Baclofen: effects and consequences of use

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Attention! The material contains information about substances, the use of which can cause serious harm to your health!

Article prepared by an expert

Terekhova Anna Vladimirovna

Psychologist-consultant on socio-psychological work with addicted clients and their families. Experience in the field of rehabilitation and social adaptation of persons with dependent behavior for more than 9 years.

Read in the article:

1. What is baclofen
2. Non-medical use
3. Symptoms of using baclofen
4. Health implications
5. Addiction treatment

Among people who use psychoactive substances, the medical drug Baclofen is in demand. It is called a “cheap high” at an affordable price. Baclofen is prescribed to relieve pain; it has a calming effect after a stroke, atherosclerosis, and meningitis. The strong effect of the drug, its ability to cause euphoria, its prevalence in pharmacies and low cost have made Baclofen one of the most popular drugs among drug addicts.

Release form, composition and packaging

Pills

white, round, biconvex, with a dividing line.

Excipients:

lactose, potato starch, gelatin, talc, magnesium stearate, ethylcellulose.

50 pcs. - polypropylene cans (1) - cardboard packs.

Pills

white, round, biconvex.

Excipients:

lactose, potato starch, gelatin, talc, magnesium stearate, ethylcellulose.

50 pcs. - polypropylene cans (1) - cardboard packs.

pharmachologic effect

Centrally acting muscle relaxant; GABAB receptor agonist. By reducing the excitability of the terminal sections of afferent sensory fibers and suppressing interneurons, it inhibits mono- and polysynaptic transmission of nerve impulses; reduces pre-tension of muscle spindles. Does not affect the transmission of impulses at neuromuscular synapses. For neurological diseases accompanied by spasticity of skeletal muscles, it weakens painful spasms and clonic convulsions. Increases the range of motion in the joints, facilitates passive and active kinesitherapy (physical exercises, massage, manual therapy).

special instructions

Side effects of Baclofen may be transient. It is important to be able to distinguish side effects from signs of the underlying disease.

For patients with epilepsy, the drug is prescribed without concomitant withdrawal of antiepileptic drugs.

In case of diabetes mellitus , pathologies of the liver system, regular monitoring of blood sugar levels and the activity of liver enzymes is carried out.

Baclofen affects concentration and driving.

Pharmacokinetics

Suction

After oral administration, baclofen is quickly and completely absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved 2-3 hours after taking the drug.

Distribution

Plasma protein binding is about 30%. Baclofen penetrates the placental barrier and is excreted in breast milk.

Metabolism

Metabolized in the liver.

Removal

It is excreted in the urine, mainly unchanged.

Baclofen

Baclofen
(lat.
baclofen
) is a muscle relaxant, antispastic medicine.

Baclofen is a chemical compound

Baclofen is a white or almost white crystalline powder, almost odorless. Slightly soluble in water, very slightly soluble in methanol and insoluble in chloroform. Chemical name of baclofen: (RS)-4-amino-3-(4-chlorophenyl)butanoic acid. Empirical formula: C10H12Cl NO2.

Baclofen is a medicine

Baclofen is the international nonproprietary name (INN) of the drug. According to the pharmacological index, baclofen belongs to the group “Neurotropic drugs”, the subgroup “Drugs affecting neuromuscular transmission”. According to ATC, baclofen is included in the group “M03. Muscle relaxants" and has the code M03BX01. Baclofen ® is also the trade name of the drug.

Indications for use of baclofen

Baclofen is used for spastic muscle conditions in multiple sclerosis, strokes, traumatic brain injury, spinal cord lesions, strokes, cerebral palsy, meningitis, inflammation of the meninges.

