IRUMED
Active material: Lisinopril
When ATH: C09AA03
CCF: ACE inhibitor
ICD-10 codes (testimony): I10, I15.0, I21, I50.0, N08.3
When CSF: 01.04.01.02
Manufacturer: BELUPO Pharmaceuticals & Cosmetics d.d. (Croatia)
Pharmaceutical form, composition and packaging
Pills white, round, lenticular, with Valium on one side.
| 1 tab. | |
| Lisinopril (in the form of dihydrate) | 2.5 mg |
Excipients: mannitol, Calcium phosphate dihydrate, corn starch, pregelatinized corn starch, colloidal silicon dioxide, magnesium stearate.
30 PC. – blisters (1) – packs cardboard.
Pills white, round, Valium, with Valium on one side.
| 1 tab. | |
| Lisinopril (in the form of dihydrate) | 5 mg |
Excipients: mannitol, Calcium phosphate dihydrate, corn starch, pregelatinized corn starch, colloidal silicon dioxide, magnesium stearate.
30 PC. – blisters (1) – packs cardboard.
Pills light yellow, round, Valium, with Valium on one side.
| 1 tab. | |
| Lisinopril (in the form of dihydrate) | 10 mg |
Excipients: mannitol, Calcium phosphate dihydrate, corn starch, pregelatinized corn starch, dye iron oxide yellow (E172), colloidal silicon dioxide, magnesium stearate.
30 PC. – blisters (1) – packs cardboard.
Pills peach-colored, round, Valium, with Valium on one side.
| 1 tab. | |
| Lisinopril (in the form of dihydrate) | 20 mg |
Excipients: mannitol, Calcium phosphate dihydrate, corn starch, pregelatinized corn starch, dye iron oxide yellow (E172), iron oxide red dye (E172), colloidal silicon dioxide, magnesium stearate.
30 PC. – blisters (1) – packs cardboard.
Pharmacological action
ACE inhibitor. Antihypertensive drugs. The mechanism of action is associated with inhibition of ACE activity, which leads to suppression of the formation of angiotensin II from angiotensin I and to the direct reduction of aldosterone release. It reduces the degradation of bradykinin, and increases the synthesis of prostaglandins.
Reduces PR, FROM, preload, the pressure in the pulmonary capillaries, It causes an increase in cardiac output and increase exercise tolerance in patients with chronic heart failure. Lisinopril exerts vasodilating effects, wherein the artery expands to a greater extent, than veins. Some effects are explained by the influence on the tissue renin-angiotensin system. It improves blood flow to ischemic myocardium. Prolonged use reduces myocardial hypertrophy and arterial walls resistive type.
The use of ACE inhibitors in patients with chronic heart failure leads to an increase in life expectancy; patients, myocardial infarction, without clinical symptoms of heart failure – to slow the progression of left ventricular dysfunction.
The onset of action observed after 1 h after dosing, maximum effect through 6-7 no, duration – 24 no. When hypertension effect observed in the first days after the start of treatment, stable operation is developed through 1-2 of the month.
With a sharp lifting of the drug was not observed pronounced increase in blood pressure. In addition to lowering blood pressure, lisinopril reduces albuminuria. Patients with hyperglycemia helps normalize the function of the damaged glomerular endothelial. Lisinopril does not affect the concentration of glucose in the blood plasma of patients with diabetes, and does not lead to increased incidence of hypoglycemia.
Pharmacokinetics
Absorption
After oral administration about 25% lisinopril is absorbed from the gastrointestinal tract. Food intake has no effect on the absorption of lisinopril. Absorption averages 30%. Bioavailability – 29%. Cmax in plasma is approximately 6-8 no.
Distribution
Weakly bound to plasma proteins. Lisinopril slightly penetrate the BBB, the placental barrier.
Deduction
T1/2 – 12 no. Lisinopril is not metabolised and is excreted unchanged in the urine.
Testimony
- Arterial hypertension (alone or in combination with other antihypertensives);
- Congestive heart failure (in a combination therapy for the treatment of patients, taking drugs digitalis and / or diuretics);
- Early treatment of acute myocardial infarction (as part of combination therapy in the first 24 hours in patients with stable hemodynamic parameters, to maintain these parameters and prevent left ventricular dysfunction and heart failure);
- Diabeticheskaya nephropathy (to reduce albuminuria in insulin-dependent patients with normal blood pressure and insulin dependent patients with hypertension).
