Release form of the drug Losartan
The drug Losartan is available in the form of tablets with different contents of the active substance. The tablets are white, round in shape. When cut, the contents are also white. A slight color deviation towards a yellow tint is acceptable.
The main active ingredient is losartan potassium. Additional components include:
- lactose monohydrate;
- pregelatinized starch;
- microcrystalline cellulose;
- Magnesium stearate.
Tablets are produced with different contents of active substance per unit of drug:
- 25mg;
- 50mg;
- 100 mg.
The difference in the concentration of the substance is needed to accurately select the dosage necessary to achieve a therapeutic effect in each specific case.
Losartan: what is it taken for?
Indications for the use of Losartan are:
- Nephropathy of the diabetic type, including damage to the tubules and glomeruli of the kidneys, as well as arterioles and arteries, developing due to disruption of metabolic processes in the renal tissue.
- Presence of a tendency to develop disorders of the cardiovascular system, including strokes.
- Arterial hypertension, in which the indicator exceeds 140 mm Hg. Art.
- Chronic heart failure, in which the circulatory system does not properly supply the body with oxygen either at rest or after exercise.
After entering the gastrointestinal tract, the drug is actively absorbed. As a result of filtration by the liver, a metabolite is formed that is many times more active than Losartan in its original form. The maximum concentration of Losartan in the blood is observed after 1 hour, and the metabolite - after 3-4 hours. About 98% of the drug actively binds to plasma proteins.
The half-life of Losartan is 2-2.5 hours, and the active metabolite is up to 9 hours, depending on the speed of metabolic processes in the body. The drug and its derivatives are excreted unchanged in feces, urine and bile. Most of the medicine comes out through the rectum.
LOSARTAN
special instructions
In patients with dehydration (for example, those receiving treatment with high doses of diuretics), symptomatic arterial hypotension may occur at the beginning of treatment with LOSARTAN (dehydration must be corrected before prescribing LOSARTAN or starting treatment with a lower dose).
In patients with liver cirrhosis, the plasma concentration of LOSARTAN increases significantly, and therefore, in the presence of a history of liver disease, it should be prescribed in lower doses.
Drugs that affect the kinin-angiotensin system may increase blood urea and serum creatinine concentrations in patients with bilateral renal stenosis or arterial stenosis of a solitary kidney.
Condition after kidney transplantation. There is no experience with the use of the drug LOSARTAN in patients with a condition after kidney transplantation.
Aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy. As with all drugs that have a vasodilating effect, angiotensin II receptor antagonists (ARA II) should be administered with caution to patients with aortic or mitral stenosis, or hypertrophic obstructive cardiomyopathy.
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 arterial hypotension or acute renal failure.
There is no experience with the use of LOSARTAN in patients with heart failure and concomitant severe renal failure, in patients with severe heart failure (NYHA functional class IV), as well as in patients with heart failure and symptomatic life-threatening arrhythmias. Therefore, LOSARTAN should be prescribed with caution to patients in these groups.
Coronary heart disease (CHD), cerebrovascular diseases. Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with coronary artery 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.
Primary hyperaldosteronism. Patients with primary hyperaldosteronism, as a rule, do not respond positively to therapy with antihypertensive drugs that act by inhibiting the RAAS, therefore the use of LOSARTAN is not recommended in this group of patients.
History of angioedema. In patients with a history of angioedema taking LOSARTAN, hypersensitivity reactions were observed in clinical practice in the post-marketing period: rarely observed angioedema involving the larynx and pharynx, causing airway obstruction, and/or angioedema of the face, lips, pharynx and/or tongue .
Children
The safety and effectiveness of the drug in children have not been established.
Elderly patients
Clinical trials have not revealed any differences in the safety and effectiveness of losartan in elderly patients.
Losartan: instructions for use
Eating does not affect the absorption and activity of the drug. The drug is swallowed whole with a sufficient amount of water. Depending on the diagnosis, a different therapeutic dose may be prescribed:
- Arterial hypertension is treated with a single dose of 50 mg of Losartan. If there is no desired effect, the single dose can be increased to 100 mg per day.
