Losartan-Richter
Losartan-Richter: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews Lozartane-Richter
- 19. Price in pharmacies
Latin name: Losartan-Richter
ATX code: C09CA01
Active ingredient: losartan (Losartan)
Manufacturer: JSC Gedeon Richter-RUS (Russia); Gedeon Richter Poland, Co. Ltd. (Poland)
Description and photo update: 2019-08-10
Losartan-Richter is an antihypertensive drug, angiotensin II receptor antagonist.
Release form and composition
The drug is available in the form of film-coated tablets: almost white or white, biconvex; dosage 50 mg - round, engraved "50" on one side, dividing risk on the other; dosage 100 mg - oval, on one side engraved "100", the other side is smooth (10 pcs. in blisters, in a cardboard box 1 or 3 blisters and instructions for the use of Losartan-Richter).
1 tablet contains:
- active substance: losartan potassium - 50 mg or 100 mg;
- auxiliary components: pregelatinized starch, colloidal silicon dioxide, croscarmellose sodium, microcrystalline cellulose, magnesium stearate;
- film cover: Opadray 33G28523 white [lactose monohydrate, triacetin, macrogol, hypromellose, titanium dioxide - CI 77891 (E171)].
Pharmacological properties
Pharmacodynamics
Losartan-Richter is an antihypertensive drug, the active ingredient of which is losartan, which is a specific antagonist of angiotensin II receptors (type AT 1).
Angiotensin II is a hormone, its selective binding to AT 1 -receptors of smooth muscle tissues of blood vessels, adrenal glands, kidneys and heart causes important biological processes, including vasoconstriction, release of aldosterone, proliferation of smooth muscle cells. The action of losartan and its pharmacologically active metabolite is aimed at blocking all physiologically important effects of angiotensin II, regardless of its synthesis.
Losartan-Richter helps to reduce the total peripheral vascular resistance (OPSS), blood pressure (BP), pressure in the pulmonary circulation, blood concentration of aldosterone and norepinephrine, afterload. In addition, losartan has a diuretic effect, prevents the onset of myocardial hypertrophy, in patients with CHF (chronic heart failure) - increases exercise tolerance.
Losartan does not inhibit angiotensin-converting enzyme (ACE), it does not have undesirable effects associated with bradykinin (including angioedema), since it does not inhibit kinase II, the enzyme degrading bradykinin.
The maximum hypotensive effect of Losartan-Richter after a single oral administration is achieved after 6 hours and gradually decreases over the next 24 hours. A stable effect develops after 21–42 days of regular administration of the drug.
The use of the drug for proteinuria (more than 2 g / day) in patients with arterial hypertension without diabetes mellitus contributes to a significant decrease in the level of protein in the urine, the excretion of immunoglobulins G and albumin.
In therapeutic doses, losartan does not affect autonomic reflexes, the level of serum concentration of total cholesterol, high density lipoprotein cholesterol (HDL), triglycerides and fasting blood glucose.
Pharmacokinetics
After oral administration, losartan is actively absorbed, systemic bioavailability is up to 33%. The maximum concentration (C max) in blood plasma is reached after 1–1.5 hours. The time to reach C max for the active metabolite of losartan varies from 3 to 4 hours. Simultaneous food intake does not affect the bioavailability of the drug.
The binding of losartan to blood plasma proteins (mainly albumin) is 92%, its active metabolite is 99%. The volume of distribution (V d) is 34 liters. Losartan practically does not overcome the blood-brain barrier.
Approximately 14% of the dose taken is metabolized by carboxylation during the first passage through the liver, with the participation of the cytochrome P450 isoenzyme CYP2C9. In this case, a metabolite is formed, the activity of which is 10–40 times higher than that of losartan. In some patients (their population is about 1%), a minimum amount of an active metabolite is formed.
Plasma clearance of losartan is 600 ml / min, the active metabolite is 50 ml / min. The renal clearance of losartan is 74 ml / min, the active metabolite is 26 ml / min.
When taken orally in doses up to 200 mg, losartan and its active metabolite are characterized by linear pharmacokinetics.
The final half-life (T 1/2) of losartan is about 2 hours, the active metabolite is from 6 to 9 hours. Against the background of taking a daily dose of 100 mg, significant cumulation of losartan and its active metabolite in the blood plasma is not observed.
35% of the drug dose is excreted through the kidneys, of which 4% is unchanged, and 6% is in the form of an active metabolite. The rest is excreted with feces through the intestines.
In patients with mild to moderate severity of alcoholic liver cirrhosis, the concentration of losartan increases 5 times, and the active metabolite - 1.7 times.
In case of impaired renal function with creatinine clearance (CC) above 10 ml / min, the level of losartan in blood plasma does not differ from that in healthy patients. During hemodialysis, the AUC value (area under the concentration-time pharmacokinetic curve) increases by about 2 times.
