Dependence and effect of baklosan on the human body

Osteochondrosis (degenerative disc disease) in the lumbar spine or lower back is caused by involutional changes in the discs, which leads to lower back pain.

Intervertebral discs are tough, fibrous structures that act as ligaments between vertebrae, absorbing shock and providing shock absorption to the spine. The discs are flexible but strong enough to facilitate movements such as bending your torso forward, backward or sideways.

Despite the name, osteochondrosis is not considered a true disease and symptoms usually do not worsen over time. Discs, like all structures of the body, degrade as we age, and disc degeneration develops in all people as part of the involutionary process.

A characteristic feature of osteochondrosis is a gradual decrease in symptoms as the spine begins to stabilize. Treatment for lumbar spine degenerative disc disease focuses on minimizing pain, stabilizing the spine, and improving or maintaining mobility.

Content:

1. General information
2. For what pathologies is Baklosan dangerous?
3. Baklosan: side effects
4. Addiction
5. Abstinence
6. Overdose

Many drugs that are produced to treat various pathologies have a pronounced narcotic effect. Baklosan is one of these - dependence on it (first mental, then physical) develops quite quickly. This must be taken into account when prescribing it, so that an ordinary patient does not turn into a drug addict.

Help with withdrawal symptoms

Many people, faced with the problem of drug addiction in their family, and seeing how bad a loved one is during the period of drug withdrawal, do not know how to ease withdrawal. Help includes:

1. Consultation with a narcologist.
2. Visiting a specialized clinic.
3. Detoxification in a hospital setting.
4. Maintenance drug therapy to restore physical health.
5. Correction of psycho-emotional disorders.

Anti-withdrawal medications are selected by the doctor individually for each patient. Based on the condition of his body and concomitant diseases. Then there is a long road of rehabilitation and social adaptation ahead. But if a person lacks desire and motivation, and without the support of loved ones, drug use can resume at any time.

General information

Baclosan is the trade name for the muscle relaxant baclofen. It is a stimulator of GABA - gamma-aminobutyric acid, the presence of which determines the processes of excitation and inhibition in the tissues of the central nervous system. The substance is well absorbed in the lumen of the small intestine, from where it enters the bloodstream. Baklosan is excreted from the body in urine (mostly unchanged).

With its help, pathological conditions such as:

• reversible spasticity - spasm or involuntary muscle contraction;
• consequences of multiple sclerosis - a chronic autoimmune disease accompanied by damage to the myelin sheath of nerve fibers;
• residual effects that occur after various spinal cord lesions.

Baklosan treats spasticity, which is bothersome when:

• cerebrovascular disorders;
• traumatic brain injuries;
• spinal cord lesions;
• cerebral palsy - a group of brain pathologies that arise due to its underdevelopment or injury during pregnancy or childbirth and are manifested by motor, speech, and mental disorders.

The product is also used in complex therapy:

• alcoholic liver disease;
• alcohol addiction;
• trigeminal neuralgia;
• gastroesophageal reflux - a pathology in which the contents of the stomach are thrown into the esophagus.

Baklosan not only eliminates muscle spasm, but also:

• relieves muscle tension;
• worsens spinal reflexes - urination, defecation and others;
• reduces muscle pain.

Exercise therapy and activity modification

Exercise is essential to maintaining healthy spinal mobility. An effective exercise program for the lumbar spine should include:

• Stretching exercises for the muscles of the lower back, hips and pelvis, as well as the harmstring muscles. Tightening of these muscles increases pressure on the lumbar spine and contributes to the development of lower back pain.
• Strengthening your lower back and abdominal muscles helps you maintain good posture and better support your spine. A muscle strengthening exercise program may include an individual exercise program, dynamic lumbar spine stabilization, tai chi, Pilates, or others.
• Low-impact aerobic exercise, which increases your heart rate, improves blood circulation and the supply of nutrients and oxygen needed to repair body tissues. For example, this could be walking, swimming and water aerobics.

Exercise programs are usually tailored on a case-by-case basis, depending on your overall health, severity of pain, and personal preference.

In addition, small adjustments to daily activities (lifestyle modifications) can effectively alleviate pain. For example, wearing a brace when lifting heavy objects or avoiding twisting when lifting heavy objects can prevent increased pain due to excessive stress on the discs. Using an ergonomic chair and orthopedic mattress can also improve your posture and reduce stress on your discs.

