Nivalin, 1 mg/ml 1 ml 10 pcs

Pharmgroup:

Cholinesterase inhibitor.

Pharmic action:

Nivaline is a reversible acetylcholinesterase inhibitor. Facilitates the conduction of nerve impulses in the area of neuromuscular synapses, enhances excitation processes in the reflex areas of the spinal cord and brain, penetrates well through the BBB.

It increases tone and stimulates contraction of smooth and skeletal muscles, secretion of digestive and sweat glands, restores neuromuscular conduction blocked by curare-like myorelaxants of non-depolarizing type.
It causes miosis and accommodation spasm, reduces intraocular pressure in closed-angle glaucoma.

Pharmacokinetics:

Intake

After oral administration, it is quickly and completely absorbed in the gastrointestinal tract. Absolute bioavailability is high – up to 90%. Therapeutic concentration is reached 30 min after drug administration. Cmax after 10 mg dose is reached by 2 hours and is 1.2 mg/ml.

Distribution
Css of galantamine is established after multiple doses. It is slightly bound to blood proteins. Easily passes through the HEB.

Metabolism
To a negligible extent (about 10%) is metabolized in the liver by demethylation.

Elimination
T1/2 – 5 hours. It is excreted (unchanged and as metabolites) mainly in the urine (up to 74%). Renal clearance is approximately 100 ml/min.

Pharmacokinetics in special clinical cases

In patients with Alzheimer’s disease an increase in plasma concentrations of galantamine is possible. In moderate to severe hepatic and renal dysfunction, plasma concentrations of galantamine are increased.

Indications

In neurology:
traumatic injuries of the nervous system;
infantile cerebral palsy;
diseases of the spinal cord (myelitis, polio, poliomyelitis form of tick-borne encephalitis);
Mononeuritis;
polyneuritis;
polyneuropathy;
polyradiculoneuritis;
Guillain-Barré syndrome;
idiopathic facial paresis;
myopathy;
nocturnal urinary incontinence.

In anesthesiology and surgery:
as an antagonist of nondepolarizing myorelaxants and for treatment of postoperative bowel and bladder atony.

In physiotherapy:
as ionophoresis in diseases of the peripheral nervous system.

In toxicology:
intoxication by choline-blocking drugs, morphine and its analogues.

In radiology:
to improve the quality of functional diagnosis of the digestive system, including the gallbladder.

Active ingredient

Composition

1 ml of the solution contains:

active ingredient:

galantamine hydrobromide 1 mg

excipients:

sodium chloride;

water for injection

How to take, the dosage

The drug is administered p/k, c/m, v/v. The dose and duration of therapy shall be set individually, depending on the severity of symptoms and individual patient’s reaction. At the beginning of treatment the drug is prescribed in minimum dose, then it is gradually increased. For adults, the maximum single dose for per oral administration is 10 mg, the maximum daily dose is 20 mg.

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

The drug is administered once a day. When using Nivalin in high doses the daily dose can be divided into 2-3 injections.
Adults as an antagonist of nondepolarizing myorelaxants Nivalin is administered by IV in a daily dose of 10-20 mg.

In radiological studies, the drug is administered to adults in a 1-5 mg dosage in m/m.

In case of peripheral nervous system diseases and for treatment of nocturnal urinary incontinence in children the drug is administered in the form of ionophoresis in a dose of 1-2 ml of 0.25% solution.

Interaction

Concomitant use of Nivalin reduces the inhibitory effect of morphine and its analogues on the respiratory center.
Concomitant use of Nivalin with m-cholinoblockers (atropine), ganglioblockers (hexamethonium, azamethonium bromide, pachycardine), nondepolarizing muscle relaxants (tubocurarine), quinine and novocainamide leads to mutual reduction of action.

The aminoglycoside antibiotics (gentamicin, amikacin) may decrease the therapeutic effect of Niwalin.
When used concomitantly, it increases the effect of depolarizing myorelaxants.

Concomitant use of cimetidine may increase the bioavailability of galantamine.

CYP2D6 and CYP3D4 are enzymes involved in the metabolism of galantamine. Quinidine, paroxetine, fluoxetine are CYP2D6 isoenzyme inhibitors, and the drugs ketoconazole, zidovudine, erythromycin are CYP3D4 isoenzymes, so they may affect galantamine metabolism, which may lead to increased serum concentrations.

Special Instructions

During treatment it is necessary to refrain from driving or operating complex machinery, as the drug may cause visual impairment, dizziness and somnolence.

Contraindications

– bronchial asthma;
– bradycardia;
– AV-blockade;
– angina pectoris;
– Chronic heart failure in decompensation stage;
– Epilepsy;
– Hyperkinesias;
– Mechanical intestinal obstruction;
– Mechanical disorders of the urinary tract patency;
– severe hepatic insufficiency;
– severe renal insufficiency;
– children under 1 year of age;
– pregnancy;
– lactation;
– hypersensitivity to the preparation components.
With caution the drug is prescribed in case of renal insufficiency, urinary disorders, recent surgery on the prostate, surgical interventions with general anesthesia.
The drug is not used in children in order to improve the quality of radiological studies.

Side effects

The digestive system: often – nausea, vomiting, abdominal cramps, diarrhea, increased salivation, anorexia; rarely – colic.

CNS disorders: frequently – fatigue, dizziness, headache, somnolence; rarely – insomnia, visual disturbances (accommodation spasm).

Others: increased sweating; rarely – rhinitis, bradycardia, urinary tract infection, bronchospasm, renal colic.

Overdose

Symptoms: nausea, vomiting, cramps, diarrhea, decreased BP, bradycardia, bronchospasm; in severe cases – seizures, coma.

Treatment: symptomatic therapy, control of respiratory and cardiovascular system function. As an antidote, atropine 0.5-1 mg w/v dose; the dose may be repeated depending on the clinical picture.

Similarities