Пироксикам химические свойства, назначение, производство
Описание
Piroxieam is a non-steroidal anti-inflammatory drug, of
the oxieam class. A contact and photocontact sensitizer,
which induced contact dermatitis in a physieal
therapist. Piroxieam generally cross reacts with thiosalicylic
acid and also with thiomersal. Cross sensitivity
is not observed to tenoxicam.
Химические свойства
Off-White to Pale Yellow Solid
Использование
Piroxicam is
used in inflammatory and degenerative diseases of the musculoskeletal system that are
accompanied by painful symptoms. It is used for rheumatic heart disease, nonspecific
infectious polyarthritis, gouty arthritis, rheumatoid arthritis, osteoarthritis, ankylosing
spondylitis, arthrosis, back pain, neuralgia, myalgia, and other diseases associated with
inflammation.
Определение
ChEBI: A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide with the exocyclic nitrogen of 2-aminopyridine.
Показания
Piroxicam
(Feldene) is indicated for the treatment of rheumatoid
arthritis and osteoarthritis. Piroxicam is a nonspecific
COX inhibitor that has a much higher affinity for
COX-1 than COX-2. This may account for the large
proportion (over 30%) of patients receiving long-term
therapy who have reported side effects.Adverse GI reactions
have been the most frequently reported side effect,
but edema, dizziness, headache, rash, and changes
in hematological parameters have also occurred in 1 to
6% of patients. Piroxicam can cause serious GI bleeding,
ulceration, and perforation, particularly in the elderly, if
the recommended dosage is exceeded or if aspirin is being
taken concurrently.
Общее описание
Piroxicam (Feldene) is the most widely used oxicam becauseof its once-daily dosing schedule. It is well absorbedafter oral administration and has a plasma half-life of 50hours, thus requiring a dose of only 20 to 30 mg oncedaily. It undergoes extensive hepatic metabolism, catalyzedby CYP2C9 to give 5-hydroxypiroxicam as its majormetabolite. Several piroxicam prodrugshave been synthesized via derivatization of the enol alcoholgroup (amipiroxicam, droxicam, and pivoxicam) to reducepiroxicam-induced GI irritation.
Биологическая активность
Anti-inflammatory; highly selective inhibitor of COX-1 (ratio of IC 50 values for COX-2/COX-1 ~ 600).
Пироксикам препаратная продукция и сырье
сырьё
препарат