Bloktran, pills 50mg, 60pcs

Composition

1 coated tablet contains:

Active ingredient:

potassium losartan 50 mg

excipients:

• core: milk sugar (lactose), microcrystalline cellulose, low molecular weight polyvinylpyrrolidone (povidone), potato starch, magnesium stearate for the pharmaceutical industry, aerosil (colloidal silicon dioxide).
• shell: gilroxypropylmethylcellulose (hypromellose), copolividone, titanium dioxide, talc, twin-80 (polysorbate), sycovite yellow-orange 85 E 110.

Pharmacological action

Pharmacodynamics

Blocktran is an antihypertensive drug that is a specific angiotensin II receptor antagonist (ATI subtype). He inhibits kinase II, an enzyme that destroys bradykinin. Reduces total peripheral vascular resistance (OPSS), blood concentrations of epinephrine and aldosterone, blood pressure( BP), pressure in the small circle of blood circulation; reduces afterload, has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with heart failure. After a single dose, the antihypertensive effect (systolic and diastolic blood pressure decreases) reaches a maximum in 6 hours, then gradually decreases over 24 hours.

The maximum antihypertensive effect is achieved 3-6 weeks after the start of taking the drug.

Pharmacological data indicate that the concentration of losartan in the blood plasma in patients with cirrhosis of the liver is significantly increased, so patients with a history of liver disease should use the drug at a lower dose.

Pharmacokinetics

Losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. It has a “first pass” effect through the liver, is metabolized by carboxylation with the participation of cytochrome P450 isoenzyme 2C9 to form an active metabolite. Binding to plasma proteins is 99%. The time to reach the maximum concentration of losartan is 1 hour, the active metabolite 3-4 hours, after oral use. The elimination half-life is 1.5-2 hours, and its main metabolite is 6-9 hours, respectively. About 35% of the dose is excreted in the urine, about 60% – through the intestines.

Indications

Arterial hypertension.

Reduced risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, resulting in a combined reduction in the incidence of cardiovascular mortality, stroke, and myocardial infarction.

Kidney protection in patients with type 2 diabetes mellitus with proteinuria — slowing the progression of renal failure, manifested by a decrease in the frequency of hypercreatininemia, the frequency of end-stage chronic renal failure requiring hemodialysis or kidney transplantation, mortality rates, and a decrease in proteinuria.

Chronic heart failure with ineffective treatment with ACE inhibitors or intolerance to ACE inhibitors. It is not recommended to transfer patients with heart failure and stable indicators when taking ACE inhibitors to therapy with Blocktran®

Use during pregnancy and lactation

It is contraindicated during pregnancy and lactation. The safety and efficacy of Blocktran in children has not been established.

Contraindications

• Arterial hypotension;
• Hyperkalemia;
• Dehydration;
• Pregnancy and lactation;
• Age up to 18 years (efficacy and safety have not been established for patients under 18 years of age).

With caution, hepatic and / or renal failure.

Side effects

* Side effects with a comparable frequency to placebo are marked. The association of side effects occurring with a frequency of less than 1% of cases with the use of losartan has not been proven. In most cases, Blocktran is well tolerated, side effects are transient and do not require discontinuation of the drug.

From the nervous system and sensory organs: 1% or more – dizziness, asthenia, headache, fatigue, insomnia; less than 1% – anxiety, sleep disorders, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hyposthesia, migraine, tremor, ataxia, depression, syncope, tinnitus, taste disorders, vision changes, conjunctivitis.

From the respiratory system: 1% or more – nasal congestion, cough*, upper respiratory tract infections (fever, sore throat, sinusopathy*, sinusitis, pharyngitis), less than 1% – dyspnoea, bronchitis, rhinitis.

From the gastrointestinal tract: 1% or more – nausea, diarrhea*, dyspeptic phenomena*, abdominal pain; less than 1% – anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.

From the musculoskeletal system: 1% or more – cramps, myalgia*, back pain, chest pain, leg pain; less than 1% – arthralgia, shoulder pain, knee pain, arthritis, fibromyalgia.

From the cardiovascular system: orthostatic hypotension (dose-dependent), palpitations, tachy – or bradycardia, arrhythmias, angina pectoris, anemia.

From the genitourinary system: less than 1% – imperative urination, urinary tract infections, impaired kidney function, decreased libido, impotence.

From the skin: less than 1% – dry skin, erythema, blood rush, photosensitization, increased sweating, alopecia.

Allergic reactions: less than 1% – urticaria, rash, pruritus, angioedema, including face, lips, pharynx and / or tongue.

Other: hyperkalemia (serum potassium greater than 5.5 mmol / l).

Interaction

It can be prescribed with other antihypertensive agents.

There were no clinically significant interactions with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, and phenobarbital.

Patients with dehydration (previous treatment with high doses of diuretics) may experience a marked decrease in blood pressure.

Increases (mutually) the effect of other antihypertensive agents (diuretics, beta-blockers, sympatholytics).

Increases the risk of hyperkalemia when combined with potassium-sparing diuretics and potassium preparations.

How to take, course of use and dosage

The drug Bloktran is taken orally, regardless of food intake, the frequency of use is 1 time a day.

With arterial hypertension, the average daily dose is 50 mg. In some cases, to achieve a greater effect, the dose is increased to 100 mg in two doses or once a day.

The initial dose for patients with heart failure is 12.5 mg once a day. As a rule, the dose is titrated at weekly intervals (i. e. 12.5 mg / day,25 mg / day and 50 mg / day ) up to an average maintenance dose of 50 mg once a day, depending on the patient’s tolerance to the drug.

When prescribing the drug to patients receiving high-dose diuretics, the initial dose should be reduced to 25 mg once a day.

No dose adjustment is required in elderly patients or patients with impaired renal function, including patients on hemodialysis.

Patients with impaired liver function should be prescribed lower doses of the drug.

Overdose

Symptoms: marked decrease in blood pressure, tachycardia, due to parasympathetic (vagal) stimulation, bradycardia may appear. Treatment: forced diuresis, symptomatic therapy; hemodialysis is ineffective.

Special instructions

It is necessary to correct dehydration before prescribing Blocktran or start treatment with a lower dose of the drug. Drugs that affect the renin-angiotensin system may increase the concentration of urea in the blood and serum creatinine in patients with bilateral renal stenosis or stenosis of the artery of a single kidney.

During treatment, the concentration of potassium in the blood should be regularly monitored, especially in elderly patients with impaired renal function.

Form of production

Bloktran tablets.

Storage conditions

In a dry place, at a temperature not exceeding 30 °C

Shelf

life is 2 years. Do not use after the expiration date.

Active ingredient

Losartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Heart Failure