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

Excipients (5 mg / 10 mg): lactose monohydrate (4.00 mg / 50.00 mg), wheat starch (4.00 mg / 10.00 mg), talc (2.00 mg / 2.00 mg), magnesium stearate (1.00 mg / 1 , 00 mg), calcium hydrophosphate dihydrate (24.00 / -), microcrystalline cellulose (type 101) (40.00 mg / 27.00 mg).

Description:

Flat, round tablets are white, with a double-faced facet and a risk on one side.

Pharmacotherapeutic group:dementia treatment

ATX: & nbsp

N.06.D.A.04 Galantamine

Pharmacodynamics:

Selective, competitive and reversible inhibitor of acetylcholinesterase. Stimulates nicotinic receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine.It facilitates the conduction of excitation in the neuromuscular synapse and restores neuromuscular conduction in cases of its blockade by muscle relaxants of a nondepolarizing action type. Increases the tone of smooth muscles, increases the secretion of digestive and sweat glands, causes miosis. Increasing the activity of the cholinergic system, galantamine improves cognitive function in patients with Alzheimer's type dementia, but does not affect the development of the disease itself.

Pharmacokinetics:

After ingestion, quickly and completely absorbed in the gastrointestinal tract. Absolute bioavailability is high - up to 90%. Therapeutic concentration is achieved after 30 minutes after administration. The maximum plasma concentration after taking in a dose of 10 mg is observed at the 2 nd hour and is 1.2 mg / ml. Half-life is 5 hours. After repeated administration, the equilibrium state of the plasma concentration of galantamine is established. To a small extent binds to blood proteins. Easily passes through the hemato-encephalic barrier. To an insignificant extent (about 10%) is metabolized in the liver by demethylation.Output (unchanged and the form of metabolites), mainly with urine (up to 74%). Kidney clearance is approximately 100 ml / min. In patients with Alzheimer's disease, the plasma concentration of galantamine can increase. With moderate and severe violations of the liver and kidney plasma concentrations of galantamine are increased.

Indications:

- Dementia of the Alzheimer's type is mild or moderate;

- poliomyelitis (immediately after the termination of the febrile period, as well as in the recovery period and the period of residual events);

- myasthenia gravis, progressive muscular dystrophy, child

Cerebral palsy, neuritis, radiculitis, myopathy.

Contraindications:

Hypersensitivity to any of the components of the drug; bronchial asthma; bradycardia; atrioventricular block; arterial hypertension, angina pectoris; chronic heart failure; epilepsy; hyperkinesis; severe renal (creatinine clearance less than 9 ml / min) and hepatic (more than 9 points on the scale Child-Plow) violations; mechanical intestinal obstruction; chronic obstructive pulmonary disease; Obstructive diseases or the recently transferred operativeinterventions on the organs of the gastrointestinal tract; Obstructive diseases or recent surgical treatment of the urinary tract or prostate; children under 9 years; pregnancy and lactation.

Carefully:

Mild and moderate impairment of kidney or liver function; syndrome of weakness of the sinus node and other supraventricular conduction disorders, simultaneous use of drugs slowing the heart rate (digoxin, beta-blockers); general anesthesia, peptic ulcer of stomach and duodenum, increased risk of erosive and ulcerative lesions of the gastrointestinal tract.

Gluteal enteropathy (the composition of the drug includes wheat starch).

Lactose deficiency, galactosemia, glucose-galactose malabsorption syndrome (lactose is included in the formulation).

Dosing and Administration:

Inside, with food, washing with water.

Adults:

The daily dose is 10-40 mg, divided into 2-4 admission.

When Myastenia gravis The daily dose is divided into 3 doses.

With Alzheimer's disease treatment is recommended to start with taking 5 mg tablets twice a day.Within 4 weeks, the daily dose can be gradually increased to 20 mg - 1 tablet 10 mg 2 times a day - in the morning and in the evening. During treatment with the drug must ensure the intake of a sufficient number of liquids. If, during treatment, it is necessary to stop taking the drug, then the restoration of treatment should begin with the lowest dose and gradually increase it.

Patients with moderate impairment of liver and kidney function

The initial dose is 5 mg once a day, which is taken in the morning for at least 1 week, after which it is increased to 5 mg twice a day, which is taken within 4 weeks.

The total daily dose should not exceed 15 mg.

Children (from 9 years old):

Treatment of poliomyelitis, cerebral palsy:

from 9 to 11 years - daily dose of 5-15 mg, divided into 2-3 doses;

from 12 to 15 years - The daily dose is 5-20 mg, divided into 2-4 admission.

Side effects:

From the side of the cardiovascular system: decrease or increase in blood pressure, orthostatic collapse, heart failure, edema, atrioventricular block, flutter or atrial fibrillation, prolongation of the QT interval, ventricular and supraventricular tachycardia, supraventricular extrasystole, "hot flashes", bradycardia, ischemia or myocardial infarction.

