ACE inhibitor. The crystalline powder is white or almost white, odorless, soluble in water, sparingly soluble in methanol and practically insoluble in ethanol. The molecular weight is 441,52.
Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs); chronic heart failure (as part of combination therapy for patients taking cardiac glycosides and/or diuretics); early treatment of acute myocardial infarction as part of combination therapy (in the first 24 hours with stable hemodynamic parameters to maintain these indicators and prevent left ventricular dysfunction and heart failure);
The incidence of side effects is characterized as often (≥1%); seldom (lt; 1%).
The most common side effects are dizziness, headache, fatigue, diarrhea, dry cough, nausea.
From the CCC: often – a pronounced decrease in blood pressure, orthostatic hypotension; rarely – chest pain, tachycardia, bradycardia, worsening of symptoms of heart failure, impaired 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 limbs and lips; rarely – asthenic syndrome.
From the hemopoietic organs: rarely – leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with prolonged treatment – anemia (decreased Hb, hematocrit, erythropenia).
From the respiratory system: rarely – shortness of breath, bronchospasm.
From the digestive system: rarely – dryness of the oral mucosa, anorexia, dyspepsia, taste change, abdominal pain, pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis.
From the skin: rarely – urticaria, skin itching, increased sweating, alopecia, photosensitivity.
From the genitourinary system: rarely – impaired renal function, oliguria, anuria, acute renal failure, uremia, proteinuria, sexual dysfunction.
Laboratory indicators: often – hyperkalemia, hyponatremia; rarely – hyperbilirubinemia, increased activity of liver enzymes, hypercreatininemia, increased concentrations of urea and creatinine.
Allergic reactions: rarely – angioedema of the face, limbs, lips, tongue, epiglottis and/or larynx, skin rashes, skin itching, fever, false-positive antinuclear antibody test results, increased ESR, eosinophilia, leukocytosis; in rare cases – intestinal angioedema.
Other: rarely – arthralgia/arthritis, vasculitis, myalgia.
Symptomatic arterial hypotension
Most often, a pronounced decrease in blood pressure occurs with a decrease in the BCC caused by diuretic therapy, a decrease in the amount of sodium chloride in food, dialysis, diarrhea, or vomiting. In patients with heart failure with simultaneous renal failure or without it, a pronounced decrease in blood pressure is possible.
Under strict medical supervision, lisinopril should be used in patients with coronary artery disease, 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 drugs. In the event of the development of arterial hypotension, the patient should be moved to the supine position with raised legs. If necessary, BCC should be replenished by iv administration of a 0,9% sodium chloride solution. Transient arterial hypotension is not an obstacle to the further use of drugs. After restoration of bcc and blood pressure, treatment can be continued.
When using lisinopril in some patients with heart failure, but with normal or reduced blood pressure, a decrease in blood pressure may occur, which is usually not a reason for stopping treatment.
Before starting treatment with lisinopril, if possible, normalize the sodium content and/or replenish the bcc, carefully monitor the effect of the initial dose of lisinopril on the patient.
In case of stenosis of the renal arteries (especially in case of 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 lack of sodium and/or fluid, the use of lisinopril can lead to impaired renal function, acute renal failure, which is usually irreversible even after drug cancellation.
Hyperkalemia can develop during treatment with ACE inhibitors, including and lisinopril. Risk factors for the development of hyperkalemia are renal failure, decreased renal function, age older than 70 years, diabetes mellitus, some concomitant conditions (dehydration, acute heart failure, metabolic acidosis), the simultaneous use of potassium-sparing diuretics (such as spironolactone, eplerenone, triamterene, amyloride), food additives/preparations of potassium or potassium-containing substitutes for edible salt, as well as the use of other drugs that increase the level of potassium in the blood (for example, heparin).
The use of food additives/potassium preparations, potassium-sparing diuretics, potassium-containing salt substitutes can lead to a significant increase in blood potassium, especially in patients with impaired renal function. Hyperkalemia can lead to serious, sometimes fatal heart rhythm disturbances.
Mitral stenosis/aortic stenosis/hypertrophic obstructive cardiomyopathy
Lisinopril, like other ACE inhibitors, should be used with caution in patients with left ventricular outflow tract obstruction (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as in patients with mitral stenosis.
Acute myocardial infarction
The use of standard therapy is shown (thrombolytics, acetylsalicylic acid as an antiplatelet agent, beta-blockers). Lisinopril can be used in conjunction with the on/in the introduction or with the use of therapeutic transdermal systems of nitroglycerin.
