active ingredient: telmisartan;
1 tablet contains telmisartan 40 mg or 80 mg
Auxiliary substances: meglumin, sodium hydroxide, povidone, Polysorbate 80, manit (E 421), magnesium stearate.
Basic physico-chemical properties:
tablets from white to almost white, without sheath, capsule-like, with prints "T" and "L" on both sides of the fault line on one side and the impression "40" (for tablets of 40 mg) or reflection " 80 " (for tablets of 80 mg) on the other side.
Antagonists, plain angiotensin II.
ATC code C09C A07.
Telmisartan is a specific receptor antagonist angiotenzina II (type AO 1 ), valid when administered orally. Having a high affinity of telmisartan displaces angiotensin II in place of its connection with the receptor subtype 1 AO responsible for the action of angiotensin II. Telmisartan not show any partial activity of JSC 1 receptor as an agonist. Telmisartan selectively binds receptor of AO 1 for a long period. The drug does not demonstrate affinity for other receptors, including AO 2, and other less characterized at receptors. The functional role of these receptors is unknown, as well as the effect of their possible excessive stimulation with angiotensin II, the level of which increases telmisartan. Telmisartan reduces the level of aldosterone in the blood plasma. Telmisartan aren't inhibited by renin of human plasma and does not block ion channels. Telmisartan does not inhibit ACE (kinase II), which also breaks down bradykinin. Thus, we should not expect an increase in adverse reactions associated with bradykinin.
In humans, telmisartan dose of 80 mg almost completely suppresses the effect of angiotensin II to increase blood pressure. The depressing effect lasts for more than 24 hours and is still observed up to 48 hours.
Clinical efficacy and safety
Treatment of essential hypertension
After the first dose telmisartan antihypertensive effect gradually begins to emerge for 3:00. The maximum decrease in blood pressure is usually achieved 4-8 weeks after the start of therapy and remains for long-term therapy.
The antihypertensive effect remains constant for more than a day after dose, including the last 4:00 before the next dose, as shown in the outpatient blood pressure measurement. This has been confirmed by the ratio of residual activity to the peak, which is over 80% after the application of doses of 40 and 80 mg telmisartan in placebo-controlled clinical trials. There is a clear link between dose and recovery time of the initial systolic blood pressure (SBP). Data concerning diastolic blood pressure (DBP) are inconsistent.
In patients with hypertension telmisartan reduces both systolic blood pressure and diastolic, while it does not affect the pulse rate. The contribution of diuretic and natriuretic action of the drug to its antihypertensive activity has not yet been determined. Efficiency telmisartan in lowering blood pressure is comparable with other agents representing other classes of antihypertensive drugs (clinical studies for comparison telmisartan with amlodipine, atenolol, enalapril, hydrochlorothiazide and lisinopril).
The sudden cessation of treatment with telmisartan, blood pressure gradually returns to the level before treatment within a few days with no signs of return of hypertension.
In clinical studies with direct comparison of two antihypertensive drugs cases of dry cough much less frequently observed when using telmisartan than when using ACE inhibitors.
Telmisartan rapidly absorbed, although the amount absorbed varies. The average value of the absolute bioavailability telmisartan is approximately 50%. When using telmizartan with food reduces the area under the curve "concentration-time" (AUC 0-EN) in the range of 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). After 3:00 after the application telmisartan concentration in blood plasma and in the fasting, and when taken with food is the same.
A slight reduction in AUC is expected to reduce the therapeutic effect. There is no linear relationship between doses and drug concentration in plasma. C max and to a lesser extent AUC increase disproportionately at a dose of 40 mg.
Telmisartan largely bound to plasma proteins (>99,5%), mainly albumin and alpha-1 acid glycoprotein. The average volume of distribution (V dss ) in equilibrium is about 500 liters.
Telmisartan metabolized by conjugation of the parent compound to the glucuronide conjugate does not have pharmacological activity.