Baclofen in gastroenterology

Baclofen, being an agonist of γ-aminobutyric acid (GABA) - GABA-B receptors, is a drug that affects the severity of GERD symptoms, the mechanism of action of which is due to the inhibition of transient relaxations (spontaneous relaxations) of the lower esophageal sphincter (LES) - reducing their frequency and duration .
Taking baclofen 5–10 mg 4 times a day for 4 weeks is accompanied by a decrease in the severity and frequency of symptoms of both erosive and non-erosive esophageal reflux disease. Baclofen (as well as other drugs that are not yet available in Russia, cholecystokinin-A antagonists and NO synthetase inhibitors: dexloxiglumide, devazepid, asperlicin; all of these drugs can be classified as modern prokinetics) improves motility of the upper gastrointestinal tract, including by inhibiting spontaneous relaxations of the LES ( Starostin B.D., Starostina G.A.). Baclofen, which inhibits short-term relaxation of the LES, reduces both the number of episodes of acid and non-acid reflux and the frequency of symptoms that occur after eating. In addition, baclofen reduces acid reflux and significantly reduces the severity of symptoms. However, due to side effects on the central nervous system, baclofen is not acceptable for all patients in whom it could have an effect (Neeraj Sharma et al). Baclofen is the only drug that reduces the number of transient relaxations of the LES and thus reduces the number of reflux episodes. In experimental studies, baclofen shows good results. However, its therapeutic band is very narrow and baclofen has not found use in gastroenterology (Trukhmanov A.S.).

Baclofen is not recommended for stomach and/or duodenal ulcers.

As a GABA-B receptor agonist, baclofen not only reduces the number of transient LES relaxations (TRNSR) in both animals and humans, but also reduces the number of episodes of acid and weak acid reflux in healthy volunteers and in patients suffering from GERD. Given that baclofen therapy can provoke the development of dizziness and drowsiness, in order to avoid GABA-mediated side effects from the central nervous system (CNS), more powerful peripherally acting GABA-B receptor agonists, or baclofen prodrugs, have been developed: arbaclofen and lezogaberan . But, unfortunately, although these drugs reduce the number of PRNPS by approximately 30–40%, their low clinical effectiveness and side effects (hepatotoxicity, side effects from the central nervous system) led to the cessation of their use in clinical practice, as well as to the cessation of the development of new reflux inhibitors (Kahrilas PJ and others).

About 15 years ago, references appeared in the literature about the ability of the GABA(B) receptor agonist baclofen to reduce the number of spontaneous relaxations of the LES in patients with GERD. A meta-analysis of 5 controlled studies showed that the use of baclofen reduces the number of episodes of spontaneous relaxation of the LES and the duration of decrease in esophageal pH. However, baclofen was never introduced into widespread clinical practice, since its use is limited by such serious neurological side effects as dizziness and confusion (Sheptulin A.A. et al.).

Baclofen is used to treat patients who have a positive relationship between symptoms of GERD (heartburn or regurgitation) and normal levels of non-acid reflux (pH 4.0-6.5). It is prescribed to patients with a similar pathology at a starting dose of 5 mg three times a day, with a possible dose increase to 20 mg three times a day. Baclofen significantly reduces symptoms, reduces postprandial acid and non-acid (duodenogastroesophageal) reflux, recorded using impedance pH-metry (Pasechnikov V.D.).

Materials for healthcare professionals regarding the use of baclofen in gastroenterology

Literature

• Stepanov Yu.M., Arbi Mohamed. The effectiveness of baclofen in the treatment of GERD refractory to antisecretory therapy // RZHGGK. - 2010. - T.20. - No. 5. - Adj. No. 36. — P.159.
• Starostin B.D., Starostina G.A. GABAb receptor agonists for GERD // Gastroenterology of St. Petersburg. - 2011. - No. 2-3. - With. M86.
• Ciccaglione AF, Marzio L. Effect of acute and chronic administration of the GABAB agonist baclofen on 24 hour pH metry and symptoms in control subjects and in patients with gastro-oesophageal reflux disease // BMJ Publishing Group & BSG. 2003;52:464-470.

On the website in the “Literature” section there are subsections “Prokinetics-stimulants of gastrointestinal motility” and “Anspasmodics”, containing publications for healthcare professionals addressing the use of prokinetics and antispasmodics in the treatment of diseases of the gastrointestinal tract.

