- The composition of 1 tablet of the drug Blocktran 50 mg included losartan potassium. Additional substances: microcrystalline cellulose, lactose monohydrate, low molecular weight povidone, sodium carboxymethyl starch, potato starch, magnesium stearate, silicon dioxide. Shell composition: titanium dioxide, hypromellose, polysorbate 80, copovidone, talc, dye yellow sunny sunset.
- The composition of 1 tablet of the drug Blocktran GT 12.5 mg included hydrochlorothiazide and 50 mg losartan potassium. Additional substances: microcrystalline cellulose, lactose monohydrate, low molecular weight povidone, sodium carboxymethyl starch, potato starch, magnesium stearate, silicon dioxide. Shell composition: polydextrose, hypromellose, medium chain triglycerides, titanium dioxide, maltodextrin, talc, dye red carmine.
- Pink-orange biconvex round tablets. 10 tablets in contour packaging; 1, 3, 2, 5 or 6 packs in a cardboard box.
- Pink biconvex tablets of a round form, on a break - white color. 10 tablets in contour packaging; 1, 3, 2, 5 or 6 packs in a cardboard box.
Pharmacodynamics and pharmacokinetics
Drugs Blocktran and Blocktran GT lower arterial pressure.
Pharmacodynamics of losartan
Angiotensin of the second type is a strong vasoconstrictor, the main mediator renin-angiotensin system and the main pathophysiological link arterial hypertension. Losartan receptor blocker angiotensin2 types. Angiotensin selectively binds to AT1-type receptorslocated in the adrenal glands, in the tissues of blood vessels, in the kidneys and heart and stimulates vasoconstriction and production aldosteroneis also able to provoke the growth of smooth muscle cells. This substance and its active metabolite block all effects angiotensin 2 types regardless of the source or method of synthesis.
Losartan does not block the rest of the receptors hormones or ion channels that regulate the cardiovascular system. Does not suppress angiotensin converting enzymeresponsible for inactivation bradykininresulting in side effects associated with bradykinin occur very rarely. Using losartan there is an increase in plasma activity renin, which in turn stimulates an increase in the content of type 2 angiotensin in blood. Antihypertensive activity and decreased concentration aldosteroneblood is retained, which indicates an effective blockade angiotensin receptors.
Losartan and its main metabolite have tropism for receptors angiotensin 1 type larger than receptors angiotensin 2 types. The specified metabolite is more active losartan 10-40 times. After administration, the action reaches its maximum strength after six hours, and then slowly decreases over the course of 24 hours. The greatest antihypertensive effect is recorded after 4-6 weeks from the start of drug therapy. This effect increases with increasing dosage. losartan.
Losartan does not affect vegetative reflexes and does not change the concentration norepinephrine in the blood for a long time.
In patients with enlarged left ventricle and arterial hypertension losartan, including in combination with hydrochlorothiazide, reduces the likelihood of cardiovascular mortality and morbidity.
Pharmacodynamics of hydrochlorothiazide
Mechanism of action thiazide-type diuretics unknown. They usually do not affect normal pressure.
Hydrochlorothiazide is both antihypertensive drug, and diuretic. It affects the reverse absorption of electrolytes in the tubules of the kidneys. Approximately the same increase ion excretion chlorine and sodium. Natriurez accompanied by weak loss bicarbonateions potassium and delay calcium. The diuretic effect is recorded 2 hours after administration, reaches a maximum after 4 hours and lasts 7-12 hours.
Pharmacodynamics of losartan and hydrochlorothiazide
Due to diuretic effecthydrochlorothiazide increases plasma activity reninstimulates excretion aldosteroneincreases concentration angiotensin 2 types and lowers concentration potassiumin plasma. Reception losartan inhibits all effects angiotensin 2 types and due to the suppression of action aldosterone helps reduce loss potassiumcaused by taking diuretic.
Also hydrochlorothiazidecauses a slight increase in blood levels uric acid, but losartan has a moderate and temporary uricosuric effect. Losartan and hydrochlorothiazide combined to reduce hyperuricemiaprovoked diuretic.
