Baclofen

Baclofen also known as beta‐4‐chlorophenyl‐gamma‐aminobutyric acid, sold by brand names Kemstro, Lioresal, Fleqsuvy, Lyvispah, Ozobax and Gablofen, is a prescription muscle relaxant drug that is used to treat pain and certain types of spasticity (muscle stiffness and tightness) most often used by people with multiple sclerosis, spinal cord injuries, or other spinal cord diseases ¹, ², ³, ⁴, ⁵, ⁶ . Baclofen reduces the number and severity of muscle spasms and relieves pain, clonus and muscle rigidity due to spasticity. Baclofen was approved for use in the United States in 1977 and is widely used with several million prescriptions filled yearly ⁷, ⁸.

Baclofen is a gamma-amino butyric acid type B (GABA_B) agonist that acts as an agonist of the GABA B receptor, thereby activating potassium channels and reducing calcium conductance leading to hypotonia and muscle relaxation ⁷. Baclofen acts on the nerves in the central nervous system (brain and spinal cord) primarily at the level of the spinal cord by stopping synaptic reflexes to reduce the messages that are sent out by the central nervous system (brain and spinal cord) to cause muscle contraction, therefore decreasing the number and severity of muscle spasms caused by multiple sclerosis or spinal cord conditions. Baclofen also relieves pain and improves muscle movement. Baclofen may also be used to relieve other conditions as determined by your doctor. Baclofen does not cure these problems, but it may allow other treatment, such as physical therapy, to be more helpful in improving your condition.

Baclofen is indicated primarily for treatment of spasticity from spinal cord injuries and multiple sclerosis. Baclofen has been used off label as add-on therapy to help people with alcohol use disorder with alcohol abstinence and withdrawal ³, ⁴, ⁵.

Baclofen comes as a tablet and a solution (liquid) to take by mouth. Baclofen is also available in various generic forms as well as under the brand names of Lioresal and Remular in tablets of 10 or 20 mg and in formulations for intrathecal injections of 0.5 mg/mL. The recommended adult dose for spasticity is 10 to 20 mg orally three to four times daily at evenly spaced intervals. The dose should be increased and tapered gradually.

Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take baclofen exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Use an oral syringe (measuring device) to accurately measure and take your dose of baclofen solution. Ask your pharmacist for an oral syringe if one is not included with your medication.

If baclofen tablets or liquid do not work well for you or your child, you may be prescribed a baclofen injection. This will be given by a specialist doctor in hospital. Baclofen can also be given through a pump that is fitted under the skin.

The most common side effects of baclofen are transient sedation, confusion, muscle weakness, vertigo, nausea, drowsiness, dizziness and fatigue ⁹.

Continue to take baclofen even if you feel well. Do not stop taking baclofen without talking to your doctor, especially if you have taken large doses for a long time. Abruptly stopping baclofen can cause seizures, fever, confusion, muscle stiffness, or hallucinations. Your doctor probably will want to decrease your baclofen dose gradually.

Baclofen key points to remember:

Baclofen reduces pain and discomfort caused by muscle spasms.
Baclofen is not recommended for use in patients with Parkinson disease and stroke due to a lack of reassuring data. In addition, baclofen is not indicated for skeletal muscle spasms associated with rheumatologic disorders.
Baclofen tablets and liquid start to work after 1 hour after taking it. However, it might take a few days before you find the right dose to control your symptoms.
Baclofen common side effects include feeling sleepy and feeling sick (nausea).
Close supervision of patients being treated with baclofen who have depression or a history of previous suicide attempts is recommended.
Recent coronial inquiries into 2 deaths have highlighted the need for health professionals to be alert to the well documented risk of overdose with baclofen ¹⁰.
Do not stop taking baclofen without talking to your doctor. Abrupt discontinuation of oral baclofen therapy might cause seizures and hallucinations. Gradual dose reduction is recommended to prevent withdrawal symptoms ¹¹, ¹².
If your doctor decides to stop your treatment, your dose will be reduced gradually over 1 to 2 weeks.
It’s best not to drink alcohol while you are taking baclofen until you know how it affects you. There’s a risk alcohol may increase drowsy side effects and make you very sleepy.

How long does baclofen take to work?

Baclofen tablets and liquid start to work after 1 hour of taking it. However, it might take a few days before you find the right dose to control your symptoms. Baclofen is usually started at a low dose and slowly increased over a few days.

What will happen if I stop taking baclofen?

