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.

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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

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Orphenadrine: MedlinePlus Drug Information

pronounced as (or fen’ a dreen)

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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

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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.

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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

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

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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.
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24. Vymazal T., JBeroušek J. et al. Neodolpasse v časném pooperačním období neovlivňuje tvorbu krevního koagula – prospektivní kohortové sledován.