Telmisartan bieksponencialno is characterized by a curve with a terminal half-life of over 20 hours. The maximum concentration in plasma (C max) and to a lesser extent the area under the concentration-time curve (AUC) increase disproportionately dose. There is no evidence of clinically significant accumulation telmisartan when using the recommended dose. In women, the concentration in blood plasma was higher than in men with no significant effect on efficiency.
After intake of telmisartan almost completely excreted in the feces, mostly unchanged. The total excretion of the drug in the urine is<1% dose. Total blood plasma clearance (CL tot ) is high (approximately 1000 ml/min) compared to blood flow through the liver (approximately 1500 ml/min).
Special groups of patients
the effect of sex
The comparison of female and male patients revealed differences in blood plasma concentrations C max and AUC, which is higher 3 and 2 times respectively in women.
Pharmacokinetics telmisartan has no differences among elderly patients and patients under the age of 65 years.
Patients with impaired renal function
Patients with slight, moderate and severe impaired renal function was observed a doubling of the concentration in the blood plasma. However, low plasma concentrations were observed in patients with renal insufficiency on dialysis. In patients with renal insufficiency, telmisartan is largely associated with plasma proteins, so it can not be excreted by dialysis. The half-life period does not change in patients with impaired renal function.
Patients with impaired liver function
Pharmacokinetic studies of patients with impaired liver function showed an increase in bioavailability of almost 100%. The half-life period does not change in patients with impaired liver function.
Treatment of essential hypertension in adults.
Prevention of cardiovascular diseases.
Reduced incidence of cardiovascular disease in patients with:
Pronounced manifestations of atherothrombotic cardiovascular disease (ischemic heart disease, stroke or peripheral artery disease in anamnesis);
diabetes mellitus type II with diagnosed defeat organs-targets.
Hypersensitivity to the active substance or to any auxiliary substance of the drug.
Pregnant women or women planning to become pregnant (see the sections "Peculiarities of use", "application during pregnancy or breastfeeding"). Obstructive diseases of the bile ducts.
Severe impairment of liver function.
Children's age (up to 18 years).
Contraindicated simultaneous application telmisartan and alisherovich products patients with diabetes mellitus or renal impairment (GFR<60 ml/min/1.73 m2 ) (see "Interaction with other medicinal products and other forms of interaction" and "Pharmacological properties") .
Interaction with other medicinal products and other forms of interaction
While the use of digoxin telmisartan and noted the average growth of peak concentrations of digoxin in plasma (49%) and minimum concentration (20%). In the beginning of the reception, in case of dose adjustment and discontinuation of telmisartan shall monitor the level of digoxin to maintain them within the therapeutic range.
As with other drugs that inhibit the renin-angiotensin-aldosterone system, telmisartan may provoke hyperkalemia (see Section "Peculiarities of use"). The risk may increase if treated in combination with other agents that may also trigger hyperkalemia (salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, nonsteroidal anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporin or tacrolimus), and trimethoprim).
Cases of hyperkalemia depend on the associated risk factors. The risk increases with the above therapeutic combinations. Particularly high risk in combination with potassium-sparing diuretics and in combination with salt substitutes containing potassium. The combination with ACE inhibitors or NSAIDs, for example, less risky, subject to strict caution in the application.
Not recommended for simultaneous use
Potassium-sparing diuretics or potassium supplements.
Angiotensin II receptor antagonists, such as telmisartan, reduce the loss of potassium caused by diuretics. Potassium-sparing diuretics such as spironolactone, eplerenone, triamterene or amiloride, food additives containing potassium or potassium-containing salt substitutes may lead to significant increase in the concentration of potassium in the blood serum. If simultaneous use has been demonstrated through a documented hypokalemia, patients should use these drugs with caution and with frequent monitoring of potassium level in the blood serum.
Lithium. During the concomitant application of lithium with ACE inhibitors and angiotensin II receptor antagonists, including telmisartan, there was a reversible increase in the concentration of lithium in serum and toxicity. If the use of this combination is necessary, it is recommended to carefully monitor the level of lithium in the blood serum.
Simultaneous use requires caution.
