About all

Is orphenadrine a narcotic. Orphenadrine: Uses, Side Effects, and Important Precautions

What is orphenadrine used for. How does orphenadrine work as a muscle relaxer. What are the potential side effects of orphenadrine. Who should not take orphenadrine. How to take orphenadrine safely. What precautions should be taken when using orphenadrine. What drug interactions may occur with orphenadrine.

Содержание

Understanding Orphenadrine: A Comprehensive Overview

Orphenadrine is a medication primarily used as a muscle relaxer. It belongs to the drug class of skeletal muscle relaxants and is often prescribed in conjunction with rest and physical therapy to treat various skeletal muscle conditions, including pain and injury. While effective in its intended use, it’s crucial to understand the proper usage, potential side effects, and precautions associated with this medication.

What is Orphenadrine?

Orphenadrine is a prescription medication that works by relaxing muscles and alleviating pain. It’s available under various brand names, including Norflex, Banflex, Orphenate, Flexoject, and Flexon, among others. The drug comes in different forms, with the most common being oral extended-release tablets and injectable solutions.

Medical Uses of Orphenadrine

The primary use of orphenadrine is to treat skeletal muscle conditions. But what specific conditions does it target?

  • Acute painful musculoskeletal conditions
  • Muscle spasms
  • Injury-related muscle pain
  • Chronic muscle pain (in some cases)

It’s important to note that orphenadrine is typically used as part of a comprehensive treatment plan. This plan often includes rest, physical therapy, and other pain management techniques. The medication helps to relax muscles and reduce pain, allowing patients to engage more effectively in their rehabilitation process.

Proper Administration and Dosage

How should orphenadrine be taken? The dosage and administration of orphenadrine can vary depending on the specific formulation and the patient’s condition. However, there are some general guidelines to follow:

  • Extended-Release Tablets: Typically taken twice daily, once in the morning and once in the evening.
  • Injectable Form: Usually administered every 12 hours as needed, either intravenously or intramuscularly.
  • Dosage: For adults, the usual dose is 100 mg twice daily for tablets, or 60 mg every 12 hours for injections.

It’s crucial to follow your doctor’s instructions precisely. Never alter your dosage without consulting your healthcare provider first. Also, extended-release tablets should be swallowed whole – do not crush, chew, or break them.

Potential Side Effects and Risks

Like all medications, orphenadrine can cause side effects. What are the most common and serious side effects of orphenadrine?

Common Side Effects

  • Dry mouth
  • Blurred vision
  • Dizziness
  • Headache
  • Nausea
  • Constipation

Serious Side Effects

While less common, some serious side effects may occur and require immediate medical attention:

  • Severe dizziness or feeling like you might pass out
  • Difficulty urinating or inability to urinate
  • Confusion, anxiety, or agitation
  • Hallucinations
  • Irregular heartbeat or palpitations

If you experience any of these serious side effects, stop taking the medication and seek medical help immediately.

Contraindications and Precautions

Not everyone can safely take orphenadrine. Who should avoid this medication?

Orphenadrine is contraindicated for individuals with:

  • Urination problems
  • Enlarged prostate
  • Glaucoma
  • Stomach ulcers
  • Blockages in the digestive tract
  • Difficulty swallowing
  • Myasthenia gravis

Additionally, caution is advised for patients with heart disease, heart rhythm disorders, or coronary artery disease. Pregnant or breastfeeding women should consult their doctor before using orphenadrine, as its effects on unborn babies and nursing infants are not fully known.

Drug Interactions and Precautions

Orphenadrine can interact with various other medications, potentially leading to harmful effects. What are some important drug interactions to be aware of?

  • Narcotic (opioid) medications
  • Sleeping pills
  • Prescription cough medicines
  • Other muscle relaxers
  • Medications for anxiety, depression, or seizures

These interactions can cause dangerous side effects or even be life-threatening. Always inform your healthcare provider about all medications you’re taking, including over-the-counter drugs, vitamins, and herbal supplements.

Potential for Abuse and Addiction

Is orphenadrine addictive? While not classified as a narcotic, orphenadrine does have the potential for abuse and addiction. It’s considered a controlled substance in many jurisdictions due to this risk. Patients should be aware of this potential and use the medication only as prescribed.

Signs of potential abuse or addiction may include:

  • Taking larger doses than prescribed
  • Using the medication more frequently than directed
  • Seeking prescriptions from multiple doctors
  • Experiencing strong cravings for the medication

If you or someone you know is struggling with orphenadrine misuse, it’s crucial to seek help from a healthcare professional.

