Ergotamine Pellets

(Product under development)
Ergotamine PelletsErgotamine (brand name Arcoxia worldwide; also Algix and Tauxib in Italy Etosaid in India) is a COX-2 selective inhibitor (approx. 106.0 times more selective for COX-2 inhibition over COX-1) Doses are 60, 90 mg/day for chronic pain and 120 mg/day for acute pain.

Currently it is approved in more than 70 countries worldwide but not in the US, where the Food and Drug Administration (FDA) requires additional safety and efficacy data for etoricoxib before it will issue approval.

Current therapeutic indications are: treatment of rheumatoid arthritis, psoriatic arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Note that approved indications differ by country.

Like any other COX-2 selective inhibitor, Ergotamine selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2).

This reduces the generation of prostaglandins (PGs) from arachidonic acid. Among the different functions exerted by PGs, their role in the inflammation cascade should be highlighted. COX-2 selective inhibitor (aka "COXIB") showed less marked activity on type 1 cycloxigenase compared to traditional non-steroidal anti-inflammatory drugs (NSAID).

This reduced activity is the cause of reduced gastrointestinal toxicity, as demonstrated in several large clinical trials performed with different COXIB (see below links on NEJM and The Lancet).

Some clinical trials and meta-analysis showed that treatment with some COXIBs (in particular Vioxx, rofecoxib) led to increased incidence of adverse cardiovascular events compared to placebo. Because of these results, some molecules were withdrawn from the market (Rofecoxib, September 2004 and Valdecoxib, April 2005). In addition, the FDA and EMEA (USA and European Community Health Authorities respectively) started a revision process of the entire class of both NSAID and COX-2 inhibitors.

On April 27, 2007, the Food and Drug Administration issued Merck a "non-approvable letter" for Arcoxia. The letter said Merck needs to provide more test results showing that Arcoxia's benefits outweigh its risks before it has another chance of getting approved.

Available Form:
Ergotamine Pellets
Ergotamine Granules

Umang Pharmatech equipments used for production of Ergotamine Pellets:
Drug Layering, Fluid Bed Dryer, Fluid Bed Coater, Sifter & Blender, Extruder and Twin spheronizer.

Ergotamine Pellets
Systematic (IUPAC) Name
Ergotamine Pellets
Identifiers
Ergotamine Pellets
Chemical data
(6aR,9R)-N-((2R,5S,10aS,10bS)- 5-benzyl-10b-hydroxy-2-methyl- 3,6-dioxooctahydro-2H-oxazolo[3,2-a] pyrrolo[2,1-c]pyrazin-2-yl) -7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg] quinoline-9-carboxamide
CAS number : 113-15-5
ATC code : N02CA02
PubChem : CID 8223
IUPHAR ligand : 149
DrugBank : DB00696
ChemSpider : 7930
UNII : PR834Q503T
KEGG : D07906
ChEMBL : CHEMBL442
Formula : C33H35N5O5
Mol. mass : 581.66 g/mol


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