Nonsteroidal anti-inflammatory drugs.
NSAIDs (e.g. acetylsalicylic acid at anti-inflammatory doses, COX-2 inhibitors and non-selective NSAIDs) may reduce the antihypertensive effect of angiotensin II receptor antagonists.
In some patients with impaired renal function (for example, in patients with dehydration or elderly patients with impaired renal function), the simultaneous use of angiotensin II receptor antagonists and means, inhibiting COX, can lead to further deterioration of renal function, including possible acute renal failure, which is usually reversible. Thus, this combination should be used with caution, especially in elderly patients. Patients should be adequately hydrated. Kidney function should be monitored after the start of concomitant therapy and periodically later.
In one study, the simultaneous use of telmisartan and ramipril led to an increase of 2.5 times the AUC 0 - 24 and C max of ramipril and ramiprilat. The clinical significance of this observation is unknown.
Diuretics (thiazides or loop diuretics). Pretreatment with high doses of diuretics such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic) can lead to lower fluid levels (dehydration) and risk of hypotension at the beginning of treatment with telmisartan.
Should be taken into account in simultaneous use.
Other antihypertensive agents. Telmisartan the ability to lower blood pressure may be increased by concurrent use of other antihypertensive drugs.
Clinical data has shown that dual blockade of the renin-angiotensin(RAAS) through the combined use of ACE inhibitors, blockers of receptors of angiotensin II or aliskiren is associated with a higher frequency of such side effects as hypotension, hyperkalemia and deterioration of renal function ( including acute renal failure) compared with use of a single RAAS-acting agent (see "peculiarities of use", "Contraindications" and "Pharmacological").
Given the pharmacological properties of baclofen, and amifostine can be expected that these drugs may enhance the hypotensive effect of all antihypertensive drugs, including telmisartan. In addition, orthostatic hypotension may worsen due to the use of alcohol, barbiturates, drugs and antidepressants.
Corticosteroids (systemic application)
Reduction of antihypertensive effect.
Pregnancy. During pregnancy you can not start treatment with antagonists of angiotensin II receptors. If the continuation of therapy with angiotensin II receptor antagonists cannot be considered essential for a patient who is planning a pregnancy, she should switch to alternative antihypertensive therapy, has a safety profile for use during pregnancy. When determining pregnancy, treatment with angiotensin II receptor antagonists should be stopped immediately and alternative treatment should be initiated (see para. The sections "Contraindications" and "Use during pregnancy or breastfeeding").
Impaired liver function
Telmisartan should not be administered to patients with cholestasis, obstructive disorders of the gallbladder, or severe hepatic impairment since telmisartan is mostly excreted in the bile. These patients can expect a decrease in hepatic clearance telmisartan. Telmisartan can be applied only with caution to patients with mild and moderate hepatic impairment.
There is an increased risk of severe hypotension and renal insufficiency when patients with bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney use of medicines affecting the renin-angiotensin-aldosterone system.
Renal impairment and kidney transplantation
It is recommended to conduct a periodic monitoring of potassium and creatinine serum when applying telmisartan in patients with impaired renal function. No experience purpose telmisartan patients following recent kidney transplantation.
Symptomatic hypotension, especially after the first dose telmisartan may occur in patients with reduced fluid volume and/or sodium, which emerged after intensive diuretic therapy, limiting salt in the diet, diarrhoea or vomiting. Such States should be removed before applying telmisartan. Before applying telmisartan to normalize the volume of the intravascular fluid and/or sodium levels.
Dual blockade of the renin-angiotensin(RAAS)
As a consequence of inhibiting the renin-angiotensin-sensitive individuals, especially if combining medicinal products that affect this system, was observed the occurrence of hypotension, syncope, hyperkalemia, and changes in kidney function (including acute renal failure). Double blockade of renin-angiotensin-(for example, when adding ACE inhibitors to angiotensin II receptor antagonists) is not recommended for patients who already have blood pressure monitored, it should be limited to separately defined cases with careful monitoring of kidney function (see para. Sections " Interaction with other drugs and other types of interactions "and" Pharmacological ").
