|
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 11e
| IV. Autacoids: Drug Therapy of Inflammation > |
Acetic Acid Derivatives: Indomethacin, Sulindac, and Etodolac
Sections: Acetic Acid
Derivatives: Indomethacin, Sulindac, and Etodolac, Indomethacin, Chemistry, Pharmacological
Properties, Pharmacokinetics
and Metabolism, Drug Interactions, Therapeutic
Uses, Common Adverse
Effects, Sulindac, Chemistry, Pharmacological
Properties, Pharmacokinetics
and Metabolism, Therapeutic
Uses, Common Adverse
Effects, Etodolac, Pharmacokinetics
and Metabolism, Therapeutic
Uses, Common Adverse
Effects.
Topics Discussed: ankylosing spondylitis; anti-inflammatory agents, non-steroidal; etodolac; indomethacin; osteoarthritis; patent ductus arteriosus; sulindac.
Excerpt:
"Indomethacin was the product of a laboratory search for drugs
with antiinflammatory properties. It was introduced in 1963 for
the treatment of rheumatoid arthritis and related disorders. It
is a nonselective COX inhibitor. Although indomethacin still is
used clinically and is effective, toxicity and the availability
of safer alternatives have limited its use. Sulindac was developed
in an attempt to find a less toxic, but effective, congener of indomethacin
and also is a nonselective COX inhibitor. The pharmacology of both
drugs has been reviewed (Rainsford, 2003; Haanen,
2001).
Etodolac
is a structurally
related tNSAID; it has been found to be a somewhat selective inhibitor
of COX-2.The structural formula of indomethacin, a methylated
indole derivative, is:Sulindac is related closely to indomethacin; its structural
formula is:Etodolac is rapidly and well absorbed orally. It is
highly bound to plasma protein and undergoes hepatic metabolism
and renal excretion (Table 26–1).
The drug may undergo enterohepatic circulation in humans; its half-life
in plasma is about 7 hours...."
The content above is only an excerpt.
For full access, log into an existing user account below, purchase an annual subscription, or purchase a short-term subscription to the complete website.
|
|
|
|
|