Brief information about the drug
The drug for high blood pressure Bloktran belongs to the pharmacological group of angiotensin 2 receptor antagonist drugs. It is produced in Russia.
Release form
The blood pressure medicine Blocktran is presented on the pharmaceutical market in a convenient tablet form. The manufacturer produces tablets packaged in blisters of 10 pieces. You can purchase either 1 blister or a box containing 2, 3, 5 or 6 blisters.
Packaging of Blocktran tablets
Composition of tablets
The main active component of the drug is potassium losartan, presented in a dose of 12.5 mg or 50 mg.
The composition of the tablets also includes additional ingredients: starch, sodium carboxymethyl starch, magnesium stearate, lactose monohydrate, povidone, silicon dioxide, microcrystalline cellulose.
Terms and conditions of storage
The tablets should be stored in a place inaccessible to children and pets, protected from moisture and direct sunlight. The recommended storage temperature should not exceed +30°C.
The maximum shelf life of the drug is 2 years.
Terms of sale
It is possible to purchase medication in pharmacy chains only after presenting an appropriate medical prescription.
Price
The cost of the drug is influenced by factors such as the dosage of the main active ingredient and the number of tablets in the package. The approximate price for Blocktran varies from 150 rubles to 400 rubles.
Pharmacological characteristics
The drug Bloktran has a pronounced antihypertensive pharmacological effect.
Release form and composition
- film-coated tablets, 12.5 mg;
- film-coated tablets, 50 mg: round, convex on both sides, light pinkish-orange in color.
Packing of tablets: 10 pcs. in blister packs, in a cardboard pack of 1, 2, 3, 5 or 6 packs.
Composition of tablets:
- active substance: losartan potassium – 12.5 or 50 mg;
- auxiliary components (kernel composition): potato starch, microcrystalline cellulose, lactose monohydrate, aerosil (colloidal silicon dioxide), magnesium stearate, low molecular weight polyvinylpyrrolidone (povidone), sodium carboxymethyl starch (sodium starch glycolate);
- shell composition: copolyvidone, hydroxypropyl methylcellulose (hypromellose), Tween-80 (polysorbate-80), talc, titanium dioxide E171, water-soluble sunset yellow dye E110 (sykovit yellow-orange 85 and Indacol sunset yellow).
Pharmacodynamics - increases or decreases blood pressure
Blood pressure tablets Blocktran suppress specific angiotensin receptors localized in the area of blood vessels, adrenal glands, heart and kidney apparatus.
Blocktran lowers blood pressure. Since the drug has a cumulative effect, the hypotensive effect becomes most noticeable after a month of the therapeutic course.
Bloktran is effective when used as a course
Increases renin levels in the blood without negatively affecting the production and functioning of other hormones responsible for the normal functioning of the cardiovascular system, which avoids a number of side effects characteristic of most antihypertensive drugs.
Helps increase life expectancy in patients suffering from cardiac ventricular hypertrophy and hypertension.
Pharmacokinetics of the drug
Blocktran reduces blood pressure 6 hours after taking the tablets. The therapeutic effect lasts throughout the day, avoiding the need for frequent medication use. The maximum concentration of the active substances of the drug in the blood is observed after 3-4 hours.
The medicine is eliminated from the body within 9 hours, through the gastrointestinal tract (60%), another 35% of the medicine is excreted through the renal apparatus, along with urine.
Bloktran GT
The components of the drug Bloktran® GT have an additive antihypertensive effect, reducing blood pressure (BP) to a greater extent than each of the components separately. Due to the diuretic effect, hydrochlorothiazide increases plasma renin activity (PRA), stimulates the secretion of aldosterone, increases the concentration of agiotensin II and reduces the potassium content in the blood serum. Taking losartan blocks all physiological effects of agiotensin II and, due to the suppression of the effects of aldosterone, may help reduce potassium loss associated with diuretic use.
Hydrochlorohiazide causes a slight increase in the concentration of uric acid in the blood plasma, losartan has a moderate and transient uricosuric effect. The combination of losartan and hydrochlorothiazide helps reduce the severity of diuretic-induced hyperuricemia.
