Lisinopril-Vertex, tablets 10 mg 60 pcs

A ACE inhibitor, reduces the formation of angiotensin II from angiotensin I. Reduction of angiotensin II leads to a direct reduction of aldosterone release. Reduces 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 tolerance to exercise in patients with chronic heart failure.

Dilates arteries to a greater extent than veins. Some effects are explained by the effect on the tissue renin-angiotensin-aldosterone system. Long-term use reduces myocardial hypertrophy and resistive arterial wall hypertrophy. It improves the blood supply to the 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 had myocardial infarction without clinical manifestations of heart failure.

The onset of action is within 1 hour. Maximal antihypertensive effect is determined after 6-7 hours and sustained for 24 hours. With arterial hypertension the effect is noted in the first days after the start of treatment, a stable effect develops after 1-2 months. In case of abrupt withdrawal of the drug no marked increase in BP was noted.

In addition to decreasing BP, lisinopril decreases albuminuria. Lisinopril does not affect blood glucose concentration in diabetic patients and does not lead to increased incidence of hypoglycemia.

Indications

Arterial hypertension (in monotherapy or in combination with other hypotensive agents).

Chronic heart failure (as part of combined therapy for the treatment of patients taking cardiac glycosides and/or diuretics).

Early treatment of acute myocardial infarction as part of combined therapy (in the first 24 hours with stable hemodynamic parameters to maintain these parameters and prevent left ventricular dysfunction and heart failure).

Diabetic nephropathy (reduction of albuminuria in patients with type 1 diabetes with normal blood pressure, and in patients with type 2 diabetes with arterial hypertension).

Active ingredient

Composition

1 tablet contains:

Active substance:

lisinopril dihydrate (corresponds to lisinopril) 10 mg,

Auxiliary substances:

Milk sugar (lactose);

MCC;

Starch 1500 (pregelatinized);

aerosil (colloidal silica);

talc;

magnesium stearate.

How to take, the dosage

Overly, once daily in the morning, regardless of meals, preferably at the same time.

In patients with arterial hypertension who are not receiving other hypotensive agents, 5 mg once daily is prescribed. If there is no 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 further reduction of BP). 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. If there is insufficient clinical effect, it is possible to combine the drug with other hypotensive agents.

If the patient has received prior treatment with diuretics, the intake of these drugs should be discontinued 2-3 days before the start of the drug Lisinopril. If this is not possible, the initial dose of Lisinopril should not exceed 5 mg per day. In this case, after the first dose it is recommended to have a physician’s control for several hours (the maximum effect is reached after about 6 hours), since a marked decrease in BP may occur.

In renovascular hypertension or other conditions with increased activity of renin-angiotensin-aldosterone system it is reasonable to prescribe also a low initial dose of 5 mg per day, under increased medical supervision (BP control, renal function, serum potassium ion content). The maintenance dose, while continuing close monitoring by a physician, should be determined depending on the dynamics of BP.
In renal insufficiency, due to the fact that lisinopril is excreted by the kidneys, the initial dose should be determined according to creatinine clearance. Further the doses should be adjusted according to individual reactions with regular control of renal function, serum potassium and sodium content.

Creatinine clearance,
ml/min Initial dose,
mg/day
30-70 5-10
10-30 5
(including patients on hemodialysis)

/p>

In persistent arterial hypertension, long-term maintenance therapy of 10-15 mg/day is indicated.

In chronic heart failure: the initial dose is 2.5 mg per day, with gradual increase after 3-5 days to 5-10 mg per day. The maximum daily dose is 20 mg.

Acute myocardial infarction (as part of combined therapy): in the first 24 hours – 5 mg, then 5 mg every other day, 10 mg every two days and then 10 mg once a day. The course of treatment is at least 6 weeks.

In case of long expressed BP lowering (systolic BP less than 90 mmHg for more than 1 hour) the drug treatment should be discontinued.
Diabetic nephropathy: In patients with diabetes mellitus type 2 the preparation 10 mg of Lisinopril 1 time per day is used. The dose can be increased to 20 mg once a day, if necessary, in order to achieve values of diastolic blood pressure below 75 mmHg in sitting position. In patients with diabetes mellitus type 1 the dose is identical in order to achieve values of diastolic BP below 90 mmHg in sitting position.

Interaction

In concomitant use of the drug with potassium-saving diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, cyclosporine the risk of hyperkalemia increases, especially with impaired renal function, so they can be used together only with regular monitoring of serum potassium ions and renal function.

Combined use of lisinopril with beta-adrenoblockers, “slow” calcium channel blockers (SCBs), diuretics, tricyclic antidepressants/neuroleptics and other hypotensive agents increases the severity of hypotensive effect.
Lisinopril slows excretion of lithium preparations. Therefore, when using together it is necessary to monitor serum lithium concentration regularly.

Antacids and colestiramine decrease absorption of lisinopril in gastrointestinal tract.

When combined with insulin and hypoglycemic agents for oral administration, there may be a risk of hypoglycemia.
Non-steroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase-2 (COX-2) inhibitors), estrogens, adrenomimetics decrease hypotensive effect of lisinopril.

When ACE inhibitors and intravenous gold drugs (sodium aurothiomalate) are used concomitantly, a symptom complex including facial hyperemia, nausea, vomiting and decreased BP has been described.

When co-administered with selective serotonin reuptake inhibitors may lead to severe hyponatremia.
Concomitant use with allopurinol, procainamide, cytostatics may lead to leukopenia.

