NIVALIN (Solution for injection)

Active material: Galantamin
When ATH: N06DA04
CCF: Cholinesterase inhibitor
ICD-10 codes (testimony): A80, A84, F98.0, G04, G51, G60, G61, G61.0, G62.1, G63.2, G80, K91.3, M54.1, M79.2, T40.2, T44, Z03
When CSF: 02.11.02.01
Manufacturer: SOPHARMA AD (Bulgaria)

Pharmaceutical form, composition and packaging

Solution for injection clear, colorless to pale yellow.

Excipients: sodium chloride, water d / and.

1 ml – colorless glass vials (10) – blisters (1) – packs cardboard.
1 ml – colorless glass vials (10) – blisters (10) – packs cardboard.

Solution for injection clear, colorless to pale yellow.

Excipients: sodium chloride, water d / and.

1 ml – colorless glass vials (10) – blisters (1) – packs cardboard.
1 ml – colorless glass vials (10) – blisters (10) – packs cardboard.

Solution for injection clear, colorless to pale yellow.

Excipients: sodium chloride, water d / and.

1 ml – colorless glass vials (10) – blisters (1) – packs cardboard.
1 ml – colorless glass vials (10) – blisters (10) – packs cardboard.

Solution for injection clear, colorless to pale yellow.

Excipients: sodium chloride, water d / and.

1 ml – colorless glass vials (10) – blisters (1) – packs cardboard.
1 ml – colorless glass vials (10) – blisters (10) – packs cardboard.

Pharmacological action

Reversible inhibitor of acetylcholinesterase. It facilitates the nerve impulses in the neuromuscular synapses, strengthens the processes of excitation in the reflex zones of the brain and spinal cord, easily penetrates through the BBB. It improves skin tone and stimulates the contraction of smooth and skeletal muscles, secretion of digestive and sweat glands, restores neuromuscular conductivity, blokirovannuû kurarepodobnymi miorelaksantami nedepolârizuûŝego type. Causes miosis, cyclospasm, lowers intraocular pressure with angle-closure glaucoma.

Pharmacokinetics

Absorption

Galantamine is rapidly absorbed after s / to the introduction. The therapeutic plasma concentration is reached within 30 m. No statistically significant difference in AUC values ​​after a single dose 10 mg (ingestion and parenteral administration). C_max in blood plasma after a single dose 10 mg (ingestion and parenteral administration) is 1.2 mg / ml is reached within 2 no.

Distribution

Period of galantamine poluraspredeleniya 10 and m is longer than the period of neostigmine and pyridostigmine poluraspredeleniya (respectively 5 and 6.6 m). Galantamine weakly bound to plasma proteins. It penetrates through the blood-brain barrier and is found in the brain tissue.

Metabolism

It is metabolized by demethylation (5-6%). Galantamine metabolites (epigalantamin and galantaminon) found in plasma and urine.

Deduction

It writes mainly by glomerular filtration. Clearing time 5 no. In small amounts excreted in the bile (0.2± 0.1% / 24). Galantamine, unedited, and its metabolites (epigalantamin and galantaminon) urine output on 89% after s / to the introduction of. Established, that renal clearance of galantamine about 100 ml / min, which is close to the inulin clearance (which corresponds to QC).

Pharmacokinetics in special clinical situations

In renal insufficiency, the clearance is reduced

Testimony

In neurology:

- Traumatic injury of the nervous system;

- cerebral palsy;

- Diseases of the spinal cord (myelitis, polio, Polio form of tick-borne encephalitis);

- Neuritis, polyneuritis, polyneuropathy, poliradikulonevrit;

- Guillain-Barre syndrome;

- Idiopathic facial nerve paresis;

- Myopathy;

- Bedwetting.

The anesthesiology and surgery:

- As antagonist nedepolyariziruyushtih miorelaksantov;

- For the treatment of postoperative atony bowel and bladder.

In physiotherapy:

- Iontophoresis as diseases of the peripheral nervous system.

