pharmachologic effect
The drug is highly active and is a macromolecular complex of the proteolytic enzyme hyaluronidase. When taken, it has the following effects:
- relieves inflammation;
- eliminates swelling;
- promotes activation of humoral immunity;
- antifibrotic.
Longidaza improves tissue nutrition, eliminates adhesions, contractures, accelerates the resorption of bruises and hematomas, and also increases joint mobility.
The drug works best in the initial stages of the disease, preventing its progression and the development of complications.
Longidaza also enhances the effect of local anesthetics, increasing their bioavailability.
The medication is characterized by incredibly low toxicity and the absence of negative effects on the body.
Longidaza, 20 pcs., 3000 IU, vaginal and rectal suppositories
Longidase® has hyaluronidase (enzymatic proteolytic) activity of prolonged action, chelating, antioxidant, immunomodulatory and moderate anti-inflammatory properties.
Prolongation of the action of the enzyme is achieved by covalent binding of it to a physiologically active high-molecular carrier (activated derivative of poly-1,4-ethylenepiperazine N-oxide, an analogue of the drug Polyoxidonium®), which has its own pharmacological activity. Longidase® exhibits antifibrotic properties, weakens the course of the acute phase of inflammation, regulates (increases or decreases depending on the initial level) the synthesis of inflammatory mediators (IL-1 and tumor necrosis factor-alpha), increases the humoral immune response and the body's resistance to infection.
The pronounced antifibrotic properties of Longidase® are ensured by the conjugation of hyaluronidase with a carrier, which significantly increases the resistance of the enzyme to denaturing influences and the action of inhibitors: the enzymatic activity of Longidase® is maintained when heated to 37 °C for 20 days, while native hyaluronidase loses under the same conditions your activity during the day. The Longidaza® preparation ensures the simultaneous local presence of the proteolytic enzyme hyaluronidase and a carrier capable of binding matrix components released during hydrolysis, enzyme inhibitors and stimulators of collagen synthesis (including iron, copper ions, heparin). Thanks to these properties, Longidaza® has not only the ability to depolymerize the connective tissue matrix in fibrogranulomatous formations, but also suppress the reverse regulatory reaction aimed at the synthesis of connective tissue components.
The specific substrate of testicular hyaluronidase is glycosaminoglycans (hyaluronic acid, chondroitin, chondroitin-4-sulfate, chondroitin-6-sulfate), which form the basis of the connective tissue matrix. As a result of depolymerization (breaking the bond between C1 acetylglucosamine and C4 glucuronic or induronic acids), glycosaminoglycans change their basic properties: viscosity decreases, the ability to bind water and metal ions decreases, the permeability of tissue barriers temporarily increases, fluid movement in the intercellular space is facilitated, and the elasticity of connective tissue increases. , which manifests itself in a decrease in tissue swelling, flattening of scars, an increase in the range of motion of joints, a decrease in contractures and prevention of their formation, and a decrease in adhesions.
Biochemical, immunological, histological and electron microscopic studies have proven that Longidaza® does not damage normal connective tissue, but causes destruction of connective tissue altered in composition and structure in the area of fibrosis.
Longidaza® does not have mutagenic, embryotoxic, teratogenic or carcinogenic effects.
The drug was well tolerated by patients; no local or general allergic reactions were noted.
The use of Longidase® in therapeutic doses during or after surgical treatment does not cause worsening of the postoperative period or progression of the infectious process; does not slow down bone tissue recovery.
Pharmacodynamics and pharmacokinetics
When the drug is administered by injection, it immediately enters the bloodstream, due to which the maximum concentration of the active substance is achieved in less than half an hour. The bioavailability of Longidase is about 90 percent, and it penetrates into any tissue of the human body. The half-life in this case is one day, and the drug is completely eliminated only after 5 days. It is excreted mainly by the kidneys, partly by the intestines.
When using suppositories, the maximum concentration is achieved only after 60 minutes. This dosage form has 70% bioavailability, and its half-life is extended to 2-3 days.
