Description
PHARMACOLOGY
PHARMACODYNAMICS OF THIOCOLCHICOSIDE
Mechanism of Action: – Thiocolchicide is a GABA-A receptor antagonist, which binds to GABA-A and strychnine sensitive glycine receptors. This results the reduction of spasticity. It also has myorelaxant effects at the supraspinal level, via complex regulatory mechanisms.
PHARMACODYNAMICS OF ACECLOFENAC
Mechanism of Action: – It inhibits cyclo-oxygenase (COX) activity and to suppress the PGE2 production by inflammatory cells, by inhibiting IL-Beta & TNF in the inflammatory cells (Intracellular Action).
It blocks degeneration and stimulates synthesis of extra cellular matrix of cartilages by inhibiting the action of different cytokines.
Drug and its metabolites inhibit IL-6 production by human chondrocytes. This leads to inhibition of increase of inflammatory cells in synovial tissue, inhibition of IL-1 amplification, inhibition of increased MMP synthesis and thus ensuring proteoglycan production.
It inhibits IL-1 and TNF production by human chondrocytes, inflammatory cells and synovial cells and therefore blocks suppression of GAG and collagen synthesis and stimulates growth factors mediated synthesis of GAG and collagen.
4`-hydroxyaceclofenac a metabolite of aceclofenac inhibits pro MMP1 and pro MMP3 produced by synovial cells (Rheumatoid Synovial Cells) in serum and in synovial fluid and thus inhibits progressive joint destruction by MMPs.
Aceclofenac inhibits Neutrophil Adhesion & Accumulation at the inflammatory site in the early phase and thus blocks the pro-inflammatory actions of Neutrophils.
Aceclofenac is also an NSAID with greater COX-2 specificity.
PHARMACOKINETICS OF ACECLOFENAC
- Absorption- It is rapidly and completely absorbed after oral administration
- Distribution- Widely distributed in the body as protein-bound form. It is highly protein-bound (>99.7%). Aceclofenac penetrates into the synovial fluid, where the concentrations reach approximately 60% of those in plasma.
- Metabolism- Metabolized into metabolites in the liver. Main metabolite is 4-hydroxyaceclofenac
- Excretion- It is excreted through urine mainly as conjugated hydroxymetabolites
INDICATIONS:
THIOCOLCHICOSIDE
- Degenerative vertebral disorders
- Torticollis
- Dorsal pain
- Low back pain
- Traumatological disorders
- Neurological disorders
ACECLOFENAC
- Ankylosing spondylitis
- Osteoarthritis
- Symptomatic treatment of pain and inflammation in Post-Traumatic pain
- Cervical pain
- Low back pain
- Acute gout
