Eperisone

Last updated
Eperisone
Eperisone.png
Eperisone3d.png
Clinical data
Trade names Myonal
AHFS/Drugs.com International Drug Names
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • (2RS)-1-(4-Ethylphenyl)-2-methyl-3-(1-piperidyl)propan-1-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C17H25NO
Molar mass 259.393 g·mol−1
3D model (JSmol)
  • CCc1ccc(cc1)C(=O)C(C)CN2CCCCC2
  • InChI=1S/C17H25NO/c1-3-15-7-9-16(10-8-15)17(19)14(2)13-18-11-5-4-6-12-18/h7-10,14H,3-6,11-13H2,1-2H3 Yes check.svgY
  • Key:SQUNAWUMZGQQJD-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Eperisone (formulated as the eperisone hydrochloride salt) is an antispasmodic drug.

Contents

Eperisone acts by relaxing both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex. The drug inhibits the vicious circle of myotonia by decreasing pain, ischaemia, and hypertonia in skeletal muscles, thus alleviating stiffness and spasticity, and facilitating muscle movement [1]

Eperisone also improves dizziness and tinnitus associated with cerebrovascular disorders or cervical spondylosis.

Eperisone has a relatively low incidence of sedation when compared with other antispasmodic drugs; this simplifies the clinical application of the drug and makes it an attractive choice for patients who require antispasmodic therapy without a reduction in alertness.

Japanese package of eperisone mionaru50mDing P6075387.jpg
Japanese package of eperisone

Eperisone also facilitates voluntary movement of the upper and lower extremities without reducing muscle power; it is therefore useful during the initial stage of rehabilitation and as a supporting drug during subsequent rehabilitative therapy.

Indications

Presentation

Eperisone hydrochloride is available as the brand name preparations Myonal and Epry as 50 mg sugar-coated tablets, or as 10% granules for oral administration. [6] An experimental form of the drug, as a transdermal patch system, has shown promising results in laboratory tests on rodents; however, this product is not currently available for human use. [7]

Dosage and administration

In adults, the usual dose of eperisone is 50–150 mg per day, in divided doses, after meals. However, the dosage is adjusted by the prescribing clinician depending on factors such as severity of symptoms, patient age and response.

Eperisone has not been established as definitely safe for paediatric use, therefore its use in paediatrics cannot be recommended without further study. [6]

If elderly patients are treated with eperisone, a reduced dose is recommended, and the patient should be closely monitored for signs of physiological hypofunction during treatment. [6]

Safety during pregnancy and breast-feeding

Eperisone has not been established to be safe for use by pregnant women; therefore the drug should not be used in pregnant women, or women who may be pregnant, if the expected therapeutic benefits will outweigh the possible risks associated with treatment. The manufacturers of Myonal recommend the drug not be used during lactation (breast-feeding). If eperisone must be used, the patient is advised to stop breast-feeding for the duration of treatment. Eperisone has been reported to be excreted in breast milk in an animal study (in rats).

Pharmacology

Contraindications

Eperisone is contraindicated in patients with known hypersensitivity to the drug. [8] Side effects: 'very rare' excessive relaxation, stomachache, nausea, vertigo, anorexia, drowsiness, skin rashes, diarrhoea, vomiting, indigestion, GI disturbances, insomnia, headache, constipation etc. [9]

Cautions

Eperisone should be administered with care in patients with a history of hypersensitivity to any medication, or with disorders of liver function (it may aggravate hepatic dysfunction).

Weakness, light-headedness, sleepiness or other symptoms may occur. In the event of such symptoms, the dosage should be reduced or treatment discontinued. Patients should be cautioned against engaging in potentially hazardous activities requiring alertness, such as operating machinery or driving a car. [6]

Side effects

Drug interactions

There have been reports of disturbances in ocular accommodation occurring after the concomitant use of the related drug tolperisone hydrochloride and methocarbamol.

Safety in overdose

Seizures have been reported in an infant after accidental ingestion of eperisone. [11]

Future developments

Eperisone suffers from a very low bioavailability when taken orally, as a result of high first pass intestinal metabolism; a transdermal patch containing eperisone is currently in development in South Korea. [1] This has shown promise, with the antispasmodic effect lasting over 24 hours, compared to one to two hours following oral administration.

Eperisone is also under investigation as an antihypertensive agent, with promising results from trials on beagles. [12]

Brand names

Eperisone is marketed under many brand names worldwide. [13]

See also

Chemically and mechanistically related drugs:

Related Research Articles

Spasticity is a feature of altered skeletal muscle performance with a combination of paralysis, increased tendon reflex activity, and hypertonia. It is also colloquially referred to as an unusual "tightness", stiffness, or "pull" of muscles.

