Lortenza tabs 5mg + 50mg #30

Instruction for Lortenza

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Lortenza is a combined antihypertensive drug.

Release form and composition

Lortenza dosage form - film-coated tablets:
    dosage 0.005 g + 0.05 g: slightly biconvex, orange to light brown, oval;
    dosage 0.01 g + 0.05 g: slightly biconvex, red-brown, oval;
    dosage 0.005 g + 0.1 g: biconvex, pink, oval;
    dosage 0.01 g + 0.1 g: biconvex, pale brownish yellow, oval.
In contoured cell packs of 7 or 10 pcs., In a cardboard box 1, 2, 4, 8 or 12 packs of 7 pcs. or 1, 3, 6 or 9 packs of 10 pcs.
Active substances in the composition of 1 tablet (0.005 g + 0.05 g, 0.01 g + 0.05 g, 0.005 g + 0.1 g, 0.01 g + 0.1 g, respectively):
    amlodipine besylate (amlodipine besylate) - 0.006 94 / 0.0138 8 / 0.006 94 / 0.0138 8 g (equivalent to amlodipine - 0.005 / 0.01 / 0.005 / 0.01 g);
    losartan A granule substance - 0.163 55 / 0.163 55 / 0.327 1/0, 327 1 g, including potassium losartan - 0.05 / 0.05 / 0.1 / 0.1 g.
Auxiliary components of Lortenza: cellactose 80 (lactose monohydrate - 75%, cellulose - 25%) - 0.036 45 / 0.036 45 / 0.072 9 / 0.072 9 g; microcrystalline cellulose - 0.212 96 / 0.206 02 / 0.212 96 / 0.206 02 g; pregelatinized starch - 0.054 / 0.054 / 0.054 / 0.054 g; sodium carboxymethyl starch - 0.022 / 0.022 / 0.022 / 0.022 g; iron dye yellow oxide (E172) - 0.000 4 / 0.000 4 / 0.000 4 / 0.000 4 g; colloidal silicon dioxide - 0.001 6 / 0.001 6 / 0.002 1 / 0.002 1 g; magnesium stearate - 0.005 1 / 0.005 1 / 0.006 6 / 0.006 6 g.
Sheath: opadry II white (talc - 14.8%, macrogol - 20.2%, titanium dioxide E171 - 25%, polyvinyl alcohol - 40%) - 0.025 71 / 0.024 4 / 0.029 75 / 0.029 g; 0.005 g + 0.05 g each - iron dye yellow oxide (E172) - 0.001 03 g; iron dye red oxide (E172) - 0.000 26 g; 0.01 g + 0.05 g and 0.005 g + 0.1 g, respectively - iron dye red oxide (E172) - 0.002 6 / 0.000 25 g; 0.01 g each + 0.1 g - iron dye yellow oxide (E172) - 0.001 g.