Longidaza por d/in 3000IU N5 (Petrovax)
A drug with proteolytic activity. It has enzymatic proteolytic (hyaluronidase) activity of prolonged action, immunomodulatory, chelating, antioxidant and anti-inflammatory effects. Prolongation of the action of the drug is carried out due to the covalent binding of the enzyme to a physiologically active high-molecular carrier (activated derivative of poly-1.4-ethylenepiperazine N-oxide), which has its own pharmacological activity : has an immunomodulatory, detoxifying and antioxidant effect. The presence of a covalent bond significantly increases the enzyme’s resistance to denaturing influences and the influence of inhibitors. The enzymatic activity of Longidase is maintained when heated to 37°C for 20 days, while native hyaluronidase under the same conditions loses its activity within 24 hours. The covalent bond ensures the simultaneous local presence of a hydrolytic enzyme and a carrier capable of binding released enzyme inhibitors and stimulants collagen synthesis (iron, copper ions, heparin). Thanks to these properties, Longidase not only has the ability to depolymerize the connective tissue matrix in fibrous granulomatous formations, but also suppress the reverse regulatory reaction aimed at the synthesis of connective tissue components. The specific substrate of testicular hyaluronidase is glycosaminoglycans (hyaluronic acid, chondroitin, chondroitin-4-sulfate, chondroitin-6-sulfate), which form the basis of the connective tissue matrix. As a result of depolymerization (breaking the bond between C 1 acetylglucosamine and C 4 glucuronic or induronic acids) under the influence of hyaluronidase, glycosaminoglycans lose their basic properties (viscosity, ability to bind water, metal ions). The formation of collagen proteins into fibers is also hampered, the permeability of tissue barriers increases, the movement of fluid in the intercellular space is facilitated, and the elasticity of connective tissue increases. The action of the drug leads to a decrease in tissue swelling, flattening of scars, an increase in the range of motion of joints, a decrease in contractures and adhesions and the prevention of their formation. The drug reduces the manifestations of the acute phase of the inflammatory process, regulates (increases or decreases depending on the initial level) the synthesis of inflammatory mediators (interleukin -1 and tumor necrosis factor), increases the body's resistance to infection and the humoral immune response. Longidase does not have antigenic properties, mitogenic, polyclonal activity, does not have allergenic, mutagenic, embryotoxic, teratogenic and carcinogenic effects.
Indications and contraindications for taking Longidaza
This drug is prescribed not only for the treatment, but also for the prevention of many diseases with connective tissue hyperplasia syndrome. It is used in the following medical fields:
- Gynecology: for inflammatory diseases of the genital organs, as well as for adhesions in the pelvic area.
- Pulmonology: fibrosing and sclerosing diseases of the lungs and respiratory tract, tuberculosis.
- Urology: chronic prostatitis and complicated cystitis.
- Surgery: prevention of adhesions after extensive abdominal surgery.
- Dermatovenereology: scleroderma, rough, keloid, disfiguring scars after various skin pathological processes.
There are also contraindications to the use of Longidase and, despite the low toxicity of the drug, there are quite a few of them:
- Individual intolerance to hyaluronidase.
- Oncological diseases.
- CKD.
- Bleeding and hemorrhage.
- Age under 18 years.
- Infections during the acute period of the disease.
Longidaza
Trade name: Longidaza International name: Hyaluronidase+Azoximer
Release forms: lyophilisate for the preparation of a solution for intramuscular and subcutaneous administration 1.5 thousand IU, 3 thousand IU (ampoules, bottles)
Composition: hyaluronidase conjugated with polyoxidonium 1.5/3 thousand IU
Pharmacological group: enzyme agent
Pharmacological group according to ATK: V03AX (Other medicinal products)
Pharmacological action: hyaluronidase, increasing tissue permeability, improving microcirculation, stimulating tissue repair,
Ingredients: Hyaluronidase + Polyoxidonium
Indications: As part of complex therapy for adults and adolescents over 12 years of age for diseases accompanied by connective tissue hyperplasia. In pulmonology, urology, gynecology with the development of inflammation of the interstitial type: - pneumofibrosis, tuberculosis, alveolitis, tuberculoma, - chronic interstitial cystitis, - adhesions in the pelvis, - tubo-peritoneal infertility. In orthopedics, surgery, cosmetology: – keloid, hypertrophic, retracted scars after pyoderma, trauma, burns, operations, – long-term non-healing wounds, – joint contractures, arthritis, hematomas, – adhesive disease. In dermatovenerology: – limited scleroderma of various localizations. To increase the bioavailability of medicinal and diagnostic drugs.
