Relatox
Relatox: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Relatox
ATX code: M03AX01
Active ingredient: botulinum toxin type A - hemagglutinin complex (botulinum toxin type A - hemagglutinin complex)
Manufacturer: FSUE "NPO Microgen" (Russia)
Description and photo updated: 20.11.2018
Relatox is a muscle relaxant of peripheral action.
Release form and composition
I release Relatox in the form of a lyophilisate for preparing a solution for intramuscular (i / m) administration: a lyophilized porous powdery mass, compressed into a white with a yellow tint or white tablet [50 or 100 U (unit of action) in vials, in a polymer can or transparent container 1 bottle, in a cardboard box 1 polymer can or container complete with one blister insert containing 1 ampoule (for bottles with 50 U of lyophilisate) or 2 ampoules of solvent (for bottles with 100 U of lyophilisate), or without solvent].
1 bottle contains:
- active substance: a complex of hemagglutinin and botulinum toxin type A - 50 U or 100 U;
- auxiliary components: maltose, gelatin.
Pharmacological properties
Pharmacodynamics
Relatox is a drug that inhibits the release of acetylcholine, the main neurotransmitter in the parasympathetic nervous system, which carries out neuromuscular transmission.
Isolated from Clostridium botulinum type A, botulinum toxin type A consists of molecules that are disulfide bonds of light and heavy chains. The heavy (molecular weight 100,000 daltons) chain has a high binding affinity for specific receptors located on the surface of target neurons. The light (molecular weight 50,000 daltons) chain has a specific Zn 2+ -dependent protease activity towards the cytoplasmic regions of the synaptosomal bound protein (molecular weight 25,000 daltons) - SNAP-25, which is involved in exocytosis processes.
The mechanism of action of botulinum toxin type A consists of three stages, the end effect of which is sustained chemodenervation. At the first stage, specific binding with the presynaptic membrane occurs, at the second, the molecule penetrates through endocytosis into the cytosol of the nerve. At the third stage, the action of the intracellular light chain is aimed at selective cleavage of SNAP-25, which causes blocking of the release of acetylcholine from the presynaptic terminals of cholinergic neurons.
The intramuscular injection of Relatox causes the development of two effects. By inhibiting alpha-motor neurons at the level of the neuromuscular synapse, there is a direct inhibition of extrafusal muscle fibers and inhibition of muscle spindle activity as a result of inhibition of gamma-motor neuron cholinergic synapse on the intrafusal fiber. Relaxation of the intrafusal fibers of the muscle spindle, which occurred against the background of a decrease in gamma activity, reduces the activity of Ia-afferent nerve fibers. As a result, the activity of muscle stretch receptors decreases, and the efferent activity of alpha and gamma motor neurons occurs. The clinical manifestations of the introduction of Relatox into the muscles are their pronounced relaxation and a significant reduction in pain. In the injected muscles, along with the denervation process, the reinnervation process takes place,the purpose of which is to restore muscle contractions. Muscle contractility is restored 4-6 months after injection as a result of the appearance of lateral processes of nerve endings.
Pharmacokinetics
Pharmacological action of Relatox develops directly at the injection site. Retrograde axonal transport from the insertion site and presynaptic uptake are negligible.
The clinical effect lasts for 4-6 months. The restoration of neuromuscular activity is facilitated by the development of new axonal processes that form new functional neuromuscular synapses. Their activity ensures the restoration of muscle contractions.
Therapeutic doses of Relatox do not cross the blood-brain barrier and do not cause significant systemic effects.
Non-toxic metabolites are excreted through the kidneys.
Against the background of repeated injections of the drug, 1–5% of patients develop antibodies to the complex of botulinum toxin type A with hemagglutinin, which reduce the effect of the complex. Their formation is facilitated by the introduction of high doses of Relatox with frequent repeated injections in small doses.
Indications for use
- blepharospasm;
- spasticity of the muscles of the upper limb due to the previous ischemic stroke;
- correction of hyperkinetic folds (mimic wrinkles) of the face in adults.
Contraindications
- acute period of infectious diseases;
- pronounced hernias in the upper and lower eyelids;
- inflammatory process at the site of the proposed injection of Relatox;
- pronounced stage of gravitational ptosis of facial tissues;
- the period after undergoing facial surgery is less than 1/4 of the year;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to the components of Relatox.
