Cardiomagnil 75mg+15.2 mg tbl p / Ob N100

Manufacturer: Такеда
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Brief information

Производитель

Такеда

Действующее вещество

Ацетилсалициловая кислота+Магния гидроксид
There are contraindications, specialist advice is required

The appearance of the product may differ from the photos on the site.

General description
Источник:  РЛС

Composition

Solution for intravenous administration1 ml
active substance: 
urapidil hydrochloride5.47 mg
in terms of urapidil5 mg
excipients: propylene glycol-100 mg; sodium hydrophosphate dihydrate-0.42 mg; sodium dihydrophosphate dihydrate-2.22 mg; water for injection-up to 1 ml 
Capsules of the prolonged action1 caps.
active substance: 
urapidil30 mg
excipients: sugar grits-62.43 mg; methacrylic acid and methyl methacrylate copolymer (1:2) - 0.62 mg; talc-1.18 mg; diethylphthalate-0.06 mg; fumaric acid-8.88 mg; hypromellose-11.28 mg; ethylcellulose-1.75 mg; stearic acid-0.47 mg; hypromellose phthalate-0.72 mg 
capsule shell: gelatin-32.707 mg; titanium dioxide (E171) - 1.2 mg; iron oxide yellow dye-0.293 mg; purified water-5.8 mg 
purified black ink for marking: (shellac, iron dye black oxide (E172), propylene glycol) - no more than 0.19 mg 
sugar grits: sucrose-80-91. 5%; corn starch-8.5-20%; purified water - no more than 1.5% 
Capsules of the prolonged action1 caps.
active substance: 
urapidil60 mg
excipients: sugar grits-124.86 mg; methacrylic acid and methyl methacrylate copolymer (1:2) - 1.24 mg; talc-2.35 mg; diethylphthalate-0.12 mg; fumaric acid-17.77 mg; hypromellose-22.55 mg; ethylcellulose-3.51 mg; stearic acid-0.95 mg; hypromellose phthalate-1.43 mg 
capsule shell: gelatin-52.071 mg; titanium dioxide (E171) - 1.764 mg; indigocarmine-0.03 mg; purified water-9.135 mg 
sugar grits: sucrose-80-91. 5%; corn starch-8.5-20%; purified water - no more than 1.5% 

Description of the dosage form

Solution for intravenous administration: transparent, colorless.

Capsules, 30 mg: gelatinous solid ( 4) with an opaque body and a yellow lid, with the black label Ebr 30 applied to the body.

Capsules, 60 mg: solid gelatin ( 2) with opaque body and light blue lid.

Capsule contents: granules of yellow color.

Pharmacokinetics

Solution for intravenous administration

After intravenous administration of 25 mg of urapidil, there is a two-phase decrease in the concentration of the drug: first, a rapid decrease (α-phase), and then a slow (β-phase).

The distribution period of the drug is about 35 minutes.

V d — 0.8 l / kg (0.6-1.2 l / kg). Most of urapidil is metabolized in the liver. The main metabolite is a derivative hydroxylated in the 4th position of the benzene ring, which practically does not have antihypertensive activity.

The o-demethylated metabolite is formed in very small amounts and is almost as active as urapidil. 50-70% of urapidil and its metabolites (15% - as an active drug) are excreted by the kidneys, the rest is excreted through the intestines as metabolites (mainly in the form of inactive parahydroxylated urapidil).

T 1/2 after I / V bolus injection is 2.7 h (1.8–3.9 h). The connection with plasma proteins is 80%. The relatively low degree of binding to plasma proteins explains that it is unknown whether urapidil can interact with drugs that bind strongly to plasma proteins.

In elderly patients, as well as in patients with severe hepatic and / or renal insufficiency, V d and urapidil clearance are reduced, and T 1/2 is increased.

Urapidil penetrates the BBB and placental barrier.

Capsules of the prolonged action

After oral administration, 80-90% of urapidil is absorbed into the gastrointestinal tract. The bond with plasma proteins is approximately 80%, and V d is 0.77 l/kg.

C max in blood plasma is reached 4-6 hours after ingestion; T 1/2 is approximately 4.7 hours (3.3–7.6 hours).

