disease. Cases of interstitial lung disease have been observed transiently with telmisartan during post-marketing surveillance. However, a causal relationship has not been established.
1 An increased incidence of sepsis has been reported with telmisartan compared with placebo. This phenomenon may be a coincidental occurrence or associated with a mechanism whose operation is currently unknown.
2Reported to occur frequently in patients with controlled blood pressure treated with telmisartan to reduce cardiovascular morbidity in addition to standard therapy.
special instructions
Pregnancy. During pregnancy, treatment with angiotensin II receptor antagonists should not be started. If continuation of therapy cannot be considered essential for a patient who is planning a pregnancy, she should switch to alternative antihypertensive therapy that has an established safety profile for use during pregnancy. If pregnancy is established, treatment with angiotensin II receptor antagonists should be stopped immediately and, if necessary, alternative treatment should be started (see contraindications and use during pregnancy or lactation).
Liver failure. Telmisartan-Teva should not be used in patients with cholestasis, obstructive diseases of the biliary system and severe liver failure, since telmisartan is mainly excreted in the bile. In patients with these diseases, the hepatic clearance of telmisartan is reduced. Telmisartan-Teva should be used with caution in patients with mild to moderate hepatic impairment.
Renovascular hypertension. There is a risk of severe hypotension and renal failure in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney when treated with drugs that affect the renin-angiotensin-aldosterone system.
Kidney failure and kidney transplantation. When using the drug in patients with impaired renal function, it is recommended to periodically monitor the level of potassium and creatinine in the blood plasma. There is no experience with the use of the drug in patients after kidney transplantation.
Decreased intravascular fluid volume. Symptomatic arterial hypotension, especially after the first dose of the drug, may occur in patients with reduced blood volume or hyponatremia, which resulted from intensive diuretic therapy, a salt-restricted diet, or diarrhea and vomiting. Such conditions should be corrected before using the drug. Before starting treatment, it is necessary to normalize sodium levels and intravascular fluid volume.
Double blockade of the renin-angiotensin-aldosterone system. There is evidence that concomitant use of ACE inhibitors, angiotensin II receptor blockers or aliskiren increases the risk of hypotension, hyperkalemia and reduces renal function (including acute renal failure).
Therefore, dual blockade of the renin-angiotensin-aldosterone system when adding an ACE inhibitor to an angiotensin II receptor antagonist is not recommended. If a double block is considered absolutely necessary, it should only be done under specialist supervision and subject to continuous close monitoring of renal function, electrolytes and blood pressure.
ACE inhibitors and angiotensin II receptor blockers should not be used concomitantly in patients with diabetic nephropathy.
Other conditions accompanied by stimulation of the renin-angiotensin-aldosterone system. In patients whose vascular tone and renal function are largely dependent on the activity of the renin-angiotensin-aldosterone system (for example, patients with severe congestive heart failure or significant kidney disease, including renal artery stenosis), treatment with drugs that also affect this system , can cause acute arterial hypotension, hyperazotemia, oliguria, or less commonly, acute renal failure.
Primary aldosteronism. Typically, patients with primary aldosteronism do not respond to antihypertensive drugs that suppress the renin-angiotensin system, so prescribing telmisartan to patients with this condition is not recommended.
Stenosis of the mitral and aortic valves, obstructive hypertrophic cardiomyopathy. As with the use of other vasodilators, the drug should be prescribed with caution to patients with mitral and aortic stenosis or obstructive hypertrophic cardiomyopathy.
Hyperkalemia. The use of drugs that affect the renin-angiotensin-aldosterone system can cause hyperkalemia. In elderly patients, patients with renal failure, patients with diabetes, patients concomitantly receiving other drugs that can increase potassium levels, and/or patients with intercurrent illnesses, hyperkalemia can be fatal.
Before concomitant use of drugs that suppress the renin-angiotensin-aldosterone system, the benefit-risk ratio should be assessed.
The main risk factors for hyperkalemia to consider are:
- diabetes mellitus, renal failure, age (70 years);
- combination with one or more drugs that affect the renin-angiotensin-aldosterone system and/or with nutritional supplements containing potassium. Drugs or therapeutic classes of drugs that may precipitate hyperkalemia include potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporine or tacrolimus), and trimethoprim;
- intercurrent manifestations, in particular dehydration, acute cardiac decompensation, metabolic acidosis, impaired renal function, unexpected deterioration of the kidneys (for example, infectious diseases), cell lysis (for example, acute limb ischemia, rhabdomyolysis, severe trauma).
