Losartan

Losartan is a specific angiotensin II receptor antagonist with antihypertensive effect.

Release form and composition

Losartan dosage form - tablets: round, biconvex, film-coated white or white with a grayish tint:

• 12.5 mg - 7 or 10 pcs. in blisters, 1, 2, 3 or 4 packs in a carton box;
• 50 mg - 7 pcs. in blisters, 1, 2 or 4 packs in a carton pack; 10 or 30 pcs. in blisters, 1, 2, 3, 4, 5, 6 or 10 packs in a carton pack; 28 each in blisters, 1 or 2 packs in a carton pack; on 10, 20, 30, 40, 50, 60 or 100 pieces. in polymer cans, 10 cans per carton packs;
• 100 mg - 7 pcs. in blisters, 1, 2 or 4 packs in a carton pack; 10 or 30 pcs. in blisters, 1, 2, 3, 4, 5, 6 or 10 packs in a carton pack; 28 each in blisters, 1 or 2 packs in a carton pack; on 10, 20, 30, 40, 50, 60 or 100 pieces. in polymer cans, 10 cans in packs of cardboard.

Each tablet contains:

• Active ingredient: losartan potassium - 12.5, 50 or 100 mg;
• Auxiliary components: microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silicon dioxide (aerosil), croscarmellose sodium, povidone;
• The composition of the film shell: opadry white (hypromellose, titanium dioxide, talc and iron oxide yellow) or a dry mixture for film coating (hypromellose, talc, titanium dioxide, macrogol 4000 and iron oxide yellow).

Indications for use

• Treatment of arterial hypertension;
• Therapy of chronic heart failure in case of failure of treatment with ACE inhibitors (angiotensin-converting enzyme);
• Kidney protection in patients with type 2 diabetes with concomitant proteinuria (the drug can slow the progression of renal failure: reduce proteinuria, the incidence of hypercreatininemia, the incidence of end-stage chronic renal failure, requiring hemodialysis or kidney transplantation, as well as death rates);
• Reducing the risk of developing cardiovascular diseases (including myocardial infarction and stroke) and mortality in patients with arterial hypertension and left ventricular hypertrophy.

Contraindications

Absolute:

• Refractory hyperkalemia;
• Dehydration;
• Lactase deficiency / lactose intolerance / glucose-galactose malabsorption syndrome;
• Severe liver failure;
• Age up to 18 years;
• Pregnancy and lactation;
• The simultaneous use of aliskiren in patients with diabetes mellitus and / or impaired renal function (glomerular filtration rate of less than 60 ml / minute);
• Hypersensitivity to any of the components of the drug.

Relative (special caution required):

• Renal failure;
• Bilateral renal artery stenosis or single kidney artery stenosis;
• Hyperkalemia;
• Conditions after kidney transplantation;
• Violation of water and electrolyte balance;
• Cerebrovascular diseases;
• Severe heart failure (functional class IV in accordance with the classification of NYHA);
• Aortic and mitral stenosis;
• Hypotension;
• Coronary heart disease;
• Obstructive hypertrophic cardiomyopathy;
• Heart failure with concomitant severe renal failure;
• Heart failure with life-threatening arrhythmias;
• Reduced circulating blood volume (BCC);
• Hepatic impairment (less than 9 points in Child-Pugh);
• Angioedema in history;
• Primary aldosteronism.

Dosing and Administration

Losartan should be taken orally. If necessary, it is prescribed in combination with other antihypertensive agents. Food intake does not affect the effectiveness of the drug.

The standard initial and in most cases, maintenance dose for arterial hypertension is 50 mg 1 time / day. The maximum antihypertensive effect is achieved 3-6 weeks after the start of treatment. In some cases, in order to achieve a greater effect, the daily dose may be increased to 100 mg once a day.

For older people over the age of 75 years, patients with reduced BCC, patients with liver failure and undergoing hemodialysis, the initial dose should be reduced to 25 mg 1 time per day.

To reduce the risk of cardiovascular morbidity and mortality, the drug is prescribed in a daily dose of 50 mg. Subsequently, hydrochlorothiazide is added to losartan or the dose of losartan potassium is increased to 100 mg in 1 or 2 doses (depending on the degree of blood pressure reduction).

When using the drug to protect the kidneys in patients with type 2 diabetes with concomitant proteinuria, treatment begins with a daily dose of 50 mg 1 time per day. In the future, if this is necessary, the dose is increased to 100 mg 1 time per day. If necessary, other antihypertensive drugs (diuretics, centrally acting antihypertensive drugs, alpha- and beta-blockers, slow calcium channel blockers), insulin or other hypoglycemic drugs (glucosidase inhibitors, sulfonylurea derivatives, glitazones) may be prescribed simultaneously with Losartan.