Dosage regimen
The drug is prescribed inside. Eating does not affect the absorption, so the drug can be taken up, during or after a meal. Multiplicity of reception 1 time / day (at about the same time).
At treatment of essential hypertension It recommended to prescribe a starting dose 10 mg. The maintenance dose is 20 mg / day. The maximum daily dose – 40 mg. For the full development of the effect may require 2-4-week course of treatment (it should be taken into account when the dose is increased). If the application of the highest dose not causing a sufficient therapeutic effect, the possible appointment of additional other agents.
Patients, taking diuretics, Treatment with diuretics should be discontinued 2-3 days before the start of treatment Irumedom®. Patients, from which it is impossible to stop treatment with diuretics, Irumed® administered in an initial dose of 5 mg / day.
At renovascular hypertension or other conditions with increased function of the renin-angiotensin-aldosterone system Irumed® administered in an initial dose of 2.5-5 mg / day under the control of blood pressure, renal function, potassium concentration in blood serum. Maintenance dose is adjusted depending on the blood pressure.
In patients with renal insufficiency and patients, hemodialysis, initial dose set depending on QC. Maintenance dose is determined depending on the blood pressure (under the control of renal function, Sodium and potassium levels in the blood).
| CC | The initial daily dose |
| 30-70 ml / min | 5-10 mg |
| 10-30 ml / min | 2.5-5 mg |
| < 10 ml / min | 2.5 mg |
At chronic heart failure Lisinopril use may simultaneously with diuretics and / or cardiac glycosides. If possible, the diuretic dose should be reduced prior to receiving lisinopril. The initial dose is 2.5 mg 1 time / day, further gradually increased (on 2.5 mg after 3-5 days) to 5-10 mg / day. The maximum dose – 20 mg / day.
At acute myocardial infarction (as part of combination therapy in the first 24 h in patients with stable hemodynamics) first 24 h prescribed 5 mg, then – 5 mg a day, 10 mg – two days later, and then – 10 mg 1 time / day. In patients with acute myocardial infarction drug is used for 6 weeks. At the start of treatment or during the first 3 days after acute myocardial infarction patients with low systolic blood pressure (120 mmHg. or below) the drug is prescribed in a dose 2.5 mg. In case of arterial hypotension (systolic blood pressure less than or equal 100 mmHg.) daily dose 5 mg can be temporarily reduced to 2.5 mg. In the case of longer hypotension (systolic BP below 90 mmHg. more 1 no) reception Irumeda® discontinue.
At diabetic nephropathy in patients with diabetes mellitus type 1 (insulin) Irumed® administered at a dose of 10 mg 1 time / day. If necessary, the dose can be increased to 20 mg / day to achieve diastolic BP values below 75 mmHg. in the sitting position. In patients with diabetes mellitus type 2 (insulinnezavisimym) The same dose to achieve diastolic BP values below 90 mmHg. in the sitting position.
Side effect
Frequently: dizziness, headache, fatigue, diarrhea, dry cough, nausea.
Cardio-vascular system: marked reduction in blood pressure, chest pain; rarely – orthostatic hypotension, tachycardia, bradycardia, worsening symptoms of heart failure, violation of AV-conduction, myocardial infarction.
From the central and peripheral nervous system: mood lability, perplexity, paresthesia, drowsiness, jerking of the limbs and lips; rarely – asthenic syndrome.
From the digestive system: dry mouth, anorexia, dyspepsia, change in taste, abdominal pain, pancreatitis, hepatocellular or cholestatic, jaundice, hepatitis, increase in liver transaminases, giperʙiliruʙinemija.
The respiratory system: dyspnoea, bronchospasm.
Dermatological reactions: increased perspiration, itching, alopecia, photosensitivity.
From the side of hematopoiesis: leukopenia, thrombocytopenia, neutropenia, agranulocytosis, anemia (decrease in hematocrit, Hemoglobin, erythropenia).
Metabolism: hyperkalemia, giponatriemiya, hyperuricemia, increase of blood creatinine.