With a high degree of caution and after a thorough assessment of the balance of benefits and risks from therapy, it is recommended to prescribe Relatox in the presence of subclinical or clinical signs of impaired neuromuscular transmission (including myasthenia gravis, Lambert-Eaton syndrome and other myasthenic-like syndromes), ecchymosis in the area of injection, pathological changes in the cornea, allergic history (especially in patients with hypersensitivity to drugs containing proteins).
It is recommended to prescribe the use of Relatox only on the basis of the results of an ophthalmologist's conclusion in patients with angle-closure glaucoma, a high degree of myopia.
Care should be taken to inject in the immediate vicinity of the lungs, especially to their upper borders.
Instructions for the use of Relatox: method and dosage
The ready-made solution of the Relatox lyophilisate is used by i / m administration
The solution should be prepared under sterile conditions in accordance with the rules of asepsis. The stopper of the vial with lyophilisate must be treated with ethyl alcohol. For dissolution, 0.9% sodium chloride solution for injection is used. Puncture the stopper with a sterile needle 23-25 mm long, inject 1-8 ml of solvent into the vial. After dissolution of Relatox, a clear, colorless liquid is formed.
It is forbidden to open the bottle and remove the cork!
Insulin syringes with a non-removable needle diameter of 0.27–0.29 mm are used to inject the injection solution.
The concentration of the finished solution depends on the volume injected into the vial of a 0.9% sodium chloride solution for injection.
When diluting a lyophilisate containing 50 units of a complex of hemagglutinin and botulinum toxin type A, its activity (amount of units in 0.1 ml) is:
- 1 ml of a solution of 0.9% sodium chloride for injection: 5 units in 0.1 ml of the finished solution;
- 2 ml: 2.5 U;
- 2.5 ml: 2 units;
- 4 ml: 1.25 U
When diluting a lyophilisate containing 100 units of a complex of hemagglutinin and botulinum toxin type A, its activity (amount of units in 0.1 ml) is:
- 2 ml of a solution of 0.9% sodium chloride for injection: 5 units in 0.1 ml of the finished solution;
- 4 ml: 2.5 U;
- 5 ml: 2 U;
- 8 ml: 1.25 U
The recommended doses expressed in units of action are suitable only for Relatox.
Recommended doses, routes of administration and schemes for the correction of facial wrinkles:
- smoothing of glabellar wrinkles [muscle, puckering eyebrow (musculus corrugator supercilii) and muscle of arrogant (musculus procerus)]: the individual dose depends on the age, the severity of wrinkles and the gender of the patient - 2.5-7.5 IU in each marked point. The maximum amount of Relatox injected at all points in this area is 25 units. The patient must frown to determine the injection points. This makes it easy to palpate the puckering muscle. Up 0.5 cm from the upper medial edge of each eyebrow is the point of the most pronounced muscle activity. The needle is inserted to a depth of 7-10 mm into the abdominal thickness at an angle of 45 ° (medially, from front to back) or at an angle of 90 °. If it rests against the periosteum, it should be pulled out 1 mm and the drug should be injected. The proud muscle is located in the center of the line connecting the medial edges of the eyebrows. The needle is inserted to a depth of 2–3 mm in the front to back position;
- smoothing of horizontal wrinkles in the forehead, which are formed by the epicranial muscle (musculus epicranius): 1.25-2.5 U in each of 5-10 marked points. With a slight severity of wrinkles, it is enough to introduce 2.0-2.5 U in the middle of the right and left sides of the frontal region. In patients with a very high forehead and formation of folds close under the hairline, an additional injection of 1.25–2.5 U of Relatox at 2–3 points located parallel to the hairline is possible. The maximum amount of the drug injected at all points in this area is 20 U. To determine the injection points, the patient must raise their eyebrows. The most pronounced mimic activity is at the points located at the maximum amplitude of the eyebrows. The injection point should be at least 2 cm from the upper edge of the eyebrow. To maintain the mobility of the tips of the eyebrows, you can arrange the injection points in a V-shape;
- smoothing of wrinkles ("crow's feet") in the periorbital region - the circular muscle of the eye (musculus orbicularis oculi): 2–2.5 U in each point. Since the radius of diffusion from one point is 5–10 mm, the distance between the points should not exceed 10–20 mm. To define the boundaries of the area with the most wrinkles, the patient must laugh. The dose is determined based on the area of this area at rest. The maximum amount of Relatox injected at all points on one side of this area is 25 U. Usually, 2 to 4 injections are made on each side, in the projection area of the circular muscle of the eye and in the places of maximum muscle activity of the lateral part of the lower eyelid. The distance from the outer corner of the eye should not be less than 10 mm. To maintain the proportions of the face, the insertion points must be positioned as symmetrically as possible. Do not allow the drug to enter as a result of diffusion into the large zygomatic muscle (musculus zygomaticus major) due to the risk of disrupting the symmetry of the nasolabial fold and corners of the mouth;
- smoothing of wrinkles in the nasal dorsum - nasal muscle (musculus nasalis): 2.5 units on each side;
- smoothing of wrinkles in the lower part of the face: directly into the wing part of the nasal muscle (musculus nasalis) - 2.5 U on each side. Intradermally, in wrinkles, 2 mm away from the edge along the red border of the upper lip (4–6 points) - 1.25 U per point. In the muscle that lowers the corner of the mouth (musculus depressor anguli oris), subcutaneously - 2.5 units. In the chin muscle (musculus mentalis) subcutaneously - 2.5 units.