In chronic heart failure, take Losartan with a dose of 12.5 mg 1 time / day with a gradual (usually once a week) increase first to 25 mg, then to 50 mg. The usual maintenance daily dose is 50 mg.

Side effects

Losartan is preemptively well tolerated. If side effects occur, they are usually transient in nature and do not require discontinuation of the drug.

Side effects occurring in more than 1% of cases:

• Respiratory system: swelling of the nasal mucosa, cough, bronchitis, sinusitis, pharyngitis, infections of the upper respiratory tract;
• Digestive system: dyspepsia, diarrhea, nausea, abdominal pain;
• Central nervous system: insomnia, dizziness, headache;
• Cardiovascular system: tachycardia, sensation of heartbeat;
• Musculoskeletal system: muscle cramps, pain in the back and legs;
• General disorders: pain in the chest, fatigue, weakness, asthenia, peripheral edema.

Side effects occurring in less than 1% of cases:

• Allergic reactions: urticaria, rash, pruritus, angioedema;
• Skin: photosensitivity, erythema, increased sweating, ecchymosis, dry skin, alopecia;
• Cardiovascular system: arrhythmias, angina pectoris, bradycardia, dose-dependent orthostatic hypotension, symptomatic arterial hypotension (especially in patients with intravascular dehydration), vasculitis, myocardial infarction;
• Nervous system and sensory organs: impaired memory, taste and vision, anxiety, migraine, conjunctivitis, hypostezia, paresthesia, tremor, tinnitus, ataxia, sleep disturbance, drowsiness, peripheral neuropathy, depression, syncope;
• Hematopoietic system: eosinophilia, anemia, Schönlein-Henoch purpura, thrombocytopenia;
• Musculoskeletal system: pain in the shoulder and knee, arthritis, fibromyalgia, arthralgia;
• Reproductive system: impotence or decreased libido;
• Digestive system: flatulence, toothache, gastritis, dryness of the oral mucosa, constipation, vomiting, anorexia, abnormal liver function, hepatitis;
• Urinary system: urinary tract infections, urgency to urinate, impaired renal function;
• Other: nosebleeds, exacerbation of the flow of gout.

Losartan may affect the results of some laboratory indicators. So, when taking the drug are marked: often - hyperkalemia; infrequently - an increase in the concentration of residual nitrogen, urea, serum creatinine; very rarely - hyperbilirubinemia, moderate increase in transaminase activity (alanine aminotransferase and aspartate aminotransferase).

special instructions

In patients with primary hyperaldosteronism, as a rule, there is no positive response to therapy with antihypertensive drugs that act by inhibiting the renin-angiotensin-aldosterone system (RAAS), so this group of patients is not recommended to use Losartan.

During treatment with Losartan, caution should be exercised when driving and performing potentially hazardous types of work that require quick psychomotor reactions and high concentration of attention.

Drug interaction

Fluconazole and rifampicin reduce the level of the active metabolite of losartan, but the clinical significance of such interactions has not been established.

In the case of simultaneous use of potassium-sparing diuretics (for example, amiloride, triamterene, eplerenone, spironolactone), potassium supplements, salts with potassium content and agents that increase the concentration of potassium (for example, heparin), it is possible to increase the concentration of potassium in the blood serum.

Losartan can reduce sodium excretion and increase the serum concentration of lithium, so when using this combination, it is necessary to control the concentration of lithium.

Non-steroidal anti-inflammatory drugs (NSAIDs) can reduce the effects of diuretics and other antihypertensive drugs.

There are cases of further deterioration of renal function in patients who received losartan during the period of use of NSAIDs. Usually this effect is reversible.

Other antihypertensive drugs may enhance the severity of the antihypertensive effect of losartan. With the simultaneous use of agents that reduce blood pressure, including as a side effect (for example, antipsychotics, tricyclic antidepressants, amifostine, baclofen), arterial hypotension may develop.

Patients who take Losartan along with other drugs that affect the RAAS, should carefully monitor kidney function, blood pressure and water-electrolyte balance. Do not appoint Losartan in combination with aliskiren in patients with renal insufficiency.

Terms and conditions of storage

Store at temperatures up to 25 ° C in a place protected from light and inaccessible to children.

Shelf life - 3 years.