What Are the Most Common Side Effects of Baclofen?

Baclofen tablets, the indication is a proven indication: for severe but reversible muscle spasms caused by multiple sclerosis. Others may apply: Spinal cord spasm due to infection, degenerative disease, trauma, or tumor.

Drug Name: Baclofen tablets

Drug type: Prescription drugs, medicines for medical workers' injuries
Use classification: Skeletal muscle relaxant

Baclofen tablets ingredients

Active Ingredient: Baclofen.
Chemical name: - (aminomethyl) -4-chlorophenylpropionic acid.
Its structural formula is:

Molecular formula: C ₁₀ H ₁₂ CINO ₂
Molecular weight: 213.7

Baclofen Tablet Properties

This product is white or slightly yellowish.

Baclofen tablets indications

Proven indications:
For severe but reversible muscle spasms caused by multiple sclerosis.
Others may apply: Spinal cord spasm due to infection, degenerative disease, trauma, or tumor.

Baclofen tablets specifications

10 mg.

Baclofen tablets usage dosage

Recommended dose <br Usually, the best daily dose of baclofen for adults is 30-75mg, divided into 3-5 times. The daily dose of individual cases can be as high as 100 mg / day. The starting dose for children is generally 0.3 mg / kg / day.
Special cases < br Stroke patients are generally poorly tolerated with baclofen, so extra care is needed for these patients.
Routine / maximum doses (single and daily) / dose intervals < br The dose at the beginning of adult treatment should be 5 mg each time, three times a day. Then according to the patient's response, a single dose can be gradually increased, each time increasing by 5mg, three days apart. In general, the average daily dose is 30-75mg, and the individual daily dose can be as high as 100mg / day as needed.
Children see [children's medicine]
Special dosage instructions < br At the beginning of treatment, patients need to be closely monitored in order to quickly detect certain potential adverse reactions, such as general weakness of the muscles, sudden loss of muscle tone (risk of sudden fall), fatigue, or mental stress Wait, then make the necessary adjustments to the dose. For physically weak patients and elderly patients with brain-derived spasms, heart disease, respiratory dysfunction, liver or kidney dysfunction, the dose increase is particularly slow.
Patients with long-term hemodialysis will have an increased plasma baclofen concentration, so low-dose baclofen should be selected (about 5 mg / day).
For patients working in hazardous work environments, special medication instructions should be given.
If you take baclofen for a long time (more than 2-3 months), baclofen should be gradually discontinued, because if it is abruptly stopped, it may cause anxiety, palpitations, hallucinations, central epilepsy, movement disorders, tachycardia, Body temperature is too high. In addition, gradual withdrawal can avoid transient rebound, including increased frequency and / or severity of epilepsy.
Correct usage / special instructions on how to take (relevant instructions)
This product should be taken with a small amount of liquid at mealtime. For adults, take the dose at least three times throughout the day; for children, take it at least four times.
If the therapeutic effect is still not obvious after taking the maximum recommended dose for 6-8 weeks, you should reconsider whether to continue baclofen tablets.
Or as directed by your doctor.

Baclofen tablets adverse reactions

The adverse reactions (Table 1) were ranked according to the frequency of occurrence. The first is a very common adverse reaction, and the corresponding classification criteria are: very common (1 / 10), common (1 / 100, <1/10). Uncommon (1 / 1,000, [1/100), rare (1 / 10,000, <1 / 1,000), very rare (<1 / 10,000), including case reports.
Adverse reactions mainly occur in the initial stage of medication (such as sedation, drowsiness). If the dose is increased too fast, or large doses are taken, adverse reactions may occur. Adverse reactions are mostly temporary. And can be reduced or disappeared by reducing the dose. Rarely, serious adverse reactions that require discontinuation occur. For patients with a history of mental illness or cerebrovascular disease (such as stroke), or for the elderly, adverse reactions may be more severe.
Reduces the threshold of seizures and may cause convulsions, especially in patients with epilepsy.
As an abnormal response to the medication, muscle cramps can worsen in some patients.
Many of the reported adverse reactions have the following manifestations:

Baclofen tablets contraindications

People who are allergic to baclofen or any other excipient.

