Composition, form of production and packaging
Tablets are brownish-pink in color, round, convex, with a notch on one side, with impregnations of a lighter and darker color.
1 tab.
lisinopril dihydrate 5.44 mg,
which corresponds to the content of lisinopril 5 mg
Excipients: calcium hydrophosphate dihydrate, mannitol, corn starch, croscarmellose sodium, magnesium stearate, iron oxide red dye (E172).
7 pcs. - blisters (1) - packs of cardboard.
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (3) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.
7 pcs. - blisters (5) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (4) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
Tablets are brownish-pink in color, round, convex, with a notch on one side, with impregnations of a lighter and darker color.
1 tab.
lisinopril dihydrate 10.89 mg,
which corresponds to the content of lisinopril 10 mg
Excipients: calcium hydrophosphate dihydrate, mannitol, corn starch, croscarmellose sodium, magnesium stearate, iron oxide red dye (E172).
7 pcs. - blisters (1) - packs of cardboard.
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (3) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.
7 pcs. - blisters (5) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (4) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
Tablets are brownish-pink in color, round, convex, with a notch on one side, with impregnations of a lighter and darker color.
1 tab.
lisinopril dihydrate 21.78 mg,
which corresponds to the content of lisinopril 20 mg
Excipients: calcium hydrophosphate dihydrate, mannitol, corn starch, croscarmellose sodium, magnesium stearate, iron oxide red dye (E172).
7 pcs. - blisters (1) - packs of cardboard.
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (3) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.
7 pcs. - blisters (5) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (4) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
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 OPSS, AD, preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and increased tolerance of the myocardium 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 approximately 6 hours later and persists for 24 hours. The duration of the effect also depends on the amount of the dose. The onset of action is after 1 hour. The maximum effect is determined after 6-7 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, 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
After taking the drug inside about 25% of lisinopril is absorbed from the digestive tract. C max is achieved after 7 hours and is 90 ng / ml.
Eating does not affect the absorption of the drug. Absorption is on average 30%, bioavailability is 29%.
Distribution
Almost does not bind to blood plasma proteins. Permeability through the BBB and the placental barrier is low.
Metabolism
Lizinopril is not biotransformed in the body.
Excretion
It is excreted by the kidneys unchanged. T 1/2 is 12 hours.
Pharmacokinetics in special clinical cases
In patients with chronic heart failure, the absorption and clearance of lisinopril are reduced.
In patients with renal failure, the concentration of lisinopril is several times higher than the plasma concentration in volunteers, with an increase in the time to reach Cmax in the blood plasma and an increase in T 1/2 .
In elderly patients, the concentration of the drug in blood plasma and AUC is 2 times greater than in patients of a young age.
INDICATIONS
- arterial hypertension (as a monotherapy or in combination with other antihypertensive agents);
- Chronic heart failure (as part of combination therapy to treat patients taking digitalis and / or diuretics);
- early treatment of acute myocardial infarction (within the first 24 hours with stable hemodynamic parameters to maintain these parameters and prevention of left ventricular dysfunction and heart failure);
- Diabetic nephropathy (decrease in albuminuria in insulin-dependent patients with normal BP and insulin-independent patients with arterial hypertension).
DOSING MODE
The drug is taken orally, regardless of food intake.
With arterial hypertension, patients who do not receive other antihypertensive drugs 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 more than 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 taking of such drugs should be stopped 2-3 days before the application of Diropress. If this is not feasible, then the initial dose of the drug Diropress should not exceed 5 mg / day. In this case, after taking the first dose, medical supervision is recommended for several hours (maximum effect is achieved after about 6 hours), because a marked decrease in blood pressure may occur.
In the case of renovascular hypertension or other conditions with increased activity of RAAS, it is advisable to administer the drug at the same low dose, 2.5-5 mg / day, under the enhanced supervision of a physician (control of blood pressure, renal function, potassium concentration in blood serum). The maintenance dose under strict supervision of the physician should be determined depending on the dynamics of blood pressure.
In case of renal insufficiency , since lisinopril is excreted by the kidneys, the initial dose should be determined depending on the QC. Further, the dose should be selected depending on the individual reaction under frequent control of kidney function, potassium level, sodium in the blood serum.