- For chronic heart failure, treatment begins with a single dose of half a tablet containing 25 mg of the active substance. After a week, the daily dose is gradually increased.
- The risk of developing problems in the functioning of the cardiovascular system is reduced by a single dose of 50 mg of Losartan or a two-time dose of 25 mg.
- Liver failure becomes a reason to prescribe 25 mg of the active substance.
Throughout the course of treatment, regardless of the diagnosis, it is necessary to monitor the patient’s blood pressure daily. If the patient takes the course at home, he must keep a diary of tonometer readings after each measurement.
If an excessive decrease in blood pressure is noted, the doctor is required to adjust the daily dose. In addition, the patient must comply with the time of taking the drug. In order to reduce the risk of overdose, the tablet is taken strictly at the same time. If one dose is missed, the next dose is taken at the allotted hour.
Concomitant use with other drugs
Concomitant use with ACE inhibitors leads to the development of such a dangerous condition as hyperkalemia, in which the level of potassium in the blood increases. In addition, this combination increases the risk of kidney failure and life-threatening low blood pressure.
In combination with diuretics, the risk of hypotension is also high. This is due to the fact that taking diuretics itself leads to a decrease in blood pressure, which enhances the effect of Losartan.
It is not recommended to drink Losartan with lithium-containing drugs, so as not to provoke an excess of lithium in the blood, since the combination of drugs disrupts natural metabolic processes.
Losartan N, 12.5 mg+50 mg, film-coated tablets, 30 pcs.
Losartan
In clinical pharmacokinetic studies, no clinically significant interactions were identified with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin. Rifampicin reduces the concentration of the active metabolite. The clinical significance of this interaction has not been established.
Concomitant use with aliskiren and drugs containing aliskiren in patients with diabetes mellitus and/or moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area) is contraindicated.
Fluconazole and rifampicin decreased plasma concentrations of the active metabolite of losartan.
The clinical significance of this interaction has not been studied.
The simultaneous use of losartan, as well as other drugs that affect the RAAS, with potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone), potassium-containing supplements or potassium salts may lead to an increase in potassium levels in the blood serum. Simultaneous use is not recommended.
As with the use of other drugs that affect the excretion of lithium, treatment with losartan may be accompanied by a decrease in excretion and an increase in the serum concentration of lithium, therefore, during simultaneous treatment with lithium preparations, its serum concentration should be monitored.
With simultaneous use of angiotensin II receptor antagonists (ARA II) with NSAIDs, including selective COX-2 inhibitors and acetylsalicylic acid in doses of more than 3 g per day, the effect of antihypertensive drugs may be reduced. Therefore, the antihypertensive effect of ARA II may be weakened by NSAIDs, including COX-2 inhibitors and acetylsalicylic acid in doses of more than 3 g per day.
In some patients with impaired renal function who have been treated with NSAIDs, including COX-2 inhibitors, treatment with ARB II may cause further deterioration of renal function, including the development of acute renal failure, and an increase in potassium levels (especially in patients with a history of renal dysfunction ). Concomitant use with NSAIDs should be done with caution, especially in elderly patients. In this case, it is necessary to adequately replenish the volume of blood volume and periodically monitor renal function from the moment of initiation of therapy and subsequently.
In some patients with impaired renal function who have used NSAIDs, including selective COX-2 inhibitors, concomitant use of ARB II may cause further deterioration of renal function.
Double blockade of the RAAS: double blockade of the RAAS, i.e. the addition of an ACE inhibitor to APAII therapy is only possible in selected cases under careful monitoring of renal function. In patients with atherosclerosis, heart failure or diabetes mellitus with target organ damage, double blockade of the RAAS (with simultaneous use of ARB II, ACE inhibitors or aliskiren) is accompanied by an increased incidence of arterial hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure) in comparison with the use of a drug from one of the listed groups. The simultaneous use of losartan with ACE inhibitors in patients with diabetic nephropathy is contraindicated.
Other drugs that cause arterial hypotension, including tricyclic antidepressants, antipsychotics, baclofen, amifostine: simultaneous use of drugs that lower blood pressure (main or side effect) may increase the risk of developing arterial hypotension.
