Peringatan Keamanan

The rate of adverse effects increases with higher doses of ketorolac. The most frequently observed adverse effects in patients occurring with an incidence of greater than 10% include: abdominal pain, dyspepsia, nausea, and headaches.L11055 Most adverse effects associated with short term use are mild in nature, related to the gastrointestinal tract and nervous system, and occur in roughly 39% of patients.A176131 Common symptoms of ketorolac overdose include nausea, vomiting, epigastric pain, gastrointestinal bleeding, lethargy and drowsiness. More rare symptoms of overdose include acute renal failure, hypertension, respiratory depression, and coma.L3674

Ketorolac is classified as Pregnancy Category C since there is a lack of evidence demonstrating safety in pregnant women.L11070 NSAIDs including ketorolac increase the risk of premature closure of the fetal ductus arteriosus in the 3rd trimester; therefore, beginning at 30 weeks gestation, pregnant women should avoid ketorolac.L11070

Ketorolac has been shown to be excreted in breast milk, and although available data has not demonstrated any adverse effects in nursing infants, practitioners should proceed with caution when suggesting ketorolac for nursing mothers.L11055,L3674 The benefits should outweigh the risks and the mother should be counselled to monitor the infant closely and to contact the infant's healthcare provider should any adverse effects arise.L11055,L3674

Women who are trying to conceive are not advised to take ketorolac since it's effect on prostaglandin synthesis may impair fertility.L11055L11055

Ketorolac

DB00465

small molecule approved

Deskripsi

Ketorolac is a Non-steroidal anti-inflammatory drug (NSAID) and is commercially available as an oral tablet, injectable, nasal spray and as an ophthalmic solution.L6358L6508L11055L3674L11070

It's analgesic properties make it a useful pain management tool across many settings including postoperative pain, rheumatoid arthritis, osteoarthritis, menstrual disorders, headaches, spinal and soft tissue pain, and ankylosing spondylitis.L6520 Impressively, ketorolac has a similar efficacy to standard doses of morphine and meperidine making it a useful opioid sparing agent.L6511

Struktur Molekul 2D

Berat 255.2686
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ketorolac tromethamine is administered as a racemic mixture, therefore the half-life of each enantiomer must be considered. The half life of the S-enantiomer is ~2.5 hours, while the half life of the R-enantiomer is ~5 hours. Based on this data, the S enantiomer is cleared about twice as fast as the R enantiomer.[L3674]
Volume Distribusi The apparent volume of distribution of ketorolac in healthy human subjects is 0.25 L/kg or less.[A176143]
Klirens (Clearance) The plasma clearance of ketorolac is 0.021 to 0.037 L/h/kg.[A176143] Further, studies have illustrated that clearance of oral, IM and IV doses of ketorolac are comparable which suggests linear kinetics.[L3674] It should also be noted that clearance in children is about double the clearance found in adults. [A176231]

Absorpsi

Ketorolac is rapidly, and completely absorbed after oral administration with a bioavailability of 80% after oral administration.L3674L3674L3674A176143 Cmax is attained 20-60 minutes after administration, and after intramuscular administration, the area under the plasma concentration-time curve (AUC) is proportional to the dose administered.A175966 After intramuscular administration, ketorolac demonstrates a time to maximal plasma concentration (tmax) of approximately 45-50 minutes, and a tmax of 30-40 minutes after oral administration.A176143 The rate of absorption may be reduced by food; however, the extent of absorption remains unaffected.A176143

Metabolisme

Ketorolac is heavily metabolized via hydroxylation or conjugation in the liver; however, it appears that the key metabolic pathway is glucuronic acid conjugation.L3674,A176143 Enzymes involved in phase I metabolism include CYP2C8 and CYP2C9, while phase II metabolism is carried out by UDP-glucuronosyltransferase (UGT) 2B7.A176234

