Lizinopril Canon - instructions for use, dose, side effects, contraindications

Composition:Dosage 5 mg
1 tablet contains:
active substance: lisinopril dihydrate - 5.44 mg, in terms of lisinopril - 5 mg; Excipients: calcium hydrophosphate dihydrate - 33 mg, corn pregelatinized corn starch - 23.36 mg, croscarmellose sodium (impellose) - 2 mg, magnesium stearate - 0.7 mg, microcrystalline cellulose - 35.5 mg.
Dosage of 10 mg
1 tablet contains:
active substance: lisinopril dihydrate-10.88 mg, calculated as lisinopril-10 mg; Excipients: calcium hydrogen phosphate dihydrate 46 mg, corn pregelatinised corn starch 29.12 mg, croscarmellose sodium (impellose) 3 mg, magnesium stearate 1 mg, microcrystalline cellulose 50 mg.
Dosage of 20 mg
1 tablet contains:
active substance: lisinopril dihydrate - 21.76 mg, in terms of lisinopril - 20 mg; Excipients: calcium hydrophosphate dihydrate - 65 mg, corn pregelatinized corn starch - 35.74 mg, croscarmellose sodium (impellose) - 4 mg, magnesium stearate -1.5 mg, microcrystalline cellulose - 72 mg.

Description:Tablets are white or almost white in color, round, flat-cylindrical with a facet and a risk. Marble is allowed.

Pharmacotherapeutic group:Angiotensin-converting enzyme (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., Decreases total peripheral vascular resistance (TPR), blood pressure (BP), preload, the pressure in the pulmonary capillaries, causes an increase in cardiac output and increase tolerance to myocardial stress in patients with chronic heart failure. Expands arteries more than veins. Some effects are explained by the effect on the renin-angiotensin-aldosterone system (PASC). 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 onset of action is after 1 hour. The maximum antihypertensive effect is achieved after 6-7 hours and persists for 24 hours. With arterial hypertension, the effect is observed in the first days after the start of treatment, stable effect develops in 1-2 months. With a sharp withdrawal of the drug, there was no pronounced increase in blood pressure.
In addition to reducing blood pressure lisinopril reduces albuminuria.

Pharmacokinetics:Suction. After oral administration lisinopril absorbed from the gastrointestinal tract (GIT) on average by 25%, but the absorption can vary from 6 to 60%. Bioavailability is 29%. Eating does not affect the absorption of the drug.
Distribution. Almost does not bind to blood plasma proteins. The maximum concentration in the blood plasma of 90 ng / ml is reached after 7 hours. Permeability through the blood-brain and placental barrier is low.
Metabolism. Lizinopril is not biotransformed in the body.
Excretion. It is excreted by the kidneys unchanged. The half-life is 12h.
Pharmacokinetics in selected patient groups
In patients with chronic heart failure, the absorption and clearance of lisinopril are reduced, bioavailability is 16%.
In patients with renal failure (creatinine clearance (CC) of less than 30 ml / min), the concentration of lisinopril is several times the concentration in plasma in healthy volunteers, the marked increase in the time to reach maximum plasma concentration and increased 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 young patients. In elderly patients, the concentration of lisinopril in the blood is increased by an average of 60%.
In patients with liver cirrhosis, the bioavailability of lisinopril is reduced by 30%, and the clearance by 50% compared to patients with normal liver function.

Indications:- Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);
- Chronic heart failure (as part of combination therapy for the treatment of patients taking cardiac glycosides and / or diuretics);
- Early treatment of acute myocardial infarction in combination therapy (within the first 24 hours with stable hemodynamic parameters to maintain
these indicators and prevention of left ventricular dysfunction and heart failure);
- Diabetic nephropathy (decreased albuminuria in patients with type 1 diabetes mellitus with normal BP, and patients with type 2 diabetes mellitus with hypertension).

Contraindications:- Hypersensitivity to lisinopril or other ACE inhibitors or excipients;
- angioedema in history, including the use of ACE inhibitors;
- Hereditary edema Quincke or idiopathic angioedema;
- age under 18 years (effectiveness and safety not established);
- Pregnancy;
lactation period.