Careful monitoring of plasma potassium is recommended in patients at risk.
Sorbitol. The drug contains sorbitol (E420), so it should not be prescribed to patients with hereditary fructose intolerance.
Ethnic differences. Telmisartan and other angiotensin receptor blockers have been found to be less effective in lowering blood pressure in blacks than in other races, possibly because renin levels in blacks with hypertension are lower than in other races. .
Other. As with the use of other antihypertensive drugs, an excessive decrease in blood pressure in patients with coronary artery disease and ischemic cardiopathy can lead to the development of myocardial infarction or stroke.
Diabetic patients who are treated with insulin or hypoglycemic drugs. Hypoglycemia may occur in patients receiving insulin or antidiabetic drugs. In these patients, it is necessary to monitor blood glucose levels, and this should also be taken into account when adjusting the dose of insulin or antidiabetic agents.
In patients with diabetes mellitus, cardiovascular risks (patients with diabetes mellitus, concomitant coronary artery disease), the risk of fatal myocardial infarction 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 coronary artery diseases may be asymptomatic and therefore they may be undiagnosed. Patients with diabetes mellitus should be carefully evaluated, such as stress testing, to identify and treat concomitant coronary artery disease before prescribing the drug.
Use during pregnancy or breastfeeding
Pregnancy. The drug is contraindicated for use in pregnant women or women planning pregnancy. If pregnancy is confirmed during treatment with the drug, its use should be stopped immediately and, if necessary, replaced with another drug approved for use in pregnant women.
There is insufficient data on the use of telmisartan in pregnant women.
The epidemiological basis for the risk of teratogenicity resulting from the use of ACE inhibitors in the first trimester of pregnancy has not been convincing, but a slight increase in risk cannot be ruled out. Although there are no controlled epidemiological data on the risk of teratogenicity with angiotensin II receptor antagonists, similar risks may exist for this class of drugs. When planning pregnancy, you should replace the drug in advance with another antihypertensive drug with an established safety profile for use during pregnancy. If pregnancy is established, treatment with angiotensin II receptor antagonists should be discontinued immediately and alternative treatment initiated if necessary.
It is known that the use of angiotensin II receptor antagonists in the second and third trimester of pregnancy causes fetotoxicity in humans (impaired renal function, oligohydramnios, delayed formation of cranial bones) and neonatal toxicity (renal failure, hypotension, hyperkalemia). If the use of angiotensin II receptor antagonists began in the second trimester of pregnancy, it is recommended to perform an ultrasound examination of the function of the fetal kidneys and skull bones. The condition of newborns whose mothers took angiotensin II receptor antagonists should be carefully monitored for the presence of arterial hypotension.
Lactation. Since there is no information regarding the use of telmisartan during breastfeeding, its use is not recommended and alternative treatments with established safety profiles should be used during breastfeeding, especially in newborns or premature infants.
Fertility. Preclinical studies did not reveal the effect of telmisartan on the fertility of men and women.
Children. The effectiveness and safety of the drug in children under 18 years of age have not been studied.
The ability to influence reaction speed when driving vehicles or working with other mechanisms. When using antihypertensive therapy, dizziness or drowsiness may sometimes occur. Therefore, if you need to drive vehicles or work with other mechanisms, this should be taken into account.
Telmisartan (Telmesteine)
Before starting and during treatment with Telmisartan, monitoring of blood pressure, renal function, and potassium levels in the blood serum is necessary. Transient arterial hypotension is not a contraindication for further treatment with Telmisartan after stabilization of blood pressure. If severe arterial hypotension reoccurs, the dose should be reduced or the drug discontinued. In the presence of renal failure, treatment is carried out with caution under the control of serum creatinine concentration.
Liver failure
Telmisartan should not be used in patients with cholestasis, biliary obstruction or severe hepatic impairment (Child-Pugh class C) (see section "Contraindications"), since telmisartan is mainly excreted in the bile. It is assumed that in such patients the hepatic clearance of telmisartan is reduced. Telmisartan should be used with extreme caution in patients with mild or moderate hepatic impairment (Child-Pugh class A and B).
Renovascular hypertension
When treated with drugs acting on the RAAS, the risk of severe arterial hypotension and renal failure increases in patients with bilateral renal artery stenosis and stenosis of the artery of a solitary kidney.
