Xeomin - instructions for use, dose, side effects, contraindications

Active substanceBotulinum neurotoxin type ABotulinum neurotoxin type A

Similar drugsTo uncover

Xeomin

lyophilizate w / m

Merz Pharma GmbH & Co. KG. KGaA Germany

Lantox

lyophilizate for injections

NIKE-MED, LLC Russia

Dosage form: & nbsp

lyophilizate for the preparation of a solution for intramuscular injection

Composition:

on 1 bottle:

botulinum toxin type A 50 ED or 100 ED, sucrose 4.7 mg, human serum albumin 1.0 mg.

Description:

Lyophilizate from white to almost white.

Pharmacotherapeutic group:muscle relaxant of peripheral action

ATX: & nbsp

M.03.A.X.01 Botulinum toxin

Pharmacodynamics:

Xeomin is a botulinum toxin produced by a bacterium strain Clostridium botulinum type A, freed from complexing proteins.

Xeoming acts selectively to the peripheral cholinergic nerve endings, inhibiting the release of acetylcholine. The introduction into the cholinergic nerve endings occurs in three stages: the binding of the molecule to the outer components of the membrane, the internalization of the toxin by endocytosis, and the translocation of the endopeptidase domain of the toxin from the endosome to the cytosol. In the cytosol, the endopeptidase domain of the toxin molecule selectively cleaves SNAP-25, an important protein component of the mechanism that controls the membrane movement of the exoesicles, thus stopping the release of acetylcholine. The final effect is relaxation of the injected muscle.

The drug begins within four to seven days after the injection. The effect of each procedure lasts, as a rule, three to four months, although it can last substantially longer or less.

Indications:

Blepharospasm, idiopathic cervical dystonia (spasmodic torticollis) predominantly of the rotational form, spasticity of the hand after a stroke, hyperkinetic folds (facial wrinkles) of the face.

Contraindications:The drug is contraindicated in people with allergies to the components of the drug, with violations of the neuromuscular transmission (gravis mastitis, Lambert-Eaton syndrome.

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

The drug is contraindicated in pregnancy and lactation.

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

Carefully:Precautions are prescribed for amyotrophic lateral sclerosis, neurological diseases as a result of degeneration of motor neurons and other diseases with neuromuscular transmission disorders).

Dosing and Administration:

The drug can be administered only by physicians with special training, as well as experience in handling botulinum toxin and with equipment for electromyography.Dosage and the number of injection sites in the muscle the doctor sets for each patient individually.

Dissolution of the preparation:

When diluting the drug, it is forbidden to open the bottle, removing the stopper.

Remove the protective plastic cover from the vial. Immediately before diluting the contents of the vial, the central part of the plug is treated with alcohol.

The solution for injection is prepared by piercing the plug with a sterile needle and injecting into the bottle a solution of sodium chloride isotonic 0.9% for injections. Caution turn the vial, stirring the lyophilizate with the solvent until complete dissolution. The dissolution time is not more than 10 seconds. After dissolution, a clear, colorless solution should be formed.

The preparation is not used if, after dissolution, the resulting solution is opaque or contains visible flakes and particles.

The preparation is dissolved in the required volume, according to the table:

Scope solvent per vial containing 100 U (ml)

The volume of solvent per bottle, containing 50 U (ml)

ED / 0.1 ml

0,5

1,0

2,0

2,5

4,0

8,0

0,25

0,5

1,0

1,25

2,0

4,0

2,5

1,25

Dosages recommended for Xeomin can not be used for recalculation when using other preparations containing botulinum toxin.

Since the drug does not contain antimicrobial agents, it is recommended to use it immediately after dissolution. If necessary, the dissolved preparation can be stored in the original vial for up to 24 hours in the refrigerator at a temperature of 2 to 8 ° C, provided that the dissolution was carried out under aseptic conditions.