Safety Measures and Storage

Proper storage and handling of orphenadrine are essential for both safety and effectiveness. How should orphenadrine be stored?

  • Keep at room temperature, away from moisture, heat, and light
  • Store in a tightly closed container
  • Keep out of reach of children and pets
  • Do not share your medication with others
  • Keep track of the amount of medicine used from each new bottle

Proper disposal of unused or expired medication is also important. Many communities offer drug take-back programs for safe disposal. If such programs are not available, the FDA provides guidelines for safe disposal at home.

Orphenadrine in Comparison to Other Muscle Relaxants

How does orphenadrine compare to other muscle relaxants on the market? While orphenadrine is effective for many patients, it’s not the only option available. Other common muscle relaxants include:

  • Cyclobenzaprine (Flexeril)
  • Methocarbamol (Robaxin)
  • Carisoprodol (Soma)
  • Tizanidine (Zanaflex)

Each of these medications has its own profile of benefits and potential side effects. The choice of muscle relaxant often depends on the specific condition being treated, the patient’s medical history, and potential drug interactions. Your healthcare provider will consider these factors when determining the most appropriate treatment for your situation.

Comparing Effectiveness

Studies have shown that orphenadrine is generally as effective as other muscle relaxants for treating acute low back pain and muscle spasms. However, its effectiveness can vary depending on the individual and the specific condition being treated.

Side Effect Profiles

One advantage of orphenadrine is that it tends to cause less sedation compared to some other muscle relaxants. This can be beneficial for patients who need to remain alert during the day. However, it may have a higher incidence of certain side effects, such as dry mouth and urinary retention, compared to some other options.

Long-term Use and Considerations

Is orphenadrine suitable for long-term use? While orphenadrine can be effective for short-term relief of muscle pain and spasms, its long-term use is generally not recommended. Prolonged use may lead to:

  • Increased risk of side effects
  • Potential for dependence or addiction
  • Masking of underlying conditions that require different treatment

If you find yourself needing to use orphenadrine for an extended period, it’s important to discuss this with your healthcare provider. They may recommend alternative treatments or a different approach to managing your condition.

Alternative Treatments

For long-term management of muscle pain or spasms, your doctor might suggest alternatives such as:

  • Physical therapy
  • Exercise programs
  • Non-pharmacological pain management techniques (e.g., heat therapy, massage)
  • Other types of medications (e.g., non-steroidal anti-inflammatory drugs)

These alternatives may provide more sustainable relief without the risks associated with long-term use of muscle relaxants.

Special Populations and Orphenadrine Use

How does orphenadrine use differ for special populations? Certain groups of people may require special consideration when it comes to orphenadrine use:

Elderly Patients

Older adults may be more sensitive to the effects of orphenadrine, particularly its anticholinergic effects. These can include confusion, blurred vision, and increased risk of falls. Dosage adjustments may be necessary, and close monitoring is often required.

Patients with Liver or Kidney Disease

Orphenadrine is metabolized in the liver and excreted by the kidneys. Patients with impaired liver or kidney function may require dosage adjustments or may need to avoid the medication altogether. Regular monitoring of liver and kidney function may be necessary for these patients.

Pregnant and Breastfeeding Women

As mentioned earlier, the effects of orphenadrine on unborn babies and nursing infants are not fully known. Pregnant or breastfeeding women should only use this medication if the potential benefits clearly outweigh the risks, as determined by their healthcare provider.

Monitoring and Follow-up

What kind of monitoring is necessary when taking orphenadrine? Regular follow-up with your healthcare provider is important when using orphenadrine. This may include:

  • Assessing the effectiveness of the medication in managing your symptoms
  • Monitoring for side effects
  • Evaluating the need for continued use
  • Adjusting the treatment plan as necessary

Be sure to keep all scheduled appointments and report any new or worsening symptoms promptly. Your healthcare provider may also recommend periodic blood tests to check liver and kidney function, especially if you’re using the medication for an extended period.