Losartan
Angiotensin II is a powerful vasoconstrictor, the main active hormone of the renin-angiotensin-aldosterone system, as well as a decisive pathophysiological link in the development of arterial hypertension. Losartan is an antagonist of agiotensin II receptors (type AT1). Angiotensin II binds selectively to AT1 receptors found in many tissues (vascular smooth muscle, adrenal glands, kidneys and heart) and performs several important biological functions, including vasoconstriction and aldosterone release. Angiotensin II also stimulates the proliferation of smooth muscle cells. Losartan and its pharmacologically active metabolite (E 3174) both in vitro and in vivo block all physiological effects of agiotensin II, regardless of the source or route of synthesis.
Losartan does not bind to or block the receptors of other hormones and ion channels that play an important role in regulating the function of the cardiovascular system. In addition, losartan does not inhibit angiotensin-converting enzyme (ACE), which is responsible for the destruction of bradykinin. Therefore, side effects indirectly associated with bradykinin (for example, angioedema) occur quite rarely. When using losartan, the lack of negative feedback influence on renin secretion leads to an increase in ARP. An increase in ARP leads to an increase in angiotensin II in the blood plasma. However, antihypertensive activity and a decrease in plasma aldosterone concentrations persist, indicating effective blockade of angiogensin II receptors. Losartan and its active metabolite have a greater affinity for angiogensin I receptors than for angiogensin II receptors. The active metabolite is 10-40 times more active than losartan. After a single oral dose, the antihypertensive effect reaches a maximum after 6 hours, then gradually decreases over 24 hours. The maximum antihypertensive effect develops 3-6 weeks after starting the drug. The antihypertensive effect increases with increasing dose of losartan.
Losartan does not affect autonomic reflexes and does not have a long-term effect on the concentration of norepinephrine in the blood plasma.
In patients with arterial hypertension and left ventricular hypertrophy, losartan, including in combination with hydrochlorothiazide, reduces the risk of cardiovascular morbidity and mortality.
Hydrochlorothiazide
The mechanism of the antihypertensive effect of thiazide diuretics is unknown. Thiazide diuretics usually have no effect on normal blood pressure. Hydrochlorothiazide is a diuretic and antihypertensive agent. It affects the reabsorption of electrolytes in the distal tubules of the kidneys. Hydrochlorothiazide increases the excretion of sodium and chlorine ions to approximately the same extent. Natriuresis may be accompanied by a slight loss of potassium ions, bicarbonates and retention of calcium ions in the body. When taken orally, the diuretic effect begins after 2 hours, reaches a maximum after an average of 4 hours and lasts from 6 to 12 hours.
Pharmacokinetics
The pharmacokinetics of losartan and gpdrochlorothiazide when administered simultaneously do not differ from those when administered separately.
Suction
Losartan
When taken orally, losartan is well absorbed from the gastrointestinal tract and undergoes first-pass metabolism through the liver, resulting in the formation of an active carboxylated metabolite and inactive metabolites involving the CYP2C9 isoenzyme. The systemic bioavailability of losartan is approximately 33%. Cmax of losartan and its active metabolite is achieved after 1 hour and after 3-4 hours, respectively. When losartan was taken with a normal meal, there was no clinically significant effect on the plasma concentration profile of losartan.
Hydrochlorothiazide
When taken orally, hydrochlorothiazide is rapidly absorbed from the gastrointestinal tract. The time to reach maximum concentration is 1.5-3 hours.
Distribution
Losartan
Losartan and its active metabolite are more than 99% bound to plasma proteins (mainly albumin). The volume of distribution of losartan is 34 liters. Studies in rats have shown that losartan practically does not penetrate the blood-brain barrier.
Hydrochlorothiazide
Hydrochlorothiazide binds to plasma proteins by 40-60%, penetrates the placental barrier, does not penetrate the blood-brain barrier, and is secreted into breast milk.
Metabolism
Losartan
Approximately 14% of a dose of losartan administered intravenously or orally is converted into its active metabolite. After oral or intravenous administration of losartan. labeled with 14C, the radioactivity of circulating blood plasma is primarily associated with the presence of losartan and its active metabolite. In addition to the active metabolite, biologically inactive metabolites are also formed, including two metabolites formed as a result of hydroxylation of the butyl side chain, and one minor one, N-2-tetrazole glucuronide.
