Urapidil Carino (Urapidil Carino)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceUrapidilUrapidil
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  • Urapidil Carino
    solution in / in 
    Karinofarm GmbH     Germany
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    • Dosage form: & nbspsolution for intravenous administration
    Composition:

    1 ml of the preparation contains:
    active substance: urapidil 5 mg;
    auxiliary substances: acid hlhydrohistoric concentrated 1,350 mg, sodium dihydrogen phosphate dihydrate 0.530 mg, sodium hydrogen phosphate 0.158 mg, propylene glycol 100,000 mg, sodium hydroxide q.s., water for injection up to 1 ml


    Description:A clear, colorless solution.
    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. It blocks postsynaptic alpha 1-adrenergic receptors, thereby reducing the overall peripheral vascular resistance (OPSS). Regulates the central mechanism of maintaining vascular tone by stimulating the serotonin 5-HT1A receptors of the vasomotor center (prevents reflex increase in the tone of the sympathetic nervous system).
    Heart rate (heart rate) and cardiac output after administration of the drug do not change. Stimulates presynaptic alpha2-adrenergic receptors.
    Reduces systolic and diastolic blood pressure, reducing OPSS, does not cause reflex tachycardia. Reduces pre- and afterload on the heart, increases the efficiency of cardiac contraction, thus (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 intravenous administration (in / in) 25 mg urapidil observed biphasic decrease in the concentration urapidil (first - rapid (alpha-phase), and then - the slow (beta-phase) reduction). The distribution period is 35 minutes; volume of distribution - 0.8 l / kg (0.6-1.2 l / kg). Connection with blood plasma proteins - 80%. Urapidil mainly metabolized in the liver. Its main metabolite is the hydroxylated derivative (in the 4-position of the benzene ring), which does not possess hypotensive activity. O-demethylated metabolite is formed in very small amounts and is as active as urapidil. The half-life period (T1 / 2) after IV bolus is 2.7 h (1.8-3.9 h). 50-70% of urapidil and its metabolites (15% in the form of an active substance) are excreted by the kidneys; The rest is through the intestines in the form of metabolites (mainly in the form of inactive p-hydroxylated urapidil).In elderly patients and in patients with severe hepatic and / or renal insufficiency, the volume of distribution and clearance is decreased, and T1 / 2 is increased. Urapidil penetrates through the blood-brain and placental barrier.
    Indications:

    Hypertensive crisis, refractory and severe degree of arterial hypertension.
    Controlled arterial hypotension during and / or after surgery

    Contraindications:

    - hypersensitivity to urapidil or any of the components of the drug;
    - violation of the vascular connection between arteries and veins (arteriovenous anastomosis) with the exception of hemodynamically ineffective dialysis anastomosis;
    - open Botallov duct;
    - age to 18 years;
    - pregnancy and lactation (efficacy and safety not established).
    - aortic stenosis.

    Carefully:

    The drug is used with caution under the following conditions:
    - abnormal liver function;
    - renal failure of moderate severity and severe;
    - chronic heart failure;
    - aortic and mitral stenosis;
    - pulmonary embolism;
    - violation of contractility of the myocardium due to diseases of the heart bag (for example, cardiac tamponade, pericarditis);
    - hypovolemia;
    - simultaneous application of cimetidine;
    - elderly age.

    Pregnancy and lactation:The drug is contraindicated in pregnancy and during breastfeeding
    Dosing and Administration:
    Urupidil Carino is administered intravenously slowly or infusional to the patient, who should be in the "lying" position.
    Apply immediately after opening the ampoule.
    The opened ampoule is not subject to storage.
    Intravenous injections of the drug can be combined with subsequent continuous infusion.
    Urupidil Carino should not be mixed with alkaline solutions for injection.
    The administration of the drug can be single or multiple.
    Therapy can be repeated with a new increase in blood pressure.

    Hypertensive crisis, refractory and severe degree of arterial hypertension.
    - intravenously slowly 10-50 mg of the drug Urapidil Karino (under the control of blood pressure (BP), the expected reduction in blood pressure observed after 5 minutes), it is possible to re-administer the drug (25 mg of the drug).
    - intravenously by infusion (by drip or continuously using a perfusion pump).
    The maintenance dose (on average) is 9 mg / h, i.e.250 mg of Urapidilo Carino (10 ampoules of 5 ml or 5 ampoules of 10 ml) are dissolved in 500 ml of the solution for infusion (0.9% solution of sodium chloride, 5% and 10% solution of dextrose (glucose) is possible). The maximum allowable ratio is 4 mg of the drug Urapidil Carino for 1 ml of the solution for infusions. The maximum initial rate of administration is 2 mg / min (depending on blood pressure).

