Baclofen is a drug used to treat muscle spasms from multiple sclerosis and Huntington’s disease, as well as spinal cord injuries and spinal cord diseases.
Medical experts do not recommend Baclofen for muscle spasms caused by rheumatoid arthritis, cerebral palsy, Parkinson’s disease or stroke because research to date does not support such use.
Baclofen is an anti-spastic muscle relaxant. Researchers don’t know exactly how baclofen works; however, in General, It blocks nerve signals from muscles at the level of the spinal cord, and can also depress the Central nervous system.
Available today, only generic versions of Baclofen.
In the report of incidents, published in “Therapeutic Advances in Psychopharmacology” in 2016, it has been shown that Baclofen may be effective for treatment of addiction to marijuana, especially for those who have long used the drug. The study also found that Baclofen can help reduce withdrawal symptoms as well as the effects of marijuana.
A separate study, published in the Journal of Neuroscience in 2014, found that Baclofen can also help people with addiction avoid possible triggers and prevent recurrence. The drug works by interfering with the brain’s early response to medication prescriptions.
How long does baclofen stay in your system?
Following This period of roughly 2 hours, one-half of the dosage is out of The System. Within four hours, one-half of the rest of the baclofen is Eliminated, leaving the individual with just 25 per cent of the original dosage.
The Quantity of baclofen left has been decline by half every two Hours until the entire body is rid of the substance.
Mechanism of action
A spasmolytic agent with a grasping point in the spinal cord. The γ-aminobutyric acid derivative (GABA) reduces skeletal muscle tone by inhibiting mono- and polysynaptic reflexes at the level of the spinal cord.
The exact mechanism of action has not been known. Baclofen stimulates GABA receptors, localised pre- and postsynaptically.
It works by increasing the pre-synaptic block of stimuli that begin mainly in the spinal cord, which leads to a weakening of their transmission.
The result is a reduction in spastic muscle tone and pathological mass reflexes observed in spasticity. As a central muscular relaxant, baclofen does not affect neuromuscular transmission.
The drug shows a general inhibitory effect on the CNS, causing sedation, drowsiness,
Absorbs quickly and completely after administration after Max concentration in the blood reaches after 2-3 h.
T 1/2 in the blood is 2.5-4 h. With blood proteins, it binds in 30%. It is metabolised in the liver in 15% and excreted mainly by the kidneys (70-80%), mainly in unchanged form.
After 72 hours, almost all administered after the dose is expelled from the body. Direct infusion into the spinal space of the spinal cord allows to bypass the drug absorption processes and allows the receptor sites in the posterior core to be exposed to baclofen.
Administration of baclofen directly to the cerebrospinal space enables the treatment of spasticity with doses at least 100-fold lower than the doses used afterPlasma concentrations of baclofen under the influence of intrathecal infusion of clinically used doses have values below the limit of quantitative analysis.
Baclofen slowly crosses the blood-brain barrier and becomes available systemically in very small amounts. T 1/2 after a single intrathecal dose is 1-5 hours.
The mean clearance from the cerebrospinal fluid is approximately 30 ml / h, which corresponds to the speed of physiological circulation of the cerebrospinal fluid.
The amount of baclofen administered as an infusion over 24 hours is almost completely excreted with cerebrospinal fluid at the same time.
Reducing Muscle Tension
To reduce muscular tension after injuries and diseases of the spinal cord (such as spinal cord tumours, spinal cavity, motor neuron diseases, transverse myelitis), multiple sclerosis, cerebrovascular accidents, cerebral palsy, meningitis – core and after head injuries.
The drug in the form of a solution for infusion into the subarachnoid space is used in adults in the treatment of patients with severe chronic spasticity in the course of multiple sclerosis, with spinal cord injuries or cerebral injuries, which can not be effectively treated with baclofen preparations for use after and in children 4.- 18.
With severe chronic spasticity of cerebral or spinal origin (in the course of an injury, multiple sclerosis or other diseases of the spinal cord) who do not respond to treatment after antispastic drugs (including oral baclofen) and/or in which there are unacceptable side effects after administration of effective dosages of drugs on.
