Eperisone
Encyclopedia
Eperisone is an antispasmodic
drug.
Eperisone acts by relaxing both skeletal muscle
s and vascular smooth muscle
s, 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 cycle of myotonia by decreasing pain, ischaemia, and hypertonia
in skeletal muscles, thus alleviating stiffness and spasticity
, and facilitating muscle movement
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
.
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
.
s, or as 10% granules for oral administration. 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. It is also available as the brand name Epry as 50 mg as sugar coated tablets.
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.
If elderly patients are treated with eperisone, a reduced dose is recommended, and the patient should be closely monitored for signs of psychological hypofunction during treatment.
(breast-feeding). If eperisone must be used, the patient is advised to stop breast-feeding for the duration of treatment. Eperisone has beed reported to be excreted in breast milk in an animal study (in rats).
to the drug.
Side effects: 'very rare' excessive relaxation, stomachache, nausea, vertigo, anorexia, drowsiness, skin rashes, diarrhoea, vomiting, indigestion, GI disturbances, insomnia, headache, constipation etc.
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.
accommodation
occurring after the concomitant use of the related drug tolperisone
hydrochloride and methocarbamol
.
when taken orally, as a result of high first pass intestinal metabolism
; a transdermal patch
containing eperisone is currently in development in South Korea
. 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.
, China
, India
, Indonesia
, Japan
, United Arab Emirates
, Malaysia, the Philippines
and Thailand
under the brand name Myonal.
Antispasmodic
An antispasmodic is a drug or a herb that suppresses muscle spasms.-Smooth muscle spasm:One type of antispasmodics is used for smooth muscle contraction, especially in tubular organs of the gastrointestinal tract...
drug.
Eperisone acts by relaxing both skeletal muscle
Skeletal muscle
Skeletal muscle is a form of striated muscle tissue existing under control of the somatic nervous system- i.e. it is voluntarily controlled. It is one of three major muscle types, the others being cardiac and smooth muscle...
s and vascular smooth muscle
Vascular smooth muscle
Vascular smooth muscle refers to the particular type of smooth muscle found within, and composing the majority of the wall of blood vessels.Vascular smooth muscle contracts or relaxes to both change the volume of blood vessels and the local blood pressure, a mechanism that is responsible for the...
s, and demonstrates a variety of effects such as reduction of myotonia
Myotonia
Myotonia is a symptom of a small handful of certain neuromuscular disorders characterized by the slow relaxation of the muscles after voluntary contraction or electrical stimulation. Generally, repeated effort is needed to relax the muscles, and the condition improves after the muscles have warmed...
, improvement of circulation
Circulatory system
The circulatory system is an organ system that passes nutrients , gases, hormones, blood cells, etc...
, and suppression of the pain reflex. The drug inhibits the vicious cycle of myotonia by decreasing pain, ischaemia, and hypertonia
Hypertonia
Hypertonia a condition marked by an abnormal increase in muscle tension and a reduced ability of a muscle to stretch. It is caused by lesions to upper motor neurons in the central nervous system, which carry information from the central nervous system to the muscles and control posture, muscle...
in skeletal muscles, thus alleviating stiffness and spasticity
Spasticity
Spasticity is a feature of altered skeletal muscle performance in muscle tone involving hypertonia, which is also referred to as an unusual "tightness" of muscles...
, and facilitating muscle movement
Eperisone also improves dizziness
Dizziness
Dizziness refers to an impairment in spatial perception and stability. The term is somewhat imprecise. It can be used to mean vertigo, presyncope, disequilibrium, or a non-specific feeling such as giddiness or foolishness....
and tinnitus
Tinnitus
Tinnitus |ringing]]") is the perception of sound within the human ear in the absence of corresponding external sound.Tinnitus is not a disease, but a symptom that can result from a wide range of underlying causes: abnormally loud sounds in the ear canal for even the briefest period , ear...
associated with cerebrovascular disorders or cervical spondylosis.
Eperisone has a relatively low incidence of sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
when compared with other antispasmodic drugs; this simplifies the clinical
Illness
Illness is a state of poor health. Illness is sometimes considered another word for disease. Others maintain that fine distinctions exist...
application of the drug and makes it an attractive choice for patients who require antispasmodic therapy without a reduction in alertness
Alertness
Alertness is the state of paying close and continuous attention, being watchful and prompt to meet danger or emergency, or being quick to perceive and act. It is related to psychology as well as to physiology...
.