Patient Education and Self-Management

How can patients effectively manage their treatment with orphenadrine? Education and self-management are crucial components of successful treatment with orphenadrine. Here are some key points for patients to remember:

  • Take the medication exactly as prescribed
  • Do not suddenly stop taking orphenadrine without consulting your doctor
  • Be aware of potential side effects and know when to seek medical attention
  • Avoid alcohol and other central nervous system depressants while taking orphenadrine
  • Use caution when driving or operating machinery, as the medication can cause drowsiness
  • Engage in recommended physical therapy or exercise programs alongside medication use
  • Keep track of your symptoms and the medication’s effectiveness

By being an active participant in your treatment plan, you can help ensure the safe and effective use of orphenadrine.

Future Developments and Research

What does the future hold for orphenadrine and muscle relaxant treatments? While orphenadrine has been in use for many years, research in the field of muscle relaxants continues. Some areas of ongoing research include:

  • Development of new muscle relaxants with fewer side effects
  • Exploration of combination therapies for more effective pain management
  • Investigation of long-term outcomes and safety profiles of various muscle relaxants
  • Research into non-pharmacological alternatives for muscle pain and spasm management

As our understanding of pain mechanisms and muscle physiology evolves, we may see new treatments emerge that offer improved efficacy and safety profiles. However, for now, orphenadrine remains an important tool in the management of acute muscle pain and spasms when used appropriately under medical supervision.

Orphenadrine Uses, Side Effects & Warnings

Generic name: orphenadrine [ or-FEN-a-drin ]
Brand names: Norflex, Banflex, Orphenate, Flexoject, Flexon,
… show all 10 brands
Mio-Rel, Myolin, Orfro, Norflex Injectable, Antiflex

Dosage form: oral tablet, extended release (100 mg)
Drug class: Skeletal muscle relaxants

Medically reviewed by Drugs.com on Feb 28, 2023. Written by Cerner Multum.

What is orphenadrine?

Orphenadrine is a muscle relaxer.

Orphenadrine is used together with rest and physical therapy to treat skeletal muscle conditions such as pain or injury.

Orphenadrine may also be used for purposes not listed in this medication guide.

Warnings

You should not take orphenadrine if you have urination problems, an enlarged prostate, glaucoma, a stomach ulcer or blockage in your digestive tract, trouble swallowing, or myasthenia gravis.

Before taking this medicine

You should not use orphenadrine if you are allergic to it, or if you have:

  • urination problems;

  • an enlarged prostate;

  • glaucoma;

  • a stomach ulcer;

  • a blockage in your stomach or intestines;

  • trouble swallowing; or

  • myasthenia gravis.

To make sure orphenadrine is safe for you, tell your doctor if you have:

  • heart disease;

  • a heart rhythm disorder;

  • coronary artery disease; or

  • if you also use a narcotic (opioid) medication.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It is not known whether orphenadrine passes into breast milk or if it could affect the nursing baby. Tell your doctor if you are breast-feeding.

Orphenadrine is not approved for use by anyone younger than 18 years old.

How should I take orphenadrine?

Follow all directions on your prescription label. Do not take orphenadrine in larger or smaller amounts or for longer than recommended.

Orphenadrine may be habit-forming. Never share orphenadrine with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it. Selling or giving away this medicine is against the law.

Orphenadrine is usually taken 2 times per day, once in the morning and once in the evening. Follow your doctor’s dosing instructions.

Do not crush, chew, or break an extended-release tablet. Swallow it whole.

Orphenadrine is only part of a complete program of treatment that may also include rest, physical therapy, or other pain relief measures.

Store orphenadrine at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

Keep track of the amount of medicine used from each new bottle. Orphenadrine is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking orphenadrine?

orphenadrine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Do not drink alcohol. Dangerous side effects or death can occur.

Orphenadrine side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Orphenadrine may cause serious side effects. Stop using orphenadrine and call your doctor at once if you have:

  • a light-headed feeling, like you might pass out;

  • painful or difficult urination;

  • little or no urination;

  • confusion, anxiety, agitation, tremors, hallucinations; or

  • pounding heartbeats or fluttering in your chest.

Common side effects of orphenadrine may include:

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

Orphenadrine dosing information

Usual Adult Dose for Muscle Spasm:

Extended-Release Tablets: 100 mg orally twice a day

Parenteral Injection: 60 mg IV or IM every 12 hours as needed

Use: As an adjunct to rest, physical therapy and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions.

What other drugs will affect orphenadrine?

Taking orphenadrine with other drugs that make you sleepy or slow your breathing can cause dangerous side effects or death. Ask your doctor before taking a sleeping pill, narcotic pain medicine, prescription cough medicine, a muscle relaxer, or medicine for anxiety, depression, or seizures.