Dosage regimen: The dosage regimen and method of administration are set individually, depending on the disease, age and severity of the patient’s condition. Longidase is administered subcutaneously (near the site of the lesion or under scar tissue) or intramuscularly. The course ranges from 5 to 15 injections with an interval between injections of 3 to 10 days. If necessary, a repeat course is recommended after 2-3 months. For diseases accompanied by a severe chronic productive process in the connective tissue, it is recommended that after the standard course, maintenance therapy with Longidase at a dose of 3000 IU is recommended with intervals between injections of 10-14 days. Recommended treatment regimens 1. In pulmonology, urology, gynecology, dermatovenerology. For respiratory diseases, the drug is prescribed intramuscularly at a dose of 3000 IU once every 3-5 days for a total course of 10 injections. Further long-term therapy is possible (from 3-4 months to 1 year) at a dose of 3000 IU once every 10-14 days. For diseases of the pelvic organs, the drug is prescribed intramuscularly at a dose of 3000 IU once every 3-5 days for a total course of 5 to 15 injections. For limited scleroderma of various shapes and localization, the drug is administered intramuscularly at a dose of 3000-4500 IU once every 3 days for a course of 5-15 injections. The dose and duration of treatment are selected individually depending on the clinical course, stage, and location of the disease. 2. In orthopedics, surgery, cosmetology For keloid, hypertrophic, retracted scars after pyoderma, burns, operations, the drug is administered inside the scar in a dose of 3000 IU in 1-2 ml 1-2 times a week for a course of 5-10 injections and/or i.v. m once every 3-5 days for a total course of up to 10 injections. For long-term non-healing wounds, the drug is prescribed intramuscularly at a dose of 1500-3000 IU once every 5 days in a course of 5-7 injections. For joint contractures, arthritis, hematomas, Longidase is prescribed intramuscularly at a dose of 3000 IU 1-2 times a week for a course of 7 to 15 injections. For adhesive disease, the drug is administered intramuscularly once every 3-5 days at a dose of 3000 IU for a total course of 7 to 15 injections. 3. To increase the bioavailability of medicinal and diagnostic drugs (antibiotics, chemotherapy drugs, anesthetics), Longidase is administered once every 3 days at a dose of 1500 IU. The course should not exceed 10 injections. For patients with renal failure, the drug should not be prescribed more than once a week. Preparation of solution For intramuscular, subcutaneous or intravenous administration, the contents of the bottle (ampoule) are dissolved in 1.5-2 ml of 0.25% or 0.5% procaine solution. If you are intolerant to procaine, the drug is dissolved with 0.9% sodium chloride solution or water for injection. For electrophoresis, the solution is prepared with distilled water, for inhalation - with a 0.9% sodium chloride solution. The prepared solution for parenteral administration cannot be stored.
Contraindications: – children under 12 years of age (efficacy and safety have not been studied), – malignant neoplasms, – pregnancy, – individual hypersensitivity to the drug. Pregnancy and lactation. The drug is contraindicated for use during pregnancy.
Side effects: Local reactions: pain at the injection site, in some cases local reactions manifest themselves in the form of skin hyperemia and swelling at the injection site. Other: rarely - allergic reactions. All adverse reactions disappear within 48-72 hours. Overdose. Currently, no cases of overdose of Longidaza have been reported.
