Tìm theo
Ketorolac
Các tên gọi khác (7 ) :
  • (+-)-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
  • (+-)-Ketorolac
  • Ketorolac
  • Kétorolac
  • Ketorolaco
  • Ketorolacum
  • rac-Ketorolac
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 66635-83-4
ATC: M01AB15, S01BC05
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C15H13NO3
PTK: 255.2686
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)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H13NO3
Phân tử khối
255.2686
Monoisotopic mass
255.089543287
InChI
InChI=1S/C15H13NO3/c17-14(10-4-2-1-3-5-10)13-7-6-12-11(15(18)19)8-9-16(12)13/h1-7,11H,8-9H2,(H,18,19)
InChI Key
InChIKey=OZWKMVRBQXNZKK-UHFFFAOYSA-N
IUPAC Name
5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
Traditional IUPAC Name
ketorolac
SMILES
OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1
Độ tan chảy
165-167 °C (tromethamine salt)
Độ hòa tan
25 mg/mL (tromethamine salt)
logP
2.1
logS
-2.7
pKa (strongest acidic)
3.84
pKa (Strongest Basic)
-7.8
PSA
59.3 Å2
Refractivity
70.19 m3·mol-1
Polarizability
26.67 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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) Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to indomethacin and tolmetin. Ketorolac tromethamine is a racemic mixture of [-]S- and [+]R-enantiomeric forms, with the S-form having analgesic activity. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis leading to decreased formation of precursors of prostaglandins and thromboxanes from arachidonic acid. The resultant reduction in prostaglandin synthesis and activity may be at least partially responsible for many of the adverse, as well as the therapeutic, effects of these medications. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity. However, inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation may also contribute to the analgesic effect. In terms of the ophthalmic applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels in aqueous humor, secondary to inhibition of prostaglandin biosynthesis.
Dược Động Học :
▧ Absorption :
Rapidly and completely absorbed after oral administration
▧ Volume of Distribution :
* 0.26 ± 0.08 L/kg [children 4 to 8 years old]
▧ Protein binding :
99%
▧ Metabolism :
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.
▧ Route of Elimination :
The principal route of elimination of ketorolac and its metabolites is renal. Approximately 6% of a dose is excreted in the feces.
▧ Half Life :
2.5 hours for the S-enantiomer compared with 5 hours for the R-enantiomer
▧ 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]
Độc Tính : LD50 = 189 mg/kg (rat, oral).
Chỉ Định : For the short-term (~5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting.
Tương Tác Thuốc :
  • Acenocoumarol The NSAID, ketorolac, may increase the anticoagulant effect of acenocoumarol.
  • Acetylsalicylic acid Acetylsalicylic acid may increase the adverse GI effects ketorolac.
  • Alendronate Increased risk of gasrtic toxicity
  • Anisindione The NSAID, ketorolac, may increase the anticoagulant effect of anisindione.
  • Azilsartan medoxomil Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Colesevelam Bile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
  • Dicoumarol The NSAID, ketorolac, may increase the anticoagulant effect of dicumarol.
  • Difluprednate NSAIDs may slow healing.
  • Eltrombopag Increases levels of Ketorolac via metabolism decrease. UDP-glucuronosyltransferase inhibition with unclear significance.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Ketoprofen Concomitant use of ketoprofen and ketorolac, two NSAIDs, is contraindicated due to the risk of additive or synergistic NSAID toxicities (e.g. GI bleeding, ulceration, renal dysfunction, etc).
  • Lithium The NSAID, ketorolac, may decrease the renal excretion of lithium. Increased risk of lithium toxicity.
  • Methotrexate The NSAID, ketorolac, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
  • Probenecid Probenecid increases toxicity of ketorolac
  • Sulindac May cause additive or synergistic NSAID toxicities (e.g. GI bleeding, renal dysfunction, etc.). Concomitant therapy is contraindicated.
  • Telmisartan Concomitant use of Telmisartan and Ketorolac may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
  • Tiaprofenic acid Concomitant therapy is contraindicated due to the risk of synergistic NSAID toxicity.
  • Timolol The NSAID, Ketorolac, may antagonize the antihypertensive effect of Timolol.
  • Tolmetin Risk of adverse NSAID toxic effects (e.g. GI bleeding, renal dysfunction). Concomitant therapy is contraindicated.
  • Trandolapril The NSAID, Ketorolac, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Ketorolac is initiated, discontinued or dose changed.
  • Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketorolac. Monitor for increased bleeding during concomitant thearpy.
  • Vilazodone Increased risk of bleeding with concomitant use of vilazodone and ketorolac
  • Warfarin The antiplatelet effects of ketorolac may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Solution - Intramuscular
Solution - Ophthalmic
Tablet - Oral
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00465
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3826
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507019
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07062
ChemSpider
http://www.chemspider.com/Chemical-Structure.3694.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50009855
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/68387-440-20
PharmGKB
http://www.pharmgkb.org/drug/PA450150
Wikipedia
http://en.wikipedia.org/wiki/Ketorolac
RxList
http://www.rxlist.com/cgi/generic/ketor.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/acu1644.shtml
Drugs.com
http://www.drugs.com/cdi/ketorolac-drops.html
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