Removal
Losartan
Plasma clearance of losartan and its active metabolite is about 600 ml/min and 50 ml/min, respectively. The renal clearance of losartan and its active metabolite is approximately 74 ml/min and 26 ml/min, respectively. When losartan is taken orally, about 4% of the dose is excreted unchanged by the kidneys and about 6% of the dose is excreted as an active metabolite. Losartan and its active metabolite exhibit linear pharmacokinetics when losartan potassium is taken orally in doses up to 200 mg. After oral administration, plasma concentrations of losartan and its active metabolite decrease polyexponentially with a final T1/2 of approximately 2 and 6-9 hours, respectively. With a single dose of 100 mg, neither losartan nor its active metabolite accumulates significantly in the blood plasma. Excretion of losartan and its metabolites occurs through the intestines and kidneys. After oral administration of 14C-labeled losartan, about 35% of the radioactive label is found in the urine and 58% in the feces. After intravenous administration of 14C-labeled losartan, approximately 43% of the radiolabel is detected in the urine and 50% in the feces.
Hydrochlorothiazide
Hydrochlorothiazide is not metabolized and is rapidly excreted by the kidneys. The half-life varies from 5.6 to 14.8 hours. At least 61% of the dose taken orally is excreted unchanged within 24 hours.
Pharmacokinetics in special groups of patients.
In patients with mild and moderate alcoholic cirrhosis of the liver, the concentration of losartan was 5 times higher, and the active metabolite was 1.7 times higher than in healthy volunteers ICB-MV gallstones.
When creatinine clearance (CC) is above 10 ml/min, the concentration of losartan in the blood plasma does not differ from that with normal renal function.
In patients on hemodialysis, the area under the concentration-time curve (AUC) is approximately 2 times higher than in patients with normal renal function.
Neither losartan nor its active metabolite is removed from the body by hemodialysis.
Plasma concentrations of losartan and its active metabolite in elderly patients with arterial hypertension do not differ significantly from the values of these parameters in young male patients with arterial hypertension.
The plasma concentrations of losartan in women with arterial hypertension are 2 times higher than the corresponding values in men with arterial hypertension. Concentrations of the active metabolite do not differ between men and women. This pharmacokinetic difference is not clinically significant.
Indications for use of Bloktran
Doctors strongly recommend that patients take Blocktran for high blood pressure in case of the following health problems:
- Arterial hypertension;
- Chronic heart failure;
- Hypertonic disease;
- Hypertrophy of the left cardiac ventricle.
Tablets are prescribed to patients with diagnosed heart failure if there are contraindications to therapy with ACE inhibitors or if such treatment is not adequately effective. Blocktran can be used both as an independent medication and as one of the components of complex therapy.
The drug is indicated for hypertension and chronic heart failure
Bloctran®
Hypersensitivity
Patients with a history of angioedema (swelling of the face, lips, pharynx/or tongue) should be closely monitored.
Arterial hypotension and water-electrolyte imbalance
Symptomatic hypotension, especially after the first dose or after dose increases, may occur in patients with hypovolemia and/or hyponatremia as a result of high-dose diuretics, a salt-restricted diet, diarrhea or vomiting. It is necessary to either correct these conditions before prescribing Bloktran®, or use or prescribe lower doses of the drug.
Fluid and electrolyte disturbances
Water and electrolyte disturbances are typical for patients with impaired nocturnal function in combination with or without diabetes mellitus and require correction.
In a clinical study conducted in patients with type 2 diabetes mellitus with nephropathy, the incidence of hyperkalemia in the group receiving losartan. was higher than in the placebo group. This indicates the need for regular monitoring of potassium levels in the blood plasma and creatinine clearance (CC) indicators - patients with heart failure and creatinine clearance from 30 to 50 ml/min require especially strict monitoring. Prescribing potassium-sparing diuretics, potassium supplements and potassium-containing salt substitutes simultaneously with Bloktran® is not recommended.
Liver dysfunction
Taking into account pharmacokinetic data indicating a significant increase in plasma concentrations of losartan in patients with cirrhosis, patients with a history of impaired liver function (more than 9 points on the Child-Pugh scale) are recommended to prescribe the drug in lower doses. There is no experience with the use of the drug in patients with severe liver failure. Taking this into account, Bloktran® is contraindicated in patients with severe liver failure.
Dual blockade of the renin-angiotensin-aldosterone system
There is evidence that the simultaneous use of ACE inhibitors, ARB II or aliskiren increases the risk of arterial hypotension, hyperkalemia and renal dysfunction (including acute renal failure).
