Active ingredients: Metadoxine
METADOXIL 500 mg tablets
METADOXIL 500 mg / 15 ml oral solution
Metadoxil package inserts are available for pack sizes: - METADOXIL 500 mg tablets, METADOXIL 500 mg / 15 ml oral solution
- METADOXIL 300 mg / 5 ml solution for injection
Why is Metadoxil used? What is it for?
METADOXIL contains the active ingredient metadoxine, used in alcohol intoxication. This medicine works by reducing the levels of alcohol in the blood (alcohol) and facilitating its elimination in the urine.
This medicine is indicated in the long-term condition caused by the habitual and prolonged use of alcoholic beverages (chronic alcoholism).
In case of acute alcohol intoxication (acute ethylism), METADOXIL 300 mg / 5 ml solution for injection is indicated.
Contraindications When Metadoxil should not be used
Do not take METADOXIL
- if you are allergic to methadoxine or any of the other ingredients of this medicine
- if you are breast-feeding (see "Pregnancy and breast-feeding" section).
Precautions for use What you need to know before taking Metadoxil
Talk to your doctor or pharmacist before taking METADOXIL.
Take this medicine with caution and tell your doctor if you have Parkinson's disease and are being treated with levodopa, as methadoxine may reduce its effects (see section "Other medicines and METADOXIL").
Children and adolescents
This medicine is not recommended for children and adolescents.
Interactions Which drugs or foods can modify the effect of Metadoxil
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.
Take this medicine with caution and tell your doctor if you are taking levodopa, used to treat Parkinson's disease, as methadoxine can reduce its effects.
Warnings It is important to know that:
Pregnancy and breastfeeding
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.
METADOXIL is not recommended during pregnancy, except in cases of absolute necessity and under direct medical supervision.
Do not take METADOXIL if you are breast-feeding because methadoxine reduces the levels of a hormone, called prolactin, in the blood (hypoprolactin-lowering action) (see section "Do not take METADOXIL").
Driving and using machines
METADOXIL does not affect the ability to drive and use machines.
METADOXIL 500 mg / 15 ml oral solution contains sucrose and methyl parahydroxybenzoate
This medicine contains sucrose, a type of sugar. If you have been told by your doctor that you have "intolerance to some sugars, contact your doctor before taking this medicine. In particular, each vial contains 7.5 g of sucrose. To be taken into consideration in people with diabetes mellitus. May be harmful to people with diabetes. teeth.
METADOXIL 500 mg / 15 ml oral solution contains methyl para-hydroxybenzoate which may cause allergic reactions (including delayed).
Dose, Method and Time of Administration How to use Metadoxil: Posology
Always take this medicine exactly as your doctor or pharmacist has told you. If in doubt, consult your doctor or pharmacist.
METADOXIL 500 mg tablets
The recommended dose is 2 tablets per day to be taken by mouth (orally) in the treatment of chronic conditions.
METADOXIL 500 mg / 15 ml oral solution
The recommended dose is 2 vials per day to be taken by mouth (orally) in the treatment of chronic conditions.
Overdose What to do if you have taken too much Metadoxil
If you take more METADOXIL than you should
There are no known cases of overdose of this medicine.
In case of accidental intake / ingestion of an overdose of METADOXIL, notify your doctor immediately or go to the nearest hospital.
If you forget to take METADOXIL
Do not take a double dose to make up for a forgotten dose.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
Side Effects What are the side effects of Metadoxil
Like all medicines, this medicine can cause side effects, although not everybody gets them.
The following side effects may occur:
Very rare (may affect up to 1 in 10,000 people)
- allergic reactions (hypersensitivity);
- numbness, tingling, tenderness and weakness in the arms and legs (peripheral neuropathy). These symptoms occur especially if you take the medicine for a long time and tend to disappear after stopping the treatment;
- dizziness, disorientation;
- diarrhea, vomiting;
- swelling of the face, lips, mouth, tongue or throat which may cause difficulty in swallowing and breathing (angioedema), skin irritation (rash, hives), itching;
- reduced appetite.
In some cases, it can be difficult to distinguish side effects from underlying disease symptoms
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. You can also report side effects directly via the national reporting system at https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse
By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Keep this medicine out of the sight and reach of children.
Do not use this medicine after the expiry date which is stated on the package after "EXP". The expiry date refers to the last day of that month.
