Baclosal
Baclosal Uses, Dosage, Side Effects, Food Interaction and all others data.
Baclosal 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. Baclosal, when used as indicated, improves mobility, increasing levels of independence, and facilitates both passive and active physiotherapy. Baclosal also stimulates gastric acid secretion .
GABA-B receptor activation by baclofen may produce protective neurological effects. Baclosal 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 | Baclosal |
| 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 | Israel, Latvia, Lithuania |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Baclosal 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
Baclosal 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 Baclosal 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 .
Baclosal 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. Baclosal exerts an antinociceptive effect. The clinical significance of this warrants further research data for clarification.
Baclosal 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
Baclosal 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:
Baclosal 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. Baclosal 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 Baclosal. Baclosal 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. Baclosal 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 Baclosal poorly). Baclosal may cause drowsiness; patients affected should not drive or operate machinery. Abrupt withdrawal of Baclosal 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 Baclosal and should be avoided. There may be increased weakness if Baclosal 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.
Baclosal Drug Interaction
Major: acetaminophen / hydrocodone, acetaminophen / hydrocodoneModerate: duloxetine, duloxetine, pregabalin, pregabalin, alprazolam, alprazolam, cetirizine, cetirizineUnknown: polyethylene glycol 3350, polyethylene glycol 3350, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Baclosal Disease Interaction
Major: renal dysfunctionModerate: autonomic dysreflexia, psychoses, seizure disorders
Volume of Distribution
Apparent volume of distribution: 59 liters .
Baclosal 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 .
Baclosal, 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
Baclosal 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
Baclosal is rapidly and extensively eliminated from the body. There is significant intersubject variation in elimination rates. Baclosal 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 Baclosal in pregnant women. So it should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus.
Baclosal 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
Baclosal is contraindicated in patients with hypersensitivity to any component of this product.
Special Warning
Renal Insufficiency: Baclosal 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 Baclosal 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 Baclosal and should be avoided. There may be increased weakness if Baclosal 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 Baclosal
Baclosal contains Baclofen see full prescribing information from innovator Baclosal Monograph, Baclosal MSDS, Baclosal FDA label
FAQ
What is Baclosal used for?
Baclosal 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 Baclosal?
Baclosal 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 Baclosal work?
Baclosal is believed to work by activating (or agonizing) GABA receptors, specifically the GABAB receptors.
What are the common side effects of Baclosal?
Common side effects of Baclosal are include:
- dizziness
- weakness
- confusion
- headache
- nausea
- constipation
- difficulty falling asleep or staying asleep
- tiredness
- frequent urination
Is Baclosal safe during pregnancy?
There is no evidence that taking Baclosal 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 Baclosal during pregnancy and did not have birth defects.
Is Baclosal safe during breastfeeding?
Limited information indicates that orally administered Baclosal 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 Baclosal?
If you, or a loved one, have been prescribed Baclosal for any condition, refrain from alcohol while taking the Baclosal.
Can I drive after taking Baclosal?
Some people may feel drowsy and/or dizzy or have problems with their eyes while they are taking Baclosal 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 Baclosal?
It usually is taken 3 times a day at evenly spaced intervals.
What time should I take Baclosal?
Take Baclosal 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 Baclosal take to work?
Most people start to feel the effects within an hour of taking Baclosal.
How long does Baclosal stay in my system?
Since Baclosal is eliminated via urine, it can be detected in a urine screen for up to two days.
How long can I take Baclosal?
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. Baclosal 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 Baclosal 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 Baclosal?
Do not use Baclosal 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 Baclosal?
Do not stop using baclofen suddenly, or you could have unpleasant withdrawal symptoms. Withdrawal from Baclosal can have clinical manifestations that include agitation, insomnia, confusion, delusions, hallucinations, seizures, visual changes, psychosis, dyskinesia, hyperthermia, and increased spasticity.
Can Baclosal affect my kidneys?
Baclosal 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 Baclosal affects my liver?
Baclosal is safe to use in patients with liver damage and even cirrhosis because most Baclosal simply passes out in the urine and doesn't rely on liver metabolism.
