Xeomin lyophilisate 100ED 1 pc.

Kseomin acts selectively on the peripheral cholinergic nerve endings to inhibit the release of acetylcholine.

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

In cytosol endopeptidase domain of toxin molecules selectively cleaves SNAP-25, an important protein components of the mechanism that controls the movement of exo-membrane vesicles stopping thus release of acetylcholine. The net effect is a relaxation of the injected muscles.

Effect of the drug begins within four to seven days after the injection. The effect of each treatment generally lasts three to four months, although it may last significantly longer or less.

Active substance:
Botulinum toxin type A

Manufacturer

Merz Pharma GmbH & Ko.KGaA, Germany

Composition

1 vial contains:

active ingredient:

Botulinum toxin type A 100 IU,

sucrose, 4.7 mg,

Human serum albumin 1.0 mg.

Indications

Blepharospasm, idiopathic cervical dystonia (spasmodic torticollis) preferably forms a rotating, arms spasticity following stroke, hyperkinetic wrinkles (wrinkles) of the person.

Contraindications

The drug is contraindicated for people with allergies to components of the drug, disorders of neuromuscular transmission (masteniya gravis, Lambert-Eaton syndrome, prescribed with caution in amyotrophic lateral sclerosis, neurological diseases resulting from degeneration of motor neurons and other diseases with impaired neuromuscular transmission) .

The drug is not administered at an elevated temperature and acute infectious or non-infectious diseases.

The drug is contraindicated during pregnancy and lactation.

The drug is not administered to children and adolescents under 18 years of age.

Side effects

Adverse reactions are classified according to frequency of occurrence: very often (≥ 1/10), often (≥1 / 100 to < 1/10), is not often (≥ 1 / 1,000 to ≤ 1/100), rare (≥1 / 10.000 to ≤ 1 / 1,000), very rarely (≤ 1 / 10,000).

Blepharospasm:
Common: ptosis (6.1%), dry eye (2,0%)
.
Uncommon: paresthesia, conjunctivitis, dry mouth, skin rash, headache, muscle weakness
.

Furthermore, by using a similar formulation containing botulinum toxin Type A, and is used in clinical trials along with Kseominom, the following were observed side effects. They are possible when using Kseomina.

Common: superficial keratitis, lagophthalmos, skin irritation, photophobia, lacrimation.

Uncommon: keratitis, ectropion, diplopia, dizziness, diffuse skin rash / dermatitis, entropion century, focal facial paralysis, weakness of facial muscles, fatigue, visual disturbances, blurred vision
.
Rarely. Local swelling of the skin century

Very rare: acute angle-closure glaucoma, corneal ulceration.

Spasmodic torticollis:

Common: dysphagia (10%), muscle weakness (1.7%), back pain (1.3%). Uncommon: inflammation or pressing sensation at the injection site, headache, asthenia, generalized sweating, tremor, hoarseness, colitis, vomiting, diarrhea, dry mouth, bone pain, myalgia, skin rash, itching, peeling of the skin, pain eyes.

Furthermore, by using a similar formulation containing botulinum toxin Type A, and is used in clinical trials along with Kseominom, the following were observed side effects. They are possible when using Kseomina.
Very often:. Pain at the injection site

Common: dizziness, high blood pressure, numbness at the injection site, fatigue, flu-like symptoms, malaise, dry mouth, nausea, headache, stiff muscles at the injection site irritation at the injection site, rhinitis, upper respiratory tract infection.

Uncommon: dyspnea, diplopia, fever, ptosis, speech disorders.

The severity of dysphagia vary from mild to severe, with the possibility of aspiration; in rare cases, it requires medical attention. Dysphagia may persist for two to three weeks after injection, but recorded case of 3 months duration. Dysphagia develops dose-dependent manner; According to clinical studies, dysphagia is rare if the total dose does not exceed 200 units per procedure.

Spasticity hands after stroke:
Common: headache, sensitivity disorder, feeling of heat
.
Furthermore, by using a similar formulation containing botulinum toxin Type A, and is used in clinical trials along with Kseominom, the following were observed side effects. They are possible when using Kseomina.
Often: hypertonicity, ecchymosis, local pain, muscle weakness, or irritation at the injection site hemorrhage
.
Uncommon: depression, sleep disturbances, paresthesia, incoordination, amnesia, vertigo, orthostatic hypotension, nausea, dermatitis, pruritus, rash, arthralgia, bursitis, fatigue, pain, and hypersensitivity at the injection site, anxiety, peripheral edema
.

Some side effects may be associated with a major illness.

Hyperkinetic wrinkles (wrinkles) of the person:

Usually, undesirable effects are observed in the first week after treatment and are temporary. Undesirable effects may be associated with the active substance and / or the introduction procedure.

Expected pharmacological effect of Botulinum toxin is localized muscle weakness. Ptosis eyelid may be caused by injection technique and is associated with the pharmacological action of the drug.

As with any injection, in connection with it is possible local appearance pain, tenderness, itching, swelling and / or bruising; also may develop transient vaso-vagal reactions such as syncope, circulatory disorders, nausea or tinnitus associated with anxiety before injection.