Features of pharmacokinetics hydrochlorothiazide and losartan with separate and simultaneous use do not differ.
Pharmacokinetics of losartan
When taken orally, it is well absorbed from the intestine, is exposed to metabolism in the liver with the formation of one carboxylated active metabolite and several inactive metabolites. Bioavailability is approaching 33%. Highest concentration losartan and its main metabolite are fixed after 1 hour and 3-4 hours after administration, respectively.
Actively binds (up to 99%) with plasma proteins (mainly with albumin) Almost does not penetrate the blood-brain barrier. Up to 14% of accepted losartan turns into a pharmacologically active metabolite. In addition, inactive biologically metabolites are also formed.
About 4% of the substance is excreted by the kidneys in its original form and about 6% is excreted in the form of the main derivative. Half-life losartan and its metabolite is approximately 2 and 7-8 hours, respectively. Excretion occurs through the intestines and urine.
Pharmacokinetics of hydrochlorothiazide
After administration, it is rapidly absorbed from the intestine. The onset of maximum concentration is 2-3 hours.
It binds to plasma proteins by 40-60%, passes through the placenta and does not penetrate the blood-brain barrier, can be excreted in breast milk during lactation.
It is not metabolized and is actively excreted by the kidneys. The elimination half-life varies between 5.5-15 hours. More than 61% of the dose is excreted in its original form during the day.
Indications for use
Indications for use of Blocktran
- arterial hypertension;
- heart failure of a chronic nature;
- as part of multicomponent therapy with treatment failure or intolerance ACE inhibitors.
Indications for use of Blocktran TG
- arterial hypertension;
- the need to lower the risk of cardiovascular disorders and mortality in patients with arterial hypertension and an increase in the left ventricle.
Contraindications for taking Blocktran
- arterial hypotension;
- age up to 18 years;
- pregnancy and lactation;
- sensitization to the components of the product.
Use the drug with caution in case of insufficient liver or kidney function.
Contraindications for taking Blocktran GT
- arterial hypotension;
- refractory hypokalemia;
- poorly controlled diabetes;
- severe renal impairment;
- Addison's disease;
- primary hyperaldosteronism;
- severe liver dysfunction, cholestasis;
- sharing with potassium-sparing diuretics or potassium preparations;
- pregnancy or lactation;
- sensitization to derivatives sulfonylamide or other components of the drug;
- age up to 18 years;
- intolerance lactosedisadvantage lactasesmalabsorption glucose galactose.
Caution is advised to prescribe the drug in the presence of the following disorders or situations: a change in water-electrolyte balance, bilateral narrowing of the renal arteries, diabetes, renal failureviolation of the liver, hypercalcemia, gout, hyperuricemia, bronchial asthma,severe allergic history, systemic diseases of the connective tissue, hypovolemia, advanced age, simultaneous reception anti-inflammatory non-steroid drugs or cardiac glycosides, coronary heart disease, acute attack angle-closure glaucoma.
Side effects characteristic of losartan
- Reactions from hematopoiesis: ecchymoses, purpure of Shenlein-Genoch, anemia.
- Reactions from metabolism: aggravation gout, anorexia.
- Allergic reactions: Quincke's edema, anaphylactic reactions, urticaria.
- Reactions from nervous activity: dizziness, insomnia, headache, paresthesia, anxiety, tremorperipheral neuropathy, migraineanxiety, fainting, panic disorder, sleep disorder, anxiety disorders, confusion, drowsiness, depressionmemory impairment.
- Reactions from of view: conjunctivitis, visual impairment, decreased severity, burning sensation.
- Reactions from hearing: noise in ears, vertigo.
- Reactions from breathing: cough, nasal congestion, respiratory tract infection, pharyngitis, dyspnea, laryngitis, bronchitis, nose bleed, rhinitisdiscomfort in the throat.
- Reactions from digestion: diarrheanausea dyspeptic symptomsdry mouth, abdominal pain, vomiting, toothache, gastritis, flatulence, constipation.