Pharmacodynamics

The drug Lortenza is a combination of two active substances with a mutually complementary antihypertensive effect: a slow calcium channel blocker - amlodipine and an angiotensin II receptor antagonist - losartan.
Amlodipine (a derivative of dihydropyridine) and losartan (a synthetic antagonist of angiotensin II receptors) have different mechanisms of antihypertensive action: the former dilates blood vessels, thereby reducing the total peripheral vascular resistance; the second has an effect on the renin-angiotensin-aldosterone system (RAAS); inhibits the effects of angiotensin II, which leads to a more pronounced decrease in blood pressure compared with that with monotherapy with each of the agents.
Amlodipine actions:
    blocking slow calcium channels and reducing the transmembrane current of calcium ions into cardiomyocytes and vascular smooth muscle cells;
    antihypertensive action by direct relaxation of the smooth muscles of the arterial vessels;
    pronounced effect on vascular smooth muscle cells;
    no negative impact on atrioventricular conduction and myocardial contractility;
    increased renal blood flow and decreased renal vascular resistance;
    no negative impact on the ejection fraction or concentration of lipids and glucose in blood plasma, exercise tolerance in chronic heart failure II-IV functional class according to NYHA classification;
    lowering blood pressure in patients in a sitting and lying position, as well as during physical exertion;
    through the gradual development of the pharmacodynamic effect, the absence of a sharp decrease in blood pressure or reflex tachycardia;
    decrease in the severity of left ventricular hypertrophy.
Its effect after a single oral administration begins after 2–4 hours and lasts for 24 hours. The maximum antihypertensive effect is achieved no earlier than 28 days after the start of treatment. With long-term use, its hemodynamic effects remain unchanged.
Losartan actions:
    performing important biological functions, including the release of aldosterone and vasoconstriction; binding to AT1 receptors present in many tissues (heart, kidneys, adrenal glands, vascular smooth muscle tissue);
    stimulating the proliferation of vascular smooth muscle cells;
    selective blocking of AT1 receptors;
    blocking all physiological effects of angiotensin II, in vitro and in vivo, regardless of the source or route of its synthesis (both losartan and its pharmacologically active carboxylated metabolite E-3174);
    lack of agonist properties and blocking of receptors of other hormones or ion channels involved in the regulation of cardiovascular activity;
    the absence of inhibition of the angiotensin-converting enzyme that destroys bradykinin, due to which an increase in the frequency of side effects mediated by bradykinin is not observed;
    suppression of the regulation of renin secretion under the action of angiotensin II by a negative feedback mechanism, which causes an increase in plasma renin activity, in turn, leading to an increase in the concentration of angiotensin II in blood plasma. Nevertheless, the decrease in the concentration of aldosterone in the blood plasma and the antihypertensive effect persist, which indicates an effective blockade of AT1 receptors;
    a decrease in the activity of renin in blood plasma and the concentration of angiotensin II in the blood plasma to the initial values ​​within 3 days after cancellation.
Losartan is an important defining pathophysiological link in the development of arterial hypertension, the main active hormone of the RAAS, and a powerful vasoconstrictor.

Pharmacokinetics

Amlodipine characteristics:
    absorption: when taken orally in a therapeutic dose, it is well absorbed; Cmax (maximum concentration in blood plasma) is reached after 6–12 hours; absolute bioavailability varies within 64–80%; food intake has no effect on its absorption;
    distribution: Vd (volume of distribution) - about 21 liters per 1 kg of body weight; equilibrium plasma concentrations are reached after 7–8 days from the start of therapy; binding to blood plasma proteins is 98%;
    metabolism: in the liver, it undergoes an active, but slow metabolism in the absence of a significant effect of presystemic biotransformation (the first passage through the liver); metabolites do not have significant pharmacological activity;
    excretion: T1 / 2 (final half-life from blood plasma) - 30–40 hours; plasma clearance - 7 ml per minute per 1 kg of body weight; approximately 60% of metabolites and 10% of amlodipine in unchanged form are excreted by the kidneys, 20-25% - by the intestines.
In case of liver dysfunction, an elongation of T½ is noted (the experience of using Lortenza in this category of patients is limited).
Losartan characteristics:
    absorption: well absorbed after oral administration; its systemic bioavailability is approximately 33%; Cmax of both losartan and its active metabolite are reached after 1 hour and 3-4 hours, respectively;
    distribution: 99% binds to blood plasma proteins, mainly albumin (as well as its active metabolite); Vd - 34 l;
    metabolism: during the first passage through the liver, it undergoes metabolism with the formation of an active carboxylated metabolite (E-3174) and other inactive metabolites; approximately 14% of losartan taken orally or intravenously is converted to its active metabolite; after the application of potassium losartan labeled with radioactive carbon, most of the radioactive label in the bloodstream corresponds to losartan and its active metabolite;
    Excretion: plasma clearance - 600 ml per 1 min, its active metabolite - 50 ml per 1 min; renal clearance - 74 ml per minute, its active metabolite - 26 ml per minute; approximately 4% of the oral dose is excreted unchanged by the kidneys and 6% as an active metabolite; its pharmacokinetics, like that of the active metabolite, is linear when taken orally in doses up to 0.2 g.
The concentration of losartan and its active metabolite in the blood plasma after oral administration decreases polyexponentially with the final T½ in about 2 hours and 6-9 hours, respectively. When taken once a day, losartan and its active metabolite (at a dose of 0.1 g) do not accumulate in blood plasma. Losartan and its metabolites are excreted through the intestines with bile and kidneys. After intravenous administration and oral administration of radioactive carbon-labeled losartan potassium, approximately 35/43% of the radioactivity of losartan and its active metabolite, respectively, was excreted by the kidneys and 58/50% through the intestine.
Special patient groups:
    elderly patients with arterial hypertension: the concentration of losartan and its active metabolite in blood plasma does not differ significantly from these indicators in young patients with arterial hypertension;
    gender: in women with arterial hypertension, the concentration of losartan in blood plasma is 2 times higher than the corresponding values ​​in men with arterial hypertension; the concentration of the active metabolite in women and men does not differ;
    liver dysfunction: with mild and moderate alcoholic cirrhosis of the liver in cases of oral administration of losartan, its plasma concentration increased 5 times, its active metabolite - 1.7 times compared with the same indicators in young healthy male volunteers;
    impaired renal function: with creatinine clearance> 10 ml per minute, the concentration of losartan in the blood plasma does not change. AUC (area under the concentration-time curve) in patients on hemodialysis is approximately 2 times higher than in normal renal function; the concentration of the active metabolite in the blood plasma does not change either with impaired renal function or while on hemodialysis; through hemodialysis, losartan and its active metabolite are not excreted.

