Pharmacological action Xeomin Injections
Muscle relaxant. Inhibitor of acetylcholine release. Xeomin acts selectively on peripheral cholinergic nerve endings by inhibiting the release of acetylcholine. The introduction of the cholinergic nerve endings occurs in 3 stages: the binding of a molecule with the external components of the membrane, the internalization of the toxin by endocytosis and translocation domain of toxin endopeptidaznogo from endosomes to the cytosol. In the cytosol endopeptidazny domain toxin molecule selectively cleaves SNAP-25, a major protein component of the mechanism that controls membrane traffic ekzovezikul, stopping, thus, release of acetylcholine. The net effect is a relaxation of the injected muscle.
Effect of the drug begins, on average, within 4-7 days after injection. The effect of each treatment lasts usually 3-4 months, although it may last significantly longer or less.
Pharmacokinetics Xeomin Injections
Data on the pharmacokinetics Xeomin not available.
Indications for use of the drug Xeomin Injections
- Blepharospasm;
- Idiopathic cervical dystonia (spasmodic torticollis), predominantly rotational form.
Dosage regimen Xeomin Injections
The drug can be entered only doctors who have specialized training and experience in the treatment of botulinum toxin and the equipment for electromyography. The dosage and number of injections into a muscle doctor sets for each patient individually.
Winking spasm
After dissolution, sterile needle is introduced Xeomin № 27-30 G. Recommended initial dose – 1.25-2.5 IU (0.05-0.1 ml) into each injection site. The drug is injected into the medial and lateral side of the circular muscles of the eye (m. orbicularis oculi) and the upper eyelid in the lateral part of the circular muscles of the eyes of the lower eyelid.
If the vision is impaired because of spasms in the forehead, in the lateral parts of the circular muscles of the eyes and upper face in these areas can be made more injections. Effect of the drug begins, on average, within 4 days after injection. The effect of each procedure is stored, usually 3-4 months, although it may last significantly longer or less.
If the effect of the initial dose was insufficient (less than 2 months), repeated procedures, the dose can be increased by 2 times. The initial dose should not exceed 25 units in one eye. At every place should not be given doses higher than the treatment of blepharospasm 5 total dosage of 12 weeks of treatment should not exceed 100
Spastic torticollis
In the treatment of spastic torticollis dosage should be titrated individually, depending on the position of head and neck, location of pain, muscle size (hypertrophy, atrophy), body weight, and its response to therapies. In practice, the maximum dose of the drug during a procedure generally should not exceed 200 units, but the dosage can be up to 300 at the same place should not be given a dose greater than 50
Spastic torticollis therapy involves injections of sternocleidomastoid muscle, the muscle, levator scapulae, scalene muscle in, the belt muscle, and / or a trapezoidal muscle (muscle).
Should not be injected into both sternocleidomastoid muscles, since it increases the risk of adverse effects of the drug (eg, dysphagia), which occur in the bilateral injection into the muscle, or at doses greater than 100 for injection into the superficial muscles use needle number 25, 27 and 30 G, and for the deep muscles – the needle number 22 G.
With spastic torticollis to determine the involved muscles may be necessary electromyography. Injection in multiple locations enables the drug evenly cover the areas of the muscles affected by dystonia (especially when injected in large muscles). The optimal number of sites of injections depends on the muscle. Effect of the drug begins, on average, within 7 days after injection. The effect of each procedure is stored about 3-4 months but can last much longer or less. The interval between treatments must be at least 10 weeks.
The dissolution of the drug
At a dilution of the drug may not open a bottle, removing the cork.
With the bottle removed the protective plastic cover. Immediately prior to breeding vial central part of the tube should be treated with alcohol.
Solution for injection is prepared by puncturing the stopper with a sterile needle into the vial and introducing sterile 0.9% sodium chloride. Carefully turn the vial, mixing the lyophilized with a solvent to dissolve completely. After the dissolution of formed clear, colorless solution.
The drug is not used if, after the dissolution of the resulting solution is opaque and flakes and contains visible particles. The drug is dissolved in the required amount, according to the table.
| volume of solvent (ml) | ED/0.1 ml |
| 0.5 | 20 |
| 1 | 10 |
| 2 | 5 |
| 4 | 2.5 |
| 8 | 1.25 |
The dosages are recommended for Xeomin can not be used to convert the use of other drugs that contain botulinum toxin.
Since the product does not contain antimicrobial agents recommended for use immediately after reconstitution. If necessary, the dissolved drug can be stored in the original bottle to 24 hours in a refrigerator at 2 ° to 8 ° C provided that dissolution was carried out under aseptic conditions.
Side effect Xeomin Injections
Winking spasm
Common: ptosis (6.1%), dry eyes (2%).