<span class="mw-page-title-main">Tetraplegia</span> Paralysis of all four limbs and torso

Tetraplegia, also known as quadriplegia, is defined as the dysfunction or loss of motor and/or sensory function in the cervical area of the spinal cord. A loss of motor function can present as either weakness or paralysis leading to partial or total loss of function in the arms, legs, trunk, and pelvis. The paralysis may be flaccid or spastic. A loss of sensory function can present as an impairment or complete inability to sense light touch, pressure, heat, pinprick/pain, and proprioception. In these types of spinal cord injury, it is common to have a loss of both sensation and motor control.

An antispasmodic is a pharmaceutical drug or other agent that suppresses muscle spasms.

A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. 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 relaxant, 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 relaxant, the term is commonly used to refer to spasmolytics only.

<span class="mw-page-title-main">Lidocaine</span> Local anesthetic

Lidocaine, also known as lignocaine and sold under the brand name Xylocaine among others, is a local anesthetic of the amino amide type. It is also used to treat ventricular tachycardia and ventricular fibrillation. When used for local anaesthesia or in nerve blocks, lidocaine typically begins working within several minutes and lasts for half an hour to three hours. Lidocaine mixtures may also be applied directly to the skin or mucous membranes to numb the area. It is often used mixed with a small amount of adrenaline (epinephrine) to prolong its local effects and to decrease bleeding.

<span class="mw-page-title-main">Hydromorphone</span> Opioid medication used for pain relief

Hydromorphone, also known as dihydromorphinone, and sold under the brand name Dilaudid among others, is a morphinan opioid used to treat moderate to severe pain. Typically, long-term use is only recommended for pain due to cancer. It may be used by mouth or by injection into a vein, muscle, or under the skin. Effects generally begin within half an hour and last for up to five hours. A 2016 Cochrane review found little difference in benefit between hydromorphone and other opioids for cancer pain.

<span class="mw-page-title-main">Clonidine</span> Pharmaceutical drug

Clonidine, sold under the brand name Catapres among others, is an α2A-adrenergic receptor agonist medication used to treat high blood pressure, ADHD, drug withdrawal, menopausal flushing, diarrhea, spasticity, and certain pain conditions. The drug is often prescribed off-label for tics. It is used orally, by injection, or as a transdermal skin patch. Onset of action is typically within an hour with the effects on blood pressure lasting for up to eight hours.

<span class="mw-page-title-main">Cyclobenzaprine</span> Muscle relaxant medication

Cyclobenzaprine, sold under several brand names including, historically, Flexeril, is a muscle relaxer used for muscle spasms from musculoskeletal conditions of sudden onset. It is not useful in cerebral palsy. It is taken by mouth.

<span class="mw-page-title-main">Spondylosis</span> Degeneration of the vertebral column

Spondylosis is the degeneration of the vertebral column from any cause. In the more narrow sense it refers to spinal osteoarthritis, the age-related degeneration of the spinal column, which is the most common cause of spondylosis. The degenerative process in osteoarthritis chiefly affects the vertebral bodies, the neural foramina and the facet joints. If severe, it may cause pressure on the spinal cord or nerve roots with subsequent sensory or motor disturbances, such as pain, paresthesia, imbalance, and muscle weakness in the limbs.

Myelopathy describes any neurologic deficit related to the spinal cord. The most common form of myelopathy in humans, cervical spondylotic myelopathy (CSM), also called degenerative cervical myelopathy, results from narrowing of the spinal canal ultimately causing compression of the spinal cord. When due to trauma, myelopathy is known as (acute) spinal cord injury. When inflammatory, it is known as myelitis. Disease that is vascular in nature is known as vascular myelopathy.

<span class="mw-page-title-main">Orphenadrine</span> Muscle relaxant drug

Orphenadrine is an anticholinergic drug of the ethanolamine antihistamine class; it is closely related to diphenhydramine. It is a muscle relaxant that is used to treat muscle pain and to help with motor control in Parkinson's disease, but has largely been superseded by newer drugs. It is considered a dirty drug due to its multiple mechanisms of action in different pathways. It was discovered and developed in the 1940s.

<span class="mw-page-title-main">Tizanidine</span> Muscle relaxant medication

Tizanidine, sold under the brand name Zanaflex among others, is an alpha-2 (α2) adrenergic receptor agonist, similar to clonidine, that is used to treat muscle spasticity due to spinal cord injury, multiple sclerosis, and spastic cerebral palsy. Effectiveness appears similar to baclofen or diazepam. It is taken by mouth.

