Lantox (Lyophilisate) Instructions for Use

ATC Code

M03AX01 (Botulinum toxin)

Active Substance

Botulinum toxin A

Botulinum toxin A (Ph.Eur. European Pharmacopoeia)

Clinical-Pharmacological Group

Muscle relaxant. Acetylcholine release inhibitor

Pharmacotherapeutic Group

MIBP

Pharmacological Action

It acts selectively on peripheral cholinergic nerve endings, inhibiting the release of acetylcholine.

The introduction into cholinergic nerve endings occurs in three stages: binding of the molecule to the external components of the membrane, internalization of the toxin by endocytosis, and translocation of the endopeptidase domain of the toxin from the endosome into the cytosol.

In the cytosol, the endopeptidase domain of the toxin molecule selectively cleaves SNAP-25, an important protein component of the mechanism controlling the membrane movement of exovesicles, thus stopping the release of acetylcholine. The final effect is relaxation of the injected muscle.

The action begins within 4-7 days after injection. The effect of each procedure usually lasts 3-4 months, although it may last significantly longer or shorter.

Indications

Adults: blepharospasm; idiopathic cervical dystonia (spasmodic torticollis) predominantly of the rotational form; spasticity of the upper limb after stroke; chronic sialorrhea; hyperkinetic facial folds (facial wrinkles).

Children aged 2 to 18 years: spastic equinus and equinovarus foot deformity in cerebral palsy; chronic sialorrhea.

ICD codes

Dosage Regimen

Reconstitute the lyophilisate strictly according to the manufacturer’s instructions using the provided diluent.

Administer via intramuscular or intraglandular injection only.

Perform treatment exclusively under the supervision of a qualified physician experienced in these procedures.

Determine the total dose, number of injection sites, and injection pattern individually for each patient based on the indication, muscle size, and severity of symptoms.

For blepharospasm, the initial recommended dose is 1.25-2.5 Units per site injected into the orbicularis oculi muscle.

For cervical dystonia, tailor the dose and injection sites to the individual muscle involvement; the mean dose is 200-300 Units per treatment session.

For upper limb spasticity post-stroke, the recommended total dose ranges from 75 Units to 400 Units, divided among the affected muscles.

For chronic sialorrhea in adults, inject a total of 75-100 Units divided between the parotid and submandibular glands.

For hyperkinetic facial folds, use low doses precisely injected into the specific facial muscles responsible for wrinkle formation.

In pediatric patients with cerebral palsy for spastic equinus foot deformity, the total dose is 4 Units/kg per affected limb, not to exceed 200 Units per limb.

For chronic sialorrhea in children, the recommended total dose is 30-50 Units for children 15-18 kg, and 60-100 Units for children over 18 kg, divided between the parotid and submandibular glands.

Avoid injections near the levator palpebrae superioris to reduce the risk of ptosis.

Exercise extreme caution when injecting in proximity to the carotid arteries, lung apices, and esophagus.

The minimum interval between treatment sessions must be three months or longer.

Do not exceed the maximum recommended total dose for a single session.

Use electromyographic guidance or similar techniques for deep or small muscles to ensure precise placement.

Adverse Reactions

The nature of adverse reactions depends on the dose and the area of administration of the drug.

From the immune system very rarely – immediate and delayed type allergic reactions.

From the nervous system very common – brow ptosis; common – headache, dizziness, head discomfort; uncommon – hypesthesia, paresthesia, asymmetry of the corners of the mouth; rare – dizziness, drowsiness, impaired coordination; very rare – difficulty closing eyelids, lagophthalmos, paresis of facial muscles, paralysis of facial muscles, impaired articulation, lip numbness; possibly – brachial plexus plexopathy, dysphonia, dysarthria, facial paresis, muscle weakness, myasthenia gravis, peripheral neuropathy, convulsions, fainting and facial paralysis. The listed reactions may occur depending on the area of administration.

Psychiatric disorders common – feeling of tension, insomnia; rare – depression.

From the organ of vision very common – eyelid edema; rare – ophthalmoplegic syndrome; very rare – accommodation disorder, dry eyes, photophobia and increased lacrimation.

From the digestive system common – dysphagia; rare – nausea; possibly – abdominal pain, diarrhea, constipation, dry mouth, vomiting.

From the musculoskeletal system and connective tissue common – muscle weakness; uncommon – arthralgia, limb pain, neck pain; very rare – drooping of the interbrow area, lateral parts of the eyebrows, ptosis.

From the skin and subcutaneous tissue common – compensatory sweating; uncommon – skin itching; possibly – alopecia, psoriasiform dermatitis, erythema multiforme, hyperhidrosis, madarosis, itching and rash.