Kidney failure and kidney transplantation
When using Telmisartan in patients with impaired renal function, periodic monitoring of potassium levels and creatinine concentrations in the blood serum is recommended. There is no clinical experience with the use of Telmisartan in patients who have recently undergone kidney transplantation.
Decrease in circulating blood volume (CBV)
In patients with a decrease in blood volume and/or sodium content due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting, symptomatic arterial hypotension may occur, especially after the first dose of Telmisartan. Fluid and/or sodium deficiency must be corrected before starting Telmisartan.
Dual blockade of the renin-angiotensin-aldosterone system (RAAS)
The following consequences of RAAS inhibition have been noted: the occurrence of arterial hypotension, fainting, hyperkalemia and impaired renal function (including acute renal failure) in predisposed patients, especially when used in combination with drugs that also act on this system. Dual blockade of the RAAS, for example by adding an ACE inhibitor to an ARA II, is not recommended for patients with already controlled blood pressure and should be limited to selected cases with enhanced monitoring of renal function (including periodic monitoring of potassium levels and plasma creatinine concentrations).
Other diseases characterized by activation of the RAAS
In patients whose vascular tone and renal function depend primarily on the activity of the RAAS (for example, patients with chronic heart failure or kidney disease, including renal artery stenosis), the use of drugs acting on this system, such as telmisartan, has been associated with the occurrence of acute arterial hypotension, hyperazotemia, oliguria, or rarely - acute renal failure (see section "Side effects").
Primary hyperaldosteronism
Patients with primary hyperaldosteronism generally do not respond to treatment with antihypertensive drugs that act by inhibiting the RAAS. In this regard, the use of Telmisartan in these cases is not recommended.
Aortic and mitral valve stenosis
,
hypertrophic obstructive cardiomyopathy (HOCM)
As with other vasodilators, for patients with aortic and mitral stenosis or HOCM
special precautions are indicated.
Hyperkalemia
The use of drugs acting on the RAAS can cause hyperkalemia.
For elderly patients, patients with renal failure, patients with diabetes mellitus and also with arterial hypertension and coronary artery disease (CHD), patients receiving concomitant therapy with drugs that may cause an increase in potassium levels, and/or patients with concomitant disease, hyperkalemia can be fatal. Before considering the possibility of concomitant use of drugs acting on the RAAS, it is necessary to assess the benefit-risk ratio.
The main risk factors to consider are:
— Diabetes mellitus, renal failure, age (patients over 70 years old).
- Combination with one or more drugs acting on the RAAS and/or increasing serum potassium levels. Drugs or therapeutic classes of drugs that may cause hyperkalemia include potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, ARB II, NSAIDs including selective COX-2 inhibitors, heparin, immunosuppressants (cyclosporine or tacrolimus) and trimethoprim .
- Intercurrent diseases, especially dehydration, acute heart failure, metabolic acidosis, impaired renal function, acute deterioration of kidney condition (for example, infectious diseases), cytolysis syndrome (for example, acute limb ischemia, rhabdomyolysis, severe trauma).
For patients at risk, regular monitoring of serum potassium levels is recommended (see section “Interaction with other drugs”).
In patients with diabetes mellitus and additional cardiovascular risk, for example, in patients with diabetes mellitus and coronary artery disease, the risk of fatal myocardial infarction and sudden cardiovascular death may be increased when taking antihypertensive agents such as ARBAs or ACE inhibitors.
In patients with diabetes mellitus, CAD may be asymptomatic and therefore may not be diagnosed. In patients with diabetes mellitus, before starting the use of Telmisartan, appropriate diagnostic studies, including exercise testing, should be carried out to identify and treat coronary artery disease.
Alternatively, Telmisartan can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which have an additional antihypertensive effect.
Racial differences
As noted for ACE inhibitors, telmisartan and other ARBs appear to be less effective in lowering blood pressure in blacks than in other races, possibly due to a greater predisposition to decreased renin activity in the black diabetic population. and also with arterial hypertension and coronary artery disease.
Other
As with other antihypertensive drugs, an excessive decrease in blood pressure in patients with ischemic cardiomyopathy or coronary artery disease can lead to the development of myocardial infarction or stroke.