Pharmacodynamics: A drug with proteolytic activity. It has prolonged enzymatic proteolytic (hyaluronidase) activity, as well as immunomodulatory, chelating, antioxidant and anti-inflammatory effects. Prolongation of the action of the drug is carried out due to the covalent binding of the enzyme to a physiologically active high-molecular carrier (an activated derivative of poly-1,4-ethylenepiperazine N-oxide), which has its own pharmacological activity: it has an immunomodulatory, detoxifying and antioxidant effect. The presence of a covalent bond significantly increases the enzyme's resistance to denaturing influences and the influence of inhibitors. The enzymatic activity of Longidase is maintained when heated to 37°C for 20 days, while native hyaluronidase loses its activity within 24 hours under the same conditions. The covalent bond ensures the simultaneous local presence of a hydrolytic enzyme and a carrier capable of binding released enzyme inhibitors and stimulators of collagen synthesis (iron, copper ions, heparin). Thanks to these properties, Longidaza not only has the ability to depolymerize the connective tissue matrix in fibrogranulomatous formations, but also suppress the reverse regulatory reaction aimed at the synthesis of connective tissue components. The specific substrate of testicular hyaluronidase is glycosaminoglycans (hyaluronic acid, chondroitin, chondroitin-4-sulfate, chondroitin-6-sulfate), which form the basis of the connective tissue matrix. As a result of depolymerization (breaking the bond between C1 acetylglucosamine and C4 glucuronic or induronic acids) under the influence of hyaluronidase, glycosaminoglycans lose their basic properties (viscosity, ability to bind water, metal ions). The formation of collagen proteins into fibers is also hampered, the permeability of tissue barriers increases, the movement of fluid in the intercellular space is facilitated, and the elasticity of connective tissue increases. The effect of the drug leads to a decrease in tissue swelling, flattening of scars, an increase in the range of motion of joints, a decrease in contractures and adhesions and the prevention of their formation. The drug reduces the manifestations of the acute phase of the inflammatory process, regulates (increases or decreases depending on the initial level) the synthesis of inflammatory mediators (interleukin-1 and tumor necrosis factor), increases the body's resistance to infection and the humoral immune response. Longidase does not have antigenic properties, mitogenic, polyclonal activity, does not have allergenic, mutagenic, embryotoxic, teratogenic and carcinogenic effects.
Pharmacokinetics: Absorption and distribution When administered subcutaneously or intramuscularly, the drug is rapidly absorbed into the systemic circulation from the injection site, with Cmax achieved within 20-25 minutes. It is characterized by a high distribution rate, the half-life of distribution is about 30 minutes. Penetrates into all organs and tissues (including through the blood-brain barrier and the blood-ophthalmic barrier). Does not accumulate. Metabolism and excretion In the body, hyaluronidase undergoes hydrolysis and is excreted primarily by the kidneys. The carrier is metabolized to low molecular weight compounds (oligomers), which are excreted by the kidneys. T1/2 for different routes of administration ranges from 42 to 84 hours.
Special instructions: The drug should not be administered into the area of infection, acute inflammation or tumor. Carefully. Acute renal failure, pulmonary hemorrhage.
Interaction: Longidase is compatible with antibiotics, antiviral, antifungal and antihistamines, bronchodilators, cytostatics, corticosteroids. When used together, it increases the bioavailability of drugs and accelerates the onset of analgesia when local anesthetics are administered.
Storage conditions: List B. The drug should be stored in a dry place, protected from light, out of reach of children, at a temperature not exceeding 15°C.
Shelf life: 2 years.
Dispensed from pharmacies: The drug is available with a prescription.
Drug registration number: LS-000764
Date of registration (re-registration) of the drug: 09/23/2005
Longidaza: how to take
- Injection form. The course of therapy ranges from 5 to 25 injections, each of which is given once every few days, the frequency depends on the prescription of the treating doctor. When using Longidase for prophylactic purposes, the interval between injections is 2 weeks.
Before administration, the powder is dissolved in 1-2 milliliters of procaine or in saline if the anesthetic is intolerant. The drug is administered slowly and immediately after preparation; it cannot be stored.
- Suppositories. They are administered vaginally before bedtime and in a lying position, rectally only after cleansing the intestines. The course of treatment ranges from 10 to 20 suppositories, depending on the pathology. The interval between administrations is from 48 to 72 hours.