Pharmacokinetic parameters in old age or in different sexes do not change significantly. In men and women, the level of plasma concentrations of the active metabolite does not differ.
Indications for use
- arterial hypertension;
- arterial hypertension in patients with left ventricular hypertrophy - to reduce the risk of cardiovascular disease and death;
- chronic heart failure - in the absence of a therapeutic effect from the use of ACE inhibitors;
- type 2 diabetes mellitus with proteinuria - in order to reduce the risk of developing proteinuria and hypercreatininemia.
Contraindications
Absolute:
- lactose intolerance, glucose or galactose malabsorption syndrome, galactosemia;
- period of pregnancy;
- lactation;
- age up to 18 years;
- hypersensitivity to the components of the drug.
Losartan-Richter should be used with caution in case of arterial hypotension, violation of water-electrolyte balance, reduced BCC (circulating blood volume), renal failure (including bilateral renal artery stenosis, stenosis of the artery of a single kidney), hepatic failure.
Losartan-Richter, instructions for use: method and dosage
Lozartan-Richter tablets are taken orally, regardless of food intake.
The frequency of administration depends on the dose of the drug, the dose of Losartan-Richter 50 mg per day is usually taken at one time, the daily dose of 100 mg is taken at one time or divided into 2 doses.
Recommended daily dosage:
- arterial hypertension: initial and maintenance dose - 50 mg. If, after 21–42 days of using the tablets, there is no maximum antihypertensive effect, then the initial dose of the drug can be increased to 100 mg. With the simultaneous administration of large doses of diuretics, it is recommended to start therapy with Losartan-Richter with 25 mg (1/2 tablet of 50 mg). Elderly patients or with impaired renal function (including patients on hemodialysis) do not require dose adjustment. In case of impaired liver function, the drug should be taken in lower doses;
- chronic heart failure: the initial dose is 12.5 mg (1/4 tablet of 50 mg). For a single dose, the usual maintenance dose is 50 mg per day. To achieve it, a gradual increase in the initial dose by 12.5 mg with an interval of 7 days is required according to the following scheme: during the first 7 days, the patient should take 12.5 mg daily, the second 7 days - 25 mg, from the 15th on the 28th day - 50 mg each. Shows the appointment of Losartan-Richter as part of complex therapy with cardiac glycosides and diuretics;
- chronic heart failure (in the absence of a clinical response to therapy with ACE inhibitors): the initial dose is 50 mg. If necessary, the dose of Losartan-Richter can be increased to 100 mg or the treatment can be supplemented with the appointment of low doses of hydrochlorothiazide;
- Reducing the risk of developing proteinuria and hypercreatininemia in patients with type 2 diabetes mellitus with proteinuria: the initial dose is 50 mg. During treatment, it can be increased to 100 mg, taking into account the patient's blood pressure.
Side effects
- on the part of the cardiovascular system: often - palpitations, tachycardia; sometimes - arrhythmias, dose-dependent orthostatic hypotension, epistaxis, bradycardia, angina pectoris, vasculitis;
- from the digestive system: often - abdominal pain, diarrhea, dyspepsia, nausea; sometimes - dry mouth, decreased appetite, toothache, flatulence, vomiting, constipation, gastritis, abnormal liver function, hepatitis;
- on the part of the musculoskeletal system: often - pain in the back and / or in the lower extremities, muscle spasms, cramps, myalgia, chest pain; sometimes - pain in the shoulder and / or knee joint, arthralgia, arthritis, fibromyalgia;
- from the nervous system and mental disorders: often - insomnia, dizziness, headache; sometimes - sleep disturbance, drowsiness, anxiety, memory disorders, ataxia, paresthesia, hypesthesia, peripheral neuropathy, tremor, syncope, migraine, depression;
- from the senses: sometimes - taste disturbance, ringing in the ears, conjunctivitis, visual impairment;
- from the respiratory system: often - cough, nasal congestion, pharyngitis, sinusitis, swelling of the nasal mucosa, dyspnea, upper respiratory tract infections, bronchitis;
- dermatological reactions: sometimes - dry skin, erythema, increased sweating, photosensitivity, alopecia;
- allergic reactions: sometimes - rash, itching, urticaria, angioedema (including swelling of the face, lips, pharynx and / or tongue and larynx with airway obstruction);
- on the part of the hematopoietic system: infrequently - eosinophilia, anemia, thrombocytopenia, Shenlein's purpura - Genoch;
- from the urinary system: sometimes - impaired renal function, urgency to urinate, urinary tract infections;
- laboratory parameters: often - hyperkalemia (an increase in the level of potassium in the blood plasma more than 5.5 mmol / l); infrequently - an increase in serum concentration of urea, residual nitrogen or creatinine; very rarely - hyperbilirubinemia, a moderate increase in the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST);
- general symptoms: often - increased fatigue, asthenia, chest pain, peripheral edema;
- others: sometimes - decreased potency, decreased libido, gout.
