Ebrantil - instructions for use, dose, side effects, contraindications

Active substanceUrapidilUrapidil

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Urapidil Carino

solution in / in

Karinofarm GmbH Germany

Ebrantil®

capsules inwards

Takeda GmbH Germany

Ebrantil®

solution in / in

Takeda GmbH Germany

Dosage form: & nbspsustained-release capsules

Composition:

1 capsule prolonged action of 30 mg contains:

Active substance: urapidil 30 mg;

Excipients: sugar grits [sucrose, molasses starch] 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; ethyl cellulose 1.75 mg; stearic acid 0.47 mg; hypromellose phthalate 0.72 mg.

Capsule shell: gelatin 32.707 mg; titanium dioxide 1.2 mg; ferric iron oxide yellow 0.293 mg, water 5.8 mg.

Inks black (shellac, iron oxide, black oxide, propylene glycol, ammonia water), not more than 0.190 mg.

Ingredients of sugar [sucrose, starch treacle]: sucrose 80.0 - 91.5%, corn starch 8.5-20%, water max. 1.5%.

1 capsule prolonged action 60 mg contains:

Active substance: urapidil 60 mg;

Excipients: sugar grits [sucrose, molasses starch] 124.86 mg; methacrylic acid and methyl methacrylate copolymer [1: 2] 1.24 mg; talc 2.35 mg; diethyl phthalate 0.12 mg; fumaric acid 17.77 mg; hypromellose 22.55 mg; ethyl cellulose 3.51 mg; stearic acid 0.95 mg; hypromellose phthalate 1.43 mg.

Capsule shell: gelatin 53.33 mg; titanium dioxide 0.504 mg; indigocarmine 0.031 mg; water 9.135 mg.

Ingredients of sugar [sucrose, starch treacle]: sucrose 80.0 - 91.5%, corn starch 8.5-20%, water max. 1.5%.

Description:

Capsules of prolonged action 30 mg:

Hard gelatin capsules (№4) with an opaque case and a lid of yellow color with an inscription of black color "E" on the bodybr 30 ".The contents of the capsules are yellow granules.

Capsules of prolonged action 60 mg:

Hard gelatin capsules (№2) with a transparent casing of light-blue color and opaque lid of white color.

The contents of the capsules are yellow granules.

Pharmacotherapeutic group:Alpha-blocker

ATX: & nbsp

C.02.C.A.06 Urapidil

C.02.C.A Alpha-blockers

Pharmacodynamics:

Urapidil has a central and peripheral mechanism of action. Blocks postsynaptic alpha₁-adrenoceptors, thereby reducing the overall peripheral vascular resistance (OPSS).

Regulates the central mechanism of maintaining vascular tone by stimulating serotonin 5-HT_1Areceptors of the vasomotor center (prevents reflex increase in the tone of the sympathetic nervous system).Heart rate (heart rate), cardiac output does not change. Low cardiac output may be increased by lowering the OPSS.

Stimulates presynaptic alpha₂-adrenoceptors.

Reduces systolic and diastolic blood pressure (BP), does not cause reflex tachycardia.

Reduces pre- and postnagruzku on the heart, increases the efficiency of cardiac contraction, so. (in the absence of arrhythmia) increases the reduced minute volume of the heart.

Does not affect the parameters of carbohydrate metabolism, the exchange of uric acid and does not cause fluid retention in the body.

Pharmacokinetics:

After ingestion of 80-90% of urapidil absorbed in the gastrointestinal tract. The connection with plasma proteins is approximately 80%, and the volume of distribution is 0.77 l / kg body weight.

The maximum concentration in the blood plasma is reached 4-6 hours after taking the drug inside; half-life (T_1/2) is about 4.7 hours (3.3-7.6 hours).

Metabolized mainly in the liver. The main metabolite is the hydroxylated derivative (in the 4-position of the benzene ring), which practically does not possess antihypertensive activity.O-demethylated metabolite is formed in very small amounts and is almost as active as urapidil.

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

In the elderly and in patients with severe hepatic and / or renal failure, the volume of distribution and clearance is reduced, and T_1/2increased.

Penetrates through the blood-brain and placental barrier.

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

Indications:

Arterial hypertension of severe degree (as part of combination therapy).

Contraindications:

Hypersensitivity to the active substance and other components of the drug; age under 18 years (efficacy and safety not established), pregnancy, lactation.

