Botulinum toxin
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Clinical Pharmacology
ATH code:
M03AH01 The type A botulinum toxin molecule consists of heavy (with a molecular weight of 100,000 daltons) and light (with a molecular weight of 50,000 daltons) chains connected by a disulfide bridge. A heavy chain has a high affinity for binding to specific receptors located on the surface of target neurons. The light chain possesses Zn2 + -dependent protease activity, specific to the cytoplasmic sites of the synaptosomally bound protein, having a molecular weight of 25,000 daltons (SNAP-25) and participating in exocytosis. The first stage of botulinum toxin type A is the specific binding of the molecule to the presynaptic membrane. The second stage is the penetration of the bound toxin into the cytosol of the nerve through endocytosis. Intracellularly, the light chain acts as a Zn2 + dependent pytosol protease. selectively cleaving SNAP-25, which in the third stage leads to blockade of acetylcholine release from the presynaptic terminals of cholinergic neurons. The end effect of this process is persistent chemodenervation.
When administered intramuscularly, 2 effects develop: direct inhibition of extrafusal muscle fibers by inhibiting alpha motoneurons at the neuromuscular synapse level and inhibiting the activity of muscle spindles by inhibiting gamma-motoneuron cholinergic synapse on the intrafusal fiber. Reduction of gamma activity leads to relaxation of the intrafusal fibers of the muscle spindle and reduces the activity of Ia-afferent nerve fibers. This leads to a decrease in the activity of muscle receptors of stretching, as well as to the efferent activity of alpha and gamma motoneurons. Clinically, this is manifested by pronounced relaxation of the injected muscles and a significant reduction in pain in them. Along with the process of denervation in these muscles, the process of reinnervation proceeds by the appearance of lateral processes of nerve endings, which leads to the restoration of muscle contractions 4-6 months after injection.
Pharmacokinetics
The pharmacological effect develops at the injection site. Presynaptic seizure and retrograde axonal transport from the site of introduction is negligible.
The duration of the clinical effect is 4-6 months. Restoration of neuromuscular activity occurs due to the development of new axonal processes that form new functional active neuromuscular synapses, which ultimately leads to the restoration of muscle contractions.
When administered in therapeutic doses, Relatox® does not penetrate the hemato-encephalic barrier and does not cause significant systemic effects. Excreted by the kidneys in the form of non-toxic metabolites.
Antibodies to the complex of botulinum toxin type A with hemagglutinin are formed in 1-5% of patients after repeated injections. The formation of antibodies is promoted by the introduction of the drug in high doses and repeated injections in small doses at short intervals. In the case of formation of antibodies to botulinum toxin type A, the effect of the subsequent reaction can be reduced.
Indications
Treatment of blepharospasm, spasticity of the muscles of the upper limb after suffering ischemic stroke, correction of hyperkinetic facial folds (facial wrinkles) in adults.
Treatment of spasticity of the upper and lower extremities in children of 13-17 years old with cerebral palsy.
Composition
1 bottle of the drug Relatox® contains:
botulinum toxin type A complex with hemagglutinin - 50 U or 100 U;
gelatin - 6 mg;
maltose - 12 mg.
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Dosage and Administration
Before dilution of the drug, the central part of the vial of the vial is treated with ethyl alcohol. The drug is dissolved by introducing into the vial 1-8 ml of 0.9% sodium chloride solution for injection by puncturing the stopper with a sterile needle with a length of 23 or 25 mm. Do not open the vial and remove the stopper. The solution of the drug is a clear, colorless liquid.
The prepared injection solution is injected with an insulin syringe with a fixed needle with a diameter of 0.27-0.29 mm. The position of the patient with the introduction of the drug into the muscles of the face - sitting on a chair, the back of the head is fixed.
Adverse reactions
The frequency of adverse reactions is presented for each indication for the use of the drug based on the experience of clinical use. The frequency is specified according to the recommendations of the World Health Organization and includes the following categories: very often (> 1/10); often (> 1/100 and <1/10), infrequently (> 1/1000 to <1/100), rarely (> 1/10000 and <1/1000), very rarely (<1/10000, including some cases ).
In the treatment of blepharospasm and correction of hyperkinetic facial folds (facial wrinkles).
Violations at the injection site:
Often: pain at the injection site, irritation and swelling, induration, erythema, tightness of the skin, hyperemia at the injection site.
Infrequently: microhematomas, ecchymosis, point keratitis.
Very rarely: spilled hyperemia.
Common disorders:
Rarely: systemic reactions in the form of general weakness and short-term rise in body temperature to subfebrile numbers (up to 37.5 ° C).
Nervous system disorders:
Infrequently: asymmetry of corners of a mouth.