From metabolism possibly – anorexia.

From the respiratory system possibly – aspiration pneumonia (in some cases with fatal outcome), dyspnea, bronchospasm, respiratory depression and respiratory failure.

General disorders common – flu-like syndrome; rare – short-term increase in body temperature to subfebrile values (up to 37.5°C (99.5°F)).

Local reactions: common – pain at the injection site, irritation and swelling, induration, erythema, skin tightness, hyperemia at the injection site; uncommon – microhematomas, ecchymoses, punctate keratitis; very rare – diffuse hyperemia.

Contraindications

Hypersensitivity to the active substance; neuromuscular transmission disorders (myasthenia gravis, Lambert-Eaton syndrome); presence of infection and inflammatory process at the injection sites; children under 2 years of age (for indications: spastic equinus and equinovarus foot deformity in cerebral palsy in children; chronic sialorrhea in children), under 18 years of age for other indications (efficacy and safety of use have not been established).

With caution

Blood clotting disorders; if the patient is receiving anticoagulant therapy or taking other substances in anticoagulant doses; in patients with amyotrophic lateral sclerosis; in patients with other diseases that lead to peripheral neuromuscular dysfunction; in patients with severe muscle weakness or atrophy of the target muscles.

Use in Pregnancy and Lactation

During pregnancy, use only in case of extreme necessity, if the potential benefit outweighs the risk.
Use during breastfeeding is not recommended.

Pediatric Use

Contraindicated in children under 2 years of age.

In children over 2 years of age, use with caution, strictly according to indications and in accordance with the recommended dosage regimen.

Geriatric Use

Use with caution in elderly patients with a burdened history and concomitant drug therapy.

Special Precautions

Patients with neuromuscular disorders may be at increased risk of developing significant muscle weakness, especially with intramuscular injection.

Drugs containing botulinum toxin should be used in such patients under special supervision and only when the expected benefit of treatment outweighs the risk.

Treatment should be carried out with caution in patients with a history of dysphagia and aspiration. Therapy for cervical dystonia in such patients should be carried out with extreme caution. The use of botulinum toxin type A for aesthetic purposes in such patients is not recommended.

Extreme caution should be exercised when treating pediatric patients with a severe degree of neurological asthenia, dysphagia, or those who have recently had aspiration pneumonia or lung disease. Treatment of such patients should be carried out only if the potential benefit for the specific patient outweighs the risk.

In case of swallowing, speech and breathing disorders, seek medical help immediately.

When treating spasmodic torticollis, spasticity of the upper limb after stroke in adults and spastic equinus and equinovarus foot deformity in cerebral palsy in children, the drug should be carefully injected into areas in close proximity to the carotid arteries, lung apices and esophagus.

Due to the presence of an anticholinergic effect, use with caution in patients at risk of developing angle-closure glaucoma.

Patients should be informed that injections of this agent for the treatment of spasmodic torticollis may cause moderate to severe dysphagia with a risk of aspiration and breathing difficulties.

To reduce the risk of eyelid ptosis, injections near the levator palpebrae superioris muscle should be avoided. Diffusion of botulinum toxin type A into the inferior oblique muscle of the eye may lead to diplopia. Avoiding injections into the medial part of the lower eyelid can reduce the number of such adverse reactions. A reduction in the number of blinks after injection of a drug containing botulinum toxin into the orbicularis oculi muscle may lead to exposure of the cornea, persistent epithelial defect and corneal ulceration.

Spontaneous reports of possible spread of the toxin to points remote from the injection sites when using botulinum toxin type A drugs in children with comorbidities, mainly cerebral palsy, have been very rare. As a rule, the dose used in these cases exceeded the recommended one for these drugs.

There are rare spontaneous reports of fatal cases, sometimes associated with aspiration pneumonia in children with severe cerebral palsy after treatment with botulinum toxin drugs, including for unregistered indications (for example, when injected into the neck area).

Effect on ability to drive vehicles and mechanisms

Due to the nature of the diseases treated with botulinum toxin type A, the patient’s ability to operate machinery may be reduced. In addition, side effects such as fatigue, muscle weakness, blurred vision, tiredness, dizziness and upper eyelid ptosis may occur and negatively affect the patient’s ability to operate machinery or perform other potentially hazardous activities. Therefore, the patient should refrain from such activities until his abilities are fully restored.

Drug Interactions

Peripheral muscle relaxants should be used with caution during simultaneous antibiotic therapy with aminoglycosides or spectinomycins (the effect of botulinum toxin type A may be enhanced).

When used concomitantly with 4-aminoquinoline derivatives, the effect of botulinum toxin type A may be reduced.

Storage Conditions

Store at from -5 to -18 °C. Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.