Lisinopril Stada, tablets 10 mg 20 pcs
€3.89 €3.46
Lisinopril is cardioprotective, natriuretic, vasodilatory, hypotensive.
Pharmacodynamics
A ACE inhibitor, reduces the formation of angiotensin II from angiotensin I.
The decrease in angiotensin II leads to a direct decrease in aldosterone release.
Decreases bradykinin degradation and increases prostaglandin synthesis.
Limits total peripheral vascular resistance, blood pressure (BP), preload, pulmonary capillary pressure, causes an increase in the minute blood volume and increases myocardial exercise tolerance in patients with chronic heart failure.
Dilates arteries to a greater extent than veins. Some effects are explained by the effect on tissue renin-angiotensin systems.
Long-term use reduces myocardial hypertrophy and arterial resistive walls. It improves the blood supply to the ischemic myocardium.
The ACE inhibitors prolong life expectancy in patients with chronic heart failure and slow the progression of left ventricular dysfunction in patients who have had myocardial infarction without clinical manifestations of heart failure.
The antihypertensive effect begins after approximately 6 hours and lasts for 24 hours. The duration of the effect also depends on the dose.
The onset of action is 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, the stable effect develops after 1-2 months.
When the drug is abruptly withdrawn, no pronounced increase in BP has been observed.
In addition to lowering BP, lisinopril decreases albuminuria. In patients with hyperglycemia, it helps to normalize the function of the damaged glomerular endothelium.
Lisinopril has no effect on blood glucose concentration in diabetic patients and does not lead to increased incidence of hypoglycemia.
Pharmacokinetics
Intake. After oral administration, approximately 25% of lisinopril is absorbed from the gastrointestinal tract.
Eating does not affect absorption of the drug. Absorption is on average 30% and bioavailability is 29%.
Distribution. Almost does not bind with blood plasma proteins. Maximal concentration in blood plasma (90 ng/ml) is reached after 7 hours.
Permeability through the blood-brain barrier and the placental barrier is low.
Metabolism. Lisinopril is not biotransformed in the body.
Elimination. It is excreted unchanged by the kidneys. The elimination half-life is 12 hours.
Pharmacokinetics in selected patient groups
In patients with chronic heart failure the absorption and clearance of lisinopril are decreased.
In patients with renal failure, lisinopril concentrations are several times higher than plasma concentrations in volunteers, with increased time to peak plasma concentrations and increased elimination half-life.
In elderly patients the plasma concentration of the drug and area under the curve are 2 times higher than in younger patients.
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)
Acute myocardial infarction (early (in the first 24 hours) treatment of patients with stable hemodynamic parameters, to maintain these parameters and prevent left ventricular dysfunction and heart failure)
Diabetic nephropathy (to reduce albuminuria in patients with type 1 diabetes mellitus with normal blood pressure and in patients with type 2 diabetes mellitus with arterial hypertension).
Pharmacological effect
Lisinopril – cardioprotective, natriuretic, vasodilating, hypotensive.
Pharmacodynamics
ACE inhibitor, reduces the formation of angiotensin II from angiotensin I.
A decrease in angiotensin II leads to a direct decrease in aldosterone release.
Reduces the degradation of bradykinin and increases the synthesis of prostaglandins.
Reduces total peripheral vascular resistance, blood pressure (BP), preload, pressure in the pulmonary capillaries, causes an increase in minute blood volume and an increase in myocardial tolerance to stress in patients with chronic heart failure.
Dilates arteries more than veins. Some effects are explained by effects on tissue renin-angiotensin systems.
With long-term use, hypertrophy of the myocardium and the walls of resistive arteries decreases. Improves blood supply to ischemic myocardium.
ACE inhibitors prolong life expectancy in patients with chronic heart failure and slow the progression of left ventricular dysfunction in patients who have suffered a myocardial infarction without clinical manifestations of heart failure.
The antihypertensive effect begins after approximately 6 hours and lasts for 24 hours. The duration of the effect also depends on the dose.
The onset of action is after 1 hour. The maximum effect is determined after 6-7 hours. In case of arterial hypertension, the effect is observed in the first days after the start of treatment, a stable effect develops after 1-2 months.
When the drug was abruptly discontinued, no pronounced increase in blood pressure was observed.
In addition to lowering blood pressure, lisinopril reduces albuminuria. In patients with hyperglycemia, it helps to normalize the function of damaged glomerular endothelium.