The drug for administration after it is not used in people with hypersensitivity to any component of the preparation, with gastric or duodenal ulcer disease, with hereditary galactose intolerance, lactase deficiency or with malabsorption of glucose-galactose.
Conditions requiring special caution
Caution should be exercised:
- in people with psychotic syndromes,
- convulsive states,
- confusional states (risk of exacerbation of the above-mentioned conditions);
- in patients whose maintenance of the vertical position of the body and balance or increase in the range of movements depends on increased muscle tone;
- in people using drugs that lower blood pressure (risk of interaction);
- in the case of cerebral stroke, respiratory disorders, liver dysfunction, increased urinary bladder tension (risk of urinary retention);
- in the elderly (increased risk of side effects);
- in people with impaired renal function (need to modify the dosage).
Hepatic impairment, diabetes
In some patients an increase in AST and alkaline phosphatase and an increase in blood glucose were observed; it is advisable to perform appropriate laboratory tests, especially in people with impaired liver function or diabetes.
Patients with epilepsy should remain under constant clinical and EEG control. The drug should be discontinued gradually, within 1-2 weeks.
The drug in the form of an infusion
The drug in the form of a solution for infusion into the subarachnoid space should not be used in case of hypersensitivity to any component of the preparation or the occurrence of refractory epilepsy; special care should be taken in patients with cerebrospinal fluid disturbances caused by flow impediments, with epilepsy or other brain diseases associated with seizures, with symptoms of bulbar infection or partial paralysis of the respiratory muscles, with acute or chronic disorientation states, with psychotic states, schizophrenia or Parkinson’s disease, with autonomic reflex disorders in history, with cerebral or respiratory system insufficiency, co-existing with increased bladder sphincteric tension, impaired renal function, peptic ulcers,
Spasticity due to a head injury
In patients with spasticity due to head injury, it is recommended that long-term IT intake of baclofen be started after stabilization of spasticity symptoms (i.e. at least one year after the injury).
Children should have sufficient body weight to allow the pump to be inserted for chronic infusions, and administration of this drug should be ordered by specialist doctors with the necessary knowledge and experience.
Data regarding use in children up to the age of 4 are limited.
Method of administration The administration
of the test dose, implantation of the infusion pump and the gradual increase in the IT dose should be carried out in centres that have the appropriate experience and under the supervision of suitably qualified doctors to ensure continuous monitoring of the patient’s condition and access to the ICU.
Monitoring the course of treatment
Because of the risk of inflammatory infiltration at the tip of an implanted catheter that can cause severe neurological disorders, patients should be closely monitored for any new or objective neurological symptoms, particularly when using opioids in parallel.
Before implanting the pump, make sure that the patient does not have an infection because the infection increases the risk of post-operative complications and makes it difficult to adjust baclofen doses.
Refilling the pump tank can only be carried out by a properly trained and qualified physician, at appropriate intervals and observing appropriate rules.
Before initiation of IT administration, tolerability and response to a single bolus injection of no more than 0.1 mg (0.05 mg/ml solution) should be checked, and the dose of other ineffective anti-spasticity medications should be reduced.
Abrupt discontinuation of intrathecal administration may result in high fever, changes in mental state, increased spasticity as a result of “rebound effect” and muscle stiffness.
In rare cases, these effects may develop into epileptic seizures (status epilepticus), a decay of striated muscles, multi-organ failure and cause death.
Therefore sudden abstraction of the preparation should be prevented.
Particular attention should be paid to patients with risk factors (e.g. patients with spinal cord injury in the area of the sixth thoracic vertebra or above, patients with communication difficulties and patients who have previously experienced withdrawal symptoms after discontinuation of oral or intrathecal baclofen therapy).
People over 65 years.
Patients aged 65 and over may be more susceptible to side effects after oral administration of baclofen; a similar relationship cannot be excluded after intrathecal administration.
Increases the effect of antihypertensive drugs, which may necessitate the adjustment of their dosage.
Tricyclic antidepressants may increase the effect of baclofen and significantly reduce muscle tone.
Drugs Enhance the effects of ethanol and depression-acting drugs on the CNS.
Parallel application with lithium salts may increase the patient’s hyperthyroidism.