Surgical intervention/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.
With the development of arterial hypotension, blood pressure should be maintained by replenishing the bcc. It is necessary to warn the surgeon/anesthetist that the patient is taking ACE inhibitors.
The same dose leads to a higher concentration of lisinopril in the blood, therefore, special care is required when determining the dose.
In patients undergoing hemodialysis using high-flow membranes (e.g. AN69®), anaphylactic reactions have been observed during treatment with ACE inhibitors. ACE inhibitors should be avoided when using this type of membrane.
While taking ACE inhibitors, neutropenia/agranulocytosis, thrombocytopenia, and anemia can occur. In patients with normal renal function and in the absence of other aggravating factors, neutropenia develops rarely. With extreme caution, lisinopril should be used in patients with systemic diseases of the connective tissue, while taking immunosuppressants, allopurinol, or procainamide, especially in patients with impaired renal function.
Some patients developed severe infections, in some cases resistant to intensive antibiotic therapy. When prescribing lisinopril in such patients, it is recommended to periodically monitor the content of white blood cells in the blood. Patients should inform their doctor of any signs of an infectious disease (e.g., sore throat, fever).
Anaphylactoid reactions during LDL apheresis
In rare cases, in patients receiving ACE inhibitors, life-threatening anaphylactoid reactions may develop during the LDL apheresis procedure using dextran sulfate. To prevent anaphylactoid reaction, ACE inhibitor therapy should be temporarily discontinued before each apheresis procedure.
Anaphylactoid reactions during desensitization
There are separate reports of the development of anaphylactoid reactions in patients receiving ACE inhibitors during desensitizing therapy, such as hymenoptera venom. ACE inhibitors should be used with caution in patients predisposed to allergic reactions undergoing desensitization procedures.
When taking ACE inhibitors, including and lisinopril, in rare cases and during any period of therapy, the development of angioedema of the face, upper and lower extremities, lips, mucous membranes, tongue, vocal folds and/or larynx can be observed (see “Side effects”). When symptoms appear, the drug should be stopped immediately, and the patient should be observed until the signs of edema disappear completely.
Angioneurotic edema, accompanied by laryngeal edema, can be fatal. Swelling of the tongue, vocal folds, or larynx can lead to airway obstruction. If such symptoms appear, emergency treatment is required, including the administration of epinephrine and/or airway patency. The patient should be under medical supervision until the symptoms disappear completely and persistently.
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In rare cases, against the background of therapy with ACE inhibitors, angioedema of the intestine develops. Moreover, patients have abdominal pain as an isolated symptom or in combination with nausea and vomiting, in some cases without prior angioedema of the face and with a normal level of C1 esterase.
Diagnosed with computed tomography
abdominal area, ultrasound examination or surgical intervention. Symptoms disappeared after stopping ACE inhibitors. Therefore, in patients with abdominal pain receiving ACE inhibitors,
differential diagnosis, it is necessary to take into account the possibility of developing angioedema of the intestine (see. “Side effects”).
There are no data on the use of lisinopril in patients after kidney transplantation.
It should be borne in mind that in patients of the Negroid race, the risk of developing angioedema is higher. Like other ACE inhibitors, lisinopril is less effective in lowering blood pressure in patients of the Negroid race.
This effect is possibly associated with a pronounced predominance of low-root status in patients of the Negroid race with arterial hypertension.
Impaired liver function
In rare cases, while taking ACE inhibitors, a syndrome of development of cholestatic jaundice was observed with a transition to fulminant necrosis of the liver, sometimes with a fatal outcome. The mechanism of development of this syndrome is unclear. If jaundice or a significant increase in the activity of liver enzymes occurs while taking ACE inhibitors, you should stop taking the medicine (see “Side effects”), the patient should be under appropriate medical supervision.
Double blockade of RAAS
Cases of arterial hypotension, fainting, stroke, hyperkalemia, and impaired renal function (including acute renal failure) have been reported in susceptible patients, especially when used with drugs that affect this system. Therefore, the double blockade of RAAS as a result of the combination of an ACE inhibitor with ARA II or aliskiren is not recommended.
The combination with aliskiren is contraindicated in patients with diabetes mellitus or impaired renal function (GFR lt; 60 ml/min/1,73 m2 (see “Contraindications” and “Interaction”).
Patients with diabetes
When prescribing lisinopril to patients with diabetes mellitus receiving hypoglycemic agents for oral administration or insulin, it is necessary to regularly monitor the concentration of glucose in the blood during the first month of therapy (see “Interaction”).
