RIZORTA [Losartan] 100 mg Film-coated tablets
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RIZORTA
instructions for medical use of the medicinal product
Tradename
Rizorta,
International non-proprietary name
Losartan , Losartan
Composition
Risorta 25 mg
Each film-coated tablet contains:
active substance: l ozartan potassium USP 25 mg
excipients: pregelatinized starch, sugar powder, microcrystalline cellulose, hypromellose, CCNa, CMS-Na, magnesium stearate.
Risorta 50 mg
Each film-coated tablet contains:
active substance: l ozartan potassium USP 50 mg
pregelatinized starch, sugar powder, microcrystalline cellulose, hypromellose, CCNa, CMS-Na, magnesium stearate.
Rizort 100 mg
Each film-coated tablet contains:
active substance: l ozartan potassium USP 100 mg
excipients: pregelatinized starch, sugar powder, microcrystalline cellulose, hypromellose, CCNa, CMS-Na, magnesium stearate.
Dosage form
Tablets.
Pharmacotherapeutic group
Drugs affecting the renin-angiotensin system. Angiotensin II antagonists.
Pharmacological properties
Rizort is an antihypertensive agent. The active substance is losartan.
Pharmacodynamics
Losartan belongs to a group of medicines known as angiotensin II receptor antagonists. Angiotensin II is a substance produced in the body that binds to receptors in blood vessels, causing them to constrict. This leads to an increase in blood pressure. Losartan prevents angiotensin-II from binding to these receptors, causing blood vessels to relax, which in turn lowers blood pressure. Losartan slows down the decline in kidney function in patients with high blood pressure and type 2 diabetes.
Pharmacokinetics
After oral administration, losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. It is metabolized during the "first pass" through the liver with the formation of a carboxyl metabolite, which has a more pronounced pharmacological activity than losartan, and a number of inactive metabolites. C max in blood plasma of losartan and the active metabolite is reached after 1 hour and 3-4 hours, respectively. Plasma protein binding of losartan and the active metabolite is high - more than 98%.
T 1/2 of losartan and the active metabolite in the final phase is about 1.5-2.5 hours and 3-9 hours, respectively. Losartan is excreted in the urine and feces (with bile) unchanged and as metabolites. About 35% is excreted in the urine and about 60% in the feces.
Indications for use
• treatment of essential hypertension;
• treatment of kidney disease in adult patients with arterial hypertension and type 2 diabetes mellitus with proteinuria ≥ 0.5 g/day - as part of antihypertensive therapy;
• reduced risk of stroke in adult patients with arterial hypertension and left ventricular hypertrophy confirmed by ECG;
• chronic heart failure (as part of combination therapy, with intolerance or ineffectiveness of therapy with ACE inhibitors).
Contraindications
• hypersensitivity to losartan;
• severe liver dysfunction;
• severe renal dysfunction (CC less than 30 ml / min);
• refractory hyponatremia;
• refractory hypokalemia or hypercalcemia;
• simultaneous use with drugs containing aliskiren , in patients with diabetes mellitus and patients with moderate and severe renal insufficiency (GFR less than 60 ml / min / 1.73 m2 of body surface area);
• pregnancy and breastfeeding period;
• children's and adolescence up to 18.
Dosage and administration
Inside, regardless of the meal, the frequency of admission - 1 time per day. The tablets are swallowed whole, without chewing, with water.
Arterial hypertension
In arterial hypertension, the standard initial and maintenance dose for most patients is 50 mg 1 time per day. To achieve a greater therapeutic effect, the dose is increased to a maximum daily dose of 100 mg 1 time per day.
Chronic heart failure
The initial dose for patients with chronic heart failure is 12.5 mg 1 time per day. As a rule, the dose is increased at weekly intervals (i.e. 12.5 mg/day, 25 mg/day and 50 mg/day) to an average maintenance dose of 50 mg 1 time per day, depending on the tolerability of the drug by the patient.
Reducing the risk of cardiovascular disease (including stroke) and mortality in patients with arterial hypertension and left ventricular hypertrophy
The initial dose of the drug is 50 mg 1 time per day. In the future, low-dose hydrochlorothiazide can be added or the dose of the drug can be increased to 100 mg in one or two doses, taking into account the reduction in blood pressure.
Renal protection in patients with type 2 diabetes mellitus and proteinuria
Assign an initial dose of 50 mg 1 time per day with a further increase in dose to 100 mg / day (taking into account the degree of reduction in blood pressure) in one or two divided doses.
Special patient groups:
In patients with a reduced volume of circulating blood (for example, when taking diuretics in high doses), the recommended initial dose is 25 mg 1 time per day.
Patients with renal insufficiency and patients on dialysis
There is no need to select the initial dose in patients with renal insufficiency, including patients on dialysis.
