Nivalin - Instructions For Use, Price, Reviews, Analogs, Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Nivalin

Nivalin: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Nivalin

ATX code: N06DA04

Active ingredient: galantamine (Galantamine)

Manufacturer: Sopharma, JSC (Bulgaria)

Description and photo updated: 2018-29-11

Prices in pharmacies: from 850 rubles.

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Nivalin is an anticholinesterase agent.

Release form and composition

• solution for injection: from colorless to pale yellow, transparent (1 ml each in colorless glass ampoules, 10 ampoules in blisters, in a cardboard box of 1 or 10 blisters);
• tablets: round, flat, white, with a double-sided bevel and a notch on one side (at a dosage of 5 mg - 10 pcs. in blisters, in a cardboard box 1 blister; 20 pcs. in blisters, in a cardboard box 1 or 3 blisters; at a dosage of 10 mg - 10 pcs. in blisters, in a cardboard box 1 or 2 blisters).

Each pack also contains instructions for the use of Nivalin.

Composition of 1 ampoule of solution:

• active substance: galantamine hydrobromide - 1; 2.5; 5 or 10 mg;
• auxiliary components: sodium chloride, water for injection.

Composition of 1 tablet:

• active substance: galantamine hydrobromide - 5 or 10 mg;
• auxiliary components: wheat starch, lactose monohydrate, microcrystalline cellulose (type 101), magnesium stearate, talc; 5 mg tablets also contain calcium hydrogen phosphate dihydrate.

Pharmacological properties

Pharmacodynamics

The active ingredient of Nivalin, galantamine hydrobromide, is a reversible acetylcholinesterase inhibitor. Stimulates n-cholinergic receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine.

The drug facilitates the conduction of nerve impulses in the area of neuromuscular synapses, enhances the processes of excitation in the reflex zones of the brain and spinal cord.

Increases tone and stimulates the contraction of skeletal and smooth muscles, enhances the secretion of sweat and digestive glands. Restores neuromuscular conductivity, which is blocked by curariform muscle relaxants of a non-depolarizing type. Reduces intraocular pressure in angle-closure glaucoma, causes accommodation spasm and miosis.

By increasing the activity of the cholinergic system, galantamine hydrobromide improves cognitive functions in patients with dementia of the Alzheimer's type, but does not affect the development of the disease itself.

Pharmacokinetics

After subcutaneous administration and oral administration of Nivalin, galantamine is rapidly absorbed. The therapeutic concentration is reached within 30 minutes. After applying a dose of 10 mg, the maximum plasma concentration is observed after 2 hours and is 1.2 mg / ml.

Absolute bioavailability can reach 90%.

With prolonged use of Nivalin, an equilibrium concentration is established. Galantamine weakly binds to blood proteins. Easily penetrates the blood-brain barrier (BBB), is found in brain tissues.

To an insignificant extent (up to 10%) it is metabolized in the liver by demethylation with the formation of metabolites galantaminone and epigalanthamine, which are found in plasma and urine.

It is excreted unchanged and as metabolites mainly by glomerular filtration in the urine (up to 74% when taken orally, up to 89% after subcutaneous administration). The half-life is 5 hours. In a small amount (0.2 ± 0.1% / 24 hours) it is excreted in the bile. Renal clearance is approximately 100 ml / min, which is close to inulin clearance, corresponding to creatinine clearance (CC).

The plasma concentration of the drug increases in patients with moderate and severe impairment of renal / liver function, with Alzheimer's disease.

Indications for use

Injection

Neurology:

• cerebral palsy;
• traumatic damage to the nervous system;
• spinal cord diseases (myelitis, poliomyelitis, polio form of tick-borne encephalitis);
• myopathy;
• idiopathic paresis of the facial nerve;
• polyneuropathy, polyneuritis, polyradiculoneuritis, neuritis;
• Guillain-Barré syndrome;
• bed-wetting.

Anesthesiology and Surgery:

• postoperative intestinal and bladder atony;
• the need to reduce the effect of non-depolarizing muscle relaxants (as an antagonist).

Other indications for use:

• toxicology: intoxication with anticholinergic drugs, morphine or its analogues;
• physiotherapy: diseases of the peripheral nervous system (in the form of iontophoresis);
• radiology: functional diagnostics of the state of the digestive system and gallbladder (in order to improve the quality of diagnostics).