Carefully:Severe renal dysfunction, bilateral renal artery stenosis or arterial stenosis of a single kidney with progressive azotemia, condition after kidney transplantation, azotemia, hyperkalemia, aortic aortic stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including insufficiency cerebral circulation), ischemic heart disease, coronary insufficiency, autoimmune systemic diseases of connective tissue (including sclerocystis (systemic lupus erythematosus), oppression of bone marrow hematopoiesis, diet with restriction of table salt, hypovolemic conditions (including as a result of diarrhea, vomiting), elderly age, hemodialysis using high-permeability dialysis membranes with high permeability (AN69®).

Pregnancy and lactation:The use of lisinopril during pregnancy is contraindicated. When you are pregnant, you should stop taking Lysinopril Canon as soon as possible. Admission of ACE inhibitors in the II and III trimester of pregnancy has an adverse effect on the fetus (there may be a marked decrease in blood pressure, renal failure, hyperkalemia, hypoplasia of the skull bones, fetal 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 isolation of lisinopril in breast milk. If taking Lisinopril Canon is necessary during lactation, then breastfeeding should be discarded.

Dosing and Administration:Inside, regardless of food intake, preferably at the same time.
With arterial hypertension in patients who do not receive other antihypertensive drugs, apply 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 therapeutic 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 use of the drug Lysinopril Canon. If this is not possible, the initial dose of Lysinopril Canon should not exceed 5 mg per day. In this case, after taking the first dose, medical supervision is recommended for several hours (the 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 use a low initial dose of 2.5-5 mg (1/2 - 1 tablet of 5 mg) per day, under enhanced medical supervision (blood pressure control, kidney function ,the content of potassium ions in the 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 excreted by the kidneys, the initial dose should be determined depending on the creatinine clearance. Further, the choice of doses should be made in - depending on individual reactions with regular monitoring of kidney function, potassium, sodium in the blood serum.

Creatinine clearance, ml / min	Initial dose, mg / day
30-70	5-10
10-30	2,5-5
Less than 10	2,5

(including patients on hemodialysis)
With persistent arterial hypertension, prolonged maintenance therapy of 10-15 mg / day is shown.
In chronic heart failure (as part of combination therapy to treat patients taking cardiac glycosides and / or diuretics), treatment is started with 2.5 mg (1/2 tablets 5 mg) once a day, followed by a dose increase through a 3- 5 days to 5-10 mg. The maximum daily dose is -20 mg.
Early treatment of acute myocardial infarction (as part of combination therapy) - on the first day - 5 mg orally, then 5 mg every other day, 10 mg after two days and then 10 mg once a day. In patients with acute myocardial infarction, the drug should be applied for at least 6 weeks.
At the beginning of treatment or within the first 3 days after an acute myocardial infarction in patients with low systolic blood pressure (120 mm Hg or lower), a smaller dose of 2.5 mg (1/2 tablets of 5 mg) should be used. In the case of a decrease in blood pressure (systolic blood pressure is less than or equal to 100 mm Hg), a daily dose of 5 mg can, if necessary, be reduced to 2.5 mg (1/2 tablet 5 mg each).
In the case of a prolonged severe decrease in blood pressure (systolic blood pressure less than 90 mm Hg for more than 1 hour), treatment with Lysinopril Canon should be discontinued.
Diabetic Nephropathy - In patients with type 2 diabetes mellitus, 10 mg of the drug Lizinopril Canon once a day is used. The dose may, if necessary, be increased to 20 mg once a day in order to achieve diastolic blood pressure values below 75 mmHg. in the "sitting" position. In patients with type 1 diabetes, the dose is the same, in order to achieve diastolic blood pressure values below 90 mm Hg. in the "sitting" position.

