LISINOPRIL 10MG PILLS
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Active ingredient: lisinopril dihydrate;
Excipients: milk sugar (lactose), microcrystalline cellulose, starch 1500 (pregelatinized), aerosil (colloidal silicon dioxide), talc, Magnesium stearate
Lisinopril - cardioprotective, natriuretic, vasodilating, hypotensive.
An ACE inhibitor, reduces the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases prostaglandin synthesis. Reduces the total 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 stress in patients with chronic heart failure. Expands arteries to a greater extent than veins. Some effects are attributed to effects on tissue renin-angiotensin systems. With prolonged use, hypertrophy of the myocardium and the walls of resistive arteries is reduced. Improves blood supply to ischemic myocardium.
ACE inhibitors prolong life expectancy in patients with chronic heart failure,slow the progression of left ventricular dysfunction in patients after myocardial infarction without clinical manifestations of heart failure. The antihypertensive effect begins after about 6 hours and persists for 24 hours. The duration of the effect also depends on the dose. Onset of action - after 1 h. The maximum effect is determined after 6-7 hours. In case of arterial hypertension, the effect is noted in the first days after the start of treatment, a stable action develops in 1-2 months. With the abrupt cancellation of the drug did not observe a pronounced increase in blood pressure.
In addition to lowering blood pressure, lisinopril reduces albuminuria. In patients with hyperglycemia, it helps normalize the function of the damaged glomerular endothelium.
Lisinopril does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not lead to an increase in hypoglycemia.
Suction. After taking the drug inside about 25% of lisinopril is absorbed from the gastrointestinal tract. Food intake does not affect the absorption of the drug. Absorption averages 30%, bioavailability - 29%.
Distribution. Almost does not bind to plasma proteins. The maximum plasma concentration (90 ng / ml) is reached after 7 hours. Permeability through the hematoencephalic and placental barrier is low.
Metabolism. Lisinopril is not biotransformed in the body.
Inference. Excreted by the kidneys in unchanged form. The half-life is 12 hours.
In patients with chronic heart failure, absorption and clearance of lisinopril are reduced.
In patients with renal insufficiency, the concentration of lisinopril is several times higher than the concentration in the blood plasma of volunteers, with an increase in the time to reach the maximum concentration in the blood plasma and an increase in the half-life.
Elderly patients have a concentration of the drug in the blood plasma and the area under the curve is 2 times greater than that of young patients.
- 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 thim ples and / or diuretics);
- Early treatment of acute myocardial infarction (in the first 24 hours with stable hemodynamic parameters to maintain these indicators and prevent left ventricular dysfunction and heart failure);
- Diabetic nephropathy (reducing albuminuria in insulin-dependent patients with normal blood pressure and insulin-independent patients with arterial hypertension).
Hypersensitivity to lisinopril or other ACE inhibitors, a history of angioedema, including the use of ACE inhibitors, hereditary Quincke, 18 years of age (efficacy and safety have not been established).
Precautions: severe renal impairment, bilateral renal artery stenosis or artery stenosis only kidneys with progressive azotemia, condition after kidney transplantation, renal insufficiency, azotemia, hyperkalemia, aortic stenosis, hypertrophic obstructive kardiomipatiya, primary hyperaldosteronism, hypotension, cerebrovascular diseases ( including cerebrovascular insufficiency), coronary heart disease, coronary insufficiency, autoimmune systemic diseases connective tissue levation (including scleroderma, systemic lupus erythematosus); oppression of bone marrow hematopoiesis; sodium-restricted diet: hypovolemic states (including as a result of diarrhea, vomiting); elderly age.
Often: dizziness, headache (in 5-6% of patients), weakness, diarrhea, dry cough (3%), nausea, vomiting, orthostatic hypotension, skin rash, chest pain (1-3%).
Immune system: (0.1%) angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities).
Cardiovascular: marked reduction in blood pressure, orthostatic hypotension, renal dysfunction, cardiac arrhythmias, heart palpitations.
From the side of the central nervous system: fatigue, drowsiness, jerky muscles of the limbs and lips.
From the hematopoietic system: possible leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with long-term treatment - a slight decrease in the concentration of hemoglobin and hematocrit, erythrocytopenia.
Laboratory indicators: hyperkalemia, azotemia, hyperuricemia, hyperbilirubinemia, increased activity of “liver” enzymes, especially in the presence of a history of kidney disease, diabetes mellitus and renovascular hypertension.
Cardiovascular: heartbeat; tachycardia; myocardial infarction; cerebrovascular stroke in patients with an increased risk of disease, due to a pronounced decrease in blood pressure.
On the part of the digestive tract: dry mouth, anorexia, dyspepsia, changes in taste, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis.
On the part of the skin: urticaria, increased sweating, pruritus, alopecia.
On the part of the urinary system: impaired renal function, oliguria, anuria, acute renal failure, uremia, proteinuria.
On the part of the immune system: a syndrome that includes the acceleration of the erythrocyte sedimentation rate (ESR), arthralgia and the appearance of antinuclear antibodies.
From the side of the central nervous system: asthenic syndrome, mood lability, confusion, decrease in potency.
Other: myalgia, fever, impaired fetal development.
Lisinopril reduces the excretion of potassium from the body during treatment with diuretics.
Special care is required when using the drug 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 prescribed only on the basis of an individual decision of the attending physician with regular monitoring of serum potassium and kidney function.