It is mainly metabolized in the liver. The main metabolite is a hydroxylated derivative (in the 4th position of the benzene ring), which has almost no antihypertensive activity. The o-demethylated metabolite is formed in very small amounts and is almost as active as urapidil.

50-70% of urapidil and its metabolites (15% - as an active substance) are excreted by the kidneys, the rest is excreted through the intestines as metabolites (mainly in the form of inactive parahydroxylated urapidil).

In the elderly and patients with severe hepatic and / or renal insufficiency, V d and clearance are reduced, and T 1/2 is increased.

Penetrates the BBB and placental barrier.

The relative bioavailability of long-acting capsules, compared with urapidil solution for oral administration, is 92% (83-103%).

Pharmacodynamics

Solution for intravenous administration

Ebrantil is a drug that blocks postsynaptic α 1-adrenergic receptors, which reduces peripheral resistance. In addition, the drug Ebrantil regulates the Central mechanism of maintaining vascular tone and has a weak β-adrenoblocking effect. The heart rate and cardiac output do not change when it is administered. Low cardiac output can be increased by reducing vascular resistance. Orthostatic phenomena, as a rule, the drug Ebrantil does not cause. It blocks vasoconstriction caused by α 2-adrenergic receptors and does not cause reflex tachycardia caused by vasodilation.

The drug Ebrantil balanced reduces sad and DAP, reducing peripheral resistance.

Urapidil reduces pre-and post-loading on the heart, increases the efficiency of cardiac contraction, thus, in the absence of arrhythmia, the drug increases the reduced minute volume of the heart.

Mechanism of action. The drug Ebrantil has a Central and peripheral mechanisms of action.

It mainly blocks peripheral postsynaptic α 1-adrenoreceptors, i.e. the drug blocks the vasoconstrictive action of catecholamines, which reduces the OPSS.

Regulates the Central mechanism of maintaining vascular tone by stimulating serotonin 5-HT 1A receptors of the vasomotor center (prevents reflex increase in the tone of the sympathetic nervous system).

Heart rate and cardiac output do not change. Low cardiac output can be increased by reducing the heart rate.

Stimulates presynaptic α 2-adrenergic receptors.

Reduces sad and DAP, does not cause reflex tachycardia.

Reduces pre-and post-load on the heart, increases the efficiency of heart contraction, thus (in the absence of arrhythmia) increases the reduced minute volume of the heart.

Urapidil does not affect the indicators of carbohydrate metabolism, uric acid metabolism and does not cause fluid retention in the body.

Indications of the drug

Solution for intravenous administration

hypertensive crisis;

refractory and severe arterial hypertension;

controlled arterial hypotension during and / or after surgery.

Capsules of the prolonged action

Severe hypertension (in combination therapy).

Contraindications

Solution for intravenous administration

hypersensitivity to the drug;

aortic stenosis;

open Botall duct;

arteriovenous fistula (except for a hemodynamically inactive dialysis shunt);

breastfeeding period (efficacy and safety not established);

the age of 18.

With caution in: elderly; impaired liver and/or kidney disease; hypovolemia; patients with heart failure, the cause of which is a violation of the mechanical function (e.g. stenosis of the aortic or mitral valve), pulmonary embolism or heart disorder as a result of diseases of the pericardium; concurrent use with cimetidine (see Interactions); concomitant use with ACE inhibitors (clinical data, the simultaneous application of urapidil is limited).

Capsules of the prolonged action

hypersensitivity to the active substance and other components of the drug;

fructose intolerance and glucose/galactose malabsorption syndrome or sucrose/isomaltase deficiency;

pregnancy, lactation;

age under 18 (efficacy and safety not established).

With caution: impaired liver function; moderate/severe renal failure; chronic heart failure; aortic or mitral valve stenosis; pulmonary embolism; impaired myocardial contractility due to heart bag disease (including tamponade, chronic pericarditis); concomitant use with cimetidine; old age.

Use during pregnancy and lactation

Solution for intravenous administration

The drug Ebrantil, a solution for intravenous administration, is not recommended for use during pregnancy due to the fact that urapidil penetrates the placental barrier, except in cases where the potential benefit to the mother exceeds the potential risk to the fetus.