Side effects:The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%.
From the cardiovascular system: often - marked decrease in blood pressure, orthostatic hypotension; infrequently - acute myocardial infarction, tachycardia, palpitation; Raynaud's syndrome; rarely - bradycardia, tachycardia, aggravation of symptoms of CHF, violation of atrioventricular conduction, chest pain.
From the central nervous system: often - dizziness, headache; infrequently - lability of mood, paresthesia, sleep disturbance, stroke; rarely - confusion, asthenic syndrome, convulsive twitching of the muscles of the limbs and lips, drowsiness.
From the hemopoietic system and lymphatic system: rarely - reduction of hemoglobin, hematocrit; very rarely - leukopenia, neutropenia, agranulocytosis, thrombocytopenia, eosinophilia, erythropenia, hemolytic anemia, lymphadenopathy, autoimmune diseases.
From the respiratory system: often - cough, infrequently - rhinitis, very rarely - sinusitis, bronchospasm, allergic alveolitis / eosinophilic pneumonia, dyspnea.
From the digestive system: often diarrhea, vomiting; infrequently - indigestion, changes in taste, abdominal pain; rarely dryness of the oral mucosa; very rarely - pancreatitis,jaundice (hepatocellular or cholestatic), hepatitis, hepatic insufficiency, intestinal edema, anorexia.
From the skin: infrequently - itchy skin, rash; rarely - angioedema, swelling of the face, limbs, lips, tongue, larynx, urticaria, alopecia, psoriasis; Very rarely - increased sweating, vasculitis, pemphigus, photosensitivity, toxic epidermal necrolysis (Lyell syndrome), erythema multiforme, Stevens-Johnson syndrome.
From the urinary system: often - renal dysfunction; infrequently uremia, acute renal failure; very rarely - anuria, oliguria proteinuria.
On the part of the reproductive system: infrequent impotence, rarely - gynecomastia.
From the side of metabolism: very rarely - hypoglycemia.
From the laboratory indicators: infrequent increase of urea concentration in the blood, hypercreatininaemia, hyperkalemia, increased activity of "hepatic" transaminases, rarely - hyperbilirubinemia, hyponatremia, increased erythrocyte sedimentation rate, false positive results of antinuclear antibodies test.
From the musculoskeletal system: rarely - arthralgia / arthritis, myalgia.

Overdose:Symptoms: pronounced blood pressure lowering, dryness of the oral mucosa, drowsiness, urinary retention, constipation, anxiety, increased irritability, disturbance of water-electrolyte balance, renal failure, rapid breathing, tachycardia, palpitations, bradycardia, dizziness, anxiety, cough.
Treatment: there is no specific antidote. Symptomatic therapy.
Gastric lavage, application of enterosorbents and laxatives. Intravenous introduction of 0.9% sodium chloride solution was shown. In the case of a sustained bradycardia, the use of an artificial pacemaker is necessary. It is necessary to monitor blood pressure, indicators of water-electrolyte balance. Lisinopril can be removed from the body by hemodialysis. When hemodialysis is carried out using high-flow membranes, anaphylactoid reactions may develop.

Interaction:With the simultaneous use of the drug with potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone), potassium preparations, salt substitutes containing potassium, cyclosporine, increases the risk of hyperkalemia, especially with impaired renal function, so they can be used together only with regular monitoring of potassium in the blood serum and kidney function.
Simultaneous use of lisinopril with beta adrenoblockers, blockers of "slow" calcium channels (BCCC), diuretics, and other antihypertensive drugs increases the severity of antihypertensive action of the drug.
With the simultaneous use of the drug with tricyclic antidepressants, antipsychotics, general anesthetic agents, muscle relaxants, the antihypertensive effect of the drug is increasing.
Sympathomimetics may reduce the antihypertensive efficacy of lisinopril.
Lizinopril slows down the excretion of lithium preparations. Therefore, with simultaneous use, it is necessary to regularly monitor the concentration of lithium in the blood serum.
Antacids and colestramine reduce the absorption of lisinopril in the gastrointestinal tract.
When combined with insulin and hypoglycemic drugs for oral administration, there is a risk of developing hypoglycemia.
Non-steroidal anti-inflammatory drugs (NSAIDs) (incl.selective inhibitors of cyclooxygenase-2 (COX-2)), estrogens, adrenomimetics reduce the antihypertensive effect of lisinopril.
With simultaneous use of ACE inhibitors and preparations of gold intravenously (sodium aurotomy malate) describes a symptom complex, which includes facial flushing, nausea, vomiting and lowering blood pressure.
When combined with selective serotonin reuptake inhibitors, it can lead to severe hyponatraemia.
Joint application with allopurinol, procainamide, cytostatics can lead to leukopenia.