- Reactions from musculoskeletal system: cramps, myalgiapain in the back or legs, pain in the arms, arthralgia, arthritisswelling of the joints, muscle weakness, fibromyalgiamusculoskeletal pain.
- Reactions from blood circulation: orthostatic hypotension, arterial hypotension, tachycardia, bradycardia, angina pectoris,chest pain, arrhythmias, Second-degree AV block, myocardial infarction, cerebrovascular disorders, vasculitis.
- Reactions from genitourinary sphere: nocturiafrequent urination, weakening libidourinary tract infections impotence.
- Reactions from skin: erythemadry skin itchy skin, photosensitization, skin rash, alopeciaincreased sweating, dermatitis.
- Other reactions: asthenia, edema facial fatigue fever.
- Lab changes: drop hematocrit and hemoglobin, hyperkalemiaincreasing content urea, creatinine, enzymes the liver.
Side effects characteristic of hydrochlorothiazide
- Reactions from hematopoiesis: agranulocytosis, hemolytic anemia, aplastic anemia, purpura, leukopenia, thrombocytopenia.
- Allergic reactions: possible anaphylactic reactions.
- Reactions from metabolism: hyperglycemia, anorexia, hypokalemia, hyperuricemia, hyponatremia.
- Reactions from nervous activity: headache, dizziness, insomnia.
- Reactions from organ of vision: xantopsia, temporary visual impairment.
- Reactions from blood circulation: necrotizing vasculitis.
- Reactions from breathing: pneumonitis, distress syndrome, pulmonary edema.
- Reactions from digestion: irritation of the gastrointestinal mucosa, sialodenitis, nausea, jaundice, diarrheavomiting constipation, pancreatitis.
- Reactions from skin: urticaria, photosensitivity, epidermal toxic necrolysis.
- Reactions from musculoskeletal system: muscle cramps.
- Reactions from genitourinary system: impaired renal function, interstitial nephritis, glucosuria, renal failure.
- General reactions: fever.
Instructions for use of Blocktran GT and Blocktran (Method and dosage)
Instructions for use of Blocktran
The drug should be taken orally once a day.
At arterial hypertension the average daily dose is 50 mg. In some cases, to achieve a stronger effect, the dose is increased to 100 mg once a day or up to 50 mg twice a day.
Initial dose for patients suffering heart failure equal to 12.5 mg once a day. As a rule, the dosage is increased with an interval of one week to an average maintenance dose of 50 mg once a day.
When prescribing funds to patients receiving diuretics in large doses, the initial dose should be reduced to 25 mg once a day.
Found that the content losartan in the blood of sufferers cirrhosis greatly increased, so people with liver diseases should use the drug in a lower dose.
Instructions for use Blocktran GT
The drug should be taken orally once a day.
At arterial hypertension initial and maintenance dosage - 1 tablet once a day. In some cases, to achieve a better effect, the dosage is increased to 2 tablets once a day. The highest daily dose is 2 tablets of the drug.
When used to reduce risk cardiovascular disorders and mortality in people with arterial hypertension and increase in left ventricle initial dose losartan equal to 50 mg once a day. Patients with 50 mg losartan a day the required level of pressure could not be reached, the selection of treatment by a combination is required losartanlow dosage hydrochlorothiazide (12.5 mg), and if necessary, increase the dosage losartanup to 100 mg per day with 12.5 mg hydrochlorothiazide in a day. Then it is allowed to increase the dosage to 2 tablets of Blocktran GT per day.
In case of an overdose, the use of the drug should be discontinued, the patient should be provided with monitoring of the performance of the heart and lungs, symptomatic treatment - gastric lavage, elimination of electrolyte disorders, dehydration, hepatic comaand depressurization by standard methods.
Overdose of losartan
Signs of an overdose: marked decrease in pressure, tachycardia, bradycardia due to parasympathetic stimulation.
Therapy: with a strong decrease in pressure, supportive treatment is recommended. Hemodialysis not effective.
Overdose of hydrochlorothiazide
Signs of an overdose: lack of electrolytes (hypochloremia, hypokalemia, hyponatremia); dehydration. When used together cardiac glycosides exacerbation is possible hypokalemia arrhythmia.
