Baclofen (brand name: Lioresal) is a prescription muscle relaxant and antispasmodic agent. It is used to help manage reversible muscle spasticity and pain due to multiple sclerosis spinal cord injuries and, when injected directly into the spine, brain damage. In addition, healthcare providers may prescribe baclofen off-label for a broad spectrum of other medical conditions.
Scientists are uncertain how baclofen works. It is chemically very similar to gamma-aminobutyric acid (GABA), a neurotransmitter found in the central nervous system that slows down nerve activity. It may work by activating GABA as an agonist, but its mechanism of action primarily involves blocking neurotransmitters that excite nerve activity. By relaxing spinal nerves that control muscles, baclofen relieves muscle tightness and contractions.
Most people take baclofen by mouth as a tablet or oral solution three to four times a day with or without food. Continuous baclofen injections, prescribed sometimes under the brand names Gablofen and Lioresal (discontinued), are delivered directly into the spinal cord through an automated pump implanted in the right side of the abdomen.
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Baclofen is mostly taken as a tablet or oral suspension.
Tablets: 5 milligrams (mg), 10 mg, 20 mg
Oral solution: 5 mg/5 mL
Baclofen tablets are approved to manage spasticity due to multiple sclerosis or spinal cord injury, particularly flexor spasms (involuntary muscle contractions at the ankle, knee, and hip), clonus (rhythmic involuntary muscle spasms), and muscle rigidity. Baclofen is also commonly prescribed off-label to treat several other medical conditions, such as intractable hiccups, trigeminal neuralgia
, gastroesophageal reflux (GERD), and alcohol abuse
.
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Baclofen dosage chart |
|||
|---|---|---|---|
| Indication | Starting dosage | Standard dosage | Maximum dosage |
| Muscle spasticity | 5 mg taken orally 3 times daily | 20–80 mg daily taken orally in 3-4 divided doses | 80 mg taken orally per day |
Baclofen spinal (intrathecal) injections are intended to treat severe spasticity due to multiple sclerosis, spinal cord injury, or brain injury. Healthcare providers turn to baclofen spinal injections as an alternative to destructive spinal cord surgery when oral baclofen is not effective. Only a tiny fraction (less than 1%) of an oral dose reaches the central nervous system, so injecting doses directly into the spinal cord allows for high doses to reach the spinal cord without the toxicity of extremely high oral doses. Each daily dose of intrathecal baclofen would require more than 100 times its dose in oral baclofen to reach the same concentration in the spine, but it has fewer and less severe adverse effects than oral baclofen.
A surgically implanted pump supplies a continuous daily dose directly into the spinal fluid or brain cavity. Before the pump is implanted, three screening doses of progressively higher doses will be used to determine if baclofen injections are effective. If intrathecal baclofen is effective at any of the trial doses, a baclofen pump will be surgically implanted in the right side of the abdomen and a spinal catheter will be surgically installed between the pump and the spinal cord. In some cases, a surgeon will place the catheter in the brain cavity to deliver injections directly into the brain (intraventricular injections).
Once implanted, the pump will then deliver a continuous, 24-hour dose to the spinal cord or brain to control muscle tone and spasticity. Programmable pumps allow the dose to change throughout the day to meet specific needs. The pump will need to be refilled every one to six months by subcutaneous injections into the pump’s refill port. The pump’s daily doses will be adjusted by a healthcare professional.
Dosing is very complex and takes some trial and error. The daily dose can range from 12 to 2003 micrograms (mcg) per a 24-hour period, but most people get satisfactory results from daily doses of 300 to 800 micrograms daily.
The U.S. Food and Drug Administration (FDA) has approved baclofen tablets and intrathecal injections to manage spasticity due to multiple sclerosis or spinal cord injury in children 12 years of age and older. Healthcare providers, however, may prescribe baclofen to younger children to treat spasticity due to spinal cord injury or multiple sclerosis or as a short-term treatment in children and teens for spasticity due to cerebral palsy.
Baclofen pediatric dosage chart |
||||
|---|---|---|---|---|
| Indication | Age | Starting dosage | Standard dosage | Maximum dosage |
| Muscle spasticity | 12 years and older | 5 mg taken orally 3 times daily | 20–80 mg per day taken orally in 3-4 divided doses | 80 mg taken orally per day |
Baclofen may not be the right medication for everyone. People who are allergic to baclofen should not be given the medication. In addition, although baclofen treats spasticity due to spinal cord injury or multiple sclerosis, it does not help manage muscle spasms due to stroke or Parkinson’s disease.
Some people with pre-existing conditions may need to be cautious about the use of baclofen, including those with epilepsy and psychiatric disorders such as schizophrenia. In some people, spasticity has beneficial effects, allowing them to stand, walk, balance, and maintain posture. Healthcare providers will use baclofen carefully in those people, as well.
Because the kidneys clear baclofen from the body, people with renal (kidney) impairment may require lower doses to reduce the risk of side effects.
Cats are not given baclofen, but veterinarians use it to treat urinary retention in dogs. As a muscle relaxant, baclofen reduces the urethra’s resistance to urine flow. Dosing can vary, but it is usually 1-2 mg of baclofen per kilogram (2.2 pounds) of body weight. A veterinarian should always be consulted for exact dosing instructions.