CK (ml / min) Initial dose (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.
In chronic heart failure, the initial dose is 2.5 mg 1 time / day, followed by a 2.5 mg dose increase 3-5 days before the usual maintenance dose of 5-20 mg. The dose should not exceed 20 mg / day.
In elderly people , a more pronounced prolonged hypotensive effect is often observed, which is associated with a decrease in the rate of excretion of lisinopril (it is recommended to start treatment with 2.5 mg / day).
In 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 1 time / day. In patients with acute myocardial infarction, the drug should be used for at least 6 weeks. At the beginning of treatment or within the first 3 days after acute myocardial infarction in patients with low systolic blood pressure (120 mm Hg or lower), the drug should be administered at a lower dose of 2.5 mg. In the case of a decrease in blood pressure (systolic blood pressure is below or equal to 100 mm Hg), a daily dose of 5 mg can, if necessary, temporarily reduce to 2.5 mg. In the case of a long pronounced decrease in blood pressure (systolic blood pressure below 90 mm Hg for more than 1 hour), treatment with Diropress should be stopped.
With diabetic nephropathy in patients with insulin-dependent diabetes mellitus, Diropress is prescribed at a dose of 10 mg 1 time / day. The dose can, if necessary, be increased to 20 mg 1 time / day in order to achieve diastolic blood pressure values ​​below 75 mm Hg. in the sitting position. In patients with non-insulin-dependent diabetes mellitus, the dose is the same, in order to achieve diastolic blood pressure values ​​below 90 mm Hg. in the sitting position.
SIDE EFFECT
Determination of the frequency of side effects: often (? 1%), rarely (<1%).
Most often: dizziness, headache, fatigue, dry cough, nausea, diarrhea.
From the immune system: (0.1%) angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities).
From the side of the cardiovascular system: often - a marked decrease in blood pressure, orthostatic hypotension; rarely - chest pain, tachycardia, bradycardia, aggravation of heart failure symptoms, violation of AV conduction, myocardial infarction.
From the side of the central nervous system: often - paresthesia, lability of mood, confusion, drowsiness, convulsive twitching of the muscles of the extremities and lips; rarely - asthenic syndrome.
On the part of the hematopoiesis system: rarely - leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with long-term treatment - anemia (a small decrease in the concentration of hemoglobin and hematocrit, erythrocytopenia).
From the respiratory system: rarely - dyspnea, bronchospasm.
Laboratory indicators: often - hyperkalemia, hyponatremia; sometimes - hyperbilirubinemia, increased activity of hepatic enzymes, increased serum urea and creatinine levels.
On the part of the digestive system: rarely - dry mouth, anorexia, dyspepsia, taste changes, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis.
Dermatological reactions: rarely - hives, increased sweating, pruritus, alopecia, photosensitivity.
From the urinary system: rarely - a violation of kidney function, oliguria, anuria, acute renal failure, uremia, proteinuria.
Allergic reactions: rarely angioedema, swelling of the face, extremities, lips, tongue, epiglottis and / or larynx, skin rashes, itching, fever, positive test results for antinuclear antibodies, increased ESR, eosinophilia, leukocytosis; very rarely - interstitial angioedema.
Other: rarely - decreased potency, myalgia, arthralgia / arthritis, vasculitis.
CONTRAINDICATIONS
- angioedema in the anamnesis, incl. and on the use of ACE inhibitors;
- hereditary edema of Quincke;
- age under 18 years (effectiveness and safety not established);
- hypersensitivity to the components of the drug;
- Hypersensitivity to other ACE inhibitors.
With caution should be used in patients with severe renal dysfunction, bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney with progressive azotemia, in a state after kidney transplantation, in renal insufficiency, azotemia, hyperkalaemia, aortic aortic stenosis, hypertrophic obstructive cardiomyopathy, in primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including cerebral circulatory insufficiency), with IHD, coronary nedos atochnosti, autoimmune systemic connective tissue diseases (including scleroderma, SLE); when oppression of bone marrow hematopoiesis; on the background of a diet with sodium restriction, with hypovolemic conditions, (including as a result of diarrhea, vomiting); in elderly patients.