Fructose intolerance and glucose / galactose absorption disorder or sugar / isomaltase deficiency.

Carefully:

Dysfunction of the liver, patients with severe and moderate severity of kidney failure; chronic heart failure,stenosis of the aortic and mitral valve; pulmonary embolism; violation of myocardial contractility due to cardiac disease (for example, tamponade, chronic pericarditis), with simultaneous use with cimetidine, the elderly.

Pregnancy and lactation:

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

Dosing and Administration:

Inside, morning and evening, while eating, squeezed a little water.

The dose of the drug must be selected individually.

1 capsule 30 mg of Ehrrantil® 2 times a day. If necessary, the dose of Egrantil® can be increased to 120 mg (2 capsules 30 mg or 1 capsule 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 and moderate severity of renal insufficiency

When using Egrantil® in this category of patients, a dose reduction may be required depending on blood pressure and laboratory parameters of liver and / or kidney function.

Side effects:

The frequency of adverse reactions was determined according to the classification of the World Health Organization: very often (> 1:10), often (> 1: 100, <1:10), infrequently (> 1: 1000, <1: 100), rarely (> 1: 10000, <1: 1000), very rarely (<1: 10000), the frequency is unknown (can not be calculated based on available data).

Frequency / System of organs	Often	Infrequently	Rarely	Frequency unknown
From the side of the cardiovascular system		Heart palpitations; tachycardia; bradycardia; a feeling of constriction or chest pain (symptoms typical of an attack of angina pectoris); orthostatic hypotension
From the gastrointestinal tract	Nausea	Vomiting, diarrhea, dryness mucous shells oral cavity
Deviations from the norm, revealed in laboratory and instrumental studies			Reversible increase in activity of "liver" enzymes, thrombocytopenia
From the central nervous system	Dizziness; head pain	Increased fatigue, sleep disorders	Dysphoria
From the side of the reproductive system and mammary glands			Priapism
From the urinary system			Increased urination and increased incontinence
From the side dermal integument		Allergic reactions (skin itching, dry skin, exanthema, redness of the skin)		Angioneurotic edema, urticaria
From the respiratory system		Nasal congestion
General disorders and disorders at the site of administration		Generalized edema

* In very rare cases thrombocytopenia was observed during the use of the drug Ebrantil®, although a causal relationship with the treatment administered by the preparation through, for example, immunological tests is not established.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: marked decrease in blood pressure, dizziness, increased fatigue, retardation, collapse.

Treatment: During the first 4 hours after an overdose, it is possible to rinse the stomach and use activated charcoal.

If there is a pronounced decrease in blood pressure, the patient should be given a horizontal position, raise the legs, carry out measures to increase the volume of circulating blood (BCC); symptomatic therapy.

Interaction:

The antihypertensive effect of urapidil can be enhanced by co-administration withalpha-adrenoblockers, vasodilators or other antihypertensive agents, as well as in conditions associated with a decrease in the volume of fluid in the body (eg, diarrhea, vomiting) and with the intake of ethanol (alcohol).

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

It is not recommended to use with angiotensin converting enzyme inhibitors, since data on such a combination is not enough.

Special instructions:

There are cases of development of prolonged erection and priapism against the background of therapy with alphaa₁adrenoblockers. If the erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy has not been carried out immediately, it can lead to damage to the tissues of the penis and an irreversible loss of potency.

Effect on the ability to drive transp. cf. and fur:

During the period of therapy with the drug Egrantil®, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

This is especially true at the beginning of treatment, with an increase in the dose of the drug or the replacement of the drug, as well as the use of alcohol during the treatment period.

Form release / dosage:

Capsules of prolonged action, 30 mg and 60 mg.

Packaging:

30, 50 or 100 capsules of prolonged action in a polyethylene bottle capped with a screwed polyethylene cover with a cavity containing silica gel and with a ring that provides "first opening" control.

The bottle together with the instruction for use is placed in a cardboard pack.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000466

Date of registration:01.03.2011 / 02.03.2016

Expiration Date:Unlimited

The owner of the registration certificate:Takeda GmbHTakeda GmbH Germany

Manufacturer: & nbsp

TAKEDA, GmbH Germany

Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.

Information update date: & nbsp11.01.2017

Illustrated instructions

Instructions

Ebrantil® (Ebrantil®)