In applying the drug reported the following adverse reactions:

Common: pruritus, headache, muscle function disorders at the injection site, feeling of heaviness
.
Uncommon: flu-like symptoms, a sense of tension at the injection site, bronchitis, nasopharyngitis, feeling “nodules in the skin”, swelling of the eyelids, ptosis, blurred vision, raising his eyebrows, nausea, muscle twitching and spasms, local facial weakness
.
In addition, for comparison, a formulation containing a conventional complex of botulinum toxin type A and is used in several clinical trials (collected to date data suggest the same activity of both drugs) known development of the following adverse effects which are likely to be observed when using Kseomina.

Uncommon: infection, paresthesia, dizziness, blepharitis, eye pain, dry mouth, sensitivity to light, dry skin.

Common side effects:

The following information is based on data on the effects of other medicines containing botulinum toxin type A.

Information about serious adverse effects that may be associated with damage to the cardiovascular system – such as arrhythmia and myocardial infarction, including fatal ones – are extremely rare.

Were these deaths are caused by injection of botulinum toxin type A or concomitant cardiovascular diseases is not clearly determined. One case of anaphylactic shock after administration of a formulation containing botulinum toxin type A.

There have side effects such as poliformnaya exudative erythema, urticaria, psoriasiform rashes, itching and allergic reactions, however, their conditioning action integrated formulation containing botulinum toxin type A is not confirmed.

Sometimes after injections of botulinum toxin type A background electrophysiological changes observed in some remote muscles; this side effect is not associated with muscle weakness or other electrophysiological abnormalities.

How to accept, acceptance rate and dosage

V / m. The drug may be administered only doctors having special training and experience of treatment with botulinum toxin and equipment for electromyography. The dosage and number of injections into the muscle the doctor places set individually for each patient.

Blepharospasm: administered after dissolution Kseomin sterile needle 27-30 G.

The recommended initial dose – 1.25-2.5 U (0.05-0.1 ml) into each injection site; formulation is injected into the medial and lateral parts of the circular muscles of the eyes (m. orbicularis oculi) of the upper eyelid and the lateral portion of the circular muscles of the lower eyelid.

If the vision impaired due to spasms in the forehead, the lateral sections of the circular muscles of the eye and the upper part of the face, in the area of ​​additional injections can be made. Effect of the drug begins, on average, within 4 days after the injection. The effect of each treatment generally lasts 3-4 months, although it may last significantly longer or less.

If the effect of the initial dose was insufficient (duration < 2 months), repeated procedures dose can be increased by 2 times. The initial dose should not exceed 25 U per 1 eye. In each place should not be administered a dose greater than 5 units. In the treatment of blepharospasm total dosage of 12 weeks of treatment should not exceed 100 units.

Spasmodic torticollis: in the treatment of spasmodic torticollis dosage should be titrated for each patient individually, depending on the position of the neck and head, location of pain, muscle size (hypertrophy, atrophy), body weight and response to therapies. In practice, the maximum dose treatment during one treatment should normally not exceed 200 units, but can be up to 300 dosage units. At one and the same spot should not be injected dose exceeding 50 IU.

Therapy spasmodic torticollis includes injection sternocleidomastoid muscle, a levator scapulae muscle; in the scalene muscles in the arm belt and / or the trapezius muscle.

You should not give injections into both sternocleidomastoid muscle because it increases the risk of adverse drug effects (in particular dysphagia), which occur in the preparation of bilateral injections into the muscle, or at doses exceeding 100 units.

For injection into the muscle using a needle surface numbers 25, 27, and 30 G, and for the deep muscles – the needle number 22 G.

When spasmodic torticollis to determine the muscles involved may be necessary electromyography. The injection of a few places allows drug evenly cover the areas of the muscles prone dystonia (especially when injected into large muscles). The optimum amount of injection sites depends on the muscles. Effect of the drug begins, on average, within 7 days after injection. The effect of each treatment lasts about 3-4 months, but can last much longer or less. The interval between treatments should be at least 10 weeks.

Dissolution of the drug: the dilution of the drug may not open a bottle by removing the plug.

With the bottle removed the protective plastic cover. Immediately before dilution vial contents central part of the stopper to be treated with alcohol.

A solution for injection is prepared by piercing the stopper with a sterile needle into the vial and introducing a sterile isotonic sodium chloride solution for injection, 0.9%. Gently rotate the vial, mixing with a solvent to completely dissolve the lyophilisate.

The drug is not in use, if after dissolution the resulting solution is opaque, or contain visible particles and flakes. It should be clear and colorless.

The drug is dissolved in the required amount in the table.

The dosages recommended for Kseomina can not be used for translation with other formulations containing botulinum toxin.

Because the drug does not contain antimicrobial agents, it is recommended to use it directly after the dissolution. If necessary, the dissolved drug can be stored in original vial to 24 hours in a refrigerator at 2 to 8 ° C, provided that the dissolution was conducted under aseptic conditions.

Storage conditions

At temperatures above 25 ° C.

Keep out of the reach of children.

Active substance

Botulinum toxin type A

Interaction

Peripherally acting muscle relaxants should be used with caution while carrying antibiotic aminoglycosides or spectinomycin (possibly increasing Kseomina action).

The effect of the drug can be reduced by the action of 4-aminoquinoline.

Overdose

High doses Kseomina can lead to the development of pronounced muscle paralysis at locations remote from the injection areas (in particular: generalized weakness, ptosis, diplopia, slurred speech and swallowing, and respiratory muscle paralysis, which leads to the development of aspiration pneumonia).

In case of overdose, hospitalization with general supportive measures. Paralysis of respiratory muscles require intubation and mechanical ventilation until the normalization of the state.