Active substanceTerlipressinTerlipressin
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  • Remestip®
    solution in / in 
    Ferring-Lechiva as     Czech Republic
  • Dosage form: & nbspsolution for intravenous administration
    Composition:

    The composition of the drug - active substance - terlipressin (LLP μg / ml), as well as auxiliary substances: sodium chloride, acetic acid, sodium acetate trihydrate, water for injection.

    Description:Colorless transparent solution.
    Pharmacotherapeutic group:antihemorrhagic remedy
    ATX: & nbsp

    H.01.B.A   Vasopressin and its analogues

    H.01.B.A.04   Terlipressin

    Pharmacodynamics:

    The active substance of the drug Remestip - terlipressin - a synthetic polypeptide analogue of the hormone of the posterior lobe of the pituitary - vasopressin.

    In the molecule of natural vasopressin, 2 changes were introduced: arginine in the 8 position is replaced by lysine, and 3 glycine residues are attached to the amino group of the final cysteine. The structural features of the terlipressin molecule are more pronounced than the vasopressin vasoconstrictive action with reduced antidiuretic activity. The most pronounced vasoconstrictive effect of terlipressin on arterioles, venules, veins and smooth muscles of visceral organs, which leads to a decrease in blood flow through the liver and a decrease in portal pressure.

    Terlipressin. stimulating contractions of smooth muscles of the intestine,causes an increase in his tone and increased peristalsis.

    Terlipressin stimulates contraction of the myometrium.

    Pharmacokinetics:

    After iv introduction pharmacokinetics is described by means of a two-chamber model. Terlipressin metabolized in the liver, kidneys and other tissues with the formation of active metabolites The action of terlipressin develops more slowly, but more prolonged than the action of lysine-vasopressin. The therapeutic concentration of active metabolites begins to be determined in the blood 30 minutes after the administration of terlipresin and reaches a maximum after 60-120 minutes. Half-life is about 40 minutes, clearance Oml / kg per minute. and the volume of distribution is about 0.5 l / kg.

    Indications:
    - Bleeding from the gastrointestinal tract (varicose veins of the esophagus, stomach and duodenal ulcers)

    - Uterine bleeding (dysfunctional, with childbirth and abortion)

    - Bleeding during surgery on the pelvic organs

    - Hepatorenal syndrome type 1
    Contraindications:

    - Hypersensitivity to the drug

    - First trimester of pregnancy

    - Toxicosis of pregnancy

    - Epilepsy

    Carefully:

    With extreme caution, prescribe Remestip® to elderly patients, with ischemic heart disease, with unstable angina and recent acute myocardial infarction, pronounced arterial hypertension, with septic shock with low cardiac output, with heart rhythm disorders, bronchial asthma, in pregnancy more than 12 weeks.

    Pregnancy and lactation:

    Terlipressin causes an increase in the contractile activity of the myometrium and a decrease in blood flow in the uterus. At the gestational age of more than 12 weeks should be in each case to evaluate the appropriateness of the drug.

    There is no information on the allocation of terligalsate from breast milk, so breastfeeding during the drug should be discontinued.

    Dosing and Administration:

    Remestip® is intended for intravenous administration in the form of bolus injections or short-term infusion.

    Bleeding from the gastrointestinal tract (gastric and duodenal ulcers, varicose veins of the esophagus): 10 ml (1.0 mg) with an interval of 4-6 hours before the bleeding stops and the next 3-5 days.To prevent repeated bleeding, the drug is canceled only after a complete absence of bleeding within 24 - 48 hours.

    The drug can be used in the provision of first aid for suspected bleeding from the gastrointestinal tract.

    Bleeding during surgery on the abdominal and pelvic organs: intravenously drip from 2 ml (0.2 mg) to 10 ml (1.0 mg) every 4 to 6 hours, depending on the activity of tissue endopeptidases.

    Uterine bleeding (dysfunctional, with childbirth and abortion): 4 ml (0.4 mg) is added to 6 ml of 0.9% sodium chloride solution and injected para- and / or intracervical in 5-10 minutes before surgery. If necessary, the dose may be increased or decreased.

    In juvenile uterine bleeding, the recommended dose is 5-20 μg / kg of the body weight of the patient.

    Hepatorenal syndrome type 1: 10 ml (1 mg) 3-4 times a day. Treatment should continue until normal plasma creatinine levels (less than 130 μmol / L), on average, 10 days. If the creatinine level does not decrease by more than 30% within 3 days, further administration of the drug is impractical.

    Side effects:

    The most common are pallor of the skin, increased arterial pressure in abdominal pain, increased intestinal peristalsis up to abdominal colic, nausea, diarrhea, headache, bradycardia.

    Rarely: myocardial infarction, heart failure, dyspnea, local necrosis at the injection site.
    Overdose:

    A dose of more than 2 mg (2000 μg) administered for 4 hours increases the risk of developing severe hemodynamic disorders. Do not exceed the recommended dose. For relief of hypertension should be used clonidine (clonidine). In the case of bradycardia, atropine.

    Interaction:

    The administration of Remestip® together with oxytocin or methylergometrin enhances vasoconstrictor and uterotonic action.

    Remestip® enhances the antihypertensive effect of nonselective p-adrenergic blockers. The simultaneous use of Remestip® with medications that slow heart rate (heart rate) can cause a pronounced bradycardia.

    Special instructions:

    Using Remestip, especially at an elevated dose of 0.8 mg (800 μg) or higher, you should monitor blood pressure,heart rate reduction by urination. This is especially important in the treatment of patients with hypertension, heart disease and elderly patients. With special care should appoint Remestip elderly patients, patients with coronary heart disease, with severe arterial hypertension, heart rhythm disturbances and bronchial asthma.

    Remestip does not replace the recovery of BCC in patients with bleeding. Avoid intramuscular injection to prevent the occurrence of local necrosis.

    The dose of 0.5 mg or more should be administered strictly intravenously!

    Effect on the ability to drive transp. cf. and fur:
    Form release / dosage:

    Solution for intravenous administration 0.1 mg / ml. 2 ml or 10 ml in an ampoule of colorless glass type I with possible color coding as a color point and / or one or more rings.

    For 5 ampoules in a cell box in a cardboard box with instructions for use.

    Packaging:(10) - ampoule (5) / 5 ampoules in a plastic box with instructions for use / - cardboard pack
    (2) - ampoule (5) / 5 ampoules in plastic cell pack with instructions for use / - cardboard package
    Storage conditions:

    Remestip should be stored in a dark place at a temperature of 2-8 ° C. Within 1 month the preparation can be stored at a temperature of no higher than 25 ° С (for example, in an ambulance).

    Keep out of the reach of children!

    Shelf life:2 years.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013886 / 01-2002
    Date of registration:11.08.2011
    The owner of the registration certificate: Ferring-Lechiva as Ferring-Lechiva as Czech Republic
    Manufacturer: & nbsp
    FERRING-LECIVA, a.s. Czech Republic
    Information update date: & nbsp25.09.2015
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