Drugs that can cause kidney failure may impair the excretion of baclofen and side effects.
Levodopa with carbidopa
In patients with Parkinson’s disease, the parallel use of baclofen and levodopa with carbidopa may cause confusion, hallucinations and agitation.
Baclofen prolongs analgesia induced by fentanyl. The concomitant use of intrathecally administered baclofen and general anaesthesia (e.g. fentanyl, propofol) may increase the risk of cardiac dysfunction and epileptic seizures.
A drug in the form of a solution for infusion into the subarachnoid space in combination with morphine may cause a fall in blood pressure. In such cases, the risk of breathing disorders and CNS disorders cannot be excluded.
- respiratory depression
- a feeling of emptiness in the head
- a headache and dizziness
- dry mouth
- taste disorders
- drop in blood pressure
- muscle weakness
- muscle aches
- visual disturbances
- accommodation disorders
- excessive sweating
- involuntary urination
- painful urination
- speech impairment
- decreased convulsive threshold and an increase in the number of seizures
- especially in patients with epilepsy
- abdominal pain
- liver dysfunction
- decreased cardiac output
- palpitations chest pain
- ankles puffiness
- urinary retention
- ejaculation disorders,
- breath suppression
- positive stool occult blood test,
- weight gain
- nasal congestion
- paradoxical worsening of spastic states.
Symptoms of overdose:
- loss of consciousness
- respiratory depression
Empty the stomach (provoke vomiting or rinsing), give activated charcoal, sometimes also laxative salts and protect the respiratory tract and administer liquids and diuretics; in case of convulsions, careful administration of diazepam may be considered.
Administration of physostigmine iv at a dose of 1-2 mg for 5-10 min in adults may help reverse the adverse effects of baclofen on the CNS. If the therapy proves to be effective, a dose of 1 mg physostigmine should be repeated at intervals of
Pregnancy and lactation
Category C. For pregnant women, use only if necessary.
Penetrates breast milk; Breastfeeding during baclofen therapy is not recommended.
Adults initially 5 mg 3 × / d, then increase the daily dose every 5 days by 5 mg to achieve the desired effect. Maintenance dose usually 30-75 mg / d, max dose – 100 mg / d (in 3-4 doses).
In children, usually 0.75-2 mg / kg; 12. milk-2. 10-20 mg / d, 2.-6. 20-30 mg / d, 6-10. 30-60 mg / d; in children after the age of 10 the maximal dose is 2.5 mg / kg; treatment starts at a dose of 5 mg 2 × / d, then, if necessary, increase gradually every 3 days.
In patients with renal failure and those on hemodialysis, the dose should be reduced to 5 mg / d.
There may be a reduction in the effectiveness of the medicine after long-term use. After sudden discontinuation, symptoms may return more severely (“rebound” effect) – the dose should be gradually reduced over several days. The drug in the form of solution for infusion into the subarachnoid space.
After the test dose (initially 25 μg, gradually increased to a maximum of 100 μg) and implantation of the pump, through which a continuous infusion of the solution is possible. Into the cerebrospinal fluid individual dosage, depending on the trial dose and effectiveness.
The maintenance dose in long-term therapy of patients with spasticity of spinal origin is 300-800 μg / d; in spasticity of brain origin, lower doses are usually used.
The experiment with doses> 1000 μg / d is limited.
Hepatic and/or renal dysfunction
Patients with renal impairment may need to adjust their dose. In the case of liver dysfunction, there is no need to adjust the dosage.
Baclofen: missed dose
Take Baclofen exactly as prescribed by your doctor.
Do not take more or less, and do not stop taking baclofen by yourself.
If you miss a dose, take it as soon as you remember. But if it’s time for the next dose, skip it and continue the regular dosing schedule.
Do not double your dose to make up for missing.
What is baclofen, history
Baclofen (baclofen) is a medication that can be purchased at the pharmacy. It provokes dependence, which is difficult to get rid of. The tablets are classified as light drugs, so they have become popular among young people.