Other drugs may interact with orphenadrine, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

More about orphenadrine

  • Check interactions
  • Compare alternatives
  • Pricing & coupons
  • Reviews (80)
  • Drug images
  • Latest FDA alerts (1)
  • Side effects
  • Dosage information
  • During pregnancy
  • Drug class: skeletal muscle relaxants
  • Breastfeeding
  • En español

Patient resources

  • Advanced Reading
  • Orphenadrine (Oral) (Advanced Reading)
  • Orphenadrine Extended-Release Tablets
  • Orphenadrine Injection
Other brands

Norflex, Antiflex, Mio-Rel, Orfro, Orphenate

Professional resources

  • Prescribing Information

Related treatment guides

  • Migraine
  • Muscle Spasm

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

Copyright 1996-2023 Cerner Multum, Inc. Version: 5.01.

Orphenadrine: MedlinePlus Drug Information


pronounced as (or fen’ a dreen)

To use the sharing features on this page, please enable JavaScript.

  • Why is this medication prescribed?
  • How should this medicine be used?
  • Other uses for this medicine
  • What special precautions should I follow?
  • What special dietary instructions should I follow?
  • What should I do if I forget a dose?
  • What side effects can this medication cause?
  • What should I know about storage and disposal of this medication?
  • In case of emergency/overdose
  • What other information should I know?
  • Brand names
  • Brand names of combination products

Orphenadrine is used with rest, physical therapy, and other measures to relieve pain and discomfort caused by strains, sprains, and other muscle injuries. Orphenadrine is in a class of medications called skeletal muscle relaxants. It works by changing the way the body senses muscle pain.

Orphenadrine comes as a tablet and an extended-release (long-acting) tablet to take by mouth. It is usually taken twice a day. Try to take orphenadrine at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take orphenadrine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the extended-release tablets whole. do not split, chew, or crush them.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Before taking orphenadrine,

  • tell your doctor and pharmacist if you are allergic to orphenadrine,any other medications, or any of the ingredients in orphenadrine tablets or extended-release tablets.
  • tell your doctor and pharmacist what 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: amantadine (Symadine, Symmetrel), fluphenazine (Prolixin), haloperidol (Haldol), medications for colds or allergies, medications for depression, perphenazine (Trilafon), prochlorperazine (Compazine), promethazine (Phenergan), sedatives, sleeping pills,and trifluoperazine (Stelazine). 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 glaucoma; myasthenia gravis; ulcers; a urinary tract or intestinal blockage; an enlarged prostate; an irregular heartbeat; or liver, kidney, or heart disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking orphenadrine, call your doctor.
  • talk to your doctor about the risks and benefits of taking orphendrine if you are 65 years of age or older. Older adults should not usually take orphenadrine because it is not as safe as other medications that can be used to treat the same condition.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking orphenadrine.
  • you should know that this medication may make you drowsy. Do not drive a car or operate machinery until you know how orphenadine will affect you.
  • ask your doctor about the safe use of alcohol while you are taking this medication. Alcohol can make the side effects of orphenadrine worse.

Unless your doctor tells you otherwise, continue your normal diet.

Take the missed dose as soon as you remember it. However, if it is almost time for the 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.

Orphenadrine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • dry mouth
  • drowsiness
  • dizziness or lightheadedness
  • upset stomach
  • vomiting
  • constipation
  • difficulty urinating
  • blurred vision
  • headache

Some side effects can be serious.

If you experience any of the following symptoms, call your doctor immediately:

  • fast or irregular heartbeat
  • fainting
  • confusion
  • hallucinations
  • skin rash

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Orphenadrine may cause other side effects. Call your doctor if you experience any unusual problems during your treatment with orphenadrine.

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

In case of 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 emergency services at 911.

  • Disipal®
  • Norflex®
  • Invagesic® (containing Aspirin, Caffeine, Orphenadrine)
  • Norgesic® (containing Aspirin, Caffeine, Orphenadrine)
  • Orphengesic® (containing Aspirin, Caffeine, Orphenadrine)

This branded product is no longer on the market. Generic alternatives may be available.

