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Ketorolac

产品号 DB00465 公司名称 DrugBank
CAS号 66635-83-4 公司网站 http://www.ualberta.ca/
分子式 C15H13NO3 电 话 (780) 492-3111
分子量 255.26862 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 348

产品价格信息

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产品别名

标题
Ketorolac
IUPAC标准名
5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
IUPAC传统名
ketorolac
商标名
Acular Preservative Free
Acular
Toradol
Acular LS
别名
Ketorolaco [Spanish]
Ketorolacum [Latin]
Ketoralac
Ketorolac Tromethamine

产品登记号

PubChem CID 3826
CAS号 66635-83-4
PubChem SID 46507019

产品性质

疏水性(logP) 2.1
溶解度 25 mg/mL (tromethamine salt)

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)
Indication For the short-term (~5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting.
Pharmacology Ketorolac, an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain. It is a peripherally acting analgesic. The biological activity of ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine possesses no sedative or anxiolytic properties.
Toxicity LD50 = 189 mg/kg (rat, oral).
Affected Organisms
Humans and other mammals
Biotransformation Primarily hepatic. Less than 50% of a dose is metabolized. The major metabolites are a glucuronide conjugate, which may also be formed in the kidney, and p-hydroxy ketorolac. Neither metabolite has significant analgesic activity.
Absorption Rapidly and completely absorbed after oral administration
Half Life 2.5 hours for the S-enantiomer compared with 5 hours for the R-enantiomer
Protein Binding 99%
Elimination The principal route of elimination of ketorolac and its metabolites is renal. Approximately 6% of a dose is excreted in the feces.
Distribution * 0.26 ± 0.08 L/kg [children 4 to 8 years old]
Clearance * 0.042 +/- 0.01 L/hr/kg [Pediatric Patients]
* 0.02 L/h/kg [Normal Subjects IM]
* 0.03 L/h/kg [Normal Subjects oral]
* 0.02 L/h/kg [Healthy Elderly Subjects IM]
* 0.02 L/h/kg [Healthy Elderly Subjects oral]
* 0.03 L/h/kg [Patients with Hepatic Dysfunction IM]
* 0.03 L/h/kg [Patients with Hepatic Dysfunction oral]
* 0.02 L/h/kg [Patients with Renal Impairment IM]
* 0.02 L/h/kg [Patients with Renal Impairment oral]
* 0.02 L/h/kg [Renal Dialysis Patients IM]
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

参考文献