Hypertonia is a term sometimes used synonymously with spasticity and rigidity in the literature surrounding damage to the central nervous system, namely upper motor neuron lesions. Impaired ability of damaged motor neurons to regulate descending pathways gives rise to disordered spinal reflexes, increased excitability of muscle spindles, and decreased synaptic inhibition. These consequences result in abnormally increased muscle tone of symptomatic muscles. Some authors suggest that the current definition for spasticity, the velocity-dependent over-activity of the stretch reflex, is not sufficient as it fails to take into account patients exhibiting increased muscle tone in the absence of stretch reflex over-activity. They instead suggest that "reversible hypertonia" is more appropriate and represents a treatable condition that is responsive to various therapy modalities like drug or physical therapy.

<span class="mw-page-title-main">Tolperisone</span> Skeletal muscle relaxant drug

Tolperisone is a centrally acting skeletal muscle relaxant used for the treatment of increased muscle tone associated with neurological diseases. It has been used since the 1960s.

<span class="mw-page-title-main">Radiculopathy</span> Medical condition

Radiculopathy, also commonly referred to as pinched nerve, refers to a set of conditions in which one or more nerves are affected and do not work properly. Radiculopathy can result in pain, weakness, altered sensation (paresthesia) or difficulty controlling specific muscles. Pinched nerves arise when surrounding bone or tissue, such as cartilage, muscles or tendons, put pressure on the nerve and disrupt its function.

Hoffmann's reflex is a neurological examination finding elicited by a reflex test which can help verify the presence or absence of issues arising from the corticospinal tract. It is named after neurologist Johann Hoffmann. Usually considered a pathological reflex in a clinical setting, the Hoffmann's reflex has also been used as a measure of spinal reflex processing (adaptation) in response to exercise training.

<span class="mw-page-title-main">Neck pain</span> Medical condition

Neck pain, also known as cervicalgia, is a common problem, with two-thirds of the population having neck pain at some point in their lives.

<span class="mw-page-title-main">Thiocolchicoside</span> Chemical compound

Thiocolchicoside is a muscle relaxant with anti-inflammatory and analgesic effects. Its mechanism of action is unknown, but it is believed to be act via antagonism of nicotinic acetylcholine receptors (nAchRs). However, it also appears to be a competitive antagonist of GABAA and glycine receptors. As such, it has powerful convulsant activity and should not be used in seizure-prone individuals.

<span class="mw-page-title-main">Lanperisone</span> Muscle relaxant drug

Lanperisone (INN) is a muscle relaxant.

An analgesic adjuvant is a medication that is typically used for indications other than pain control but provides control of pain (analgesia) in some painful diseases. This is often part of multimodal analgesia, where one of the intentions is to minimize the need for opioids.

References

  1. 1 2 Yang SI, Park HY, Lee SH, Lee SJ, Han OY, Lim SC, et al. (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone". Pharmacology. 71 (3): 150–156. doi:10.1159/000077449. PMID   15161997. S2CID   24474033.
  2. "eperisone Summary Report - CureHunter". www.curehunter.com.
  3. Bose K (April 1999). "The efficacy and safety of eperisone in patients with cervical spondylosis: results of a randomized, double-blind, placebo-controlled trial". Methods and Findings in Experimental and Clinical Pharmacology. 21 (3): 209–213. doi:10.1358/mf.1999.21.3.534831. PMID   10389124.
  4. 1 2 "Myonil®" (PDF). Archived from the original (PDF) on 2009-02-06. Retrieved 2008-09-01.
  5. "Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study". europeanreview.org. 17 October 2012.
  6. 1 2 3 4 "Myonal Tablets 50 mg" (PDF). Archived from the original (PDF) on 2009-12-29. Retrieved 2008-09-01.
  7. Yang SI, Park HY, Lee SH, Lee SJ, Han OY, Lim SC, et al. (July 2004). "Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone". Pharmacology. 71 (3): 150–156. doi:10.1159/000077449. PMID   15161997. S2CID   24474033.
  8. Clinical trial number NCT00327730 for "Evaluation of Eperisone HCl in the Treatment of Acute Musculoskeletal Spasm Associated With Low Back Pain" at ClinicalTrials.gov
  9. "Myonil®" (PDF). Archived from the original (PDF) on 2010-11-28. Retrieved 2010-06-12.
  10. Ueno T, Kawana S (July 2007). "[A case of eperisone hydrochloride (myonal)--induced drug eruption leading to erythema and angioedema]". Arerugi = [Allergy] (in Japanese). 56 (7): 709–713. PMID   17671415. Archived from the original on 2014-12-19. Retrieved 2008-09-28.
  11. Tanno K, Narimatsu E, Takeyama Y, Asai Y (May 2007). "Infantile case of seizure induced by intoxication after accidental consumption of eperisone hydrochloride, an antispastic agent". The American Journal of Emergency Medicine. 25 (4): 481–482. doi:10.1016/j.ajem.2006.09.002. PMID   17499672.
  12. EP 0310259 Eperisone as a hypotensive agent
  13. "International eperisone brands". Drugs.com. Retrieved 10 March 2016.

Further reading