Last Revised – 05/15/2017

Browse Drugs and Medicines

Baralgin drug – High pills

Contents:

For medical purposes, baralgin is used quite often as a pain reliever, and for drug addicts, baralgin pills for high. This is far from a harmless drug, and its overdose can lead to serious consequences, even death. Despite such dangers, some people take the drug in high doses, as a drug. Gradually, psychological dependence can develop, and frequent use of the drug quickly destroys the body. If you or your loved ones are addicted to baralgin, treatment should begin immediately. The narcological clinic “Hummingbird” can help with this.

What is baralgin and how does it work

This is an effective drug for the suppression of severe pain. The main active ingredient is metamizole sodium, but, unlike analgin, the action is much stronger and more pronounced (mainly due to special components that are also included in the medicine).

Baralgin is prescribed mainly for spinal lesions and pain associated with them. The pain goes away, muscle spasms are relieved, motor activity increases, and tissue repair is accelerated.

All the described effects are effective when the drug is taken correctly, in the dosage prescribed by the doctor. In the case of taking high doses, various side effects may occur – headaches, nausea and vomiting, and other disorders of the gastrointestinal tract. In addition, the load on the liver increases significantly, so it is undesirable to take baralgin for a long time even at recommended doses. A severe overdose requires immediate hospitalization, gastric lavage, and detoxification measures.

Action similar to narcotic

Metamizole sodium itself and other components of the drug are not able to have a real narcotic effect, however, with a complex effect and high dosages, such a situation is possible. There is a strong muscle relaxation (anticonvulsant muscle relaxant effect of the drug), sensations change (even a hard surface is perceived as a soft bed), problems, anxieties and fear disappear. Brief dream-like visions are possible.

With a large overdose, the “pleasant” effects are less pronounced, as they overlap with side effects, one of the most severe forms of which is toxic nephritis. Perhaps the development of anemia, fainting (therefore, for patients with anemia, the drug is categorically contraindicated).

Causes of addiction to baralgin

Now narcologists identify three main reasons why people become addicted to baralgin:

  • Frequent use of high doses of the drug for “recreational” purposes, to obtain the effects described above in the form of relaxation and some change in consciousness. Given the availability of the drug, this quickly becomes a problem, you want to repeat the pleasant sensations again and again. So in a short time there is a psychological dependence.
  • Admission for pain. Statistics show that for many citizens baralgin is the main analgesic in the home medicine cabinet, and they take this medicine for any reason, at the slightest pain. This approach can also provoke the development of addiction. Even if the cause of the pain has already been eliminated, the addict continues to take baralgin, often in doses exceeding those recommended.
  • The use of baralgin to overcome withdrawal. People addicted to hard drugs (especially opiates) use baralgin to reduce the pain effects caused by withdrawal symptoms. The action of the drug depresses pain, relaxes, soothes up to serenity – that is, the effect is similar to a narcotic one. This provokes the use of high doses, which can be fatal for an organism weakened by hard drugs.

If someone close to you takes baralgin regularly, without special reasons, without observing the dosage, this is a cause for concern and referral to specialists. The sooner narcologists start working with the addict, the less harm to the body will be, and the faster recovery will come.

Services of the narcological clinic “Kolibri”

Fortunately, baralgin does not act directly as a drug, and the appearance of physiological dependence is practically excluded. Only minor effects of such a plan are possible, but they quickly disappear without creating much discomfort. The situation is different with the psychological addiction to the drug. It is inexpensive, highly accessible, and therefore it is advisable for the patient to be placed in a hospital for a while. In this case, he will not get access to a new dose, which means that the treatment will achieve its goals.

Narcological clinic “Kolibri” offers the following program of treatment and rehabilitation:

  • Detoxification of the body, aimed at the rapid removal of the active substances of the drug. Efficiency is especially important in case of overdose. This stage of treatment is carried out in a special regime, when access to the patient is limited. These restrictions eliminate the risk that the patient will receive a new dose of the drug.
  • Psychological courses. In the case of baralgin, this is the main therapeutic stage, which allows you to understand the causes of addiction. Knowing these reasons, it will be much easier to choose the correct and most effective treatment methods. The main task of specialists is to explain to the patient the essence of his problem and show that a normal life is possible even if the drug is abandoned.
  • Rehabilitation activities. At this stage, the task of the specialists of the Hummingbird clinic is to help the patient return to everyday life in society, without the painful craving for the use of high doses of dangerous drugs. Special psychotherapeutic techniques will help to correct behavior so that after leaving the clinic, other interests that are not related to taking dangerous drugs are formed.