If your doctor decides to stop your treatment, your Baclofen dose will be reduced gradually over 1 to 2 weeks.

This will stop you getting withdrawal symptoms such as:

feeling anxious or confused
seeing things that are not there (hallucinations)
seizures or fits
changes in mood or behavior
a fast heartbeat
muscle spasms getting worse

Can I drive or ride a bike while taking baclofen?

Baclofen may make you feel tired, sleepy or dizzy and can affect your vision. It might be best to stop driving and cycling for the first few days of treatment until you know howBaclofen makes you feel.

It’s an offence to drive a car if your ability to drive safely is affected. It’s your responsibility to decide if it’s safe to drive.

Can I drink alcohol while taking baclofen?

Alcohol may increase the drowsy (sedative) effects of baclofen tablets and make you very sleepy. It’s best not to drink alcohol while you are taking baclofen until you know how the medicine makes you feel.

Will recreational drugs affect baclofen?

Using cannabis, heroin or methadone with baclofen will increase the drowsy effects of baclofen. It can make you go into a very deep sleep. There’s a risk you will not be able to breathe properly, and you may have difficulty waking up.

Using cocaine or other stimulants like MDMA (ecstasy) and amphetamines with baclofen can also make you drowsy.

Talk to your doctor if you think you might use recreational drugs while taking baclofen.

Is baclofen addictive?

Yes, Baclofen is addictive. Those who engage in baclofen abuse – including taking higher doses than prescribed or mixing it with alcohol or drugs – are at an increased risk of developing an addiction to the drug.

Usually, baclofen addiction begins with increased tolerance, which is when the person has to use more of the drug to experience the same effect. A patient who’s becoming tolerant to the drug may take more than their doctor prescribed to them to experience relief.

Eventually, physical dependence may occur, which is when the person experiences withdrawal symptoms when they aren’t taking the drug. Oftentimes, people who are physically dependent on a drug may keep taking it simply to avoid withdrawals.

After a while, however, their tolerance will continue to grow, and their drug use will become more severe. There are also some people who take baclofen to get high.

Like alcohol and other GABA agonists, baclofen can produce a high when taken in high enough doses, which can encourage further drug-taking behavior. As previously mentioned, there’s a high risk of baclofen overdose when the drug is consistently abused.

If you notice that your tolerance to baclofen has increased, speak to your doctor right away. Do not take higher doses than you’ve been prescribed.

Signs of Baclofen Abuse

People who abuse their prescription drugs may exhibit certain physical and behavioral signs. Some signs of baclofen abuse to look out for include:

Doctor shopping (switching from one doctor to the next for prescriptions)
Lying or stealing to get more of the drug
Mood swings
Decreased performance at school, work, or home
Withdrawal from loved ones
Lack of interest in activities they once liked
Stupor
Hallucinations
Seizures
Shock
Difficulty breathing
Cardiac arrest
Coma
Death

If you’re taking baclofen or any prescription muscle relaxers, be sure to take them exactly as prescribed. If you experience any adverse side effects while taking a prescription medication, speak to your doctor about adjusting your dose or other alternatives.

Will baclofen affect my contraception?

Baclofen does not affect any type of contraception, including the combined pill or emergency contraception.

However, if baclofen makes you sick (vomit) or have severe diarrhea for more than 24 hours, your contraceptive pills may not protect you from pregnancy. Check the pill packet to find out what to do.

Baclofen Mechanism of Action

Baclofen also known as beta‐4‐chlorophenyl‐gamma‐aminobutyric acid (GABA-B) is an agonist at the beta subunit of gamma-aminobutyric acid on mono and polysynaptic neurons at the spinal cord level and brain ¹³. The thinking is that baclofen reduces the release of excitatory neurotransmitters in the pre-synaptic neurons and stimulates inhibitory neuronal signals in the post-synaptic neurons with resultant relief of spasticity ¹⁴. Baclofen is also found to have an affinity for voltage-gated calcium channels. However, its clinical efficacy in this regard is still unclear ¹.

Baclofen has a 70% to 85% bioavailability and is rapidly absorbed through the gastrointestinal tract following oral administration. Peak plasma concentrations are generally observed 2 to 3 hours after ingestion. The absorption is dose-dependent and increases with higher doses. Due to the short half-life of 2 to 6 hours, baclofen should be administrated frequently to achieve optimal effect. Seventy percent of baclofen is eliminated in an unchanged form by renal excretion and the remaining via feces. Thereby, baclofen is a useful agent in patients with impaired hepatic function or a high potential for cytochrome P450-mediated drug-drug interactions. Research has observed significant inter-individual variability in baclofen’s absorption and elimination processes.