Store at a temperature not exceeding 30 ° C and protected from light.
Do not throw any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.
What METADOXIL contains
METADOXIL 500 mg tablets
- The active ingredient is methadoxine. Each tablet contains 500 mg of methadoxine.
- The other ingredients are: microcrystalline cellulose, magnesium stearate.
METADOXIL 500 mg / 15 ml oral solution
- The active ingredient is methadoxine. Each 15 ml vial contains 500 mg of methadoxine.
- The other ingredients are: sucrose, sorbic acid, sodium edetate, methyl p-hydroxybenzoate, mandarin flavor, purified water.
Description of what METADOXIL looks like and contents of the pack
METADOXIL 500 mg tablets
Box of 30 tablets.
METADOXIL 500 mg / 15 ml oral solution
Box of 10 vials of 15 ml.
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
METADOXIL
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
500 mg tablets : one tablet contains
Active principle: methadoxine (pyridoxol L-2-pyrrolidon-5-carboxylate) 500 mg
300 mg / 5 ml solution for injection : a 5 ml vial contains:
Active principle: methadoxine (pyridoxol L-2-pyrrolidon-5-carboxylate) 300mg
500 mg / 15 ml oral solution : a 15 m vialLcontains:
Active principle: methadoxine (pyridoxol L-2-pyrrolidon-5-carboxylate) 500mg.
For the full list of excipients see section 6.1
03.0 PHARMACEUTICAL FORM
• tablets
• injectable solution
• oral solution
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Acute and chronic ethylism
04.2 Posology and method of administration
Adults
Acute ethylism: 1-2 ampoules intramuscularly or intravenously.
Chronic ethylism: 2 tablets or 2 vials per day orally or one ampoule per day intramuscularly or intravenously.
Children
The use of Metadoxil is not recommended in children and adolescents due to a lack of data on safety and efficacy in this age group.
04.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients. Feeding time.
04.4 Special warnings and appropriate precautions for use
Caution should be exercised in parkinsonians treated with levodopa because the product may reduce its therapeutic efficacy.
Warnings on excipients :
Metadoxil injectable solution contains sodium metabisulfite; this substance can cause allergic reactions and severe asthmatic attacks in sensitive subjects and particularly in asthmatics. The product also contains methyl p-hydroxybenzoate which can cause allergic reactions (even delayed) and, exceptionally, bronchospasm.
Metadoxil oral solution contains methyl p-hydroxybenzoate which may cause allergic reactions (including delayed).
Each vial contains 7.5 grams of sucrose, this should be taken into account in case of diabetes mellitus; it should also be borne in mind that sucrose can be harmful to the teeth.
04.5 Interactions with other medicinal products and other forms of interaction
Methadoxine may increase the peripheral decarboxylation of levodopa, reducing its efficacy.
04.6 Pregnancy and lactation
No clinical data are available on the use of Metadoxil in pregnancy therefore the potential risks for human pregnancy are not known. Metadoxil should therefore not be used in pregnancy unless judged strictly necessary.
Metadoxil is contraindicated during lactation because metadoxine exerts a hypoprolactinemizing action.
04.7 Effects on ability to drive and use machines
No studies on the ability to drive and use machines have been performed; however, there are no known negative effects of Metadoxil on these functions.
04.8 Undesirable effects
Adverse drug reactions have been reported very rarely; It should be noted that in some cases it may be difficult to distinguish adverse events from underlying disease symptoms.
Prolonged use may rarely lead to the onset of peripheral neuropathies which regress after some time from the suspension of therapy.
Adverse reactions reported, resulting from both clinical studies and post-marketing as spontaneous reports from healthcare professionals, are listed below, by system organ class and frequency.
Frequency is defined as: very common (≥ 1/10), common (≥ 1/100,
(≥ 1/1.000,
frequency class, undesirable effects are reported in order of decreasing severity.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions occurring after authorization of the medicinal product is important as it allows continuous monitoring of the benefit / risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system. "address https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse.
04.9 Overdose
There have been no reports of overdose with the use of methadoxine and therefore no experience is available. If overdose occurs, the patient should be monitored and treatment directed at symptom management.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: Drugs used in alcohol dependence: ATC code: N07BB.
