Radachlorin® (Radahlorin®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbspconcentrate for solution for infusion
Composition:

Active substance: Radachlorin ® - 5,00 g (which corresponds to the sum of the sodium salts of chlorin e6, chlorine p6, purpurin 5 - 0.35 g).

Excipients: meglumine - 0.20 g, water for injection - up to 100 ml.

Description:

Transparent liquid of a dark green color, with a weak characteristic odor.

Pharmacotherapeutic group:photosensitizing agent
ATX: & nbsp
  • Drugs used in photodynamic and radiation therapy
    • Pharmacodynamics:

    Radachlorin® is a second generation photosensitizer intended for fluorescent diagnosis (FD) and photodynamic therapy (PDT) of malignant tumors.

    The PDT method is based on the ability of Radachlorin® to selectively accumulate in the skin tumor with its intravenous administration and generate a singlet oxygen, which has a toxic effect on tumor cells and a modifying effect on their plasma membranes when exposed to light with a wavelength corresponding to one of the absorption peaks of the preparation (402, 502, 532, 608 or 662 nm).

    In the development of the effect after PDT with the drug Radachlorin ®, there are 3 stages:

    - Stage 1 - a characteristic reaction to light exposure in PDT, manifested in the form of edema and hyperemia of the irradiation zone of different severity;

    - Stage 2 - necrosis of the tumor, which is formed 2-4 days after the PDT session;

    - Stage 3 - rejection of necrotic masses and epithelization of the wound defect in 2-8 weeks, depending on the size of the tumor.

    Radachlorin® in doses of 0.5-2.4 mg / kg with irradiation of the tumor with laser radiation 3 hours after the administration of the drug does not have a mutagenic effect and does not damage the DNA of normal cells.

    Pharmacokinetics:

    After a single intravenous administration of Radachlorin® in doses of 0.5-2.4 mg / kg, it is distributed between the blood and tissues for 0.5-5 hours. The concentration of Radachlorin in the blood serum reaches a maximum after 15-30 minutes and rapidly decreases, making after injection at a dose of 0.5 mg / kg after 1 hour - 10 μg / l, after 3 hours - 5 μg / l, after 24 hours - 1 μg / l.

    The concentration of Radachlorin® in the tumor reaches a maximum after 1 hour (10-20 μg / ml), but with a faster excretion of it from the healthy surrounding tissues, the maximum therapeutic index (contrast index) is observed 3 hours after the administration of the drug. The concentration of the drug in the tumor tissue is higher than in the surrounding healthy tissues, on average 3-6 times, depends on the morphological structure of the tumor, and is 2-10 μg / ml.

    Rapid excretion of Radachlorin® from blood, skin and mucous membranes and a high contrast index exclude damage to healthy organs and tissues and hypersensitivity of skin to daylight.

    The highest levels of Radachlorin® 3 hours after the administration are created in the liver, kidneys, tumor tissue.

    About 70-80% Radachlorin® is metabolized in the liver to biladienes (linear tetrapyrroles, which are also products of heme metabolism). The drug is excreted unchanged with faeces (15%) and urine (3%). The cumulative excretion of Radachlorin® with feces and urine in the first 12 hours averages 15-20% of the administered dose of the drug. The main part (98%) of Radachlorin® is excreted or metabolized in the first 48 hours. Trace amounts of the drug are determined in the skin up to 6 days.
    Indications:
    - Fluorescent diagnosis of skin cancer;
    - fotdynamic therapy of superficial skin tumors (excluding melanoma);
    - fotdynamic therapy precancerous (dysplasia I-III degree, erosion) and tumor (cancer in situ) pathology of the cervix.
    Contraindications:

    - Hypersensitivity to any of the components of the drug;

    - bVariability and lactation;

    - d(experience of medical use in children is absent).

    Carefully:People with hypertension, diabetes.
    Pregnancy and lactation:

    Contraindicated in pregnancy.

    For the duration of treatment, breastfeeding should be discontinued.

    Dosing and Administration:

    The drug is administered once as an intravenous drip infusion for 30 minutes.