Lisinopril does not affect the concentration of glucose in the blood in patients with diabetes and does not lead to an increase in cases of hypoglycemia.
Pharmacokinetics
Suction. After taking the drug orally, about 25% of lisinopril is absorbed from the gastrointestinal tract.
Eating does not affect the absorption of the drug. Absorption averages 30%, bioavailability – 29%.
Distribution. Almost does not bind to blood plasma proteins. The maximum concentration in blood plasma (90 ng/ml) is reached after 7 hours.
Permeability through the blood-brain and placental barrier is low.
Metabolism. Lisinopril is not biotransformed in the body.
Excretion. It is excreted unchanged by the kidneys. The half-life is 12 hours.
Pharmacokinetics in selected patient groups
In patients with chronic heart failure, the absorption and clearance of lisinopril is reduced.
In patients with renal failure, the concentration of lisinopril is several times higher than the concentration in the blood plasma of volunteers, and there is an increase in the time to reach the maximum concentration in the blood plasma and an increase in the half-life.
In elderly patients, the concentration of the drug in the blood plasma and the area under the curve are 2 times greater than in young patients.
Special instructions
Therapy with ACE inhibitors should be started under the control of blood pressure, taking into account the maximum effect of lisinopril after 6-8 hours (for myocardial infarction 8-10 hours).
Patients at high risk of developing dangerous adverse reactions are patients with heart failure (with or without renal failure).
In such cases, treatment with Lisinopril should be started under the strict supervision of a physician in a hospital setting.
Similar rules should also be followed when prescribing to patients with coronary heart disease or cerebrovascular insufficiency, in whom a sharp decrease in blood pressure can lead to myocardial infarction or stroke.
First-dose hypotension may occur, particularly in patients with high plasma renin activity (eg, during high-dose diuretic therapy or congestive heart failure).
A pronounced decrease in blood pressure occurs with an initially reduced volume of circulating blood due to diuretic therapy, a low-salt diet, hemodialysis, diarrhea and vomiting.
Before starting treatment with Lisinopril, it is necessary to replenish the circulating blood volume and normalize water and electrolyte imbalances.
Transient arterial hypotension is not a contraindication for taking the next dose of the drug.
When using Lisinopril, some patients with chronic heart failure with normal or low blood pressure may experience a decrease in blood pressure, which is not a reason to discontinue treatment.
For renal artery stenosis (especially with bilateral stenosis, or with stenosis of the artery of a single kidney), as well as with circulatory failure due to lack of sodium and/or fluid, use
Lisinopril can lead to an increase in the concentration of urea and creatinine in the blood, impaired renal function, and acute renal failure. Treatment with Lisinopril in acute myocardial infarction is carried out against the background of standard therapy (thrombolytics, acetylsalicylic acid (no more than 300 mg/day), beta-blockers).
Compatible with intravenous nitroglycerin and with the transdermal therapeutic system (TTS) of nitroglycerin. Surgery/general anesthesia.
During extensive surgical interventions, as well as when using other drugs that cause a decrease in blood pressure, Lisinopril, by blocking the formation of angiotensin II, can cause a pronounced, unpredictable decrease in blood pressure.
Before surgery, including dental surgery, the surgeon/anesthesiologist should be informed about the use of an ACE inhibitor. In elderly patients, the same dose leads to a higher concentration of the drug in the blood plasma, so special care is required when determining the dose.
Angioedema when using ACE inhibitors, including lisinopril, can develop at any stage of treatment. With swelling of the tongue, pharynx, and larynx, airway obstruction can develop with a fatal outcome.
If the described complaints occur, you should immediately stop taking the drug and consult a doctor.
In such cases, rapid subcutaneous administration of a solution of adrenaline 0.1% (0.3–0.5 ml), administration of glucocorticosteroids, antihistamines and/or measures to ensure airway patency are necessary.
In patients with chronic heart failure, diabetes mellitus, and concomitantly taking potassium supplements, potassium-containing salt substitutes, potassium-sparing diuretics or other drugs,
ACE inhibitors that increase the content of potassium ions in the serum (heparin) increase the risk of developing hyperkalemia.
Taking Lisinopril, like all ACE inhibitors, may be accompanied by a dry cough, which stops when the dose of the drug is reduced or treatment is stopped.
Since the potential risk of agranulocytosis cannot be excluded, periodic monitoring of the blood picture is required.