Experimental Pharmacology: Methadoxine decreases the alcohol level and the duration of exposure of the tissues to the damaging action of alcohol by facilitating the metabolism and increasing the urinary elimination of alcohol and its toxic metabolite: acetaldehyde. It carries out a protective action on the cell, preventing alterations deriving from redox imbalance, in fact it facilitates the oxidation of excess NADH, keeps glutathione levels high, helping to safeguard the membranes from lipoperoxidative damage, opposes the fall in hepatic and cerebral levels of ATP, stimulating its "de novo" synthesis. It also acts on neurotransmitters, increasing the release of GABA and acetylcholine. Finally, metadoxine has been recognized as having anti-emetic properties.
Clinical Pharmacology:
Treatment with metadoxine in acute alcoholism has allowed to highlight the efficacy and rapidity of action on the excitomotor component of acute alcoholic intoxication. In chronic alcoholism, without alcohol abstinence during treatment, a trend towards statistically significant normalization of serum biochemical parameters such as gGT (main altered marker in chronic alcoholism), bilirubin and GOT is generated. Finally, in the alcoholemic load curves, in the healthy subject, a more rapid kinetics of elimination of alcohol from the blood were highlighted and an approach to the limit levels of the ornithyl-carbamyl-transferase (OCT) enzyme that reports, especially in the liver, damage to the mitochondrial apparatus, generator of chemical energy.
05.2 "Pharmacokinetic properties
The oral absorption of 20 and 50 mg / kg of medication corresponds to 60 - 80% after 3 hours (dog). Intravenously the same rates are reached in 25 min. In correspondence with the respective plateaux (about 3 hours orally and 1 hour by vein) no noticeable increase in urinary excretion is noted. This means that methadoxine is involved in the metabolism of amino acids and pyridoxine.
05.3 Preclinical safety data
The toxicity of the product was found to be very low. The lethal dose 50 i.v. corresponds to 3480 mg / kg (mouse), while via i.p. the LD50 is higher than 6 g / kg (rat). Subacute toxicity was tested for 40 days in 3 animal species at 2 dose levels of which the higher was 1.5 g / kg orally. The humoral findings and the autopsy examination did not show deviations from the norm. Subchronic toxicity was evaluated with oral treatment in the dog and in the rat continued for 26 weeks. In the dog, motility disturbances appeared for doses corresponding to 0.5 g / kg of body weight In summary, it can be said that METADOXIL has revealed low toxic properties for both acute and chronic treatment. Mutagenesis: Negative investigations for tests used internationally (Ames test and tests on mammalian cells cultured in vitro). Teratogenesis: No harmful effects were noted in female rats and rabbits in gestation, nor teratogenic activity on fetuses and offspring
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
500mg tablets:
Excipients: microcrystalline cellulose, magnesium stearate.
300mg / 5ml solution for injection:
Excipients: sodium metabisulfite, sodium edetate, methyl p-hydroxybenzoate, water for injections.
500mg / 15ml oral solution:
Excipients: sucrose, sorbic acid, sodium edetate, methyl p-hydroxybenzoate, mandarin aroma, purified water.
06.2 Incompatibility
In the absence of incompatibility studies, the medicinal product must not be mixed with other products
06.3 Period of validity
Tablets: 5 years, unopened;
Oral solution: 3 years, in unopened packaging.
Solution for injection: 3 years, when unopened.
06.4 Special precautions for storage
Store at a temperature not exceeding 30 ° C and protected from light.
06.5 Nature of the immediate packaging and contents of the package
- Tablets: blister of PVC / PE / PVDC-Aluminum coupled. Box containing 30 tablets.
- Injectable solution: neutral colored glass vials. Box containing 10 vials of 5 ml.
- Oral solution: glass bottles. Carton containing 10 vials of 15 ml.
06.6 Instructions for use and handling
No special instructions.
07.0 MARKETING AUTHORIZATION HOLDER
Laboratori Baldacci S.p.A., Via San Michele degli Scalzi 73 - Pisa.
08.0 MARKETING AUTHORIZATION NUMBER
500 mg tablets-30 tablets AIC 025316011
300mg / 5ml solution for injection - 10 ampoules 5ml AIC 025316023
500mg / 15ml oral solution - 10 vials of 15ml AIC 025316035
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
July 1984 / June 2010
10.0 DATE OF REVISION OF THE TEXT
15 October 2015