Pills

• cerebral palsy;
• myopathy;
• dementia of the Alzheimer's type, mild to moderate;
• progressive muscular dystrophy;
• radiculitis;
• neuritis;
• myasthenia gravis;
• poliomyelitis (immediately after the end of the febrile period, as well as in the recovery period and the period of residual effects).

Contraindications

Absolute contraindications for both dosage forms of Nivalin:

• obstructive diseases of the urinary tract (mechanical obstruction);
• chronic heart failure;
• atrioventricular block;
• bradycardia;
• angina pectoris;
• hyperkinesis;
• epilepsy;
• bronchial asthma;
• mechanical intestinal obstruction;
• severe hepatic impairment (> 9 points on the Child-Pugh scale);
• severe renal failure (CC <9 ml / min);
• period of pregnancy and lactation;
• hypersensitivity to any component of the drug.

Additionally for Nivalin injection solution:

• age up to 1 year;
• age up to 18 years when used to improve the quality of X-ray studies.

Additionally for Nivalin tablets:

• chronic obstructive pulmonary disease (COPD);
• arterial hypertension;
• recently underwent surgery on the organs of the gastrointestinal tract (GIT), urinary tract or prostate gland;
• age up to 9 years.

Relative contraindications for injection solution (caution should be exercised):

• renal failure;
• disorders of urination;
• operations using general anesthesia;
• recent surgery on the prostate gland.

Relative contraindications for tablets (care should be taken):

• mild to moderate renal / liver dysfunction;
• sick sinus syndrome and other disorders of supraventricular conduction;
• peptic ulcer of the stomach and duodenum or the risk of developing erosive and ulcerative lesions of the gastrointestinal tract;
• gluten enteropathy;
• glucose / galactose malabsorption syndrome, galactosemia, lactase deficiency;
• operations using general anesthesia;
• the simultaneous use of drugs that can slow down the heart rate (for example, beta-blockers or digoxin).

Nivalin, instructions for use: method and dosage

Injection

In this dosage form, Nivalin is administered subcutaneously (subcutaneously), intramuscularly (intramuscularly) or intravenously (intravenously).

The dose and duration of treatment is determined by the doctor, taking into account the severity of the symptoms of the disease and the individual characteristics of the patient.

Treatment begins with a minimum dose and is gradually increased.

For adults, with subcutaneous administration, the maximum doses are: single - 10 mg, daily - 20 mg.

Recommended dosages of Nivalin (for subcutaneous administration) for children, depending on their age:

• 1-2 years - 0.1-0.2 ml of 0.25% solution (0.25-1 mg);
• 3-5 years - 0.2-0.4 ml of 0.25% solution (0.5-5 mg);
• 6-8 years old - 0.3-0.42 ml of 0.25% solution (0.75-7.5 mg);
• 9-11 years old - 0.5 ml of 0.25% solution - 0.6 ml of 0.5% solution (1-10 mg);
• 12-15 years - 0.7 ml of 0.25% solution - 1 ml of 0.5% solution (1.25-12.5 mg);
• over 15 years old - 0.2-0.7 ml of 1% solution (12.5-20 mg).

The duration of treatment depends on the severity and characteristics of the disease, on average 40-60 days. If necessary, courses are repeated 2–3 times at intervals of 1–2 months.

For children with bedwetting and diseases of the peripheral nervous system, Nivalin is administered in the form of iontophoresis. Assign in a dose of 1-2 ml of 0.25% solution.

Nivalin is usually administered 1 time. If a high daily dose is prescribed, it can be divided into 2 administrations.

As an antagonist of non-depolarizing muscle relaxants for adult patients, Nivalin is prescribed in a daily dose of 10–20 mg, administered intravenously.

To improve the quality of X-ray studies in adults, the drug is prescribed in a dose of 1–5 mg, administered intramuscularly.

Pills

In the form of tablets, Nivalin should be taken orally, with meals, washed down with the tablets with water.

The daily dose for adults is 10-40 mg, depending on the volume it is divided into 2-4 doses, with myasthenia gravis - into 3 doses.