Do you or your loved ones need drug treatment? Do not put off solving the problem for later, do not try to cope with it on your own. In most cases, this only causes torment to the addict, but does not eliminate the craving for the drug. Turning to the narcological clinic “Hummingbird”, you can be sure that experienced specialists of various profiles will do everything possible to return the patient to a normal life, to a life without drug addiction.

Didn’t find what you were looking for?

If you need urgent help, call now and our consultants will help you

(050) 224-03-03
(096) 224-03-03

You may be interested

Fixed combination of orphenadrine and diclofenac

Centrally acting muscle relaxants are a heterogeneous group of drugs with various mechanisms of direct influence on various parts of the central nervous system involved in the regulation of muscle tone. They are able to reduce pathologically increased skeletal muscle tone and do not have a direct effect on the neuromuscular synapse (do not cause myasthenia gravis and respiratory arrest), cardiomyocytes (do not reduce cardiac output), vascular smooth muscle elements (do not cause direct myogenic vasodilation) and internal organs (do not have antispasmodic properties). They are widely used in the treatment of muscle spasticity developed as a result of damage to the central motor neuron in cerebral or spinal strokes [1], multiple sclerosis [2], myelopathy [3], cerebral palsy and some other diseases of the central nervous system.

Painful muscle spasm is much more common due to primary muscle damage or its secondary reflex tension. Painful muscle tension of varying severity is observed in the so-called nonspecific musculoskeletal pain in the back, neck, radiculopathy, sports injuries, orthopedic diseases, etc. [4]. Pain and muscle spasm significantly limit the professional and daily activities of a person, reduce the quality of his life, and therefore should be stopped in full and as soon as possible [5–8]. The mechanism of muscle relaxation in the application of this class of drugs is associated mainly with the inhibition of spinal intercalary neurons or suprasegmental influences of neurons of the reticular formation.

Of the centrally acting muscle relaxants, baclofen, tizanidine, tolperisone and orphenadrine are registered in Russia as part of a fixed combination with diclofenac (Table 1).

Tizanidine is a centrally acting α2 receptor agonist [9, 10]; by stimulating presynaptic α2-adrenergic receptors, it inhibits the release of excitatory amino acids that stimulate NMDA receptors. As a result, at the level of intermediate neurons of the spinal cord, polysynaptic transmission of excitation is suppressed. In addition to muscle relaxant properties, tizanidine also has a central moderate analgesic effect and has a gastroprotective effect (reduces the formation of hydrochloric acid), which can reduce the risk of gastrointestinal complications of NSAIDs when used together.

The mechanism of baclofen muscle relaxation is associated with the activation of GABA receptors in the CNS, which leads to a decrease in the release of excitatory amino acids (glutamate and aspartate) and inhibition of mono- and polysynaptic transmission of nerve impulses, as well as a decrease in muscle spindle tension [11].

The exact mechanism of action of tolperisone is not fully understood. It is known that as a result of the membrane-stabilizing action, the conduction of excitation in the primary afferent fibers slows down, mono- and polysynaptic reflexes of the spinal cord are blocked. A secondary mechanism of action associated with blocking the entry of calcium ions into the synapses is also likely. Tolperison reduces reflex readiness in the reticulospinal tracts of the brain stem, increases peripheral circulation. This is not associated with the effect of the drug on the central nervous system and may be due to its weak antispasmodic and antiadrenergic effects.

Tab. 1. Clinical pharmacology of muscle relaxants Table 1. Clinical pharmacology of muscle relaxants

Preparation

CNS spasticity

Local painful muscle spasm

Additional features

Tolperisone

+

+

Vasodilator

Baclofen

+

No indication

Sedation for associated pain, anxiety and insomnia

Tizanidin

+

+

Central analgesia Gastroprotection (NSAIDs)

Orphenadrine

No indication

+

Central analgesic action (NMDA receptor antagonist – antihyperalgesia) Anticholinergic effect

Mild antihistamine effect

(promotes analgesic effect)