If a double blockade is considered absolutely necessary, it should be carried out only under the supervision of a specialist and under the condition of constant careful monitoring of kidney function, electrolytes and blood pressure.
ACE inhibitors and blockers of angiotensin II receptors should not be used in patients with diabetic nephropathy.
Other conditions with stimulation the renin-angiotensin-
Patients vascular tone and renal function which is predominantly dependent on the activity of the renin-angiotensin(e.g., patients with severe congestive heart failure or kidney disease, including renal artery stenosis), treatment with medicinal products that affect this system such as telmisartan has been associated with the occurrence of acute hypotension, giperazotemii, oliguria or acute renal failure, which happened only rarely (see "Adverse reactions").
Patients with primary aldosteronism generally will not respond to antihypertensive drugs that inhibit the renin-angiotensin system. Thus, the use of telmisartan is not recommended.
Stenosis of the aortic or mitral valve, obstructive hypertrophic cardiomyopathy
As the use of other vasodilators should be used with caution in patients with stenosis of the aortic or mitral valves or obstructive hypertrophic cardiomyopathy.
Diabetic patients who are treated with insulin or hypoglycemic drugs.
During treatment with telmisartan, such patients may develop hypoglycemia. In such patients, blood glucose should be monitored, and this should be taken into account when correcting the dose of insulin or antidiabetic drugs.
In patients with diabetes mellitus, cardiovascular risks (patients with diabetes mellitus, with concomitant coronary artery disease), the risk of developing a myocardial infarction with fatal outcome and sudden cardiovascular death may be higher in the treatment of 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 may be asymptomatic and therefore they may be undiagnosed. Patients with diabetes should be carefully examined, for example, stress testing, to identify and treat concomitant diseases of the coronary arteries before prescribing the drug.
The use of drugs that affect the renin-angiotensin-aldosterone system can lead to hyperkalemia.
In elderly patients, with renal insufficiency, diabetes mellitus, patients who concurrently receive other drugs that may increase potassium level and/or in patients with intercurrent diseases, hyperkalemia can be fatal.
Before deciding on the simultaneous use of drugs that affect the renin-angiotensin-aldosterone system, the ratio of benefit to risk should be assessed.
The main risk factors for hyperkalemia:
Diabetes mellitus, impaired renal function, age>70 years.
Combination with other drugs affecting the renin-angiotensin-aldosterone system, and/or the use of potassium-containing supplements. Medicinal products that may provoke hyperkalemia, include salt substitutes with potassium, potassium-sparing diuretics, ACE inhibitors, antagonists of angiotensin II receptor, non-steroidal anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporine or tacrolimus), and trimethoprim .
Intercurrent conditions, especially dehydration, acute cardiac decompensation, metabolic acidosis, worsening of renal function, sudden worsening of the renal condition (e.g. infectious diseases), cellular lysis (e.g. acute limb ischemia, rhabdomyolysis, major trauma).
It is recommended to carefully monitor the level of potassium in patients at risk.
ACE inhibitors, telmisartan and other angiotensin II receptor antagonists are less effective at lowering blood pressure in patients of the Negroid race, than in representatives of other races, probably because patients with arterial hypertension of the Negroid race more often have a low level of renin.
When using any antihypertensive drugs, excessive reduction of blood pressure in patients with ischemic cardiopathy or ischemic cardiovascular disease can lead to myocardial infarction or stroke.
Use during pregnancy or lactation
The drug is contraindicated for pregnant women or women planning pregnancy. If, during treatment, this tool confirmed a pregnancy, its use must be discontinued immediately and, if necessary, to replace another drug approved for use in pregnant women (see Sections "Contraindications" and "precautions").
No relevant data on the application telmisartan pregnant women.
Epidemiological justification of the risk of teratogenicity from ACE inhibitors during the first trimester of pregnancy was not convincing, but a slight increase in the risk cannot be ruled out. Although there are no controlled epidemiological data on the risk of teratogenicity in the use of angiotensin II receptor antagonists, similar risks may exist for this class of drugs.
