Aminolevulinic acid (Acidum aminolevulinicum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Diagnostic tools

Antineoplastic agents

Included in the formulation
  • Alasens®
    powder inwards 
    NIOPIK SRC, FSUE     Russia
    • АТХ:

    V.04   Diagnostic drugs

    L.01   Antineoplastic agents

    Pharmacodynamics:

    A prodrug that is in situ converted to protoporphyrin IX, accumulating intracellularly in the skin. The cytotoxic effect upon irradiation with light of a certain wavelength in the presence of oxygen is due to the excitation of protopophyrin molecules, the formation of active oxygen radicals from oxygen molecules with the further formation of superoxide and hydroxyl radicals

    Pharmacological effects

    Photosensitizing. The effect occurs 6 hours after ingestion2, as much as possible after 11 hours.

    Pharmacokinetics:

    The prodrug is in situ converted to protoporphyrin, then to heme. T1 / 2 - 0.7-0.83 h (aminolevulinic acid when ingested or parenterally administered), 30 h (protoporphyrin IX when applied to the damaged skin), 8 h (protoporphyrin IX, ingestion).

    Indications:

    Fluorescent diagnosis of superficial tumors of the bladder.

    Fluorescence diagnosis of Ta / T1 of transitional cell bladder cancer with subsequent resection of the bladder: the use of aminolevulinic acid "in comparison with conventional cystoscopy causes prolongation of the median duration of the disease-free period in the case of multiple or recurrent carcinomas.In primary and single carcinomas, the extension of the disease-free period is statistically insignificant. B4.


    ICD-10

    XXI.Z00-Z13.Z03   Medical surveillance and evaluation in case of suspected disease or pathological condition

    Contraindications:

    Hypersensitivity, porphyria. With caution - Violations of blood clotting.

    Carefully:

    Violations of blood clotting.

    Pregnancy and lactation:

    Pregnancy

    Recommendations FDA category C. Qualitative studies in animals and in humans are not conducted.

    Lactation

    There is no information on the penetration into breast milk, complications in humans are not documented.

    Dosing and Administration:

    Intravesically injected at a dose of 1.5 g as a 3% solution. 50 ml of the solution is injected through the catheter into the bladder for 1.5-2 hours before the fluorescent diagnostic session and subsequent treatment (electrosection, etc.). To prepare the solution: 1.5 g of the drug is dissolved in 50 ml of sterile 5% sodium hydrogen carbonate solution immediately before use. Diagnosis is carried out 1.5-2 hours after instillation of the solution into the bladder. As a radiation source that stimulates the fluorescence of protoporphyrin IX in tissues, optical radiation with a wavelength in the range of 385-440 nm is used.

    Use in children

    Efficiency and safety have not been studied.

    Side effects:

    Bleeding (2-4%).

    Overdose:

    When administered orally, a transient increase in hepatic transaminase activity occurs. The effects of overdose on topical application are not established. Treatment is symptomatic. Avoid exposure to sunlight for 40 hours.

    Interaction:

    Other photosensitizing drugs (thiazide diuretics, griseofulvin, phenothiazines, sulfonamides, sulfonylureas, tetracyclines, as well as preparations of St. John's Wort) - increased photosensitivity.

    Special instructions:

    The effectiveness of the photodynamic damage of the sensitized cell is determined by the intracellular concentration (level of accumulation) of the sensitizer, its localization in the cell, and photochemical activity (the quantum yield of generation of singlet oxygen or free radicals) supplied by the light dose of laser irradiation and the method of its application. In addition to direct cytotoxic effects on tumor cells in PDT, an important role in the destruction of abnormal cells is played by the violation of blood supply due to damage to the endothelium of the blood vessels of tumor tissue andcytokine reactions due to stimulation of TNF-α production, activation of macrophages, leukocytes and lymphocytes.

    PDT, in addition to bleeding, can be accompanied by dysesthesia (at the place of application): redness, itching, tingling sensation, numbness, tingling. Dysaesthesia is severe in 50% of patients. In the course of PDT, the maximal intensity of dysesthesias occurs at the 6th minute of irradiation (manifestations subside at different time intervals - depending on the individual characteristics after 1 min-24 h - after the irradiation has ceased). In addition, puffiness, erosion, hypo- and hyperpigmentation of the skin, blisters, and crusts in the application area are possible. After PDT, redness, swelling and lamellar peeling of surrounding tissues can develop. However, these lesions are temporary and completely resolved after 4 weeks after treatment.

    In the USA and Great Britain they are used for the treatment of senile keratoses (non-hyperkeratotic) by the method of PDT.

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