Rileys-sanovel - instructions for use, dose, side effects, contraindications

Excipients: mannitol 41.319 mg, calcium phosphate dihydrate 124 mg, corn starch 31 mg, pregelatinized starch 4 mg, magnesium stearate 1.7 mg, ferric iron oxide red (E 172) 56 μg, ferric oxide yellow oxide (E 172) 145 μg.

Description:

Tablets 5, 10 mg: Flat, round tablets are white, with a risk on one side.

Tablets of 20 mg: Round, biconvex tablets of light pink with weak brownish shade of color, with a risk on one side.

Pharmacotherapeutic group:ACE inhibitor

ATX: & nbsp

C.09.A.A.03 Lisinopril

C.09.A.A ACE Inhibitors

Pharmacodynamics:

The ACE inhibitor reduces the formation of angiotensin II from angiotensin I. Reducing angiotensin II leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases the synthesis of prostaglandins. Reduces the overall peripheral vascular resistance, blood pressure (BP), preload, pressure in the pulmonary capillaries,causes an increase in the minute volume of blood and an increase in myocardial tolerance to loads in patients with chronic heart failure. Expands arteries more than veins. Some effects are explained by the effect on tissue renin-angiotensin systems. With prolonged use, myocardial hypertrophy and the walls of arteries of resistive type decrease. Improves the blood supply of the ischemic myocardium.

ACE inhibitors prolong life expectancy in patients with chronic heart failure, slow the progression of left ventricular dysfunction in patients who underwent myocardial infarction without clinical manifestations of heart failure.

The antihypertensive effect begins in about 6 hours and persists for 24 hours. The duration of the effect also depends on the size of the dose. The beginning of the action is after 1 hour. The maximum effect is determined in 6-7 hours. With arterial hypertension, the effect is observed in the first days after the start of treatment, stable action develops after 1-2 months. With a sharp withdrawal of the drug, no pronounced increase in blood pressure was observed.

In addition to reducing blood pressure lisinopril reduces albuminuria.

In patients with hyperglycemia contributes to the normalization of the function of the damaged glomerular endothelium.

Lizinopril does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not increase the incidence of hypoglycemia.

Pharmacokinetics:

Suction. Absorption is an average of 30%; bioavailability is 25%. Eating does not affect the absorption of the drug.

Distribution. Almost does not bind to blood plasma proteins. The maximum concentration in blood plasma (90 ng / ml) is achieved after 7 hours. Permeability through the blood-brain and placental barrier is low.

Metabolism. Lisinopril not biotransformed in the body.

Excretion. It is excreted by the kidneys unchanged. The half-life is 12 hours.

Pharmacokinetics in selected patient groups

In patients with chronic heart failure absorption, clearance of lininopril reduced.

In patients with renal insufficiency the concentration of lisinopril is several times higher than the concentration in the blood plasma in volunteers, with an increase in the time to reach the maximum concentration in the blood plasma and an increase in the half-life.

In elderly patients the concentration of the drug in the blood plasma and the area under the "concentration-time" curve is 2 times greater than in patients of a young age.

Indications:

- Arterial hypertension (in monotherapy or in combination with other antihypertensive agents);

- chronic heart failure (as part of combination therapy for the treatment of patients taking digitalis and / or diuretics).

Contraindications:

- Hypersensitivity to lisinopril or other ACE inhibitors, angioedema in the anamnesis, including the use of ACE inhibitors, hereditary edema of Quincke;

- age to 18 years (efficacy and safety not established).

Carefully:

Severe renal dysfunction, bilateral renal artery stenosis or arterial stenosis of a single kidney with progressive azotemia, condition after kidney transplantation, renal insufficiency, azotemia, hyperkalemia, aortic aortic stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including cerebral circulation insufficiency), ischemic heart disease, coronary insufficiency, autoimmune systemic connective tissue diseases (incl.scleroderma, systemic lupus erythematosus); oppression of bone marrow hematopoiesis; diet with sodium restriction; hypovolemic conditions (including as a result of diarrhea, vomiting); elderly age.

Pregnancy and lactation:

The use of lisinopril during pregnancy is contraindicated. When establishing a pregnancy, the drug should be stopped as soon as possible. ACE inhibitors in the II and III trimester of pregnancy has adverse effects on the fetus (expressed may decrease blood pressure, renal failure, hyperkalemia, skull hypoplasia, intrauterine death). Data on the negative effects of the drug on the fetus in case of application during the I trimester are not present.

