What is Muscle Relaxants and What is the Main Side Effect of Muscle Relaxants ?

Muscle relaxers or muscle relaxants are medications used to treat acute muscle pain and discomfort caused by muscle spasms. Muscle spasms are involuntary contractions that cause excessive strain in muscles and are often associated with conditions such as lower back pain and neck pain.

Medications used as muscle relaxers can differ in their chemical structures and the way they work in the brain. In general, muscle relaxers act as central nervous system depressants and cause a sedative effect or prevent your nerves from sending pain signals to your brain. The onset of action is rapid and effects typically last from 4-6 hours.

Muscle Relaxants for Muscle Spasms

Muscle spasms are painful and may restrict mobility, which can limit your ability to perform even basic activities. Painful, tight muscles can also interfere with getting a good night’s sleep.

Muscle relaxants may help reduce pain, and improve movement and range of motion, but your doctor will likely recommend that you first try acetaminophen or a nonsteroidal anti-inflammatory drug (NSAID). In some cases, these over-the-counter medications will be enough to help alleviate your pain.

If your muscle pain persists, your doctor may prescribe a muscle relaxant in addition to your pain medication. Below are common muscle relaxants (the generic names are listed first, with a brand name example in parentheses):

  • Baclofen (Lioresal)
  • Carisoprodol (Soma)
  • Cyclobenzaprine (Amrix)
  • Metaxalone (Skelaxin)
  • Methocarbamol (Robaxin)

When You Might Need a Muscle Relaxer

Your doctor might first suggest you try an over-the-counter medicine like acetaminophen (Tylenol) or ibuprofen (Advil) to treat your pain. But if those don’t work, or you can’t take them because you have another issue like liver problems or ulcers, you may need to try a muscle relaxant.

Muscle relaxants are ideally prescribed for acute rather than chronic pain. They may be an option if pain is preventing you from getting enough sleep. Because muscle relaxants cause drowsiness, they can help you get rest when you take them at night.

Some of the common side effects of muscle relaxers include:

  • Drowsiness
  • Dizziness
  • Agitation
  • Irritability
  • Headache
  • Nervousness
  • Dry mouth
  • Decreased blood pressure

The most commonly prescribed muscle relaxers are carisoprodol (Soma) and cyclobenzaprine (Flexeril). According to data from IMS Health, there were 4.2 million prescriptions of Soma and 28.4 million prescriptions of Flexeril dispensed in the United States in 2017.

Muscle Relaxant List
Muscle Relaxant List

What Are Side Effects of Flexeril?

Common side effects of Flexeril include:

  • dry mouth or throat
  • headache
  • blurred vision
  • drowsiness
  • dizziness
  • fatigue
  • loss of appetite
  • stomach pain
  • nausea
  • diarrhea
  • constipation
  • gas, or
  • muscle weakness.

Dosage for Flexeril –  For most patients, the recommended dose of Flexeril is 5 mg three times a day.

You shouldn’t drink alcohol while taking muscle relaxants. These medications make it hard to think and function normally, even if you take a low dose, so combining them with alcohol can increase your risk of an accident.

You also shouldn’t drive or operate heavy machinery while taking muscle relaxants. Some muscle relaxers start working within 30 minutes of taking them, and the effects can last anywhere from 4 to 6 hours

Muscle Relaxant Abuse

Muscle relaxers have a potential for abuse and addiction. Prolonged use can lead to increased tolerance and physical dependence, especially with Soma.3 For this reason, muscle relaxers are intended as a short-term treatment not to be prescribed for more than 2-3 weeks.