Clinical data on its use in the first and second trimesters of pregnancy are not available, data on the use of the drug in the third trimester are limited. Animal studies have shown no signs of fetal damage.

It is currently unknown whether urapidil is excreted in breast milk, so breastfeeding should be stopped during urapidil treatment.

Capsules of the prolonged action

Ebrantil should not be used during pregnancy and during breastfeeding due to the lack of clinical data on its use.

Dosage and administration

Solution for intravenous administration

In/in.

Enter the jet or by prolonged infusion in the patient's supine position.

Hypertensive crisis, severe arterial hypertension, refractory hypertension

1. In/in-10-50 mg of the drug Ebrantil is slowly administered under the control of blood PRESSURE. Blood PRESSURE is expected to decrease within 5 minutes after administration. Depending on the therapeutic effect, re-administration of the drug Ebrantil is possible .

2. IV drip or continuous infusion — using a perfusion pump. The maintenance dose is an average of 9 mg / h, i.e. 250 mg of Ebrantil (10 amp. 5 ml or 5 amp. 10 ml each) in 500 ml of infusion solution (1 mg = 44 drops = 2.2 ml).

The maximum allowable ratio is 4 mg of Ebrantil per 1 ml of infusion solution.

The recommended maximum initial speed is 2 mg / min.

The rate of drip administration depends on the patient's blood PRESSURE.

The solution for drip infusion, designed to maintain blood PRESSURE, is prepared as follows.

Usually 250 mg (10 amp. 5 ml or 5 amp. 10 ml) of the drug Ebrantil is added to 500 ml of a solution for infusions, such as saline, 5 or 10% dextrose (glucose) solution.

If a perfusion pump is used to administer the maintenance dose, then 100 mg (4 amp. 5 ml or 2 amp each. 10 ml) of the drug Ebrantil is injected into a syringe of a perfusion pump and diluted to 50 ml with saline, 5 or 10% dextrose (glucose) solution.

Controlled (controlled) decrease in blood pressure when IT increases during and / or after surgery

Continuous infusion using a perfusion pump or drip infusion is used to maintain blood PRESSURE at the level reached by intravenous injection.

The dosing scheme is shown in the figure.

Drawing. Dosing scheme of the drug Ebrantil .

Notes:

- if other antihypertensive agents were previously used, the drug Ebrantil can only be administered after a period of time sufficient for the previously administered drug(s) to work. The dose of Ebrantil should be adjusted accordingly.

- When using antihypertensive drugs in elderly patients, care should be taken. The initial dose should be reduced compared to the recommended dose, since the sensitivity of elderly patients to drugs of this type is often changed (V d is reduced, and T 1/2 is increased).

The drug can be administered once or multiple times. Injection of the drug can be combined with subsequent drip infusion. Parenteral therapy can be repeated with a new increase in blood PRESSURE.

Capsules of the prolonged action

Inside.

Ebrantil in the form of capsules is used for the treatment of severe hypertension ( as part of combination therapy).

Take in the morning and evening, at the same time with food, drinking a small amount of water.

The dose of the drug must be selected individually.

1 caps each. 30 mg of the drug Ebrantil 2 times a day. If necessary, the dose of the drug Ebrantil can be increased to 120 mg (2 caps. 30 mg or 1 caps. 60 mg 2 times a day).

The maximum daily dose is 180 mg divided into two doses.

Use in elderly patients, as well as patients with impaired liver function and / or severe to moderate renal failure

When using Ebrantil in this category of patients, it may be necessary to reduce the dose depending on blood PRESSURE and laboratory parameters of liver and/or kidney function.

Side effect

Solution for intravenous administration

Most of the following side effects are caused by a sharp drop in blood PRESSURE, but clinical experience shows that they disappear within a few minutes even after a drip infusion of the drug Ebrantil . Severe side effects may require discontinuation of treatment.

The frequency of side effects was determined in accordance with the who classification: very often (≥10%); often (≥1% and <10%); infrequently (≥0.1% and <1%); rarely (≥0.01% and <0.1%); very rare (<0.01%); frequency unknown (cannot be calculated based on available data).

