Baclofène

Baclofène Uses, Dosage, Side Effects, Food Interaction and all others data.

Baclofène is a centrally acting skeletal muscle relaxant and an antispastic agent with a spinal site of action.

In neurological diseases associated with spasm of the skeletal muscles, the clinical effects of baclofen occur due to baclofen action on reflex muscle contractions and of significant relief from painful spasm, automatism, as well as clonus. Baclofène, when used as indicated, improves mobility, increasing levels of independence, and facilitates both passive and active physiotherapy. Baclofène also stimulates gastric acid secretion .

GABA-B receptor activation by baclofen may produce protective neurological effects. Baclofène also possesses anti-inflammatory properties that may be of interest in the study of addiction treatment . Preclinical studies have shown that GABA-B receptors have roles in memory storage and retrieval, reward, motivation, mood, as well as anxiety. Neuroimaging studies in humans indicate that baclofen produces region-specific alterations in brain activity.

Trade Name Baclofène
Availability Prescription only
Generic Baclofen
Baclofen Other Names Baclofen, Baclofène, Baclofeno, Baclofenum, DL-Baclofen
Related Drugs Botox, dantrolene, trihexyphenidyl, Artane, Lioresal, onabotulinumtoxinA, Lyvispah, Gablofen, Dantrium, Fleqsuvy
Type
Formula C10H12ClNO2
Weight Average: 213.661
Monoisotopic: 213.05565634
Protein binding

30%

Groups Approved
Therapeutic Class Centrally acting Skeletal Muscle Relaxants
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Baclofène
Baclofène

Uses

Baclofène is used for:

  • Spasm.
  • Spinal cord diseases.
  • Cerebrovascular accidents or neoplastic or degenerative brain disease.
  • Muscle spasm of cerebral origin especially infantile cerebral palsy.
  • The alleviation of spasticity resulting from multiple sclerosis

Baclofène is also used to associated treatment for these conditions: Joint Pain, Soreness, Muscle, Flexor spasm, Reversible Spasticity, Severe cerebral origin Spasticity, Severe spinal cord origin Spasticity

How Baclofène works

The exact mechanism of action of baclofen is not fully understood at this time , . Many studies indicate that baclofen is a GABA-B receptor agonist , , , , . Despite this, there is no conclusive evidence that the effects of baclofen on GABA systems are involved in the production of its clinical effects .

Baclofène is an effective and widely used antispastic agent with a spinal site of action. Its mechanism of action and pharmacological properties are different from the effects of other antispastic agents. In addition, baclofen has central sites of action, shown by its adverse event profile and general CNS depressant properties . GABA-B receptors interact with signal transduction pathways and neurotransmitter systems. Baclofène exerts an antinociceptive effect. The clinical significance of this warrants further research data for clarification.

Baclofène depresses monosynaptic and polysynaptic reflex transmission, by various actions, and possibly including the stimulation of GABAβ-receptors. This stimulation results in the inhibition of excitatory neurotransmitter (glutamate and aspartate) release, which may normally contribute to pain and spasticity. Although baclofen is an analog of the inhibitory neurotransmitter gamma-amino-butyric acid (GABA), there are no conclusive data indicating GABA systems are involved in its clinical effects .

Dosage

Baclofène dosage

Adults:

Treatment should be started with low dose and increased gradually until optimum effect is achieved. The following dosage titration schedule is suggested:

5 mg 3 times daily for 3 days,

10 mg 3 times daily for 3 days,

15 mg 3 times daily for 3 days,

20 mg 3 times daily for 3 days,

25 mg 3 times daily for 3 days.

Thereafter, additional increases may be necessary. The optimum dosage generally ranges from 30 - 80 mg daily in 3 - 4 divided doses. Daily doses of 100 - 120 mg may be given to carefully supervised patients in hospitals.

Children:

Treatment should be started at a very low dose, e.g., 0.3 mg/kg per day in divided (preferably 4) doses. The dosage should be raised cautiously at 1-2 week intervals until it is sufficient for the child\'s individual needs. The usual dosage range for maintenance therapy is 0.75 to 2 mg/kg body weight per day. In children aged over 10 years a maximum daily dose of 2.5 mg/kg body weight may be given.