The toxicology:

- Intoxication anticholinergic drugs, Morphine and its analogues;

In radiology:

- To improve the quality of functional diagnosis of the condition of the digestive system and gall bladder.

Dosage regimen

The drug is administered s / c, / m, I /. The dose and duration of therapy is determined individually, depending on the severity of the disease and the individual response of the patient. At the beginning of the treatment drug is prescribed in the minimum dose, then gradually increase. To Adult The maximum single dose for the p / to the introduction of 10 mg, the maximum daily dose – 20 mg.

To children dose for s / c administration depends on the age:

The duration of treatment depends on the nature and severity of the disease and averages 40-60 days. The course of treatment can be repeated 2-3 times at intervals 1-2 Months.

The drug is administered 1 time / day. In applying Nivalin^® at higher doses the daily dose can be divided into 2 introduction.

Adults in of qualitative antagonist nedepolyarizuyushtih miorelaksantov Nivalin^® introduced into / in a daily dose of 10-20 mg.

During the X-ray studies the drug is administered to adults / m at a dose 1-5 mg.

At peripheral nervous system diseases and for the treatment of nocturnal enuresis children preparation is administered as a dose of iontophoresis 1-2 ml 0.25% solution.

Side effect

From the digestive system: often – nausea, vomiting, cramping abdominal pain, diarrhea, increased salivation, anorexia; rarely – kišečnaâ how.

CNS: often – fatigue, dizziness, headache, drowsiness; rarely – insomnia, visual impairment (cyclospasm).

Other: increased perspiration; rarely – rhinitis, bradycardia, urinary infection, bronchospasm, počečnaâ how.

Contraindications

- Bronchial asthma;

- Bradycardia;

- AV блокада;

- Angina;

- Chronic heart failure decompensation;

- Epilepsy;

- Hyperkinesis;

- Mechanical intestinal obstruction;

- Mechanical patency of the urinary tract;

- Severe hepatic impairment;

- Severe renal insufficiency;

- Children up to age 1 year;

- Pregnancy;

- Lactation (Grun vskarmlivanyai);

- Hypersensitivity to the drug.

FROM caution prescribe the drug in renal failure, micturition disorders, recently adjourned surgery on the prostate gland, during surgery with general anesthesia.

To improve the quality of X-ray studies the drug is not used in children.

Pregnancy and lactation

Is contraindicated in pregnancy and lactation.

Cautions

Effects on ability to drive vehicles and management mechanisms

During treatment, patients should refrain from driving cars and other activities, require high concentration and speed of psychomotor reactions, tk. the drug can cause drowsiness, dizziness, visual impairment.

Overdose

Symptoms: nausea, vomiting, spasms, diarrhea, decrease in blood pressure, bradycardia, bronchospasm; in severe cases – convulsions, coma.

Treatment: symptomatic therapy, Control functions of the respiratory and cardiovascular system. As an antidote – in / in a dose of atropine 0.5-1 mg / in; dose may be repeated depending on the clinical picture.

Drug Interactions

Nivalin^® while the application reduces the inhibitory effect of morphine and its analogs on the respiratory center.

In an application Nivalin^® M-holinoblokatorami (atropyn), ganglioblokatorami (geksametonïy, azametoniya bromide, paxikarpin), non-depolarizing muscle relaxants (tuʙokurarin), quinine and novokainamidom a mutual reduction in action.

Aminoglikozidnыe Antibiotics (gentamicin, amikacin) may reduce the therapeutic effect of Nivalin^®.

In an application enhances the effect of depolarizing muscle relaxant.

With simultaneous application of cimetidine may increase the bioavailability of galantamine.

CYP2D6 and CYP3D4 are isoenzymes, involved in the metabolism of galantamine. Quinidine, paroxetine, fluoxetine are inhibitors of CYP2D6 isoenzyme, and drugs ketoconazole, zidovudine, Erythromycin – isoenzyme CYP3D4, thus, they can influence the metabolism of galanthamine, which may lead to an increase in its concentration in the serum.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

A List. The drug should be stored in a dry, dark place at a temperature no higher than 25 ° C. Shelf life – 5 years.