Tolperisone, a piperidine

Piperidine

Piperidine is an organic compound with the molecular formula 5NH. This heterocyclic amine consists of a six-membered ring containing five methylene units and one nitrogen atom...

 derivative, is a centrally-acting muscle relaxant

Muscle relaxant

A muscle relaxant is a drug which 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...

. Trade names include Biocalm,Muscodol, Mydeton, Mydocalm, Myolax, Myoxan and Viveo.

Clinical use

Typically, tolperisone is indicated in the treatment of acute muscle spasms in back pain and spasticity in neurological diseases.

Manufacturer claims

Tolperisone is currently marketed in Europe as a centrally-acting muscle relaxant, which reportedly has special advantages over other drugs of its class, in that it reportedly does not cause drowsiness or lethargy, according to some manufacturers.

Besides claiming "tolperisone has an excellent efficacy and safety profile", these manufacturers also state tolperisone has the unique property of mediating muscle relaxation "without concomitant sedation" and it does not cause incoordination, weakness, mental confusion or withdrawal phenomena, in contrast to other muscle relaxants.

Indications

Tolperisone is reportedly used in the typical treatment of the following conditions:

• Pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, 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...
  
  , myelopathy
  Myelopathy
  Myelopathy refers to pathology of the spinal cord. When due to trauma, it is known as spinal cord injury. When inflammatory, it is known as myelitis. Disease that is vascular in nature is known as vascular myelopathy....
  
  , encephalomyelitis
  Encephalomyelitis
  Encephalomyelitis is a general term for inflammation of the brain and spinal cord, describing a number of disorders:* Acute disseminated encephalomyelitis or postinfectious encephalomyelitis, a demyelinating disease of the brain and spinal cord, possibly triggered by vaccination or viral...
  
  )
• Spastic paralysis and other encephalopathies manifested with muscular dystonia
• Spondylosis
  Spondylosis
  Spondylosis is a term referring to degenerative osteoarthritis of the joints between the centra of the spinal vertebrae and/or neural foraminae. If this condition occurs in the zygapophysial joints, it can be considered facet syndrome...
  
  
• Spondylarthrosis
• Cervical and lumbar syndromes
• Arthrosis of the large joints
• Obliterating atherosclerosis
  Atherosclerosis
  Atherosclerosis is a condition in which an artery wall thickens as a result of the accumulation of fatty materials such as cholesterol...
  
   of the extremity vessels
• Diabetic angiopathy
  Diabetic angiopathy
  Diabetic angiopathy is a form of angiopathy associated with diabetes mellitus. While not exclusive, the two most common forms are Diabetic retinopathy and Diabetic nephropathy, whose pathophysiologies are largely identical.-Pathophysiology:...
  
  
• Thromboangiitis obliterans
• Raynaud's syndrome

Contraindications and cautions

Manufacturers report that tolperisone should not be used in the following conditions:

• Myasthenia
  Myasthenia gravis
  Myasthenia gravis is an autoimmune neuromuscular disease leading to fluctuating muscle weakness and fatiguability...
  
  
• Children under 1 years of age
• Pregnancy
• Breastfeeding

Side effects and adverse reactions

Some people using tolperisone have reported the following reactions:

• In hypersensitivity: muscle weakness, headache, arterial hypotension
  Hypotension
  In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...
  
  , nausea, vomiting, dyspepsia
  Dyspepsia
  Dyspepsia , also known as upset stomach or indigestion, refers to a condition of impaired digestion. It is a medical condition characterized by chronic or recurrent pain in the upper abdomen, upper abdominal fullness and feeling full earlier than expected when eating...
  
  .
• Skin allergic reactions: skin rash, hives, Quincke's edema, anaphylactic shock.

The side effects and reactions listed above may not include all effects reported by the drug's manufacturer.

Interactions

Tolperisone is believed to have few interactions with other medicines, but this does not rule out any interactions that may not have been reported to caregivers thus far.

Some manufacturers have stated tolperisone may enhance the effects of other neuromuscular blocking agents.

Dosage

According to various sources, the typical oral adult dose for tolperisone is 150-450 mg in a 24-hour period, divided into two or three portions. It is highly advised that dosage information be confirmed by information provided from the manufacturer and prescriber.

More detailed dosage information is as follows:

Adults over 12 years old:

• Oral: 50-150 mg every 8 hours
• IM: 100 mg every 12 hours.
• IV: 100 mg over 24 hours.

Pediatric dosage (minimum weight of 20 kg, minimum age 6 years):

• Oral dosage: 1.0 mg/kg every 8 hours.

Neonatal dosage (minimum weight of 3 kg)

• 2.5 mg/kg every 8 hours.

Also see

• Tolperisone at Drug Info Systems (www.druginfosys.com)
• Papers and safety and efficacy studies of tolperisone at BioInfo
• Tolperisone at Sanochemia Austria