For what pathologies is Baklosan dangerous?

The drug used in a therapeutic dose has contraindications. If a drug addict is unable to refuse the drug being described, then he should at least understand for what pathologies Baklosan is contraindicated. This:

• Parkinson's disease is a degenerative lesion of nervous tissue that causes trembling of the arms and legs, stiffness, and slowness of movements;
• cerebrovascular insufficiency - a disorder of cerebral circulation due to vascular damage;
• persistent renal failure - deterioration of kidney function;
• atherosclerosis of cerebral vessels - deposition of cholesterol plaques on their inner surface;
• peptic ulcer of the stomach and duodenum - the formation of one or more deep defects in the wall of these organs.

Choice of pharmacological therapy for spastic muscle hypertonicity

The main drugs used to reduce muscle tone are muscle relaxants. According to the mechanism of action, muscle relaxants are distinguished between central action (affect the synaptic transmission of excitation in the central nervous system) and peripheral action (inhibit the direct excitability of striated muscles). When using muscle relaxants, quite significant side effects can occur, which must be carefully assessed when choosing a drug [1, 2].

When choosing antispastic drugs, they mainly take into account their ability to inhibit polysynaptic reflexes (reducing spasticity), while having the least effect on monosynaptic reflexes (muscle strength). An antispastic drug should reduce muscle spasticity with a minimal decrease in muscle strength [3, 4].

Drug therapy is based on the use of tablet and injection forms. Antispastic agents used internally, by reducing muscle tone, can improve motor functions, facilitate care for an immobilized patient, relieve painful muscle spasms, enhance the effect of physical therapy, and prevent the development of contractures [5]. With mild spasticity, the use of muscle relaxants can lead to a significant positive effect, but with severe spasticity, large doses of muscle relaxants may be required, the use of which often causes unwanted side effects. Treatment with muscle relaxants begins with a minimum dose, then it is slowly increased to achieve effect [6].

The centrally acting muscle relaxants most often used in Russia for the treatment of spastic muscle hypertonicity include baclofen, tizanidine, tolperisone, and diazepam [7, 8].

Baclofen (Baklosan, Lioresal) has an antispastic effect mainly at the spinal level. The drug is an analogue of gamma-aminobutyric acid (GABA), which binds to presynaptic GABA receptors, leading to a decrease in the release of excitatory amino acids (glutamate, aspartate) and suppression of mono- and polysynaptic activity at the spinal level, which causes a decrease in spasticity. The drug also exhibits a moderate central analgesic effect. Baclofen is used for spinal and cerebral spastic muscle hypertonicity of various origins. The initial dose is 5–15 mg/day (in one or three doses), then the dose is increased by 5 mg every day until the desired effect is obtained. The drug is taken with meals. The maximum dose of baclofen for adults is 60–75 mg/day. Side effects often include sedation, drowsiness, decreased concentration, dizziness, and often subside during treatment. Nausea, constipation and diarrhea, arterial hypertension, increased ataxia, and the appearance of paresthesia may occur. Caution is required when treating elderly patients, patients who have had a stroke, patients with gastric and duodenal ulcers. Baclofen is contraindicated in case of epilepsy or a history of seizures [9, 10].

For severe spasticity, when the usual oral use of antispastic drugs is not effective, intrathecal administration of baclofen is indicated, which was first proposed in 1984 by R. Penn. To achieve the required concentration of the drug in the cerebrospinal fluid, it is necessary to take quite significant doses of baclofen, which can lead to disturbances of consciousness, drowsiness, and weakness. Therefore, systems have been developed that deliver baclofen directly into the intrathecal space of the spinal cord using the intrathecal baclofen pump system. In this case, the clinical effect is achieved with much smaller doses of baclofen than when using tablet forms [11, 12].

This system consists of a reservoir containing baclofen or a similar drug, a pump (pump), with the help of which the drug is dosed into the intrathecal space of the spinal cord through a lumbar catheter and a power supply. From the reservoir, baclofen enters directly into the cerebrospinal fluid, and its dosage is controlled by a special radiotelemetry device. The amount of drug entering the cerebrospinal fluid can be changed depending on the clinical picture. Baclofen is added to the reservoir after 2–3 months using percutaneous puncture [13].