Interactions
Digoxin. with simultaneous use of telmisartan and digoxin, an average increase in digoxin Cmax in blood plasma (by 49%) and minimum concentrations (by 20%) was noted. At the beginning of treatment, in case of dose adjustment and discontinuation of telmisartan, digoxin levels should be monitored to maintain them within the therapeutic range.
Like other drugs that affect the renin-angiotensin-aldosterone system, telmisartan can cause hyperkalemia. This risk may increase when combined with other drugs that may also cause hyperkalemia (potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporine or tacrolimus) and trimethoprim).
The incidence of hyperkalemia depends on associated risk factors. The risk increases with the use of the therapeutic combinations mentioned above. This risk is especially high when combined with potassium-sparing diuretics and salt substitutes containing potassium. Combination, for example, with ACE inhibitors or NSAIDs creates a lower risk if strict caution is observed during use.
Concomitant use is not recommended
With potassium-sparing diuretics or nutritional supplements containing potassium. Angiotensin II receptor antagonists, such as telmisartan, reduce potassium loss caused by diuretics. Potassium-sparing diuretics such as spironolactone, eplerenone, triamterene or amiloride, potassium-containing dietary supplements, or potassium-containing salt substitutes may lead to significant increases in plasma potassium levels. If concomitant use is indicated due to diagnosed hypokalemia, these drugs should be used with caution with frequent monitoring of plasma potassium.
With lithium. With simultaneous use of lithium with ACE inhibitors and angiotensin II receptor antagonists, including telmisartan, a reversible increase in plasma lithium concentration and toxicity was observed. If the use of such a combination is necessary, careful monitoring of lithium plasma levels is recommended.
Concomitant use requiring caution
NSAIDs. NSAIDs (eg acetylsalicylic acid in doses intended for the treatment of inflammatory processes, COX-2 inhibitors and non-selective NSAIDs) may reduce the antihypertensive effect of angiotensin II receptor antagonists.
In some patients with impaired renal function (eg, dehydrated patients or elderly patients with impaired renal function), concomitant use of angiotensin II receptor antagonists and COX depressants may lead to a further deterioration of renal function, including possible acute renal failure, which is usually reversible. Therefore, this combination should be used with caution, especially in elderly patients. Patients should receive adequate fluids and should consider monitoring renal function after initiating concomitant treatment and periodically thereafter.
An almost 2.5-fold increase in AUC0-24 and Cmax was reported when used simultaneously with ramipril and ramiprilat. The clinical significance of this report is unknown.
Diuretics (thiazide or loop). Pre-treatment with high doses of diuretics such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic) may lead to dehydration and the risk of hypotension when starting treatment with telmisartan.
Should be taken into account when used simultaneously
Other antihypertensive drugs. The effect of telmisartan - lowering blood pressure - may be enhanced when used simultaneously with other antihypertensive drugs.
Given the pharmacological properties, it can be expected that drugs such as baclofen, amifostine can cause the hypotensive effects of all antihypertensive drugs, including telmisartan. Orthostatic hypotension may also be worsened by alcohol use, barbiturates, narcotics, or antidepressants.
GCS (systemic use). Decreased antihypertensive effect.
Double blockade of the renin-angiotensin-aldosterone system. It has been demonstrated that double blockade of the renin-angiotensin-aldosterone system with simultaneous use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren is characterized by a higher incidence of adverse reactions such as arterial hypotension, hyperglycemia, decreased renal function (including acute renal failure), compared with using monotherapy.