Therapy: gastric lavage, application enterosorbentsCorrection of electrolyte disturbances as necessary.
Rifampicin reduces the concentration of the main active metabolite losartan.
Concomitant use potassium-containing additives, potassium-sparing diuretics (Amiloride, Triamteren, Spironolactone, Eplerenone) and salts, including potassiummay cause an increase in concentration potassium in blood.
Treatment losartan provokes a decrease in excretion and an increase in concentration lithium in the blood, therefore, with joint treatment with lithium preparations should monitor its concentration.
Non-steroidal anti-inflammatory drugs may lower effect diuretics and other antihypertensive drugs.
In a number of patients with impaired renal function receiving treatment anti-inflammatory non-steroid drugssimultaneous reception angiotensin receptor antagonists can cause impaired renal function, up to acute renal failure. Usually this effect is reversible.
Combined use angiotensin receptor blocker2 types with ACE inhibitor causes a significant increase in the frequency of adverse reactions, such as fainting, arterial hypotension, impaired renal function, hyperkalemiaacute renal failure. The highest risk is in those with a diagnosis of heart failure, atherosclerosis, diabetes.
Fluconazole lowers the concentration of the main metabolite and increases the concentration of losartan.
When combined with narcotic analgesics, barbiturates, ethanol appearance is possible orthostatic hypotheism.
When combined with hypoglycemic drugs dosage adjustment may be required hypoglycemic drugs.
Due to the risk of lactic acidosis due to possible kidney damage when using hydrochlorothiazide Metformin should be prescribed with caution.
When combined with other antihypertensive drugsadditive effect comes to light.
When used simultaneously with adrenocorticotropic hormone, corticosteroids, glycyrrhizic acid (licorice), Amphotericin B a pronounced decrease in the concentration of electrolytes is detected, especially potassium.
When combined with muscle relaxants of a non-depolarizing type (tubocurarine)stimulation of their action is possible.
Non-steroidal anti-inflammatory drugs may weaken diuretic, antihypertensive and natriuretic effects hydrochlorothiazide.
With the simultaneous use of the drug with butpressorized mines (Norepinephrine, Epinephrine) a slight decrease in the effect of the latter is not excluded.
Thiazide diuretics lower kidney excretion cytotoxic drugs (cyclophosphamide, methotrexate)and stimulate their myelosuppressive effect.
Concomitant treatment with Cyclosporine increases the likelihood hyperuricemia and gout.
Thiazide diuretics stimulate toxic effects salicylates on the nervous system when used in high doses.
Simultaneous use thiazide diuretics with some antipsychotics, antiarrhythmic drugsmay be accompanied hypokalemia.
When combined with Carbamazepine there is a chance of occurrence symptomatic hyponatremia.
Terms of sale
Keep out of the reach of children. Store at room temperature.
In the initial period of treatment with the drug, it is recommended to refrain from driving vehicles.
AnalogsMatches for ATX Level 4 code:TelmisartanIrbesartanPresartanNortianCandesartanCozaarAprovelTevetenCardosalValsartanLosartanAtacandDiovanMikardisVasarWalsLoristaLozapCandesar
Analogues of Blocktran: Brozaar, Vero-Lozartan, Vazotens, Cardomin-Sanovel, Cozaar, Karzartan, Lakea, Lozarel, Lozap, Lozartan, Presartan, Losacor, Lorista, Lotor, Renicard.
Not applicable in children under 18 years of age.
During pregnancy and lactation
The above drugs are not used during pregnancy and with lactation.
Reviews of doctors and patients about the drug indicate a high ability of the drug to lower blood pressure, however, side effects when using Blocktran are not uncommon, mainly fatigue and joint pain.
Blocktran price, where to buy
In Russia, the price of Blocktran No. 30 starts at 135 rubles, and the price of Blocktran GT No. 30 starts at 160 rubles.
- Online Pharmacies in Russia
- Blocktran Tab. p.p.o. 50mg n60Pharmstandard-Leksredstva OAO321 rub.order
- Blocktran tablets 50mg No. 60331 rub.order