PREGNANCY AND LACTATION
The use of the drug Diropress during pregnancy is contraindicated.
Lizinopril penetrates the placental barrier. When establishing a pregnancy, the drug should be stopped 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, skull hypoplasia, 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.
It is not known whether lisinopril is excreted in breast milk. For the period of treatment the drug should be abolished breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in patients with severe renal dysfunction, bilateral stenosis of the renal arteries, or stenosis of the artery of a single kidney with progressive azotemia, in a condition after kidney transplantation, with renal failure, and azotemia.
APPLICATION FOR CHILDREN
Contraindication: age under 18 years (efficacy and safety not established).
APPLICATION IN ELDERLY PATIENTS
In elderly people , a more pronounced prolonged hypotensive effect is often observed, which is associated with a decrease in the rate of excretion of lisinopril (it is recommended to start treatment with 2.5 mg / day).
SPECIAL INSTRUCTIONS
Symptomatic hypotension
Most often, a marked decrease in blood pressure occurs with a decrease in bcc caused by diuretic therapy, a decrease in the amount of 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.
Diropress should be administered under strict medical supervision to patients with IHD, cerebrovascular insufficiency, in whom a sharp decrease in blood pressure can lead to myocardial infarction or stroke.
Transient arterial hypotension is not a contraindication for taking the next dose of the drug.
With the use of the drug Diropress 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 discontinuing treatment.
Before starting treatment with Diropress, if possible, normalize the concentration of sodium and / or replenish the BCC, carefully monitor the effect of the initial dose of Diropress 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 Diropress can lead to impaired renal function, acute renal failure, which usually is irreversible after drug discontinuation.
With acute myocardial infarction
The use of standard therapy (thrombolytics, acetylsalicylic acid, beta-adrenoblockers) is shown. Diropress can be used in conjunction with intravenous administration or with the use of therapeutic transdermal systems of nitroglycerin.
Surgery / general anesthesia
With extensive surgical interventions, as well as using 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 polyacrylonitrile membrane, anaphylactic shock may occur, so either a different type of dialysis membrane or other antihypertensive agents is recommended.
Impact on the ability to manage vehicles and mechanisms
There is no data on the effect of the drug Diropress on the ability to drive vehicles and mechanisms, applied in therapeutic doses, but it must be taken into account that there may be dizziness, so you should be careful.
OVERDOSE
Symptoms (occur when taken in a single dose of 50 mg): a marked decrease in blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability. There is no specific antidote.
Treatment: gastric lavage, use of enterosorbents and laxatives, intravenous injection of 0.9% sodium chloride solution. In the case of treatment-resistant bradycardia, the use of a pacemaker is necessary. It is necessary to monitor blood pressure, water-electrolyte balance. Lizinopril can be removed from the body by hemodialysis.
DRUG INTERACTION
With the simultaneous use of the drug Diropress with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt potassium-substituted substitutes, with cyclosporine, the risk of hyperkalemia increases, especially with impaired renal function. The doctor decides individually the need for a joint appointment under regular control of potassium level in the blood serum and kidney function.
With the combined use of lisinopril with beta adrenoblockers, slow calcium channel blockers, diuretics, tricyclic antidepressants, and other agents that reduce blood pressure, increases the severity of blood pressure lowering.
Lizinopril slows the excretion of lithium. Therefore, when combined with lithium preparations, it is necessary to regularly monitor the concentration of lithium in the blood serum.
Antacids and colestyramine reduce the absorption of lisinopril from the gastrointestinal tract.
When used simultaneously with insulin and hypoglycemic agents for oral administration, there is a risk of developing hypoglycemia.
NSAIDs (including selective inhibitors of COX-2), estrogens, adrenostimulators reduce the antihypertensive effect of lisinopril.
With simultaneous use of ACE inhibitors and drugs gold (sodium aurothiomalate) discloses simptmokompleks including facial flushing, nausea, vomiting and reduced blood pressure.
While the use of selective inhibitors of the reuptake sertotonina possible expressed hyponatremia.
Joint application with allopurinol, procainamide, cytostatics can lead to leukopenia.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 4 years.
