Active ingredients: L-acetylcarnitine
NICETILE 500 mg GASTRORESISTANT TABLETS
NICETYL 500 mg POWDER FOR ORAL SOLUTION
NICETYL 308 mg / mL POWDER FOR ORAL SOLUTION
Why is Nicetile used? What is it for?
Pharmacotherapeutic group
Agonist of mitochondrial function, growth and reparative factors (NGF) with antioxidant activity in neurons of the central and peripheral nervous system.
Therapeutic indications
Mechanical and inflammatory truncular and radicular lesions of the peripheral nerve.
Contraindications When Nicetile should not be used
Individual ascertained hypersensitivity to the product.
Precautions for use What you need to know before taking Nicetile
The oral administration of NICETYL does not require special precautions for use. While the intravenous administration must be carried out slowly. In this last form of administration, redness with a sensation of heat in the face is possible.
Use in case of pregnancy and lactation
Although no harmful effects on the fetus have ever been observed in animal studies, in women in the first trimester of pregnancy and during lactation it will be advisable to administer the drug in cases of real need, under the direct supervision of the doctor.
Interactions Which drugs or foods can modify the effect of Nicetile
There are no known negative interactions with other drugs.
Warnings It is important to know that:
The drug presents no risk of addiction or dependence
Effects on ability to drive and use machines
L-acetylcarnitine has no negative effect on the ability to drive or use machines
Dosage and method of use How to use Nicetile: Dosage
0.5-1.5 g per day in 2-3 administrations, according to medical prescription
The injectable form can be administered both intramuscularly and intravenously
Preparation of the oral solution
Dilute the contents of the bottle with tap water up to the guideline shown on the label (total volume 33 mL).
Each mL of solution contains 308 mg of L-acetylcarnitine internal salt.
The sachets must be dissolved in half a glass of water.
Overdose What to do if you have taken an overdose of Nicetile
There are no known phenomena of overdose with L-acetylcarnitine.
Side Effects What are the side effects of Nicetile
Sporadic cases of mild arousal have been reported which promptly regress with decreasing posology.
Compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects.
It is important to inform the doctor or pharmacist of any undesirable effect, even if not described in the package leaflet.
Expiry and Retention
Warning: do not use the drug after the expiration date indicated on the packaging.
Method of conservation
POWDER AND SOLVENT FOR SOLUTION FOR INJECTION Store in the refrigerator at a temperature between + 2 ° C and + 8 ° C.
POWDER FOR ORAL SOLUTION IN BOTTLE After reconstitution it can be kept for 25 days in the refrigerator.
TABLETS AND POWDER FOR ORAL SOLUTION IN SACHETS Do not store above 25 ° C.
KEEP THE MEDICINAL PRODUCT OUT OF THE REACH AND SIGHT OF CHILDREN
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT
NICETILE
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
500 mg gastro-resistant tablets:
One tablet contains:
Active principle:
L-acetylcarnitine HCl 590.0 mg
(equal to 500 mg of internal salt)
308 mg / ml powder for oral solution:
A 12.316 g bottle contains:
Active principle:
L-acetylcarnitine HCl 12.0 g
(equal to 10.17 g of internal salt)
500 mg powder for oral solution:
One sachet contains:
Active principle:
L-acetylcarnitine HCl 590 mg
(equal to 500 mg of internal salt)
500 mg / 4 ml powder and solvent for solution for injection:
One vial contains:
Active principle:
L-acetylcarnitine 500 mg
For excipients see 6.1.
03.0 PHARMACEUTICAL FORM
Gastro-resistant tablets, powder for oral solution in bottle, powder for oral solution in sachet, powder and solvent for solution for injection.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Mechanical and inflammatory truncular and radicular lesions of the peripheral nerve.
04.2 Posology and method of administration
0.5 - 1.5 g per day in 2-3 administrations, according to medical prescription.
The injectable form can be administered both intramuscularly and intravenously.
Preparation of the solution:
Dilute the contents of the bottle with tap water up to the guideline shown on the label.
The reconstituted solution has a volume of 33 ml and can be stored for 25 days in the refrigerator.
Each ml of solution contains 308 mg of L-acetylcarnitine internal salt.
The sachets must be dissolved in half a glass of water.
04.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients.
04.4 Special warnings and appropriate precautions for use
The drug presents no risk of addiction or dependence.
The oral administration of Nicetile does not require special precautions for use while the intravenous administration must be carried out slowly. In this form of administration, redness with a sensation of heat on the face is possible.
Keep this medicine out of the reach of children.
04.5 Interactions with other medicinal products and other forms of interaction
There are no known negative interactions with other drugs.
04.6 Pregnancy and lactation
Although no harmful effects on the fetus have ever been observed in animal studies, in women in the first trimester of pregnancy and during lactation it will be advisable to administer the drug in cases of real need, under the direct supervision of the doctor.
04.7 Effects on ability to drive and use machines
L-acetylcarnitine does not affect the ability to drive or use machines.
04.8 Undesirable effects
Sporadic cases of mild arousal have been reported which promptly regress with decreasing posology.
04.9 Overdose
No cases of overdose have been reported.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: Agonist of mitochondrial function, growth and reparative factors (NGF) with antioxidant activity in neurons of the central and peripheral nervous system.
ATC: N06BX12
L-acetylcarnitine (gamma-trimethyl-beta-acetyl-butyro-betaine) is the natural isomer of a substance present under physiological conditions in various organs including the brain. It is synthesized by reversible acetylation from carnitine at the mitochondrial level through the "Acetyl-L-Carnitine Transferase enzyme.
L-acetylcarnitine, structurally similar to Acetyl Choline, plays an indispensable role for the correct cellular and transmitting energy metabolism at the level of the CNS.