Telmisartan-Teva tablet 80 mg No. 28
TELMISARTAN-TEVA TELMISARTANUM C09C A07
Teva
COMPOSITION AND FORM OF RELEASE:
table 80 mg blister, No. 28
Telmisartan
| 80 mg |
PHARMACOLOGICAL PROPERTIES:
pharmacodynamics. Telmisartan is an oral specific angiotensin II receptor antagonist (AT1 type). With high affinity, telmisartan replaces angiotensin II at the sites of its binding to a type of AT1 receptor, through which the action of angiotensin II is mediated. Telmisartan selectively binds to the AT1 receptor for a long time, without even a partial agonistic effect on it. Telmisartan has no affinity for other receptors, including AT2 receptors and other AT receptors. The functional role of these receptors is not clear, as is the effect of their possible stimulation by angiotensin II, the levels of which are increased by telmisartan. Telmisartan reduces plasma aldosterone levels, does not block ion channels and does not reduce plasma renin levels. It does not inhibit ACE (kininase II), an enzyme that also breaks down bradykinin. Therefore, bradykinin-mediated side effects are not expected. In humans, telmisartan at a dose of 80 mg almost completely inhibits the increase in blood pressure caused by angiotensin II. The inhibitory effect lasts more than 1 day and is determined up to 48 hours. After the first use, the hypotensive effect of the drug appears gradually over 3 hours. The maximum reduction in blood pressure is usually achieved 4–8 weeks after the start of treatment with telmisartan and persists with long-term therapy. The antihypertensive effect is continuously maintained for 24 hours after taking 1 dose, including the last 4 hours before the next dose. A dose-dependent effect was noted on systolic blood pressure, but data on diastolic blood pressure are contradictory. In patients with hypertension, telmisartan reduces both systolic and diastolic blood pressure without affecting pulse rate. Pharmacokinetics. Telmisartan is rapidly absorbed, but the amount of drug that is absorbed is not the same. The average bioavailability of telmisartan is approximately 50%. When telmisartan is administered with food, the AUC for telmisartan decreases from approximately 6% (40 mg dose) to approximately 19% (160 mg dose). 3 hours after administration, the concentration in the blood plasma becomes the same as when using telmisartan without food. It is believed that a slight decrease in AUC does not reduce the therapeutic effectiveness of the drug. Telmisartan is highly bound to plasma proteins (>99.5%), mainly to albumin and α1-acid glycoprotein. The mean volume of distribution (Vss) at equilibrium is approximately 500 L. Telmisartan is metabolized by conjugation to a glucuronide, which has no pharmacological activity. Telmisartan is characterized by a biexponential pharmacokinetic curve with a terminal T½ >20 hours. Cmax in blood plasma and, to a lesser extent, AUC increases disproportionately to the dose. When using telmisartan in recommended doses, no clinically significant accumulation was detected. After oral administration and intravenous administration, telmisartan is almost completely excreted in the feces, mainly unchanged. Cumulative urinary excretion is less than 1% of the administered dose. Total plasma clearance (CLtot) is high (≈1000 ml/min) compared with hepatic blood flow (≈1500 ml/min).
INDICATIONS:
treatment of essential hypertension. Prevention of cardiovascular diseases in patients with: severe manifestations of atherothrombotic cardiovascular disease (coronary heart disease, stroke or history of peripheral arterial disease); diabetes mellitus type II with complications (diagnosed target organ damage).
APPLICATION:
Telmisartan-Teva should be taken orally, regardless of meals. Treatment of essential hypertension The recommended dose is 40 mg/day. For some patients, a dose of 20 mg/day will be sufficient. If the blood pressure level does not decrease to the desired values, then the dose can be increased to a maximum of 80 mg 1 time per day. Telmisartan-Teva can be prescribed in combination with thiazide diuretics, such as hydrochlorothiazide, which have an additional effect on lowering blood pressure when used in combination with telmisartan. When deciding whether to increase the dose, it should be borne in mind that the maximum hypotensive effect occurs 4–8 weeks from the start of treatment. Prevention of cardiovascular diseases The recommended dose is 80 mg 1 time per day. It is unknown whether a dose of telmisartan <80 mg is effective in reducing cardiovascular morbidity. At the beginning of treatment with telmisartan, in order to reduce the risk of cardiovascular diseases, careful monitoring of blood pressure is recommended. It may be necessary to appropriately adjust the regimen of drugs that lower blood pressure. Kidney failure. In patients with mild or moderate renal failure, there is no need for dose adjustment. There is limited experience with use in patients with severe renal impairment or on hemodialysis. For these patients, a low initial dose of 20 mg is recommended. Liver failure. For patients with mild to moderate liver failure, the dose should not exceed 40 mg/day. The drug is contraindicated in patients with severe liver failure. Elderly patients. No dose adjustment is required.
CONTRAINDICATIONS:
hypersensitivity to the active substance or any of the excipients of the drug. Period of pregnancy or planning pregnancy (see Use during pregnancy and lactation). Obstructive diseases of the bile ducts. Severe liver failure. Concomitant use of aliskiren-containing drugs in patients with diabetes mellitus or impaired renal function (glomerular filtration rate <60 ml/min/1.73 m2).
