Losartan - instructions for use, dose, side effects, contraindications

Competitive blockade of angiotensin II receptors. Internalization of receptors is possible. Blocks all the physiological effects of angiotensin II regardless of the source or route of synthesis. It does not bind or block receptors of other hormones and ion channels, which play an important role in regulating the function of the cardiovascular system. It does not inhibit the angiotensin-converting enzyme, which contributes to the degradation of bradykinin, so side effects mediated by bradykinin (eg, angioedema) are rare.

Pharmacokinetics:

Absorption - 35.8 ± 15.5%. V_d - 0,45 ± 0,24 l / kg. Biotransformation in the liver (CYP2C9, CYP3A4) to the active metabolite EXP-3174, possessing the properties of a non-competitive AT blocker₁receptors. The half-life of losartan is 2 hours. The connection with the plasma proteins of losartan is 98.7%. Clearance - 8.1 ± 1.8 ml / min (decreases with chronic renal failure, liver failure). Eliminated by the kidneys (35%, including 4% unchanged, 6% in the form of EXP-3174), with feces (60%). It is not excreted by hemodialysis.

Indications:

Arterial hypertension.

Reducing the risk of associated cardiovascular morbidity and mortality in patients with hypertension and left ventricular hypertrophy, manifested by a decrease in the total incidence of cardiovascular mortality, stroke and myocardial infarction.

Protection of the kidneys in patients with type 2 diabetes mellitus with proteinuria is a slowdown in the progression of renal failure, manifested by a decrease in the frequency of hypercreatininemia, the incidence of the terminal stage of chronic renal failure requiring hemodialysis or kidney transplantation, mortality rates, and a decrease in proteinuria.

Chronic heart failure with ineffective treatment with ACE inhibitors.

ICD-10

IV.E10-E14.E11.9 Non-insulin-dependent diabetes mellitus without complications

IX.I10-I15.I10 Essential [primary] hypertension

IX.I10-I15.I15 Secondary Hypertension

IX.I30-I52.I50.0 Congestive heart failure

XIV.N00-N08.N08.3 * Glomerular lesions in diabetes mellitus (E10-E14 + with the common fourth sign .2)

Contraindications:

Hypersensitivity, pregnancy, breast-feeding, children under 18 years of age, bilateral stenosis of the renal arteries, stenosis of the renal artery of a single kidney.

Carefully:

Arterial hypotension, hyperkalemia, dehydration, renal (hepatic) insufficiency.

Pregnancy and lactation:

Contraindicated in pregnancy and lactation.

FDA recommendation category D.

Dosing and Administration:

The average dose for oral administration is 50 mg once a day. If necessary, the dose may be reduced to 25 mg per day or increased to 100 mg per day, in the latter case, application of 2 times per day is possible.

Side effects:

Dizziness, upper respiratory tract infection, headache, unusual fatigue, dry cough, back pain, diarrhea, nasal congestion, insomnia, leg pain, cramps or muscle pain, sinusitis.

Overdose:

Bradycardia due to excitation of the vagus nerve, hypotension, tachycardia. There is no specific antidote.

Treatment: correction of hypotension, dehydration and electrolyte disorders.

Interaction:

Alcohol, diuretic drugs, drugs that reduce blood pressure - an increase in the hypotensive effect.

Non-steroidal anti-inflammatory drugs (especially indomethacin), estrogens, sympathomimetic drugs - weakening of the hypotensive effect.

Blood from blood banks (if stored for more than 10 days), ciclosporin, potassium-sparing diuretics, potassium-containing preparations, salt substitutes - hyperkalemia; it is often necessary to determine the concentration of potassium in the blood serum.

Special instructions:

Angiotensin II receptor antagonist of medium duration. The ancestor and the most studied drug from his group.

Positively affects endothelial dysfunction in patients with arterial hypertension.

Improves erectile function in patients with hypertension and sexual dysfunction.

Instructions

Losartan (Losartanum)