Orphenadrine is an o-methyl derivative of diphenhydramine, has anticholinergic, antihistamine properties and is used to eliminate pathologically increased skeletal muscle tone [12–16]. In spinal cord injury, orphenadrine citrate has been shown to have an antispastic effect, which has also been found to be a noncompetitive NMDA glutamate receptor antagonist [15–16]. Orphenadrine has proven to be an effective treatment for pain associated with muscle spasms [16]. A number of studies have shown that the drug has an independent analgesic effect, which is realized not only by reducing muscle spasm, but also indirectly, by influencing the dopaminergic and histaminergic antinociceptive neurotransmitter systems of the brain [17, 18]. However, the exact mechanism of the antinociceptive action of orphenadrine remains to be determined [19]., 20]. In Russia, orphenadrine is registered as a solution for infusion combined with diclofenac under the commercial name Neodolpasse (diclofenac 75 mg and orphenadrine 30 mg). With this combination, the analgesic and anti-inflammatory effect of NSAIDs is potentiated by the antinociceptive and muscle relaxant effects of orphenadrine [21]. This makes it possible to achieve more pronounced and rapid analgesia and reduce the treatment time for patients with various pain syndromes accompanied by painful spasm.

In Russia, muscle relaxants are presented in tablet dosage forms of short or prolonged action for oral administration (tolperisone, tizanidine, baclofen). Tolperisone and orphenadrine in combination with diclofenac have injection forms for intramuscular and intravenous administration (Table 2).

The intravenous route of administration seems to be the most appropriate if it is necessary to achieve rapid and highly predictable analgesia in patients with severe pain and muscle spasm. Intravenous administration makes it easy to adjust the dosage of the drug, as well as immediately stop its administration if adverse effects occur. This route of administration also becomes a priority in cases of restrictions on intramuscular administration of drugs (for example, stay in the intensive care unit) or when it is impossible to swallow.

For baclofen, a special injection system for intrathecal administration has been developed, which allows the use of doses at least 100 times smaller than when taken orally. Indications for intrathecal use of baclofen are severe cases of spasticity resistant to other methods of administration of muscle relaxants, for example, in severe spasticity in multiple sclerosis, myelopathy.

More than a hundred studies have been devoted to the study of the effectiveness and safety of muscle relaxants. All drugs studied were more effective than placebo in treating painful muscle spasm. RCTs have shown a significant reduction in back pain, muscle tension, and improvement in functional status after using these agents for 1–2 weeks, with comparable efficacy. (R. Chou, K. Peterson, 2004). It is not possible to conduct a direct comparative assessment of the effectiveness of muscle relaxants due to insurmountable differences in study design, end points of evaluation, and the methods used for this. These circumstances do not allow to make an unambiguous conclusion about the clinical advantage of centrally acting muscle relaxants over each other. However, the feasibility of their use in painful muscle spasm is reflected in the European guidelines (EFNS, 2014). Orphenadrine is also included in the European guidelines for the treatment of perioperative pain (2017). The results of a double-blind, randomized, placebo-controlled, multicenter study show a significant 30% reduction (p=0.0004) in the need for opioid analgesics (in terms of morphine equivalent) during Neodolpasse infusion therapy in patients (120 people) operated on for diseases of the musculoskeletal system. apparatus [22]. In patients with postoperative pain after surgical treatment of the joints, Neodolpasse was more effective than tramadol, and when they were used together, it allowed to significantly reduce the consumption of an opioid analgesic [23].

Tab. 2. Comparative pharmacokinetics of injectable muscle relaxants Table 2. Comparative pharmacokinetics of injectable muscle relaxants

Parameter

Orphenadrine citrate

Tolperisone hydrochloride

Route of administration

IV (infusion)

IM, IV (injection)

T max (min) 2 (not mentioned in instructions)
T1/2 (hrs) 14 1. 5
Multiplicity of reception 1-2 times a day
no more than 2 days
(restriction on diclofenac, which is part of the medicinal product)
IM, 1 ml 2 times a day daily
In / in, 1 ml 1 time per day

It is important to note that Neodolpass does not violate the hemostasis system. Thus, when using the drug in the early postoperative period, no small and large hemorrhagic complications were registered in patients who underwent surgery for hip arthroplasty [24]. A clinical study of Neodolpass compared with diclofenac and orphenadrine demonstrated greater efficacy of the fixed combination. According to the authors, this is achieved by potentiation of the central antinociceptive effects of NSAIDs and orphenadrine, and not by a simple summation of the effects of each of them [25].

The use of muscle relaxants may be accompanied by side effects, which patients should be informed about. The choice of muscle relaxant should be based on the clinical task and the expected duration of treatment. The shorter the course of treatment, the lower the risk of adverse events. Possible drug interactions must be considered. The most common side effects of muscle relaxants are dizziness and drowsiness, while the sedative properties may be useful for insomnia caused by pain and muscle spasms.