From the side of the psyche: very rarely — an excited state (a sense of anxiety).

From the Central nervous system: often-dizziness, headache.

From the CCC: often — palpitations, tachycardia, bradycardia, feeling of compression or chest pain (anginal complaints nature), shortness of breath, heart palpitations, decrease in blood pressure when changing body position, for example when moving into an upright position from a lying position (orthostatic hypotension).

From the respiratory system, chest and mediastinal organs: rarely-nasal congestion.

From the digestive tract: often-nausea; infrequently-vomiting.

On the part of the skin and subcutaneous tissue: infrequently-increased sweating; rarely-allergic reactions, such as itching, redness of the skin, exanthema; unknown — angioedema, urticaria.

From the urinary system: often-proteinuria; rarely-nephropathy, nephrotic syndrome.

From the reproductive system and mammary glands: rarely-priapism.

Systemic disorders and disorders at the site of administration: infrequent-increased fatigue.

Deviations from the norm detected in laboratory and instrumental studies: very rarely — thrombocytopenia*; infrequently-cardiac arrhythmia.

* Very rarely, there was a decrease in the number of platelets during the use of urapidil. However, it was not possible to establish any causal relationship with ebrantil therapy, for example through immunohematological studies.

Capsules of the prolonged action

The frequency of adverse reactions was determined in accordance with the who classification: very often (≥1: 10); often (≥1: 100, <1: 10); infrequently (≥1: 1000, <1:100); rarely ≥1:10000, <1: 1000); very rare (<1:10000); frequency unknown (cannot be calculated based on available data).

CCC: infrequently-palpitations, tachycardia, bradycardia, feeling of compression or chest pain (symptoms typical of an attack of angina), orthostatic hypotension.

From the digestive tract: often-nausea; infrequently-vomiting, diarrhea, dryness of the oral mucosa.

Deviations from the norm detected in laboratory and instrumental studies: very rarely — a reversible increase in the activity of liver enzymes, thrombocytopenia * .

From the Central nervous system: often-dizziness, headache; infrequently-fatigue, sleep disorders; very rarely — dysphoria.

From the reproductive system and mammary glands: very rarely — priapism.

From the urinary system: very rarely — frequent urination and increased cases of urinary incontinence.

From the skin: infrequently-allergic reactions (skin itching, dry skin, exanthema, redness of the skin); the frequency is unknown-angioedema, urticaria.

From the respiratory system: infrequently-nasal congestion.

General disorders and disorders at the site of administration: infrequently-generalized convulsions.

 * In very rare cases, thrombocytopenia was observed during the use of the drug Ebrantil, although a causal relationship with the drug being treated by, for example, immunological tests has not been established.

If any of the side effects specified in the instructions are aggravated or any other side effects not specified in the instructions appear, you should inform your doctor about this.

Interaction

The antihypertensive effect of urapidil can be enhanced when used together with alpha-blockers, vasodilators or other hypotensive agents, as well as in conditions associated with a decrease in the volume of fluid in the body (diarrhea, vomiting) and when taking ethanol (alcohol).

With simultaneous administration of cimetidine C, the maximum urapidil in blood plasma can increase by 15%.

Use with ACE inhibitors is not recommended, since data on this combination is not yet sufficient.

Overdose

Solution for intravenous administration

Symptoms: dizziness, orthostatic collapse, fatigue, lethargy.

Treatment: with a sharp drop in blood PRESSURE, you need to lift the patient's legs and start infusion therapy to increase the BCC. If these measures are ineffective, you can start infusion of vasoconstrictors under AD control. In very rare cases, it is necessary to administer catecholamines (0.5–1 mg of epinephrine (epinephrine) diluted in 10 ml of saline).

Capsules of the prolonged action

Symptoms: a marked decrease in blood PRESSURE, dizziness, fatigue, lethargy, collapse.

Treatment: during the first 4 hours after an overdose, gastric lavage and the use of activated charcoal may occur. If there is a marked decrease in blood PRESSURE, the patient should be given a horizontal position, his legs should be raised, and measures should be taken to increase the BCC; symptomatic therapy.

