エトドラク
WordNet
- a nonsteroidal anti-inflammatory drug (trade name Lodine) (同)Lodine
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/09/20 04:03:58」(JST)
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Etodolac
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| Systematic (IUPAC) name |
|
(RS)-2-(1,8-Diethyl-4,9-dihydro-3H-pyrano[3,4-b]indol-1-yl)acetic acid
|
| Clinical data |
| AHFS/Drugs.com |
monograph |
| MedlinePlus |
a692015 |
Pregnancy
category |
|
| Legal status |
- AU: Prescription Only (S4)
- UK: Prescription-only (POM)
- US: ℞-only
|
Routes of
administration |
oral |
| Pharmacokinetic data |
| Protein binding |
100% |
| Metabolism |
liver |
| Biological half-life |
7.3 ± 4.0 hours |
| Excretion |
renal |
| Identifiers |
| CAS Registry Number |
41340-25-4 Y |
| ATC code |
M01AB08 |
| PubChem |
CID: 3308 |
| IUPHAR/BPS |
7185 |
| DrugBank |
DB00749 Y |
| ChemSpider |
3192 Y |
| UNII |
2M36281008 Y |
| KEGG |
D00315 Y |
| ChEBI |
CHEBI:4909 Y |
| ChEMBL |
CHEMBL622 Y |
| Chemical data |
| Formula |
C17H21NO3 |
| Molecular mass |
287.35 g/mol |
SMILES
-
O=C(O)CC3(OCCc2c3nc1c(cccc12)CC)CC
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InChI
-
InChI=1S/C17H21NO3/c1-3-11-6-5-7-12-13-8-9-21-17(4-2,10-14(19)20)16(13)18-15(11)12/h5-7,18H,3-4,8-10H2,1-2H3,(H,19,20) Y
-
Key:NNYBQONXHNTVIJ-UHFFFAOYSA-N Y
|
| Physical data |
| Melting point |
145 to 148 °C (293 to 298 °F) |
| Solubility in water |
3.92e-02 mg/mL [ALOGPS] mg/mL (20 °C) |
| Y (what is this?) (verify) |
Generic brand of etodolac
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) approved by the U.S. Food and Drug Administration in January 1991.[1]
Contents
- 1 Action
- 2 Indications
- 3 Interactions
- 4 Pregnancy and nursing
- 5 Brand names
- 6 References
- 7 External links
Action
Main article: NSAIDs
NSAIDs are used for the management of mild to moderate pain, fever, and inflammation. They work by reducing the levels of prostaglandins, which are chemicals that are responsible for pain and the fever and tenderness that occur with inflammation. Etodolac blocks the cyclooxygenase (abbrev. COX) enzymes which form prostanoids, resulting in lower concentrations of prostaglandins. As a consequence, inflammation, pain and fever are reduced.
Post-marketing studies demonstrated that etodolac inhibition of cyclooxygenase is somewhat COX-2 selective [2] similar to celecoxib and other "COX-2 inhibitors." Unlike rofecoxib, both etodolac and celecoxib can fully inhibit COX-1 and are designated as having "preferential selectivity" toward COX-2. The R-enantiomer of etodolac is inactive against COX enzymes, but inhibits beta-catenin levels in hepatoma cells.[3]
Indications
Etodolac is licensed for the treatment of inflammation and pain caused by osteoarthritis and rheumatoid arthritis.[4]
Interactions
Etodolac should be avoided by patients with a history of asthma attacks, hives, or other allergic reactions to aspirin or other NSAIDs. Rare but severe allergic reactions have been reported in such individuals. It also should be avoided by patients with peptic ulcer disease or poor kidney function, since this medication can worsen both conditions. Etodolac is used with caution in patients taking blood thinning medications (anticoagulants), such as warfarin (Coumadin), because it increases the risk of bleeding. Patients taking both lithium and etodolac may develop toxic blood lithium levels. Additionally, etodolac has been found to interact with certain anti-depressant medications, such as sertraline or fluoxetine, which can increase risks of stroke, heart attack, and other cardiovascular conditions. Patients also taking ciclosporin (Sandimmune) can develop kidney toxicity. Use in children has not been adequately studied. Etodolac is not habit-forming. NSAIDs should be discontinued prior to elective surgery because of a mild interference with clotting that is characteristic of this group of medicines. Etodolac is best discontinued at least four days in advance of surgery.
