He suppresses the kinase II – the enzyme that destroys bradykinin. Reduces the total peripheral vascular resistance (SVR), the blood concentration of adrenaline and aldosterone blood pressure (BP), the pressure in the pulmonary circulation; reduces afterload, it has a diuretic effect. It prevents the development of myocardial hypertrophy, increases exercise tolerance in heart failure patients.
After a single dose of the anavar hypotensive effect (reduced systolic and diastolic blood pressure) reaches a maximum after 6 hours, then for 24 hours, gradually decreasing.
The maximum antihypertensive effect is achieved within 3-6 weeks after starting the drug.
Pharmacological data indicate that losartan plasma concentration in patients with cirrhosis is significantly increased, so that patients with a history of liver disease should be used at a lower dose.
The pharmacokinetics of
losartan is rapidly absorbed from the gastrointestinal tract. Biodostupnost- about 33%. It has the effect of “first pass” through the liver, metabolized by carboxylation with the participation of isoenzyme of cytochrome P450 2C9 to the active metabolite. Contact with blood plasma proteins – 99%.
The time to reach maximum concentration of losartan 1 hour active metabolite 3-4 hours after ingestion. The half-life of 1.5 – 2 hours, and its main metabolite 6-9 hours, respectively. About 35% of the dose is excreted in the urine, about 60% – through the intestines.
Indications for use
- Arterial hypertension;
- Chronic heart failure (in a combination therapy, in case of intolerance or failure of therapy with ACE inhibitors).
- Hypersensitivity to the drug; –
- Pregnancy and lactation;
- Age 18 years (effectiveness and safety have been established).
Dosage and administration
Losartan is taken orally, regardless of food intake, the multiplicity of reception – 1 times per day.
When hypertension the average daily dose is 50 mg. In some cases, for greater effect dose increased to 100 mg in one or two doses per day.
The starting dose for patients with heart failure is 12.5 mg 1 time per 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 per day, depending on patient tolerability of the drug.
In appointing the drug to patients receiving high doses of diuretics, the initial dose of Losartan should be reduced to 25 mg 1 time per day. No need to adjust the dose in patients of advanced age or patients with impaired renal function, including patients on hemodialysis. Patients with impaired hepatic function should be prescribed lower doses of Losartan.
Elderly patients and patients with impaired renal function, including patients on dialysis, there is no need for initial dose adjustment.
Safety and efficacy have not been established in children.
* Marked side effects, anavar the incidence of which is comparable to placebo.
Communication of side effects occurring with a frequency of less than 1% of cases, has not been proved with the use of losartan.
In most cases, losartan is well tolerated, side effects are transient in nature and do not require discontinuation of therapy.
From the nervous system and sensory organs: 1% or more – dizziness, asthenia, headache, fatigue, insomnia; less than 1% – anxiety, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, gipostezii, migraine, tremor, ataxia, depression, syncope, tinnitus, taste disturbance, changes in vision, conjunctivitis.
The respiratory system: 1% or more – nasal congestion, cough *, upper respiratory tract infection (fever, sore throat, sinusopatiya *, sinusitis, pharyngitis), less than 1% – dyspnea, bronchitis, rhinitis.
On the part of the gastrointestinal tract: 1% or more – nausea, diarrhea *, dyspepsia *, abdominal pain; less than 1% -anoreksiya, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.
From the musculoskeletal system: 1% or more – cramps, myalgia *, back pain, chest, legs; less than 1% -artralgiya, shoulder pain, knee arthritis, fibromyalgia.
Since the cardiovascular system: orthostatic hypotension (dose-dependent), palpitations, tachy or bradycardia, arrhythmia, angina, anemia.
With the genitourinary system: less than 1% – urgent need to urinate, urinary tract infection, renal failure, weakening of libido, impotence.
For the skin: less than 1% – dry skin, erythema, flushing, photosensitivity, increased sweating, alopecia.
Allergic reaction: less than 1% – urticaria, rash, pruritus, angioedema, including face, lips, pharynx and / or language.
Other: hyperkalemia (serum potassium greater than 5.5 mmol / l).
Symptoms: marked reduction of blood pressure, tachycardia, due to parasympathetic (vagal) stimulation may occur bradycardia.
Treatment: forced diuresis, symptomatic therapy; Hemodialysis is ineffective.
Interactions with other drugs
may be administered with other antihypertensive agents. There was no clinically significant interaction with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital. In patients with dehydration (previous treatment with high doses of diuretics) may occur marked reduction in blood pressure. (Mutually) the effect of other antihypertensive agents (diuretics, beta-blockers, simpatolitikov). It increases the risk of hyperkalemia when combined with potassium-sparing diuretics and potassium preparations.
necessary to carry out the correction of dehydration to losartan or to start treatment with the drug at a lower dose. Drugs that affect the renin-angiotensin system may increase the concentration of urea in the blood and serum creatinine in patients with bilateral renal artery stenosis or stenosis of a solitary kidney. During treatment should regularly monitor the concentration of potassium in the blood, especially in elderly patients with renal impairment.
Pregnancy and lactation
Data on the use of losartan during pregnancy does not. However, it is known that drugs acting directly on the renin-angiotensin system, when used in the II and III trimester of pregnancy can cause defects or even death of the developing fetus. Therefore, anavar in the event of pregnancy, losartan should be stopped immediately.