Rute Eliminasi

Ketorolac is primarily renally eliminated and approximately 92% of the dose can be recovered in the urine with 60% of this proportion recovered unchanged, and 40% recovered as metabolites. In addition 6% of a single dose is eliminated in the feces.L3674

Interaksi Makanan

1 Data
  • 1. Take with food. Food reduces GI irritation.

Interaksi Obat

1635 Data
Amlodipine The metabolism of Ketorolac can be decreased when combined with Amlodipine.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Ketorolac.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Ketorolac.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Ketorolac.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Ketorolac.
Ziprasidone The risk or severity of hypertension can be increased when Ziprasidone is combined with Ketorolac.
Methysergide The risk or severity of hypertension can be increased when Methysergide is combined with Ketorolac.
Cabergoline The risk or severity of hypertension can be increased when Cabergoline is combined with Ketorolac.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Ketorolac.
Dihydroergotamine The risk or severity of hypertension can be increased when Dihydroergotamine is combined with Ketorolac.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Ketorolac.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Ketorolac.
Mirtazapine The risk or severity of hypertension can be increased when Mirtazapine is combined with Ketorolac.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Ketorolac.
Promazine The risk or severity of hypertension can be increased when Promazine is combined with Ketorolac.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Ketorolac.
Doxapram The risk or severity of hypertension can be increased when Ketorolac is combined with Doxapram.
Atropine The risk or severity of hypertension can be increased when Ketorolac is combined with Atropine.
Lisuride The risk or severity of hypertension can be increased when Ketorolac is combined with Lisuride.
Linezolid The risk or severity of hypertension can be increased when Ketorolac is combined with Linezolid.
Metaraminol The risk or severity of hypertension can be increased when Ketorolac is combined with Metaraminol.
Furazolidone The risk or severity of hypertension can be increased when Ketorolac is combined with Furazolidone.
Thioridazine The risk or severity of hypertension can be increased when Ketorolac is combined with Thioridazine.
Ergotamine The risk or severity of hypertension can be increased when Ketorolac is combined with Ergotamine.
Nicergoline The risk or severity of hypertension can be increased when Ketorolac is combined with Nicergoline.
Sufentanil The risk or severity of hypertension can be increased when Ketorolac is combined with Sufentanil.
Methoxamine The risk or severity of hypertension can be increased when Ketorolac is combined with Methoxamine.
Risperidone The risk or severity of hypertension can be increased when Ketorolac is combined with Risperidone.
Isoflurane The risk or severity of hypertension can be increased when Ketorolac is combined with Isoflurane.
Propiomazine The risk or severity of hypertension can be increased when Ketorolac is combined with Propiomazine.
Alfentanil The risk or severity of hypertension can be increased when Ketorolac is combined with Alfentanil.
Minaprine The risk or severity of hypertension can be increased when Ketorolac is combined with Minaprine.
Orciprenaline The risk or severity of hypertension can be increased when Ketorolac is combined with Orciprenaline.
Phenmetrazine The risk or severity of hypertension can be increased when Ketorolac is combined with Phenmetrazine.
Trifluoperazine The risk or severity of hypertension can be increased when Ketorolac is combined with Trifluoperazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Ketorolac is combined with Pseudoephedrine.
Benzphetamine The risk or severity of hypertension can be increased when Ketorolac is combined with Benzphetamine.
Ritodrine The risk or severity of hypertension can be increased when Ketorolac is combined with Ritodrine.
Flupentixol The risk or severity of hypertension can be increased when Ketorolac is combined with Flupentixol.
Remifentanil The risk or severity of hypertension can be increased when Ketorolac is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Ketorolac is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Ketorolac is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Ketorolac is combined with Diethylpropion.
Naratriptan The risk or severity of hypertension can be increased when Ketorolac is combined with Naratriptan.
Formoterol The risk or severity of hypertension can be increased when Ketorolac is combined with Formoterol.
Frovatriptan The risk or severity of hypertension can be increased when Ketorolac is combined with Frovatriptan.
Methoxyflurane The risk or severity of hypertension can be increased when Ketorolac is combined with Methoxyflurane.
Ergoloid mesylate The risk or severity of hypertension can be increased when Ketorolac is combined with Ergoloid mesylate.