    If a perfusion pump is used to administer a maintenance dose, then 100 mg of the preparation (4 ampoules of 5 ml or 2 10 ml ampoules) are introduced into the syringe of the perfusion pump and diluted to 50 ml with 0.9% sodium chloride solution, 5 or 10% dextrose solution (glucose).

    Controlled arterial hypotension during and / or after surgery.
    Continuous infusion (using a perfusion pump) or drip infusion is used to maintain blood pressure at the level achieved by intravenous administration.

    In elderly patients and patients with impaired liver and kidney function, the initial dose of the drug Urapidil Carino should be reduced compared to the recommended one.
    If previously used other antihypertensives, then Urupidil Carino can be administered only after a period of time, sufficient,(s) previously administered (s). The dose of the drug Urapidil Carino should be adjusted accordingly.

    Side effects:
    The frequency of adverse reactions was determined in accordance with the recommendations 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), including individual messages.

    Frequency


    System
    bodies

    Often

    Infrequently

    Rarely

    Rarely

    from the side of cardio-
    cardiovascular system

    sensation
    palpitation,
    tachycardia,
    bradycardia,
    feeling
    compression in
    breast,
    dyspnea,
    arrhythmias

    gastrointestinal tract

    nausea

    vomiting

    from

    systems

    hematopoiesis

    thrombocyte-
    singing

    from the central nervous system

    dizziness-
    tion,
    head
    pain,
    increased
    fatigue

    feeling
    anxiety

    from the reproductive system and mammary glands

    priapism

    from the urinary system

    proteinuria

    nephropathy,
    nefroti-
    physical
    syndrome

    from
    dermal
    integument

    increased
    perspiration
    the

    allergies and
    reactions (cutaneous
    itching, redness of the skin, exanthema)

    Overdose:

    Symptoms:
    dizziness, ringing in the ears, orthostatic hypotension, increased fatigue and retardation (see also the "Side effect" section).
    Treatment:
    With valuesReduced blood pressure should be given to the patient with a horizontal position with raised legs and infusion solutions to replenish the volume of circulating blood (BCC). If these measures are ineffective, intravenous administration of vasoconstrictive drugs is required, with simultaneous monitoring of blood pressure. The use of catecholamines is required only in rare cases (for example, epinephrine (epinephrine) in a dose of 0.5-1.0 mg, diluted in 10 ml of 0.9% sodium chloride solution).

    Interaction:

    The simultaneous use of urapidil and preparations of different pharmacological groups used to lower blood pressure leads to an increase in the antihypertensive effect of urapidil. The hypotensive effect of urapidil is enhanced against hypovolemia and ethanol intake.
    With the simultaneous use of cimetidine and urapidil, the concentration of the latter in blood plasma increases by 15%.
    It is not recommended to combine urapidil with inhibitors of angiotensin-converting enzyme because of the lack of clinical data on joint use.

    Special instructions:Dehydration of the body, which can be caused by excessive vomiting or diarrhea, also leads to an increase in the hypotensive effect of the drug.
    Effect on the ability to drive transp. cf. and fur:Data on the impact on the ability to drive vehicles and work with complex mechanisms are absent.
    Form release / dosage:Solution for intravenous administration 5 mg / ml.
    Packaging:

    For 5, 10 or 20 ml of the drug in a vial of colorless neutral glass, hydrolytic type I, with a blue break point and green (for ampoules, 5 ml) or yellow (for ampoules, volume 10 and 20 ml) ring.
    5 ampoules with instructions for use in cardboard packs with cardboard separators.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.
    Keep out of the reach of children.
    Apply immediately after opening the ampoule.

    Shelf life:

    4 years.
    The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002382
    Date of registration:26.02.2014
    The owner of the registration certificate:Karinofarm GmbHKarinofarm GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspSVYCH LLC SVYCH LLC Russia
    Information update date: & nbsp26.11.2015
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