Rarely: headache, dizziness, drowsiness.
Very rarely: difficulty of closing the eyelids, lagophthalmos, paresis of the facial muscles, paralysis of the facial muscles, impaired articulation, lip numbness.
Violation of the organ of vision:
Very rarely: disturbance of accommodation, dry eyes, photophobia and increased tearing.
Disruption of the digestive system:
Seldom: nausea.
Disorders of the musculoskeletal and connective tissues:
Very rarely: omission of the eyebrow, lateral areas of the eyebrows, ptosis.
In the treatment of spasticity of the muscles of the upper limb after ischemic stroke.
Violations at the injection site:
Very often: pain, swelling, irritation of the skin at the injection site.
Infrequently: hemorrhage in the place of an injection.
Violations of the skin and subcutaneous fat:
Infrequently: pruritus.
Disorders of the musculoskeletal and connective tissues:
Often: muscle weakness.
Infrequently: arthralgia, pain in limbs.
Nervous system disorders:
Often: headache, dizziness.
Infrequently: hypesthesia, paresthesia.
Rarely: poor coordination.
Disruption of the digestive system:
Seldom: nausea.
Mental Disorders:
Often: insomnia.
If the procedure is unqualified, needle injuries to vital structures (nerves, vessels) are possible.
In the treatment of spasticity of the muscles of the upper and lower extremities with cerebral palsy.
Common disorders:
Rarely: hyperthermia to 37.1 ° C.
Violations at the injection site:
Very often: pain, irritation of the skin at the injection site.
Infrequently: puffiness, hemorrhage in the place of an injection.
Violations of the skin and subcutaneous fat:
Infrequently: pruritus.
Disorders of the musculoskeletal and connective tissues:
Often: muscle weakness.
Infrequently: arthralgia, pain in the limbs.
Nervous system disorders:
Often: headache.
Infrequently: hypostezia, paresthesia.
Rarely: poor coordination, dizziness.
Violations by the organ of vision:
Rarely: ophthalmoplegic syndrome.
Violations of the cardiovascular system:
Seldom: orthostatic hypotension.
Disruption of the digestive system:
Seldom: nausea.
Mental Disorders:
Rarely: insomnia, depression.
If the procedure is unqualified, needle injuries to vital structures (nerves, vessels) are possible.
Contraindications
- Age up to 13 years;
- inflammatory process at the site of the intended injection;
- acute phase of infectious diseases;
- pronounced gravitational ptosis of facial tissues;
- pronounced hernia in the upper and lower eyelids;
- a period of less than 3 months after surgery on the face;
- hypersensitivity to the drug.
Drug interactions
The effect of the drug is enhanced with the simultaneous use of antibiotics of the aminoglycoside group, erythromycin, tetracycline, polymyxins, and neuromuscular transmission agents (including non-depolarizing muscle relaxants).
Pregnancy and Lactation
Contraindicated in pregnancy and lactation.
Special instructions
It should be used with extreme caution and under constant control in patients with subclinical or clinical signs of impaired neuromuscular transmission, for example, with myasthenia gravis or myasthenoid-like syndromes (including Lambert-Eaton syndrome), as well as in patients with corneal pathological changes, ecchymosis ( in the area of drug administration). Patients with neuromuscular diseases may be at risk for the occurrence of clinically significant systemic effects, including severe dysphagia and respiratory failure, with the usual doses of Relatox®. The treatment of such patients should be carried out with caution.
With a high degree of myopia, angle-closure glaucoma, administration of the drug is determined by the results of the conclusion of an ophthalmologist. Rare blinking associated with the introduction of botulinum toxin into the circular muscle of the eye, can lead to the occurrence of pathological changes in the cornea and requires further observation by a specialist.
When allergic history, especially hypersensitivity to drugs containing proteins, should take into account the risk of an allergic reaction in assessing the potential benefits of treatment.
It is necessary to enter the drug with caution in the immediate vicinity of the lungs, especially their tops.
When conducting injections of the drug into the muscles of the hand, special care must be taken and be guided by the principle of minimum doses, since possible development of weakness in the injected muscles and, as a result, a pronounced impairment of the manipulative function of the hand.
Overdosage
Patients with symptoms of botulinum toxin A poisoning (general weakness, ptosis, diplopia, difficulty swallowing and speech disorder, paresis of the respiratory muscles) should be hospitalized.
In case of paralysis of the respiratory muscles, it is necessary to carry out intubation and transfer to artificial ventilation of the lungs to improve the patient's condition.
- Brand name: Relatox
- Active ingredient: Botulinum toxin type A-hemagglutinin complex
- Dosage form: Lyophilisate for preparation of solution for intramuscular administration
- Manufacturer: Evalar
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