The use of Bloktran® together with aliskiren is contraindicated in patients with diabetes mellitus or impaired renal function (GFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended for other patients (see section “Contraindications”).
The use of Blocktran in combination with an ACE inhibitor is contraindicated in patients with diabetic nephropathy and is not recommended for other patients (see section “Contraindications”).
Coronary heart disease (CHD) and cerebrovascular diseases
As with any antihypertensive drugs, too sharp a decrease in blood pressure in patients with coronary artery disease and cerebrovascular diseases can lead to myocardial infarction or ischemic stroke.
Heart failure
In patients with heart failure with or without renal impairment, as with other drugs acting on the RAAS, there is a risk of severe hypotension and acute renal failure. There is virtually no experience with the use of losartan in the treatment of patients with heart failure and concomitant severe renal failure, in patients with severe chronic heart failure (NYHA functional class IV), as well as in patients with heart failure and life-threatening arrhythmias. Taking this into account, caution should be exercised when prescribing Bloktran® to these categories of patients.
Combined use with ACE inhibitors in chronic heart failure (CHF)
When using Bloktran® in combination with ACE inhibitors, the risk of side effects may increase, especially renal dysfunction and hyperkalemia (see section "Side Effects"). In these cases, careful observation and monitoring of laboratory parameters is necessary.
Hemodialysis
During hemodialysis, the sensitivity of blood pressure to the action of AT2 receptor antagonists increases as a result of a decrease in blood volume and activation of the RAAS. It is necessary to adjust the dose of Bloktran® under careful monitoring of blood pressure in patients on hemodialysis.
Kidney transplant
There are no data on the use of Bloktran® in patients who have recently undergone a kidney transplant.
General anesthesia
In patients receiving angiotensin II antagonists, arterial hypotension may develop during general anesthesia and surgical procedures as a result of blockade of the renin-angiotensin-aldosterone system. Very rarely, severe hypotension may occur, requiring intravenous fluids and/or vasopressors.
Aortic and mitral valve stenosis, hypertrophic obstructive cardiomyopathy
When using the drug Bloktran®, as well as other vasodilators, caution should be exercised in patients with hypertrophic obstructive cardiomyopathy or hemodynamically significant stenosis of the aortic or mitral valve.
Primary hyperaldosteronism
Patients with primary hyperaldosteronism are usually resistant to treatment with antihypertensive drugs that affect the RAAS. In this regard, the drug Blocktran is not recommended for such patients.
Patients over 75 years of age
As a rule, patients over 75 years of age are recommended to be treated with Blocktran® at a dose of 25 mg per day.
Other special instructions and precautions
As clinical experience with the use of ACE inhibitors, losartan and other AT1 receptor antagonists shows, these drugs are less effective in reducing blood pressure in patients of the Black race than in representatives of other races, possibly due to low renin activity in patients of this race.
When use is contraindicated
Medical specialists categorically prohibit drinking Blocktran for high blood pressure in patients who have the following clinical contraindications:
- Dehydration;
- Hypotonic disease (stably reduced blood pressure);
- Hyperkalemia;
- Individual intolerance and hypersensitivity to substances included in the tablets.
With particular caution, the drug is prescribed to persons with diagnosed liver failure or renal dysfunction. Treatment of this category of patients requires strict medical supervision, individual dosing and constant monitoring of health status.
Instructions for use and dosage
Instructions for use of Bloktran recommend taking the tablets once a day, regardless of your meal schedule. The optimal dosage, as well as the duration of the therapeutic course, are determined by a specialist individually, depending on the diagnosis and other features of a particular clinical case.
It is important to note that since in patients with liver cirrhosis the concentration of the active ingredients of the drug in the blood is much higher than in other people, they will be prescribed tablets in minimal doses.
For arterial hypertension
Blocktran for hypertension is started at a dosage of 50 mg per day. If necessary, the daily dose of the drug can be increased to 100 mg, divided into two equal doses.
For heart failure
For patients suffering from heart failure, Blocktran therapy begins with a dosage of 1.25 mg throughout the day. Gradually, after each week of treatment, the daily dose of the medication is increased to 25 mg or 50 mg (depending on the severity of the disease, the age and health of the patient, and the reaction of his body to the proposed treatment).