LONGIDAZE lyophilized powder for the preparation of solution for infusion 3000me No. 5
Longidaza is applied subcutaneously (near the site of the lesion or under scar tissue) or intramuscularly at a dose of 3000 IU in a course of 5 to 25 injections (depending on the disease) with an interval between injections of 3 to 10 days. Methods of application are selected by the doctor depending on the diagnosis, severity of the disease, clinical course, and age of the patient. If necessary, a repeat course is recommended after 2-3 months. In the case of treatment of diseases accompanied by a severe chronic productive process in the connective tissue, after a standard course, long-term maintenance therapy with Longidaza is recommended with breaks between injections - 10-14 days. To increase the bioavailability of drugs and diagnostic agents, a dose of 1500 IU is recommended with a preliminary 10-15 minutes intramuscular or subcutaneous injection into the same place as the main drug. Dilution The contents of the Longidaza ampoule or bottle are dissolved in 1-2 ml of procaine solution (0.25% or 0.5%). In case of intolerance to procaine, the drug is dissolved in the same volume of 0.9% sodium chloride solution for injection or water for injection. When used to increase bioavailability, the contents of the Longidaza ampoule or vial are dissolved in 2 ml, and with a dose of 1500 IU - in 1 ml of 0.9% sodium chloride solution for injection. The solvent must be introduced into the vial or ampoule slowly, wait for 2-3 minutes, and carefully mix without shaking so as not to foam the protein. The prepared solution for parenteral administration cannot be stored. Do not administer IV! Recommended prevention and treatment regimens For the prevention of adhesive disease and severe scarring after surgical interventions on the abdominal and pelvic organs IM at a dose of 3000 IU 1 time every 3 days for a course of 5 injections. If necessary, the use of the drug can be continued with a general course of up to 10 injections when administered once every 5 days. For treatment in gynecology: adhesions in the pelvis for inflammatory diseases of the internal genital organs - intramuscularly once every 3-5 days for a course of 10-15 injections; tubo-peritoneal infertility - IM with a general course of up to 15 injections: the first 5 injections 1 time in 3 days, then - 1 time in 5 days. in urology: chronic prostatitis - intramuscularly once every 5 days, in a course of 10-15 injections; interstitial cystitis - intramuscularly once every 5 days, for a course of up to 10 injections. in surgery: adhesive disease after surgical interventions on the abdominal organs - intramuscularly once every 3-5 days for a course of 10 to 15 injections; long-term non-healing wounds - intramuscularly once every 5 days with a course of 5-10 injections. in dermatovenereology, cosmetology: limited scleroderma - intramuscularly once every 3-5 days for a course of up to 20 injections. The dose and course are selected individually depending on the clinical course, stage, location of the disease and the individual characteristics of the patient; keloid, hypertrophic and developing scars after pyoderma, burns, operations, injuries - intra-scar or subcutaneous injection near the site of the lesion, administration 1 time every 3 days, for a course of up to 15 injections at a dosage of 3000-4500 IU. The volume of dilution of the drug Longidaza is selected by the doctor depending on the number of points of administration. If necessary, the course can be continued according to the scheme once every 5 days up to 25 injections. Depending on the area of skin damage and the age of scar formation, alternating subcutaneous and intramuscular administration is possible once every 5 days at a dose of 3000 IU, for a course of up to 20 injections. in pulmonology and phthisiology: pneumosclerosis - intramuscularly once every 5 days for a course of 10 injections; fibrosing alveolitis - intramuscularly once every 5 days for a course of 15 injections, then maintenance therapy once every 10 days for a total course of up to 25 injections; tuberculosis - intramuscularly once every 5 days for a course of up to 25 injections; Depending on the clinical picture and severity of the disease, long-term therapy is possible (from 6 months to 1 year at a dose of 3000 IU once every 10 days). in orthopedics: joint contractures - subcutaneously near the site of the lesion at a dose of 3000 IU once every 3 days for a course of 5 to 15 injections; arthrosis, ankylosing spondylitis - subcutaneous injection near the site of the lesion in a dose of 3000 IU once every 3 days for a course of up to 15 injections, if necessary, treatment can be continued with injections once every 5 days. The duration of maintenance therapy is selected by the doctor depending on the severity of the disease; hematomas - subcutaneously near the site of the lesion at a dose of 3000 IU once every 3 days for a course of up to 5 injections. To increase bioavailability: when administered subcutaneously or intramuscularly with diagnostic or medicinal drugs (antibiotics, chemotherapy drugs, anesthetics and others), Longidase is administered 10-15 minutes beforehand at a dose of 1500 IU in the same way and in the same place, as the main drug.