Unfortunately, many individuals take muscle relaxers alone or in combination with other illicit drugs for nonmedical reasons, such as to produce or enhance feelings of euphoria and dissociation. According to the Drug Enforcement Administration, Soma is one of the most commonly diverted drugs in the United States.2 Evidence also indicates prevalent misuse of Flexeril. In 2010 there were over 12,000 emergency room visits associated with Flexeril, and in 2016 over 10,000 calls to the Poison Control Centers had involved Flexeril.1

Muscle relaxer abuse can lead to serious dangers such as an increased risk of overdose, which can result in:

  • stupor
  • hallucinations
  • seizures
  • shock
  • respiratory depression
  • cardiac arrest
  • coma
  • death

Alcohol and Muscle Relaxers

Like muscle relaxers, alcohol also depresses the central nervous system. When alcohol is consumed with muscle relaxers the side effects are exacerbated. This can be very dangerous, leading to symptoms like:

  • Blurred vision
  • Urine retention
  • Extreme dizziness
  • Extreme drowsiness
  • Low blood pressure
  • Fainting
  • Memory problems
  • Liver damage
  • Increased risk of overdose

It is recommended to not drive or operate heavy machinery when under the influence of muscle relaxers. It is especially important to avoid drinking, as combining muscle relaxers with alcohol greatly increases your risk of an accident.

Withdrawal and Treatment

Regular use of muscle relaxers causes the brain to become used to its effects. If you attempt to suddenly stop using muscle relaxers you may experience withdrawal symptoms. Depending on the specific drug and how long you have been using it, there are various treatment options available to help you overcome your addiction.

For many people, Flexeril withdrawal causes mild symptoms such as nausea, headache, drowsiness, malaise, and discomfort. Symptoms tend to peak about 2-4 days after you last took the Flexeril, although in some people withdrawal symptoms may last for up to 1-2 weeks. For many people Flexeril detox can be done at home. However, if Flexeril addiction is accompanied by alcohol or opioid abuse the withdrawal symptoms from these other substances can be severe. In these situations, it may be best to undergo professional medical detox.

Soma withdrawal is usually more severe and can include symptoms like hallucinations and seizures. For your safety and comfort, it is often best to find an inpatient treatment program that includes a detox program to manage withdrawal symptoms. After detox patients can transition into the actual treatment phase of the program. Some people may not require a supervised detox program and will be able to undergo treatment on an outpatient basis.

Most inpatient and outpatient rehab programs include cognitive behavioral therapy that will help you learn the coping skills needed for long-term recovery.

Which Muscle Relaxants Are Best for Neck and Back Pain?

Stiffness and soreness in your neck and back can be difficult to deal with, especially when sleeping. Maybe you have a new injury, or you’ve aggravated an old one. Either way, if you feel this kind of pain at night, you may not sleep well. And then you may have more pain when you wake up.

In some cases, muscle relaxants can help relieve this pain and get you through these tough days. They do exactly what their name says: relax muscles. Reducing muscle tightness may improve new (acute) neck and back pain, especially when used at night.

But you need a prescription for muscle relaxers. And the evidence is mixed regarding how well they workTreatment guidelines don’t even agree on whether they should be prescribed.

Over-the-counter (OTC) pain relievers work better for neck and back pain than muscle relaxants alone. Examples of these are acetaminophen (Tylenol) and nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen (Advil) and naproxen (Aleve). Plus, there are effective treatments that don’t involve any medication at all, like home exercises, physical therapy, and/or posture training. That said, some people may benefit from taking an NSAID and a muscle relaxer together, especially at night.

Muscle relaxers work in different ways. They act on the muscles, nerves, or central nervous system. There isn’t enough evidence to suggest one muscle relaxer is better than another. So let’s look at nine popular muscle relaxants, including how well they work and their side effects.

1. Methocarbamol

Methocarbamol (Robaxin) is a well-studied medication that treats back pain. Compared to other options, it’s inexpensive and less likely to make you sleepy (sedated).

Taken as needed, 1,500 mg every 6 to 8 hours is a cheap and well-tolerated option for people who have new neck and back pain. It’s less sedating than other options, like cyclobenzaprine and carisoprodol. However, it may be less effective. In one study, almost 20% of those taking it stopped because it wasn’t helping their pain go away.