Baclofen tablets precautions

Mental neurological disorders For patients with mental illness, schizophrenia, depression or mania; Parkinson's disease, or confusion, special care should be taken when using baclofen and close monitoring of patients is required , Because these conditions may worsen.
Epilepsy should also be given special attention in patients with epilepsy, because the seizure threshold may be lower, and there have been individual cases of epilepsy due to baclofen discontinuation or excessive use. Adequate anticonvulsant therapy should be continued and patients should be closely monitored.
Other patients with peptic ulcer (including a history of peptic ulcer), cerebrovascular disease, or respiratory or liver insufficiency. Baclofen tablets should be used with caution.
Renal insufficiency This product can be used in patients with renal insufficiency. Only when the benefits far outweigh the risks can they be used in patients with advanced renal failure. These patients need to be closely monitored for rapid diagnosis of early signs and / or symptoms of toxicity (eg, lethargy, burnout).
In particular, it should be noted that renal function should be closely monitored when this product is used in combination with other drugs that affect renal function. And the daily dose of this product should be adjusted to prevent toxic effects of baclofen.
In addition to discontinuation of treatment with this product, patients with severe baclofen poisoning can be treated with irregular hemodialysis. Hemodialysis can effectively remove baclofen from the body. Reduce the symptoms of drug overdose and shorten the recovery period for patients.
Urinary system disorders affect the emptying of the bladder after neurological dysfunction, after taking baclofen tablets. It may improve; but in patients who already have increased sphincter tone, acute urinary retention may occur. Therefore, such patients should be used with caution.
Laboratory tests have reported serum SGOT in rare cases. Alkaline phosphatase and blood glucose levels are elevated, so appropriate laboratory tests should be performed regularly on patients with liver disease or diabetes to ensure that the drug does not cause changes in the primary disease.
Baclofen tablets contain wheat starch, and wheat starch may contain gluten, but the content is quite small. Therefore, the use of baclofen tablets is still safe for patients with celiac disease.
Impact on driving and machine use power Olase may cause dizziness, sedation, lethargy, and visual disturbances (see [Adverse Reactions]). These adverse reactions may affect the patient's ability. Therefore, patients with these adverse reactions should try to avoid driving or using machinery. Elderly patients and patients with brain-derived spasticity are more likely to have adverse reactions. Therefore, it is recommended that this type of patients should be carefully formulated with dosage tables and moderately monitor the use of this product.
Sudden discontinuation of medication should not be stopped suddenly. Especially after long-term use, otherwise anxiety, confusion and hallucinations may be caused. Mental illness, mania or convulsions (epilepsy status). Tachycardia, hyperthermia, and rebound-spasticity temporarily increased.
In the use of intrathecal injection of olisole. Discontinuation of drug use may lead to clinical manifestations similar to abnormal autonomic reflexes, malignant hyperthermia, malignant nerve block syndrome, or other symptoms associated with hypermetabolic or rhabdomyolysis.
Except in the case of emergency overdose or severe adverse reactions, discontinuation of medication should be gradually reduced to stop (completed in about 1 to 2 weeks).

Baclofen tablets for pregnant and lactating women

In pregnant women, the incidence of fetal umbilical hernias (abdominal wall hernias) has been increased in rats taking baclofen 13 times the human recommended dose (calculated as mg / kg). But this abnormality did not occur in mouse or rabbit experiments.
There are currently no adequate and well-matched controlled studies on the use of this drug in pregnant women. Baclofen can penetrate the placental barrier and should not be used in pregnant women unless the benefits of the medication outweigh the risks to the fetus.
Medication for lactating women For lactating women taking baclofen at clinical doses, a small amount of baclofen can enter breast milk, but the dose is small enough to have no adverse effects on the infant.

Baclofen tablets for children

In general, treatment should start at a very low dose, such as 0.3 mg / kg / day, and be divided into 2 to 4 doses. Therefore, this product is not suitable for children weighing less than 33kg. Carefully increase the dose over approximately 1-2 weeks. Until the individual treatment requirements of the child are met, the daily dose of maintenance treatment is 0.75-2 mg / kg body weight. The maximum daily dose for children under 8 years should not exceed 40 mg / day. For children over 8 years. The maximum daily dose can reach 60mg / day.

Baclofen tablets for elderly

See [Usage and Dosage] and other items, or follow the doctor's advice.

Baclofen tablets drug interactions

When liostatin is used together with other drugs acting on the central nervous system (with opioids or alcohol), it will have a stronger sedative effect (see [Precautions]). The risk of respiratory depression also increases accordingly.
Respiratory and cardiovascular functions need to be closely monitored, especially in patients with cardiopulmonary disease or respiratory muscle weakness.
Taking tricyclic antidepressants at the same time may enhance the effect of baclofen. Causes noticeable reduction in muscle tone.
Because the use of antihypertensive agents may cause a decrease in blood pressure, the amount of antihypertensive agents must be adjusted accordingly. Hypotension occurred in one patient who used both morphine and intrathecal baclofen.
When patients with Parkinson's disease take baclofen and levodopa at the same time, there have been reports of palpitations, hallucinations, headaches, nausea, and irritability.
Other drugs that significantly affect renal function will reduce the excretion of baclofen and cause toxic reactions (see [Cautions]) The simultaneous use of the disease drugs levodopa and carbidopa, sleeping pills, opioids, antidepressants with sedative effects) or antihypertensive drugs may cause mutual enhancement of the effects.
It has been reported that Parkinson's patients can cause palpitations, hallucinations, headaches, nausea and anxiety when taking baclofen and levodopa simultaneously.
Taking tricyclic antidepressants at the same time may enhance the effect of baclofen, resulting in significant muscle tone loss.
Combination with centrally acting drugs increases the risk of respiratory depression.
For patients with cardiopulmonary disease or respiratory muscle weakness, close monitoring of respiratory and cardiovascular function is required.
Special care should be taken to avoid alcohol consumption during medication, as the interaction between baclofen and alcohol is unpredictable.