The use of a baclofen pump improves the speed and quality of walking of patients with unfixed reflex contractures caused by high spasticity of synergistic muscles and imbalance of antagonist muscles. The existing 15-year clinical experience of using baclofen intrathecally in patients who have suffered a stroke indicates the high effectiveness of this method in reducing not only the degree of spasticity, but also pain syndromes and dystonic disorders. A positive effect of the baclofen pump on the quality of life of stroke patients was noted [14].

Tizanidine (Sirdalud) is a centrally acting muscle relaxant, an alpha-2 adrenergic receptor agonist. The drug reduces spasticity due to suppression of polysynaptic reflexes at the level of the spinal cord, which can be caused by inhibition of the release of excitatory amino acids L-glutamate and L-aspartate and activation of glycine, which reduces the excitability of spinal cord interneurons. Tizanidine also has a moderate central analgesic effect. The drug is effective for cerebral and spinal spasticity, as well as for painful muscle spasms. The initial dose of the drug is 2–6 mg/day in one or three doses; with individual selection, the dose is increased on days 3–4 by 2 mg. When taken orally, the effect of the drug appears within 30–45 minutes, the maximum effect occurs within 1–2 hours. The average therapeutic dose is 12–24 mg/day, the maximum dose is 36 mg/day. Side effects may include drowsiness, dry mouth, dizziness and decreased blood pressure, which limits the use of the drug for post-stroke spasticity. The antispastic effect of tizanidine is comparable to the effect of baclofen, however, tizanidine, with adequate dosage selection, is better tolerated, since it does not cause general muscle weakness and does not increase muscle weakness in the paralyzed limb [15, 16].

Tolperisone (Mydocalm) is a centrally acting antispastic drug that inhibits the caudal part of the reticular formation and has N-cholinolytic properties. Tolperisone reduces the activity of spinal neurons involved in spasticity by limiting the flow of sodium across the nerve cell membrane. The most commonly used dose is 300–450 mg/day in two or three doses. A decrease in muscle tone when tolperisone is prescribed is sometimes accompanied by a vasodilator effect, which should be taken into account when prescribing to patients with a tendency to arterial hypotension. The drug can also cause or worsen urinary incontinence in patients [17].

The main side effect of baclofen, tizanidine and tolperisone is the rapid onset of muscle weakness, and in each case the doctor must find a balance between decreased tone and increased weakness. The balance curve between a decrease in spastic tone and an increase in muscle weakness in patients with an increase in the dose of Mydocalm, Sirdalud or Baclofen shows that the most rapid increase in weakness occurs when taking Baclofen, and the mildest drug that allows you to effectively select an individual dosage is Mydocalm. In all cases, given the presence of a narrow therapeutic window, the course of treatment begins with a small dose of the drug, gradually increasing it until a clear antispastic effect is achieved, but not until weakness appears [18, 19].

Diazepam (Realanium, Relium, Sibazon) is a muscle relaxant because it has the ability to stimulate reduced presynaptic inhibition at the spinal level. It does not have direct GABAergic properties, increases the concentration of acetylcholine in the brain and inhibits the reuptake of norepinephrine and dopamine at synapses. This leads to increased presynaptic inhibition and is manifested by a decrease in stretch resistance and an increase in range of motion. Diazepam also has the ability to reduce pain caused by muscle spasms. Along with a decrease in muscle tone, lethargy, dizziness, impaired attention and coordination develop due to the toxic effect on the central nervous system. This significantly limits the use of diazepam as a muscle relaxant. It is used mainly for the treatment of spasticity of spinal origin when a short-term decrease in muscle tone is necessary. For the treatment of spasticity, a dose of 5 mg once or 2 mg 2 times a day is prescribed. The maximum daily dose can be 60 mg. At high doses, disturbances of consciousness, transient liver dysfunction and blood changes may occur. The duration of treatment is limited due to the possible development of drug dependence [20].

Clonazepam is a benzodiazepine derivative. Clonazepam has a sedative, central muscle relaxant, and anxiolytic effect. The muscle relaxant effect is achieved by enhancing the inhibitory effect of GABA on the transmission of nerve impulses, stimulating benzodiazepine receptors located in the allosteric center of the postsynaptic GABA receptors of the ascending activating reticular formation of the brain stem and interneurons of the lateral horns of the spinal cord, as well as reducing the excitability of the subcortical structures of the brain and inhibition of polysynaptic spinal reflexes.

