Baclofen – a drug used in surgery. Dosage and composition

Baclofen is a prescription medicine. It is mainly used in general surgery, oncological surgery, internal diseases, general and pediatric neurology, pediatric oncology and hematology, and clinical oncology. The active substance in the medicine, baclofen, causes the muscles to relax by relieving the excessive tension in the skeletal muscles (spasms) that occurs in various disease states. What is the composition and action of Baclofen? What are the indications and contraindications to its use and what side effects can it cause? How to use and dose the drug and with what medicinal products not to combine it?

Baclofen – general characteristics of the drug

Baclofen is a muscle relaxant drug used in children and adults. This drug is available only on prescription, prescribed to a specific person. Therefore, the drug must not be passed on to others, as it may harm another person, even though the symptoms are the same. The international name of this medicinal product is Baclofenum.

This drug was first produced in 1962 by Heinrich Keberle. It was originally used as a drug for epilepsy and after careful research, it began to be used as a muscle relaxant. In 1970, however, it was introduced to the generally available pharmaceutical market.

Baclofen can be in the form of an infusion solution, an injection solution and in the form of tablets, which are the most common form of this drug. Packages containing 50 or 100 tablets with doses of 10 mg or 25 mg are usually available on the market. In both ancestors, the tablets are white, round and biconvex, and in the case of the 10 mg tablets, additionally they have a line dividing the tablet in half.

The tablets are packed in a polyethylene (HDPE) container with a polyethylene tamper-evident lid, in a cardboard box. The price of the drug depends on the size of the drug dose, it is not refundable and amounts to:

1. 100 tablets, 10 mg each, about PLN 33;
2. 50 tablets, 10 mg each, about PLN 20;
3. 100 tablets, 25 mg each, about PLN 51;
4. 50 tablets, 25 mg each, about PLN 25.

The drug should be stored in the original package in order to protect it from light and moisture out of the sight and reach of children at a temperature of up to 25 degrees Celsius.

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Baclofen – composition and mode of action of the drug

The active substance in Baclofen is a spasmolytic drug derived from y-aminobutyric acid (GABA) called baclofen.

This substance is a receptor antagonist that reduces skeletal muscle tone by inhibiting the mono- and polysynaptic reflex at the level of the spinal cord.

The exact mechanism of its operation has not been fully elucidated. On the other hand, it is suspected that baclofen increases the blockade of stimuli coming from the spinal cord, reducing their transmission.

The drug Baclofen due to the presence of the active substance shows inhibitory effect on the central nervous, respiratory and circulatory systemscausing you to feel calm and sleepy.

This preparation is rapidly and completely absorbed after oral administration. It is metabolized in the liver in 15%, and it is mainly excreted by the kidneys (70-80%) in unchanged form.

In addition to the active substance, Baclofen consists of additional substances that perform auxiliary functions, these are: lactose, potato starch, gelatin, talc, magnesium stearate, ethylcellulose.

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Baclofen – indications for the use of the drug

Baclofen is a medicine that relaxes the muscles by reducing excessive muscle tension. In addition, it inhibits skin reflexes and muscle tension, to a small extent reducing the amplitude of tendon reflexes.

It is mainly used to reduce and relieve excessive skeletal muscle tension, the so-called spastic conditions, caused by various disease states such as:

1. multiple sclerosis;
2. spinal cord injury;
3. cerebral palsy;
4. degenerative changes;
5. head injuries;
6. meningitis;
7. spinal cord infections and diseases;
8. neoplastic changes;
9. spinal cord paralysis;
10. amyotrophic lateral sclerosis;
11. paresis of the lower limbs;
12. compression of the spinal cord;
13. transverse myelitis;
14. syringomyelia;
15. traumatic paralysis.

Baclofen can also be used in children and adolescents up to 18 years of age of life in the treatment of spastic conditions of cerebral origin resulting from:

1. cerebral palsy;
2. neoplastic changes;
3. degenerative disease of the brain;
4. cerebrovascular accidents.