Caution can be applied together:
- with diuretics: with the additional administration of a diuretic to a patient taking Lisinopril, as a rule, an additive antihypertensive effect occurs - the risk of a pronounced decrease in blood pressure;
- with other antihypertensive agents (additive effect);
- with nonsteroidal anti-inflammatory drugs (indomethacin, etc.), estrogens, and also adrenostimulants - reduction of the antihypertensive effect of lisinopril;
- with lithium (lithium secretion may decrease, so you should regularly monitor the concentration of lithium in the serum);
- with antacids and Kolestiramine - reduce absorption in the gastrointestinal tract.
Alcohol enhances the effect of the drug.
Inside, regardless of the meal. In hypertension, patients who do not receive other antihypertensive drugs are prescribed 5 mg 1 time per 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 (an increase in dose over 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 after 2-4 weeks from the start of treatment, which should be considered when increasing the dose.With insufficient clinical effect, it is possible to combine the drug with other antihypertensive drugs.
If the patient received prior treatment with diuretics, then the use of such drugs should be stopped 2-3 days before starting to use Lisinopril. If this is not feasible, then the initial dose of Lisinopril should not exceed 5 mg per day. In this case, after taking the first dose, medical control is recommended for several hours (the maximum effect is reached after about 6 hours), since a pronounced decrease in blood pressure may occur.
In case of 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 enhanced medical control (control of blood pressure, kidney function, serum potassium concentration). Maintenance dose, continuing strict medical supervision, should be determined depending on the dynamics of blood pressure.
In renal insufficiency, due to the fact that lisinopril is excreted through the kidneys, the initial dose should be determined depending on creatinine clearance, then, in accordance with the reaction, a maintenance dose should be established under conditions of frequent monitoring of renal function, serum potassium, sodium levels.
With persistent arterial hypertension, long-term maintenance therapy is indicated at 10-15 mg / day.
In chronic heart failure, start with 2.5 mg 1 time per day, with a subsequent increase in dose of 2.5 mg in 3-5 days to the usual, supporting daily dose of 5-20 mg. The dose should not exceed 20 mg per day.
In elderly people, a more pronounced long-term hypotensive effect is often observed, which is associated with a decrease in the rate of elimination of lisinopril (it is recommended to begin treatment with 2.5 mg / day).
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 per day. In patients with acute myocardial infarction, use the drug for at least 6 weeks.
At the beginning of treatment or during the first 3 days after acute myocardial infarction in patients with low systolic blood pressure (120 mm Hg or less), a lower dose of 2.5 mg should be prescribed. In case of a decrease in blood pressure (systolic blood pressure is less than or equal to 100 mm Hg), the daily dose of 5 mg can, if necessary, be temporarily reduced to 2.5 mg. In the case of a prolonged pronounced decrease in blood pressure (systolic blood pressure below 90 mmHg for more than 1 hour), treatment with Lisinopril should be stopped.
In patients with non-insulin dependent diabetes mellitus, 10 mg of Lisinopril is used once a day. The dose may, if necessary, be increased to 20 mg.
1 time per day in order to achieve diastolic blood pressure values below 75 mm Hg. in a sitting position. In patients with insulin-dependent diabetes mellitus, the dosage is the same in order to achieve diastolic blood pressure values below 90 mm Hg. in a sitting position.
Symptoms (occur when taking a single dose of 50 mg and above): a pronounced decrease in blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, irritability.
Treatment: symptomatic therapy, intravenous fluids, control of blood pressure, water and electrolyte balance and the normalization of the latter.
Lisinopril can be removed from the body through hemodialysis.
Most often, a pronounced decrease in blood pressure occurs when a decrease in the volume of fluid 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 failure or without it, a pronounced decrease in blood pressure is possible. It is more often detected in patients with 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 with Lisinopril should begin under the strict supervision of a physician (with careful selection of the dose of the drug and diuretics).
Similar rules should be followed when prescribing patients with coronary heart disease, cerebrovascular insufficiency, in which 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 Lisinopril is used in some patients with chronic heart failure, but with normal or lowered BP, there may be a decrease in BP, which is usually not a reason to stop treatment.
Before starting treatment with Lisinopril, if possible, normalize the concentration of sodium and / or fill up the lost volume of fluid, carefully monitor the effect of the initial dose of Lisinopril on the patient.
In case of stenosis of the renal artery (especially in bilateral stenosis, or in the presence of stenosis of the artery of a single kidney), as well as circulatory failure due to lack of sodium and / or fluid, the use of Lisinopril can lead to impaired renal function, acute renal failure, which is usually turns out to be irreversible after drug withdrawal.
In acute myocardial infarction
The use of standard therapy (thrombolytics, Acetylsalicylic acid, beta-blockers) is shown. Lisinopril may be used in conjunction with intravenous administration or with the use of therapeutic transdermal systems Nitroglycerin.
Surgical intervention / general anesthesia
With extensive surgical interventions, as well as 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, so special care is required in determining the dose.
Since the potential risk of agranulocytosis cannot be excluded, periodic monitoring of the blood picture is required.When using the drug in dialysis conditions with a polyacryl-nitrile membrane, anaphylactic shock may occur, therefore either a different type of dialysis membrane or the appointment of other antihypertensive agents is recommended.
Impact on the ability to drive vehicles and mechanisms
There is no data on the effect of lisinopril on the ability to drive vehicles and mechanisms used in therapeutic doses, however, it must be borne in mind that dizziness may occur, therefore care should be taken.
In a dry place protected from light and inaccessible to children, at a temperature not higher than 25 ° C.