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

Cholinesterase inhibitor of reversible action. It facilitates the carrying out of nerve impulses in the field of neuromuscular synapses; intensifies excitation processes in the reflex zones of the spinal cord and brain, penetrates well through the blood-brain barrier.Increases the tone and stimulates the reduction of smooth and skeletal muscles, the secretion of digestive and sweat glands, restores neuromuscular conduction blocked by muscle relaxants of nondepolarizing type. Causes miosis, spasm of accommodation, reduces intraocular pressure in closed-angle glaucoma.

Pharmacokinetics:

Galantamine is rapidly absorbed after subcutaneous injection. The therapeutic concentration in the blood plasma is reached within 30 minutes. There was no statistically significant difference in the area under the concentration-time curve (AUC) after a single dose of 10 mg administered orally or parenterally.

The maximum concentration in the blood plasma after a single dose of 10 mg administered orally or parenterally is 1.20 mg / ml and is reached within 2 hours. The elimination time is 5 hours.

The half-distribution period of galantamine is 10 min, which is longer than in the half-distribution of neostigmine methyl sulfate and pyridostigmine bromide (0.54-3.5 min and 5.0-6.6 min, respectively). The half-life is also longer, indicating that galantamine is a drug with a "mild" but stable effect. Galantamine weakly binds to plasma proteins. Well penetrates the blood-brain barrier.

Metabolized by demethylation (5-6%). Metabolites galantamine - epigalanthamn and galantamine, are found in plasma and urine.

Galantamine is excreted mainly through glomerular filtration. The renal clearance of galantamine is 1.40 ml / min per kg. It is not conjugated in the liver and its biliary excretion is poorly expressed - 0.2 ± 0.1% for 24 hours. Galantamine in unchanged form and its metabolites (galantamine, epigalanthamine) are excreted in urine in 89% after subcutaneous injection. It is established that the renal clearance of galantamine is about 100 ml / min, which is close to the clearance of inulin. With renal failure, the clearance decreases.

Indications:

Neurology

- diseases of the peripheral nervous system (polyradiculoneuritis, radiculoneuritis, neuritis, polyneuritis, polyneuropathy);

- conditions associated with damage to the anterior horn of the spinal cord (after poliomyelitis, myelitis, spinal muscular atrophy);

- cerebral palsy (conditions after stroke of the brain, cerebral palsy);

- disorders of the neuromuscular synapse (myasthenia gravis, muscular dystrophy).

Anaesthesiology and surgery

- for the removal of the effects of nondepolarizing neuromuscular blockers and in the treatment of postoperative paresis of the small intestine and bladder.

Physiotherapy

- for iontophoresis with neurological lesions of the peripheral nervous system, and night incontinence of urine.

Toxicology

- when poisoning with anticholinergic drugs.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- brohnhialnaya asthma;

- atAcute heart failure, bradycardia, stenocardia, atrioventricular block;

- ahyperthermia;

- epilepsy;

- giperkinesis, severe hepatic insufficiency, mechanical intestinal obstruction;

- tsevere renal failure, mechanical impairment of the urinary tract;

- dEthnic age up to 1 year;

- pregnancy and lactation.

Carefully:

Renal failure, urination disorder, recent surgery on the prostate gland, surgery with general anesthesia (anesthesia).

When treatment with cholinesterase inhibitors, including galantamine, is associated with a decrease in body weight,it is necessary to monitor the body weight of patients.

Pregnancy and lactation:

The use of the drug during pregnancy is contraindicated.

Since there is no data on the penetration into breast milk, this drug is contraindicated in breastfeeding. If Nivalin® is needed during breastfeeding, breast-feeding should be discontinued.

Dosing and Administration:

Parenterally: subcutaneously, intramuscularly or intravenously.

Dose and duration of treatment Nivalin® is prescribed by the attending physician depending on the severity of the symptoms of the disease and the patient's individual response to the treatment.

Neurology

Nivalin® in the form of a solution for injection is used for short-term treatment if it is impossible to take the drug inside. At the first opportunity, they switch to oral administration of the drug.

Adults

Nivalin® injection is usually administered at a dose of 0.03-0.28 mg / kg.

An initial dose of 2.5 mg per day is recommended. The daily dose is gradually increased after 3-4 days by 2.5 mg, in 2-3 doses at equal doses.

The maximum single dose for adults is 10 mg subcutaneously, and the maximum daily dose is 20 mg.

Children

Doses are set by the doctor according to the calculation per kg of body weight of the child, the severity of the symptoms and individual tolerability.

It is applied subcutaneously in the following daily doses:

Children from 1 to 2 years old: 0.25-1 mg (0.02-0.08 mg / kg)

In children older than 3 years, Nivalin® injection is used at a dose of 0.03-0.28 mg / kg or:

from 3 to 5 years: 0.5 - 5 mg;

from 6 to 8 years: 0.75 - 7.5 mg;

from 9 to 11 years: 1-10 mg;

from 12 to 15 years: 1.25 - 12.5 mg;

older than 15 years: 1.25-15 mg.