Renal Insufficiency:

Baclofène is excreted principally in urine as unchanged drug. So it may be necessary to reduce the dosage in patients with impaired renal function.

Side Effects

The most common side effects include drowsiness, nausea, dizziness, lassitude, lightheadedness, confusion, fatigue, muscular pain & weakness and hypotension.

Toxicity

LD50 after oral administration in rats: 145 mg/kg

Overdosage: Vomiting, muscular hypotonia, drowsiness, accommodation disorders, coma, respiratory depression, and seizures may occur with overdosage .

Pregnancy: This drug is a pregnancy category C drug. There are no adequate and well-controlled studies that have been performed with pregnant women. Baclofène should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus .

Excretion in breastmilk: It is unknown whether this drug is excreted in human breast milk. Because many drugs are excreted in human milk, caution is warranted when baclofen is administered to a nursing woman .

Precaution

Patients suffering from psychotic disorders, schizophrenia, depressive or manic disorders, confusional states or Parkinson\'s disease, should be treated cautiously with Baclofène. Baclofène stimulates gastric acid secretion and should be used with caution in patients with a history of peptic ulcer and avoided in those with active peptic ulcer disease . Liver function should be monitored in patients with liver disease; patients with renal impairment need a reduced dose. Baclofène should be used with caution in patients with respiratory impairment. Observations of increased blood sugar concentrations suggest caution in patients with diabetes mellitus. Care is also required in the elderly, in whom adverse effects may be more common, and in patients with cerebrovascular disease (who tolerate Baclofène poorly). Baclofène may cause drowsiness; patients affected should not drive or operate machinery. Abrupt withdrawal of Baclofène may result in a withdrawal syndrome and exacerbation of spasticity; dosage should be reduced gradually over at least 1 to 2 weeks, or longer if symptoms occur.

Interaction

Alcohol and other CNS depressants may exacerbate the CNS effects of Baclofène and should be avoided. There may be increased weakness if Baclofène is given to patients taking a tricyclic antidepressant and an increased hypotensive effect if it is given to patients receiving antihypertensive therapy.

Food Interaction

  • Avoid alcohol.
  • Take with food. Take with food or milk to reduce gastric irritation.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Volume of Distribution

Apparent volume of distribution: 59 liters .

Baclofène does not readily cross the blood-brain barrier .

Elimination Route

Rapidly and almost completely absorbed from the gastrointestinal tract. Absorption may be dose-dependent, being reduced with increased doses .

Baclofène, when introduced directly into the intrathecal space, allows for effective CSF concentrations to be achieved with resulting plasma concentrations 100 times less than concentrations occurring with oral administration , .

Half Life

Elimination half-life: Approximately 5.5 hours .

Clearance

Total systemic clearance: 180 mL/min Renal clearance: 103 mL/min

Baclofène is primarily excreted unchanged by the kidneys. It should be administered cautiously, and it may be necessary to reduce the dosage in patients with reduced renal function .

Elimination Route

Baclofène is rapidly and extensively eliminated from the body. There is significant intersubject variation in elimination rates. Baclofène is excreted mainly by the kidney as unchanged drug. Seventy to eighty (70 - 80%) of a dose is measured in the urine as unchanged drug. The remainder of the dose is excreted as unchanged drug in the feces or as metabolites in the urine and feces. Excretion is complete within 72 hours after administration .

Pregnancy & Breastfeeding use

There are no adequate and well controlled studies of Baclofène in pregnant women. So it should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus.

Baclofène is excreted in breast milk. However, evidence suggests that the quantities are so small that no undesirable effect on the infant would be expected.

Contraindication

Baclofène is contraindicated in patients with hypersensitivity to any component of this product.

Special Warning

Renal Insufficiency: Baclofène is excreted principally in urine as unchanged drug. So it may be necessary to reduce the dosage in patients with impaired renal function.

Acute Overdose

Prominent features are signs of central nervous system depression. No specific antidote of Baclofène is known. Elimination of the agent from GI tract, artificial respiration, administration of fluid with a diuretic and dialysis should be considered.