The rapid onset of drowsiness, dizziness and addiction limits the use of this drug. To reduce the occurrence of possible adverse reactions, it is necessary to achieve a therapeutic dose by slow titration over two weeks. For oral administration to adults, an initial dose of no more than 1 mg/day is recommended. Maintenance dose: 4–8 mg/day. It is possible to prescribe small doses in combination with other muscle relaxants. Clonazepam is effective for paroxysmal increases in muscle tone. Contraindicated in acute diseases of the liver, kidneys, myasthenia gravis [21].

Dipotassium clorazepate (Tranxen) is a benzodiazepine analogue, transforms into the main metabolite of diazepam, has greater activity and duration of antispastic action than diazepam. It has been noted to have a good effect in treatment in the form of a decrease in phasic stretch reflexes and has a slight sedative effect. The initial dose is 5 mg 4 times a day, then reduced to 5 mg 2 times a day [22].

Dantrolene is an imidazoline derivative that acts outside the central nervous system, mainly at the level of muscle fibers. The mechanism of action of dantrolene is to block the release of calcium from the sarcoplasmic reticulum, which leads to a decrease in the degree of contractility of skeletal muscles, a reduction in muscle tone and phasic reflexes, and an increase in the range of passive movements. An important advantage of dantrolene in relation to other muscle relaxants is its proven effectiveness against spasticity not only of spinal, but also of cerebral origin. The initial dose is 25 mg/day; if tolerated, the dose is increased over 4 weeks to 400 mg/day. Side effects: drowsiness, dizziness, nausea, diarrhea, decreased glomerular filtration rate. A serious danger, especially in elderly patients at a dose of more than 200 mg/day, is the hepatotoxic effect, so liver function should be regularly monitored during treatment. Elimination of dantrolene is 50% due to hepatic metabolism, and therefore it is contraindicated in liver diseases. Caution should also be exercised in case of severe cardiac or pulmonary diseases.

Catapresan - used mainly for spinal injuries, acts on alpha-2 agonists in the brain, has presynaptic inhibition. Side effects include decreased blood pressure and depression. The initial dose is 0.05 mg 2 times a day, the maximum is 0.1 mg 4 times a day.

Temazepam - interacts with benzodiazepine receptors of the allosteric center of postsynaptic GABA receptors located in the limbic system, ascending activating reticular formation, hippocampus, interneurons of the lateral horns of the spinal cord. As a result, channels are opened for incoming currents of chlorine ions and thus the action of the endogenous inhibitory transmitter, GABA, is potentiated. The recommended dose is 10 mg 3 times a day. Its combination with baclofen is effective [23, 24].

The main drugs used to treat spastic muscle hypertonicity are presented in Table.

Thus, the choice of drug is determined by the underlying disease, the severity of muscle spasticity, as well as side effects and characteristics of the action of a particular drug.

For example, tizanidine and baclofen have a greater effect on the tone of the extensor muscles, therefore, in cases of significant hypertonicity of the flexor muscles of the arm, mild spasticity of the leg muscles, their use is not indicated, since a slight increase in the tone of the extensor muscles of the leg compensates for muscle weakness in the leg and stabilizes the patient's gait. In this case, the means of choice are methods of physical impact on the muscles of the upper limb.

In the treatment of cerebral spasticity, Sirdalud and Baclofen are most often used, and for spinal spasticity - Sirdalud and Baclofen. Mydocalm has an important advantage over other muscle relaxants, which does not have a sedative effect and has a favorable tolerability spectrum, therefore it is the drug of choice for treatment on an outpatient basis and for the treatment of elderly patients.

A combination of several drugs is acceptable, which allows you to effectively reduce tone at lower doses of each drug. Combining drugs with different points of application, from centers in the brain to muscles, can lead to a cumulative therapeutic effect.

The effectiveness of oral antispastic drugs decreases with their long-term use; there is often a need for increasing dosages to maintain the initial clinical effect, which is accompanied by an increase in the frequency and severity of adverse reactions [25–27].

In a situation where spasticity is local in nature and the systemic effect of oral muscle relaxants is undesirable, local methods of exposure are preferable, one of which is the local administration of botulinum toxin [28, 29].

