TAPENTADOL+THIOCHOLCHISOSIDE

RATIONALE JUSTIFICATION

Spasticity is a state of increased muscular tone with exaggeration of the tendon

reflexes. Some of the more common conditions associated with spasticity and
requiring treatment include multiple sclerosis, spinal cord injury, traumatic brain
injury, cerebral palsy, and poststroke syndrome. In many patients with these
conditions, spasticity can be disabling and painful with a marked effect on
functional ability and quality of life.

The upper motor neuron syndrome is a complex of signs and symptoms that can
be associated with exaggerated cutaneous reflexes, autonomic hyperreflexia,
dystonia, contractures, paresis, lack of dexterity, and fatigability. Spasticity from
the upper motor neuron syndrome can result from a variety of conditions
affecting the cortex or spinal cord.

Muscle spasm is defined as a sudden involuntary contraction of one or more

muscle groups and is usually an acute condition associated with muscle strain
(partial tear of a muscle) or sprain (partial or complete rupture of a ligament).
Common musculoskeletal conditions causing tenderness and muscle spasms
include fibromyalgia, tension headaches, myofascial pain syndrome, and
mechanical low back pain or neck pain. If muscle spasm is present in these
conditions, it is related to local factors involving the affected muscle groups.
There is no hypertonicity or hyperreflexia, and the other symptoms associated
with the upper motor neuron syndrome are not present. These conditions are
commonly encountered in clinical practice and can cause significant disability
and pain in some patients.

Most studies have shown the skeletal muscle relaxants to be more effective than
placebo in the treatment of acute painful musculoskeletal disorders and muscle
spasm, while efficacy was less consistent when treating chronic disorders. When
muscle relaxants were used alone, they were not consistently superior to simple
analgesics in relieving pain. When the skeletal muscle relaxants were used in
combination with analgesics, pain relief is superior to either agent used alone.
Studies have suggested that these drugs are effective, have tolerable side
effects, and can be an adjunct in the treatment of painful musculoskeletal
conditions with associated muscle spasm.

A new semi-opioid analgesic with a dual mechanism of action has been released
for market by PriCara, a division of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
Tapentadol is a mu-opioid receptor agonist as well as an inhibitor of
norepinephrine reuptake. The drug was originally approved by the FDA last year.
It is non another but tapentadol a novel, centrally acting analgesic with two
mechanisms of action that confers broad efficacy, as demonstrated in a variety of
preclinical analgesia models. The pharmacologic activity of tapentadol is due to
both mu-opioid receptor (MOR) agonism and norepinephrine reuptake inhibition.
Tapentadol has favorable side effect profile and rapid onset of action.

This novel analgesic, tapentadol is an attractive treatment option for the relief of
moderate-to-severe acute pain, acute postoperative pain, osteoarthritis pain
and/or low back pain.

Thiocolchicoside, a semi-synthetic derivative of the naturally occurring compound

colchicoside. It is highly effective and better alternative muscle relaxant agent
with anti-inflammatory and analgesic actions. It is also used topically for the
treatment of muscular spasms and for rheumatologic, orthopedic, and
traumatologic disorders.

Therefore, the combination of tapentadol and thiocolchicoside is better

alternative for the treatment option of pain and inflammation associated with
muscular spasm of any etiology because efficacy and safety goes hand-in-hand
with tapentadol.

REFERRENCE

• Efficacy of thiocolchicoside in Indian patients suffering from low back pain associated
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the relief of moderate-to-severe acute pain. Hartrick CT. Anesthesiology Research,
William Beaumont Hospital, Department of Anesthesiology, 3601 W. 13 Mile Rd., Royal
Oak, MI 48073, USA. chartrick@beaumont.edu
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metabolite in healthy humans. Trellu M, Filali-Ansary A, Françon D, Adam R, Lluel P,
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mechanisms of action in a single molecule. Tzschentke TM, Jahnel U, Kogel B, Christoph
T, Englberger W, De Vry J, Schiene K, Okamoto A, Upmalis D, Weber H, Lange C,
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in: Drugs Today (Barc). 2009 Sep;45(9):711.
• Tolerability of tapentadol immediate release in patients with lower back pain or
osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study. Hale M,
Upmalis D, Okamoto A, Lange C, Rauschkolb C.Curr Med Res Opin. 2009
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