Special instructions:Symptomatic arterial hypotension
Most often, a marked decrease in blood pressure arises with a decrease in the volume of circulating blood (BCC), caused by diuretic therapy, reduction of table 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.
Under the strict supervision of a doctor, lisinopril patients with ischemic heart disease, cerebrovascular insufficiency, in whom a sharp decrease in blood pressure can lead to myocardial infarction or to a stroke.Transient arterial hypotension is not a contraindication for taking the next dose of the drug.
When using Lysinopril Canon, 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 the reason for stopping treatment.
Before the start of treatment with the drug, if possible, should normalize the sodium content and / or make up the BCC, carefully monitor the effect of the initial dose of Lysinopril Canon on the patient.
In the case of stenosis of the renal arteries (in particular, with bilateral stenosis or in the presence of stenosis of the artery of a single kidney), as well as in case of circulatory failure due to a lack of sodium and / or liquid ions, the use of the drug Lizinopril Canon can lead to impaired renal function, acute renal failure, which is usually irreversible even after drug withdrawal.
With acute myocardial infarction
The use of standard therapy (thrombolytics, acetylsalicylic acid as an antiaggregant agent, beta-blockers). Lisinopril it is possible to use together with intravenous administration or with the use of therapeutic transdermal systems of nitroglycerin.
Surgery / general anesthesia
Before surgery (including dental surgery), you should inform your doctor / anesthesiologist about the use of an ACE inhibitor. With extensive surgical interventions, as well as with the use of other means 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 use of standard doses leads to a higher concentration of lisinopril in the blood, therefore special care is required in determining the dose, despite the fact that there is no difference in the antihypertensive effect of Lysinopril Canon in elderly and young patients. It is not recommended to use Lysinopril Canon in patients who underwent acute myocardial infarction if systolic blood pressure does not exceed 100 mm Hg. Art.
Because the potential risk of agranulocytosis can not be ruled out, periodic monitoring of the blood picture is required.
Allergic reactions
In patients taking ACE inhibitors while carrying out desensitization of the venom, hymenoptera (Hymenoptera) is extremely rare, the appearance of a life threatening anaphylactoid reaction is possible. It is necessary to temporarily stop treatment with an ACE inhibitor before starting the course of desensitization.
It is possible "the occurrence of anaphylactoid reactions while hemodialysis is carried out using high-flow membranes (including AN69®). Another type of membrane for dialysis or another antihypertensive agent should be considered.
Possible development of anaphylactoid reactions in the conduct of apheresis with low-density lipoproteins (LDL).
Angioedema, swelling of the face, limbs, lips, tongue can occur during any period of treatment, requires withdrawal of the drug, the use of antihistamines and monitoring of the patient by the doctor until the symptoms regress completely. Angioedema with edema of the larynx can be the cause of airway obstruction and, as a result, a lethal outcome. It is necessary to carry out emergency therapy (0.3-0.5 ml of a 1: 1000 solution of epinephrine (epinephrine) subcutaneously) and provide airway patency.

Effect on the ability to drive transp. cf. and fur:There is no evidence of the effect of the drug Lisinopril Canon on the ability to drive vehicles and mechanisms, applied in therapeutic doses. However, it must be borne in mind that it is possible to develop arterial hypotension, which can affect the ability to drive vehicles and work with potentially dangerous mechanisms, and possibly lead to dizziness and drowsiness, so you should be careful.

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

Packaging:By 7, 10, 28 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
According to 2.4, 8 contour cell packs of 7 tablets or 1, 2, 3, 6 contour cell packs of 10 tablets, or 1, 2 contourcell packs of 28 tablets, or 1, 2, 3 contour mesh packs of 30 tablets together with instructions for use are placed in a pack of cardboard.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000905

Date of registration:18.10.2011

Expiration Date:18.10.2016

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp2016-11-16

Illustrated instructions

Instructions

Lizinopril Canon (Lisinopril Canon)