Video

Still from video: Simanenkov V.I. Acid suppressive therapy for refractory forms of GERD

Still from the video with simultaneous translation into Russian: Bisschops R. European standards for the diagnosis and treatment of erosive and non-erosive esophagitis

On the website in the “Video” section there is a subsection for patients “Popular Gastroenterology” and a subsection “For Doctors”, containing video recordings of reports, lectures, webinars in various areas of gastroenterology for healthcare professionals.

How to take baclofen and dosage

Baclofen is taken orally.
Adults at the beginning of treatment: 5 mg of baclofen 3 times a day. On every fourth day of therapy, the single dose is increased by 5 mg until the optimal therapeutic effect is obtained. The average daily dose is 30–75 mg; if necessary, it can be increased to 100–120 mg. The final daily dose of baclofen is set individually so that, along with the weakening of clonus and muscle spasm, muscle tone is maintained sufficient for active movements. For patients with hypersensitivity to drugs, the initial dose may be 5-10 mg of baclofen per day, followed by a slower increase. For patients with renal failure, as well as with hemodialysis, the dose of baclofen is 5 mg per day. For children under 10 years of age, the daily dose is 0.75–2 mg per kg of weight, over 10 years of age - 2.5 mg per kg of weight. Treatment begins with a dose of 2.5 mg 4 times a day. The daily dose, as in adults, is selected individually, increasing it every three days. The maintenance daily dose for children 1-2 years old is 10-20 mg, for children 2-10 years old - 30-60 mg.

Special instructions for treatment with baclofen

It is recommended to select an individual dose in a hospital setting.
Side effects usually disappear or decrease as the dose is reduced. There is rarely a need to discontinue treatment with baclofen. Side effects of baclofen should be distinguished from the symptoms of the disease for which therapy is being administered. Baclofen is discontinued gradually, reducing the dose over 1–2 weeks, unless serious side effects occur.

Baclofen is used with caution in cerebrovascular disorders, psychotic conditions, schizophrenia, respiratory disorders, liver and kidney dysfunction, as well as in older patients. With concomitant epilepsy, treatment is carried out under strict medical supervision and without interrupting adequate therapy with anticonvulsants. Patients with dysuria treated with baclofen may experience bladder sphincter hypertonicity and urinary retention. In patients with liver disease and diabetes mellitus, it is necessary to monitor the level of liver transaminases, alkaline phosphatase and blood sugar.

During therapy with baclofen, you should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions, including driving.

Restrictions on the use of baclofen

• stomach ulcer
• duodenal ulcer
• renal dysfunction
• age up to 12 years

Use of baclofen during pregnancy, lactation and in infants

The use of baclofen during pregnancy is possible only if the expected effect of therapy outweighs the potential risk to the fetus. Baclofen has an FDA Fetal Category of C (animal studies have shown adverse effects on the fetus and there have been no adequate studies in pregnant women, but the potential benefit associated with the use of this drug in pregnant women may justify its use despite existing risk). Breastfeeding is discontinued while taking baclofen and can be resumed after stopping taking baclofen. Baclofen is not prescribed for children under 12 years of age.

Side effects of baclofen

Nervous system and sensory organs:
drowsiness, insomnia, dizziness, headache, weakness, fatigue, confusion, imbalance, decreased reaction speed, mental agitation, euphoria, hallucinations, depression, nightmares.
Cardiovascular system:
arterial hypotension, palpitations, chest pain, collapse.
Digestive system:
aversion to food, perversion of taste, nausea, vomiting, constipation, dyspeptic symptoms, abdominal pain.
Genitourinary system:
involuntary urination, enuresis, urinary retention, anuria, hematuria, impotence, ejaculation disorders.
Respiratory system:
feeling of nasal congestion and suffocation, respiratory depression.
Others
: muscle pain, skin rash, itching, swelling of the feet, sweating, weight gain, paradoxical reaction.

Pharmacodynamics of baclofen

Baclofen is quickly and completely absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved 2–3 hours after administration. Plasma protein binding of baclofen is approximately 30%. Penetrates the placental barrier and is excreted in breast milk. Baclofen is metabolized in the liver. It is excreted in the urine, mainly unchanged.