2. Cyclobenzaprine

Cyclobenzaprine is a reasonable first choice because it’s a cheap generic. But it has more potential for side effects, like sedation. This limits how you can use it during the day. Cyclobenzaprine may also cause dry mouth, especially in older adults. If this is a concern, consider a better non-sedating option.

At the standard dose of 10 mg to 30 mg a day, cyclobenzaprine (formerly branded as Flexeril) will make you sleepy. If you use it during the day, you’ll want to break your 10 mg tab in half and take 5 mg to lessen the drowsiness. Interestingly, one study found that a lower dose (15 mg per day) worked just as well as a higher dose (30 mg per day). There may not be any benefit when you take it alongside an NSAID like naproxen.

3. Carisoprodol

Carisoprodol (Soma) is a Schedule 4 drug (similar to benzodiazepines Ativan, Valium, and Xanax). Because of this, it has the potential for misuse. For this reason, you should not use it if you have a history of substance use.

Many believe that carisoprodol should be phased out as a muscle relaxant in favor of much better options. If prescribed, you should only use it for short periods of 2 to 3 weeks. Scientists don’t know how effective it is when taken for longer periods. Carisoprodol may cause drowsiness and dizziness. People over age 65 should not use it.

4. Metaxalone

Taken as 800 mg tablets 3 to 4 times a day, metaxalone (Skelaxin) has the fewest reported side effects. It’s also the least likely of the muscle relaxants to make you sleepy. It may work better for chronic lower back pain that is flaring up, rather than for pain that is new.

Metaxalone is a generic alternative for the brand medication Skelaxin, but it still costs more than most others. Insurance companies often don’t cover it because there are cheaper alternatives. But it works as well as cyclobenzaprine and carisoprodol (more info on those above) with fewer side effects and less sedation. So, paying cash may be worth it.

5. Tizanidine

Tizanidine (Zanaflex) is often used for spasticity in people with multiple sclerosis or cerebral palsy. Spasticity is where the muscles contract continuously, which leads to tightness and stiffness. The FDA has not approved tizanidine to treat neck or back pain.

For multiple sclerosis or cerebral palsy, tizanidine tends to have fewer side effects than Baclofen. But either medication may not make much difference in new low back pain when compared with ibuprofen alone. Tizanidine is not a first choice for new neck or back muscle pain.

6. Baclofen

Similar to tizanidine, Baclofen (Gablofen, Lioresal) is primarily used for spasticity in people who have multiple sclerosis or spinal cord injuries. Up to 20% of people taking it have drowsiness.  It’s not a first choice: There are better options for neck and back muscle pain. The FDA has not approved baclofen to treat neck or back pain.

7. Oxazepam and diazepam

Benzodiazepine medications like oxazepam (Serax, Zaxopam) and diazepam (Valium) are anti-anxiety medications. They are sometimes prescribed as muscle relaxants. But these really aren’t recommended because they don’t work well, are sedating, and can be habit-forming.

Plus, the FDA has not approved benzodiazepines for neck or back pain. Avoid these medications for neck and back muscle pain. There are much better options.

8. Chlorzoxazone

Chlorzoxazone (Lorzone) is not well studied for new low back and neck pain in adults. It wasn’t found to be effective for pain after spine surgery. Chlorzoxazone has also been reported as a rare cause of acute liver toxicity. Don’t choose this medication until you’ve exhausted all other options.

9. Orphenadrine

For neck and back pain in adults, the first four medications on this list work better than orphenadrine (Norflex), so save this as another last resort in the event the others don’t work.

Do muscle relaxers make you sleepy?

Yes, they can make you sleepy. In fact, sedation is one of the most common side effects reported. Dizziness and drowsiness are also commonly reported. That’s why they usually have a warning on the label that instructs you to avoid certain things while taking them, such as driving, caring for children, and operating heavy machinery.

