 |
|
| |
|
||||
Missing image Indomethacin.png Indomethacin is an indole derived non-steroidal anti-inflammatory drug. Indomethacin (also indometacin) is a non-steroidal anti-inflammatory drug commonly used to reduce fever, pain, stiffness, and swelling. It works by inhibiting the production of prostaglandins, molecules known to cause these symptoms. It is marketed under many trade names, including Indocin, Indocid, Indochron E-R, and Indocin-SR.
IndicationsClinical indications for indomethacin include:
Indomethacin has also been used clinically to delay premature labor, reduce amniotic fluid in polyhydramnios, and to treat patent ductus arteriosus. Mechanism of actionMain article: Non-steroidal anti-inflammatory drug Indomethacin is a nonselective inhibitor of cyclooxygenase (COX) 1 and 2, enzymes that participate in prostaglandin synthesis from arachidonic acid. Prostaglandins are hormone-like molecules normally found in the body, where they have a wide variety of effects, some of which lead to pain, fever, and inflammation. Prostaglandins also cause uterine contractions in pregnant women. Indomethacin is an effective tocolytic agent, able to delay premature labor by reducing uterine contractions through inhibition of PG synthesis in the uterus and possibly through calcium channel blockade. Indomethacin easily crosses the placenta, and can reduce fetal urine production to treat polyhydramnios. It does so by reducing renal blood flow and increasing renal vascular resistance, possibly by enhancing the effects of vasopressin on the fetal kidneys. Adverse effectsMain article: Non-steroidal anti-inflammatory drug Since indomethacin inhibits both COX-1 and COX-2, it inhibits the production of prostaglandins in the stomach and intestines which maintain the mucous lining of the gastrointestinal tract. Indomethacin, therefore, like other nonselective COX inhibitors, can cause ulcers. To reduce the possibility of peptic ulcers, indomethacin should be prescribed at the lowest dosage needed to achieve a therapeutic effect, usually between 50–200 mg/day. It should always be taken after a meal. Many NSAIDs, but particularly indomethacin, cause lithium retention by reducing its excretion by the kidneys. Thus indomethacin users have an elevated risk of lithium toxicity. For patients taking lithium supplements (e.g. for treatment of depression or bipolar disorder), less toxic NSAIDs such as sulindac or aspirin, are preferred. Indomethacin also reduces plasma renin activity and aldosterone levels, and increases sodium and potassium retention. It also enhances the effects of vasopressin. Together these may lead to:
Chemical propertiesIndomethacin is a methylated indole derivative and a member of the arylalkanoic acid class of NSAIDs. Its chemical formula is C19H16ClNO4 and its chemical name is 1-(4-chlorobenzoyl)-5-methoxy- 2-methyl-1-H-indole-3-acetic acid. It is slightly soluble in alcohol and even less so in water. Its pKa is 4.5 and it has a molecular weight of 357.79. HistoryIndomethacin was discovered in 1963 and it was first approved for use in the U.S. by the Food and Drug Administration in 1965. Its mechanism of action, along with several other NSAIDs that inhibit COX, was described in 1971. References
External links
|
||||||||||||
|
|
||||||||||||
|
|
|
|
Copyright 2008 WordIQ.com - Privacy Policy
::
Terms of Use
:: Contact Us
:: About Us This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Indomethacin". |