References

1. Young R.R. Spasticity: a review. Neurology 1994; 44(11 Suppl 9): S12–S20.
2. Andersson P.B., Goodkin D.E. Current pharmacological treatment of multiple sclerosis symptoms. West J Med 1996; 165(5): 313–317.
3. Burchiel K.J., Hsu F.P. Pain and spasticity after spinal cord injury: mechanisms and treatment. Spine 2001; 26(24 Suppl): S146–S160.
4. Neurology. Pharmacotherapy without mistakes. Guide for doctors. / Ed. A.A. Skoromets, A.V. Amelina. Moscow: E-noto, 2019; 53–58. Neurology. Pharmacotherapy without errors. A guide for doctors. / ed. A.A. Skoromets, A.V. Ameline. M.: E-noto, 2019; 53–58 pp.
5 Barnes M.P. Medical management of spasticity in stroke. Age Aging 2001; 30(Suppl. 1): 13–16.
6. Anonymous. spasticity. Lancet 1989; 2(8678–8679): 1488–1490.
7. Deyo R.A., Bergman J., Phillips W.R. Drug therapy for back pain: Which drugs help which patients? Spine 1996; 21(24): 2840–2850.
8. Arnold L.M., Keck P.E, Jr., Welge J.A. Antidepressant treatment of fibromyalgia. A meta-analysis and review. Psychosomatics 2000; 41(2): 104–113.
9. Cherkin D.C., Wheeler K.J., Barlow W., et al. Medication use for low back pain in primary care. Spine 1998; 23(5): 607–614.
10. Wagstaff A.J., Bryson H.M. Tizanidine. A review of its pharmacology, clinical efficacy and tolerability in the management of spasticity associated with cerebral and spinal disorders. Drugs 1997; 53(3): 435–452.
11. Nance P.W. Tizanidine: An α2-agonist imidazoline with antispasticity effects. Today’s Ther Trends 1997; 15(1): 11–25.
12. Bijlsma U.G., Harms A.F., Funcke A.B.H., et al. The pharmacology of β-dimethylaminoethyl-2-methylbenzhydrylether hydrochloride. Arch Int Pharmacodyn Ther 1956; 1:332–68.
13. Ginzel K.H. The blockade of reticular and spinal facilitation of motor function by orphenadrine. J Pharmacol Exp Ther 1966; 154:128–41.
14. Onuaguluchi G., Lewis J.J. Some aspects of the pharmacology of orphenadrine. J Pharm Pharmacol 1963; 15:329–36.
15. Smith C.M. Relaxation of decerebrate rigidity by orphenadrine. Proc Soc Exp Biol Med 1964; 116:75–6.
16. Steinbrecher W. Myotonolyse durch Orphenadrincitrat. Arzneimittel Forschung 1966; 16:147–53.
17. Hunskaar S., Donell D. Clinical and pharmacological review of the efficacy of orphenadrine and its combination with paracetamol in painful conditions. J Int Med Res 1991; 19:71–87.
18. Schaffler K., Reitmeir P. Analgesic effects of low-dose intravenous orphenadrine in the state of capsaicin hyperalgesia: a randomized, placebo-controlled, double-blind cross-over study: using laser somatosensory evoked potentials obtained from capsaicin-irritated skin in healthy volunteers. Arzneimittel Forschung 2004; 54:673–9.
19. Winter L., Post A. Analgesic combinations with orphenadrine in oral post surgical pain. J Int Med Res 1979; 7:240–6.
20.Raffa R.B. Antihistamines as analgesics. J Clin Pharm Ther 2001; 26:81–5.
21. Olsen U.B., Eltorp C.T., Ingvardsen B.K., et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol 2002; 435:43–57.
22. Gombotz H., Lochner R., Sigl R., et al. Opiate sparing effect of fixed combination of diclophenac and orphenadrine after unilateral total hip arthroplasty: A double-blind, randomized, placebo-controlled, multi-centre clinical trial. Wien Med Wochenschr 2010; 160 (19-20): 526-534.
23. Borsodi M., Nagy E., Darvas K.. Diclofenac/orphenadrine as a combined analgetic in post-operative relief of pain Orv Hetil. 2008 Sep 28; 149(39): 1847–52.
24. Vymazal T., JBeroušek J. et al. Neodolpasse v časném pooperačním období neovlivňuje tvorbu krevního koagula – prospektivní kohortové sledován.