Flupirtine
Encyclopedia
Flupirtine is an aminopyridine
that functions as a centrally acting non-opioid
analgesic
. It first became available in Europe
in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Flupirtine is available as "Pruf",Snepdol in India. It is unique as a non-opioid, non-NSAID, non-steroidal analgesic.
market for any indication. In 2008, Adeona
obtained an option to license issued and patent pending
applications relating to flupirtine’s use in the treatment of ophthalmic
indications.
that also has NMDA receptor antagonist
properties.
, postoperative care, and gynaecology
.
Flupirtine has been noted for its neuro-protective properties, and it is being investigated for possible use in Creutzfeld-Jakob disease, Alzheimer's disease
, and multiple sclerosis
. It has also been proposed as a possible treatment for Batten disease
.
Flupirtine underwent a clinical trial
as a treatment for multiple sclerosis
and fibromyalgia
. Flupirtine showed promise for fibromyalgia due to its different action than the three approved US Food and Drug Administration
drugs: Lyrica, Savella, and Cymbalta. Additionally, there are case reports regarding flupirtine as a treatment for fibromyalgia. Adeona sub-licensed its patents for using flupirtine for fibromyalgia to Meda AB
in May 2010.
toxicity
and rare cardiac effects related to its mechanism of action in patients predisposed to cardiac disease. Flupirtine is notably devoid of any addictive properties, negative psychological or motor function effects, or effects on reproductive function. Drug tolerance does not develop in most cases; however, tolerance may develop in single cases.
Aminopyridine
Aminopyridine may refer to any of several chemical compounds:* 2-Aminopyridine* 3-Aminopyridine* 4-Aminopyridine...
that functions as a centrally acting non-opioid
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
. It first became available in Europe
Europe
Europe is, by convention, one of the world's seven continents. Comprising the westernmost peninsula of Eurasia, Europe is generally 'divided' from Asia to its east by the watershed divides of the Ural and Caucasus Mountains, the Ural River, the Caspian and Black Seas, and the waterways connecting...
in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Flupirtine is available as "Pruf",Snepdol in India. It is unique as a non-opioid, non-NSAID, non-steroidal analgesic.
History
Flupirtine was originally developed by Asta Medica and was approved for the treatment of pain in 1984 in Europe. However, it has never been introduced to the United StatesUnited States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
market for any indication. In 2008, Adeona
Adeona
Adeona is a genus of bryozoan in the family Adeonidae. A typical example is the Australian species Adeona cellulosa that forms large colonies with bifoliate sheets containing numerous holes .-Selected species:* Adeona albida...
obtained an option to license issued and patent pending
Patent pending
The expressions "patent pending" or "patent applied for" refer to a warning that inventors are entitled to use in reference to their product or process once a patent application has been filed, but prior to the patent being issued or the application abandoned...
applications relating to flupirtine’s use in the treatment of ophthalmic
Ophthalmic
Ophthalmic means pertaining to the eye, and can refer to:* Ophthalmology* Ophthalmic nerve* Ophthalmic artery* Ophthalmic veins* Ophthalmic drug administration, as with eye dropsSee also:* Ophthalmia...
indications.
Mechanism of action
Flupirtine is a selective neuronal potassium channel openerPotassium channel opener
A potassium channel opener is a type of drug which facilitates ion transmission through potassium channels.Some examples include:* Diazoxide vasodilator used for hypertension, smooth muscle relaxing activity...
that also has NMDA receptor antagonist
NMDA receptor antagonist
NMDA receptor antagonists are a class of anesthetics that work to antagonize, or inhibit the action of, the N-methyl d-aspartate receptor . They are used as anesthesia for animals and, less commonly, for humans; the state of anesthesia they induce is referred to as dissociative anesthesia...
properties.
Uses
Flupirtine is used as an analgesic for acute and chronic pain, in moderate to severe cases. Its muscle relaxant properties make it popular for back pain and other orthopaedic uses, but it is also used for migraines, in oncologyOncology
Oncology is a branch of medicine that deals with cancer...
, postoperative care, and gynaecology
Gynaecology
Gynaecology or gynecology is the medical practice dealing with the health of the female reproductive system . Literally, outside medicine, it means "the science of women"...
.
Flupirtine has been noted for its neuro-protective properties, and it is being investigated for possible use in Creutzfeld-Jakob disease, Alzheimer's disease
Alzheimer's disease
Alzheimer's disease also known in medical literature as Alzheimer disease is the most common form of dementia. There is no cure for the disease, which worsens as it progresses, and eventually leads to death...
, and multiple sclerosis
Multiple sclerosis
Multiple sclerosis is an inflammatory disease in which the fatty myelin sheaths around the axons of the brain and spinal cord are damaged, leading to demyelination and scarring as well as a broad spectrum of signs and symptoms...
. It has also been proposed as a possible treatment for Batten disease
Batten disease
Batten disease is a rare, fatal autosomal recessive neurodegenerative disorder that begins in childhood...
.
Flupirtine underwent a clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
as a treatment for multiple sclerosis
Multiple sclerosis
Multiple sclerosis is an inflammatory disease in which the fatty myelin sheaths around the axons of the brain and spinal cord are damaged, leading to demyelination and scarring as well as a broad spectrum of signs and symptoms...
and fibromyalgia
Fibromyalgia
Fibromyalgia is a medical disorder characterized by chronic widespread pain and allodynia, a heightened and painful response to pressure. It is an example of a diagnosis of exclusion...
. Flupirtine showed promise for fibromyalgia due to its different action than the three approved US Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
drugs: Lyrica, Savella, and Cymbalta. Additionally, there are case reports regarding flupirtine as a treatment for fibromyalgia. Adeona sub-licensed its patents for using flupirtine for fibromyalgia to Meda AB
Meda AB
MEDA AB is a Swedish pharmaceutical company that concentrates on "marketing and market-adapted product development". Through their purchase of Medpointe, they own the pharmaceutical products of Carter-Wallace, now marketed under the name Wallace Pharmaceuticals....
in May 2010.
Side effects
The main side effects of Flupirtine are possible 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...
toxicity
Toxicity
Toxicity is the degree to which a substance can damage a living or non-living organisms. Toxicity can refer to the effect on a whole organism, such as an animal, bacterium, or plant, as well as the effect on a substructure of the organism, such as a cell or an organ , such as the liver...
and rare cardiac effects related to its mechanism of action in patients predisposed to cardiac disease. Flupirtine is notably devoid of any addictive properties, negative psychological or motor function effects, or effects on reproductive function. Drug tolerance does not develop in most cases; however, tolerance may develop in single cases.