SARTENO [Amlodipine + Losartan] 5 + 100 mg Tablets
SARTENO
instructions for medical use of the medicinal product
Tradename
Sarteno,
International non-proprietary name
Amlodipine + Losartan
Kompozisyon
Composition
Each film-coated tablet contains:
active substances: amlodipine 5 mg, losartan (as losartan potassium) 100 mg (for 5/100 mg dosage), amlodipine 10 mg, losartan (as losartan potassium) 100 mg (for 10/100 mg dosage)
excipients: corn starch, dextrin, microcrystalline cellulose, CMS- Na , hypromellose, silicon dioxide, magnesium stearate, talc
Dosage form
Tablets.
Pharmacotherapeutic group
Antihypertensive combined agent (BMCC + angiotensin II receptor antagonist) .
Pharmacological properties
The composition of the drug contains two active ingredients: amlodipine and losartan, the antihypertensive effect of which complements each other. Amlodipine is a calcium channel inhibitor and losartan is an AT1 receptor blocker. Therapy with Sarteno leads to a decrease in blood pressure by reducing the resistance of peripheral vessels. At the same time, blocking the process of calcium incorporation into the cell and vascular vasodilation are complementary effects.
Amlodipine causes relaxation of smooth muscles and prevents narrowing of the walls of blood vessels, which leads to a decrease in their resistance and, subsequently, a decrease in pressure in the arteries. After oral administration, the maximum therapeutic concentration accumulates within 6-12 hours, and stationary - for 7-8 days (daily use). The bioavailability index of the substance is about 64 - 90%, while the use of food products does not affect this factor. Amlodipine actively binds to plasma protein compounds (93%) and undergoes intense metabolic reactions in the liver. Elimination occurs mostly with the help of the urinary system (10% - unchanged and 60% in the form of metabolites) with an elimination half-life of 30 to 50 hours.
Losartan inhibits the activity of the oligopeptide hormone (angiotensin II), which causes vasoconstriction, by selectively blocking the formation of its bonds with AT1 receptors. After internal use, it is actively absorbed in the gastrointestinal tract, while the bioavailability of the substance is about 33%. Metabolic reactions of this component occur in the liver, with the formation of one active metabolite and inactive derivatives. The maximum therapeutic concentration accumulates within 1 hour for losartan and its metabolite - from 3 to 4 hours. The use of food products does not have a serious impact on the bioavailability of the agent. Losartan forms bonds with plasma protein compounds (by 99%) and practically does not have the ability to pass through the blood-brain barrier. Elimination of losartan occurs with the help of the urinary system (35%) and with excrement (58%).
Indications for use
Arterial hypertension (in patients who are indicated for combination therapy).
Contraindications
• hypersensitivity to the active ingredients and / or auxiliary components of the drug;
• pregnancy and breastfeeding period ;
• severe liver failure (more than 9 points on the Child-Pugh scale) ;
• hemodynamically expressed stenosis of the aortic mouth ;
• severe arterial hypotension ;
• children and adolescents up to 18 years of age.
Dosage and administration
Taken orally, regardless of the meal. Tablets are swallowed whole, without chewing, drinking plenty of water.
The dose is selected after the previously performed dose titration of the individual components of the drug. If a change in the dose of one of the active ingredients in the fixed combination product is required (for example, due to a newly diagnosed disease, a change in the patient's condition or drug interaction), an individual selection of doses of individual components is necessary.
Patients taking both losartan and amlodipine can be switched to a combination drug containing losartan and amlodipine at the same doses.
The recommended dose of the drug is 1 tablet per day.
The drug at a dose of 5 mg + 100 mg is prescribed to patients who have not achieved adequate blood pressure control when using losartan at a dose of 100 mg or a combination drug at a dose of 5 mg + 50 mg.
The drug at a dose of 10 mg + 100 mg is prescribed to patients who have not achieved adequate blood pressure control when using a combination drug at a dose of 5 mg + 100 mg or 10 mg + 50 mg.
The maximum daily dose is 10 mg + 100 mg.
In patients with renal insufficiency with CC from 50 to 20 ml / min , dose adjustment is not required. The drug is contraindicated in patients with CC <20 ml / min and patients on hemodialysis.