Baclofen special precautions

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if baclofen is working properly and to decide if you should continue to take it.

Do not suddenly stop using baclofen without checking first with your doctor. You may need to slowly decrease your dose before stopping it completely. Unwanted side effects (eg, hallucinations, seizures, high fever, rhabdomyolysis) may occur if baclofen is stopped suddenly.

Baclofen will add to the effects of alcohol and other central nervous system depressants (medicines that slow down the nervous system, possibly causing drowsiness). Some examples of central nervous system depressants are antihistamines or medicine for hay fever, other allergies, or colds, sedatives, tranquilizers, or sleeping medicine, prescription pain medicine or narcotics, medicine for seizures or barbiturates, other muscle relaxants, or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the above while you are using baclofen.

Baclofen may cause dizziness, drowsiness, vision problems, or clumsiness or unsteadiness in some people. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are not alert, well-coordinated, and able to see well.

Baclofen may affect blood sugar levels. If you notice a change in the results of your blood or urine sugar tests or if you have any questions, check with your doctor.

Using Baclofen while you are pregnant may cause neonatal withdrawal syndrome in your newborn babies. Tell your doctor right away if your baby has shakiness or tremors, seizures, or increased muscle tone.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Before taking Baclofen:

Use with caution when used in patients with urinary retention or respiratory disease.
History of autonomic dysreflexia: Abrupt baclofen withdrawal or the presence of nociceptive stimuli can cause an autonomic dysreflexic episode.
Gastrointestinal disorders: Use caution in patients with peptic ulcer disease, decreased GI motility, and/or GI obstructive disorders.
Use caution in patients with confusional states, psychotic issues, or schizophrenia; it may cause exacerbation of the condition. In addition, patients treated with baclofen injection should be kept under surveillance because exacerbations of these conditions have been observed with oral administration.
Use caution in patients with kidney impairment, as baclofen is primarily eliminated via the kidneys.
Seizure disorder: Loss of seizure control is reported in patients treated with baclofen; monitor patients with a history of seizure disorder by checking electroencephalogram periodically.
Co-administration of epidural morphine and baclofen injection is reported to cause dyspnea and hypotension.
Because of the risk of sedation, patients should refrain from operating automobiles or other dangerous machinery, and activities made hazardous by decreased alertness. In addition, the central nervous system effects of baclofen may be additive to those of alcohol and other central nervous system (CNS) depressants.
Tell your doctor and pharmacist if you are allergic to baclofen, any other medications, or any of the ingredients in baclofen tablets and oral solution. Ask your pharmacist for a list of the ingredients.
Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antidepressants, medications for anxiety, medications for mental illness, medications for seizures, sedatives, sleeping pills, or tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
Tell your doctor if you have or have ever had epilepsy, a stroke, a rheumatic disease, cerebral palsy, Parkinson’s disease, a psychiatric condition such as schizophrenia or a confusional state, or kidney disease.
Tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking baclofen, call your doctor immediately.
You should know that baclofen may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
Ask your doctor about the safe use of alcoholic beverages while you are taking baclofen. Alcohol can make the side effects from baclofen worse.

In deciding to use a medicine, the risks of taking Baclofen must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Who can take baclofen?

Most adults and children aged 1 month and older can take baclofen tablets and liquid.

Baclofen injection can be given to adults and children aged 4 years and over.

How long to take baclofen for?

You may need to take baclofen for a long time to control muscle spasms.

If you’ve been having baclofen through an injection or pump for a long time, you may find that it stops working as well as it used to. You may need to stop having treatment for a short time to give your body a rest. Your doctor will be able to give you advice on this.

Stopping baclofen

If you stop taking baclofen suddenly, you may get withdrawal side effects such as:

feeling anxious or confused
seeing things that are not there (hallucinations)
seizures or fits
changes in mood or behavior
a fast heartbeat
muscle spasms getting worse

You doctor will reduce your dose gradually before stopping it completely. This will help prevent these side effects.

Who may not be able to take baclofen?