Influence on the ability to drive vehicles and perform work requiring a high speed of mental and physical reactions. Lisinopril should be used with caution in patients driving vehicles and engaging in activities that require an increased concentration of attention and speed of response due to the risk of hypotension and dizziness.
The drug has a hypotensive, cardioprotective, vasodilating and natriuretic effect on the human body.
Being an inhibitor of angiotensin-converting enzyme (ACE), Lisinopril has pronounced hypotensive (lowers blood pressure) properties.
This drug is also valuable for its cardioprotective (correcting the functional state of the myocardium), vasodilating and natriuretic (excretes sodium salts in the urine) action.
Long-term use of lisinopril can reduce hypertrophy (weight gain) of the walls of the arteries and myocardium, improve blood circulation.
Lisinopril reviews and the results of clinical trials are characterized as a drug with the ability to prolong the life of patients suffering from chronic heart failure, as well as inhibit the progression of left ventricular dysfunction after myocardial infarction.
Lisinopril begins to act 1 hour after administration, after 4-6 hours – the maximum effect of the drug is observed, the total duration of the therapeutic effect is 24 hours.
When Lisinopril is used by patients with arterial hypertension, relief of the patient’s condition occurs in the first days of taking the drug, and a stable effect is fixed after 1-2 months.
Pharmacodynamics and pharmacokinetics
Lisinopril tablets block ACE, increase the content of endogenous vasodilating PG and prevent the transition of angiotensin I to angiotensin II. They also reduce the conversion of arginine-vasopressin and endothelin-1, reduce myocardial afterload, total peripheral vascular resistance, pulmonary capillary pressure and systemic blood pressure.
The medicine blocks the tissue renin-angiotensin system of the heart, prevents the appearance of myocardial hypertrophy and dilatation of the left ventricle, or helps in their disappearance.
The effect of the drug appears after about 60 minutes, increases over 6-7 hours and lasts for a day. The maximum hypotensive effect is manifested during a course of several weeks.
The active substance is absorbed by about 25%. Meal time does not affect absorption. Communication with plasma proteins is low. The active substance is not biotransformed and excreted by the kidneys unchanged. The elimination half-life is 12 hours.
Indications for the use of lisinopril
This medicine should not be taken without the appointment of a specialist. Indications for the use of lisinopropyl may be different. How to take and from what the tablets will help in each case, only the doctor knows.
As a rule, lisinopril tablets are indicated for use as follows:
- arterial hypertension ;
- chronic heart failure;
- diabetic nephropathy in case of insulin-dependent and type II diabetes mellitus;
- acute myocardial infarction without arterial hypotension.
The drug should not be taken with hypersensitivity to its components, lactation and pregnancy.
It is undesirable to prescribe this remedy for:
- anaphylactoid reactions;
- cerebrovascular insufficiency;
- impaired kidney and liver function;
- bilateral renal artery stenosis;
- transplanted kidney;
- advanced age;
- a history of Quincke’s edema;
- bone marrow depression;
- obstructive changes that prevent the outflow of blood from the heart;
- hyponatremia, as well as when eating with a limited intake of sodium;
- stenosis of a single kidney artery;
Lisinopril recommends the use of lisinopril for: various forms of arterial hypertension, diabetic nephropathy, as well as in combination therapy for the early treatment of acute myocardial infarction and chronic heart failure.
The indications indicated in the instructions for Lisinopril cannot be regarded as a guide to self-treatment, since the use of this drug can be dangerous for some categories of patients.
So, Lisinopril is not prescribed to persons with hypersensitivity to ACE inhibitors, in particular to lisinopril, as well as pregnant and breast-feeding women.
Hereditary Quincke edema and a history of angioedema are also a reason for refusing to use Lisinopril.
With caution, taking lisinopril should be with diseases such as:
- aortic stenosis;
- cardiac ischemia;
- cerebrovascular disease;
- coronary insufficiency;
- oppression of bone marrow hematopoiesis;
- severe systemic connective tissue diseases;
- kidney failure;
- primary aldosteronism.
The feasibility of using Lisinopril should definitely be discussed with a doctor for elderly patients and those on a salt-restricted diet.
Lisinopril effectively helps with high blood pressure, but the drug has many side effects. If you follow the dosage and adhere to the correct treatment regimen, then the negative consequences after taking the medicine are not observed or disappear within a few days.
- chest pain, a sharp decrease in blood pressure;
- deterioration in potency;
- disorders in the digestive system that provoke the appearance of nausea and vomiting;
- an increase in ESR, a decrease in hemoglobin level;
- increased nitrogen content of urea and keratin;
- joint pain;
- muscle weakness, migraine, dizziness.