    Light exposure to radiation with a wavelength of 662 ± 3 nm begins 3 hours after the end of the infusion. The optimal mode of exposure is the administration of the drug at a dose of 1.0-1.2 mg / kg and light exposure to radiation with a wavelength of 662 ± 3 mm at a dose of 300 J / cm2.

    Subject to the possibility of re-treatment of patients with partial effect or stabilization, it is possible to use regimens of 0.5-0.6 mg / kg - 300 J / cm2 and 1.0-1.2 mg / kg - 200 J / cm2. In this case, the choice of treatment should be carried out individually, taking into account the form and prevalence of the tumor process.

    When exposed to the laser, remote surface irradiation through a quartz light guide is used with or without microlenses in photodynamic therapy of superficial skin tumors, or with the use of a macro lens with a light a spot 2.5 to 3.0 cm in diameter with photodynamic therapy pre-tumoral and tumor pathology of the cervix. As a source of laser radiation, a diode laser with a wavelength of 662 ± 3 Mr.m.

    To identify additional foci and clarify the boundaries of the tumor, it is recommended to combine the administration of Radachlorin® with fluorescent diagnostics, for example, using spectrofluorimeters. The intensity of fluorescence reaches a maximum 3 hours after the administration of the drug and is substantially higher for a dose of 1.2 mg / kg. The fluorescent contrast at the "tumor / norm" border varies within the limits of (2 ÷ 4) / 1 (for a dose of 0.6 mg / kg) and (4 ÷ 6) / 1 (for a dose of 1.2 mg / kg).

    Preparation of a solution for intravenous infusion

    The contents of one or more vials are diluted in 200 ml of one of the infusion solutions listed below:

    - 0.9% solution of sodium chloride;

    - 5% or 10% dextrose solution;

    - 10% mannitol solution;

    - Ringer's solution;

    - 4% or 8% potassium chloride solution.

    To prepare the solution, do not use infusion solutions with an acidic pH.

    Side effects:

    When photodynamic therapy (PDT) with Radachlorin ® is possible:

    Local Reactions

    Often:

    - pain in the place of the irradiated focus during the entire procedure of PDT and up to 1 hour after PDT. The severity of the pain syndrome varies depending on the prevalence of the pathological process and the individual sensitivity of the patients;

    - edema of surrounding tissues and soft tissues of the head, lasting 2-7 days.

    For the relief of painful reactions, the use of analgesics is recommended.

    From the skin

    Rarely: itchy skin.

    On the part of the organs of hematopoiesis

    Often an increase in the absolute number of leukocytes in peripheral blood can be observed with an increase in the number of granulocytes.

    Overdose:

    Symptoms of overdose are similar to adverse side effects.

    Symptomatic and disintoxication therapy is shown (infusion therapy according to indications, taking analgesics, antihistamines, antioxidants).

    Interaction:

    The incompatibility of Radachlorin® with drugs having an acid pH of the medium, for example, with ascorbic acid, has been revealed.

    Special instructions:

    Necrosis in the treatment zone usually begins to form in 2-4 days, and the rejection of the scab occurs in 2-8 weeks after exposure to the laser.

    Precautions for use
    - During laser exposure, the doctor and patient should use protective glasses with a light filter that absorbs radiation at 662 ± 3 nm.
    - The patient, after the administration of Radachlorin®, must observe a limited light regime (avoid bright light) during the week.
    - Radachlorin® should not be administered with the same syringe or through the same system for intravenous administrations, through which other medications were administered.

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

    Direct contraindications to driving after the PDT session Radachlorin® are not currently detected. In case of any side effects, the issue of driving and working with other mechanisms requires individual consideration.

    Form release / dosage:Concentrate for solution for infusion, 0.35%.
    Packaging:
    • vials (1) - packs cardboard
    • vials (10) - packaging
    Storage conditions:
    At temperatures from 0 to 8 ° C, protected from light.
    The drug can be stored diluted at a temperature of 2 to 8 ° C not more than 24 hours before the introduction. The prepared solution is stable under room light or in daylight, however direct light exposure should be avoided.
    Keep out of the reach of children.
    Shelf life:

    2.5 years.

    Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-001868
    Date of registration:16.12.2011 / 28.07.2015
    The owner of the registration certificate:RADA-PHARMA, LLC RADA-PHARMA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp03.03.2016
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