If a patient with heart failure takes diuretics, then the starting daily dose of Bloktran is 25 mg.
The dosage is determined by the doctor depending on the condition of the individual patient.
Blocktran, 50 mg, film-coated tablets, 60 pcs.
Hypersensitivity reactions
In patients with a history of angioedema (swelling of the face, lips, pharynx/larynx and/or tongue), monitoring of the use of the drug is necessary (see “Side effects”).
Embryotoxicity
The use of drugs that affect the RAAS during the second and third trimester of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and mortality. The development of oligohydramnios may be associated with fetal lung hypoplasia and skeletal deformities. Possible adverse events in neonates include calvarial hypoplasia, anuria, hypotension, renal failure and death. When diagnosing pregnancy, the drug Blocktran® should be taken immediately.
Arterial hypotension and water-electrolyte imbalance or decreased circulating blood volume
In patients with reduced blood volume (for example, those receiving treatment with large doses of diuretics), symptomatic arterial hypotension may occur. Correction of such conditions must be carried out before prescribing Bloktran® or starting treatment with a lower dose of Bloktran® (see “Dosage and Administration”). Fluid and electrolyte imbalance is common in patients with impaired renal function with or without diabetes mellitus, so careful monitoring of these patients is necessary.
Losartan in patients with type 2 diabetes mellitus with proteinuria increases the incidence of hyperkalemia.
During treatment with Bloktran®, it is not recommended to take potassium-sparing diuretics, potassium supplements or potassium-containing salt substitutes.
Aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy
Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with aortic or mitral stenosis or hypertrophic obstructive cardiomyopathy.
Coronary heart disease and cerebrovascular diseases
Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with coronary heart disease or cerebrovascular diseases, since an excessive decrease in blood pressure in this group of patients can lead to the development of myocardial infarction or stroke.
Chronic heart failure
As with the use of other drugs that act on the RAAS, in patients with CHF and with or without impaired renal function, there is a risk of developing severe hypotension or acute renal impairment.
Since there is insufficient experience with the use of losartan in patients with heart failure and concomitant severe renal impairment, in patients with severe heart failure (NYHA functional class IV), as well as in patients with heart failure and symptomatic life-threatening arrhythmias, the drug Blocktran® should be prescribed with caution to patients in these groups.
Primary hyperaldosteronism
Since patients with primary hyperaldosteronism, as a rule, do not have a positive response to therapy with antihypertensive drugs that act by inhibiting the RAAS, the use of Bloktran® is not recommended in this group of patients.
Liver dysfunction
Data from pharmacokinetic studies indicate that the concentration of losartan in the blood plasma in patients with cirrhosis of the liver increases significantly, therefore patients with a history of impaired liver function should be prescribed Bloktran® at a lower dose. There is no experience with the use of losartan in patients with severe liver dysfunction, so the drug should not be used in this group of patients (see “Pharmacological properties” (Pharmacokinetics); “Contraindications”; “Dosage and administration”).
Renal dysfunction
Due to inhibition of the RAAS, changes in renal function, including the development of renal failure, have been observed in some susceptible patients. These changes in renal function may return to normal after treatment is stopped.
Some drugs that affect the RAAS may increase blood urea and serum creatinine concentrations in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney. Similar effects have been reported with losartan. Such renal dysfunction may be reversible after discontinuation of therapy. Losartan should be used with caution in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney.
Concomitant use of angiotensin II receptor antagonists with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or with moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended in other patients ( see section "Contraindications").
Concomitant use of angiotensin II receptor antagonists with ACE inhibitors is contraindicated in patients with diabetic nephropathy and is not recommended in other patients (see section "Contraindications").
Special patient groups
Race
Losartan, compared with atenolol, reduces cardiovascular morbidity and mortality in patients with hypertension and left ventricular hypertrophy of all races except blacks.
Children and teenagers
The effectiveness and safety of losartan in children and adolescents under 18 years of age have not been established.
If oliguria or arterial hypotension develops in newborns whose mothers took losartan during pregnancy, symptomatic therapy aimed at maintaining blood pressure and renal perfusion is necessary. Blood transfusions or dialysis may be required to prevent hypotension and/or maintain renal function.
Elderly patients
Clinical studies have not revealed any particularities regarding the safety and effectiveness of losartan in elderly patients (over 65 years of age).