Recommended doses, schemes and method of administration of Relatox in the treatment of blepharospasm: superficially intramuscularly - 2.5-5 U in each of the following points (needle gauge 28-30): at the lateral corner of the eye - one point, on the upper eyelid - two points, on the lateral half of the lower eyelid - one point. The initial dose of the drug for one side is on average 15-25 units.
The maximum allowable dose for the periorbital area is up to 25 units per side.
Depending on the individual characteristics of the organism, a pronounced clinical effect after the injection of Relatox may appear in 2-14 days, and persist for 120-180 days.
The effect of the drug is assessed by examination 30 days after the administration of Relatox, comparing with the initial state.
In the absence of a significant clinical effect, the following measures are required:
- clinical confirmation, including electromigraphic (EMG) studies, of the effect of the toxin on the injected muscle or muscles;
- analysis of the reasons that caused the ineffectiveness of the procedure (low dose, inadequate choice of points for the injection of Relatox, incorrect injection technique, weakness of antagonist muscles, signs of fixed contracture, formation of toxin neutralizing antibodies);
- reassessment of the feasibility of using botulinum toxin type A;
- the repeated procedure - in the absence of undesirable effects associated with the first injection of Relatox - should be carried out in compliance with the following conditions: dose assignment, taking into account the analysis of the reasons for the ineffectiveness of the previous procedure, EMG control, the interval between procedures is at least 90 days.
The absence or decrease in the severity of the effect after repeated injections is the basis for offering the patient other methods of treatment.
The doctor calculates the dose of Relatox for the treatment of spasticity of the muscles of the upper limb in patients after ischemic stroke and determines the number of injection points individually for each patient. This takes into account the size and number of muscles involved in the pathological process, their localization, the severity of spasticity.
For more accurate administration of the drug solution, it is possible to use an electromyograph.
For the introduction of Relatox into the superficial muscles, needles of 30 G, 27 G or 25 G are used, into the deep muscles of the upper limb - needles of greater length.
Recommended doses, regimens and method of administration of the drug in the treatment of spasticity of the muscles of the upper limb caused by a previous ischemic stroke:
- flexor muscles of the fingers: deep flexor of the fingers (musculus flexor digitorum profundus) - 15-50 U, superficial flexor of the fingers (musculus flexor digitorum superficialis) - 15-50 U, muscle adductor thumb (musculus adductor pollicis) - 20 U, long flexor of the thumb of the hand (musculus flexor pollicis longus) - 20 units;
- flexor muscles of the hand: radial flexor of the wrist (musculus flexor carpi radialis) - 15–60 units, ulnar flexor of the wrist (musculus flexor carpi ulnaris) - 10–50 units;
- flexor muscles of the elbow joint: biceps muscle of the shoulder (musculus biceps brachii) - 100-150 U, brachial muscle (musculus brachialis) - 20-60 U, brachioradialis muscle (musculus brachioradialis) - 20-100 U, round rotator of the forearm (musculus teres) - 10-30 U;
- muscles leading the shoulder joint to the body: the pectoralis major muscle (musculus pectoralis major) - 20–100 units, the large round muscle (musculus teres major) - 5–40 units, the broadest muscle of the back (musculus latissimus dorsi) - 20–100 units.
