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.

Recrease risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a combined reduction in cardiovascular mortality, stroke rate and myocardial infarction.

Kidney protection in patients with type 2 diabetes mellitus with proteinuria – slowing the progression of renal failure, manifested by decreased incidence of hypercreatininemia, frequency of development of end-stage chronic renal failure requiring hemodialysis or renal transplantation, mortality rates, and decreased 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 values while taking ACE inhibitors to therapy with Bloctran®.

Active ingredient

Composition

1 film-coated tablet contains:

the active ingredient:

potassium losartan 50 mg

auxiliary substances:

How to take, the dosage

The drug Bloktran is taken orally, regardless of meals, the frequency of intake is once a day.

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

The starting dose for patients with heart failure is 12.5 mg once daily. Typically, the dose is titrated at weekly intervals (i.e., 12.5 mg/day, 25 mg/day, and 50 mg/day ) to an average maintenance dose of 50 mg once daily, depending on patient tolerance.

When the drug is administered to patients receiving high-dose diuretics, the starting dose should be reduced to 25 mg once daily.

There is no need to adjust the dose 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.

Interaction

Can be administered with other hypotensive agents.

No clinically significant interaction with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital has been noted.

In patients with dehydration (previous treatment with high doses of diuretics) a significant decrease of BP may occur.

It potentiates (mutually) the effect of other hypotensive agents (diuretics, beta-adrenoblockers, sympatholytics).

Induces risk of hyperkalemia when combined with potassium-saving diuretics and potassium preparations.

Special Instructions

Correction of dehydration should be performed before prescribing Bloctran or treatment should be started with a lower dose of the drug. Drugs affecting the renin-angiotensin system may increase blood urea and serum creatinine concentrations in patients with bilateral renal stenosis or arterial stenosis of the single kidney.

The blood potassium concentration should be monitored regularly during treatment, especially in elderly patients with impaired renal function.

Contraindications

With caution hepatic and/or renal failure.

Side effects

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

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

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

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

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

Cardiovascular system: orthostatic hypotension (dose-dependent), palpitation, tachy or bradycardia, arrhythmias, angina pectoris, anemia.

Urogenital system disorders: less than 1% – imperative urge to urinate, urinary tract infections, impaired renal function, impaired libido, impotence.

Skin disorders: less than 1% – dry skin, erythema, flushing, photosensitization, increased sweating, alopecia.

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

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

Overdose

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

Pregnancy use

It is contraindicated in pregnancy and lactation. Safety and effectiveness of the drug Bloktran in children has not been established.

Similarities