In patients taking ACE inhibitors, during desensitization with hymenoptera (bees and wasps) venom, a life-threatening anaphylactoid reaction may occur.
It is necessary to temporarily stop treatment with an ACE inhibitor before starting a course of desensitization.
Anaphylactoid reactions may occur during simultaneous hemodialysis using high-flow membranes (including AN 69®), as well as during apheresis of low-density lipoproteins with adsorption on dextran sulfate.
A different type of dialysis membrane or a different antihypertensive agent should be considered.
Patients with diabetes require careful monitoring of blood sugar, especially during the first month of therapy with Lisinopril;
Caution should be exercised when performing physical exercises and hot weather (risk of dehydration and excessive reduction in blood pressure due to a decrease in circulating blood volume).
During the treatment period, it is not recommended to drink alcoholic beverages, since alcohol enhances the hypotensive effect of the drug.
Impact on the ability to drive vehicles and operate machinery
There is no data on the effect of lisinopril in therapeutic doses on the ability to drive vehicles and machines. However, be aware that dizziness may occur, so caution should be exercised.
Active ingredient
Lisinopril
Composition
1 tablet contains:
Active substance:
Lisinopril dihydrate 5.445 mg, 10.89 mg and 21.78 mg (in terms of lisinopril 5 mg, 10 mg and 20 mg, respectively);
Excipients:
Mannitol 12.5 mg/13.0 mg/30.0 mg,
Microcrystalline cellulose 23.255 mg/25.0 mg/27.0 mg,
Ludipress LCE (lactose monohydrate 94.7–98.3%, povidone 3–4%) – 60.0 mg/61.0 mg/78.02 mg,
Povidone-K25 – 4.0 mg/4.5 mg/6.4 mg,
Colloidal silicon dioxide 2.5 mg/3.61 mg/6.0 mg,
Magnesium stearate 1.3 mg/1.5 mg/2.2 mg,
Croscarmellose sodium 5.0 mg/5.0 mg/5.0 mg,
Calcium hydrogen phosphate 16.0 mg/25.5 mg/43.6 mg.
Pregnancy
The use of lisinopril during pregnancy is contraindicated. If pregnancy is established, the drug should be stopped as soon as possible.
Taking ACE inhibitors in the second and third trimester of pregnancy has an adverse effect on the fetus (a marked decrease in blood pressure, renal failure, hyperkalemia, cranial hypoplasia, and intrauterine death are possible).
There is no data on the negative effects of the drug on the fetus when used during the first trimester.
For newborns and infants who have been exposed in utero to ACE inhibitors, it is recommended to conduct careful monitoring for timely detection of a pronounced decrease in blood pressure, oliguria, and hyperkalemia.
Lisinopril crosses the placenta. There is no data on the penetration of lisinopril into breast milk. During treatment with the drug, breastfeeding should be discontinued.
Contraindications
Hypersensitivity to lisinopril and/or other components of the drug, hypersensitivity to other ACE inhibitors, history of angioedema, including those associated with the use of inhibitors
ACE, hereditary angioedema or idiopathic angioedema, age under 18 years (efficacy and safety have not been established), pregnancy, lactation, lactase deficiency, galactosemia, glucose-galactose malabsorption syndrome.
With caution
Aortic stenosis, hypertrophic obstructive cardiomyopathy, arterial hypotension, coronary heart disease, coronary insufficiency; diet with limited salt, hyperkalemia; double-sided
renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia, condition after kidney transplantation, renal failure (creatinine clearance less than 30 ml/min), hemodialysis using high-flow dialysis membranes (AN 69®); primary hyperaldosteronism;
cerebrovascular diseases, incl. cerebrovascular insufficiency; systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus); inhibition of bone marrow hematopoiesis; hypovolemic conditions (including as a result of diarrhea, vomiting); old age (over 65 years).
Side Effects
Side effects are classified by frequency: often (1-10%), not often (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%).
From the cardiovascular system: often – marked decrease in blood pressure, orthostatic hypotension; rarely – palpitations, tachycardia, Raynaud’s syndrome, myocardial infarction, cerebrovascular stroke in patients with an increased risk of the disease.
From the central nervous system: often – dizziness, headache; not often – mood lability, paresthesia, drowsiness/insomnia; rarely – confusion; frequency unknown – depression, fainting.
From the senses: not often – disturbances of taste and smell.