Impact on the ability to drive vehicles and machinery
During the treatment period, caution should be exercised when driving and engaging in other potentially hazardous activities, since some of the side effects observed with the use of losartan, such as dizziness, drowsiness, may adversely affect the ability to drive a vehicle and perform potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.
Manifestations of side effects
Treatment with Blocktran tablets can cause the following adverse reactions:
- Arterial hypotension (excessive decrease in blood pressure);
- Pulse abnormalities (tachycardia or bradycardia);
- Decreased sexual desire;
- Erectile dysfunction in male patients;
- Rhinitis;
- Convulsive syndrome;
- Increased urge to empty the bladder;
- Cough syndrome;
- Conjunctivitis;
- Noise and ringing in the ears;
- Deterioration of visual function;
- Diarrhea or constipation;
- Dyspeptic disorders;
- Bronchitis;
- Dizziness;
- Migraine attacks;
- Depressive states;
- Nausea and vomiting;
- Toothache;
- Permanent lack of appetite, up to anorexia;
- Painful sensations localized in the sternum, lower extremities, back, knee joint, shoulder region;
- Skin itching;
- Rash on the skin like urticaria;
- Anemia;
- Tremor;
- Problems with sleep (insomnia or increased sleepiness);
- Chronic fatigue syndrome, weakness, asthenia, decreased performance;
- Hair loss;
- Increased sweating;
- Excessive dryness of the skin;
- Memory impairment;
- Psycho-emotional instability, causeless nervousness, anxiety, restlessness.
In most cases, the drug is well tolerated, and possible side effects disappear on their own after a few days of treatment. If the condition worsens, you should definitely inform your doctor about it!
Lack of appetite may be a side effect of taking the pills
Bloctran
Release form, composition and packaging
Light pinkish-orange film-coated tablets, round, biconvex. 1 tab. losartan potassium 50 mg. Excipients: lactose, microcrystalline cellulose, povidone (low molecular weight polyvinylpyrrolidone), potato starch, magnesium stearate, colloidal silicon dioxide (Aerosil). Shell composition: hypromellose (hydroxypropyl methylcellulose), copovidone (copolyvidone), titanium dioxide, talc, polysorbate-80 (Tween-80), sikovit yellow-orange 85 (E110).
Clinical and pharmacological group: Angiotensin II receptor antagonist.
pharmachologic effect
Antihypertensive drug. Specific angiotensin II receptor antagonist (AT1 subtype). It does not inhibit kinase II, an enzyme that destroys bradykinin. Reduces peripheral vascular resistance, blood concentrations of adrenaline and aldosterone, blood pressure, and 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 antihypertensive effect (decrease in systolic and diastolic blood pressure) 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.
Pharmacokinetics
Suction
Losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability - about 33%. Tmax of losartan is achieved after 1 hour.
Metabolism
It is subject to the “first pass” effect through the liver, metabolized by carboxylation with the participation of the CYP2C9 isoenzyme to form an active metabolite. Tmax of the active metabolite is achieved after 3-4 hours. Plasma protein binding is 99%.
Removal
T1/2 of losartan is 1.5-2 hours, and its main metabolite is 6-9 hours. About 35% of the dose is excreted in the urine, about 60% through the intestines.
Pharmacokinetics in special clinical situations
It has been established that the concentration of losartan in the blood plasma of patients with liver cirrhosis increases significantly, so patients with a history of liver disease should use the drug at a lower dose.
Indications
- arterial hypertension;
- chronic heart failure (as part of combination therapy, with intolerance or ineffectiveness of therapy with ACE inhibitors).
Dosage regimen
The drug is taken orally, regardless of food intake, the frequency of administration is 1 time/day. For 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 2 doses or 1 time / day. The initial dose for patients with heart failure is 12.5 mg 1 time / day.
Typically, 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/day, depending on the patient's tolerability of the drug. When prescribing the drug to patients receiving diuretics in high doses, the initial dose of the drug should be reduced to 25 mg 1 time / day.
It has been established that the concentration of losartan in the blood plasma of patients with liver cirrhosis increases significantly, therefore patients with a history of liver disease should use the drug at a lower dose. In elderly patients, as well as in patients with impaired renal function, including patients on hemodialysis, there is no need to adjust the initial dose. The safety and effectiveness of the drug in children have not been established.
