Expiration date: 01/2025
Release form and composition:
Tablets, film-coated light pink-orange, round, lenticular.
1 tablet contains:
losartan potassium 50 mg
Excipients: lactose, cellulose microcrystalline, povidone (polyvinylpyrrolidone low molecular weight), potato starch, magnesium stearate, silicon dioxide colloidal (Aerosil).
The shell: polymer (hydroxypropyl methylcellulose), copovidone (copolyvidone), titanium dioxide, talc, Polysorbate-80 (tween-80), sikovit yellow-orange 85 (E110).
10 PCs. - packaging sells contoured (1) - packs of cardboard.
10 PCs. - packaging sells contoured (2) - packs of cardboard.
10 PCs. - packaging sells contoured (3) - packs cardboard.
10 PCs. - packaging sells contoured (5) - packs of cardboard.
10 PCs. - packaging sells contoured (6) - packs cardboard.
Pharmacological action:
Antihypertensive drug. Specific receptor antagonist angiotenzina II (subtype AT1). He inhibits kinase II enzyme that destroys bradykinin. Reduces PR, blood concentration of adrenaline and aldosterone, HELL, pressure in the pulmonary circulation. Reduces afterload, has a diuretic effect. Prevents the development of myocardial hypertrophy, increases tolerance to physical load in patients with heart failure.
After receiving a single antihypertensive effect (reduction in systolic and diastolic BP) reaches a maximum after 6 h, then for 24 h gradually decreases.
Maximum antihypertensive effect is achieved 3 to 6 weeks after starting this drug.
Pharmacokinetics:
Suction
Losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. The Tmax of losartan is reached after 1 h.
Metabolism
Undergoes first pass effect through the liver, metabolised by carboxylation with the participation of isoenzyme CYP2C9 with the formation of active metabolite. The Tmax of the active metabolite is achieved through 3-4 h. Linking blood plasma proteins - 99%.
Excretion
T1/2 of losartan is 1.5-2 h, and its main metabolite is 6-9 h. About 35% of the dose is excreted in the urine, about 60% - through the intestines.
Pharmacokinetics in special clinical cases
Concentrations of losartan in plasma in patients with cirrhosis of the liver significantly increases, therefore, patients with diseases of the liver disease should use the drug at a lower dose.
Indications:
— arterial hypertension
— chronic heart failure (in combination therapy, intolerance or failure of therapy with ACE inhibitors).
Dosing regimen:
The drug is taken orally regardless of the meal, the multiplicity of reception - 1 time/day.
When hypertension average daily dose is 50 mg. In some cases, to maximize the effect, increase the dose to 100 mg in 2 divided doses or 1 times/day.
Starting dose for patients with heart failure is 12.5 mg 1 times/day. As a rule, the dose increases with weekly intervals (i.e. 12.5 mg/day 25 mg/day and 50 mg/day) to the average maintenance dose 50 mg 1 times/day depending on tolerability by the patient.
In appointing the drug patients, receiving diuretics in high doses, the initial dose should be reduced to 25 mg 1 times/day.
Concentrations of losartan in plasma in patients with cirrhosis of the liver significantly increases, therefore, patients with diseases of the liver disease should use the drug at a lower dose.
In elderly patients, and patients with impaired renal function, including patients on hemodialysis, is not necessary initial dose adjustment.
The safety and efficacy of the drug in children have not been established.
Side effects:
CNS and peripheral nervous system: ge1% - dizziness, asthenia, headache, fatigue, insomnia t1% - anxiety, insomnia, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypoesthesia, migraine, tremor, ataxia, depression, syncope.
From the sensory organs: ge1% - tinnitus, taste disturbance, vision changes, conjunctivitis.
The respiratory system: ge1% - nasal congestion, cough*, upper respiratory tract infection (fever, sore throat, cinespace*, sinusitis, pharyngitis) t1% - dyspnea, bronchitis, rhinitis.
From the digestive system: ge1% - nausea, diarrhea*, dyspepsia symptoms* abdominal pain e1% - anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.
From the side of musculoskeletal system: ge1% - cramps, myalgia*, back pain, chest, legs e1% arthralgia, pain in the shoulder, knee, arthritis, fibromyalgia.
Of the cardiovascular system: orthostatic hypotension (dose related), palpitation, Tahi - or bradycardia, arrhythmia, angina.
With the genitourinary system: t1% - urgent need to urinate, urinary tract infections, kidney dysfunction, reduced libido, impotence.
Dermatological reactions: t1% - dry skin, erythema, flushing, photosensitivity, increased sweating, alopecia.
Allergic reactions: t1% - urticaria, rash, itching, angioneurotic edema (including face, lips, pharynx and/or tongue).
Other: hyperkalemia (serum potassium more than 5.5 mmol/l), anemia.
* - side effects, the incidence of which is comparable to placebo.
Communication of side effects occurring with a frequency t1% of cases, with the use of losartan is not proven.
In most cases Bloctran® is well tolerated, side effects are transient in nature and do not require discontinuation of the drug.
Contraindications:
— hypotension
— hyperkalemia
— dehydration
— pregnancy
— lactation (breast-feeding)
— the age 18 years (effectiveness and safety have not been established)
— hypersensitivity to the drug.
With caution should designate product in the hepatic and/or renal failure.
Pregnancy and lactation:
Data on the use of losartan during pregnancy not. However, it is known that drugs that act directly on the renin-angiotensin system, when you apply them in II and III trimestrah pregnancy can cause a defect of development or even death of the developing fetus. Therefore, in the event of pregnancy received Bloctran should cease immediately.
In appointing lactation should decide on the termination of breastfeeding or discontinuing treatment Blockrandom.
Special instructions:
It is necessary to carry out the correction of dehydration before the appointment Bloctran or to begin treatment with the drug at a lower dose.
Drugs that affect the renin-angiotensin system, can increase the concentration of blood urea and serum creatinine in patients with bilateral renal stenosis or stenosis of the artery to a solitary kidney.
During treatment should regularly monitor the concentration of potassium in the blood, especially in elderly patients when impaired renal function.
Overdose:
Symptoms: expressed lower AD, tachycardia due to parasympathetic (vagal) stimulation may occur bradycardia.
Treatment: forced diuresis, symptomatic therapy, hemodialysis is ineffective.
Drug interactions:
The drug may be administered in combination with other antihypertensive agents. However, note that Bloctran® do (mutually) effect of other antihypertensive drugs (including diuretics, beta-adrenoblokatorov, simpatolitikov).
Not clinically significant interactions with hydrochlorothiazide, digoxin, indirect antikoagulyantami, cimetidine, phenobarbital.
In patients with dehydration (previous treatment dioretikami in high doses) may be expressed lower AD.
In a joint application with kalisberegatmi dioretikami drugs and potassium increase the risk giperkaliemii.
Terms and conditions of storage:
List B. the Drug should be stored in a dry, inaccessible for children place at temperature not exceeding 30°C. shelf Life - 2 years.
