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IMAGE 2010-11 ISSN: 2229-5658 Vol No: 11 ISSUE No: 4 47
SYNERGISTIC COMBINATION OF ACECLOFENAC AND
THIOCOLCHICOSIDE
An advanced and modern treatment modality.
Dr.Shilpa Burundy
ABSTRACT
Dental surgeons encounter many muscular disorders in their clinical practice. Trismus, Dry socket, TMJ
disorders, Neuro Muscular conditions, etc need fixed dose combination of NSAID and muscle relaxants.
This article presents a synergistic combination of Aceclofenac and Thiocolchicoside- an advanced and
modern treatment for the above said conditions.
CLINICAL PHARMACOLOGY
Pharmacodynamics
Aceclofenac
Aceclofenac is a non-steroidal agent with
marked anti-inflammatory and analgesic
properties.
The mode of action of aceclofenac is largely
based on the inhibition of prostagiandin
synthesis. Aceclofenac is a potent inhibitor of
the enzyme cyclo-oxygenase, which is involved
in the production of prostaglandins.
Thiocolchicoside
In-vitro thicolchicoside only binds to GASA-A
and strychnino sensitive glycine
receptors. Thicolchicoside act as a GABA-A
receptor antagonist, its myorelaxant effects
could be exerted at the supraspinal level, via
complex regulatory mechanisms, although a
glycinergic mechanism of action cannot be
excluded. The characteristics of the interaction
of thiocolchicoside with GABA-A receptors are
quaitatively and quantitatively shared by its
main circulating metabolite, glucuronidated
derivative.
In vivo, the myorelaxant properties of
thiocolchicoside and its main metabolite have
been demonstrated in various predictive models.
The lack of myorelaxant effect of
thiocokhicoside in spinalized rats suggests a
predominant supraspinal action for this
compound. Thiocolchicoside was also found to
possess anti-inflammatory and analgesic
activities in a variety of experimental models
after oral, subcutaneous, intraperitoneal and
intramuscular administration.
Pharmacokinetics
Aceclofenac
CLINICAL PHARMACOLOGY
After oral administration, aceclofenac is rapidly
absorbed and the bioavailability is almost 100%.
Peak concentrations are reached approximately
1.25 to 3 hours following ingestion. Time is
delayed with concomitant food intake whereas
the degree of absorption is not influenced.
Aceclofenac is highly protein-bound (99.7%).
Aceclofenac penetrates into the synovial fluid
where the concentrations reach
approximately 60% of those in plasma. the
volume of distribution is approximately 30L.
Aceclofenac is probably metabolized via
CYP2C9 to the main metabolite
4-hydroxyaceclofenac. The mean plasma
elimination half-life is 4-4,3 hours.
Approximately two-thirds of the administered
dose is excreted via the urine mainly as
conjugated hydroxymetabolites. Only 1% of an
oral single dose is excreted unchanged. A slower
rate of elimination of aceclofencac has been
detected in patients with
decreased liver function after a single dose of
aceclofenac. In a multiple dose study using
100mg once daily, there was no difference in the
pharmacokinetic parameters between subjects
with mild to moderate liver cirrhosis and normal
subjects. In
patients with mild to moderate renal impairment,
no clinically significant differences inn the
pharmacokinetics were observed after a single
dose.
Thiocolchicoside
Thiocoichicoside is rapidly absorbed after oral
administration, and metabolized into 3 main
metabolites. The two main circulating forms
were the thiocolchicoside
aglycon and the glucuronidated derivative of
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The International Journal of Indian Dental Association, Kunnamkulam Branch. Indexed in Journals Master List of IC TM