SIDE EFFECTS:
infectious diseases and infestations: infectious diseases of the upper respiratory tract (including pharyngitis and sinusitis), infectious diseases of the urinary tract (including cystitis), sepsis, including deaths1. From the blood and lymphatic system: anemia, thrombocytopenia, eosinophilia. From the immune system: hypersensitivity, anaphylactic reactions. Metabolism disorders: hyperkalemia, hypoglycemia (in patients with diabetes mellitus). Mental disorders: depression, insomnia, anxiety. Neurological disorders: syncope, drowsiness. From the organ of vision: visual impairment. From the organ of hearing and vestibular apparatus: vertigo. From the cardiovascular system: bradycardia, tachycardia, arterial hypotension2, orthostatic hypotension. From the respiratory system, thoracic cavity and mediastinum: shortness of breath, cough, interstitial lung disease. From the digestive tract: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting, indigestion, dry mouth. From the hepatobiliary system: abnormal liver function indicators/liver dysfunction. Patients of Japanese nationality have been reported to be more susceptible to these adverse reactions. From the skin and subcutaneous tissue: hyperhidrosis, itching, rash, erythema, angioedema (including fatal), drug dermatitis, toxic dermatitis, eczema, urticaria. From the musculoskeletal system and connective tissue: myalgia, back pain (eg sciatica), muscle cramps, arthralgia, pain in the limbs, pain in the tendons (tendonitis-like symptoms). From the urinary system: impaired renal function, including acute renal failure. General disorders: chest pain, asthenia (weakness), flu-like symptoms. Laboratory indicators: increased level of creatinine in the blood, increased level of uric acid in the blood, increased level of liver enzymes, increased level of CPK in the blood, decreased level of hemoglobin. 1 An increased incidence of sepsis has been reported with telmisartan compared with placebo. This phenomenon may be a coincidental occurrence or associated with a mechanism whose operation is currently unknown. 2Reported to be common in patients with controlled blood pressure treated with telmisartan to reduce cardiovascular morbidity in addition to standard therapy.
SPECIAL INSTRUCTIONS:
pregnancy During pregnancy, treatment with angiotensin II receptor antagonists should not be started. If continued therapy cannot be considered essential for a patient planning a pregnancy, she should switch to alternative antihypertensive therapy that has an established safety profile for use during pregnancy. If pregnancy is established, treatment with angiotensin II receptor antagonists should be immediately discontinued and, if necessary, alternative treatment should be initiated (see CONTRAINDICATIONS and Use during pregnancy and lactation). Liver failure Telmisartan-Teva should not be used in patients with cholestasis, obstructive diseases of the biliary system and severe liver failure, since telmisartan is mainly excreted in the bile. In patients with these diseases, the hepatic clearance of telmisartan is reduced. Telmisartan-Teva should be used with caution in patients with mild to moderate hepatic impairment. Renovascular hypertension There is a risk of severe hypotension and renal failure in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney when treated with drugs that affect the renin-angiotensin-aldosterone system (RAAS). Renal failure and kidney transplantation When using the drug in patients with impaired renal function, it is recommended to periodically monitor the level of potassium and creatinine in the blood plasma. There is no experience with the use of the drug in patients after kidney transplantation. Decreased blood volume Symptomatic arterial hypotension, especially after the 1st dose of the drug, may occur in patients with reduced blood volume or hyponatremia, which developed as a result of intensive diuretic therapy, a diet with limited salt intake, or diarrhea and vomiting. Such conditions should be corrected before using the drug. Before starting treatment, it is necessary to normalize sodium levels and intravascular fluid volume. Dual blockade of the RAAS: due to blockade of the RAAS, in particular when combining drugs that affect this system, symptoms of arterial hypotension, syncope, hyperkalemia and changes in renal function (including acute renal failure) have been observed in patients with a corresponding predisposition. Therefore, dual blockade of the RAAS (for example, when adding an ACE inhibitor to an angiotensin II receptor antagonist) is not recommended in patients with controlled blood pressure and should be limited to selected cases, subject to careful monitoring of renal function. Other conditions accompanied by stimulation of the RAAS In patients whose vascular tone and renal function are largely dependent on the activity of the RAAS (for example, with severe congestive heart failure or renal pathology, including renal artery stenosis), treatment with drugs that also affect this system may cause acute arterial hypotension, hyperazotemia, oliguria, or less commonly, acute renal