You should not begin therapy with antagonists of a receptor of angiotensin II during pregnancy. If the continuation of therapy with angiotensin II antagonists is considered necessary, and the patient is planning a pregnancy, it is recommended to replace the treatment with antihypertensive therapy with an established safety profile during pregnancy. If pregnancy is established, treatment with angiotensin II receptor antagonists should be stopped immediately and appropriate alternative therapy should be initiated.
As is known, the use of angiotensin II receptor antagonists during the II and III trimesters of pregnancy causes fetotoxicity in humans (impaired renal function, oligohydramniosis, delayed formation of skull bones) and neonatal toxicity (renal failure, hypotension, hyperkalemia). If the use of angiotensin II receptor antagonists began with the second trimester of pregnancy, it is recommended to conduct an ultrasound examination of the renal function and fetal bones. The condition of newborns, whose mothers took angiotensin II receptor antagonists, should be carefully monitored for the presence of arterial hypotension (see Sections "Contraindications" and "Features").
Telmisartan is not recommended during breast-feeding because it is not known, it is allocated in breast milk in humans. Preference is given to alternative treatment with a better studied safety profile, especially when breastfeeding a newborn or premature baby.
The ability to influence the reaction rate when driving motor transport or operating other mechanisms
While driving and other mechanisms must take into account the possibility of dizziness or hypersomnia during antihypertensive therapy, including Tacarcuna.
Method of application and doses
Pills telmisartan it is recommended to apply orally once a day with liquid, regardless of meals.
Telmisartan should be stored in a sealed blister pack from the hygroscopic properties of tablets.
Tablets out of the blister immediately before use.
Treatment of essential arterial hypertension
The usual effective dose is 40 mg once a day. Some patients may have a therapeutic effect of a dose of 20 mg per day. If you are unable to achieve target blood pressure telmisartan the dose can be increased to a maximum of 80 mg per day.
Alternative possible to use telmisartan in combination with thiazide diuretics hydrochlorothiazide, which has the ability to further reduce blood pressure with telmisartan. When deciding to increase the dose should be borne in mind that the maximum antihypertensive effect is usually achieved in the period from 4 to 8 weeks after the start of therapy.
Prevention of cardiovascular diseases
The recommended dose is 80 mg once a day. It is unknown whether the dose telmisartan below 80 mg to be effective in reducing cardiovascular morbidity.
At the beginning of therapy with telmisartan for reducing cardiovascular morbidity it is recommended that careful monitoring of blood pressure, and may also require appropriate dose adjustment of drugs for lowering blood pressure.
Violation of kidney function
Patients with mild to moderate renal impairment do not require dose adjustment. Experience regarding patients with severe impairment of renal function and patients on hemodialysis is limited. For this category of patients below the recommended initial dose telmisartan 20 mg (see Section "Peculiarities of use").
Impaired liver function
Telmisartan is contraindicated in patients with severely impaired liver function.
Patients with mild to moderate hepatic impairment should not exceed the dose of 40 mg once a day (see section "Features").
Dose adjustment in elderly patients is not required.
The safety and efficacy of the drug ALSARTAN in children (under 18 years) has not been investigated.
Information about drug overdose in people is limited.
Symptoms. The most notable phenomena in the telmisartan overdose were hypotension and tachycardia were also reported bradycardia, dizziness, increased creatinine in the serum and acute renal failure.
Treatment. Telmisartan not excreted from the body during hemodialysis. Patients should be carefully monitored and prescribed symptomatic and supportive therapy. Treatment depends on the time elapsed after taking an excessive dose, and the severity of the symptoms. Suggested measures include induction of vomiting and/or gastric lavage. Activated charcoal can be useful in the treatment of overdose. You should frequently check the levels of electrolytes and creatinine in serum. If the patient has a hypotension, he should take a lying position, and you need to quickly start measures to restore the balance of fluid and electrolytes.