Side effect
- From the central nervous system and peripheral nervous system: ≥1% - dizziness, asthenia, headache, fatigue, insomnia; <1% - anxiety, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypoesthesia, migraine, tremor, ataxia, depression, syncope.
- From the senses: ≥1% - ringing in the ears, taste disturbances, changes in vision, conjunctivitis.
- From the respiratory system: ≥1% - nasal congestion, cough, upper respiratory tract infections (fever, sore throat, sinusopathy, sinusitis, pharyngitis); <1% - dyspnea, bronchitis, rhinitis.
- From the digestive system: ≥1% - nausea, diarrhea, dyspeptic symptoms, abdominal pain; ≤1% - anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.
- From the musculoskeletal system: ≥1% - cramps, myalgia, pain in the back, chest, legs; ≤1% - arthralgia, pain in the shoulder, knee, arthritis, fibromyalgia.
- From the cardiovascular system: orthostatic hypotension (dose-dependent), palpitations, tachy- or bradycardia, arrhythmias, angina pectoris.
- From the genitourinary system: <1% - imperative urge to urinate, urinary tract infections, impaired renal function, weakened libido, impotence.
Dermatological reactions: <1% - dry skin, erythema, flushing, photosensitivity, increased sweating, alopecia.
Allergic reactions: <1% - urticaria, rash, itching, angioedema (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.
The association of side effects occurring with a frequency of <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.
Contraindications
- arterial hypotension;
- hyperkalemia;
- dehydration;
- pregnancy;
- lactation period (breastfeeding);
- age under 18 years (efficacy and safety have not been established);
- hypersensitivity to the components of the drug.
The drug should be prescribed with caution in case of liver and/or renal failure. Use during pregnancy and lactation There are no data on the use of losartan during pregnancy. However, it is known that drugs that act directly on the renin-angiotensin system, when used in the second and third trimesters of pregnancy, can cause developmental defects or even death of the developing fetus. Therefore, if pregnancy occurs, taking Bloktran should be stopped immediately.
When prescribed during lactation, a decision should be made to stop breastfeeding or to stop treatment with Bloktran.
Use for liver dysfunction
Patients with impaired liver function (including liver cirrhosis) should be prescribed lower doses of Blocktran and the drug should be used with caution.
Use for renal impairment
In patients with impaired renal function, including patients on dialysis, there is no need to adjust the initial dose, but Bloktran should be used with caution.
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.
Overdose
Symptoms: marked decrease in blood pressure, tachycardia; bradycardia may appear due to parasympathetic (vagal) stimulation.
Treatment: forced diuresis, symptomatic therapy; hemodialysis is ineffective.
Drug interactions
The drug may be prescribed in combination with other antihypertensive drugs. It should be taken into account that Bloktran enhances (mutually) the effect of other antihypertensive drugs (including diuretics, beta-blockers, sympatholytics). There were no clinically significant interactions with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, or phenobarbital. In patients with dehydration (previous treatment with diuretics in high doses), a pronounced decrease in blood pressure may occur. When used together with potassium-sparing diuretics and potassium supplements, the risk of developing hyperkalemia increases.
Storage conditions and periods
List B. The drug should be stored in a dry place, out of reach of children, at a temperature not exceeding 30°C. Shelf life: 2 years.
Important Notes
During the therapeutic course, it is necessary to regularly monitor potassium levels in the blood, especially if we are talking about elderly people or patients with diagnosed renal dysfunction.
Before starting treatment, it is recommended to correct dehydration. If this cannot be done for certain reasons, then therapy begins with minimal dosages of the drug.
In patients suffering from dehydration, tablets can provoke the development of a hypotensive crisis.
Is it possible to drive a car?
Possible side effects of Bloktran include dizziness, increased drowsiness, and asthenia. For this reason, in the first days of the therapeutic course you should refrain from driving. In the future (if the condition is normal and there are no undesirable reactions from the central nervous system), the patient can get behind the wheel, using extreme caution.
Driving a car while taking Blocktran is possible in the absence of adverse reactions to the drug
Drug interactions
Combination with potassium-containing drugs and diuretics increases the likelihood of developing hyperkalemia.
Tablets can be combined with other antihypertensive medications, diuretics, beta-blockers, but in smaller doses, due to an increased hypotensive effect.
You should ask your doctor about compatibility with other drugs.
