1890
Author of the article
Evgeniy Nikolaevich Konoplev
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Baclofen (from the Latin name Baclophenum) is a drug that reduces reflex muscle tension and leads to their relaxation, considered a derivative of GABA. Used for various spinal cord injuries. Almost insoluble in water and alcohols. The medicine suppresses the reflexes of the dermis and inhibits the reaction of the nerves. If used not according to instructions, it may cause hallucinations.
Pharmacodynamics and pharmacokinetics
The active substance is a GABA stimulant, a derivative of gamma-aminobutyric acid. The mechanism of action is aimed at suppressing interneurons, reducing the excitability of the terminal sections of sensory afferent fibers, and suppressing monosynaptic and polysynaptic transmission of nerve impulses, which leads to a decrease in the preliminary tension of muscle tissue.
The drug Baclofen does not affect neuromuscular transmission . The medication is able to facilitate active and passive kinesitherapy , increase the range of motion in joints, weaken clonic convulsions and painful spasms in neurological diseases, which are manifested by spasticity of skeletal muscles.
Indications
Baclofen was developed in 1962 by a Swiss chemist as a drug for neurological diseases. Experiments revealed that Baclofen has a positive effect on patients with high skeletal muscle tone. And in 2001, it was also proven that the drug is effective in the treatment of gastric reflux.
Has several names. In the Register of Medicinal Products (RLS) - Baclofen. International nonproprietary name (INNA) is Baklosan.
Typically, the drug is prescribed for frequent muscle spasms or paralysis with pronounced reflex muscle tension . Baclofen is a psychotropic drug that allows you to think outside the box and work more efficiently, which is why it is very popular among intellectuals. It is also used by athletes to relieve pain after hard training.
In addition, the drug guarantees the following effect:
- treats hiccups;
- inhibits reflexes in the spine;
- causes a feeling of peace and drowsiness;
- improves joint performance;
- relieves physical stress and pain during massage.
Since 1975, it has been used to treat involuntary tension and relaxation of muscle fibers of cerebral origin. The drug is also prescribed for a trip.
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 effects
Baclofen causes asthenia , dizziness, drowsiness, vomiting, nausea, paresthesia, drop in blood pressure , constipation , diarrhea, urinary retention, gait disturbances, confusion , ataxia, myasthenia , myalgia, depression, euphoria, apathy , enuresis, dysuria, hallucinations , accommodation paresis , nystagmus, decreased seizure threshold, convulsions.
Long-term therapy causes disturbances in the functioning of the hepatic system.
Overdose of the drug Baclofen
Acute Baclofen intoxication may be accompanied by insomnia, loss of consciousness, coma, and breathing problems. Dizziness, hallucinations, anxiety, impaired accommodation, loss of pupillary reflex, muscle hypotonia, clonic convulsions, hyporeflexia or areflexia, convulsions, peripheral vasodilation, bradycardia, decreased body temperature, nausea, vomiting, diarrhea, hypersalivation, increased levels of LDH, ALT may also develop. and AST. Treatment: it is necessary to rinse the stomach and take activated charcoal. If necessary, use saline laxatives. Patients who are in a comatose state must be intubated before gastric lavage. Measures are taken to maintain the functions of the respiratory and cardiovascular systems. There is no specific antidote. In cases of mild intoxication, physostigmine is administered intravenously to eliminate adverse effects from the central nervous system, especially insomnia and respiratory depression. To enhance the removal of baclofen from the body, forced diuresis is used. For convulsions, careful intravenous administration of diazepam is indicated.
Baclofen tablets, instructions for use (Method and dosage)
The drug is taken orally before meals.
The initial dosage is 5 mg three times a day, then every three days the dose of Baclofen is increased by 5 mg to achieve a therapeutic effect. The maximum dosage for adults is 100 mg per day under inpatient supervision.
The final dosage is selected taking into account such a decrease in muscle tone that will not impair motor function or lead to excessive myasthenia gravis.
Persons with hypersensitivity are prescribed 5-10 mg per day with a possible subsequent dose increase.
When carrying out hemodialysis, for chronic renal failure, the daily dosage is 5 mg.
Baclofen is discontinued gradually over 1-2 weeks.
Instructions for use of Baclofen by children
At the age of one to two years, 10-20 mg of the substance is prescribed per day, for two to six years - 20-30 mg per 24 hours, for six to ten years - 30-60 mg per day. At the age of over ten years, the maximum dose is 1.5–2 mg per 1 kg.