Indications for use

According to the instructions, Lortenza is prescribed for the treatment of patients with arterial hypertension, who are shown combined treatment with amlodipine and losartan.

Contraindications

Absolute:
    severe arterial hypotension (systolic blood pressure <90 mm Hg);
    severe renal dysfunction (creatinine clearance <20 ml per minute), stay on hemodialysis;
    severe hepatic impairment (on the Child-Pugh scale exceeding 9 points);
    hemodynamically unstable heart failure after acute myocardial infarction;
    hemodynamically pronounced aortic stenosis;
    shock, including cardiogenic shock;
    syndrome of glucose-galactose malabsorption, lactase deficiency, lactose intolerance (since the drug contains lactose);
    combined therapy with aliskiren for diabetes mellitus or impaired renal function (creatinine clearance <60 ml per minute);
    age under 18;
    pregnancy;
    lactation period;
    individual intolerance to the components of the drug.
Relative (diseases / conditions in the presence of which the appointment of Lortenza requires caution):
    low level of BCC (circulating blood volume);
    a history of angioedema;
    cerebrovascular diseases;
    primary hyperaldosteronism;
    stenosis of an artery of a solitary kidney or bilateral stenosis of the renal arteries;
    condition after kidney transplantation (since there is no experience with this category of patients);
    unstable angina;
    heart failure with life-threatening arrhythmias;
    coronary heart disease;
    chronic heart failure of non-ischemic etiology (II-IV functional class according to NYHA classification);
    acute myocardial infarction (period 1 month after);
    stay on a diet with limited consumption of table salt;
    hyperkalemia;
    arterial hypotension;
    liver failure (on the Child-Pugh scale <9 points);
    sick sinus syndrome (tachycardia, severe bradycardia);
    hypertrophic obstructive cardiomyopathy;
    mitral and / or aortic stenosis;
    elderly age.

Instructions for use of Lortenza: method and dosage

The tablets are taken orally, regardless of food, with a small amount of water. The dose is 1 pc. in a day.
Lortenza 5 + 50 mg tablets are used when monotherapy with 0.005 g of amlodipine and 0.05 g of losartan does not lead to adequate blood pressure control.
Lortenza tablets 5 + 100 mg are used when therapy with tablets of 0.005 g + 0.05 g or losartan at a dose of 0.1 g does not lead to adequate blood pressure control.
Lortenza tablets 10 + 5 mg are used when therapy with tablets of 0.005 g + 0.05 g or amlodipine at a dose of 0.01 g does not lead to adequate blood pressure control.
Lortenza tablets 10 + 100 mg are used when therapy with tablets of 0.005 g + 0.1 g or 0.01 g + 0.05 g does not lead to adequate blood pressure control.
The dose is determined by titrating the doses of the active components of the drug. If it is necessary to change the dose of one of the active substances in the fixed combination preparation, the doses of the individual components are selected on an individual basis. The maximum dose of the drug is 0.01 g + 0.1 g per day.
It is allowed to transfer patients receiving combination therapy with losartan and amlodipine to Lortenza in the same doses of active substances.
In patients with reduced BCC, the initial dose of losartan should be reduced to 0.025 g once a day. Due to the lack of a dosage containing 0.025 g of losartan in Lortenza, this dose of the substance should be prescribed in monotherapy.
Before using the drug, it is necessary to restore the BCC and the sodium content in the blood plasma.