Baclofen is not suitable for some people. To make sure it’s safe for you, tell your doctor before taking Baclofen if you:

have ever had an allergic reaction to baclofen or any other medicine
have a stomach ulcer
have lung, kidney or liver disease
have a mental health condition
have epilepsy
have Parkinson’s disease
have diabetes
have ever had a stroke
are being treated for high blood pressure
have difficulty peeing
have a rare blood disorder called porphyria
are pregnant, trying to get pregnant or breastfeeding

Baclofen contraindications

Baclofen is contraindicated in patients with hypersensitivity to baclofen or any component of its formulation. The baclofen injection solution is not recommended for intravenous, subcutaneous, intramuscular, or epidural administration.

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children

Appropriate studies have not been performed on the relationship of age to the effects of Baclofen oral liquid and granules in children younger than 12 years of age. Safety and efficacy have not been established.

Appropriate studies have not been performed on the relationship of age to the effects of Baclofen tablets in the pediatric population. Safety and efficacy have not been established..

Elderly people

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of Baclofen oral liquid and granules in the elderly. However, elderly patients are more likely to have age-related kidney, liver, or heart problems, which may require caution for patients receiving Baclofen.

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of baclofen tablet in the elderly. Side effects such as hallucinations, confusion or mental depression, other mood or mental changes, and severe drowsiness may be especially likely to occur in elderly patients, who are usually more sensitive than younger adults to the effects of Baclofen.

Balofen and pregnancy warnings

Baclofen should be used during pregnancy only if the benefit outweighs the risk.

US FDA pregnancy category: Not Assigned. The US FDA has amended the pregnancy labeling rule for prescription drug products to require labeling that includes a summary of risk, a discussion of the data supporting that summary, and relevant information to help health care providers make prescribing decisions and counsel women about the use of drugs during pregnancy. Pregnancy categories A, B, C, D and X are being phased out.
Australian TGA pregnancy category B3: Drugs which have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malformation or other direct or indirect harmful effects on the human fetus having been observed. Studies in animals have shown evidence of an increased occurrence of fetal damage, the significance of which is considered uncertain in humans.

Baclofen given orally in animal studies has been shown to increase the incidence of omphaloceles (ventral hernias) in fetuses at approximately 13 times on a mg/kg basis, or 3 times on a mg/m² basis, the maximum oral dose recommended for humans; this dose also caused reductions in food intake and weight gain in the dams. There are no controlled data in human pregnancy. It is not known whether this drug can cause fetal harm or adversely affect reproductive capacity in humans.

Baclofen and breastfeeding

There are no adequate studies in women for determining infant risk when using Baclofen during breastfeeding, but information shows that it passes into breast milk in small amounts. Weigh the potential benefits against the potential risks before taking Baclofen while breastfeeding.

Contact your pharmacist or doctor as soon as possible if your baby:

is not feeding as well as usual or seems to have a dry mouth
seems unusually sleepy
is sweaty or develops a rash
is being sick or has diarrhea
is causing you any other concerns

Drug interactions

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking Baclofen, it is especially important that your healthcare provider know if you are taking any of medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using Baclofen with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Alfentanil
Alprazolam
Amifampridine
Benzhydrocodone
Bromazepam
Buprenorphine
Bupropion
Butorphanol
Calcium Oxybate
Cannabidiol
Cannabis
Cetirizine
Clobazam
Clonazepam
Codeine
Daridorexant
Dexmedetomidine
Dihydrocodeine
Donepezil
Doxylamine
Esketamine
Fentanyl
Flibanserin
Gabapentin
Gabapentin Enacarbil
Hydrocodone
Hydromorphone
Ketamine
Lacosamide
Lemborexant
Levocetirizine
Levorphanol
Lofexidine
Loxapine
Magnesium Oxybate
Meperidine
Methadone
Metoclopramide
Midazolam
Morphine
Morphine Sulfate Liposome
Nalbuphine
Oxycodone
Oxymorphone
Pentazocine
Periciazine
Phenobarbital
Potassium Oxybate
Pregabalin
Primidone
Remifentanil
Remimazolam
Ropeginterferon Alfa-2b-njft
Scopolamine
Sodium Oxybate
Sufentanil
Tapentadol
Topiramate
Tramadol
Trazodone
Zolpidem
Zuranolone

Other Interactions

Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of Baclofen with alcohol or tobacco.

Mixing baclofen with herbal remedies and supplements

There’s not enough information to say that herbal remedies and supplements are safe to take with baclofen. They’re not tested in the same way as pharmacy and prescription medicines. They’re generally not tested for the effect they have on other medicines.