Special instruction

Solution

Possible simultaneous use with other, used internally, hypotensive agents.

There is no clinical data on the use of the drug in children under 18 years of age.

If antihypertensive drugs were previously prescribed, the drug Ebrantil, a solution for intravenous administration, should not be used until enough time has passed for the development of the effect of taking the previous drug (s). The dosage of Ebrantil should be reduced accordingly.

An excessively rapid drop in blood PRESSURE can cause bradycardia or cardiac arrest.

In elderly patients, use with caution and initially administer in small doses, because the sensitivity of older patients is higher or changed to such drugs.

Patients who are on a diet with a controlled sodium content should take into account that the drug Ebrantil, a solution for intravenous administration, contains sodium in an amount not exceeding 1 mmol (23 mg) in 5 ml of the drug, and 2 mmol (46 mg) in 10 ml of the drug.

There may be cases of long-term erection and priapism on the background of alpha 1-blockers therapy. If you maintain an erection for more than 4 hours, you should immediately seek medical help. If priapism therapy was not carried out immediately, it can lead to damage to the tissues of the penis and irreversible loss of potency.

Influence on the ability to drive a car and other mechanisms. The drug may affect the ability to drive vehicles or work with various mechanisms. This is especially true at the beginning of treatment, when increasing the dose of the drug or replacing the drug, as well as drinking alcohol during treatment.

Capsules of the prolonged action

There may be cases of long-term erection and priapism on the background of alpha 1-blockers therapy. If you maintain an erection for more than 4 hours, you should immediately seek medical help. If priapism therapy was not carried out immediately, it can lead to damage to the tissues of the penis and irreversible loss of potency.

Influence on the ability to drive a car and other mechanisms. During therapy with Ebrantil, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions. This is especially true at the beginning of treatment, when increasing the dose of the drug or replacing the drug, as well as drinking alcohol during treatment.

Form release

Solution for I/V administration, 5 mg/ml: ampoules of neutral colourless glass (type I, European Pharmacopoeia) with the point of the fault and two marking strips, 5 ml; in vials of neutral colourless glass (type I, European Pharmacopoeia), with point break and one marker strip, 10 ml; in a contour plastic packaging 5 PCs.; in the paper cartons 1 package.

Long-acting capsules, 30 and 60 mg: in PE bottles, capped with screw-on PE lids with cavities containing silica gel, and rings that provide control of the first opening, 30, 50 or 100 PCs.; in a pack of cardboard 1 bottle.

Conditions of supply of pharmacies

By prescription.

Manufacturer

Takeda GmbH, Germany, BIC-Gulden Strasse 2, 78467, Constance, Germany.

Takeda GmbH, Germany, Byk-Gulden-Strasse 2, 78467 Konstanz, Germany.

Manufacturer and company that produces quality control (intravenous solution): Takeda GmbH, Germany, Robert-Bosch-Strasse 8, 78224, Singen, Germany.

Takeda GmbH, Germany, Robert-Bosch-Strasse 8, 78224 Singen, Germany.

Takeda Austria GmbH, Austria, St. Peter Strasse 25, 4020 Linz, Austria.

Takeda Austria GmbH, Austria, St.Peter-Strasse 25, 4020 Linz, Austria.

(long-acting capsules) Takeda GmbH, Germany, Lenitzstrasse, 70-98, 16515, Oranienburg, Germany.

Takeda GmbH, Germany, Lehnitzstrasse 70-98, 16515, Oranienburg, Germany.

Send consumer complaints to Takeda pharmaceuticals LLC: 119048, Moscow, Usacheva str., 2, p. 1.

Tel.: (495) 933-55-11; Fax: (495) 502-16-25.

www.takeda.com.ru; russia@takeda.com

The appearance of the product may differ from the photos on the site.

Information about prescription drugs is for professionals only. The information provided should not be used by patients to make an independent decision on the use of the presented drugs and cannot serve as a substitute for a full-time consultation with a doctor.

A description of the active substances of the drug is provided. The scientific information provided is generalized and cannot be used to decide on the possibility of using a specific drug.

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