Side effects

Possible adverse reactions (> 10% - very often;> 1% and <10% - often;> 0.1% and <1% - infrequently;> 0.01% and <0.1% - rarely; <0, 01% - very rare).
Side effects due to amlodipine:
    blood and lymphatic system: very rarely - thrombocytopenia, leukopenia;
    immune system: very rarely - angioedema, hypersensitivity reactions;
    metabolism and nutrition: very rarely - hyperglycemia;
    psyche: infrequently - mood lability, including anxiety, insomnia, depression; rarely - confusion of consciousness;
    nervous system: often - headache, drowsiness, dizziness; infrequently - dysgeusia, tremor, hypesthesia, paresthesia; very rarely - peripheral neuropathy, muscle hypertonia;
    organ of vision: infrequently - visual impairment (including diplopia);
    organ of hearing and labyrinthine disorders: infrequently - tinnitus;
    heart: often - palpitations; very rarely - atrial fibrillation, ventricular tachycardia, bradycardia, arrhythmia, myocardial infarction;
    vessels: often - a feeling of rush of blood to the skin of the face; infrequently - a marked decrease in blood pressure; very rarely - vasculitis;
    respiratory system, chest and mediastinal organs: infrequently - rhinitis, shortness of breath; very rarely - cough;
    digestive system: often - nausea, abdominal pain; infrequently - thirst, dryness of the oral mucosa, changes in bowel movements (including diarrhea and constipation), dyspepsia, vomiting; very rarely - pancreatitis, gingival hyperplasia, gastritis;
    liver and biliary tract: very rarely - increased activity of liver enzymes, jaundice, hepatitis;
    skin and subcutaneous tissues: infrequently - itching / rash, rash, rash, increased sweating, skin discoloration, purpura, alopecia; very rarely - Stevens-Johnson syndrome, exfoliative dermatitis, exudative erythema multiforme, photosensitivity, urticaria;
    musculoskeletal and connective tissue: often - ankle swelling; infrequently - arthralgia, myalgia, muscle cramps;
    kidneys and urinary tract: infrequently - frequent urination, nocturia, painful urge to urinate;
    genitals and mammary gland: infrequently - gynecomastia, impotence, erectile dysfunction;
    general disorders and disorders at the injection site: often - peripheral edema, increased fatigue; infrequently - pain, malaise, asthenia;
    laboratory and instrumental data: infrequently - decrease / increase in body weight.
Side effects due to losartan:
    infections and parasitic diseases: frequency unknown - urinary tract infection;
    blood and lymphatic system: frequency unknown - anemia, thrombocytopenia;
    immune system: rarely - hypersensitivity reactions, angioneurotic edema, vasculitis, including Shenlein-Henoch purpura, anaphylactic reactions;
    psyche: frequency unknown - depression;
    nervous system: often - dizziness; infrequently - sleep disorders, headache, drowsiness; frequency unknown - migraine, dysgeusia;
    hearing organ and labyrinthine disorders: often - vertigo; frequency unknown - tinnitus;
    heart: infrequently - angina pectoris, palpitations;
    vessels: infrequently - orthostatic hypotension (including dose-dependent orthostatic reactions);
    respiratory system, chest and mediastinal organs: frequency unknown - cough;
    digestive system: infrequently - constipation, abdominal pain; frequency unknown - diarrhea, pancreatitis;
    liver and biliary tract: rarely - hepatitis; frequency unknown - impaired liver function;
    skin and subcutaneous tissue: infrequently - skin rash; frequency unknown - photosensitivity, urticaria, pruritus;
    kidneys and urinary tract: frequency unknown - back pain, rhabdomyolysis, arthralgia, myalgia;
    genitals and mammary gland: frequency unknown - impotence / erectile dysfunction;
    disorders and disorders at the injection site: infrequently - asthenia, peripheral edema, fatigue; frequency unknown - flu-like symptoms, malaise;
    laboratory and instrumental data: often - hyperkalemia; rarely - an increase in the activity of alanine aminotransferase; frequency unknown - hyponatremia.

Overdose

There are no cases of overdose of Lortenza, however, there is evidence of an overdose of each of the active components of the drug, which should be taken into account when prescribing them in monotherapy.