Baclofen uses

Baclofen is a muscle relaxant that is used to relieve muscle spasms, cramping or tightness caused by conditions such as ¹⁵, ¹⁶, ¹⁷, ¹⁸, ¹⁹, ¹⁹, ²⁰:

Cerebral palsy. Baclofen is also considered for short-term treatment for spasticity associated with cerebral palsy in children and adolescents.
Meningitis
Motor neurone disease
Multiple sclerosis (MS)
Conditions affecting your brain, spinal cord and nervous system causing stiff limbs and/or some bladder dysfunctions.

Long-term (chronic) muscle stiffness can happen in conditions where the nerves that supply your muscles have been damaged. In these conditions, the muscles shorten (contract) tightly, and can then become stiff and harder to use. This is called muscle spasticity. Baclofen works by relaxing your muscles, which reduces pain and discomfort.

FDA-approved indications ²¹:

Baclofen is FDA-approved for managing reversible spasticity, particularly to relieve flexor spasms, clonus, concomitant pain, common sequelae of spinal cord lesions, and multiple sclerosis.
Intrathecal baclofen administration is FDA-approved for managing spasticity of cerebral origins, such as traumatic brain injury or severe spasticity of spinal cord origin that is unresponsive to treatment with maximum doses of oral baclofen, tizanidine, and/or dantrolene. However, intrathecal baclofen might be considered for patients who experience intolerable adverse effects or fail to respond to oral therapy.

Baclofen Off-labeled Uses ²², ¹³, ²³:

Baclofen is currently prescribed off-label to treat alcohol use disorder²⁴, ²⁵, ²⁶:
- Baclofen is used off-label to manage alcoholic liver disease.
- Maintain alcohol abstinence by decreasing alcohol cravings and alcohol-related anxiety.
Trigeminal neuralgia, gastroesophageal reflux disease, and hiccups.

Intrathecal baclofen

Baclofen is a muscle relaxant that works on the nerves in the brain and spinal cord, reducing the messages that are sent out by the nervous system to cause muscle contraction. It is used in children to treat severe muscle spasm (spasticity), due to cerebral palsy or other conditions that affect the brain or spinal cord. It acts on the whole body and does not target specific muscles.

The benefits of baclofen relaxing muscles include:

Improved ability to move joints
Less pain due to muscle spasm or cramps

Before you or your child’s doctors decide if intrathecal baclofen is right for you or your child, many specialists will thoroughly assess your child. You or your child may be seen by an orthopaedic surgeon, a neurosurgeon, different specialists, an occupational therapist and a physiotherapist.

There are many factors to consider when deciding who should have intrathecal baclofen treatment. Intrathecal baclofen does not suit every person or every family. You will need to live close to a medical center that can manage the baclofen therapy and you or your child will need to attend many appointments. All the people who help care for you or your child need to learn about baclofen and its side effects.

Once you or your child’s doctors and you have decided that intrathecal baclofen therapy might be right for you or your child, you will be booked in for a trial of the therapy, which will take place in hospital and involve a general anaesthetic. There are two types of trial:

A bolus trial also called a single-dose test trial involves an injection of baclofen into the space surrounding your child’s spinal cord.
A five-day catheter trial also called a tube trial involves an operation to have a tube placed in the spine. The tube is joined to an access port through which baclofen is delivered to your child’s spine.

The doctor will choose the most appropriate trial for you or your child. If you or your child responds well to the trial, you will have an appointment with a neurosurgeon to discuss the operation to insert the pump and how the pump works.

While your child is asleep (under a general anaesthetic), a neurosurgeon will implant the pump (about the size of a computer mouse) into you or your child’s abdomen on one side near the hip bone. Joined to the pump is a long catheter, which is inserted into the space surrounding your spinal cord. You or your child will be in the operating theatre for about two hours.
A very small computer, called a programmer, tells the pump how much medicine to release. The baclofen will last from one to six months, depending on you or your child’s dose. When the medicine is running low, you or your child will have an appointment to have you or your child’s pump refilled.

Intrathecal baclofen works differently for every person. Even though they have done a trial, your doctors cannot predict exactly how you or your child will respond to intrathecal baclofen therapy.

Complications of intrathecal baclofen therapy

Complications are rare, but it is important to know the possible side effects and what to do if something goes wrong. Side effects of baclofen may include constipation, nausea and blurred vision. These usually settle over time, but if they continue, they can be managed in various ways, which you can discuss with your child’s doctor.

Possible complications of intrathecal baclofen include:

overdose of baclofen
underdose (not enough) of baclofen
infection of the site around the pump or tube
infection of the wound from the surgery
catheter kink (bent tubing), which prevents the flow of baclofen
catheter break, causing a leak of baclofen
catheter disconnection from pump, preventing baclofen from reaching spinal cord
pump stops working properly.