failure. Dual blockade of the RAAS It has been reported that the simultaneous use of ACE inhibitors, angiotensin II receptor blockers or aliskiren increases the risk of arterial hypotension, hyperglycemia, and renal dysfunction (including acute renal failure). Thus, double blockade of the RAAS by combined use of ACE inhibitors, angiotensin II receptor blockers or aliskiren is not recommended. If dual blockade therapy is necessary, it should be carried out under specialist supervision and renal function, electrolyte levels and blood pressure should be regularly monitored. Patients with diabetic nephropathy are not recommended to use ACE inhibitors and angiotensin II receptor blockers simultaneously. Primary hyperaldosteronism Typically, patients with primary aldosteronism do not respond to antihypertensive drugs that suppress the RAAS, so prescribing telmisartan to patients with this condition is not recommended. Mitral and aortic valve stenosis, obstructive hypertrophic cardiomyopathy As with the use of other vasodilators, the drug should be prescribed with caution to patients with mitral and aortic stenosis or obstructive hypertrophic cardiomyopathy. Hyperkalemia The use of drugs that affect the RAAS can lead to hyperkalemia. In elderly patients, patients with renal insufficiency, patients with diabetes mellitus, patients concomitantly receiving other drugs that may increase potassium levels, and/or patients with intercurrent illnesses, hyperkalemia may be fatal. Before simultaneous use of drugs that affect the RAAS, the benefit-risk ratio should be assessed. The main risk factors for hyperkalemia that should be taken into account are: diabetes mellitus, kidney damage, age (>70 years); combination with one or more drugs that affect the RAAS and/or with nutritional supplements containing potassium. Drugs or therapeutic classes of drugs that may precipitate hyperkalemia include potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs including selective COX-2 inhibitors, heparin, immunosuppressants (cyclosporine or tacrolimus), and trimethoprim; intercurrent manifestations, in particular dehydration, acute cardiac decompensation, metabolic acidosis, impaired renal function, unexpected deterioration of the kidneys (infectious diseases), cell lysis (for example, acute limb ischemia, rhabdomyolysis, severe trauma). Careful monitoring of plasma potassium is recommended in patients at risk. Sorbitol The drug contains sorbitol, so it should not be prescribed to patients with hereditary fructose intolerance. Ethnic differences As found with ACE inhibitors, telmisartan and other angiotensin receptor blockers are less effective in lowering blood pressure in blacks than in other races, possibly because renin levels are lower in blacks with hypertension than in other races. race Others As with the use of other antihypertensive drugs, an excessive decrease in blood pressure in patients with coronary artery disease and ischemic cardiopathy can lead to the development of myocardial infarction or stroke. Patients with diabetes Hypoglycemia may occur in patients receiving insulin or antidiabetic drugs. In these patients, it is necessary to monitor blood glucose levels, and this should also be taken into account when adjusting the dose of insulin or antidiabetic agents. In patients with diabetes mellitus at cardiovascular risk (patients with diabetes mellitus with underlying coronary artery disease), the risk of fatal myocardial infarction 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 coronary artery diseases may be asymptomatic and therefore they may be undiagnosed. Patients with diabetes mellitus should be carefully evaluated, such as stress testing, in order to identify and treat concomitant coronary artery disease before prescribing the drug. Use during pregnancy and lactation. Pregnancy. The drug should not be used in pregnant women or women who are planning pregnancy. If pregnancy is confirmed during drug therapy, its use should be stopped immediately and, if necessary, replaced with another drug approved for use in pregnant women. Lactation. Since there is no information regarding the use of telmisartan during breastfeeding, its use is not recommended. Alternative treatments with an established safety profile should be used during breastfeeding, especially when feeding newborns or premature infants. Preclinical studies did not reveal the effect of telmisartan on the fertility of men and women. Children. The effectiveness and safety of the drug in children have not been established, therefore it is not recommended to use the drug in this category of patients. The ability to influence reaction speed when driving vehicles or working with other mechanisms. No studies have been conducted to establish the effect of telmisartan on the ability to drive vehicles and operate machinery. However, it should be noted that when using antihypertensive therapy, dizziness or drowsiness may sometimes occur. Therefore, if it is necessary to drive vehicles or other machinery, you should be careful and refrain from these actions until your individual reaction to the drug is established.