For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, careful monitoring is recommended to timely detect a marked decrease in blood pressure, oliguria, and hyperkalemia.

Lizinopril penetrates the placenta. There is no data on the penetration of lisinopril into breast milk. For the period of treatment the drug should be abolished breastfeeding.

Dosing and Administration:

Inside, regardless of food intake.

With arterial hypertension patients who do not receive other antihypertensives are prescribed 5 mg once a day. In the absence of effect, the dose is increased every 2-3 days by 5 mg to an average therapeutic dose of 20-40 mg / day (increasing the dose above 40 mg / day usually does not lead to a further decrease in blood pressure). The usual daily maintenance dose is 20 mg. The maximum daily dose is 40 mg. The full effect usually develops in 2-4 weeks from the start of treatment, which should be taken into account when increasing the dose. With insufficient clinical effect, it is possible to combine the drug with other antihypertensive drugs.

If the patient received a preliminary treatment with diuretics, the use of such drugs should be stopped 2-3 days before the application of Rileys-sanovel. If this is not feasible, the initial dose of Rileys-sanovel should not exceed 5 mg per day. In this case, after taking the first dose, medical supervision is recommended for several hours (maximum effect is achieved after about 6 hours), since there may be a pronounced decrease in blood pressure.

With Renovascular Hypertension or other conditions with increased activity of the renin-angiotensin-aldosterone system, it is also advisable to prescribe a low initial dose of 2.5-5 mg per day,under the strengthened medical control (the control of a BP, functions of kidneys, concentration of a potassium in blood serum). The maintenance dose, continuing strict medical control, should be determined depending on the dynamics of blood pressure.

With renal insufficiency due to the fact that lisinopril is released through the kidneys, the initial dose should be determined depending on the creatinine clearance, then, in accordance with the reaction, a maintenance dose should be established in conditions of frequent monitoring of kidney function, potassium level, sodium in the blood serum.

Creatinine clearance ml / min	Initial dose of mg / day
30-70	5-10
10-30	2,5-5
less than 10 (including patients treated with hemodialysis)	2,5

With persistent arterial hypertension, prolonged maintenance therapy of 10-15 mg / day is shown.

With chronic heart failure - begin with 2.5 mg once a day, followed by an increase in the dose of 2.5 mg 3-5 days before the usual, maintaining a daily dose of 5-20 mg. The dose should not exceed 20 mg per day.

In elderly people often more pronounced prolonged hypotensive effect, which is associated with a decrease in the rate of excretion of lisinopril (it is recommended to begin treatment with 2.5 mg / day).

Side effects:

The most common side effects: dizziness, headache, fatigue, diarrhea, dry cough, nausea.

From the side of the cardiovascular system: marked decrease in blood pressure, chest pain; rarely - orthostatic hypotension, tachycardia, bradycardia, worsening of symptoms of heart failure, violation AV conduction, myocardial infarction, palpitations.

From the central nervous system: emotional lability, confusion, paresthesia, drowsiness.

On the part of the organs of hematopoiesis: leukopenia, neutropenia, agranulocytosis, thrombocytopenia, anemia (reduction of hemoglobin, hematocrit, erythropenia).

From the respiratory system: dyspnea, bronchospasm.

From the digestive system: dry mouth, anorexia, dyspepsia, changes in taste, abdominal pain, pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis.

From the skin: increased sweating, alopecia, photosensitivity.

From the genitourinary system: a violation of kidney function, oliguria, anuria, acute renal failure, uremia, proteinuria, decreased potency.

Allergic reactions: angioedema, facial edema, extremities, lips, tongue, epiglottis and / or larynx, skin rashes, urticaria, pruritus, fever, positive test results for antinuclear antibodies, increased ESR, eosinophilia, leukocytosis; very rarely - intestinal angioedema.

Other: asthenia, myalgia, arthralgia / arthritis, vasculitis, convulsive twitching of the muscles of the extremities and lips.

Laboratory indicators: hyperkalemia, hyponatremia; rarely - increased activity of "hepatic" enzymes, hyperbilirubinemia, hypercreatininaemia, increased urea concentration.

Overdose:

Symptoms (occur when taking a single dose of 50 mg): a marked decrease in blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability.

Treatment: symptomatic therapy, intravenous fluid administration, control of blood pressure, water-electrolyte balance and normalization of the latter.

Lizinopril can be removed from the body by hemodialysis.