In addition, Baclofen is used in convalescence as a preparation facilitating the patient’s rehabilitation.

How to fight the effects of muscle cramps? Check: Ways to shrink. Types, causes, home remedies for muscle spasms

Baclofen – contraindications to the use of the drug

Baclofen preparation, although there are indications for its use, cannot always be used in every patient.

The main contraindication to the use of this drug is hypersensitivity, i.e. allergy to the active substance beclofen and any of the auxiliary components of the drug.

Contraindications to the use of Baclofen also include some diseases and circumstances that may require you to completely abandon this drug or change the dosage of the preparation. Among other things, such a contraindication is gastric ulcer and duodenal ulcer.

The use of the preparation may require specific control tests and a detailed medical interview.

In addition, there are cases in which the preparation is contraindicated, and in the case of its use, caution and under the constant supervision of a doctor are required, these are patients:

1. with impaired renal or hepatic function;
2. over the age of 65;
3. suffering from epilepsy or a history of seizures;
4. with mental illnesses (e.g. psychotic syndrome, schizophrenia, confusional state);
5. who have recently had a stroke
6. with disorders of the respiratory system;
7. in whom maintaining the vertical position of the body and balance as well as increasing the range of movements requires increased muscle tension;
8. with increased tone of the bladder sphincter;
9. who have been diagnosed with alcoholism or have a history of substance abuse or dependence.

When using Baclofen, especially in the above-mentioned situations, be especially careful and discuss any doubts with your doctor before starting to use the drug.

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Baclofen – method of application and dosage of the drug

Baclofen is a drug in the form of tablets intended for oral use. Always take the drug as prescribed by your doctor and consult him in any doubt.

Baclofen dose it is determined by a physician after a thorough interview and evaluation of the patient’s condition. For adults, it is usually recommended starting dose 5 mg (1/2 tablet of 10 mg) taken 3 times a day for 3 days. The dose is gradually increased every 3 days until the expected results are achieved, i.e .:

1. 10 mg, 3 times a day for 3 days;
2. 15 mg, 3 times a day for 3 days;
3. 20 mg, 3 times daily for 3 days.

The use of the drug brings its first effects, usually at a dose of 30 mg to 75 mg per day. A dose higher than 100 mg a day is not recommended, and for patients who require a higher dose, 75-100 mg daily is given.

In the case of using Baclofen in the treatment of children and adolescents under 18 years of age, treatment with the drug begins with a dose of about 0,3 mg / kg body weight, daily in 2-4 divided doses. The dose is increased gradually, usually at intervals of one week. The most common dose for children is 0,75 to 2 mg / kg body weight, and for children up to 8 years of age it is a maximum of 40 mg. However, in children over 8 years of age, the maximum dose is 60 mg. Baclofen should not be given to children weighing less than 33 kilograms.

Your doctor may change the dosage of your medicine in special patient groups. Elderly patients should increase the dose with particular care, due to the higher risk of side effects.

Patients suffering from impaired renal function or undergoing dialysis should have their dose reduced to 5 mg daily.

Baclofen should be taken with meals with plenty of water.

Always follow the instructions of your doctor and if you take more than the dose prescribed by your doctor, contact your doctor immediately or go to the nearest hospital.

If you miss a dose, do not double the dose to make up for it, but take it as soon as possible and take the next dose at the usual time.

Treatment with the drug should be carried out under the supervision of a physician who decides about its completion. You must not make your own decisions about stopping treatment, as this may lead to hallucinations and worsening of spastic conditions.

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Baclofen – possible side effects

Like any other Baclofen medicinal product, it may cause side effects that may not occur in every person using this medicine.

After authorization of the medicinal product, it is important to report any suspected adverse reactions so that the benefit / risk balance of the medicinal product can be monitored.