Hydrochlorothiazide
With thiazide diuretics, drugs such as ethanol, barbiturates and narcotics may potentiate the risk of orthostatic hypotension.
Hypoglycemic agents (for oral administration and insulin) - dose adjustment of hypoglycemic agents may be required, because hydrochlorothiazide affects glucose tolerance.
Metformin should be used with caution due to the risk of lactic acidosis due to renal impairment caused by hydrochlorothiazide.
Other antihypertensive drugs have an additive effect.
Cholestyramine and colestipol - in the presence of anion exchange resins, the absorption of hydrochlorothiazide is impaired. Cholestyramine and colestipol in a single dose bind hydrochlorothiazide and reduce its absorption in the gastrointestinal tract by 85% and 43%, respectively.
Corticosteroids, ACTH (adrenocorticotropic hormone) or glycyrrhizic acid (found in licorice root) - marked reduction in electrolytes, in particular the risk of hypokalemia.
Pressor amines (eg, epinephrine, norepinephrine) - decreased response to pressor amines.
Muscle relaxants of a non-depolarizing type of action (for example, tubocurarine) - enhance the effect of muscle relaxants.
Lithium - diuretics reduce the renal clearance of lithium and increase the risk of lithium toxicity; simultaneous use is not recommended.
NSAIDs (including COX-2 inhibitors) may reduce the diuretic, natriuretic and antihypertensive effects of diuretics.
Medicines used to treat gout (probenecid, sulfinpyrazone and allopurinol): Dosage adjustment of uricosuric drugs may be required as hydrochlorothiazide may cause an increase in serum uric acid concentrations. Thiazide diuretics may increase the incidence of hypersensitivity reactions to allopurinol.
Anticholinergic drugs (eg, atropine, biperiden): increase the bioavailability of thiazide diuretics by reducing gastrointestinal motility and the rate of gastric emptying.
Cytostatic drugs, for example, cyclophosphamide, methotrexate: the myelosuppressive effect increases by slowing elimination from the body.
Salicylates - when taking high doses of salicylates, hydrochlorothiazide can enhance their toxic effect on the central nervous system.
Methyldopa: Isolated cases of hemolytic anemia have been described with the simultaneous use of hydrochlorothiazide and methyldopa.
Concomitant use of cyclosporine increases the risk of developing hyperuricemia and exacerbation of gout.
Cardiac glycosides: Hypokalemia and hypomagnesemia caused by the use of thiazide diuretics increases the risk of developing arrhythmias during treatment with cardiac glycosides.
Calcium salts - thiazide diuretics can increase the calcium level in the blood serum due to a decrease in its excretion. If it is necessary to use calcium supplements, the dose is selected under the control of calcium levels in the blood serum.
Vitamin D - increases the risk of hypercalcemia.
Interference with Laboratory Tests - Due to their effects on calcium excretion, thiazides may interfere with tests of parathyroid function.
Carbamazepine - increases the risk of symptomatic hyponatremia. Serum sodium levels must be monitored.
Iodine-containing contrast agents - with dehydration caused by taking diuretics, the risk of developing acute renal failure increases, especially when high doses of iodine-containing drugs are administered. Before administering such drugs, the patient must be rehydrated.
Amphotericin B (intravenous), stimulant laxatives, or ammonium glycyrrhizinate (found in licorice)—hydrochlorothiazide may increase electrolyte disturbances, especially hypokalemia.
Drugs that bind intensively to proteins enhance the diuretic effect. Dosage adjustments of oral anticoagulants probenecid and sulfinpyrazone may be necessary as hydrochlorothiazide may inhibit their effect.
Concomitant use of thiazide diuretics with antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide, amiodarone, sotalol, dofetilide, ibutilide), some antipsychotic drugs (neuroleptics) (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, sulpiride, sultopride, amisulpride, tiapride, pi mosid, haloperidol, droperidol) and other drugs (bepridil, cisapride, difemanil, erythromycin, halofantrine, mizolastine, pentamidine, terfenadine, vincamine, pentamidine) may be accompanied by the development of hypokalemia, which in turn can cause the development of ar.