Pharmacological properties of the drug
A persistent increase in the tone of skeletal muscles occurs due to the disinhibition of the segmental apparatus of the spinal cord observed in various pathological conditions, disturbances in the conduction of nerve impulses and an imbalance of signals conducted from the central nervous system to muscle fibers and in the opposite direction.
The therapeutic effect of Baclofen is based on its ability to change the body's stereotypical reaction to a stimulus, coordinated by the nervous system. Baclofen inhibits spinal cord reflexes - spinal, carried out with the help of striated muscles (stretch reflex, flexion, extensor, tendon, positional, rhythmic) and visceral, responsible for the functioning and operational state of internal organs and regulated by the efferent structures of the autonomic nervous system. This occurs due to the stimulation of presynaptic metabotropic GABA receptors, classified as class B. These cellular receptors are found in all parts of the nervous system, activate potassium ion channels that control many physiological functions of the cell, and prevent the release of amino acid neurotransmitters that facilitate the transfer of information between neurons and glands and muscle tissue.
The result of the influence is:
- muscle relaxant effect – reduces the sensitivity of neurotendon and muscle spindles and their aggressive reaction to changes in the length and force of contraction of fibers, relieves skeletal muscles from hypertonicity;
- antispastic effect – relieves spastic syndrome by suppressing mono and polysynaptic spinal reflexes and improving electrical transmission in the spinal cord;
- analgesic effect - reduces pain by activating specific opioid receptors, increasing the synthesis of neurotransmitters, endogenous opioid peptides, thereby reducing the body's pain sensitivity;
- antidepressant effect - fights excessive excitability of the subcortical parts of the brain, has a calming effect, suppresses fear, anxiety, and reduces the effects of stress. The effect is achieved due to the presence of the body's main inhibitory neurotransmitter, gamma-aminobutyric acid, which is responsible for the production and maintenance of the balance of hormones, neurotransmitters and other substances that provoke overexcitation.
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.
Analogs
Level 4 ATC code matches: Tizanil
Tizanidine
Tolperisone-OBL
Tizalud
Mydocalm
Baklosan
Sirdalud
Lioresal , Baklosan .
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.
Composition, release forms
Baclofen is currently marketed under the trade name Baclosan. The holder of the registration certificate for the muscle relaxant is the largest Polish pharmaceutical drug manufacturer. The drug is manufactured by Medana Pharma. Baclofen is marketed in a single dosage form - round, convex tablets on both sides, intended for oral use. The tablets are white and have a score line. Placed in white opaque polypropylene bottles containing 50 tablets.
The active substance is an artificially synthesized analogue of natural gamma-aminobutyric acid (abbreviated GABA), this is the most significant inhibitory neurotransmitter of the central nervous system. There are 2 types of Baclofen tablets - with a dosage of the active substance of 10 mg and 25 mg.
The composition of the auxiliary ingredients is similar, according to the instructions it is:
- lactose, potato starch – fillers;
- gelatinous easily digestible mass – binding component;
- talc, magnesium stearate – glidants;
- ethylcellulose – leavening agent.
Baclofen price, where to buy
The price of Baclofen in 25 mg tablets costs 380 rubles per pack of 50 pieces.
- Online pharmacies in UkraineUkraine
Pharmacy24
- Baclofen 25 mg No. 50 tablets Pharmaceutical plant "POLFARMA" S.A., Poland
214 UAH. order - Baclofen 10 mg N50 tablets Pharmaceutical plant "POLFARMA" S.A., Poland
122 UAH order
Interaction with other drugs and cost
Baclofen interacts with psychotropic drugs, due to which it greatly reduces muscle tension. When Baclofen comes into contact with Levodopa and Carbidopa, hallucinations, loss of orientation in space and excessive agitation occur.
The drug can be purchased at any pharmacy in the city, as well as on the Internet. The price of Baclofen tablets is as follows:
- average cost in a pharmacy: 160 rubles. (10 mg), 210 rub. (25 mg);
- on the Internet the drug costs about 265 rubles. (25 mg).
The medicine must be stored in a dry place, protected from light and out of reach of children, at a temperature below 25 degrees. The shelf life is indicated on the packaging and does not exceed 5 years.
Terms of sale in pharmacies - only with a prescription from a doctor. This is argued by the fact that the drug is capable of causing hallucinations, therefore it is widespread among people with drug addiction.
