It prevents the development of myocardial hypertrophy, improves exercise tolerance in patients with chronic heart failure (CHF). Admission lozartana once daily resulted in a statistically significant reduction in systolic and diastolic blood pressure (BP).equipoise side effects uniformly controls the pressure throughout the day, with the antihypertensive effect corresponds to the natural circadian rhythm. Lowering blood pressure (BP) at the end of the action of the drug dose was approximately 70-80% at the peak of the effect of the drug, 5-6 hours after administration. .
Lozartan well absorbed from the gastrointestinal tract. Subject to significant metabolism in the “first pass” through the liver to form the active metabolite (EXP-3174) with a carboxylic acid and other inactive metabolites. The bioavailability is approximately 33%. The drug with food has no clinically significant impact on its serum concentrations. T Cmax – 1 hour after ingestion, and its active metabolite (EXP-3174.) – 3-4 hours
More than 99% lozartana and EXP-3174 binds to plasma proteins, mainly to albumin. Lozartana volume of distribution is 34 liters. Very poorly penetrates the blood-brain barrier.
Lozartan metabolized to form an active (EXP-3174), a metabolite (14%) and inactive, including two major metabolite produced by hydroxylation butyl group chain and less significant metabolite, N-2-tetrazol-glucuronide.
Plasma clearance lozartana and its active metabolite is about 10 ml / sec. (600 ml / min.) And 0.83 ml / sec. (50 ml / min.), Respectively. Renal clearance lozartana and its active metabolite is about 1.23 ml / sec. (74 ml / min.) And 0.43 ml / sec. (26 ml / min.). Lozartana and half-life of the active metabolite of 2 hours or 9.6 hours, respectively. Write mainly in the bile -58% -35% by the kidneys.
- Arterial hypertension.
- Reducing the risk of stroke in patients with hypertension and left ventricular hypertrophy.
- Chronic heart failure (in a combination therapy, in case of intolerance or failure of therapy with ACE inhibitors).
- Protection of renal function in patients with type 2 diabetes mellitus with proteinuria to reduce proteinuria, reduce the progression of renal disease, end-stage reduction of the risk (to prevent the need for dialysis, the probability of increasing the level of serum creatinine) or death.
: Hypersensitivity to lozartanu or to other components of the drug, hypotension, hyperkalemia, dehydration, pregnancy and lactation, age 18 years (effectiveness and safety have not been established), lactose intolerance, galactosemia or malabsorption syndrome glucose / galactose.
Precautions: hepatic and / or renal failure, decreased blood volume, fluid and electrolyte balance, bilateral renal artery stenosis or stenosis of the artery to a solitary kidney.
Pregnancy and lactation
Data on the use during pregnancy lozartana not. Fetal renal perfusion, which is dependent on the development of the renin-angiotensin system, begins to operate in the third trimester of pregnancy. The risk to the fetus increases when taking lozartana in the second and third trimesters. In establishing pregnancy lozartanom therapy should be discontinued immediately. No data on the allocation of lozartana in mother’s milk. Therefore, you should resolve the issue of termination of breastfeeding or cancellation lozartanom therapy, given its importance to the mother.
Dosing and Administration
Inside, regardless of the meal, the multiplicity of reception -1 once a day.
Arterial gipertetiya: the average daily dose is 50 mg. The maximum antihypertensive effects achieved within 3-6 weeks of therapy. Some patients may be more pronounced effect achieved by increasing the dose up to 100 mg per day in two steps or in one step.
In patients receiving high doses of diuretics Loristoy therapy is recommended to start with 25 mg per day in one portion. Elderly patients and patients with impaired renal function, including patients on hemodialysis, does not require correction of the initial dose.
No need to adjust the dose in patients of advanced age or patients with impaired renal function, including patients on hemodialysis.
Patients with impaired function liver should be prescribed lower doses of the drug.
Chronic heart failure: initial dose of 12.5 mg per day in one portion. In order to achieve the usual maintenance dose is 50 mg daily dose should be gradually increased at intervals of one week (for example, 12.5 mg, 25 mg, 50 mg for single dose per day). Lorista usually given in combination with diuretics and cardiac glycosides.
Dose should be increased as follows:
Week 1:. 1 to 7 day – 1 tablet of 12.5 mg once daily
2 weeks from 8 to 14 day – 1 tablet of 25 mg once a day.
3 Week .: from 15 to 21 days – 1 tablet of 50 mg once a day
4 weeks; 22 to 28 day – 1 tablet of 50 mg once a day.