Muscle relaxers can also cause other side effects and interact with other medications. It’s important to let your healthcare provider know about your medical history and which medications and supplements you’re taking.

What are Skeletal Muscle Relaxants?

Muscle relaxers, or muscle relaxants, are medications used to treat muscle spasms or muscle spasticity.

skeletal Muscle Relaxants-classification
skeletal Muscle Relaxants-classification

Skeletal muscle relaxants are drugs that are used to relax and reduce tension in muscles. They are more simply referred to as muscle relaxants.

Some work in the brain or spinal cord to block or dampen down excessively stimulated nerve pathways. These are called centrally acting muscle relaxants and examples include baclofen, methocarbamol, and tizanidine.

skeletal Muscle Relaxants
skeletal Muscle Relaxants

Others act directly on muscle fibers and are classified as peripherally acting muscle relaxants. Examples include dantrolene and the different types of botulinum toxin. Although dantrolene acts directly on the muscle itself, it also appears to indirectly act on the central nervous system and can cause drowsiness.

Cannabis extract also has muscle relaxing properties and is thought to act both centrally and peripherally.

Muscle spasms or cramps are sudden, involuntary contractions of a muscle or group of muscles. They can be caused by too much muscle strain and lead to pain. They’re associated with conditions such as lower back pain, neck pain, and fibromyalgia.

Muscle spasticity, on the other hand, is a continuous muscle spasm that causes stiffness, rigidity, or tightness that can interfere with normal walking, talking, or movement. Muscle spasticity is caused by injury to parts of the brain or spinal cord involved with movement. Conditions that can cause muscle spasticity include multiple sclerosis (MS), cerebral palsy, and amyotrophic lateral sclerosis (ALS).

Prescription drugs can help relieve the pain and discomfort from muscle spasms or spasticity. In addition, certain over-the-counter medications may be used to treat aches and pains associated with muscle spasms.

What are skeletal muscle relaxants used for?

Skeletal muscle relaxants are mainly used to treat:

  • spasticity, which is another term for stiff and rigid muscles caused by conditions such as cerebral palsy, multiple sclerosis, or stroke
  • muscle spasms which are temporary muscular contractions that are often associated conditions such as tension headache, low back pain, or fibromyalgia
  • cervical dystonia – a painful condition where the neck muscles involuntarily contract, causing your head to uncontrollably tilt forward or backward.

Which Prescriptions are  skeletal muscle relaxants?

Skeletal muscle relaxants differ in the way they work (centrally or peripherally as discussed above), their side effects, and their effectiveness for certain conditions.

Note that several other medicines, notably diazepam, may also be used as a muscle relaxant and are not listed below.

Note that several other medicines, notably diazepam, may also be used as a muscle relaxant and are not listed below.

Generic name Brand name FDA approval (spasm-related)
abobotulinumtoxinA Dysport Cervical dystonia, Muscle spasms
baclofen Gablofen, Lioresal General spasticity
carisoprodol Soma, Vanadom Muscle spasms
chlorzoxazone Lorzone Muscle spasms
cyclobenzaprine Amrix, Flexeril, Fexmid Muscle spasms
dantrolene Dantrium General spasticity
onabotulinumtoxinA Botox Cervical dystonia, Muscle spasms
orphenadrine Norflex Muscle spasms
metaxalone Skelaxin Muscle spasms
methocarbamol Robaxin Muscle spasms
rimabotulinumtoxinB Mybloc Cervical dystonia
tizanidine Zanaflex General spasticity

Are skeletal muscle relaxants safe?

Evidence supporting the effectiveness of skeletal muscle relaxants for muscle spasm is sparse; most trials are old and not of good quality.

Skeletal muscle relaxants consist of a varied range of medicines and some may not be suitable for people with certain medical conditions such as an enlarged prostate, epilepsy, glaucoma, intestinal problems, liver or kidney disease, or myasthenia gravis. Many also interact with other medications.