Eperisone also facilitates voluntary movement of the upper and lower extremities
Extremities
Extremities may refer to:* Extremities , a play by William Mastrosimone* Extremities , a film based on the play* limbs of the body, in medical terminology...
without reducing muscle power; it is therefore useful during the initial stage of rehabilitation
Physical medicine and rehabilitation
Physical medicine and rehabilitation , physiatry or rehabilitation medicine, is a branch of medicine that aims to enhance and restore functional ability and quality of life to those with physical impairments or disabilities. A physician having completed training in this field is referred to as a...
and as a supporting drug during subsequent rehabilitative therapy
Physical therapy
Physical therapy , often abbreviated PT, is a health care profession. Physical therapy is concerned with identifying and maximizing quality of life and movement potential within the spheres of promotion, prevention, diagnosis, treatment/intervention,and rehabilitation...
.
Indications
- Spastic paralysis in conditions such as cerebrovascular disease
- Spastic spinal paralysisParalysisParalysis is loss of muscle function for one or more muscles. Paralysis can be accompanied by a loss of feeling in the affected area if there is sensory damage as well as motor. A study conducted by the Christopher & Dana Reeve Foundation, suggests that about 1 in 50 people have been diagnosed...
- Cervical spondylosis
- Postoperative sequelae (including from cerebrospinal tumour)
- Sequelae to traumaPhysical traumaTrauma refers to "a body wound or shock produced by sudden physical injury, as from violence or accident." It can also be described as "a physical wound or injury, such as a fracture or blow." Major trauma can result in secondary complications such as circulatory shock, respiratory failure and death...
(e.g. spinal trauma or head injuryHead injuryHead injury refers to trauma of the head. This may or may not include injury to the brain. However, the terms traumatic brain injury and head injury are often used interchangeably in medical literature....
) - Amyotrophic lateral sclerosisAmyotrophic lateral sclerosisAmyotrophic lateral sclerosis , also referred to as Lou Gehrig's disease, is a form of motor neuron disease caused by the degeneration of upper and lower neurons, located in the ventral horn of the spinal cord and the cortical neurons that provide their efferent input...
- Cerebral palsyCerebral palsyCerebral palsy is an umbrella term encompassing a group of non-progressive, non-contagious motor conditions that cause physical disability in human development, chiefly in the various areas of body movement....
- Spinocerebellar degeneration
- Spinal vascular diseaseVascular diseaseVascular disease is a form of cardiovascular disease primarily affecting the blood vessels.Some conditions, such as angina and myocardial ischemia, can be considered both vascular diseases and heart diseases .Cigarette smoking is the major risk factor....
s and other encephalomyelopathies - Cervical syndrome, periarthritis of the shoulderShoulderThe human shoulder is made up of three bones: the clavicle , the scapula , and the humerus as well as associated muscles, ligaments and tendons. The articulations between the bones of the shoulder make up the shoulder joints. The major joint of the shoulder is the glenohumeral joint, which...
, and lumbago.
Presentation
Eperisone hydrochloride is available as the brand name preparation Myonal as 50 mg enteric coated tabletTablet
A tablet is a pharmaceutical dosage form. It comprises a mixture of active substances and excipients, usually in powder form, pressed or compacted from a powder into a solid dose...
s, or as 10% granules for oral administration. 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. It is also available as the brand name Epry as 50 mg as sugar coated tablets.
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 prescribingMedical prescription
A prescription is a health-care program implemented by a physician or other medical practitioner in the form of instructions that govern the plan of care for an individual patient. Prescriptions may include orders to be performed by a patient, caretaker, nurse, pharmacist or other therapist....
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.
If elderly patients are treated with eperisone, a reduced dose is recommended, and the patient should be closely monitored for signs of psychological hypofunction during treatment.
Safety during pregnancy and breast-feeding
Eperisone has not been established to be safe for use by pregnant women; therefore the drug should only 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 lactationLactation
Lactation describes the secretion of milk from the mammary glands and the period of time that a mother lactates to feed her young. The process occurs in all female mammals, however it predates mammals. In humans the process of feeding milk is called breastfeeding or nursing...
(breast-feeding). If eperisone must be used, the patient is advised to stop breast-feeding for the duration of treatment. Eperisone has beed reported to be excreted in breast milk in an animal study (in rats).
Pharmacology
- Skeletal muscleSkeletal muscleSkeletal muscle is a form of striated muscle tissue existing under control of the somatic nervous system- i.e. it is voluntarily controlled. It is one of three major muscle types, the others being cardiac and smooth muscle...
relaxationRelaxation techniqueA relaxation technique is any method, process, procedure, or activity that helps a person to relax; to attain a state of increased calmness; or otherwise reduce levels of anxiety, stress or anger... - Relaxation of hypertonicHypertoniaHypertonia a condition marked by an abnormal increase in muscle tension and a reduced ability of a muscle to stretch. It is caused by lesions to upper motor neurons in the central nervous system, which carry information from the central nervous system to the muscles and control posture, muscle...
skeletal muscles - Improves intramuscular blood flowBlood flowBlood flow is the continuous running of blood in the cardiovascular system.The human body is made up of several processes all carrying out various functions. We have the gastrointestinal system which aids the digestion and the absorption of food...