Box, strip and tablet of etodolac (Lodine SR) 600mg
Pregnancy and nursing
Etodolac is generally avoided during pregnancy and nursing. NSAIDs may cause adverse cardiovascular effects in the fetus during pregnancy. [1]
Brand names
Etodolac is manufactured by Almirall Limited under the trade name Lodine SR[5] and by Meda Pharmaceuticals under the name Eccoxolac.[6] Non-proprietary etodolac is also available [7]
The drug is also sold under several other brand names, including:
- Etova (India)
- Dualgan (Portugal)
- Etodin (South Korea)
- Etofree (India)
- Etopan (Israel)
- Flancox®[8] (Brazil)
- Haipen (Japan)
- Lodine (France, Switzerland)
- Proxym (S Etodolac) (India)
- Etol (Turkey)
- Lonine (Taiwan)
- Etodine (Egypt)
References
- ^ a b http://www.medicinenet.com/etodolac/article.htm
- ^ http://www.pnas.org/content/96/13/7563.short
- ^ Behari, J; Zeng, G; Otruba, W; Thompson, MD; Muller, P; Micsenyi, A; Sekhon, SS; Leoni, L; Monga, SP (2007). "R-Etodolac Decreases Beta-Catenin Levels Along with Survival and Proliferation of Hepatoma Cells". Journal of hepatology 46 (5): 849–57. doi:10.1016/j.jhep.2006.11.017. PMC 1924913. PMID 17275129.
- ^ BNF 55 - Etodolac
- ^ Summary of Product Characteristics Lodine SR
- ^ Summary of Product Characteristics Eccoxolac
- ^ BNF 55: Etodolac preparations
- ^ http://www.apsen.com.br/bula.php?id_bula=5
External links
|
Wikimedia Commons has media related to Etodolac. |
- DrugBank info
- Medicinenet.com
|
Prostanoid signaling
|
|
Receptor
(ligands) |
|
|
Enzyme
(inhibitors) |
| Cyclooxygenase |
|
|
| PGD2 synthase |
- Retinoids
- Selenium (selenium tetrachloride, sodium selenite, selenium disulfide)
|
|
| PGE synthase |
HQL-79
|
|
| PGF synthase |
Bimatoprost
|
|
| PGI2 synthase |
Tranylcypromine
|
|
| TXA synthase |
- Camonagrel
- Dazmegrel
- Dazoxiben
- Furegrelate
- Isbogrel
- Midazogrel
- Nafagrel
- Nicogrelate
- Ozagrel
- Picotamide
- Pirmagrel
- Ridogrel
- Rolafagrel
- Samixogrel
- Terbogrel
- U63557A
|
|
|
| Others |
- Precursors: Linoleic acid
- γ-Linolenic acid (gamolenic acid)
- Dihomo-γ-linolenic acid
- Diacylglycerol
- Arachidonic acid
- Prostaglandin G2
- Prostaglandin H2
|
|
|
See also: Leukotrienergics
|
|
UpToDate Contents
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English Journal
- Water avoidance stress induces frequency through cyclooxygenase-2 expression: A bladder rat model.
- Yamamoto K, Takao T, Nakayama J, Kiuchi H, Okuda H, Fukuhara S, Yoshioka I, Matsuoka Y, Miyagawa Y, Tsujimura A, Nonomura N.SourceDepartment of Urology, Osaka University Graduate School of Medicine, Suita, Osaka, Japan.
- International journal of urology : official journal of the Japanese Urological Association.Int J Urol.2012 Feb;19(2):155-62. doi: 10.1111/j.1442-2042.2011.02905.x. Epub 2011 Dec 5.