INTERACTIONS:
interaction studies were performed in adults only. Like other drugs that affect the RAAS, telmisartan can cause hyperkalemia. This risk may increase when combined with other drugs that may also cause hyperkalemia (potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporine or tacrolimus) and trimethoprim. The incidence of hyperkalemia depends on the associated risk factors. The risk is increased with the use of the therapeutic combinations mentioned above. This risk is especially high when combined with potassium-sparing diuretics and potassium-containing salt substitutes. Combinations, for example, with ACE inhibitors or NSAIDs pose a lower risk in severe use with caution. Concomitant use is not recommended With potassium-sparing diuretics or dietary supplements containing potassium Angiotensin II receptor antagonists, such as telmisartan, reduce potassium loss caused by diuretics. Potassium-sparing diuretics, such as spironolactone, eplerenone, triamterene or amiloride, dietary supplements containing potassium or potassium-containing salt substitutes may lead to a significant increase in plasma potassium levels. If concomitant use is indicated due to diagnosed hypokalemia, these drugs should be used with caution with frequent monitoring of plasma potassium levels. With lithium When lithium was used simultaneously with ACE inhibitors and angiotensin II receptor antagonists, including telmisartan, a reversible increase in plasma lithium concentrations and toxicity was observed. If the use of such a combination is necessary, careful monitoring of lithium plasma levels is recommended. Concomitant use, which requires caution, NSAIDs NSAIDs (for example, acetylsalicylic acid in a dose intended for the treatment of inflammatory processes, COX-2 inhibitors and non-selective NSAIDs) may reduce the antihypertensive effect of angiotensin II receptor antagonists. In some patients with impaired renal function (eg, dehydrated patients or the elderly with impaired renal function), concomitant use of angiotensin II receptor antagonists and COX depressants may lead to a further deterioration of renal function, including possible acute renal failure, which is usually reversible. Therefore, this combination should be used with caution, especially in elderly patients. Patients need to receive adequate fluids. The ability to monitor renal function should be assessed after initiation of concomitant treatment and periodically after its completion. An almost 2.5-fold increase in AUC0-24 and Cmax was reported when administered concomitantly with ramipril and ramiprilat. The clinical significance of this report is unknown. Diuretics (thiazide or loop) Pre-treatment with high doses of diuretics such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic) may lead to dehydration and the risk of hypotension when starting treatment with telmisartan. It should be taken into account when used simultaneously with other antihypertensive drugs. The effect of telmisartan - lowering blood pressure - may increase when used simultaneously with other antihypertensive drugs. Given the pharmacological properties, it can be expected that drugs such as baclofen, amifostine can cause the hypotensive effects of all antihypertensive drugs, including telmisartan. Alcohol, barbiturates, narcotics, or antidepressants can also increase the severity of orthostatic hypotension. GCS (systemic use) Reduced antihypertensive effect. Double blockade of the RAAS It has been demonstrated that double blockade of the RAAS with simultaneous use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren is characterized by a high incidence of adverse reactions, such as arterial hypotension, hyperglycemia, impaired renal function (including acute renal failure) compared with the use of monotherapy.
OVERDOSE:
Information on overdose of telmisartan is limited. The most pronounced symptoms of telmisartan overdose were arterial hypotension and tachycardia, and bradycardia, syncope, increased plasma creatinine levels and acute renal failure were also reported. Telmisartan is not excreted from the body by hemodialysis. The patient should be closely monitored and receive symptomatic and supportive therapy. Treatment depends on the length of time since the overdose and the severity of symptoms. It is recommended to induce vomiting and/or lavage the stomach. Activated carbon can be used to treat an overdose. Plasma levels of electrolytes and creatinine should be monitored frequently. If arterial hypotension occurs, the patient should be placed in a supine position and the balance of fluid and electrolytes in the body should be restored.
STORAGE CONDITIONS:
no special storage conditions required.
Overdose
Information on overdose of telmisartan is limited.
The most pronounced symptoms of telmisartan overdose were arterial hypotension and tachycardia; Bradycardia, dizziness, increased plasma creatinine and acute renal failure have also been reported.
Telmisartan is not excreted from the body by hemodialysis. The patient should be closely monitored and receive symptomatic and supportive therapy. Treatment depends on the length of time since the overdose and the severity of symptoms. It is recommended to induce vomiting and/or lavage the stomach. Activated carbon can be used to treat an overdose. Plasma electrolyte and creatinine levels should be monitored frequently. If arterial hypotension occurs, the patient should be placed in a supine position and the balance of fluid and salt in the body should be restored.
Note!
Description of the drug Telmisartan-Teva table. 80mg No. 28 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