Some, like dantrolene, can adversely affect the liver and blood samples should be taken before treatment to check for any pre-existing liver disease or to establish how well the liver is functioning before treatment, and what effect the drug subsequently has.

Muscle relaxants can affect overall muscle tone and may be dangerous if muscle tone is needed for safe balance or movement. Alcohol can enhance these effects. Many muscle relaxants need to be tapered off slowly, rather than abruptly stopped.

A List of Skeletal muscle relaxants

muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone.

muscle relaxant
muscle relaxant

It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term “muscle relaxant” is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics. Neuromuscular blockers act by interfering with transmission at the neuromuscular end plate and have no central nervous system (CNS) activity.

They are often used during surgical procedures and in intensive care and emergency medicine to cause temporary paralysis. Spasmolytics, also known as “centrally acting” muscle relaxants, are used to alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions. While both neuromuscular blockers and spasmolytics are often grouped together as muscle relaxants, the term is commonly used to refer to spasmolytics only.

How Skeletal Muscle Contracts

A single α-motor neuron can innervate up to 200 muscle fibers, forming a complex called motor unit (Figure 1).10 With movement, an action potential originates from the UMN in the motor cortex.9 This action potential depolarizes the motor neuron terminal, resulting in the opening of voltage-gated calcium (Ca2+) channels and the subsequent release of the neurotransmitter acetylcholine (Ach) into the synaptic cleft. In the synaptic cleft, Ach binds to nicotinic cholinergic receptors on the muscle fiber membrane, leading to an influx of sodium (Na+) and a discharge of potassium (K) across the muscle fiber’s membrane, which results in depolarization of the muscle fiber.11 This depolarization opens voltage-gated Ca2+ channels on the sarcoplasmic reticulum (via ryanodine and inositol triphosphate receptors), allowing for Ca2+ influx into the cytoplasm of striated muscle cells.12  The Ca2+ then binds to troponin C, which exposes myosin-binding sites on actin filaments. A cross-link forms between actin and myosin, leading to muscle contraction. The pumping of Ca2+ back into the sarcoplasmic reticulum, using adenosine triphosphate, leads to cessation of contraction.

 

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Orphenate
Generic name: orphenadrine
0 reviews Add rating
Ozobax (Pro)
Generic name: baclofen
0 reviews Add rating
Paraflex
Generic name: chlorzoxazone
0 reviews Add rating
Remular-S
Generic name: chlorzoxazone
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Generic name: dantrolene
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Further information

Muscle Spasms

A muscle spasm is a sudden involuntary contraction of a muscle group that involves jerking and twitching. Unlike spasticity, which is a disorder of the CNS, muscle spasms arise from a variety of peripheral musculoskeletal conditions, such as mechanical low back pain. Common skeletal muscle conditions that cause spasms include fibromyalgia, myofascial pain syndrome, and mechanical low back or neck pain.

Antispasm Agents

Most of the agents discussed here are FDA approved for adjunctive use to treat muscle spasms and pain associated with acute musculoskeletal conditions (Table 4). Health data from 2003 to 2004 revealed that cyclobenzaprine (Amrix, Fexmid, others), carisoprodol (Soma, others), and metaxalone (Metaxall, Skelaxin, others) accounted for more than 45% of medications prescribed for acute musculoskeletal pain.

Due to CNS depression, cyclobenzaprine, metaxalone, orphenadrine (Norflex, others), methocarbamol (Robaxin, others), carisoprodol, and chlorzoxazone (Lorzone, Parafon Forte DSC, others) are on the American Geriatrics Society’s Beers List of inappropriate drugs for elderly patients.

Despite this, approximately 300,000 annual prescriptions for skeletal muscle relaxants (15%) are issued to patients older than 65 years of age.

Skeletal muscle relaxants represent a diverse pharmacotherapeutic group of medications across several chemical classes that are structurally dissimilar. These agents are effective for spasticity, skeletal muscle spasms, or both.