- Objectives: Water avoidance stress is a potent psychological stressor and it is associated with visceral hyperalgesia, which shows degeneration of the urothelial layer mimicking interstitial cystitis. Cyclooxygenase-2 inhibitors have been recognized to ameliorate frequency both in clinical and ex
- PMID 22142485
- A comparison of the therapeutic efficacy of diclofenac in osteoarthritis: a systematic review of randomised controlled trials.
- Pavelka K.SourceInstitute of Rheumatology and Clinic of Rheumatology, Charles University , Prague , Czech Republic.
- Current medical research and opinion.Curr Med Res Opin.2012 Jan;28(1):163-78.
- Abstract Objective: Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) commonly prescribed for pain relief in osteoarthritis (OA). The relative efficacy of diclofenac compared to other pain relief medications used in OA (e.g., alternative NSAIDs, cyclooxygenase type 2 [COX-2] inhibitor
- PMID 22168216
- Impact of the counterion on the solubility and physicochemical properties of salts of carboxylic acid drugs.
- David SE, Timmins P, Conway BR.SourceFormulation Process and Analysis, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex.
- Drug development and industrial pharmacy.Drug Dev Ind Pharm.2012 Jan;38(1):93-103.
- AIM: Salt formation is a widely used approach to improve the physicochemical and solid state properties of an active pharmaceutical ingredient. In order to better understand the relationships between the active drug, the selected counterion and the resultant salt form, crystalline salts were formed
- PMID 22118222
Japanese Journal
- Efficacy and Safety of Celecoxib Compared with Placebo and Etodolac for Acute Postoperative Pain: A Multicenter, Double-Blind, Randomized, Parallel-Group, Controlled Trail
- ITO MASANORI,OKADA TOSHIYUKI,HANAOKA AKIO,ISHIGURO NAOKI
- Nagoya Journal of Medical Science 77(1-2), 81-93, 2015-02
- NAID 120005549554
- フェンタニルとアモキサピンの併用によりセロトニン症候群を発症したがん性疼痛患者の1例
- 下山 恵美,松岡 鐘文
- Palliative Care Research 10(2), 501-504, 2015
- 【緒言】セロトニン症候群はセロトニン性神経伝達を亢進させる複数の薬剤の相乗作用で惹起されることが多い.フェンタニルとアモキサピンを併用投与し，本症候群を発症した症例を経験した.【症例】37歳女性，子宮頸がんの再発による臀部痛に対し，オキシコドン徐放錠とエトドラクを投与していたが，胃穿孔のため緊急開腹術を施行した.術中よりフェンタニル持続投与を開始し，術後も継続した.翌日よりフェンタニルパッチに変更 …
- NAID 130004943672
- Bitterness Evaluation of Acidic Pharmaceutical Substances (NSAIDs) Using a Taste Sensor
- , ,
- Chemical and Pharmaceutical Bulletin 62(12), 1252-1258, 2014
- … The 'Change in membrane Potential caused by Adsorption' (CPA) of sodium diclofenac and etodolac were also determined in the presence of increasing concentrations of tartaric acid using membrane C00. … There were concentration-dependent changes in the bitterness intensities of diclofenac sodium and etodolac without any change in their sourness intensities. …
- NAID 130004712920
Related Links
- Etodolac comes as a tablet, a capsule, and an extended-release tablet to take by mouth. To treat arthritis, the tablet and capsule are usually taken two to three times a day and the extended-release tablet is usually ...
- エトドラク(Etodolac)の検索ならお薬検索QLife（キューライフ）。お医者さんが処方する処方薬と、薬局で買える市販薬(OTC)、の効果と副作用、写真、添付文書、保管方法等を掲載。商品名だけでなく一般名や剤形、色などからも検索可能。
★リンクテーブル★
[★]
- 英
- etodolac
- 同
- エトドリン酸 etodolic acid
- 商
- オステラック、ハイペン、オスペイン、ニコナス、パイペラック、ライペック
- 関
- NSAID