- Suppression of spinal reflex potentials
- Reduction of muscle spindleMuscle spindleMuscle spindles are sensory receptors within the belly of a muscle, which primarily detect changes in the length of this muscle. They convey length information to the central nervous system via sensory neurons. This information can be processed by the brain to determine the position of body parts...
sensitivity via motor neurons - Vasodilatation and augmentation of blood flow
- AnalgesicAnalgesicAn analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
action and inhibition of the pain reflex in the spinal cordSpinal cordThe spinal cord is a long, thin, tubular bundle of nervous tissue and support cells that extends from the brain . The brain and spinal cord together make up the central nervous system...
Contraindications
Eperisone is contraindicated in patients with known hypersensitivityHypersensitivity
Hypersensitivity refers to undesirable reactions produced by the normal immune system, including allergies and autoimmunity. These reactions may be damaging, uncomfortable, or occasionally fatal. Hypersensitivity reactions require a pre-sensitized state of the host. The four-group classification...
to the drug.
Side effects: 'very rare' excessive relaxation, stomachache, nausea, vertigo, anorexia, drowsiness, skin rashes, diarrhoea, vomiting, indigestion, GI disturbances, insomnia, headache, constipation etc.
Cautions
Eperisone should be administered with care in patients with a history of hypersensitivity to any medication, or with disorders of liverLiver
The liver is a vital organ present in vertebrates and some other animals. It has a wide range of functions, including detoxification, protein synthesis, and production of biochemicals necessary for digestion...
function (it may aggravate hepatic dysfunction).
Weakness
Weakness
Weakness is a symptom represented, medically, by a number of different conditions, including: lack of muscle strength, malaise, dizziness, or fatigue. The causes are many and can be divided into conditions that have true or perceived muscle weakness. True muscle weakness is a primary symptom of a...
, 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.
Side effects
- Shock and anaphylactoid reactions: In the event of symptoms such as redness, itching, urticariaUrticariaUrticaria is a kind of skin rash notable for pale red, raised, itchy bumps. Hives is frequently caused by allergic reactions; however, there are many non-allergic causes...
, oedema of the face and other parts of the body, dyspnoea, etc., treatment should be discontinued and appropriate measues taken. - Oculomucocutaneous syndrome and toxic epidermal necrolysis: Serious dermatopathy such as oculomucocutaneous syndrome (Stevens–Johnson syndrome) or toxic epidermal necrolysisToxic epidermal necrolysisToxic epidermal necrolysis is a rare, life-threatening dermatological condition that is usually induced by a reaction to medications...
may occur. Patients should be carefully observed, treatment discontinued and appropriate measures taken, in the event of symptoms such as feverFeverFever is a common medical sign characterized by an elevation of temperature above the normal range of due to an increase in the body temperature regulatory set-point. This increase in set-point triggers increased muscle tone and shivering.As a person's temperature increases, there is, in...
, erythemaErythemaErythema is redness of the skin, caused by hyperemia of the capillaries in the lower layers of the skin. It occurs with any skin injury, infection, or inflammation...
, blistering, itching, ocular congestion or stomatitisStomatitisStomatitis is an inflammation of the mucous lining of any of the structures in the mouth, which may involve the cheeks, gums, tongue, lips, throat, and roof or floor of the mouth...
, etc. - CNS side effects: depletion of myelin sheath of nerves
- Other side effects: anaemia, rashRashA rash is a change of the skin which affects its color, appearance or texture. A rash may be localized in one part of the body, or affect all the skin. Rashes may cause the skin to change color, itch, become warm, bumpy, chapped, dry, cracked or blistered, swell and may be painful. The causes, and...
, pruritus, sleepiness, insomniaInsomniaInsomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...
, headacheHeadacheA headache or cephalalgia is pain anywhere in the region of the head or neck. It can be a symptom of a number of different conditions of the head and neck. The brain tissue itself is not sensitive to pain because it lacks pain receptors. Rather, the pain is caused by disturbance of the...
, nauseaNauseaNausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
and vomitingVomitingVomiting is the forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose...
, anorexiaAnorexia (symptom)Anorexia is the decreased sensation of appetite...
, abdominal pain, diarrhoea, constipationConstipationConstipation refers to bowel movements that are infrequent or hard to pass. Constipation is a common cause of painful defecation...