Isoprenaline The risk or severity of hypertension can be increased when Ketorolac is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Ketorolac is combined with Arbutamine.
Dutasteride The risk or severity of hypertension can be increased when Ketorolac is combined with Dutasteride.
Halothane The risk or severity of hypertension can be increased when Ketorolac is combined with Halothane.
Moclobemide The risk or severity of hypertension can be increased when Ketorolac is combined with Moclobemide.
Pergolide The risk or severity of hypertension can be increased when Ketorolac is combined with Pergolide.
Desflurane The risk or severity of hypertension can be increased when Ketorolac is combined with Desflurane.
Bromocriptine The risk or severity of hypertension can be increased when Ketorolac is combined with Bromocriptine.
Finasteride The risk or severity of hypertension can be increased when Ketorolac is combined with Finasteride.
Aripiprazole The risk or severity of hypertension can be increased when Ketorolac is combined with Aripiprazole.
Isocarboxazid The risk or severity of hypertension can be increased when Ketorolac is combined with Isocarboxazid.
Ergometrine The risk or severity of hypertension can be increased when Ketorolac is combined with Ergometrine.
Lisdexamfetamine The risk or severity of hypertension can be increased when Ketorolac is combined with Lisdexamfetamine.
Fenoterol The risk or severity of hypertension can be increased when Ketorolac is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Ketorolac is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Ketorolac is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Ketorolac is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Ketorolac is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Ketorolac is combined with Procaterol.
Yohimbine The risk or severity of hypertension can be increased when Ketorolac is combined with Yohimbine.
Methotrimeprazine The risk or severity of hypertension can be increased when Ketorolac is combined with Methotrimeprazine.
Clenbuterol The risk or severity of hypertension can be increased when Ketorolac is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Ketorolac is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Ketorolac is combined with MMDA.
Midomafetamine The risk or severity of hypertension can be increased when Ketorolac is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Ketorolac is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Ketorolac is combined with 4-Methoxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Ketorolac is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Ketorolac is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Ketorolac is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Ketorolac is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Ketorolac is combined with Phendimetrazine.
Solifenacin The risk or severity of hypertension can be increased when Ketorolac is combined with Solifenacin.
Periciazine The risk or severity of hypertension can be increased when Ketorolac is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Ketorolac is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Ketorolac is combined with Thioproperazine.
Zuclopenthixol The risk or severity of hypertension can be increased when Ketorolac is combined with Zuclopenthixol.
Epicaptopril The risk or severity of hypertension can be increased when Ketorolac is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Ketorolac is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Ketorolac is combined with 1-benzylimidazole.
Nialamide The risk or severity of hypertension can be increased when Ketorolac is combined with Nialamide.
Lysergic acid diethylamide The risk or severity of hypertension can be increased when Ketorolac is combined with Lysergic acid diethylamide.
Dronedarone The risk or severity of hypertension can be increased when Ketorolac is combined with Dronedarone.
Flibanserin The risk or severity of hypertension can be increased when Ketorolac is combined with Flibanserin.
Iloperidone The risk or severity of hypertension can be increased when Ketorolac is combined with Iloperidone.
Indacaterol The risk or severity of hypertension can be increased when Ketorolac is combined with Indacaterol.
Rotigotine The risk or severity of hypertension can be increased when Ketorolac is combined with Rotigotine.
Amibegron The risk or severity of hypertension can be increased when Ketorolac is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Ketorolac is combined with Naluzotan.
Cariprazine The risk or severity of hypertension can be increased when Ketorolac is combined with Cariprazine.
Mianserin The risk or severity of hypertension can be increased when Ketorolac is combined with Mianserin.
Pizotifen The risk or severity of hypertension can be increased when Ketorolac is combined with Pizotifen.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Prostaglandin G/H synthase 1 PTGS1