At the initial stage of treatment, allergic reactions in the form of skin rashes may occur, sometimes Quincke’s edema can occur. Often, taking a drug is accompanied by an unproductive cough.
The main contraindications are individual intolerance to the components of the drug and lactose, hypersensitivity to drugs from the group of ACE inhibitors, angioedema, idiopathic edema. Lisinopril is contraindicated during pregnancy at any time, and use during lactation is possible only if breast-feeding is suspended. There is no reliable data on the safety of using the drug in pediatrics, so it is not prescribed to people under 18 years of age.
Caution and under the constant supervision of a physician should take lisinopril for people of advanced age, diabetics, if there is a history of chronic renal diseases, problems with cerebral circulation.
We can definitely say about the lack of compatibility of Lisinopril and alcohol. During treatment, drinks and preparations that contain ethanol should be completely eliminated. The drug enhances the negative effect of alcohol on the body, which can cause the development of serious liver disorders.
Important! Before taking Lisinopril for pressure, it is necessary to undergo a complete examination to exclude the presence of kidney pathologies, eliminate dehydration.
Hypersensitivity to lisinopril or other ACE inhibitors; history of angioedema, including against the background of the use of ACE inhibitors; hereditary Quincke edema or idiopathic angioedema; age up to 18 years (effectiveness and safety have not been established); pregnancy and the period of breastfeeding (see
Interactions with other active substances
The most common adverse effects of Lisinopril include increased fatigue, headache, dizziness, dry cough, nausea, and diarrhea.
According to the instructions, Lisinopril can also cause adverse reactions of the body, such as:
- chest pain, a significant decrease in blood pressure, bradycardia, tachycardia, heart palpitations, myocardial infarction;
- drowsiness, confusion, emotional lability;
- anemia, thrombocytopenia, neutropenia, agranulocytosis, leukopenia;
- bronchospasm, shortness of breath;
- taste changes, dry mouth, dyspepsia, anorexia, pancreatitis, hepatitis, jaundice;
- photosensitivity (hypersensitivity to sunlight), hair loss, increased sweating;
- anuria (lack of flow of urine into the bladder), oliguria (decrease in the amount of urine released), impaired renal function, decreased potency, proteinuria (the presence of protein in the urine), uremia (accumulation of urea in the blood), acute renal failure;
- skin rashes, angioedema, fever;
- neuropsychic weakness, joint pain, muscle pain, cramps, vasculitis (inflammation and destruction of the walls of blood vessels).
Side effects can be different, they arise from different systems and organs:
- nervous system – irritability, headache, ataxia, fatigue, transient cerebrovascular accident, tremor, drowsiness, blurred vision, confusion, nervousness, fainting, peripheral neuropathy, memory loss, dizziness, insomnia, paresthesia, cramps, tinnitus;
- gastrointestinal tract – dry mouth, heartburn, vomiting, flatulence, abdominal pain, gastritis, indigestion, nausea, diarrhea, constipation, cramping, hepatotoxicity, pancreatitis;
- musculoskeletal system – arthralgia, myalgia, arthritis, neck and back pain;
- respiratory system – malignant tumors of the lungs, embolism and pulmonary infarction, dry cough, asthma, respiratory pain, hemoptysis, laryngitis, pharyngitis, nosebleeds, paroxysmal postural dyspnea, infiltration, pleural effusion, rhinitis, bronchitis, bronchospasm, sinus;
- genitourinary system – acute renal failure, problems with kidney function, pyelonephritis, oliguria, uremia, impotence, dysuria, anuria, edema, decreased libido;
- skin – urticaria, alopecia, pemphigus, Lyell syndrome, photosensitivity, rash, damage and infection of the skin, Stevens-Johnson syndrome.
In addition, the following manifestations are possible: the development of infections, weight loss, sweating, diabetes mellitus, an increase in the titer of antinuclear antibodies and urea, gout, an increase in creatinine, hyperkalemia, hyperuricemia, fever, allergies, dehydration, hyponatremia.
If any side effects are detected, you should immediately consult a specialist.
Nosological classification (ICD-10)
Instructions for use of lisinopril and doses
Symptoms (occur when taking a single dose of 50 mg): marked decrease in blood pressure, dry mucous membrane of the oral cavity, drowsiness, urinary retention, constipation, anxiety, increased irritability.