Baclofen overdose primarily arises from drug screening before pump implantation or human error during pump refilling and programming. Baclofen overdose may cause altered mental status, somnolence, seizure, hypothermia, respiratory depression, and coma. In the presence of Baclofen overdose symptoms, the medical staff should empty the pump reservoir, and the patient should receive symptomatic management ²⁷. In patients when the lumbar puncture is not contraindicated, consider withdrawing 30-40 mL of CSF to reduce baclofen CSF concentration.

See your child’s baclofen doctor or take your child to the hospital emergency room if:

your child has a temperature higher than 100.4 °F (38 ºC)
there is redness or inflammation around the surgery site
there is swelling around the pump area
your child is drowsy or you can’t wake them
your child has slow breathing
you think your child is too ‘floppy’
your child is unusually sweaty, itchy or grumpy
your child’s muscles are tighter than usual
you are concerned about the pump
you hear beeping from the pump.

Monitoring

Administration of baclofen with any other central nervous system depressants requires close monitoring. Patients with epilepsy should be monitored with a regular electroencephalogram due to deterioration in seizure control when receiving baclofen ²⁸.

Monitor for signs and symptoms of baclofen withdrawal if the dose is reduced or discontinued ²⁹.

Intrathecal baclofen use requires careful attention to program the infusion pump and monitor its function, pump alarms, and refill schedules ³⁰.

Closely monitor when the initial phase of pump use and when adjusting the dosing rate and/or the concentration in the reservoir as small errors can result in subtherapeutic level or toxic levels.

Monitor for signs or symptoms of overdose which may occur suddenly, especially in the initial screening phase, dose-titration phase, and reintroduction of therapy after temporary cessation of treatment.

Baclofen dosage

Take Baclofen exactly as directed by your doctor. Do not take more of it, do not take it more often, or do not take it longer than your doctor ordered.

Baclofen comes with a patient information and instructions leaflet. Read and follow the instructions carefully. Ask your doctor if you have any questions.

To use Baclofen granules:

Open the packet and empty all the granules directly into your mouth. The granules will dissolve in your mouth or can be swallowed. You may drink water after taking the medicine.
You may mix the granules with 1 tablespoon (15 mL) of liquid (eg, apple juice or milk) or soft foods (eg, applesauce, pudding, or yogurt). Take this mixture within 2 hours of mixing.
Baclofen can also be given using a nasogastric or gastric feeding tube. Mix the granules with 1 tablespoon (15 mL) of liquid (eg, apple juice or milk). Give this mixture within 2 hours of mixing. After Baclofen is given, flush the tube with an additional 1 tablespoon (15 mL) of water.
Take all the contents of the packet to get a full dose. Do not take only part of this medicine. Do not save a portion for later use.

Measure the oral liquid with a marked measuring spoon, oral syringe, or medicine cup.

The dose of Baclofen will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of Baclofen. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of Baclofen. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take Baclofen depend on the medical problem for which you are using Baclofen.

Muscle relaxation

For oral dosage form (granules):
- Adults and children 12 years of age and older: At first, 5 milligrams (mg) 3 times a day for 3 days. Your doctor may increase your dose by 5 mg every 3 days as needed and tolerated. However, the dose is usually not more than 80 milligrams (mg) per day (20 mg four times a day).
- Children younger than 12 years of age: Use and dose must be determined by your doctor.
For oral dosage form (solution):
- Adults and children 12 years of age and older: At first, 5 milliliters (mL) 3 times a day for 3 days. Your doctor may increase your dose by 5 mL every 3 days as needed and tolerated. However, the dose is usually not more than 80 milligrams (mg) per day (20 mg four times a day).
- Children younger than 12 years of age: Use and dose must be determined by your doctor.
For oral dosage form (tablets):
- Adults and teenagers: At first, 5 milligrams (mg) 3 times a day. Your doctor may increase your dose by 5 mg every 3 days until the desired response is reached. However, the dose is not more than 80 mg per day.
- Children: Use and dose must be determined by your doctor.

What should I do if I forget a dose?

