Universal reference book for medicines
Product name: LANTOX (LANTOX)

Active substance: botulinum A toxin

Type: Muscle relaxant.
Inhibitor of acetylcholine release
Manufacturer: NIKE-MED (Russia) manufactured by Lanzhou Institute of Biological Products (China)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Miorelaxant.
The molecule of the active substance consists of heavy (with a molecular weight of 100,000 daltons) and a light chain (with a molecular weight of 50,000 daltons) connected by a disulfide bridge. The heavy chain has a high affinity for binding to specific receptors located on the surface of target neurons. The light chain has a Zn 2+ -dependent protease activity specific for the cytoplasmic regions of the synaptosomal-binding protein having a molecular weight of 25,000 daltons (SNAP-25) and participating in exocytosis processes. The first stage of the action of botulinum toxin type A is the specific binding of the molecule to the presynaptic membrane, this process takes 30 min. The second stage is the internalization of the bound toxin into the cytosol through endocytosis. After internalization, the light chain acts as a Zn 2+ -dependent cytosol protease, selectively cleaving SNAP-25, which in the third stage results in a blockade of the release of acetylcholine from the presynaptic terminals of the cholinergic neurons. The final effect of this process is persistent chemodenervation.
With the introduction of botulinum toxin type A, two effects develop: direct inhibition of extrafusal muscle fibers by inhibiting alpha-motoneurons at the level of the neuromuscular synapse and inhibiting the activity of muscle spindles by inhibiting the gamma motor neuron 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 1a-afferents. This leads to a decrease in the activity of muscle stretch receptors, as well as the efferent activity of alpha and gamma motor neurons. Clinical manifestations are marked relaxation of muscles at the injection site 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 terminals, which leads to the restoration of muscle contractions 4-6 months after injection.
When intradermal injection in the localization of exocrine sweat glands (armpits, palms, feet), blockade of postganglionic sympathetic nerves develops and hyperhidrosis stops for 6-8 months.

When administered locally in therapeutic doses, the active substance does not penetrate the BBB and does not cause significant systemic effects.
Apparently, there is minimal presynaptic seizure and reverse axonal transport from the site of its administration.
Antibodies to botulinum toxin type A are formed in 1-5% of patients after repeated injections.
The formation of antibodies is promoted by administration in high doses (more than 250 units), booster injections (in small doses at short intervals). In the case of antibodies to botulinum toxin type A, other serological types (B, F) are used.
PHARMACOKINETICS
The haemagglutinin complex of botulinum toxin type A is concentrated for some time at the site of its intramuscular injection before it enters the systemic circulation.In the future, the active substance is very rapidly metabolized with the formation of simpler molecular structures.

It is excreted as metabolites mainly by the kidneys.

INDICATIONS
Blepharospasm, hemifacial spasm, paralytic strabismus, spasmodic torticollis, local muscular spasm in adults and children over 2 years of age (including cerebral palsy and spasticity).

DOSING MODE
Doses and points for injection are determined individually for each patient in accordance with the nature, severity and localization of muscular hyperactivity.
In some cases, EMG control is used to more accurately localize injected muscles.
The average total dose when injected into the facial muscles is 25-100 ED, in the neck muscles - 100-200 units, in the muscles of the limbs - 50-300 ED.
The interval between repeated injections should be at least 2 months.
The maximum total dose for 1 procedure in adults is 400 units, for 1 procedure in children over 2 years old - 12 units / kg body weight (no more than 300 units).
The toxic dose is 38-42 U / kg body weight.
SIDE EFFECT
Local reactions: 2-5% of cases - microhematomas (up to 7 days), pain at the injection site (up to 1 day).

Systemic reactions: arise when used in a high dose (more than 200 units) - a slight general weakness within 1 week.

Reactions associated with spreading to muscle groups located near the site of injection depend on the area of ​​administration of botulinum toxin type A. In the treatment of blepharospasm, hemifacial spasm - ptosis (5-10%), lacrimation (0.5-1%);
rarely - ectropion, keratitis, diplopia, entropion, ecchymosis. When injected into both nipping muscles - dysphagia (2-5%). As a rule, these side effects do not require additional therapy and regress within 1 month after the injection.
CONTRAINDICATIONS
Myasthenia gravis, myasthenic and myasthenic-like syndromes (including Lambert-Eaton syndrome), inflammation at the injection site, pregnancy, lactation, hypersensitivity to botulinum toxin type A.

PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.

APPLICATION FOR CHILDREN
Do not recommend for use in children under 2 years of age.

SPECIAL INSTRUCTIONS
Injections of botulinum toxin type A should be carried out by a highly qualified doctor who has special training and permission from the manufacturer.

Complications after the injection are extremely rare and may occur when the needle traumatizes vital structures (nerves, vessels, trachea) in the case of unqualified procedure.
Complications in the form of anaphylaxis are not described, nevertheless, during the injection, it is necessary to have means for urgent relief of anaphylactic reactions.
At present, the effectiveness of botulinum toxin type A has been proven in patients with myofascial syndromes, tension headaches, contractures of facial muscles, trismus, bruxism, hyperkinetic face wrinkles, cardiac achalasia, spasm of the rectum and bladder spasm, local hyperhidrosis.

The specific botulinum antitoxin is effective within 30 minutes after the injection of botulinum toxin.

After the injection, the syringes and the needle should be destroyed using the methods provided for the destruction of biological waste.

Do not recommend for use in children under 2 years of age.

DRUG INTERACTION
The action of botulinum toxin type A is enhanced with the simultaneous use of antibiotics of the group of aminoglycosides, erythromycin, tetracycline, lincomycin, polymyxins, agents that reduce neuromuscular transmission (including curare-like muscle relaxants).

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