From the respiratory system: often – dry cough; not often – rhinitis; very rarely – bronchospasm, sinusitis, allergic alveolitis/eosinophilic pneumonia.
From the digestive system: often – diarrhea, vomiting; not often – nausea, abdominal pain, dyspepsia; rarely – dryness of the oral mucosa; very rarely – pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, isolated cases of liver failure.
From the urinary system: often – impaired renal function; rarely – uremia, acute renal failure; very rarely – oliguria, anuria.
From the reproductive system: rarely – decreased potency, gynecomastia.
From the hematopoietic organs: rarely – decrease in hemoglobin and hematocrit; very rarely – suppression of bone marrow function, anemia, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, hemolytic anemia, lymphadenopathy.
From the skin: not often – itching; rarely – rash, alopecia, psoriasis; very rarely – increased sweating, pemphigus.
Allergic reactions: rarely – urticaria, angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities); very rarely – toxic epidermal necrolysis,
syndrome
Stevens-Johnson, erythema multiforme, cutaneous pseudolymphoma; in some cases – intestinal angioedema, a syndrome including fever, vasculitis, myalgia, arthralgia, acceleration
erythrocyte sedimentation rate (ESR) and positive test results for antinuclear antibodies, eosinophilia, leukocytosis, photosensitivity.
Laboratory indicators: not often – increased concentrations of urea and creatinine, increased activity of “liver” transaminases, hyperkalemia; rarely – hyperbilirubinemia, hyponatremia.
Other: not often – increased fatigue, asthenia; very rarely – hypoglycemia, autoimmune diseases; in some cases – inadequate secretion of antidiuretic hormone.
Interaction
Lisinopril can be used simultaneously with beta-blockers, acetylsalicylic acid (not more than 300 mg/day), thrombolytics, nitrates.
With simultaneous use of lisinopril with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, potassium-containing salt substitutes, cyclosporine, the risk of developing hyperkalemia increases, especially with impaired renal function.
Combined use is allowed only with regular monitoring of potassium levels in the blood and kidney function.
When using lisinopril with other antihypertensive agents, including diuretics, beta-blockers, slow calcium channel blockers, etc., the additive antihypertensive effect should be taken into account.
The combination of lisinopril with tricyclic antidepressants/neuroleptics, barbiturates, vasodilators, phenothiazines can lead to a significant decrease in blood pressure.
Lisinopril slows down the elimination of lithium drugs, so the concentration of lithium in the blood should be regularly monitored.
Antacids and cholestyramine reduce the absorption of lisinopril in the gastrointestinal tract.
Concomitant use of lisinopril with insulin and oral hypoglycemic agents increases the risk of hypoglycemia, especially during the first month of ACE inhibitor therapy.
Nonsteroidal anti-inflammatory drugs, including selective cyclooxygenase-2 inhibitors, estrogens and adrenergic agonists help reduce the antihypertensive effect of lisinopril.
With the simultaneous use of ACE inhibitors and gold preparations for intravenous administration (sodium aurothiomalate), a symptom complex has been described, including facial flushing, nausea, vomiting and decreased blood pressure.
The combined use of lisinopril with selective serotonin reuptake inhibitors can lead to severe hyponatremia and a pronounced decrease in blood pressure.
Combined use with allopurinol, procainamide, cytostatics can lead to leukopenia.
Ethanol enhances the effect of the drug.
Overdose
Symptoms:
marked decrease in blood pressure, cough, dryness of the oral mucosa, dizziness, anxiety, increased irritability, drowsiness, vascular collapse, increased breathing, palpitations, tachycardia, bradycardia, water-electrolyte imbalance, renal failure, urinary retention.
Treatment:
gastric lavage, absorbent agents, placing the patient in a horizontal position with raised legs, intravenous administration of 0.9% sodium chloride solution, if necessary, vasopressor drugs, monitoring blood pressure, water-electrolyte balance, creatinine. For persistent bradycardia, use an artificial pacemaker. Hemodialysis is effective.
Storage conditions
In a dry place, protected from light and out of reach of children, at a temperature not exceeding 25°C.
Shelf life
3 years
Manufacturer
Hemofarm LLC, Russia
Shelf life | 3 years |
---|---|
Conditions of storage | In a dry place out of the reach of children, protected from light, at a temperature not exceeding 25°C. |
Manufacturer | Chemopharm LLC, Russia |
Medication form | pills |
Brand | Chemopharm LLC |
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