The general classification of the frequency of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare ( ≥100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

There are side effects, the occurrence of which requires immediate contact with a doctor, and among them we can distinguish:

1.  chest pain, shortness of breath;
2.  swoon;
3.  hematuria;
4.  depression and confusion;
5.  hallucinations and visual disturbances;
6. skin rash
7. severe muscle weakness;
8. vomiting;
9. seizures.

Other side effects that may be caused by Baclofen are the following:

1. very often (more than 1 in 10 patients): nausea, excessive calmness, sleepiness and confusion;
2. often (may affect up to 1 in 10 patients): feeling tired and weak, low body temperature, insomnia, ataxia, shortness of breath, shortness of breath, lightheadedness, dementia, confusion, retching, taste disturbance, dry mouth, anorexia , constipation or diarrhea, low blood pressure, muscle weakness, muscle tremors, excessive sweating, increased urine output, and involuntary and painful urination;
3. rarely (less than 1 in 1000 patients): Tingling and numbness in the extremities, impaired speech, excessive euphoria and agitation, depression, hallucinations and nightmares, lowering the seizure threshold and increasing the number of seizures, liver dysfunction, abdominal pain, pain in chest, palpitations, shortness of breath, fainting, ankle swelling, bedwetting, urinary retention, haematuria, ejaculation failure, impotence, respiratory depression;
4. frequency unknown (cannot be estimated from the available data): positive fecal occult blood test, itching, weight gain, nasal congestion, difficulty breathing during sleep (sleep apnea syndrome), an increase in spasticity has been observed in some patients.

If you notice any of the above or other symptoms during or after taking Baclofen, please inform your doctor or pharmacist immediately. It allows continued monitoring of the benefit / risk balance of the medicinal product.

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Baclofen – interactions with other pharmacological preparations

The initiation of treatment with the use of Baclofen requires a detailed interview with regard to all currently and recently taken medications, including over-the-counter medications.

The use of certain drugs at the same time as Baclofen can cause serious side effects.

Before taking the drug, tell your doctor or pharmacist about all the drugs you are taking or have recently taken, and about any drugs you plan to start taking.

Combining Baclofen with certain preparations may result in an increase in side effects or a decrease or increase in the effect of drugs. Particular care should be taken when using:

1. antidepressants (clomipramine, amitriptyline, doxepin, opipramol) – the effect of baclofen may be enhanced and the muscle tone may decrease significantly;
2.  soli litu used in the treatment of certain mental illnesses – it may worsen motor overactivity;
3. ibuprofen for pain and arthritis – may delay the process of baclofen excretion, and thus increase its toxicity;
4.  medicines to lower blood pressure (Amlodipine, Benazepril, Bisoprolol, Eplerenone, Irbesartan, Candesartan, Captopril, Karteolol, Carvedilol, Lacidipine, Lercanidipine, Lisinopril, Losartan, Metoprolol, Nebivolol, Nitrendipine, Telmisartan, Valsartan may cause excessive blood pressure reduction);
5. levodopa from carbidopą used in Parkinson’s disease – can cause confusion, hallucinations and agitation;
6. antiepileptic drugs (Diphenhydramine, Carbamazepine, Lamotrigine, Topiramate) – can lead to excessive sedation;
7. leki with agonistic-antagonistic effect on opioid receptors (Buprenorphine, Fentanyl, Codeine, Morphine, Oxycodone, Tramadol) – may cause excessive sedation, weakness of breathing (through central effect) and coma.

Due to the interaction of Baclofen with other medicinal products, the physician should be informed about all drugs currently or recently taken, including those sold without a prescription.

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Baclofen and pregnancy and breastfeeding

The use of any medications or dietary supplements during pregnancy requires consultation with the attending physician. If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking Baclofen.

This drug should only be used during pregnancy if absolutely necessary.

If you are breastfeeding, ask your doctor or pharmacist for advice before taking this medicine. Baclofen passes into breast milk, breastfeeding is not recommended while taking the drug.

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