Blepharospasm

After dissolution, Xeomin is administered with a sterile 27-30 needle G. The recommended initial dose is 1.25-2.5 units (0.05-0.1 mL) at each injection site; the drug is injected into the medial and lateral parts of the circular eye muscle (m. orbicularis oculi) of the upper eyelid, and in the lateral part of the circular muscle of the eye of the lower eyelid.

If vision is impaired due to spasms in the forehead, in lateral areas of the circular eye muscle and in the upper part of the face, additional injections can be made to these areas. The effect of the drug begins, on average, for four days after the injection. The effect of each procedure lasts, as a rule, three to four months, although it can last substantially longer or less.

If the effect of the initial dose was insufficient (duration less than two months), with repeated procedures, the dose of the drug can be doubled. The initial dose should not exceed 25 units per eye.Each dose should not be administered in a dose exceeding 5.0 units. In the treatment of blepharospasm, the total dosage for twelve weeks of treatment should not exceed 100 units.

Spasmodic torticollis

When treating spasmodic torticollis, the dosage should be selected for each patient individually, depending on the position of the neck and head, the localization of pain, muscle volume (hypertrophy, atrophy), the body weight of the patient.

In the practice of treatment, the maximum dose of the drug in a single procedure usually should not exceed 200 units, but a dosage of up to 300 units is possible. In the same place should not be administered a dose of the drug, exceeding 50 units.

Spastic torticollis therapy involves injections into the sternocleidomastoid muscle, into the muscle that lifts the scapula, into the stair muscles, into the belt muscle, and / or into the trapezius muscle (muscles).

Do not inject into both the sternocleidomastoid muscles, as this increases the risk of adverse drug effects (in particular, dysphagia) that occur with bilateral injections of the drug into this muscle, or at doses exceeding 100 units.

For injections, the needles of numbers 25, 27 and 30 are used in the superficial muscles G, and for the deep muscles - needle number 22 G.

With a spastic curve, electromyography may be necessary to determine the involved muscles. Carrying out injections in several places allows the drug to evenly cover the areas of muscles prone to dystonia (especially when injected into large muscles). Optimal the number of injection sites depends on the size of the muscle. The effect of the drug begins, on average, within seven days after the injection. The effect of each procedure lasts about three to four months, but it can last substantially longer or less. The interval between the procedures should be at least ten weeks.

Spasticity of the hand after a stroke

The drug is administered using suitable sterile needles (for example, for the superficial muscles, needles 26 G diameter 0.45 mm long 37 mm, for the deep-seated muscles use needles 22 G diameter 0.7 mm long 75 mm).

Electromyography may be necessary to determine the involved muscles. Carrying out injections in several places allows the drug to evenly cover the areas of muscles prone to dystonia (especially when injected into large muscles).

In the treatment of spasticity, dosage should be selected for each patient individually, depending on the size, amount and location of the involved muscles, the degree of stasis, and the presence of local muscle weakness.

The proposed dosages are presented in the table:

Clinical symptom Muscle	Units
Hand bent in the wrist
Radial flexor flexor	50
The ulnar flexor flexor	40
Compressed fist
Superficial flexor of fingers	40
DlubFinger flexor	40
Hand bent at the elbow
Plecherous	60
Bites	80
Shoulder	50
Pierced forearm
The square pronator	25
Round Proton	40
Thumb, reduced to the palm of your hand
The long flexor of the thumb	20
The muscle that leads to the thumb	10
Short flexor of the thumb / muscle, opposing the thumb	10

In the treatment of spasticity, the recommended dosage for the course of treatment is 170-400 units, depending on the location of the spasmodic muscles.

Improvement occurs within the first 2 weeks, reaching a maximum by the 4th week. The effect lasts usually 12 weeks.

Hyperkinetic folds (facial wrinkles) of the face

The use of the drug for the treatment of facial wrinkles in persons younger than 18 years and older than 65 years is not recommended due to the lack of clinical experience.

Vertical wrinkles between the eyebrows (glabellar wrinkles): the recommended injection volume - 0.1 ml (4 units) - is injected into each of the 5 sites: 2 injections in m. corrugator on both sides and 1 injection in m.procerus, which corresponds to a total dose of 20 units (see Fig.). In some cases, an increase in the total dose of up to 30 units is possible.