, urinary retentionUrinary retentionUrinary retention, also known as ischuria, is a lack of ability to urinate. It is a common complication of benign prostatic hyperplasia , although it can also be caused by nerve dysfunction, constipation, infection, or medications...
or incontinenceUrinary incontinenceUrinary incontinence is any involuntary leakage of urine. It is a common and distressing problem, which may have a profound impact on quality of life. Urinary incontinence almost always results from an underlying treatable medical condition but is under-reported to medical practitioners...
.
Drug interactions
There have been reports of disturbances in ocularHuman eye
The human eye is an organ which reacts to light for several purposes. As a conscious sense organ, the eye allows vision. Rod and cone cells in the retina allow conscious light perception and vision including color differentiation and the perception of depth...
accommodation
Accommodation (eye)
Accommodation is the process by which the vertebrate eye changes optical power to maintain a clear image on an object as its distance changes....
occurring after the concomitant use of the related drug tolperisone
Tolperisone
Tolperisone, a piperidine derivative, is a centrally-acting muscle relaxant. Trade names include Biocalm,Muscodol, Mydeton, Mydocalm, Myolax, Myoxan and Viveo.- Clinical use :...
hydrochloride and methocarbamol
Methocarbamol
Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms...
.
Safety in overdose
Seizures have been reported in an infant after accidental ingestion of eperisone.Future developments
Eperisone suffers from a very low bioavailabilityBioavailability
In pharmacology, bioavailability is a subcategory of absorption and is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. By definition, when a medication is administered...
when taken orally, as a result of high first pass intestinal metabolism
Metabolism
Metabolism is the set of chemical reactions that happen in the cells of living organisms to sustain life. These processes allow organisms to grow and reproduce, maintain their structures, and respond to their environments. Metabolism is usually divided into two categories...
; a transdermal patch
Transdermal patch
A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. Often, this promotes healing to an injured area of the body. An advantage of a transdermal drug delivery route over other types of...
containing eperisone is currently in development in South Korea
South Korea
The Republic of Korea , , is a sovereign state in East Asia, located on the southern portion of the Korean Peninsula. It is neighbored by the People's Republic of China to the west, Japan to the east, North Korea to the north, and the East China Sea and Republic of China to the south...
. 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
Antihypertensive
The antihypertensives are a class of drugs that are used to treat hypertension . Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34%, of ischaemic heart disease by 21%, and reduce the likelihood of dementia, heart failure, and mortality from...
agent, with promising results from trials on beagles.
Brand names
Eperisone is sold in BangladeshBangladesh
Bangladesh , officially the People's Republic of Bangladesh is a sovereign state located in South Asia. It is bordered by India on all sides except for a small border with Burma to the far southeast and by the Bay of Bengal to the south...
, China
People's Republic of China
China , officially the People's Republic of China , is the most populous country in the world, with over 1.3 billion citizens. Located in East Asia, the country covers approximately 9.6 million square kilometres...
, India
India
India , officially the Republic of India , is a country in South Asia. It is the seventh-largest country by geographical area, the second-most populous country with over 1.2 billion people, and the most populous democracy in the world...
, Indonesia
Indonesia
Indonesia , officially the Republic of Indonesia , is a country in Southeast Asia and Oceania. Indonesia is an archipelago comprising approximately 13,000 islands. It has 33 provinces with over 238 million people, and is the world's fourth most populous country. Indonesia is a republic, with an...
, Japan
Japan
Japan is an island nation in East Asia. Located in the Pacific Ocean, it lies to the east of the Sea of Japan, China, North Korea, South Korea and Russia, stretching from the Sea of Okhotsk in the north to the East China Sea and Taiwan in the south...
, United Arab Emirates
United Arab Emirates
The United Arab Emirates, abbreviated as the UAE, or shortened to "the Emirates", is a state situated in the southeast of the Arabian Peninsula in Western Asia on the Persian Gulf, bordering Oman, and Saudi Arabia, and sharing sea borders with Iraq, Kuwait, Bahrain, Qatar, and Iran.The UAE is a...
, Malaysia, the Philippines
Philippines
The Philippines , officially known as the Republic of the Philippines , is a country in Southeast Asia in the western Pacific Ocean. To its north across the Luzon Strait lies Taiwan. West across the South China Sea sits Vietnam...
and Thailand
Thailand
Thailand , officially the Kingdom of Thailand , formerly known as Siam , is a country located at the centre of the Indochina peninsula and Southeast Asia. It is bordered to the north by Burma and Laos, to the east by Laos and Cambodia, to the south by the Gulf of Thailand and Malaysia, and to the...
under the brand name Myonal.