Special instructions

Perhaps the development of symptomatic arterial hypotension in patients with reduced BCC at the beginning of the drug intake. Before starting therapy with Lortenza, the deficiency of the BCC must be eliminated.
The vasodilation, which has developed as a result of taking amlodipine, due to the prolonged T½ can persist even after discontinuation of treatment. In this regard, after the abolition of amlodipine, another vasodilator is used with caution, conducting an individual assessment of the dose, dosing interval and actively monitoring the patient's condition.
During therapy, it is important to monitor body weight and consumption of table salt, and observe an appropriate diet. Frequent visits to the dentist and maintenance of oral hygiene are recommended, since gingival hyperplasia, bleeding and soreness may develop.
In 1.5% of patients receiving monotherapy with losartan, the development of hyperkalemia was noted. Lortenza's abolition was not required in any of these cases. The combined use of losartan with potassium-containing salt substitutes, potassium preparations, potassium-sparing diuretics and drugs that can increase the plasma potassium content should be justified (especially in elderly patients with impaired renal function). You should also monitor the content of potassium in the blood plasma.
The use of losartan can serve the development of transient arterial hypotension, accompanied by shortness of breath, fainting and shock.
With a history of angioedema, Lortenza should be taken under medical supervision.
Since the drug has an effect on the RAAS, its administration by patients with chronic heart failure with or without impaired renal function may lead to the development of severe arterial hypotension or acute renal impairment.

Influence on the ability to drive vehicles and complex mechanisms

Patients during the period of taking Lortenza should be careful when conducting potentially hazardous activities and driving vehicles, since dizziness may develop.

Application during pregnancy and lactation

Lortenza is contraindicated for use during pregnancy and lactation.

Childhood use

Due to the lack of data on the safety and efficacy of using the drug in children under the age of 18, Lortenza is contraindicated in patients of this age group.

With impaired renal function

The drug is contraindicated in severe renal impairment and in patients on hemodialysis.

For violations of liver function

The drug is contraindicated in severe hepatic impairment.
In cases of liver dysfunction in history, Lortenza is used in lower doses. Since the drug does not have a dosage containing 0.025 g of losartan, it is recommended that this dose be prescribed as monotherapy.
The drug is prescribed with caution to patients with impaired liver function.

Use in the elderly

Lortenza is used with caution in elderly patients.

Drug interactions

Antihypertensive drugs can enhance the antihypertensive effect of Lortenza, and therefore, their intake should be justified.
With the combined use of amlodipine with inhibitors of the isoenzyme CYP3A4, careful monitoring of symptoms of arterial hypotension and peripheral edema is necessary.
The effect of drugs / substances on amlodipine in combination therapy:
    erythromycin: increases its Cmax in blood plasma;
    strong inhibitors of the isoenzyme CYP3A4 (ritonavir, itraconazole, ketoconazole): may increase its concentration in blood plasma;
    antipsychotics and isoflurane: enhance its antihypertensive effect;
    calcium preparations: can reduce its antihypertensive effect.
The systemic exposure of amlodipine (at a dose of 0.005 g per day) increases when combined with diltiazem (at a dose of 0.18 g per day) by 60% in elderly patients.
When combined treatment with amlodipine with inducers of the isoenzyme CYP3A4, regular monitoring of blood pressure is required; with beta-blockers - an exacerbation of the course of chronic heart failure is possible; with dantrolene for intravenous administration - the development of hyperkalemia, arrhythmia, collapse, decreased heart rate; with lithium preparations - an increase in the manifestation of neurotoxicity.
Losartan can reduce the excretion of lithium when taken in combination with lithium-containing drugs, and therefore requires careful monitoring of the concentration of lithium in the blood serum.
The effect of drugs / substances on losartan when used in combination:
    non-steroidal anti-inflammatory drugs, including selective inhibitors of COX-2: may reduce its effects;
    rifampicin: reduces its concentration in blood plasma;
    fluconazole: increases its concentration in blood plasma and decreases the concentration of its active metabolite.

Terms and conditions of storage

Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.

Reviews about Lortenza

According to reviews, Lortenza is an effective drug that practically does not cause side effects.

Terms of sell

You can buy Lortenza Lortenza without a prescription.