From the digestive system: abdominal distention, dyspepsia, gastrointestinal discomfort, anorexia, diarrhea, abdominal pain, nausea, vomiting, gastritis, dysphagia, dry mouth, increased salivation, diverticulitis, gastroenteritis, duodenitis, hepatitis, perforation of the esophagus mucosa, bleeding from the upper and lower gastrointestinal tract.

Co hand musculoskeletal system: muscle spasms, muscle weakness, fever.

Laboratory indicators: an increase in liver enzymes, anemia, hypokalemia, an increase in the level of sugar or alkaline phosphatase in the blood.

Hematological: thrombocytopenia, purpura.

From the urinary system: urinary incontinence, hematuria, frequent urination, urinary tract infections, urinary retention, calculosis, renal colic.

From the nervous system: often tremor, syncope, inhibition, taste distortion, visual and auditory hallucinations, behavioral reactions, including agitation / aggression; transient impairment of cerebral circulation or stroke; headache, dizziness, convulsions, muscle spasms, paresthesia, ataxia, hypo- or hyperkinesis, apraxia, aphasia, anorexia, drowsiness, insomnia.

From the sense organs: rhinitis, epistaxis, visual impairment, accommodation spasm, infrequent tinnitus.

From the side of the psyche: depression (very rarely with suicide), apathy, paranoid reactions, increased libido, delirium.

Are common: pain in the chest, excessive sweating, weight loss, fatigue, dehydration (in rare cases with the development of renal failure), bronchospasm.

Overdose:

Symptoms: depression of consciousness (up to coma); convulsions; increased severity of side effects; pronounced muscular weakness in combination with hypersecretion of the mucous membrane of the trachea and bronchospasm, can lead to a lethal blockade of the airways.

Treatment: gastric lavage, symptomatic therapy. As an antidote is used atropine in doses of 0.5-1 mg intravenously. Subsequent doses of atropine are determined depending on the therapeutic response and the patient's condition.

Interaction:

It is not recommended to combine with other holinomimetics.

It is an opioid antagonist by action on the respiratory center. It shows pharmacodynamic antagonism to m-cholinolytics (atropine, gomatropine methyl bromide, etc.), ganglion blockers,Nondepolarizing muscle relaxants, quinine, procainamide.

Aminoglycoside antibiotics can reduce the therapeutic effect of galantamine.

Galantamine enhances neuromuscular blockade during general anesthesia (including when used as peripheral muscle relaxant suksamethonium); drugs that reduce heart rate (digoxin, beta-adrenoblockers) - the risk of aggravation of bradycardia.

Cimetidine may increase the bioavailability of galantamine.

All drugs that inhibit enzymes and isoenzymes of the cytochrome P450 system (CYP2D6, CYP3A4) can increase plasma concentrations of galantamine while simultaneously using them, as a result of which the frequency of cholinergic side effects (mainly nausea and vomiting) may increase. In this case, depending on the tolerability of therapy by a specific patient, a reduction in the maintenance dose of galantamine may be necessary.

Inhibitor inhibitors CYP2D6 (amitriptyline, fluoxetine, fluvoxamine, paroxetine, quinidine) reduce the clearance of galantamine by 25-30%. For this reason, it is not recommended to appoint simultaneously with ketoconazole, zidovudine, erythromycin.

Increases the inhibitory effect on the central nervous system of ethanol and sedatives.

Special instructions:

Treatment with inhibitors of acetylcholinesterase is accompanied by a decrease in body weight. Especially it should be borne in mind when treating patients with Alzheimer's disease, who usually have weight loss. In this regard, you need to monitor the body weight.

During the treatment period, sufficient fluid intake should be ensured.

Like other holinomimetics, the drug can cause vagotonic effects on the part of the cardiovascular system (including bradycardia), which must be taken into account in patients with sinus node weakness syndrome and other conductivity disorders, as well as with simultaneous use with drugs that reduce heart rate (digoxin or beta-blockers).

In the treatment of Nivalin®, there is a risk of syncope, in connection with which, it is necessary to control blood pressure more often, especially when taking the drug at higher doses (40 mg daily dose).

In order to prevent such side effects, it is necessary to carefully select the dose of the drug at the beginning of treatment.

The effectiveness of the drug in patients with other types of dementia and memory impairment is not established.

The drug is not intended for the treatment of patients with mild cognitive impairment, i.e. with isolated memory impairment exceeding the expected level for their age and education, but not satisfying the criteria of Alzheimer's disease.

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

During the treatment period, one should refrain from performing work that requires a high concentration of attention and speed of psycho-motor reactions, including driving.

Form release / dosage:Tablets, 5 mg and 10 mg.

Packaging:

For 10 or 20 tablets (5 mg tablets) or 10 tablets (10 mg tablets) in a blister of PVC film and aluminum foil.

1 blister for 10 tablets (tablets 5 or 10 mg) with instructions for use in a pack of cardboard.

1 or 3 blisters for 20 tablets (5 mg tablets) with instructions for use in a pack of cardboard.

2 blisters for 10 tablets (10 mg tablets) with instructions for use in a pack of cardboard.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001755/09

Date of registration:10.03.2009

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®)