Treatment: there is no specific antidote. Symptomatic Therapy Gastric lavage, the use of enterosorbents and laxatives. It is shown in/in the introduction of a 0,9% solution of sodium chloride. In the case of bradycardia resistant to treatment, the use of an artificial pacemaker is necessary. Need to control blood pressure, indicators of water-electrolyte balance. Hemodialysis is effective.
The medicine is taken daily 1 time in the morning, regardless of the meal. This should be done at the same time, while washing down with a certain amount of liquid.
The exact dosage and treatment regimen is selected individually by a specialist. It depends on what lisinopropil is used, what drugs are taken with it and what is the condition of the kidneys.
In case of arterial hypertension, in the case of treatment without other antihypertensive drugs, the dosage is 2,5 mg once a day. For maximum effectiveness, a 2-4 week therapy is performed. Only then can the daily dosage be increased to a maximum of 20 mg. The daily dose should not be more than 40 mg.
If the desired hypotensive effect is not achieved, you must additionally take another antihypertensive drug of a different pharmacotherapeutic group.
In case of acute myocardial infarction, if the medicine Lisinopril was prescribed, the instructions for use report that it should be taken within 5 hours after the onset of the first symptoms of the disease. The initial dosage is 10 mg once a day. May be increased to 120 mg. People with arterial systolic pressure up to mm Hg. Art.
In case of heart failure, the daily initial dosage is 2,5 mg. It can be gradually increased depending on the individual indications of the patient. Therapeutic daily dosage is 20 mg.
In case of insulin-dependent diabetes mellitus and nephropathy, therapy is started with low doses and is carried out under close supervision by a specialist. The initial daily dosage for type II diabetes is 10 mg. It is forbidden to exceed a daily dose of 20 mg.
In renal failure, a dosage adjustment is required depending on the QC:
- 30-70 ml/min – you need to take 5-10 mg/day;
- 10-30 ml/min – you need to take 2,5-5 mg/day;
- up to 10 ml/min – you need to take 2,5 mg/day.
The daily dose of 20 mg cannot be exceeded, and for people with CC up to 30 ml/min, the maximum daily dosage is 10 mg.
In some cases, it is also possible to extend the interval between doses of the drug from one to two days.
There may be some changes in the regimen of the drug, depending on the manufacturer. So the instruction for use of Lisinopril-Astrafarm reports the following daily dosages, depending on the diagnosis:
- arterial hypertension – to start, the dosage should be 10 mg per day. In this case, after the first application, a significant decrease in blood pressure may occur. In this case, the initial dosage is 2,5-5 mg. Therapy should be supervised by a specialist. The maintenance daily dosage is 20 mg. If the proper effect has not been achieved in 14-28 days, it can be increased. But you can not exceed the daily dosage of 80 mg;
- chronic heart failure – the medicine can be used as a component of therapy with diuretics, beta-blockers and digitalis drugs. At the beginning of treatment, a daily dosage of 2,5 mg is prescribed. The medicine should be consumed under the supervision of a specialist. It is possible to increase the dose, but not more than 10 mg and not earlier than 14 days. The maximum daily dosage should not exceed 35 mg. The exact dose depends on the individual patient;
- acute myocardial infarction – the drug is taken as part of the therapy with thrombolytic drugs, beta-blockers and acetylsalicylic acid. The dosage of Lisinopril-Astrafarm in the first two days is 5 mg. The course should be started when the first symptoms occur and if the systolic blood pressure does not exceed 100 mmHg. Art. Two days later, a daily dosage of 10 mg is prescribed. If blood pressure is up to 120 mmHg. Art., in the first 3 days you need to take 2,5 mg. When prolonged arterial hypotension occurs, therapy is immediately discontinued. The course is designed for 6 weeks, after which the patient’s condition must again be assessed for further treatment;
- diabetic nephropathy – the initial dosage is 10 mg per day. If necessary, the dose is increased to 20 mg.
For any diagnosis in case of renal failure, the dosage is adjusted according to QC. So the initial dose may be:
- KK up to 10 ml/min – you need to take 2,5 mg/day;
- KK 10-30 ml/min – you need to take 2,5-5 mg/day;
- KK 31-80 ml/min – you need to take 5-10 mg/day.
Instructions for use Lisinopril-Ratiopharm, Lisinopril Teva, Lisinopril Stada have no significant differences in the dosage regimen.
In case of an overdose, as a rule, acute arterial hypotension appears. As a treatment, physiological saline is administered. Symptomatic therapy is performed.
