LIORESAL ® - Baclofen

LIORESAL ® is a medicinal product based on a racemic mixture of Baclofen isomers

THERAPEUTIC GROUP: Central-acting muscle relaxants

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications LIORESAL ® - Baclofen

LIORESAL ® is a medicinal specialty indicated in the treatment of spastic hypertonia of the skeletal musculature during pathologies such as multiple sclerosis, spastic muscular hypertonia due to bone marrow, infectious, degenerative, traumatic or neoplastic diseases, amyotrophic lateral sclerosis, spastic spinal paralysis, compression medullary, paraplegia or traumatic paraparesis, spinal cord compression and central muscular hypertonia.

Mechanism of action LIORESAL ® - Baclofen

LIORESAL ®, a medicinal specialty used in the treatment of central pathologies characterized by muscular hypertonicity, is a drug consisting of the various isomers of Baclofen, chemically known as beta aminomethyl-para-chlorohydrocinnamic acid.

Taken orally it is rapidly absorbed from the gastrointestinal tract, with very high bioavailability, reaching the maximum plasma concentration between 30 and 90 minutes; partially bound to plasma proteins, Baclofen reaches the central nervous system where it performs its therapeutic action, interacting and activating receptors for GABA.

This action results in a control of the release of excitatory neurotransmitters, thereby reducing muscle tone, clonus and associated pain, as well as clearly improving muscle mobility.

Following a half-life of about 3 - 4 hours, the Baclofen is eliminated mainly unchanged by the urine and only in 5% with the faeces.

Studies carried out and clinical efficacy

SELECTIVITY OF ACTION OF BACLOFENE

J Neurosci. 2013 Jul 31; 33 (31): 12898-907. doi: 10.1523 / JNEUROSCI.1552-13.2013.

Interesting study that tries to characterize from the molecular point of view the activity of the Baclofen, describing the greater activity of this active principle on the spinal rather than cortical GABA receptors. This selectivity would explain the reduced ability of the Baclofen to influence voluntary movements.

BACLOFENE IN PSYCHIATRIC DISEASES

Alcohol Alcohol. 2013 Nov 12. [Epub ahead of print]

Interesting study that seeks to characterize the therapeutic management system of alcoholic patients with psychiatric illnesses that arose following intoxication with Baclofen.

The evidence therefore, in addition to providing a therapeutic system of emergency management, suggest particular caution in the use of Baclofen in patients with psychiatric pathologies with previous suicide attempts.

BACLOFENE IN THE TREATMENT OF ALCOHOLISM

Eur Neuropsychopharmacol. 2013 Oct 1.

French study that seeks to characterize the safety and efficacy of the use of Baclofen in the treatment of alcoholism, following over 650 patients.

The evidences, generally positive, show however the necessity to modulate the dosage in patients with contextual psychiatric pathologies, and underlines the continuous increase relative to the use of this active principle.

Method of use and dosage

LIORESAL ®

10 - 25 mg tablet of Baclofen.

The definition of the therapeutic scheme is up to the doctor who is expert in the treatment of muscular diseases on a neurological basis, after having carefully evaluated the patient's overall health and the severity of his clinical picture.

The dosage, which varies from individual to individual, should be formulated in such a way as to guarantee the use of the lowest possible level necessary to guarantee the therapeutic effect, taking care however to modulate the dosage based on clinical needs.

An adjustment of the dosages normally used, for example, would be necessary in patients suffering from renal diseases, for which the excretion of the final metabolite is compromised.

Warnings LIORESAL ® - Baclofen

The therapy with LIORESAL ® must necessarily be defined and supervised by a specialist doctor in the treatment of muscular diseases on a nervous basis, so that it can periodically assess its clinical efficacy and safety of use, avoiding the onset of clinically relevant adverse reactions.

The particular mechanism of action of LIORESAL ® imposes the maximum caution in the use of the drug in patients suffering from psychiatric or neurological pathologies, epilepsy, renal insufficiency, peptic ulcer and urinary retention syndromes.

Particular caution should also be used in the therapy interruption phase, avoiding the abrupt elimination, potentially associated with the risk of hallucinations, confusional states, psychotic states, manic with a consequent worsening of the patient's clinical conditions.

LIORESAL ® contains among its excipients wheat starch, a potential source of gluten, fortunately in quantities that are generally tolerated even by patients with celiac disease.

It is recommended to keep the medicine out of the reach of children.

PREGNANCY AND BREASTFEEDING

The ability of Baclofen to easily cross the placental barrier and concentrate in pharmacologically active doses in breast milk, extends the aforementioned contraindications to the use of LIORESAL ® also to pregnancy and the subsequent period of breastfeeding.

Interactions

In order to reduce potential variations in the therapeutic efficacy of Baclofen, the patient receiving LIORESAL ® should avoid the simultaneous intake of alcohol and drugs active on the central nervous system.

In the same way, the patient receiving LIORESAL ® should avoid taking drugs that can aggravate renal function, thus increasing the risk of Baclofen toxicity.

Contraindications LIORESAL ® - Baclofen

The use of LIORESAL ® is contraindicated in patients suffering from severe kidney disease and in patients with hypersensitivity to the active ingredient or to one of its excipients.

Undesirable effects - Side effects

Therapy with LIORESAL ® could expose the patient to the risk of side effects such as sedation, drowsiness, respiratory depression, apathy, fatigue, confusion, headache, insomnia, euphoria, dry mouth, tremors, ataxia, visual disturbances, nausea, malaise gastrointestinal, hyperhidrosis, skin rash, dysuria, and in some cases even hypotension.

Therefore, given the frequency of the aforementioned side effects, the need for continuous medical supervision appears evident.