Brands of medicines containing the active ingredient baclofen

Currently, two drugs with the active ingredient baclofen are registered in Russia: Baklosan ® and Lioresal ® intrathecal. The trademark Baclofen ® was also previously registered. Brands with the active ingredient baclofen sold in Western countries: Kemstro ®, Lioresal ®.

Instructions for use of baclofen

For Russia (in Russian, pdf):

• Instructions from the manufacturer Pharmaceutical JSC, Poland (pdf): “Instructions for medical use of the drug Baklosan”, tablets 10 and 25 mg.
• Instructions from the manufacturer Novartis Pharma Stein AG, Switzerland, “Instructions for medical use of the drug Lioresal Intrathecal”, solution for intrathecal administration.

For the USA (in English, pdf):

• "Lioresal Intrathecal (baclofen injection)", manufacturer Novartis Pharma Stein AG, Stein, Switzerland

Baclofen has contraindications, side effects and application features; consultation with a specialist is necessary. Back to section

Dosage regimen

Installed individually.

Adults Baclofen /baclosan/

the drug is prescribed at an initial dose of 5 mg 3 times a day; gradually increase the dose every 3 days until the optimal therapeutic effect develops (usually up to 30-75 mg/day). For patients who require the use of the drug in higher doses (usually up to 30-75 mg/day), Baklosan is prescribed in tablets of 25 mg. The maximum daily dose is 100 mg.

In patients over 65 years of age

The dose of the drug should be increased with caution due to the increased risk of side effects.

Initial single dose of the drug for children

is 5 mg, dosage frequency 3 times/day.
If necessary, increase the dose every 3 days with caution. The average recommended doses are for children aged 1 to 2 years
- 10-20 mg/day,
from 2 to 6 years
- 20-30 mg/day,
from 6 to 10 years
- 30-60 mg/day.
In children over 10 years of age,
the maximum daily dose is determined at the rate of 1.5-2 mg/kg body weight.

The drug is taken with meals. If you miss the next dose, you should not take a double dose of the drug.

Contraindications

Baclofen is not used for Parkinson's disease, psychosis, a history of seizures, epilepsy, intolerance to the main substance, cerebral atherosclerosis , or chronic renal failure.

During pregnancy, ulcerative lesions of the digestive tract, cerebrovascular insufficiency, breastfeeding , children under 12 years of age and the elderly, Baclofen is prescribed with caution.

Side effect

From the central nervous system and peripheral nervous system:

drowsiness, dizziness, gait disturbance, increased fatigue, confusion, apathy, euphoria, depression, paresthesia, ataxia, tremor, nystagmus, accommodation paresis, hallucinations, convulsions, decreased seizure threshold.

From the digestive system:

nausea, vomiting, dry mouth, constipation, diarrhea.

From the urinary system:

urinary retention, dysuria, enuresis; with long-term use - impaired renal function.

From the cardiovascular system:

decrease in blood pressure.

Other:

myalgia, muscle weakness.

Storage conditions and periods

List B. The drug should be stored in a dry place, protected from light and out of reach of children, at a temperature not exceeding 25°C. Shelf life: 5 years.

Baclofen (baclosan) is a good choice. The quality of goods, including Baclofen /baclosan/, undergo quality control by our suppliers. You can buy Baclofen /baclosan/ on our website by clicking on the “Add to cart” button. We will be happy to deliver Baclofen /baklosan/ to you at any address within our delivery area indicated in the “Delivery” section, or you can order Baclofen /baklosan/ for pickup.

Reviews of Baclofen

An effective drug to combat muscle stiffness. Quickly relaxes stiff muscles, eliminates clonic convulsions and spasms.

Reviews of Baclofen often mention side effects of the drug, such as nausea and vomiting.

The medication can also cause drug addiction, the consequences of which can be very sad, even death. Addicts typically consume large amounts of this drug, experiencing severe side effects, in an attempt to achieve the desired psychedelic state. Baclofen in large dosages “rushes” or causes a so-called “trip”, which can result in a dropper or death.

Dependence on this type of substance is very dangerous, since quitting drugs is always more difficult than starting.