Most people will take baclofen by mouth as tablets. For those who cannot swallow a tablet, baclofen is available in a liquid formulation under the brand name Ozobax or as an oral suspension that can be prepared by a pharmacist. Oral baclofen can be taken with or without food, but patients are encouraged to take baclofen with food or milk to minimize the incidence of gastrointestinal problems. Here are some tips on how to take baclofen:
Take this medicine as directed by a healthcare provider. The dose may need to be changed throughout the course of treatment.
Please read the medication guide and instructions that come with this medicine. If there is no medication guide, ask a pharmacist to provide a copy.
Do not stop taking baclofen suddenly. Abrupt withdrawal can cause severe adverse reactions. If the medicine does not seem to be working or the side effects of baclofen make it difficult to take, talk to a healthcare professional about discontinuing this medication.
TABLETS
Take baclofen tablets with a glass of water.
Store baclofen tablets at room temperature (59°–86°F) in a closed container out of sight and reach of children.
ORAL SOLUTION
Shake the medication well before measuring out a dose.
Use the calibrated syringe or other calibrated dosing device to measure out a dose. If a calibrated dosing device is not included with the medicine, a pharmacist can supply one on request. Do not use kitchen utensils to measure out a dose.
Store baclofen oral solution in a refrigerator (36°–46°F) in a child-proof, light-resistant, closed container that is out of the reach of children.
BACLOFEN PUMP
The baclofen pump will be refilled by a healthcare professional every few months.
Keep all refill appointments. If the pump runs out of medicine, the abrupt withdrawal of baclofen can cause serious side effects. If you can’t make an appointment, have the pump refilled early.
Learn the pump alarms and what they mean. At least one type of alarm will signal when baclofen is no longer flowing, and another will signal if the pump is malfunctioning. Both are urgent medical emergencies that require the immediate attention of a healthcare professional.
Because the drug is quickly absorbed by the body, the effects of baclofen should be noticeable in about 30 minutes and reach their peak about 2 hours after taking a dose. Injections into the spinal cord, however, will produce immediate results. However, for both oral administration and injections, it usually takes a few days to a couple of weeks
after starting baclofen treatment for patients to notice improvements in their symptoms.
With a half-life of 5.7 hours, it takes more than a day for a dose of baclofen to be cleared from the body. However, it may take large doses up to three days to be eliminated from the body.
Take a missed dose as soon as it’s remembered. If it is almost time for the next dose, do not take the missed dose. Instead, take the next regular dose on schedule. Do not take extra medicine to make up for a missed dose.
Do not stop taking baclofen without talking to a healthcare provider first. The abrupt discontinuation of oral baclofen can cause side effects, but the abrupt discontinuation of intrathecal baclofen can be life-threatening. Baclofen withdrawal is most commonly caused by intrathecal pumps running out of medicine. Healthcare providers will teach patients about refill schedules, pump alarms, and the symptoms of baclofen withdrawal to prevent severe withdrawal.
The withdrawal symptoms of oral baclofen include fever, muscle rigidity, muscle spasms, rapid heart rate, confusion, mood changes, psychiatric disorders, hallucinations, and seizures. Intrathecal baclofen withdrawal can cause fever, muscle rigidity, muscle spasm, muscle damage (rhabdomyolysis), organ failure, and death.
Whether baclofen is taken orally or as an automated spinal injection, a healthcare provider will discontinue baclofen by prescribing a steadily decreasing dose over a two-week period. There are good reasons to stop taking baclofen. Allergies, drug interactions, or serious side effects such as allergic reactions or respiratory depression may require baclofen to be discontinued immediately. Some people develop resistance to the drug and it stops providing relief of muscle spasms and pain. Other people may not be able to live with common side effects such as drowsiness, constipation, headache, low blood pressure (hypotension), or urinary frequency.
If baclofen needs to be stopped, patients with muscle spasticity due to spinal cord injury or MS can turn to alternative drugs, including benzodiazepines, dantrolene, or tizanidine.
Taking too much baclofen can be a medical emergency. While overdose is more likely when taking oral baclofen, people on a baclofen pump can overdose during the initial titration of the medication, if the pump is programmed incorrectly, or if the pump is malfunctioning. It is very important to learn and recognize the symptoms of an overdose when taking baclofen. These symptoms include vomiting, somnolence, muscle weakness (hypotonia), problems with visual focus, respiratory depression (shallow and slow breathing), seizures, and coma. If a baclofen overdose is suspected, seek emergency medical help right away.
Pregnant women should be cautious about the use of baclofen during pregnancy. In addition, healthcare providers are advised to reduce and eventually discontinue the drug in the third trimester. Baclofen treatment near the end of a pregnancy has been known to produce baclofen withdrawal symptoms in newborns.
While a small amount of baclofen is present in breast milk, there is no evidence that it harms a nursing infant. However, breastfeeding mothers are cautioned
to monitor their babies for signs of sedation.
Josephine Bawab, Pharm.D., graduated from Virginia Commonwealth University School of Pharmacy. She began working in community pharmacy in 2012 and has worked for multiple chain pharmacies since then. She is passionate about helping patients and precepting students. She currently works and resides in Virginia, where she is just a few minutes away from the beach.
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