Longidaza

General characteristics. Structure:

Active agent: лонгидаза®, substance (a hyaluronidase conjugate with copolymer of N-oxide of a 1,4-etilenpiperazin and (N-carboxymethyl) - bromide 1,4-etilenpiperaziniya) 3000 ME

Basis: cocoa butter - before receiving suppository weighing 1,3 g.

Pharmacological properties:

Longidaza has gialuronidazny (enzymatic proteolytic) activity of the prolonged action, the chelating, antioxidant, immunomodulatory and moderately expressed antiinflammatory properties.
Prolongation of effect of enzyme is reached by covalent linkng of enzyme with physiologically active high-molecular carrier (to the activated derivatives of N-oxide poly-1,4 - этиленпиперазина, an analog a polioksidoniya) having own pharmacological activity. Longidaza shows antifibrous properties, weakens a current of an acute phase of an inflammation, regulates (raises or reduces depending on initial level) synthesis of mediators of an inflammation (interleykina-1 and a tumor necrosis factor - an alpha), raises a humoral immune response and resistance of an organism to an infection.
The expressed antifibrous properties of Longidaza are provided with conjugation of hyaluronidase with the carrier that considerably increases resistance of enzyme to denaturant influences and effect of inhibitors: enzymatic activity of Longidaza remains when heating to 37 °C within 20 days while native hyaluronidase in the same conditions loses the activity within a day. In the drug Longidaza simultaneous local presence of proteolytic enzyme of hyaluronidase and the carrier capable to connect the inhibitors of enzyme and stimulators of synthesis of collagen which are released at hydrolysis of components of a matrix is provided (ions of iron, copper, heparin, etc.). Thanks to the specified Longidaza properties possesses not only ability to depolymerize a matrix of connecting fabric in a fibrous granulematoznykh educations, but also to suppress the back regulatory reaction directed to synthesis of components of connecting fabric.
Specific substrate of testicular hyaluronidase are glikozaminoglikana (hyaluronic acid, chondroitin, chondroitin-4-sulfate, chondroitins-6-sulfates) making a basis of a matrix of connecting fabric. As a result of a depolymerization (a rupture of communication between C1 of an atsetilglyukozamin and C4 of glucuronic or induronovy acids) glikozaminoglikana change the main properties: viscosity decreases, ability to connect water, ions of metals decreases, permeability of fabric barriers temporarily increases, the movement of liquid in intercellular space is facilitated, elasticity of connecting fabric increases that is shown in reduction of puffiness of fabric, flattening of hems, increase in volume of the movement of joints, reduction of contractures and the prevention of their formation, reduction of commissural process. Biochemical, immunological, histologic and electronic microscopic examinations it is proved that Longidaza does not damage normal connecting fabric, and causes destruction changed on structure and structure of connecting fabric in the field of fibrosis.

Longidaza does not possess mutagen, embriotoksichesky, teratogenic and cancerogenic action.
Drug is well transferred by patients, local and general allergic reactions are noted.
Use of Longidaza in therapeutic doses in time or after operational treatment does not cause deterioration in a current of the postoperative period or progressing of infectious process; does not slow down recovery of a bone tissue.

Pharmacokinetics. Experimental studying of pharmacokinetics of suppositories c the enzyme carrier, marked hyzone, allowed to establish that at rectal administration drug is characterized by the high speed of distribution in an organism, is well soaked up in a system blood stream and reaches the maximum concentration in blood in 1 hour. The semi-distribution period - about 0,5 hours, the period of semi-elimination from 42 to 84 hours. It is removed preferential by kidneys.
Drug gets into all bodies and fabrics, including passes through hematoencephalic and hemato-ophthalmic barriers. Lack of fabric cumulation is established.
Bioavailability of rectal suppositories of Longidaza not less than 70%.

Indications to use:

To adults and teenagers 12 years in the form of monotherapy and as a part of complex therapy of the diseases which are followed by a hyperplasia of connecting fabric including against the background of inflammatory process are more senior:

• in urology: chronic prostatitis, intersticial cystitis, strictures of an urethra and ureters, Peyroni's disease, an initial stage of a benign hyperplasia of a prostate, prevention of formation of hems and strictures after operative measures on an urethra, a bladder, ureters;
• in gynecology: commissural process (prevention and treatment) in a small basin at chronic inflammatory diseases of internal generative organs, after gynecologic manipulations, including artificial abortions postponed earlier operative measures on bodies of a small pelvis; intrauterine synechias, pipe and peritoneal infertility, chronic endomyometritis;
• in a dermatovenereology: limited scleroderma, prevention of fibrous complications of infections, sexually transmitted;
• in surgery: prevention and treatment of commissural process after operative measures on abdominal organs; it is long not healing wounds;
• in pulmonology and phthisiology: pneumofibrosis, siderosis, tuberculosis (cavernous and fibrous, infiltrative, tuberculoma), intersticial pneumonia, fibroziruyushchy alveolitis, pleurisy;
• for increase in bioavailability of antibacterial therapy in urology, gynecology, a dermatovenereology, surgery, pulmonology, etc.

Route of administration and doses:

Longidaza suppositories 3000 ME is recommended for rectal or vaginal use for the night by a course from 10 to 20 introductions once a day.
Rektalno: on 1 suppository of 1 times a day after purgation.

Vaginalno: on 1 suppository of 1 times a day (for the night) suppository is entered into a vagina in a prone position.
The scheme of introduction is adjusted depending on weight, a stage and duration of a disease: Longidaza is appointed every other day or with breaks in 2-3 days.

The recommended schemes and doses:
• in urology: on 1 suppository every other day 10 introductions, further in 2-3 days of 10 introductions, the general rate of 20 suppositories.
• in gynecology: rektalno or vaginalno on 1 suppository in 2 days of 10 introductions, further if necessary the maintenance therapy is appointed.
• in a dermatovenereology: on 1 suppository in 1-2 days of 10-15 introductions.
• in surgery: on 1 suppository in 2-3 days of 10 introductions.
• in pulmonology and phthisiology: on 1 suppository in 2-4 days of 10-20 introductions.
If necessary the repeated rate of Longidaza is recommended not earlier than in three months or a long maintenance therapy on 1 suppository of 1 times in 5-7 days within 3-4 months.

Features of use:

To interrupt use of Longidaza at development of allergic reaction. At use against the background of an aggravation of the centers of an infection for the prevention of spread of an infection to appoint under cover of antimicrobic means.

Side effects:

Seldom - allergic reactions at the increased individual sensitivity.

Interaction with other medicines:

When using Longidaza at the patients receiving high doses of salicylates, a cortisone, AKTG, estrogen or antihistaminic drugs efficiency of effect of enzyme of hyaluronidase can be reduced.

At appointment in a combination with other medicines it is necessary to consider a possibility of increase in their absorption (bioavailability) and strengthening of systemic action.

Contraindications:

The increased individual sensitivity to drugs with gialuronidazny activity, Longidaza; malignant new growths. Pregnancy (clinical experience of use is absent). Children's age up to 12 years (efficiency and safety were not studied).

WITH CARE
With care to apply not more often than 1 time a week at patients with a renal failure, pulmonary bleedings in the anamnesis.

Overdose:

There are no data.

Storage conditions:

In the dry place protected from light at a temperature from 2 to 15 °C. To protect from children.

Issue conditions:

Without recipe

Packaging:

Suppositories vaginal and rectal 3000 ME.

5 suppositories in a blister strip packaging from a film polyvinyl chloride. One or two blister strip packagings in a pack from a cardboard together with the application instruction.