Special Instructions

Symptomatic hypotension

Most often a pronounced decrease in BP occurs with a decrease in circulating blood volume (CBC) caused by diuretic therapy, reduction of table salt in food, dialysis, diarrhea or vomiting. In patients with chronic heart failure with or without concomitant renal failure, a pronounced decrease in BP is possible.

Under strict medical supervision, Lisinopril should be used in patients with coronary heart disease, cerebrovascular insufficiency, in whom a sharp decrease in BP may lead to myocardial infarction or stroke. Transient arterial hypotension is not a contraindication for the next dose of the drug.

When using Lisinopril, some patients with chronic heart failure but with normal or reduced BP may experience a decrease in BP, which is usually not a reason to discontinue treatment.

Before starting treatment with the drug, if possible, sodium should be normalized and/or the BOD should be replenished and the effect of the initial dose of Lisinopril on the patient should be carefully monitored.

In cases of renal artery stenosis (especially with bilateral stenosis or in the presence of artery stenosis of the only kidney), as well as circulatory failure due to lack of sodium ions and/or fluid, use of Lisinopril may lead to renal dysfunction, acute renal failure, which is usually irreversible even after drug withdrawal.

In acute myocardial infarction

Standard therapy (thrombolytics, acetylsalicylic acid, beta-adrenoblockers) is indicated. Lisinopril may be combined with intravenous or therapeutic nitroglycerin transdermal systems.

Surgery/general anesthesia

In major surgical interventions, as well as when using other agents that cause BP reduction, Lisinopril, by blocking angiotensin II formation, may cause a pronounced unpredictable decrease in BP.

In elderly patients, the same dose results in higher blood concentrations of the drug, so special caution is required in determining the dose.

Because the potential risk of agranulocytosis cannot be excluded, periodic monitoring of blood counts is required. Anaphylactic shock may occur when the drug is used in dialysis with polyacrylonitrile membranes, so either a different type of dialysis membrane or administration of other antihypertensive agents is recommended.

Impact on the ability to drive and operate vehicles

There are no data about the effect of the drug Lisinopril on the ability to drive vehicles and operate mechanisms when used in therapeutic doses, but it should be taken into account that at the beginning of treatment arterial hypotension may occur, which may affect the ability to drive vehicles and operate potentially dangerous mechanisms, and dizziness and somnolence may occur, so caution should be exercised.

Contraindications

Hypersensitivity to lisinopril or other ACE inhibitors.

An history of angioedema, including during use of ACE inhibitors.

Hereditary Quincke’s edema or idiopathic angioedema.

Pregnancy and lactation.

Age under 18 years (efficacy and safety not established).

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome.

With caution

. Severe renal dysfunction, bilateral renal artery stenosis or artery stenosis of the sole kidney with progressive azotemia, post renal transplantation condition, azotemia, hyperkalemia, aortic orifice stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular disease (including cerebrovascular insufficiency), coronary heart disease, coronary artery disease, autoimmune systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus); Inhibition of medullary hematopoiesis; diet with restriction of table salt; hypovolemic conditions (including those caused by diarrhea, vomiting, and diarrhea). including those caused by diarrhea and vomiting; elderly age; hemodialysis with high permeability dialysis membranes (AN69®).

Side effects

The frequency of side effects is described as frequent (1%), rare (1%).

The most common side effects: dizziness, headache, increased fatigue, diarrhea, dry cough, nausea.

Cardiovascular system: often – marked BP decrease, orthostatic hypotension; rarely – chest pain, tachycardia, bradycardia, worsening of symptoms of chronic heart failure, atrioventricular conduction disorder, myocardial infarction.

The central nervous system: often – paresthesias, mood lability, confusion, somnolence, convulsive twitching of limbs and lips muscles, rarely – asthenic syndrome.

Blood organs: rarely – leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with prolonged treatment – anemia (decrease of hemoglobin, hematocrit, erythropenia).

Respiratory system: rarely – shortness of breath, bronchospasm.

Gastrointestinal system: rare – dry mouth, anorexia, dyspepsia, changes in taste, abdominal pain, pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis.

Skin disorders: rarely – urticaria, itching, increased sweating, alopecia, photosensitization.

Urinary system disorders: rarely – renal dysfunction, oliguria, anuria, acute renal failure, uremia, proteinuria, decreased potency.

Laboratory indices: frequently – hyperkalemia, hyponatremia; rarely – hyperbilirubinemia, increased liver enzymes activity, hypercreatininemia, increased concentration of urea and creatinine.

Allergic reactions: rare – angioedema of the face, limbs, lips, tongue, epiglottis and/or larynx, skin rash, skin itching, fever, false positive results of antinuclear antibodies test, increased sedimentation rate of red blood cells (sed rate), eosinophilia, leukocytosis. In rare cases, intestinal angioedema.

Other: arthralgia/arthritis, vasculitis, myalgia.

Overdose

Symptoms (occurring with a single dose of 50 mg): marked decrease in BP, dry mouth, drowsiness, urinary retention, constipation, restlessness, increased irritability.

Treatment:no specific antidote. Symptomatic therapy. Gastric lavage, use of enterosorbents and laxatives. Intravenous administration of 0.9% sodium chloride solution is indicated. In the case of treatment-resistant bradycardia, it is necessary to use an artificial rhythm driver. Control of BP and water-electrolyte balance is necessary. Hemodialysis is effective.

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