In Alzheimer's disease, the initial recommended dose is 5 mg 2 times a day. Over the next 4 weeks, if necessary, the daily dose is gradually increased to 20 mg - 10 mg each morning and evening. Patients during the period of therapy should consume sufficient liquid. In cases where it is necessary to take a break in treatment, therapy should be resumed with a low dose and gradually increased.

Daily doses of Nivalin for children with cerebral palsy and poliomyelitis, depending on age:

• 9-11 years old: 5-15 mg in 2-3 divided doses;
• 12-15 years: 5-20 mg in 2-4 doses.

Patients with moderately severe impaired renal / liver function should take 5 mg 1 time per day (in the morning) for at least the first week of therapy, and 5 mg 2 times a day for the next 4 weeks. The total daily dose of Nivalin should not exceed 15 mg.

Side effects

Injection

• from the digestive system: often - increased salivation, cramping abdominal pain, nausea, diarrhea, vomiting, anorexia; rarely - intestinal colic;
• from the central nervous system: often - drowsiness, headache, dizziness, fatigue; rarely - accommodation spasm, insomnia;
• others: increased sweating; rarely - urinary tract infection, rhinitis, bronchospasm, bradycardia, renal colic.

Pills

• from the central and peripheral nervous system: often - visual and auditory hallucinations, taste perversion, lethargy, syncope, tremors, behavioral reactions (including agitation and aggression); infrequently - headache, insomnia, drowsiness, dizziness, aphasia, apraxia, hypo- or hyperkinesis, ataxia, muscle spasms, convulsions, paresthesia, apathy, depression (very rarely with suicide), anorexia, transient cerebrovascular accident, stroke, delirium, paranoid reactions, increased libido;
• from the digestive system: dry mouth, increased salivation, dyspepsia, abdominal pain, diarrhea, gastrointestinal discomfort, bloating, duodenitis, gastritis, nausea, gastroenteritis, dysphagia, vomiting, anorexia, diverticulitis, hepatitis, perforation, digestion bleeding from the upper and lower gastrointestinal tract, an increase in the level of alkaline phosphatase, an increase in the activity of liver enzymes;
• from the cardiovascular system: supraventricular premature beats, ventricular and supraventricular tachycardia, decrease or increase in blood pressure, AV block, bradycardia, orthostatic collapse, atrial flutter or atrial fibrillation, prolongation of the QT interval, hot flashes, edema, heart failure, ischemia;
• from the hematopoietic system: purpura, thrombocytopenia, anemia;
• from the urinary system: frequent urination, incontinence or urinary retention, urinary tract infections, hematuria, calculus, renal colic;
• from the musculoskeletal system: muscle weakness, muscle spasms;
• on the part of the senses: accommodation spasm, visual disturbances, epistaxis, rhinitis; infrequently - tinnitus;
• laboratory parameters: hyperglycemia, hypokalemia;
• others: increased sweating, fever, fatigue, chest pain, weight loss, bronchospasm, dehydration (in rare cases with the development of renal failure).

Overdose

Injection

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

Treatment: symptomatic therapy, monitoring and, if necessary, maintaining the functions of the cardiovascular and respiratory systems. Intravenous administration of atropine (0.5–1 mg) is shown as an antidote; if necessary, its repeated administration is possible.

Pills

Symptoms: increased severity of side effects, convulsions, depression of consciousness up to coma. The combination of severe muscle weakness with hypersecretion of the tracheal mucosa and bronchospasm can lead to a fatal airway blockage.

Treatment: gastric lavage and symptomatic therapy. Atropine is administered as an antidote. If necessary, it is re-administered, the doses are determined depending on the patient's condition and the therapeutic response.

special instructions

Acetylcholinesterase inhibitors contribute to weight loss, which should be especially taken into account when treating Alzheimer's disease, since patients with this disease usually have a decrease in weight.

The effectiveness of Nivalin in other types of dementia and memory impairment has not been established. The drug is not used to treat patients with mild cognitive impairment, that is, with isolated memory impairment that exceeds the expected level for education and age of the person, but does not meet the criteria for Alzheimer's disease.

Adequate fluid intake is recommended during the period of taking Nivalin tablets.

Galantamine increases the risk of syncope (fainting), and therefore requires periodic monitoring of blood pressure, especially when using Nivalin in a daily dose of 40 mg. In order to avoid the occurrence of side effects at the beginning of treatment, the dose should be carefully selected.