L-acetylcarnitine, in fact, represents a form of storage of acetyl groups that can be associated with the Coenzyme A necessary to trigger the Krebs cycle, thus intervening both in the metabolism of fatty acids and carbohydrates. In situations of pathology, L-acetylcarnitine has been shown to be active both as a neuroprotection factor for the cell and its organelles, especially the mitochondrion, and as a trophic factor for the restoration of cellular integrity.
In particular in the nervous system, both central and peripheral, on the occasion of insult due to hypoxia, aging, toxic (alcohol, MPTP, MAM), resection or crushing of the nerve, diabetes due to aloxan or streptozocin, L-acetylcarnitine has shown an activity of neuroprotection by intervening on the cascade of events that lead to cell death:
formation of free radicals; accumulation of lipids (from destruction of membranes) responsible for the pathological increase in intramitochondrial calcium;
reduced activity of mitochondrial respiratory complexes;
reduced mitochondrial RNA formation due to reduced DNA transcriptase activity.
L-acetylcarnitine also exerts a trophic action on the nervous system, promoting post-lesional recovery through:
better cellular utilization of NGF (nerve growth factor);
an increase in the neosynthesis of phospholipids for the construction of membranes;
an increase in energy production (ATP) without which reparative mechanisms cannot take place.
In the "animal" the neuroprotective and trophic action of L-acetylcarnitine was highlighted with the maintenance and / or recovery of the trophic (number of neurons) and functional situation: better learning, memory, locomotion skills in various models:
aging;
hypoxia;
Experimental Parkinson's;
microcephaly;
lesions of the peripheral nerve both on a traumatic and disendocrine basis (diabetes).
In men, controlled clinical trials, even of long duration, have been conducted in various pathologies:
involutional syndromes on a degenerative basis
vascular-based involutional syndromes
acute and / or chronic neuropathies on a disendocrine basis (diabetes)
05.2 Pharmacokinetic properties
Intravenous rat blood levels of 333 mg / kg are maximal at 5 min (5375 μmol / l) and decrease in the six hours following administration (106 μmol / l). Orally at the dose of 500 mg / kg the blood peak is reached 4 hours after administration with levels of 40 μmol / l which remain constant up to the 8th hour.
The marked L-acetylcarnitine reaches, largely unchanged, numerous tissues including the brain.
05.3 Preclinical safety data
Non-clinical data reveal no risk for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, reproductive toxicity. Acute toxicity: in mice the LD50 by the i.m. route is higher than 3000 mg / kg, by the i.p. is greater than 3,600 mg / kg, i.v. is greater than 1,600 mg / kg, per os is greater than 18,000 mg / kg; in the rat via i.m. is higher than 3000 mg / kg, by i.p. is 2748 mg / kg, i.v. is 1000 mg / kg, per os is greater than 10,000 mg / kg. Chronic toxicity: mini pigs and rabbits treated for 26 weeks with oral L-acetylcarnitine with doses of 250-500 mg / kg / day and i.m. with doses of 50 mg / kg / day, they did not show significant changes in the course of body weight, blood count, liver function, biochemical blood tests, urinalysis. The macro-microscopic examination of the main organs did not reveal any pathological changes.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
500 mg gastro-resistant tablets:
Polyvinylpyrrolidone, microcrystalline cellulose, magnesium stearate, cellulose acetophthalate, diethylphthalate, dimethicone.
308 mg / ml powder for oral solution:
methyl p-hydroxybenzoate, propyl p-hydroxybenzoate, polyvinylpyrrolidone.
500 mg powder for oral solution:
Precipitated silica, sodium saccharin, hydroxypropylcellulose, 1x1000 tonic water, mannitol.
500 mg / 4 ml powder and solvent for solution for injection:
Mannitol.
One solvent vial contains: water for injections.
06.2 Incompatibility
Incompatibilities with other medicines are unknown.
06.3 Period of validity
Stability is 24 months for gastro-resistant tablets and powder for oral solution in sachets, 36 months for powder for oral solution in bottle and 18 months for powder and solvent for injection vials.
06.4 Special precautions for storage
Powder and solvent for solution for injection:
Store at a temperature between 2 ° C and 8 ° C in the refrigerator.
Tablets and powder for oral solution in sachets:
Do not store above 25 ° C
Powder for oral solution:
The reconstituted solution can be stored for 25 days in the refrigerator.
06.5 Nature of the immediate packaging and contents of the package
Box of 30 gastro-resistant tablets of 500 mg in blister packs
Bottle of powder for oral solution containing 10.17 g of active ingredient
Box of 20 sachets of 500 mg powder for oral solution
5 vials of 500 mg powder for injection + 5 solvent ampoules for injectable use
06.6 Instructions for use and handling
See section 4.2 "Posology and method of administration"
07.0 MARKETING AUTHORIZATION HOLDER
Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
Viale Shakespeare, 47 - 00144 Rome
Factory: Via Pontina km. 30.400 - 00040 Pomezia (Rome)
Dealership for sale
BIOFUTURA PHARMA S.p.A. - Via Pontina km 30,400 00040 Pomezia (RM)
08.0 MARKETING AUTHORIZATION NUMBER
5 vials of 500 mg powder for solution for injection + 5 solvent ampoules AIC n. 025369075
30 gastro-resistant tablets of 500 mg AIC n. 025369048
bottle of powder for oral solution containing 10.17 g of active ingredient - AIC n. 025369063
20 sachets of powder for oral solution of 500 mg - AIC n. 025369051
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
Authorization:
Gastro-resistant tablets and powder for oral solution in sachets: June 1984
Powder for oral solution in bottle: January 1986
Powder and solvent for solution for injection: March 1993
Renewal: June 2000
10.0 DATE OF REVISION OF THE TEXT
01/12/2007