Bloctran, 50 mg 60 pcs.

Pharmacodynamics

Blocktran is a hypotensive drug and is a specific angiotensin II receptor antagonist (ATI subtype). It inhibits kinase II, an enzyme that degrades bradykinin. Reduces total peripheral vascular resistance (TPR), blood concentrations of adrenaline and aldosterone, blood pressure (BP), pressure in the small circle of the circulation; reduces post-load, has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with heart failure. After a single dose, the hypotensive effect (systolic and diastolic BP decreases) reaches its maximum after 6 hours and then gradually decreases within 24 hours.

The maximum hypotensive effect is reached 3-6 weeks after the start of the drug.

Pharmacologic data indicate that plasma concentrations of losartan are significantly increased in patients with cirrhosis, so patients with a history of liver disease should use the drug in a lower dose.

Pharmacokinetics

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

Indications

Arterial hypertension.

Reduced risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a cumulative 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 incidence of hypercreatininemia, the incidence of end-stage chronic renal failure requiring hemodialysis or kidney transplantation, mortality rates, as well as 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 while taking ACE inhibitors to therapy with Blocktran®

Pharmacological effect

Pharmacodynamics

Bloktran is an antihypertensive drug that is a specific antagonist of angiotensin II receptors (ATI subtype). Does not inhibit kinase II, an enzyme that destroys bradykinin. Reduces total peripheral vascular resistance (TPVR), blood concentrations of adrenaline and aldosterone, blood pressure (BP), pressure in the pulmonary circulation; reduces afterload and has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with heart failure. After a single dose, the hypotensive effect (systolic and diastolic blood pressure decreases) reaches a maximum after 6 hours, then gradually decreases over 24 hours.

The maximum hypotensive effect is achieved 3-6 weeks after starting the drug.

Pharmacological data indicate that the concentration of losartan in the blood plasma in patients with cirrhosis of the liver increases significantly, 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 – about 33%. It has a “first pass” effect through the liver, is metabolized by carboxylation with the participation of the 2C9 isoenzyme of cytochrome P450 to form an active metabolite. Communication with blood plasma proteins – 99%. The time to reach the maximum concentration of losartan is 1 hour, the active metabolite is 3-4 hours, after oral administration. The 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.

Special instructions

It is necessary to correct dehydration before prescribing Bloktran or begin treatment with the drug at a lower dose. Drugs that affect the renin-angiotensin system may increase blood urea and serum creatinine concentrations in patients with bilateral renal stenosis or arterial stenosis of a solitary kidney.

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

Active ingredient

Losartan

Composition

1 film-coated tablet contains:

active ingredient:

losartan potassium 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: gilroxypropyl methylcellulose (hypromellose), copolyvidone, titanium dioxide, talc, Tween-80 (polysorbate), yellow-orange sikovit 85 E110.

Pregnancy

Contraindicated during pregnancy and breastfeeding. The safety and effectiveness of Bloktran 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).

Be careful with liver and/or renal failure.

Side Effects

* Side effects are marked, the incidence of which is comparable to placebo.
The association of side effects occurring in less than 1% of cases with the use of losartan has not been proven.
In most cases, Bloktran 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 disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypoesthesia, migraine, tremor, ataxia, depression, syncope, tinnitus, taste disturbance, 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% – dyspnea, bronchitis, rhinitis.

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

From the musculoskeletal system: 1% or more – convulsions, myalgia*, pain in the back, chest, legs; less than 1% – arthralgia, pain in the shoulder, knee, 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 urge to urinate, urinary tract infections, impaired renal function, weakened libido, impotence.

From the skin: less than 1% – dry skin, erythema, flushing, photosensitivity, increased sweating, alopecia.

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

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

Interaction

May be prescribed with other antihypertensive drugs.

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

In patients with dehydration (previous treatment with large doses of diuretics), a pronounced decrease in blood pressure may occur.

Strengthens (mutually) the effect of other antihypertensive drugs (diuretics, beta-blockers, sympatholytics).

Increases the risk of hyperkalemia when used together with potassium-sparing diuretics and potassium supplements.

Overdose

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

Storage conditions

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

Shelf life

3 years. Do not use after expiration date.

Manufacturer

Pharmstandard-Leksredstva, Russia