Before and during injection, the thumb and index finger should be pressurized below the upper edge of the orbit, preventing diffusion of the solution into this area. During the injection, the needle should be directed upward and medially. In order to reduce the risk of ptosis of the eyelids, it is necessary to avoid injections near the muscle that lifts the upper eyelid and at the site of attachment of the circular muscle of the eye. Injections in m. corrugator should be carried out in the medial muscle and the central abdominal muscle, at least 1 cm above the upper edge of the orbit.

Reducing the severity of vertical wrinkles between the eyebrows (glabellar wrinkles) usually develops within 2-3 days, the maximum effect is observed by the 30th day, and persists up to 4 months after the injection. Intervals between injections should not be less than 3 months.If the result of treatment is unsatisfactory, alternative methods of treatment are used.

Side effects:

Adverse reactions are classified according to the frequency of occurrence: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1 / 1,000 to <1/100), rarely (> 1 / 10,000 to < 1 / 1,000), very rarely (<1 / 10,000).

Blepharospasm:

Often: ptosis (6.1%), dry eyes (2.0%).

Infrequently: paresthesia, conjunctivitis, dry mouth, skin rash, headache, muscle weakness.

In addition, when using a similar preparation containing botulinum toxin type A and used in clinical trials along with Xeomin, the following side effects were noted. They are also possible with the application of Xeomin.

Often: superficial keratitis, lagophthalmus, skin irritation, photophobia, lacrimation.

Infrequent: keratitis, ectropia, diplopia, dizziness, diffuse skin rash / dermatitis, eyelid twist, focal paralysis of facial nerves, weakness of facial muscles, fatigue, vision disorders, blurred vision.

Rarely: local skin swelling of the eyelid.

Very rarely: acute angle-closure glaucoma, ulceration of the cornea.

Spasmodic torticollis:

Often: dysphagia (10%), muscle weakness (1.7%), back pain (1.3%).

Infrequent: inflammation or pressure at the injection site, headache, asthenia, generalized increased sweating, tremor, hoarseness, colitis, vomiting, diarrhea, dry mouth, bone pain, myalgia, skin rashes, itching, scaling of the skin, pain in the eyes.

Very often: pain at the injection site.

Often: dizziness, high blood pressure, numbness at the injection site, general weakness, flu-like symptoms, general malaise, dry mouth, nausea, headache, stiff musculature at the injection site, irritation at the injection site, rhinitis, upper respiratory tract infections.

Infrequently: shortness of breath, diplopia, fever, ptosis, speech disorders.

The severity of dysphagia varies from mild to severe, with the possibility of aspiration; in rare cases, this requires medical care. Dysphagia can persist for two to three weeks from the time of injection, but a 3-month case is documented.Dysphagia develops dose-dependent; according to clinical studies, dysphagia is rare if the total dose of the drug does not exceed 200 units per procedure.

Spasticity of the hand after a stroke:

Often: headache, impaired sensation, feeling hot.

Often: hypertension, ecchymosis, local pain, muscle weakness, irritation or hemorrhage at the injection site.

Infrequent: depression, sleep disorders, paresthesia, impaired coordination, amnesia, vertigo, orthostatic hypotension, nausea, dermatitis, itching, rash, arthralgia, bursitis, asthenia, pain, hypersensitivity at injection site, anxiety, peripheral edema.

Some side effects may be related to the underlying disease.

Hyperkinetic folds (mimic wrinkles) of the face:

Usually, undesirable effects are observed in the first week after application of the drug and are temporary.Undesirable effects may be associated with the active substance and / or with the administration procedure. The expected pharmacological effect of botulinum toxin is localized muscle weakness. Ptosis of the eyelids can be caused by injection technique and is associated with the pharmacological action of the drug.