Because of the breadth of pharmacologic mechanisms and variable pharmacokinetics, the drugs have a huge range of AEs and potential drug interactions.

Considering that these agents are most often used in the elderly and also as adjuvants for the treatment of chronic pain patients with multiple comorbidities who are likely receiving a polypharmaceutical regimen (including opioids), skeletal muscle drug selection for each patient requires careful attention to these factors.

Warnings for prescription muscle relaxants

Muscle relaxants such as carisoprodol and diazepam can be habit forming. Be sure to take your medication exactly as prescribed by your doctor.

Muscle relaxants can also cause withdrawal symptoms, such as seizures or hallucinations (sensing things that aren’t real). Do not suddenly stop taking your medication, especially if you’ve been taking it for a long time.

Also, muscle relaxants depress your central nervous system (CNS), making it hard to pay attention or stay awake. While taking a muscle relaxant, avoid activities that require mental alertness or coordination, such as driving or using heavy machinery.

You should not take muscle relaxants with:

  • alcohol
  • CNS depressant drugs, such as opioids or psychotropics
  • sleeping medications
  • herbal supplements such as St. John’s wort

Talk to your doctor about how you can safely use muscle relaxants if you:

  • are older than 65 years
  • have a mental health problem or brain disorder
  • have liver problems

Off-label medications for spasticity

Doctors can use certain medications to treat spasticity even when the drugs are not approved for that purpose by the U.S. Food and Drug Association (FDA). This is called off-label drug use. The following drugs are not actually muscle relaxants, but they can still help relieve symptoms of spasticity.

Benzodiazepines

Benzodiazepines are sedatives that can help relax muscles. They work by increasing the effects of certain neurotransmitters, which are chemicals that relay messages between your brain cells.

Examples of benzodiazepines include:

  • clonazepam (Klonopin)
  • lorazepam (Ativan)
  • alprazolam (Xanax)

Side effects of benzodiazepines can include drowsiness and problems with balance and memory. These drugs can also be habit forming.

Clonidine

Clonidine (Kapvay) is thought to work by preventing your nerves from sending pain signals to your brain or by causing a sedative effect.

Clonidine should not be used with other muscle relaxants. Taking it with similar drugs increases your risk of side effects. For instance, taking clonidine with tizanidine can cause very low blood pressure.

Clonidine is available in brand-name and generic versions.

Gabapentin

Gabapentin (Neurontin) is an anticonvulsant drug typically used to relieve seizures. It’s not fully known how gabapentin works to relieve muscle spasticity. Gabapentin is available in brand-name and generic versions.

Over-the-counter options for muscle spasms

OTC treatment is recommended as first-line therapy for muscle spasms caused by conditions such as acute lower back pain or tension headache. This means you should try OTC treatments before prescription medications.

OTC treatment options include nonsteroidal anti-inflammatory drugs (NSAIDs), acetaminophen, or a combination of both. Your doctor or pharmacist can help you choose an OTC treatment.

Nonsteroidal anti-inflammatory drugs (NSAIDs)

NSAIDs work by blocking your body from making certain substances that cause inflammation and pain. NSAIDs are available in generic and brand-name versions. They’re typically sold over the counter. Stronger versions are available by prescription.

NSAIDs come as oral tablets, capsules, or suspensions. They also come as chewable tablets for children. Side effects of these drugs can include upset stomach and dizziness.

Examples of NSAIDs include:

  • ibuprofen (Advil, Motrin)
  • naproxen (Aleve)

Acetaminophen

Acetaminophen (Tylenol) is thought to work by blocking your body from making certain substances that cause pain. Acetaminophen is available in generic and brand-name versions. It comes as immediate-release and extended release oral tablets and capsules, orally disintegrating tablets, chewable tablets, and oral solutions.

The more common side effects of acetaminophen can include nausea and upset stomach.