The use of this combination is possible in patients with impaired liver function (less than 9 points on the Child-Pugh scale), who, according to the decision of the doctor, are recommended to use losartan at a dose of 50 mg.
In elderly patients, dose adjustment of the drug is not required, but the dose should be increased carefully.
In patients with reduced BCC (for example, due to treatment with high doses of diuretics), the initial dose of losartan should be reduced to 25 mg 1 time / day. Due to the lack of a dosage containing 25 mg of losartan in this combination, this dose should be administered in monotherapy with losartan. Before using the drug, it is necessary to restore the BCC and the sodium content in the blood plasma.
Special instructions and precautions
Special instructions and precautions related to amlodipine. Due to the long half -life, vasodilation that has developed as a result of taking amlodipine may persist after its withdrawal. Thus, the use of another vasodilator after discontinuation of amlodipine should be carried out with caution, an individual assessment of the dose, dosing interval and active monitoring of the patient's condition is necessary.
During the period of treatment, it is necessary to control body weight and salt intake, the appointment of an appropriate diet. It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gum hyperplasia).
Special instructions and precautions related to losartan. Hyperkalemia (the content of potassium in the blood plasma> 5.5 mmol / l) was observed in 1.5% of patients taking losartan as monotherapy. The simultaneous use of potassium-sparing diuretics (eg spironolactone, triamterene, amiloride, eplerenone), potassium preparations, potassium-containing salt substitutes, as well as drugs that can lead to an increase in the content of potassium in the blood plasma (eg heparin), with losartan should be justified (especially in elderly patients with impaired renal function), and the content of potassium in the blood plasma should be controlled.
Taking losartan can lead to transient arterial hypotension, accompanied by shock, fainting and shortness of breath.
Apply with caution: bilateral renal artery stenosis or solitary kidney artery stenosis, condition after kidney transplantation (no experience with use), ischemic heart disease, heart failure with life-threatening arrhythmias, cerebrovascular disease, primary hyperaldosteronism, history of angioedema, unstable angina, use in patients with low BCC (for example, with the use of high doses of diuretics, severe diarrhea, vomiting, and other conditions leading to hypovolemia), in patients on a salt-restricted diet, hyperkalemia, arterial hypotension, liver failure (less than 9 points on the Child-Pugh scale) , sick sinus syndrome (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology ( II - IV functional class according to the NYHA classification ), aortic and / or mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month and after a heart attack), elderly patients.
Influence on the ability to drive vehicles and mechanisms
Care should be taken when driving vehicles and working with other technical devices that require increased concentration of attention and speed of psychomotor reactions, given the risk of dizziness.
Use during pregnancy and during breastfeeding
Use during pregnancy and during breastfeeding is contraindicated.
Interaction with other drugs
The antihypertensive effect of the drug may be enhanced when used simultaneously with other antihypertensive drugs. Therefore, the simultaneous use of various antihypertensive drugs should be justified.
Amlodipine
The simultaneous use of amlodipine with thiazide diuretics, alpha-blockers or ACE inhibitors is considered safe.
It is possible to enhance the antihypertensive effect of calcium channel blockers with simultaneous use with thiazide and "loop" diuretics, ACE inhibitors and nitrates, as well as with simultaneous use with alpha 1 -blockers, antipsychotics.
The simultaneous use of amlodipine with inhibitors of the CYP3A4 isoenzyme requires careful monitoring of symptoms of arterial hypotension and peripheral edema.
Beta-blockers, when used simultaneously with amlodipine, can exacerbate the course of chronic heart failure.
Some calcium channel blockers may potentiate the negative inotropic effect of antiarrhythmic agents that prolong the QT interval (eg, amiodarone and quinidine).
Antipsychotics and isoflurane enhance the antihypertensive effect of dihydropyridine derivatives.
With the on / in the introduction of dantrolene during therapy with amlodipine, collapse, arrhythmias, a decrease in the strength of heart contractions and hyperkalemia are possible.
Calcium preparations can reduce the antihypertensive effect of calcium channel blockers.