In addition, shock, hyperventilation, acute renal failure, bradycardia, cough, electrolyte imbalance in the blood, tachycardia, palpitations, dizziness, and anxiety are possible.
The drug must be canceled. If the patient is conscious, they rinse the stomach, lay the patient on his back with a low head restraint, raised legs and head set aside. In addition, enterosorbents are given.
When taking medication in particularly high doses, the patient should be hospitalized immediately. In a hospital, treatment is carried out aimed at maintaining normal perfusion pressure, blood circulation, respiration, restoring the volume of circulating blood and normal kidney function. Hemodialysis is effective. It is imperative to monitor indicators of vital functions, as well as the level of creatinine and electrolytes in blood serum.
At what pressure should lisinopril be taken? The drug is part of the ACE inhibitor group. After taking the drug, vasodilation occurs, so it is indicated for hypertension. With regular use, the work of the heart muscle and blood circulation improves, excess sodium salts are removed from the body. The drug effectively reduces diastolic and systolic indicators, while not affecting the heart rate.
The drug is released in the form of tablets with different dosages. The color of the tablets depends on the amount of active substance. Saturated orange – 2,5 mg, pale orange – 5 mg, pink – 10 mg, white – 20 mg. The price of Lisinopril is 70-200 rubles. depending on the dosage and the number of tablets in the package.
Important! Lisinopril increases life expectancy in the presence of serious diseases of the heart and blood vessels, stops ventricular dysfunction after a heart attack.
The composition of the drug includes lisinopril dihydrate, depending on the manufacturer of the tablet may include various additional substances that do not have a therapeutic effect.
- hypertension and hypertension of various etiologies;
- myocardial infarction in the acute stage;
- chronic heart failure;
- lesions of the peripheral nervous system that are caused by diabetes.
The drug has many analogues that have similar therapeutic effects and practically do not differ in cost – Lysitar, Vitopril, Dapril, Lipril.
Lisinopril, indications suggest taking various doses of the drug, is available in tablets containing 2,5 mg, 5 mg, 10 mg and 20 mg of the active substance. Take Lisinopril instructions once a day, preferably at the same time.
The use of Lisinopril for essential hypertension should begin with 10 mg per day, followed by a transition to a maintenance dose of 20 mg per day, while in extreme cases, the maximum daily dose of 40 mg is allowed.
Reviews of lisinopril indicate that the full therapeutic effect of the drug can develop 2-4 weeks after the start of treatment.
If after applying the maximum doses of the drug the expected results have not been achieved, the additional intake of other antihypertensive drugs is recommended.
Patients taking diuretics, 2-3 days before the start of the use of Lisinopril, you must stop taking them. If for some reason cancellation of diuretics is not possible, the daily dose of lisinopril should be reduced to 5 mg.
In conditions with increased activity of the renin-angiotensin-aldosterone system that regulates blood volume and blood pressure, Lisinopril recommends the use of a daily dose of 2,5-5 mg. The maintenance dose of the drug for such diseases is set individually depending on the value of blood pressure.
In renal failure, the daily dose of lisinopril depends on creatinine clearance and can vary from 2,5 to 10 mg per day.
Persistent arterial hypertension involves taking 10-15 mg of lisinopril per day for a long time.
Acceptance of the drug in chronic heart failure begins with 2,5 mg per day, and after 3-5 days increase to 5 mg. The maintenance dose of lisinopril for this disease is 5-20 mg per day.
The use of lisinopril in acute myocardial infarction involves complex therapy and is carried out according to the following scheme: on the first day – 5 mg, then the same dose once a day, after which the amount of the drug is doubled and taken once every two days, the final stage is 10 mg once a day. Lisinopril, indications determine the duration of treatment, for acute myocardial infarction take at least 6 weeks.
With diabetic nephropathy, Lisinopril recommends taking 10 mg to 20 mg per day.
It inhibits ACE, prevents the transition of angiotensin I to angiotensin II, increases the concentration of endogenous vasodilating PG. Reduces the formation of arginine-vasopressin and endothelin − 1, which have vasoconstrictor properties. Lowers OPSS, systemic blood pressure, afterload on the myocardium, pressure in the pulmonary capillaries.
Increases cardiac output and myocardial exercise tolerance in patients with heart failure. The effect manifests itself after 1 hour, increases within 6–7 hours, lasts up to 24 hours. The antihypertensive effect reaches optimal values with repeated administration over several weeks. It inhibits the tissue renin-angiotensin system of the heart, prevents the development of myocardial hypertrophy and dilatation of the left ventricle, or promotes their reverse development (cardioprotective effect).