Adverse reactions are distributed in frequency as follows: very often (?1/10); often (?1/100 to<1/10); rare (?1/1000 to<1/100); liquid (?1/10000 to<1/1000); very rare (<1/10 000).
In each group the frequency of adverse reactions are presented in order zmenshennya seriousness.
Infections and infestation:
rarely infection of the upper respiratory tract, including pharyngitis and sinusitis, urinary tract infections, including cystitis
fluid: sepsis, including fatal outcome.
From the blood and lymphatic system:
liquid thrombocytopenia, eosinophilia.
From the immune system:
liquid: hypersensitivity, anaphylactic reactions.
Metabolism and eating disorders:
liquid: hypoglycemia (in patients with diabetes).
infrequently depression, insomnia
liquid: a source of concern.
From the nervous system:
not often fainting.
By the organs of vision:
liquid: visual impairment.
On the part of hearing and vestibular apparatus:
not often vertigo.
rare: arterial hypotension, orthostatic hypotension.
From the respiratory system, chest and mediastinal organs:
not often shortness of breath.
rare: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting
liquid: discomfort in the stomach, dry mouth.
Disorders of the digestive system:
liquid: impaired liver function/hepatic disorders.
On the part of the skin and subcutaneous tissue:
infrequently increased perspiration, itching, rash,
liquid: erythema, angioneurotic edema (including deaths), urticaria, drug-induced dermatitis, toxic dermatitis, eczema.
On the part of the musculoskeletal system and connective tissue:
infrequently myalgia, back pain (e.g. sciatica), muscle cramps;
liquid: arthralgia, limb pain, tendon pain (symptoms similar to tendinitis).
From the kidneys and urinary system:
rare: impaired renal function, including acute renal failure.
infrequently chest pain, asthenia (weakness)
liquid: flu-like symptoms.
rare: increased creatinine in the blood
the liquid: the increase of uric acid in the blood, increased liver enzymes, increased levels of CPK (CPK) in the blood, decreased hemoglobin.
Description of selected adverse reactions
In clinical studies an increased incidence of sepsis observed in the application of telmisartan placebo. This phenomenon may be accidental or related to an unknown mechanism.
This adverse reaction was reported as frequent in patients with controlled blood PRESSURE, who were treated with telmisartan to reduce cardiovascular disease in addition to standard therapy.
The abnormal liver function/liver disorder
Most cases of liver dysfunction/liver disorders were observed in postmarketing period in Japanese patients. Japanese patients are more likely to have such adverse reactions.
Keep out of reach of children in the original packaging at a temperature not exceeding 25 ° C.
There are 10 tablets in blister, 1 or 3 blisters in a cardboard box.
Category home away from home
Dr. Reddy's laboratories Ltd, Industrial area - II.
Plot No. 42, 45, 46, p Bachupally, Qutbullapur Mandal, district Rank Reddy, Telangana, India 500090.
MOXAHALA 0.3 MG NO. 30
Moxahala tablets 0.3 mg No. 30 – modern synthetic pharmaceuticals, belongs to the group of agonists of imidazoline receptors. The drug has a pronounced antihypertensive effect, it is used for effective therapeutic treatment of hypertension. LS reduces upper, lower blood PRESSURE due to the effect of the active substance on the functioning of sympathetic NS and reduce vascular resistance. The main indication for the technique is arterial hypertension. Current component – monoside.
Dosing regimen, contraindications
At the initial stage of treatment, adult patients are prescribed a minimum daily dosage of 0.2 mg. it is allowed to increase the daily dose to 0.4 milligrams if the expected effect is insufficient. The medical product is taken in the morning, washed down with a small amount of liquid. The total dosage should not be more than 0.6 milligrams per day. The list of contraindications includes:
The age of eighteen.
Lactation and pregnancy.
Pronounced intolerance to lactose/galactose.
Pathology of the kidney, liver.
Abnormalities in the heart (less rhythm, chronic heart failure conduction disorder).
The medication is prescribed with caution in epilepsy, Parkinson's disease, Raynaud, increased intraocular pressure.