If you miss a dose of Baclofen, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Baclofen side effects

Baclofen may cause side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common side effects:

confusion
constipation
dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
headache
increased need to urinate
nausea
passing urine more often
sweating
trouble sleeping
unusual tiredness or weakness

Less common or rare side effects:

diarrhea
loss of appetite
muscle or joint pain
numbness or tingling in the hands or feet
stomach pain or discomfort
stuffy nose
weight gain

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Tell your doctor if any of these symptoms are severe or do not go away:

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

Some side effects can be serious. If you experience either of the following symptoms, see your doctor immediately:

seeing things or hearing voices that do not exist (hallucinations)
seizures

Baclofen overdose

The risks of Baclofen overdose are particularly pronounced when using high doses for off-label treatment of alcohol-use disorder. In case of Baclofen overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call your local emergency services number for help.

Symptoms of Baclofen overdose may include:

blurred vision or vision problems
dizziness
vomiting
drowsiness
irregular, fast or slow, or shallow breathing
difficulty breathing
lightheadedness
loss of strength or energy
muscle pain or weakness
weak muscle tone
pale or blue lips, fingernails, or skin
seizures
sleepiness or unusual drowsiness
trouble breathing
unusual weak feeling
coma.

Overdosed on baclofen tablets has reported vomiting, drowsiness, muscular hypotonia, accommodation disorders, coma, respiratory depression, and seizures. When the patient is alert, consider vacating the stomach immediately by inducing emesis and then performing lavage. In the unconscious patients, do not induce vomiting. Before beginning lavage, secure the airway with an endotracheal tube. Avoid the use of respiratory stimulants and adequately maintain respiratory exchange.