From the urinary system: impairment of renal function, oligurija, anurija, uremia, proteinemiya.
Allergic reactions: hives, angioneurotic edema of the face, limbs, lips, language, epiglottis and / or larynx, skin rash, itch, fever, test positive for antinuclear antibodies, increased erythrocyte sedimentation rate, eozinofilija, leukocytosis; in some cases – Interstitial angioedema.
Other: arthralgia / arthritis, myalgia, vasculitis, reduced potency.
Contraindications
- A history of angioedema (incl. the application of ACE inhibitors);
- Hereditary angioedema or idiopathic edema;
- Pregnancy;
- Lactation (breast-feeding);
- Up to 18 years (efficacy and safety have not been established);
- Hypersensitivity to lisinopril other ACE inhibitors;
FROM caution should be prescribed the drug for aortic stenosis, cerebrovascular diseases (incl. cerebrovascular insufficiency), CHD, coronary insufficiency, severe autoimmune systemic diseases of connective tissue (incl. SLE, scleroderma), the oppression of bone marrow hematopoiesis, diabetes, hyperkalemia, bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, if condition after kidney transplantation, renal failure, azotemii, primary hyperaldosteronism, hypotension, hypoplasia of the bone marrow, hypertrophic obstructive cardiomyopathy, hypotension, against a diet restricted salt, states, accompanied by a decrease in the bcc (incl. diarrhea, vomiting), elderly patients.
Pregnancy and lactation
Application Irumeda® Pregnancy and lactation (breast-feeding) contraindicated.
Lisinopril crosses the placental barrier. In the event of pregnancy treatment Irumedom® should cease immediately. ACE inhibitors in the II and III trimester of pregnancy can cause the death of the fetus and newborn. Newborns can develop skull hypoplasia, oligogidramnion, deformation of the bones of the skull and face, pulmonary hypoplasia, violation of kidney. For newborns and babies, whose mothers during pregnancy, ACE inhibitors, careful monitoring is recommended for early detection of significant decrease in blood pressure, oligurii, hyperkalemia.
No data on the penetration of lisinopril in breast milk. During treatment with Irumed® breastfeeding should be abolished.
Cautions
It should be taken into account, marked reduction in blood pressure that occurs with a decrease in the volume of liquid, caused by diuretic therapy, while reducing salt in foods, during dialysis in patients with diarrhea or vomiting. Patients with chronic heart failure with simultaneous renal insufficiency or without may develop symptomatic hypotension, which is often seen in patients with severe heart failure, as a consequence of the use of high doses of diuretics, hyponatremia or impaired renal function. In these patients, treatment should start under close medical supervision (with caution in the selection of dose and diuretics). This tactic should be followed in the appointment of Irumeda® patients with coronary artery disease, cerebrovascular insufficiency, in which the sharp decline in blood pressure can lead to heart attack or stroke.
In the case of significant decrease in blood pressure patient should be given a horizontal position and, if necessary, in / enter 0.9% sodium chloride solution. Transient hypotensive response is not a contraindication to receiving the next dose.
When using Irumeda® in some patients with chronic heart failure, but with normal or low blood pressure may experience a decrease in blood pressure, which is usually not a cause for discontinuation of treatment. When, If hypotension becomes symptomatic, you need to decrease the dose or discontinuation of treatment Irumedom®.
In acute myocardial infarction shows the use of standard therapy (thrombolytics, acetylsalicylic acid, beta-blockers). Irumed® It can be applied in conjunction with / in the introduction or use of transdermal nitroglycerin systems.
Irumed® should not be administered to patients with acute myocardial infarction, in which there is a risk of further deterioration of the hemodynamic expressed after application of vasodilators: patients with systolic blood pressure 100 mmHg. or below, or cardiogenic shock.
In patients with chronic heart failure, marked reduction in blood pressure after initiation of therapy with ACE inhibitors may result in further deterioration of renal function. Cases of acute renal failure. In patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, ACE inhibitor, was an increase in urea and serum creatinine, usually reversible upon discontinuation of treatment (more frequent in patients with renal insufficiency).