Interaction with other Medicine

Alcohol and other CNS depressants may exacerbate the CNS effects of Baclofène and should be avoided. There may be increased weakness if Baclofène is given to patients taking a tricyclic antidepressant and an increased hypotensive effect if it is given to patients receiving antihypertensive therapy.

Storage Condition

Store in cool & dry place, away from children.

Innovators Monograph

You find simplified version here Baclofène

Baclofène contains Baclofen see full prescribing information from innovator Baclofène Monograph, Baclofène MSDS, Baclofène FDA label

FAQ

What is Baclofène used for?

Baclofène is used to help relax certain muscles in your body. It relieves the spasms, cramping, and tightness of muscles caused by medical problems, such as multiple sclerosis or certain injuries to the spine.

How safe is Baclofène?

Baclofène can cause a severe allergic reaction. Symptoms can include trouble breathing and swelling of your throat or tongue. If you have an allergic reaction, call your doctor or local poison control center right away.

How does Baclofène work?

Baclofène is believed to work by activating (or agonizing) GABA receptors, specifically the GABAB receptors.

What are the common side effects of Baclofène?

Common side effects of Baclofène are include:

  • dizziness
  • weakness
  • confusion
  • headache
  • nausea
  • constipation
  • difficulty falling asleep or staying asleep
  • tiredness
  • frequent urination

Is Baclofène safe during pregnancy?

There is no evidence that taking Baclofène during pregnancy increases the chance of having a baby with birth defects above the background risk. There are also several case reports of children that were exposed to Baclofène during pregnancy and did not have birth defects.

Is Baclofène safe during breastfeeding?

Limited information indicates that orally administered Baclofène appears in low levels in milk and would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months.

Can I drink alcohol with Baclofène?

If you, or a loved one, have been prescribed Baclofène for any condition, refrain from alcohol while taking the Baclofène.

Can I drive after taking Baclofène?

Some people may feel drowsy and/or dizzy or have problems with their eyes while they are taking Baclofène tablets. If this happens, you should not drive or do anything that requires you to be alert (such as operate tools or machinery) until these effects have worn off.

How often can I take Baclofène?

It usually is taken 3 times a day at evenly spaced intervals.

What time should I take Baclofène?

Take Baclofène with a snack or just after eating a meal. Try to take your doses at the same times of day each day, as this will help you to remember to take them.

How long does Baclofène take to work?

Most people start to feel the effects within an hour of taking Baclofène.

How long does Baclofène stay in my system?

Since Baclofène is eliminated via urine, it can be detected in a urine screen for up to two days. 

How long can I take Baclofène?

The simple answer is as long as it's needed. There's no upper or lower limit on the length of treatment. I generally suggest starting with 12 months of treatment and reviewing from there. Baclofène has been used in patients for over 40 years so we know that it's safe over the long term.

What happens if I miss a dose?

Take the Baclofène as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention. Overdose symptoms may include muscle weakness, vomiting, severe dizziness or drowsiness, dilated or pinpoint pupils, shallow breathing, seizure, or loss of consciousness.

Who should not take Baclofène?

Do not use Baclofène at a time when you need muscle tone for safe balance and movement during certain activities. Do not drive or operate heavy machinery until you know how this medicine affects you.

What happen If I stop taking Baclofène?

Do not stop using baclofen suddenly, or you could have unpleasant withdrawal symptoms. Withdrawal from Baclofène can have clinical manifestations that include agitation, insomnia, confusion, delusions, hallucinations, seizures, visual changes, psychosis, dyskinesia, hyperthermia, and increased spasticity.

Can Baclofène affect my kidneys?

Baclofène a commonly prescribed muscle relaxant, is primarily excreted via the kidneys; toxicity is a potentially serious adverse outcome in patients with decreased kidney function.

Can Baclofène affects my liver?

Baclofène is safe to use in patients with liver damage and even cirrhosis because most Baclofène simply passes out in the urine and doesn't rely on liver metabolism.

*** Taking medicines without doctor's advice can cause long-term problems.
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