Literature

1. Skoromets A. A., Amelin A. V., Pchelintsev M. V. et al. Prescription reference book for a neurologist. SPb: Polytechnic. 2000. 342 p.
2. Shtok V.N. Pharmacotherapy in neurology: A practical guide. 4th ed., revised. and additional M.: Medical Information Agency LLC, 2006. 480 p.
3. Methodological recommendations for organizing neurological care for patients with strokes in St. Petersburg / Ed. V. A. Sorokoumova. SPb: St. Petersburg, 2009. 88 p.
4. Lehmann-Horn F., Ludolf A. Treatment of diseases of the nervous system. M.: MEDpress-inform. 2005. 528 p.
5. O'Dwyer N., Ada L., Neilson P. Spasticity and muscle contractur in stroke // Brain. 2006. Vol. 119. P. 1737–1749.
6. Damulin I.V. Spasticity syndrome and the main directions of its treatment // Journal of Neurology and Psychiatry named after. S. S. Korsakova. 2003. No. 12. P. 4–9.
7. Zavalishin I. A., Barkhatova V. P., Shitikova I. E. Spastic paresis // In the book. Multiple sclerosis. Selected issues of theory and practice. Ed. I. A. Zavalishina, V. I. Golovkina. Elf IPR LLC. 2000. pp. 436–455.
8. Levin O. S. Basic drugs used in neurology: Handbook. M.: MEDpress-inform, 2007. 336 p.
9. Boyko A. N., Lashch N. Yu., Batysheva T. T. Increased muscle tone: etiology, pathogenesis, correction // Handbook of a polyclinic doctor. 2004. T. 4. No. 1. P. 28–30.
10. Damulin I.V. Spasticity syndrome and the main directions of its treatment // Journal of Neurology and Psychiatry named after. S. S. Korsakova. 2003. No. 12. P. 4–9.
11. Selected lectures on neurology: ed. V. L. Golubeva. M.: EidosMedia, 2006. 624 p.
12. Parziale J., Akelman E., Herz D. Spasticity: pathophysiology and management // Orthopedics. 2003. Vol. 16. P. 801–811.
13. Katz R., Rymer Z. Spastic hypertonia: mechanisms and measurement // Arch. Phys. Med. Rehab. 2009. Vol. 70. P. 144–155.
14. Barnes M. An overview of the clinical management of spasticity // In: Upper motor neuron syndrome and spasticity. Cambridge University Press. 2001. P. 5–11.
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A. A. Korolev, Candidate of Medical Sciences

FSBI All-Russian Center for Emergency and Radiation Medicine named after. A. M. Nikiforova" EMERCOM of Russia, St. Petersburg

Contact information about the author for correspondence

Baklosan: side effects

Those who like to “expand consciousness” use the drug as a substitute for strong psychotropics:

• hallucinogens;
• sodium hydroxybutyrate.

Under its influence the following are observed:

• euphoria;
• improved mood;
• the feeling that problems don’t exist.

Such effects occur when Baklosan is present in the bloodstream - removal from the body leads to their weakening. With regular use of the drug in large quantities, various disorders occur. The most common mental and neurological disorders are:

• depression;
• hallucinations;
• nervous exhaustion;
• drowsiness;
• dizziness;
• convulsions.

Somatic disorders also appear. From the cardiovascular system, this is arterial hypotension (low blood pressure). From the gastrointestinal tract, nausea with vomiting, dry mouth, diarrhea or constipation are observed. Urinary retention and involuntary leakage of urine during sleep may be a concern.

Diagnostics

• The medical history includes a detailed study of the patient's symptoms, their intensity and the relationship of pain with exercise or body position. Information about regular physical activity, sleep habits, and past injuries is also needed.
• A physical examination is necessary to examine range of motion and muscle condition. The presence of painful areas on palpation or physical abnormalities is also determined. In addition, neurological tests are performed to determine neurological deficits.
• The above diagnostic methods are usually sufficient to diagnose osteochondrosis, but an accurate diagnosis requires the use of imaging methods.
• CT
• Radiography
• MSCT
• PAT
• MRI is a diagnostic method that allows you to clarify the degree of degeneration, the presence of fractures, herniated discs and stenosis. Often, an MRI examination is necessary in preparation for surgical treatment in order to accurately determine the location of the degenerated disc and plan the operation.