Uncommon: paraesthesia, conjunctivitis, dry mouth, skin rash, headache, muscular weakness.
In addition, when using a similar formulation containing botulinum toxin type A, and is used in clinical trials along with drug Xeomin, noted the following side effects. They are possible when using the drug Xeomin.
Common: superficial keratitis, lagophthalmos, irritation, photophobia, lacrimation.
Uncommon: Keratitis, ectropion, diplopia, dizziness, diffuse skin rash, dermatitis, entropion century, focal facial paralysis, weakness, facial muscles, fatigue, visual disturbances, blurred vision.
Rare: local swelling of eyelid skin.
Very rare: acute angle-closure glaucoma, corneal ulceration.
Spastic torticollis
Common: dysphagia (10%), muscle weakness (1.7%), back pain (1.3%).
Uncommon: Inflammation or pressing sensation at the injection site, headache, asthenia, sweating, tremors, hoarseness, colitis, vomiting, diarrhea, dry mouth, pain in bones, joints, skin rash, itching, peeling skin, eye pain .
In addition, when using a similar formulation containing botulinum toxin type A, and is used in clinical trials along with drug Xeomin, noted the following side effects. They are possible when using the drug Xeomin.
Very common: pain.
Common: dizziness, high blood pressure, numbness, weakness, cold symptoms, malaise, dry mouth, nausea, headache, stiff muscles, irritation at the injection site, rhinitis, infections of upper respiratory tract.
Uncommon: dyspnea, diplopia, fever, ptosis, speech disorders.
Dysphagia is usually of varying severity (from mild to very severe, with the possibility of aspiration), and in rare cases it requires medical attention. Dysphagia may persist for 2-3 weeks after injection, however, recorded a three-month case of dysphagia. Dysphagia develops a dose-dependent. According to clinical studies, dysphagia is rare if the total dose does not exceed 200 units per procedure.
Common side effects
The following information is based on data on the effects of other complex products containing botulinum toxin type A. For information about serious adverse reactions that may be associated with damage to the cardiovascular system (such as arrhythmia and myocardial infarction, including those with fatal outcome) is extremely small. Were these deaths caused by injections of botulinum toxin type A, or concomitant cardiovascular disease, not determined. We report one case of anaphylactic shock after administration of a complex preparation containing botulinum toxin type A.
There have side effects such as exudative erythema multiforme, urticaria, psoriasiform rash, itching, and allergic reactions, but they are conditioned by a complex preparation containing botulinum toxin type A has not been confirmed. Sometimes after an injection of botulinum toxin type A were observed oscillations of the electrophysiological background in some distant muscles, this side effect is not associated with muscle weakness or other electrophysiological abnormalities.
Contraindications to the use of the drug Xeomin Injections
- Violations of neuromuscular transmission (myastenia gravis, Lambert-Eaton syndrome);
- Fever;
- Acute infectious and communicable diseases;
- Pregnancy
- Lactation (breastfeeding);
- Age 18 years;
- Hypersensitivity to the drug.
Be wary prescribers with amyotrophic lateral sclerosis, and neurological diseases as a result of motor neuron degeneration and other diseases with impaired neuromuscular transmission.
Use of the drug Xeomin Injections in pregnancy and breastfeeding
The drug is contraindicated during pregnancy and lactation.
Cautions
Immediately after the injection of the remaining solution in the vial or syringe should be inactivated in a solution of sodium hydroxide (0.1 N NaOH). All support materials were in contact with the drug should be autoclaved, or inactivated at least 18 hours a solution of sodium hydroxide (0.1 N NaOH). Spilled product should be wiped with a napkin absorbent soaked in a solution of sodium hydroxide.
Effects on ability to drive and control mechanisms
Because of the nature of diseases treatable drug, the patient’s ability to manage various techniques can be reduced. In addition, drug side effects can negatively affect a patient’s ability to manage technology, respectively, the patient should refrain from such activities as long as his abilities are not restored in full.
Overdose Xeomin Injections
In applying Xeomin in high doses may develop pronounced muscle paralysis in places remote from the injection site (generalized weakness, ptosis, diplopia, swallowing and speech difficulties, and paralysis of respiratory muscles, leading to the development of aspiration pneumonia).
Treatment: If overdose requiring hospitalization with general supportive measures. When paralysis of respiratory muscles is required intubation and mechanical ventilation until the normalization of the state.
Drug Interactions Xeomin Injections
The simultaneous use of aminoglycosides or spectinomycin is not recommended.
Muscle peripheral actions should be used with caution.
The effect of the drug can be reduced by the simultaneous action of derivatives of 4-aminoquinoline.