Interaction:

Special care is required when using the drug simultaneously with:

- potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium, salt substitutes containing potassium (increases the risk of hyperkalemia), especially with impaired renal function, so they can be jointly administered only on the basis of an individual decision of the treating physician with regular monitoring of serum potassium and kidney function.

Cautiously can be applied together:

- with diuretics: with the additional administration of a diuretic to a patient receiving lisinopril, as a rule, there is an additive antihypertensive effect - the risk of a pronounced decrease in blood pressure;

- with other antihypertensive agents (additive effect);

- with non-steroidal anti-inflammatory drugs (including selective inhibitors of COX-2), estrogens, as well as adrenostimulators - a decrease in antihypertensive action of lisinopril;

- with lithium (liberation of lithium may decrease, therefore, the concentration of lithium in serum should be monitored regularly);

- with antacids and colestyramine - reduced absorption in the gastrointestinal tract.

With simultaneous use of ACE inhibitors and preparations of gold (sodium aurotomy malate) describes a symptom complex, which includes facial flushing, nausea, vomiting and lowering blood pressure.

Insulin and oral hypoglycemic drugs are a risk of developing hypoglycemia.

Alcohol enhances the effect of the drug.

Lizinopril reduces the excretion of potassium from the body when treated with diuretics.

Special instructions:

Symptomatic hypotension

Most often, a marked decrease in blood pressure occurs with a decrease in fluid volume caused by diuretic therapy, a decrease in salt in food, dialysis, diarrhea, or vomiting.

In patients with chronic heart failure with simultaneous renal insufficiency or without it, a marked decrease in blood pressure is possible. It is more often detected in patients with a severe stage of chronic heart failure, as a result of the use of large doses of diuretics, hyponatremia or impaired renal function. In such patients treatment Rileysom-sanovel should be started under the strict supervision of a doctor (with care to select the dose of the drug and diuretics).

Similar rules should be adhered to when appointing patients with ischemic heart disease, cerebrovascular insufficiency,in whom a sharp decrease in blood pressure can lead to myocardial infarction or stroke.

Transient hypotensive reaction is not a contraindication for taking the next dose of the drug.

When Rileys-sanovel is used, in some patients with chronic heart failure, but with normal or low blood pressure, there may be a decrease in blood pressure, which is usually not a reason for stopping treatment.

Before the start of treatment, Rileys-sanovel, if possible, should normalize the sodium concentration and / or replenish the lost volume of the liquid, carefully monitor the effect of the initial dose of Rileys-sanovel on the patient.

In the case of stenosis of the renal artery (especially with bilateral stenosis, or in the presence of stenosis of the artery of a single kidney), as well as inadequate circulation due to lack of sodium and / or liquid, the use of Rileys-sanovel can lead to impaired renal function, acute renal failure, which is usually irreversible after drug discontinuation.

Surgery / general anesthesia

With extensive surgical interventions, as well as with the use of other drugs that cause a decrease in blood pressure, lisinopril, blocking the formation of angiotensin II, can cause a pronounced unpredictable decrease in blood pressure.

In elderly patients the same dose leads to a higher concentration of the drug in the blood, therefore special caution is required when determining the dose.

Because the potential risk of agranulocytosis can not be ruled out, periodic monitoring of the blood picture is required.

When the drug is used in dialysis with a polyacryl-nitrile membrane, anaphylactic shock can occur, so either a different type of dialysis membrane or other antihypertensive agents is recommended.

Effect on the ability to drive transp. cf. and fur:

There is no data on the effect of lisinopril on the ability to drive vehicles and mechanisms, applied in therapeutic doses, but it must be borne in mind that dizziness may occur, therefore, care must be taken.

Form release / dosage:Tablets, 5, 10 and 20 mg.

Packaging:

For 14 tablets in a blister of PVC-aluminum foil.

For 2 blisters in a cardboard pack together with instructions for use

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003168/09

Date of registration:24.05.2009 / 18.10.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sanovel Pharmaco-industrial trading companySanovel Pharmaco-industrial trading company Turkey

Manufacturer: & nbsp

SANOVEL PHARMACEUTICAL PRODUCTS IND., Inc. Turkey

Representation: & nbspSANOVEL branch of the company pharmaco-industrial trading companySANOVEL branch of the company pharmaco-industrial trading companyRussia

Information update date: & nbsp17.12.2016

Illustrated instructions

Instructions

Rileys-sanovel (Rilace-sanovel)