Nivalin can cause the development of vagotonic effects on the part of the cardiovascular system (including bradycardia). This should be taken into account when prescribing the drug to patients with conduction disorders (including sick sinus syndrome) or taking medications that can reduce the heart rate.

Influence on the ability to drive vehicles and complex mechanisms

Nivalin can cause visual impairment, dizziness and drowsiness, therefore, during the period of therapy, patients should refrain from performing potentially hazardous activities, including driving a car and working with complex mechanisms.

Application during pregnancy and lactation

The use of Nivalin during pregnancy and lactation is contraindicated.

Pediatric use

The solution, when used to improve the quality of X-ray examinations, is contraindicated in patients under 18 years of age, for other indications - under 1 year.

Nivalin tablets are not prescribed for children under 9 years of age.

With impaired renal function

The use of Nivalin is contraindicated in severe renal failure (CC <9 ml / min).

Patients with mild to moderate renal impairment should be treated with caution.

For violations of liver function

The use of Nivalin is contraindicated in severe hepatic failure (> 9 points on the Child-Pugh scale).

Patients with mild to moderate hepatic impairment should be treated with caution.

Drug interactions

A mutual decrease in the effects is noted with a combination of Nivalin and m-cholinergic blockers (atropine), non-depolarizing muscle relaxants (tubocurarine), ganglion blockers (hexamethonium, azamethonium bromide, pachicarpin), novocainamide, quinine.

With the simultaneous use of galantamine enhances the effect of depolarizing muscle relaxants.

Cimetidine is able to increase the bioavailability of galantamine.

The therapeutic effect of Nivalin can be reduced by aminoglycoside antibiotics (for example, gentamicin or amikacin).

Galantamine reduces the inhibitory effect on the respiratory center of opioids (morphine and its analogues). Strengthens neuromuscular blockade during general anesthesia (including when using suxamethonium as a peripheral muscle relaxant). Strengthens the depressing effect on the central nervous system of ethanol and sedatives.

With the combined use of drugs that reduce the heart rate (for example, beta-blockers or digoxin), bradycardia is aggravated.

Nivalin is not recommended to be taken in combination with other cholinomimetics.

CYP2D6 and CYP3D4 are isozymes involved in galantamine metabolism. Erythromycin, zidovudine and ketoconazole are inhibitors of the CYP3D4 isoenzyme, fluoxetine, paroxetine, quinidine, fluvoxamine and amitriptyline are inhibitors of the CYP2D6 isoenzyme. Consequently, these drugs can affect the metabolism of galantamine, which may lead to an increase in its concentration in serum and, as a consequence, an increase in the frequency of cholinergic side effects (especially nausea and vomiting). In this case, a reduction in the maintenance dose of Nivalin may be required.

Analogs

Analogs of Nivalin are: Axamon, Alzepil, Alcenorm, Berinert, Galnora SR, Dementis, Ipigrix, Kalimin 60 N, Proserin, Reminil, Exelon, Yasnal.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C out of reach of children, protected from light and moisture.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Nivaline

Despite the wide range of uses of the drug, reviews of Nivalin are mainly left by relatives and guardians of elderly people receiving the drug for dementia. The nature of the messages is predominantly negative: no benefit from the therapy is noted, and the condition does not improve.

The price of Nivalin in pharmacies

Approximate prices for Nivalin (for a pack of 10 ampoules):

• solution of 1 mg / ml - 841–904 rubles;
• solution of 2.5 mg / ml - 1128-1232 rubles;
• solution 5 mg / ml - 1793-1850 rubles;
• solution 10 mg / ml - 3326–3519 rubles.

Nivalin: prices in online pharmacies

Drug name Price Pharmacy

Nivalin 1 mg / ml solution for injection 1 ml 10 pcs. 850 RUB Buy

Nivalin 2.5 mg / ml solution for injection 1 ml 10 pcs. 1080 RUB Buy

Nivalin 5 mg / ml solution for injection 1 ml 10 pcs. 1639 RUB Buy

Nivalin rr d / in. 1% amp. 1ml No. 10 3312 RUB Buy

Nivalin 10 mg / ml solution for injection 1 ml 10 pcs. 3418 RUB Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!