Lisinopril is not indicated for acute myocardial infarction in patients with severe renal impairment with serum creatinine content 177 mmol / l or more proteinuria 500 mg / day. If renal dysfunction develops during treatment with the drug (of serum creatinine 265 mmol / l or increase in 2 times, as compared with before treatment), It should assess the need to continue therapy with Irumed®.
Patients, taking ACE inhibitors, including lisinopril, rarely develop angioedema face, limbs, lips, language, epiglottis and / or larynx, and its development is possible at any time during treatment. In this case, treatment Irumedom® as soon as possible to stop the sick and set up observation of complete regression of symptoms. However, in cases, When swelling occurs only on the face and lips and most of the state is normalized without treatment, possible appointment of antihistamines.
In the propagation of the language of angioedema, epiglottis or larynx may occur airway obstruction fatal, why you should immediately conduct appropriate therapy (0.3-0.5 ml 1:1000 epinephrine solution n / a) and / or measures to ensure airway. Noted, that patients with blacks, taking ACE inhibitors, angioneurotic edema develops most, than patients of other races. Patients, a history which has been angioedema, not related to previous treatment with an ACE inhibitor, It may be at increased risk of its development during treatment Irumedom®.
Patients, taking ACE inhibitors, during desensitization to Hymenoptera venom (this, Bees, Ants), rarely may develop anaphylactoid reactions. This can be avoided, if temporarily discontinue treatment with an ACE inhibitor prior to each desensitization.
It should be taken into account, that patients, taking ACE inhibitors and undergoing hemodialysis using highly permeable dialysis membranes (eg, AN69), can develop an anaphylactic reaction. In such cases it is necessary to consider the use of another type of membrane dialysis or other antihypertensives.
When using ACE inhibitors observed cough (dry, long, which disappears after discontinuation of treatment with an ACE inhibitor). In the differential diagnosis of cough and cough should be considered, resulting from the use of an ACE inhibitor.
When using drugs, lowering blood pressure, in patients with extensive surgery or during general anesthesia lisinopril may block the formation of angiotensin II, secondary to compensatory renin release. Marked decrease in blood pressure, which is considered a consequence of this mechanism, You can eliminate the increase in BCC. Before surgery (including dental surgery) should inform the surgeon / anesthesiologist on the use of an ACE inhibitor.
In some cases, there is hyperkalemia. Risk factors for the development of hyperkalemia include renal insufficiency, diabetes mellitus, and the simultaneous use of potassium-sparing diuretics (spironolactone, triamterene or amiloride), drugs or potassium salt substitutes, containing potassium, especially in patients with impaired renal function. If necessary, the application of these combinations should regularly monitor the level of potassium in the blood serum.
Patients, in which there is a risk of symptomatic hypotension (are on a salt-free diet or malosolevoy) with / without hyponatremia, and in patients, who received high doses of diuretics, above the state before treatment is necessary to compensate (loss of fluids and salts). It is necessary to monitor the effect of the initial dose Irumed® the value of BP.
Effects on ability to drive vehicles and management mechanisms
No data on the effect Irumeda®, used in therapeutic doses, the ability to drive vehicles and mechanisms, However, it should be taken into account, that may cause vertigo. Therefore, during treatment, patients should be careful when driving and work, require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: marked reduction in blood pressure, dry mouth, drowsiness, urinary retention, constipation, anxiety, irritability.
Treatment: symptomatic therapy, in / in a saline solution and, if necessary, the use of vasopressor agents under the control of blood pressure and water and electrolyte balance. Perhaps the use of hemodialysis.
Drug Interactions
In an application Irumeda® with potassium-sparing diuretics (spironolactone, triamterene, amilorid), potassium supplements, salt substitutes, containing potassium, increased risk of hyperkalemia, especially in patients with impaired renal function.
In an application Irumeda® diuretics observed marked reduction of blood pressure.
In an application Irumeda® with other antihypertensive agents observed an additive effect.
In an application Irumeda® NSAIDs, Estrogen, adrenostimulyatorov reduced antihypertensive effect of lisinopril.
In an application Irumeda® lithium slows excretion of lithium from the body.
In an application Irumeda® kolestiraminom with antacids and reduced absorption from the gastrointestinal tract of lisinopril.
Ethanol enhances the effect of the drug.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children at a temperature of 25 ° C. Shelf life – 2 year.