As medical product baclofen is suitable for the treatment of traumatic brain injuries, spasmodic and spastic conditions. Take it should be strictly under the supervision of a doctor. Throw the reception of a dramatic work, because after a few days of habituation takes place and the patient requires continued administration of the doses. So throw the intake gradually.
The drug was made to treat epilepsy. It has a powerful effect on the Central nervous system, is used as an analgesic and antidepressant.
Tablets are taken orally or inhaled through the sinuses.
Effects on the body
The use of the drug extends to the psyche and the body as a whole. Within an hour after receiving the consumer becomes overly cheerful and active. The addict feels a surge of strength and energy, improves mood and performance. He does not feel tired, does not need rest. This condition lasts for several hours.
As there is a dependence on bakasana?
Baclofen can enhance the effect of other drugs, so it is often used in combination with other components or alcohol. The dependence of a person on the drug is caused by the fact that it “opens” great opportunities in a person, which he had not previously suspected. Creative fear, complexes, nervousness disappears. A person becomes filled with energy, fame, and desire to achieve more. But the condition lasts as long as the effect of baclofen lasts.
The drug does not cause chemical dependence, so there is no physical addiction. The threat to a person is psychological dependence. Therefore, one of the main criteria for the treatment of a drug addict is his complete isolation.
Signs of baclofen use
Signs of consumption of cormorant for a long time:
• muscle spasticity;
• nausea and vomiting;
• asthenic state;
• drowsiness and apathy;
• the appearance of dizziness and headaches;
• dry mouth;
• constipation appearance up to one week;
• a tremor of limbs;
• illusions and hallucinations;
Consequences of the use of baclofen
Drug addicts use baclofen in increased doses to get a sense of pleasure, illusions, and hallucinations. Often the consumer is inhibited respiratory function, so the symptoms are the cause of sudden death.
The drug addict loses touch with reality; he has a broken heart and internal organs:
- manifests itself manic-depressive syndrome;
- obsessive-compulsive disorder;
- loss of sense of reality;
Regular use of the drug for several weeks can lead to death.
Physical dependence manifests itself in muscle hypotension, that is, the addict acquires energy and strength, his consciousness becomes clear and distinct. Then comes the oppression of breathing, disturbed accommodation, pupillary reflex disappears, there is a sense of anxiety and danger, so the addict begins to behave inadequately.
Deteriorating brain activity, digestion, respiratory system.
How does consumption affect the psyche
Using the drug in large quantities or combination with other drugs or alcohol, a person falls into a psychedelic state. In plain language, it is called “trip”. Included are the strange emotions, nervousness, delusions of persecution.
Can I quit on my own?
The dependence of the baclofen treated is very difficult and problematic. Save a drug addict is possible only with the participation of competent professionals. Self-refusal of the drug entails atony, aching throughout the body, hallucinations, depression, headaches, pain in the limbs, loss of consciousness, convulsions.
Dependence treatment baclofen (behaviour)
Dependence treatment baclosan in rehab gives addicts a chance to return to normal living conditions. In medical institutions take patients in any state of severity, try to help everyone who applied for it. Patients undergo a detailed examination of the body.
Only after that, he is diagnosed and prescribed complex therapy for recovery. First of all, the addict’s body is cleaned of harmful and toxic substances. The patient then goes through a course of treatment and psychological rehabilitation. Addicts in the past strengthen their psyche, begin to control their behaviour.
What is the difference between baclofen and intrathecal baclofen?
When an oral medication or gastrostomy is used to act directly on the central nervous system, this medication must be absorbed in the digestive tract, fall into the bloodstream, cross the blood-brain barrier, and then be released into the cerebrospinal fluid, where it will reach its target of the action.
However, many medications go far beyond the blood-brain barrier and high blood concentrations are required to achieve small concentrations in the cerebrospinal fluid.
With a direct intrathecal infusion of baclofen, the concentrations reached in the CSF are much higher than the concentrations of the same medication even when used at the maximum oral dose.
In the case of baclofen, it is estimated that its concentration around the marrow is 40 times higher than the maximum oral dose.
Intrathecal baclofen pump: The drug reservoir is usually implanted in the belly region, below the skin, and it leaves a catheter that takes the medication directly to the cerebrospinal fluid, distributing it in the central nervous system.