With the simultaneous use of amlodipine with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Losartan
As with other drugs that block the formation of angiotensin II and its effects, the simultaneous use of potassium-sparing diuretics (for example, spironolactone, triamterene, amiloride, eplerenone), potassium preparations and potassium-containing salt substitutes can lead to an increase in serum potassium.
As with other drugs that affect the excretion of sodium, losartan can reduce the excretion of lithium, therefore, with the simultaneous use of lithium preparations and angiotensin II receptor antagonists, it is necessary to carefully monitor the concentration of lithium in the blood serum.
In some patients with impaired renal function who received treatment with NSAIDs, including selective COX-2 inhibitors, the simultaneous use of ACE inhibitors and / or angiotensin II receptor antagonists, including losartan, may cause a further deterioration in renal function up to the development of acute renal failure. Usually this effect is reversible. NSAIDs, including selective COX-2 inhibitors, may reduce the effect of angiotensin II receptor antagonists, including losartan. Therefore, the antihypertensive effect of angiotensin II receptor antagonists may be weakened by the simultaneous use of NSAIDs, in particular, selective COX-2 inhibitors. Thus, the simultaneous use of the combination of amlodipine / losartan with NSAIDs should be carried out with caution in patients with impaired renal function.
Dual RAAS blockade (simultaneous use of ACE inhibitors and angiotensin II receptor antagonists) in patients with atherosclerosis, chronic heart failure, or diabetes mellitus with target organ damage is associated with a higher incidence of arterial hypotension, syncope, hyperkalemia, and renal dysfunction (including acute renal insufficiency) compared with the use of the drug of one of the listed groups. Double blockade of the RAAS is possible only in selected cases under careful monitoring of renal function.
Taking rifampicin, an inducer of drug metabolism, reduces plasma concentrations of losartan and its active metabolite.
Side effect
Amlodipine/losartan combination
From the side of the nervous system: often - dizziness, headache; infrequently - drowsiness.
From the digestive system: infrequently - constipation, discomfort in the abdomen, dyspepsia, vomiting, esophageal reflux.
On the part of the skin and subcutaneous tissues: infrequently - pruritus, urticaria.
From the side of the cardiovascular system: infrequently - a feeling of palpitations, flushes of blood to the skin of the face, orthostatic hypotension.
From the respiratory system: infrequently - shortness of breath.
On the part of the organ of hearing and labyrinth disorders: infrequently - systemic dizziness.
From the urinary system: infrequently - increased frequency of urination.
General disorders: infrequently - asthenia, discomfort or pain in the chest, feeling of fullness in the abdomen, peripheral edema.
Side effects observed with a separate intake of the components of the drug (amlodipine and losartan) may also be its potential side effects.
If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Cases of overdose with amlodipine/losartan fixed combination are unknown. The following are data on overdose of amlodipine and losartan taken separately.
Amlodipine
Symptoms: a pronounced decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of developing severe and persistent arterial hypotension, including with the development of shock and death).
Treatment: administration of activated charcoal. If necessary, gastric lavage is indicated. Clinically significant arterial hypotension with an overdose of amlodipine requires a set of measures to normalize the state of the cardiovascular system, it is necessary to give an elevated position to the lower extremities, to constantly monitor the functional parameters of the heart and respiratory system, BCC and diuresis. Intensive symptomatic therapy. To restore vascular tone and blood pressure, vasoconstrictor drugs are used (in the absence of contraindications to their use) in order to eliminate the blockade of calcium channels - intravenous administration of calcium gluconate. Hemodialysis is ineffective.
Losartan
There are limited data on overdose of losartan.
Symptoms: pronounced decrease in blood pressure, tachycardia; bradycardia due to parasympathetic (vagal) stimulation.
Treatment: with the development of symptomatic arterial hypotension, supportive therapy is carried out. Hemodialysis for losartan and its active metabolite is ineffective.
Storage conditions
Store in a cool and dry place, at a temperature not exceeding 30º C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiry date stated on the package.
Holiday conditions
Released by prescription.
Release form
10 tablets in an aluminum foil blister. 3 blisters with instructions for use in a cardboard box.