References

Ghanavatian S, Derian A. Baclofen. [Updated 2022 Dec 11]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK526037
Baclofen. https://medlineplus.gov/druginfo/meds/a682530.html
Burnette EM, Nieto SJ, Grodin EN, Meredith LR, Hurley B, Miotto K, Gillis AJ, Ray LA. Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder. Drugs. 2022 Feb;82(3):251-274. doi: 10.1007/s40265-021-01670-3
Andrade C. Individualized, High-Dose Baclofen for Reduction in Alcohol Intake in Persons With High Levels of Consumption. J Clin Psychiatry. 2020 Aug 4;81(4):20f13606. doi: 10.4088/JCP.20f13606
Agabio R, Saulle R, Rösner S, Minozzi S. Baclofen for alcohol use disorder. Cochrane Database of Systematic Reviews 2023, Issue 1. Art. No.: CD012557. https://doi.org/10.1002/14651858.CD012557.pub3
Steardo L, Leo A, Marano E. Efficacy of baclofen in trigeminal neuralgia and some other painful conditions. A clinical trial. Eur Neurol. 1984;23(1):51-5. doi: 10.1159/000115677
Kent CN, Park C, Lindsley CW. Classics in Chemical Neuroscience: Baclofen. ACS Chem Neurosci. 2020 Jun 17;11(12):1740-1755. doi: 10.1021/acschemneuro.0c00254
LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Baclofen. [Updated 2017 Jan 30]. Available from: https://www.ncbi.nlm.nih.gov/books/NBK548081
Alstermark C, Amin K, Dinn SR, Elebring T, Fjellström O, Fitzpatrick K, Geiss WB, Gottfries J, Guzzo PR, Harding JP, Holmén A, Kothare M, Lehmann A, Mattsson JP, Nilsson K, Sundén G, Swanson M, von Unge S, Woo AM, Wyle MJ, Zheng X. Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors. J Med Chem. 2008 Jul 24;51(14):4315-20. doi: 10.1021/jm701425k
Use caution when prescribing baclofen off label. https://www.tga.gov.au/news/safety-updates/use-caution-when-prescribing-baclofen-label
Greenberg MI, Hendrickson RG. Baclofen withdrawal following removal of an intrathecal baclofen pump despite oral baclofen replacement. J Toxicol Clin Toxicol. 2003;41(1):83-5. doi: 10.1081/clt-120018277
Dario A, Tomei G. A benefit-risk assessment of baclofen in severe spinal spasticity. Drug Saf. 2004;27(11):799-818. doi: 10.2165/00002018-200427110-00004
Albright AL. Baclofen in the treatment of cerebral palsy. J Child Neurol. 1996 Mar;11(2):77-83. doi: 10.1177/088307389601100202
Gracies JM, Nance P, Elovic E, McGuire J, Simpson DM. Traditional pharmacological treatments for spasticity. Part II: General and regional treatments. Muscle Nerve Suppl. 1997;6:S92-120.
Simon O, Yelnik AP. Managing spasticity with drugs. Eur J Phys Rehabil Med. 2010 Sep;46(3):401-10. https://www.minervamedica.it/en/journals/europa-medicophysica/article.php?cod=R33Y2010N03A0401
Bendtsen L, Zakrzewska JM, Abbott J, Braschinsky M, Di Stefano G, Donnet A, Eide PK, Leal PRL, Maarbjerg S, May A, Nurmikko T, Obermann M, Jensen TS, Cruccu G. European Academy of Neurology guideline on trigeminal neuralgia. Eur J Neurol. 2019 Jun;26(6):831-849. doi: 10.1111/ene.13950
Harmer JP, Larson BS. Pain relief from baclofen analgesia in a neuropathic pain patient who failed opioid and pharmacotherapy: case report. J Pain Palliat Care Pharmacother. 2002;16(3):61-4. doi: 10.1080/j354v16n03_06
Xiao W, Naso L, Bennett GJ. Experimental studies of potential analgesics for the treatment of chemotherapy-evoked painful peripheral neuropathies. Pain Med. 2008 Jul-Aug;9(5):505-17. doi: 10.1111/j.1526-4637.2007.00301.x
Bauer MR, Hernández M, Kasten CR, Boehm SL 2nd. Systemic administration of racemic baclofen reduces both acquisition and maintenance of alcohol consumption in male and female mice. Alcohol. 2022 Sep;103:25-35. doi: 10.1016/j.alcohol.2022.06.003
Johnstone A, Grigoras I, Petitet P, Capitão LP, Stagg CJ. A single, clinically relevant dose of the GABAB agonist baclofen impairs visuomotor learning. J Physiol. 2021 Jan;599(1):307-322. doi: 10.1113/JP280378
Ertzgaard P, Campo C, Calabrese A. Efficacy and safety of oral baclofen in the management of spasticity: A rationale for intrathecal baclofen. J Rehabil Med. 2017 Mar 6;49(3):193-203. doi: 10.2340/16501977-2211
Addolorato G, Leggio L, Ferrulli A, Cardone S, Vonghia L, Mirijello A, Abenavoli L, D’Angelo C, Caputo F, Zambon A, Haber PS, Gasbarrini G. Effectiveness and safety of baclofen for maintenance of alcohol abstinence in alcohol-dependent patients with liver cirrhosis: randomised, double-blind controlled study. Lancet. 2007 Dec 8;370(9603):1915-22. doi: 10.1016/S0140-6736(07)61814-5
Guelaud C, Similowski T, Bizec JL, Cabane J, Whitelaw WA, Derenne JP. Baclofen therapy for chronic hiccup. Eur Respir J. 1995 Feb;8(2):235-7. doi: 10.1183/09031936.95.08020235
Agabio R, Sinclair JM, Addolorato G, Aubin HJ, Beraha EM, Caputo F, et al. Baclofen for the treatment of alcohol use disorder: the Cagliari Statement. Lancet Psychiatry. 2018;5(12):957–960. doi: 10.1016/S2215-0366(18)30303-1
Pierce M, Sutterland A, Beraha EM, Morley K, van den Brink W. Efficacy, tolerability, and safety of low-dose and high-dose baclofen in the treatment of alcohol dependence: a systematic review and meta-analysis. Eur Neuropsychopharmacol. 2018;28(7):795–806. doi: 10.1016/j.euroneuro.2018.03.017
Rose AK, Jones A. Baclofen: its effectiveness in reducing harmful drinking, craving, and negative mood. A meta-analysis. Addiction. 2018;113(8):1396–1406. doi: 10.1111/add.14191
May CR. Baclofen overdose. Ann Emerg Med. 1983 Mar;12(3):171-3. doi: 10.1016/s0196-0644(83)80562-9
Saulino M, Anderson DJ, Doble J, Farid R, Gul F, Konrad P, Boster AL. Best Practices for Intrathecal Baclofen Therapy: Troubleshooting. Neuromodulation. 2016 Aug;19(6):632-41. doi: 10.1111/ner.12467
Ross JC, Cook AM, Stewart GL, Fahy BG. Acute intrathecal baclofen withdrawal: a brief review of treatment options. Neurocrit Care. 2011 Feb;14(1):103-8. doi: 10.1007/s12028-010-9422-6
Lake W, Shah H. Intrathecal Baclofen Infusion for the Treatment of Movement Disorders. Neurosurg Clin N Am. 2019 Apr;30(2):203-209. doi: 10.1016/j.nec.2018.12.002

Baclofen