Composition, form of production and packaging
The tablets covered with a film shell of white or almost white color, in the form of "heart", with a facet, with engraving "Z" on one side and "25" - on another.
1 tab.
Losartan potassium 25 mg
Excipients: starch, microcrystalline cellulose, sodium carboxymethyl starch, sodium lauryl sulfate, magnesium stearate, talc, silicon dioxide colloid, hypromellose, macrogol 6000.
7 pcs. - blisters (1) - packs of cardboard.
The tablets covered with a film shell of white or almost white color, in the form of "heart", with a facet, with engraving "Z" on one side and "50" - on another.
1 tab.
Losartan potassium 50 mg
Excipients: starch, microcrystalline cellulose, sodium carboxymethyl starch, sodium lauryl sulfate, magnesium stearate, talc, silicon dioxide colloid, hypromellose, macrogol 6000.
7 pcs. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
PHARMACHOLOGIC EFFECT
Antihypertensive drug, is a specific antagonist of angiotensin II receptors (subtype AT 1 ). He suppresses kinase II - an enzyme that destroys bradykinin. Reduces OPSS, concentration in the blood of adrenaline and aldosterone, blood pressure, pressure in a small circle of blood circulation; reduces afterload, has a diuretic effect.It interferes with the development of myocardial hypertrophy, increases tolerance to exercise in patients with heart failure.
After a single dose, the hypotensive effect (decrease of systolic and diastolic blood pressure) reaches a maximum after 6 hours, then gradually decreases within 24 hours.
The maximum hypotensive effect is achieved in 3-6 weeks after the start of the drug.
Pharmacological data indicate that the concentration of losartan in blood plasma in patients with cirrhosis of the liver is significantly increased, so patients with a history of liver disease should be used at a lower dose.
PHARMACOKINETICS
Absorption and Metabolism
Losartan is rapidly absorbed from the digestive tract. Bioavailability is about 33%. Subjected to the effect of "first passage" through the liver, it is metabolized by carboxylation with the participation of the CYP2C9 isoenzyme with the formation of an active metabolite. T max - losartan is 1 h, the active metabolite is 3-4 h.
Distribution
Binding to blood plasma proteins - 99%.
Excretion
T 1/2 of losartan is 1.5-2 hours and its main metabolite is 6-9 hours. About 35% of the dose is excreted in the urine, about 60% - through the intestine.
INDICATIONS
- arterial hypertension;
- chronic heart failure (as part of combination therapy, with intolerance or inefficiency of therapy with ACE inhibitors).
DOSING MODE
The drug is taken orally, regardless of food intake, the frequency of intake is 1 time / day.
With arterial hypertension, the average daily dose is 50 mg. In some cases, to achieve a greater effect, the dose is increased to 100 mg in 2 divided doses or 1 time / day.
The initial dose for patients with heart failure is 12.5 mg 1 time / day. Typically, the dose increases with a weekly interval (ie 12.5 mg / day, 25 mg / day and 50 mg / day) to an average maintenance dose of 50 mg 1 time / day, depending on the patient's tolerance of the drug.
When appointing the drug to patients receiving diuretics in high doses, the initial dose of losartan should be reduced to 25 mg 1 time / day.
It is not necessary to adjust the dose (including the initial dose) to elderly patients or patients with impaired renal function, including patients on hemodialysis.
Patients with impaired liver function should be prescribed lower doses of the drug.
Safety and efficacy of the drug in children are not established.
SIDE EFFECT
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, hyposthenia, migraine, tremor, ataxia, depression, fainting, ringing in the ears, taste disorder, vision change, conjunctivitis.
On the part of the respiratory system: 1% or more - nasal congestion, cough *, upper respiratory tract infections (elevated body temperature, sore throat, sinusopathy *, sinusitis, pharyngitis); less than 1% - dyspnea, bronchitis, rhinitis.
On the part of the digestive system: 1% or more - nausea, diarrhea *, dyspeptic phenomena *, abdominal pain; less than 1% - anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.
From the musculoskeletal system: 1% or more - convulsions, myalgia *, pain in the back, chest, legs; less than 1% - arthralgia, shoulder pain, knee, arthritis, fibromyalgia.
From the cardiovascular system: orthostatic hypotension (dose-dependent), palpitation, tachy- or bradycardia, arrhythmias, angina.
On the part of the genitourinary system: less than 1% - mandatory urination, urinary tract infections, renal dysfunction, weakening of libido, impotence.
Dermatological reactions: less than 1% - dry skin, erythema, blood flow, photosensitivity, increased sweating, alopecia.
Allergic reactions: less than 1% - hives, rash, itching, angioedema (including face, lips, pharynx and / or tongue).
Other: hyperkalemia (serum potassium more than 5.5 mmol / l), anemia.
* There are side effects, the incidence of which is comparable to placebo.
The association of side effects occurring with a frequency of less than 1% of cases with the use of losartan is not proven.
In most cases, losartan is well tolerated, side effects are transient and do not require withdrawal of the drug.
CONTRAINDICATIONS
- arterial hypotension;
- Hyperkalemia;
- dehydration;
- Pregnancy;
- lactation period;
- age under 18 years (effectiveness and safety not established);
- Hypersensitivity to the components of the drug.
With caution should prescribe the drug for hepatic and / or renal failure.
PREGNANCY AND LACTATION
There are no data on the use of losartan in pregnancy. However, it is known that drugs acting directly on the renin-angiotensin system, when used in the II and III trimesters of pregnancy, can cause a developmental defect or even the death of a developing fetus. Therefore, when pregnancy occurs, losartan should be discontinued immediately.
When appointing during lactation, a decision should be made to stop breastfeeding or stop treatment with losartan.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure.
SPECIAL INSTRUCTIONS
It is necessary to correct the dehydration before the appointment of losartan, or to begin treatment with the use of the drug in a lower dose.
Drugs that affect the renin-angiotensin system can increase the concentration of urea and serum creatinine in the blood in patients with bilateral renal stenosis or stenosis of the artery of a single kidney.
During the treatment period, the concentration of potassium in the blood should be monitored regularly, especially in elderly patients, with renal dysfunction.
OVERDOSE
Symptoms: marked decrease in blood pressure, tachycardia, because of parasympathetic (vagus) stimulation, bradycardia may appear.
Treatment: forced diuresis, symptomatic therapy; Hemodialysis is ineffective.
DRUG INTERACTION
Can be prescribed with other antihypertensive drugs.
There was no clinically significant interaction with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital.
In patients with dehydration (previous treatment with large doses of diuretics), there may be a marked decrease in blood pressure.
Strengthens (mutually) the effect of other antihypertensive drugs (diuretics, beta-adrenoblockers, sympatholytics).
Increases the risk of hyperkalemia when combined with potassium-sparing diuretics and potassium preparations.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a place protected from light, inaccessible to children, at a temperature of no higher than 25 В° C.