Studies have shown that MRI findings of moderate to severe disc degeneration are found in scans of patients with both severe pain and minimal or no pain. In addition, many disease conditions may not show up on MRI. For this reason, the diagnosis cannot be made solely on the basis of imaging results, and verification of the diagnosis is possible only on the basis of a combination of all clinical and instrumental examination methods.

Abstinence

Abstinence is associated with the development of physical dependence. This is a pathological condition that appears when you abruptly stop using the described drug. This happens if the product has been used for more than two months. Observed:

• hypermetabolism - an increase in energy expenditure that is not associated with mental or physical activity;
• muscle rigidity (stiffness);
• a sharp increase in temperature - more than 41 degrees Celsius.

In complex cases, disturbances in the functioning of internal organs may occur. Nausea, vomiting, abdominal pain, increased heart rate, and decreased blood pressure appear. Such symptoms disappear if the suffering addict takes the dose of the drug that he usually uses for its psychotropic effect.

Associated symptoms

With osteochondrosis of the lumbar spine, in addition to low back pain, other symptoms associated with disc degeneration may occur. For example:

• Proteins contained within the disc can cause significant inflammation if they come into contact with the surrounding spinal structures, and this inflammation can lead to spasms of the lower back muscles as well as radicular pain radiating to the hips and the back of the lower extremities (also called sciatica).
• Lumbar disc degeneration can contribute to the development of lumbar stenosis and/or lumbar osteoarthritis, as well as other conditions in the lower back.
• A degenerated disc can also lead to a herniated lumbar disc. Neurological symptoms from a herniated disc can be acute and intense.
• Symptoms caused by disc degeneration in the lumbar spine can vary widely depending on how quickly or completely the disc degenerates and how it affects surrounding spinal structures.
• Pain from osteochondrosis is usually caused by deformation of the muscles that support the spine and inflammation around the structures adjacent to the disc.

Overdose

Baklosan is a drug, the body develops insensitivity to it, so the addict is forced to take an increased dose. He may incorrectly calculate the amount of the drug needed to generate positive emotions - an “overdose” occurs. This is evidenced by:

• decreased muscle tone - observed for about three days, even if Baklosan has already been removed from the body;
• involuntary emptying of the bladder and colon;
• convulsions;
• deterioration of breathing - it becomes more rare and superficial;
• confusion, which transforms into stupor - a state similar to drowsiness.

The drug addict often loses control over his actions and takes another dose of the drug - the overdose gets worse. In severe cases, coma (persistent loss of consciousness) develops, leading to death.

Withdrawal: what is it

Withdrawal syndrome or withdrawal is a complex of disorders of the functions of many organs and vital systems

. Occurs when the concentration of an intoxicating substance in the body decreases. This happens 7-8 hours after the last use of psychoactive substances. Pleasant sensations are replaced by painful ones.

Depriving a drug addict of the opportunity to continue using psychostimulants causes him to become depressed. All thoughts are only about finding a new dose. There is anxiety and irritability, a tendency to conflict.

At this moment, those who decide to quit drugs themselves have a breakdown.

The person begins to convince himself that he will now take the dose for the last time, and then he will be able to cope with withdrawal symptoms himself. This is the mistake that pulls him to the very bottom.

If the patient makes up his mind and does not take the drug, he begins to experience withdrawal symptoms, which gradually increase. At this moment, qualified help is needed. Often relatives try to treat a drug addict on their own. They use unverified advice, not realizing that relieving withdrawal symptoms at home worsens the patient’s condition and he will resume taking it in order not to suffer. Or there will be a threat to life, you will still have to contact doctors, but it will be too late.

Literature:

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2. Pharmacokinetics and toxicity of high doses of baclofen in ICU patients / Vourc'h M, Dailly E, Hourmant Y, Bellouard R, Mahe PJ, Deslandes G, Grégoire M, Asehnoune K. / Prog Neuropsychopharmacol Biol Psychiatry. 2021 Jun 8;92:450-456. doi: 10.1016/j.pnpbp.2019.02.016. Epub 2021 Feb 28. / PMID: 30826461.
3. Baclofen: mechanisms of therapeutic and toxic action (review) / Romanova O.L., Blagonravov M.L., Kislov M.A./ 2021 / General resuscitation.