Elderly patients
There is no need for dose adjustment in elderly patients, although it is recommended to start treatment with a dose of 25 mg in patients over 75 years of age.
Patients with liver failure
Patients with a history of liver disease are advised to prescribe the drug at lower doses. Contraindicated for use in patients with severe hepatic impairment.
Special instructions and precautions
Use with caution in: arterial hypotension; reduced volume of circulating blood; violation of water and electrolyte balance; bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; renal failure; hyperkalemia; hypertrophic obstructive cardiomyopathy; heart failure with life-threatening arrhythmias; heart failure with concomitant severe renal dysfunction; ischemic heart disease; cerebrovascular diseases; primary hyperaldosteronism; angioedema in history.
Influence on the ability to drive vehicles and mechanisms
It should be borne in mind that against the background of treatment with antihypertensive drugs when driving or working with mechanisms, dizziness or drowsiness may occur, especially at the beginning of treatment or when the dosage of the drug is increased.
Use during pregnancy or lactation
Use during pregnancy and during breastfeeding is contraindicated. If you need to take the drug during lactation, then breastfeeding should be stopped.
Interaction with other drugs
With simultaneous use with diuretics in high doses, arterial hypotension is possible.
With simultaneous use with potassium preparations, potassium-sparing diuretics, the risk of developing hyperkalemia increases.
With simultaneous use with indomethacin, a decrease in the effectiveness of losartan is possible.
There is a report on the development of lithium intoxication with simultaneous use with lithium carbonate.
With simultaneous use with orlistat, the antihypertensive effect of losartan decreases, which can lead to a significant increase in blood pressure, the development of a hypertensive crisis.
With simultaneous use with rifampicin, the clearance of losartan increases and its effectiveness decreases.
Side effect
In most cases, losartan is well tolerated, side effects are mild and transient and do not require discontinuation of the drug. Side effects observed when taking the drug are classified into categories depending on the frequency of their occurrence: very often > 1/10 (10%); often > 1/100 (1%) < 1/10 (10%); sometimes > 1/1000 (0.1%), < 1/100 (1%): rarely > 1/10000 (0.01%), < 1/1000 (0.1%); very rarely < 1/10000 (0.01%), including isolated events.
Side effects occurring with a frequency of more than 1%
General disorders: asthenia, weakness, fatigue, chest pain, peripheral edema.
From the side of the cardiovascular system: palpitations, tachycardia.
From the digestive system: abdominal pain, diarrhea, dyspepsia, nausea.
From the musculoskeletal system: pain in the back, legs, muscle cramps.
From the side of the central nervous system: dizziness, headache, insomnia.
From the respiratory system: cough, bronchitis, swelling of the nasal mucosa, pharyngitis, sinusitis, infections of the upper respiratory tract.
Side effects occurring with a frequency of less than 1%.
Since the cardiovascular system: angina pectoris, symptomatic arterial hypotension (especially in patients with intravascular dehydration, for example, patients with severe heart failure or when taking diuretics in high doses), dose-dependent orthostatic hypotension, bradycardia, arrhythmias, myocardial infarction, vasculitis.
From the digestive system: anorexia, dryness of the oral mucosa, toothache, flatulence, gastritis, constipation, hepatitis, liver dysfunction, vomiting.
On the part of the skin: dry skin, ecchymosis, erythema, photosensitivity, increased sweating, alopecia.
Allergic reactions: urticaria, itching, skin rash, angioedema (including swelling of the larynx, vocal cord, causing airway obstruction, and / or swelling of the face, lips, pharynx and / or tongue).
On the part of the hematopoietic system: anemia, thrombocytopenia, eosinophilia, Shenlein-Genoch purpura.
From the nervous system and sensory organs: anxiety, sleep disturbance, drowsiness, memory impairment, peripheral neuropathy, paresthesia, hypoesthesia. tremor, ataxia, depression, syncope, tinnitus, taste disturbance, visual impairment, conjunctivitis, migraine.
From the musculoskeletal system: arthralgia, arthritis, shoulder and knee pain, fibromyalgia.
From the urinary system: imperative urge to urinate, urinary tract infections, impaired renal function.
From the reproductive system: decreased libido, impotence.
Others: exacerbation of the course of gout, nosebleeds.
On the part of laboratory parameters: often - hyperkalemia (potassium content more than 5.5 mmol / l); infrequently - an increase in the concentration of urea, residual nitrogen, creatinine in the blood serum; very rarely - a moderate increase in the activity of grapsaminases (aspartate aminotransferase, alanine aminotransferase), hyperbilirubinemia.
Attention! 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.
Symptoms: pronounced decrease in blood pressure, tachycardia, bradycardia.
Treatment: forced diuresis, symptomatic therapy. With the help of hemodialysis, losartan and its active metabolite are not removed from the bloodstream.
Storage conditions
Store in a cool and dry place at temperature