Referensi & Sumber

Synthesis reference: Peter J. Harrington, Hiralal N. Khatri, George C. Schloemer, "Preparation of ketorolac." U.S. Patent US6323344, issued October, 1989.
Artikel (PubMed)
  • PMID: 1458761
    Brocks DR, Jamali F: Clinical pharmacokinetics of ketorolac tromethamine. Clin Pharmacokinet. 1992 Dec;23(6):415-27. doi: 10.2165/00003088-199223060-00003.
  • PMID: 2292174
    Litvak KM, McEvoy GK: Ketorolac, an injectable nonnarcotic analgesic. Clin Pharm. 1990 Dec;9(12):921-35.
  • PMID: 15102238
    Macario A, Lipman AG: Ketorolac in the era of cyclo-oxygenase-2 selective nonsteroidal anti-inflammatory drugs: a systematic review of efficacy, side effects, and regulatory issues. Pain Med. 2001 Dec;2(4):336-51. doi: 10.1046/j.1526-4637.2001.01043.x.
  • PMID: 2178916
    Buckley MM, Brogden RN: Ketorolac. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs. 1990 Jan;39(1):86-109. doi: 10.2165/00003495-199039010-00008.
  • PMID: 10223774
    Kauffman RE, Lieh-Lai MW, Uy HG, Aravind MK: Enantiomer-selective pharmacokinetics and metabolism of ketorolac in children. Clin Pharmacol Ther. 1999 Apr;65(4):382-8. doi: 10.1016/S0009-9236(99)70131-1.
  • PMID: 8148223
    Hayball PJ, Wrobel J, Tamblyn JG, Nation RL: The pharmacokinetics of ketorolac enantiomers following intramuscular administration of the racemate. Br J Clin Pharmacol. 1994 Jan;37(1):75-8.
  • PMID: 7731074
    Yarboro TL Sr: Intramuscular Toradol, gastrointestinal bleeding, and peptic ulcer perforation: a case report. J Natl Med Assoc. 1995 Mar;87(3):225-7.
  • PMID: 28429492
    Valitalo PA, Kemppainen H, Kulo A, Smits A, van Calsteren K, Olkkola KT, de Hoon J, Knibbe CAJ, Allegaert K: Body weight, gender and pregnancy affect enantiomer-specific ketorolac pharmacokinetics. Br J Clin Pharmacol. 2017 Sep;83(9):1966-1975. doi: 10.1111/bcp.13311. Epub 2017 May 14.

Contoh Produk & Brand

Produk: 428 • International brands: 12
Produk
  • Acular
    Solution • 5 mg/1mL • Ophthalmic • US • Approved
  • Acular
    Solution / drops • 5 mg/1mL • Ophthalmic • US • Approved
  • Acular
    Solution / drops • 50 mg/1mL • Ophthalmic • US • Approved
  • Acular
    Solution / drops • 5 mg/1mL • Ophthalmic • US • Approved
  • Acular
    Solution • 0.5 % • Ophthalmic • Canada • Approved
  • Acular Ls
    Solution • 40 mg/1mL • Ophthalmic • US • Approved
  • Acular Ls
    Solution / drops • 4 mg/1mL • Ophthalmic • US • Approved
  • Acular Ls
    Solution • 0.4 % • Ophthalmic • Canada • Approved
Menampilkan 8 dari 428 produk.
International Brands
  • Bedoral — Be-Tabs Pharmaceuticals
  • Dolten — Pfizer
  • Dolten SL — Pfizer
  • Dorixina forte NF — Roemmers
  • Emodol — Jayson
  • Etorac — Incepta
  • Ketonic — Eskayef
  • Ketora — Medicon
  • Lixidol — Roche
  • Syndol — Roche

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