After oral administration, about 25% (6-60%) is absorbed. Eating does not affect absorption. Poorly bound to plasma proteins. Tmax – 6 hours. It is not biotransformed and excreted by the kidneys unchanged, T1/2 is 12 hours. Clinically significant changes in pharmacokinetic parameters that require correction of the dosage regimen are observed with a decrease in GFR of less than 30 ml/min (Cmax in plasma increases, T1/lengthens/2 and duration of action.) In elderly patients, the plasma concentration and AUC increase by 2 times. It is removed during hemodialysis.
Carcinogenicity, mutagenicity, effect on fertility
When lisinopril was administered to rats for 105 weeks at doses up to 90 mg/kg/day (56 times more than the MPD) and mice for 92 weeks at doses up to 135 mg/kg/day (84 times more than the MPD), no signs of carcinogenicity were detected . Does not possess mutagenic and genotoxic properties. At doses up to 300 mg/kg/day, it does not adversely affect reproductive function in male and female rats.
The administration to mice on the 6-15th day of pregnancy in doses up to 625 times higher than the MPD was not accompanied by manifestations of teratogenic effects. In rats that received doses 6 times higher than the MPDs on the 17–188th day of pregnancy, no teratogenic and fetotoxic effects were detected, although there was a decrease in the average body weight of newborn rats.
When administered to rats, it passes slightly through the BBB, does not accumulate in tissues with repeated use, is found in breast milk and the placenta (but not in fetal tissues).
However, it should be borne in mind that in humans, the use of other ACE inhibitors during pregnancy can cause an increase in fetal and neonatal mortality, and administration in the II and III trimesters of pregnancy is accompanied by a decrease in placenta mass, delayed ossification of the skeleton, development of oligohydramnios (due to decreased renal function), anuria , renal failure in the fetus, up to death, pulmonary hypoplasia, contractures of the limbs and craniofascial deformities, non-closure of the Botallus duct and toxic direct effect on the mother’s body.
With the simultaneous use of lisinopril with potassium-sparing diuretics (spironolactone, eplerenone, triamteren, amiloride), potassium preparations, salt substitutes containing potassium, cyclosporine, the risk of hyperkalemia increases, especially with impaired renal function, so they can only be used together with regular monitoring of potassium in blood serum and kidney function.
The simultaneous use of beta-blockers, BKK, diuretics and other antihypertensive drugs enhances the severity of antihypertensive action.
Lisinopril slows the elimination of lithium preparations. Therefore, when used together, it is necessary to regularly monitor the concentration of lithium in the blood serum.
Antacids and colestyramine reduce the absorption of lisinopril in the digestive tract.
Hypoglycemic agents (insulin, hypoglycemic agents for oral administration). The use of ACE inhibitors can enhance the hypoglycemic effect of insulin and hypoglycemic agents for oral administration up to the development of hypoglycemia. As a rule, this is observed in the first weeks of concurrent therapy and in patients with impaired renal function.
NSAIDs (including selective COX-2 inhibitors), estrogens, adrenergic agonists reduce the antihypertensive effect of lisinopril. The simultaneous use of ACE inhibitors and NSAIDs can lead to impaired renal function, including the development of acute renal failure, and an increase in serum potassium, especially in patients with reduced renal function.
With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) iv, a symptom complex has been described, including facial flushing, nausea, vomiting, and a decrease in blood pressure.
Joint use with SSRIs can lead to severe hyponatremia.
Joint use with allopurinol, procainamide, cytostatics can lead to leukopenia.
In the literature, it was reported that in patients with established atherosclerotic disease, heart failure, or diabetes mellitus with target organ damage, simultaneous therapy with an ACE inhibitor and ARA II is associated with a higher incidence of arterial hypotension, syncope, hyperkalemia, and impaired renal function (including acute renal failure ) compared with the use of only one drug that affects RAAS.
Concomitant use is contraindicated (see. “Contraindications”)
Aliskiren. In patients with diabetes mellitus or impaired renal function (GFR less than 60 ml/min), the risk of hyperkalemia, impaired renal function and an increased frequency of cardiovascular morbidity and mortality are increased.
Estramustine. Concomitant use may increase the risk of side effects, such as angioedema.
Baclofen. Enhances the antihypertensive effect of ACE inhibitors. Blood pressure should be carefully monitored and, if necessary, the dosage of antihypertensive drugs.
Gliptins (linagliptin, saxagliptin, sitagliptin, vitagliptin). Joint use with ACE inhibitors may increase the risk of angioedema due to the suppression of the activity of DPP-4 by gliptin.