Baclofen tablets overdose

Signs and symptoms are most obviously characterized by signs of central nervous system depression; lethargy, impaired consciousness, coma, and respiratory depression.
It is also possible that: consciousness, illusion. Irritability, convulsions, EEG changes (burst suppression or triple wave), pupillary dysfunction, disappearance of pupillary reflexes, decreased muscle tone throughout the body, myoclonus, weakened or disappeared reflexes, peripheral vasodilation, hypotension or hypertension , Bradycardia or tachycardia, arrhythmia 0, hypothermia, nausea, vomiting, diarrhea, increased saliva secretion, and elevated liver enzymes (such as LDH, SGOT-, and AP).
If you take multiple centrally acting substances or drugs (such as alcohol, diazepam, and tricyclic antidepressants) at the same time, the situation may worsen.
No known specific antidote is currently available for treatment.
Complications such as hypotension, hypertension, convulsions, gastrointestinal disorders, and respiratory or cardiovascular depression require symptomatic treatment and support.
Once baclofen is overdose, the use of activated carbon should be considered, especially during the initial period after ingestion. In individual cases, gastrointestinal disinfection (e.g., vomiting and gastric lavage) needs to be considered, especially during the first period of time (60 minutes) after taking a life-threatening overdose. Patients with coma or convulsions should be intubated before undergoing gastrointestinal disinfection.
Because the drug is mainly excreted through the kidneys, the patient should be given a lot of fluids. Diuretics can be used concurrently. When severe poisoning occurs with renal failure, hemodialysis (sometimes temporary) can be considered. The use of diazepam requires special care when convulsions occur.

Baclofen tablets pharmacology and toxicology

Pharmacological effects Baclofen tablets-a muscle relaxant acting on the spinal cord. Baclofen inhibits the release of the excitatory amino acids glutamic acid and aspartic acid by stimulating the GABAB receptor, and inhibits single and multiple synaptic reflexes in the spinal cord.
Baclofen has no effect on impulse transmission between neuromuscular muscles and has analgesic effects. For neurological diseases related to skeletal muscle spasm, the clinical role of baclofen is mainly to relieve reflex muscle spasm, and significantly relieve painful spasms, automatisms and clonics. Baclofen can effectively improve mobility, facilitate daily life, catheterization and physical therapy. The indirect effects of taking baclofen include preventing and promoting the healing of bedsores, improving sleep (due to the elimination of painful muscle spasms), and improving the function of the bladder and anal sphincter. This can significantly improve the quality of life of patients.
Baclofen can stimulate the secretion of gastric acid.
Preclinical safety data Trial data to date indicate that baclofen is not carcinogenic or mutagenic.
In female rats taking baclofen for two years, the incidence of ovarian cysts and enlargement and / or an increase in hemorrhagic adrenals was clearly observed after the maximum dose (50-100 mg / kg) and was dose-dependent.

Baclofen tablets pharmacokinetics

Baclofen can be absorbed quickly and completely through the gastrointestinal tract.
After a single oral dose of 10 mg, 20 mg, or 30 mg of baclofen, peak plasma drug concentrations were reached within 0.5-1.5 hours. The average peak plasma concentrations were approximately 180 ng / ml, 340 ng / ml, and 650 ng / ml, respectively. The area under the corresponding serum concentration curve (AUC) is approximately 1135ng × h / ml, 2345ng × h / ml, and 3353ng × h / ml, which are proportional to the dose.
The distribution volume of baclofen in vivo is 0.71 / kg, the serum protein binding rate is about 30%, and the concentration of active ingredients in cerebrospinal fluid is about 8.5 times lower than that in plasma.
Metabolic range of baclofen is small. Deamination produces the main metabolite: the non-pharmacologically active - (p-chlorophenyl) --hydroxybutyric acid.
Plasma clearance The average half-life for plasma clearance is 3-4 hours, and most of baclofen is excreted as a prototype. Within 72 hours, about 75% of the drug is excreted by the kidneys, 5% of which is excreted as metabolites, and the remaining drugs, including 5% of the metabolites, are excreted in the feces.
The pharmacokinetics of baclofen in elderly patients under specific clinical conditions is the same as in young patients.

Baclofen tablets storage

Stored under 25 ° C, protected from moisture. Avoid mistaking by children.

Baclofen tablets packaging

Aluminum plastic packaging, 10 pieces / board, 3 plates / box.

Baclofen tablets expiration date

48 months.

Baclofen tablets implementation standards

Import drug registration standard JX20000333 ^[1]