The maximum single dose of one course of treatment is 400 U, distributed between the selected muscles.
The effect of Relatox begins to appear 7 days after the injection, the maximum decrease in muscle tone occurs within the next 30-60 days.
Side effects
Side effects recorded during clinical trials arising in the treatment of blepharospasm and correction of hyperkinetic folds (mimic wrinkles) of the face:
- from the nervous system: infrequently - asymmetry of the corners of the mouth; rarely - drowsiness, dizziness, headache; very rarely - difficult closure of the eyelids, paresis of facial muscles, lagophthalmos, numbness of the lips, impaired articulation, paralysis of facial muscles;
- local reactions: often - irritation, pain at the injection site, induration, edema, feeling of tightness of the skin, hyperemia at the injection site, erythema; infrequently - microhematomas, punctate keratitis, ecchymosis; very rarely - diffuse hyperemia;
- on the part of the organ of vision: very rarely - increased lacrimation, violation of accommodation, photophobia, dry eyes;
- from the musculoskeletal and connective tissue: very rarely - drooping of the lateral areas of the eyebrows, the glabellar region, ptosis;
- from the digestive system: rarely - nausea;
- general disorders: rarely - a short-term increase in body temperature up to 37.5 ° C, general weakness.
Side effects recorded in clinical trials in the treatment of upper limb muscle spasticity that arose in patients after ischemic stroke:
- from the nervous system: often - dizziness, headache; infrequently - paresthesia, hypesthesia; rarely - lack of coordination;
- local reactions: very often - pain, skin irritation, swelling; infrequently - hemorrhage at the injection site;
- mental disorders: often - insomnia;
- from the musculoskeletal and connective tissue: often - muscle weakness; infrequently - pain in the arm, arthralgia;
- dermatological reactions: infrequently - itchy skin;
- from the digestive system: rarely: nausea.
During the procedure, the needle may damage vital structures - blood vessels and nerves.
Overdose
Symptoms: general weakness, difficulty swallowing, diplopia, speech disorder, ptosis, paresis of the respiratory muscles.
Treatment: immediate hospitalization. In the case of paralysis of the muscles of the respiratory system, intubation and transfer of the patient to artificial ventilation are necessary.
special instructions
Relatox is dispensed and used only in specialized medical institutions.
Injections should be carried out by a highly qualified doctor in a treatment room of specialized hospitals or on an outpatient basis.
With neuromuscular diseases, even with the use of conventional doses of the drug, the risk of developing clinically pronounced systemic effects (including severe dysphagia, respiratory failure) increases.
The use of Relatox for spasticity of the muscles of the upper limb after ischemic stroke should be combined with the standard treatment regimen for post-stroke spasticity.
The remains of an unused solution of the drug in a vial or after injection in a syringe must be inactivated. To do this, use a diluted sodium hypochlorite solution containing 1% active chlorine. The auxiliary materials in contact with the solution must be disposed of in accordance with the regulations for the destruction of biological waste.
Influence on the ability to drive vehicles and complex mechanisms
According to the instructions, Relatox can cause visual disturbances, muscle weakness, and dizziness. Therefore, in order to avoid danger, it is recommended to temporarily refrain from driving.
Application during pregnancy and lactation
The use of Relatox is contraindicated during the period of gestation and breastfeeding.
Pediatric use
The use of a muscle relaxant in children and adolescents under the age of 18 is contraindicated.
Drug interactions
The simultaneous use of antibacterial agents (tetracyclines, aminoglycosides, polymyxins, erythromycin), non-depolarizing muscle relaxants and other drugs that reduce neuromuscular transmission enhances the action of Relatox.
Analogs
The analogues of Relatox are Dysport, Lantoks, Xeomin, Botox.
Terms and conditions of storage
Keep out of the reach of children.
Store at 2–8 ° C in a closed, labeled package.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Relatox
Reviews about Relatox are positive. Patients who have used the drug to smooth out facial wrinkles write more often. The procedure is a little painful, but quite bearable. Relatox does not cause any undesirable effects. The achieved effect lasts for a long time. The advantages of the domestic drug include the quite affordable price of the procedures.
Patients are advised to entrust injections only to a doctor with special training.
Price for Relatox in pharmacies
The price for Relatox has not been set because the drug is not available in the pharmacy chain.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