Sympathomimetics. May weaken the antihypertensive effect of ACE inhibitors.
Tricyclic antidepressants, antipsychotics, and general anesthetics. Concomitant use with ACE inhibitors can lead to increased antihypertensive action (see “Precautions”).
Taking the drug together with antihypertensive drugs can provoke an additive antihypertensive effect.
Potassium-sparing diuretics, substitutes for edible salt with potassium, as well as drugs with potassium increase the possibility of developing hyperkalemia.
Combination with ACE blockers and NSAIDs increases the likelihood of impaired renal function. In rare cases, hyperkalemia is also possible.
And use in conjunction with loop and thiazide diuretics is fraught with increased antihypertensive action. This also significantly increases the risk of impaired renal function.
Indomethacin or estrogen products in combination with lisinopril reduce the antihypertensive effect of the latter. And the simultaneous use of insulin and hypoglycemic drugs can cause hypoglycemia.
The combination with clozapine leads to an increase in its content in plasma. With the simultaneous intake of lithium carbonate, its level in the blood serum increases. This may be accompanied by symptoms of lithium intoxication.
The drug also increases the effect of ethanol. The symptoms of alcohol intoxication intensify. At the same time, an increase in the hypotensive effect of Lisinopril is possible, so it is necessary to avoid alcohol during therapy with this drug or not to take it within a day after drinking alcohol.
The use of this medication in conjunction with drugs for anesthesia, narcotic analgesics, antidepressants, muscle relaxants with antihypertensive effect, as well as sleeping pills leads to an increase in the hypotensive effect.
Thrombolytics increase the likelihood of arterial hypotension. This combination should be prescribed with caution and carefully monitor the patient’s condition.
Sympathomimetics significantly weaken the hypotensive effect of the drug. A combination with drugs that have myelosuppressive effects increase the risk of agranulocytosis and/or neutropenia.
Concomitant use with Allopurinol, immunosuppressants, procainamide, cytostatics, GCS can cause leukopenia.
With dialysis therapy, anaphylactoid reactions are possible in the case of high-flow polyacrylonitrile metal sulfonate membranes.
Restrictions on the use
Severe renal impairment; bilateral renal artery stenosis or artery stenosis of a single kidney with progressive azotemia; condition after kidney transplantation; azotemia; hyperkalemia aortic stenosis/mitral stenosis/hypertrophic obstructive cardiomyopathy; primary hyperaldosteronism;
arterial hypotension; cerebrovascular disease (including cerebrovascular insufficiency); coronary artery disease; chronic heart failure; autoimmune systemic diseases of the connective tissue (including scleroderma, systemic lupus erythematosus); inhibition of bone marrow hematopoiesis;
salt restriction diet; hypovolemic conditions (including as a result of diarrhea, vomiting); elderly age; hemodialysis using high-flow dialysis membranes with high permeability; simultaneous use of potassium-sparing diuretics, potassium preparations, potassium-containing substitutes for edible salt and lithium; diabetes; surgery/general anesthesia; desensitizing therapy; apheresis of LDL; patients of the Negroid race.
Application in pregnancy and lactation
The FDA category of action on the fetus is D.
The use of lisinopril during pregnancy is contraindicated. When diagnosing pregnancy, the drug should be discontinued as soon as possible. Acceptance of ACE inhibitors in the II and III trimesters of pregnancy has an adverse effect on the fetus (a pronounced decrease in blood pressure, renal failure, hyperkalemia, hypoplasia of the skull bones, intrauterine death are possible).
There are no data on the negative effects of lisinopril on the fetus if used in the first trimester. It is recommended to monitor newborns and infants who have undergone intrauterine exposure to ACE inhibitors to timely detect a pronounced decrease in blood pressure, oliguria, hyperkalemia. Lisinopril crosses the placenta.
There is no data on the release of lisinopril into breast milk. If admission is necessary during lactation, breastfeeding must be canceled.
Detonic – a unique medicine that helps fight hypertension at all stages of its development.
The complex effect of plant components of the drug Detonic on the walls of blood vessels and the autonomic nervous system contribute to a rapid decrease in blood pressure. In addition, this drug prevents the development of atherosclerosis, thanks to the unique components that are involved in the synthesis of lecithin, an amino acid that regulates cholesterol metabolism and prevents the formation of atherosclerotic plaques.
Detonic not addictive and withdrawal syndrome, since all components of the product are natural.
Detailed information about Detonic is located on the manufacturer’s page.