Overdose
Symptoms of an overdose of Losartan-Richter: a pronounced decrease in blood pressure, tachycardia, the development of bradycardia.
Treatment: the appointment of symptomatic therapy, forced diuresis. The use of hemodialysis is ineffective to remove losartan or its active metabolite from the body.
special instructions
The side effects of Losartan-Richter are usually transient and do not require discontinuation of the drug.
Treatment with the drug is recommended to begin after the restoration of the water-electrolyte balance and to be accompanied by regular monitoring of the level of potassium in the blood serum. With a reduced BCC (including patients taking high doses of diuretics), therapy should be started with a low dose of Losartan-Richter.
Consideration should be given to the effect of Losartan-Richter on the RAAS (renin-aldosterone-angiotensin system), which in patients with severe CHF or a history of renal dysfunction may worsen the functional state of the kidneys, in patients with bilateral renal artery stenosis or stenosis of an artery of a single kidney, increase the concentration of residual nitrogen or creatinine in blood plasma.
With severe renal failure or in patients after kidney transplantation while taking Losartan-Richter, the risk of anemia increases. The treatment of such patients requires special attention.
The lactose content in tablets with a dosage of 50 mg is 1.05 mg, with a dosage of 100 mg - 2.1 mg.
Influence on the ability to drive vehicles and complex mechanisms
There is no information about the effect of Losartan-Richter on the patient's ability to drive vehicles or other complex mechanisms.
Application during pregnancy and lactation
The use of Losartan-Richter is contraindicated during gestation and lactation.
In case of conception during therapy, the drug should be discontinued immediately.
Pediatric use
The efficacy and safety of Losartan-Richter in children has not been established, therefore its use is contraindicated under the age of 18 years.
With impaired renal function
It is recommended to exercise caution when prescribing Losartan-Richter to patients with renal insufficiency (including bilateral renal artery stenosis, stenosis of an artery of a single kidney).
No dose adjustment is required (including in patients on hemodialysis).
For violations of liver function
Use Losartan-Richter with hepatic failure with caution. In case of arterial hypertension, it is recommended to use lower doses of the drug.
Use in the elderly
The use of Losartan-Richter in elderly patients requires concomitant monitoring of serum potassium levels; dose adjustment is not required.
Drug interactions
- diuretics, beta-blockers, sympatholytics: taking other antihypertensive drugs contributes to the mutual enhancement of the effect;
- hydrochlorothiazide, digoxin, phenobarbital, ketoconazole, erythromycin, warfarin, cimetidine: no pharmacokinetic interactions have been established against the background of concomitant therapy with each of these agents;
- rifampicin, fluconazole: reduce the level of the active metabolite of losartan in blood plasma, but the clinical consequences of this interaction are unknown;
- spironolactone, amiloride, triamterene and other potassium-sparing diuretics, potassium and potassium-containing salts preparations: the combination with these agents leads to an increased risk of hyperkalemia;
- acetylsalicylic acid (in a daily dose of more than 3 g), selective inhibitors of COX-2 (cyclooxygenase-2) and other nonsteroidal anti-inflammatory drugs (NSAIDs): it should be borne in mind that taking NSAIDs can reduce the effectiveness of losartan, cause reversible renal dysfunction, including acute renal insufficiency, and an increase in the level of potassium in the blood plasma (more often with reduced renal function);
- lithium preparations: a careful assessment of the benefits and risks is required if it is necessary to jointly prescribe lithium salts due to the increased risk of an increase in their content in blood plasma. With joint therapy, it is recommended to carefully monitor the concentration of lithium in the blood plasma.
Analogs
Losartan-Richter analogues are Losartan, Losartan Canon, Losartan McLeodz, Losartan-TAD, Losartan-Teva, Agilosartan, Zisakar, Cardomin-Sanvel, Blocktran, Vasotenz, Karzartan, Kozaar, Lorista, Losakor, Prezaparte, Lozaparte, Lozarelan …
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lozartan-Richter
A few reviews of Losartan-Richter describe the effective use of the drug in elderly patients for a systemic decrease in blood pressure, as a substitute for a combination of diuretic and antihypertensive drugs. At the same time, it is recommended to start taking with the minimum therapeutic dose, which can provide a completely satisfactory result. It is also advised to take into account that, in comparison with analogues with the same active ingredient, the auxiliary composition of Losartan-Richter does not contain povidone, which is intended to soften the effect of the active substance, which enhances the effect of this drug at equal dosages with similar drugs.
The price of Lozartan-Richter in pharmacies
For a package containing 30 tablets, the price of Losartan-Richter 50 mg can be from 161 rubles, 100 mg - from 216 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