Reducing the risk of stroke in patients with hypertension and left ventricular hypertrophy: the standard initial dose Loristy is 50 mg per day in one step. Further hydrochlorothiazide may be added in low doses and / or dose Loristy increased to 100 mg per day.
Renal protection in patients with type 2 diabetes mellitus with proteinuria: the standard initial dose Loristy is 50 mg per day in one step. The dose may be increased to 100 mg per day in terms of reduction in blood pressure.
Safety and efficacy have not been established in children.
In most cases, Lorista well tolerated, side effects are mild and transient and did not require discontinuation of therapy.
Blood system: rare anemia, purpura Shenlyayna-Henoch. Allergic reaction: less than 1% – hives, skin rash, itching, angioedema (including swelling of the larynx and tongue, causing airway obstruction and / or swelling of the face, lips, throat) . Sometimes angioedema previously developed while taking other drugs, including ACE inhibitors.
On the part of the central nervous system and sensory organs: 1% or more -golovokruzhenie, asthenia, headache, fatigue, insomnia; less than 1% -bespokoystvo, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, gipostezii, equipoise side effects migraine, tremor, ataxia, depression, syncope, tinnitus, taste disturbance, blurred vision, conjunctivitis.
Since the cardiovascular system: orthostatic hypotension (dose-dependent), palpitations, tachy-and bradycardia, arrhythmia, angina pectoris, vasculitis.
With the genitourinary system: less than 1% – urgent need to urinate, urinary tract infection, renal dysfunction, decreased libido, impotence.
The respiratory system: 1% or more – nasal congestion, cough *, infection of the upper respiratory tract, pharyngitis, dyspnea, bronchitis, swelling of the nasal mucosa.
On the part of the digestive tract: 1% or more – nausea, diarrhea *, dyspepsia *, abdominal pain; less than 1% – anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation, hepatitis, abnormal liver function.
For the skin: less than 1% – dry skin, erythema, photosensitivity, increased sweating, alopecia.
From the musculoskeletal system: 1% or more – cramps, myalgia *, back pain, chest, legs; less than 1% – arthralgia, arthritis, pain in the shoulder, knee, fibromyalgia.
Laboratory indicators: hyperkalemia; rare: a moderate increase in levels of urea and creatinine in blood serum; very rare: increase in liver enzymes, hyperbilirubinemia.
* – Marked side effects, the incidence of which is comparable to placebo.
Symptoms: marked reduction of blood pressure, tachycardia; as a result of parasympathetic (vagal) stimulation may develop bradycardia. Treatment: forced diuresis, symptomatic therapy. Hemodialysis is ineffective.
Interaction with other drugs
not mentioned any clinically significant drug interactions with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital, ketoconazole and erythromycin. During the simultaneous reception with rifampicin and fluconazole was observed decrease in the level of the active metabolite of potassium lozartana. The clinical implications of this phenomenon are unknown.
Simultaneous treatment with potassium-sparing diuretics (eg, spnronolakton, triamterene, amiloride) and potassium supplements increase the risk of hyperkalemia.
When co-administered with non-steroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 inhibitors can reduce the effect of diuretics and other antihypertensive agents.
If lozartan appointed concurrently with thiazide diuretics, blood pressure reduction lozartana potassium is approximately additive character. (Mutually) the effect of other antihypertensive agents (diuretics, beta-blockers, simpatolitikov).
Patients with decreased volume of circulating blood (for example, in the treatment with high doses of diuretics) may develop symptomatic hypotension. Prior to the reception lozartana necessary to remove existing disorders, or initiate therapy with small doses.
Patients with mild to moderate concentration lozartana cirrhosis and its active metabolite in blood plasma after oral administration higher than that of healthy people. Therefore patients with a history of liver disease therapy recommended lower doses.
In patients with impaired renal function, as a diabetic, and without it, often develop electrolyte disturbances (hyperkalemia), to which you should pay attention. However, only in rare cases, discontinue treatment due to hyperkalemia. During treatment should regularly monitor the concentration of potassium in the blood, especially in elderly patients with renal dysfunction.
Drugs acting on the renin-angiotensin system may increase the content of urea and serum creatinine in patients with bilateral or unilateral stenosis of the artery to a solitary kidney. Changes in renal function may be reversible upon discontinuation. In the period of treatment should regularly monitor the concentration of creatinine in the blood serum, at regular intervals. Effects on ability to drive equipoise side effects and other mechanical means: data on the effect lozartana on the ability to drive or other technical means available. oxydrolone for sale