Anesthesiology, surgery and toxicology

As an anticuracary agent and an antidote for an overdose of peripheral nondepolarizing neuromuscular blockers, Nivalin® is administered intravenously at a dose of 10-20 mg per day.

When the postoperative paresis of the gastrointestinal tract and bladder is administered subcutaneously, intramuscularly or intravenously in doses, according to age, divided into 2-3 doses per day.

Children

Doses are set by the doctor, and are applied according to the calculation per kg of body weight of the child, the severity of the symptoms and individual tolerability.

It is administered intravenously in the following doses:

Children from 1 year to 2 years: 0,25 - 1 mg (0,03-0,08 mg / kg)

In children older than 3 years of age, Nivalin® injection is administered at a dose of 0.03 -0.28 mg / kg or:

from 3 to 5 years: 0.5 - 5 mg;

from 6 to 8 years: 0.75 - 7.5 mg;

from 9 to 11 years: 1-10 mg;

from 12 to 15 years: 1.25 - 12.5 mg;

over 15 years and adults: 1.25-15 mg.

Physiotherapy

When iontophoresis - from 2.5 to 5 mg galantamine (with an electric current from 1 to 2 mA) for 10 minutes for 10-15 days.

Side effects:

Hypersensitivity to galantamine.

Expressed nicotinic or muscarinic (to a lesser extent) effects characteristic of the pharmacological class.

From the side of the cardiovascular system: bradycardia, AV blockade, angina pectoris, palpitations, hypotension or hypertension.

From the nervous system: dizziness, headache, insomnia.

From the side of the organs of sight: narrowing of the pupils, increased lacrimal secretion.

Respiratory, thoracic and mediastinal disorders: tachypnea, bronchospasm, increased nasal and bronchial secretion.

From the gastrointestinal tract: nausea; vomiting, diarrhea, increased salivation, increased intestinal peristalsis, abdominal pain.

Co hand immune system: itching, rashes, hives, rhinitis.

AT single cases there are acute reactions of hypersensitivity, including anaphylactic shock with loss of consciousness.

With intensified parasympatomimetic reactions, the daily dose should be reduced or discontinued for 2-3 days and then continued with lower doses.

Other: loss of appetite, weight loss, increased sweating, muscle spasms;

Overdose:

Symptoms of an overdose of Nivalin®: nausea, vomiting, colicky pains (spasms) in the abdomen, diarrhea, lowering of blood pressure, bradycardia, bronchial spasm, and in more severe cases - convulsions and coma.

Treatment: symptomatic therapy, control of respiratory and cardiovascular systems. As an antidote can be used atropine in a dose of 0.5-1 mg intravenously; the dose can be re-entered depending on the clinical picture.

Interaction:

Nivalin® is a weak anthogenist of morphine and its structural analogues in relation to the inhibitory effect on the respiratory center.

Between Nivalin® and m-holinoblokatorami (atropine, gomatropine methyl bromide), ganglion blockers (benzohexonium benzenesulfonate, azamethonium bromide, pakhikarpine hydroiodite), nondepolarizing muscle relaxants (tubocurarine chloride, etc.), quinine and procainamide, antagonism is possible.

Aminoglycoside antibiotics (gentamicin, amikacin) may reduce the therapeutic effect of Nivalin®.

Strengthens the effect of depolarizing muscle relaxants (suxamethonium, etc.)

Cimetidine can increase the bioavailability of galantamine.

In the metabolism of galantamine, isozymes participate CYP2D6 and CYP3A4. Quinidine, paroxetine, fluoxetine suppress isoenzyme CYP2D6, a ketoconazole, zidovudine, erythromycin suppress isoenzyme CYP3A4. Thus, they can affect the metabolism of galantamine, which can lead to an increase in its concentration in the serum.

Special instructions:

Treatment should be carried out in conjunction with physiotherapeutic procedures (massage, medical gymnastics), which should be started 1-2 hours after the administration of the drug.

During treatment, the use of ethanol and sedatives is unacceptable.

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

During treatment with Nivalin® it is necessary to refrain from driving or working with machinery, as the use of the drug may cause visual impairment, dizziness and drowsiness.

Form release / dosage:

Solution for injection, 1 mg / ml, 2.5 mg / ml, 5 mg / ml, 10 mg / ml.

Packaging:

1 ml per ampoule of colorless glass I hydrolytic class with a label for opening the ampoule (color point).

10 ampoules per blister of PVC film.

1 blister with instructions for use in a pack of cardboard.

10 blisters in a box of cardboard with instructions for use (for inpatient).

* In case of production necessity, an additional application of the color ring / colored rings is possible for encoding the ampoule.

Storage conditions:

Store in a dry and protected from light place, at a temperature not exceeding 25 FROM.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N008777

Date of registration:04.08.2010 / 22.04.2013

Expiration Date:Unlimited

The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria

Manufacturer: & nbsp

SOPHARMA, AD Bulgaria

Representation: & nbspSOFARMA SA SOFARMA SA Bulgaria

Information update date: & nbsp18.07.2016

Illustrated instructions

Instructions

Nivalin® (Nivalin®)