Project Description

«Solution carnosine 5%»

Solutio Сarnosini 5%

international nonproprietary name

Not established

Ref

BP-0132

Pharmacotherapeutic group

Preparationforeyetreatment. Preparation for local application for nose diseases. Antioxidants. Antihypoxants.

Composition of the preparation

Active agent – L-carnosineарнозин (β-alanil-L-histidine) – 50 mg/ml;  auxiliary agents  – sodium chloride, benzalconium chloride, water for injections

Pharmacological action

Pharmacodynamics

Carnosine is a histine-containing containing dipeptide, one of the natural products of metabolism in humans. It is a biologically active dipeptide influencing metabolic processes: glycolisis, oxidative phosphorylation. L-carnosine is found in the organism of mammals (in the muscle and nerve tissue, in the crystalline lens, retina and other tissues of the eyeball.

The mechanism of action is conditioned by antioxidant and membrane-protection action. Carnosine inhibits lipid peroxidation, enhances antioxidant protection, increases the organism resistance to exposure of different pathological factors on oxygen-dependent conditions. It is a mobile buffer of protons, modulates the activity of glutamate receptor complexes. Carnosine has an intensifying action on oxidative phosphorylation processes that leads to resynthesis of high-energy compounds necessary for muscle activity. It intensifies ATP, enhances the ration of Са++/АTP on impaired active transport of sodium ions in the sarcoplasmic reticulum, intensifies the effectiveness of active transport of sodium and potassium ions. It provides the elimination of lactate from the muscle tissue, eliminates muscular weakness, enhances the force and duration of muscular contractions. Carnosine improves the blood supply, microcirculation and rheological blood properties, stabilizes the membrane structures.

Thepreparationhasalocalanti-inflammatoryandanti-allergicaction. It neutralizes hypochlorite-anion generated by myeloperoxidase (formed on allergic damages, virus and bacteria infection as a result of neutrophil degranulation); blocks the acidulation in the inflammatory tissue. It has a modulating action on the cell immunity.

It enhances the healing of defects and damages of the cornea epithelium of traumatic, chemical, irradiation, infection and trophic aethiology. It has a marked therapeutic effectiveness on treatment of trophic keratitis, post-herpetic epithelia, primary and secondary dystrophy of the cornea, recurrent corneal erosion, bullous keratopathy. Carnosine being part of the complex therapy enhances the healing of ulcer cornea keratopathy on herpes viral and bacteria infection, dry keratoconjunctivitis. It contributes to the elimination of symptoms of seasonal allergic rhynoconjunctivitis, seasonal allergic rhinitis (reduces stuffiness in the nose, itching in the nose, sneezing, secretion from the nose).

 Pharmacokinetics

On use of eye drops of carnosine the active agent in biologically active concentrations does not penetrate in the systemic blood flow. The therapeutic concentration is achieved on the local application of the preparation in the tissues and biological fluids of the eye and nasal mucosa.

Carnosine is completely metabolizes in the human organism and sot not accumulate in the organs and tissues. It is subject to hydrolysis by carnosinase enzyme located in the small intestine, liver, eye tissues, olfactory nasal epithelia, spleen, heart, skeletal muscles, blood serum. It is excreted with urine.

Indications 

Ulcer keratitis, keratopathy (of various aetiology), metabolic diseases of the cornea tissues, метаболические. Seasonal allergic phynoconjunctivis. Seasonal allergic rhenitis.

special indication

Not established

special warning

Not established

Dosage and method of administration

In the form of instillation in the conjunctival bag in the amount of 1-3 drops 4-6 times per day.  The duration of treatment depends on the patient’s condition (usually 1-3 weeks) and is determined by the doctor.

On seasonal allergic rhynoconjunctivitis the preparation is prescribed in the form of instillations in the conjunctival bag in the amount of 1-2 drops 4-6 times a day. The duration of treatment is 8 weeks.

On seasonal allergic rhinitis the preparation is prescribed in 5 drops in the both halves of the nose 3 times a day during 8 weeks.

overdosage

Cases of overdosing on the administration of carnosine have not been specified.

safety measures

Not established

Side effects

As a rule, no negative effects have been specified.

In rare cases the feeling of burning is possible, and in such cases the administration of the preparation shall be stopped.

Contraindications

Higher sensitivity to carnosine.

Due to absence of corresponding tests in humans, there is a potential risk of development of negative effects on pregnancy and lactation. Therefore the preparation is contraindicated on pregnancy and lactation (lactation shall be stopped during the treatment period).

Interactions with other medicinal preparations

No negative effects on the administration of carnosine in combination with other medications have been specified.

In ophthalmology the preparation may be used in the complex therapy together with idoxuridine, acyclovir (eye ointment), dexamethasone.

The form of release

5% solution (eye drops and nasal drops).