As with any injection, in connection with it, the local occurrence of pain, soreness, itching, swelling and / or bruising is possible; it is also possible to develop transient vasovagal reactions such as syncope, circulatory disorders, nausea, or tinnitus associated with excitement before injection.

When applying the drug, the following adverse reactions were reported:

Often: pruritus, headache, impaired muscle function at the injection site, a feeling of heaviness.

Infrequent: flu-like symptoms, a feeling of tension at the injection site, bronchitis, rhinopharyngitis, a sensation of "nodules in the skin," eyelid edema, ptosis, blurred vision, eyebrow lift, nausea, muscle twitching and spasms, local weakness of facial muscles.

In addition, for a reference preparation containing a conventional botulinum toxin type A complex and used in several clinical studies(the data collected so far suggest the same activity of both drugs), it is known to develop the following undesirable effects, which probably can also be observed with the use of Xeomin.

Infrequent: infection, paresthesia, dizziness, blepharitis, pain in the eyes, dry mouth, photosensitivity, dry skin.

Common side effects:

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

Information on the severe negative effects that may be associated with cardiovascular disease - such as arrhythmia and myocardial infarction, including fatal outcome - are extremely rare. Whether these deaths were caused by injections of botulinum toxin type A, or concomitant cardiovascular disease, is not accurately established. One case of anaphylactic shock has been reported after administration of a preparation containing botulinum toxin type A.

There are side effects such as exudative erythema polyforma, urticaria, psoriasis-like rashes, pruritus and allergic reactions, but their conditionality by the action of a complex preparation containing botulinum toxin type A is not confirmed.

Sometimes after the injection of botulinum toxin type A, there were changes in the electrophysiological background in some distant muscles; this side effect is not associated with either muscle weakness or other electrophysiological abnormalities.

Overdose:

High doses of Xeomin can lead to the development of severe muscle paralysis in places far from the injection site (in particular: general weakness, ptosis, diplopia, difficulty speech and swallowing, and respiratory muscle paralysis, leading to the development of aspiration pneumonia).

When an overdose is required, hospitalization with general supportive measures. When paralysis of the respiratory musculature requires intubation and artificial ventilation of the lungs up to the normalization of the condition.

Interaction:

Muscle relaxants of peripheral action should be used with caution, while performing antibiotic therapy with aminoglycosides or spectinomycins (possibly enhancing the effect of Xeomin).

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

Special instructions:

Precautionary measures

Immediately after the injection, the remaining solution in a vial or syringe should be inactivated with sodium hydroxide solution (OD N NaOH). All auxiliary materials in contact with the preparation should be autoclaved or inactivated with a solution of 0.1 N NaOH (for at least 18 hours). The shed preparation should be wiped off with an absorbent cloth soaked in a solution of sodium hydroxide.

Effect on the ability to drive transp. cf. and fur:

Due to the nature of the diseases cured by the drug, the patient's ability to control various techniques can be reduced. In addition, the side effects of the drug may adversely affect the patient's ability to control the technique; accordingly, the patient should refrain from such activities until his abilities are fully restored.

Form release / dosage:Lyophilizate for the preparation of solution for intramuscular injection, 50 units and 100 units.

Packaging:

For 50 units or 100 units in a vial.

1 bottle in a plastic pallet in a cardboard box with the control of the first autopsy together with instructions for use in Russian.

2, 3 or 6 cardboard packs are packed in a cardboard pack.

Storage conditions:

At room temperature (not above 25 ° C).

Keep out of the reach of children.

Shelf life:

3 years.

The drug with expired shelf life is not subject to application.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004746/08

Date of registration:23.06.2008

The owner of the registration certificate:Merz Pharma GmbH & Co. KG. KGaAMerz Pharma GmbH & Co. KG. KGaA Germany

Manufacturer: & nbsp

MERZ PHARMA GmbH & Co., KGaA Germany

Representation: & nbspMERZ PHARMA LLCMERZ PHARMA LLCRussia

Information update date: & nbsp05.12.2015

Illustrated instructions

Instructions

Xeomin (Xeomin)