ChemicalBook > Product Catalog > API > Antipyretic analgesics > Nonsteroidal Anti-Inflammatory Drugs (NSAIDS) > Ketorolac
Ketorolac Chemical Properties
- Melting point:160-161°C
- Boiling point:493.2±40.0 °C(Predicted)
- Density 1.33±0.1 g/cm3(Predicted)
- pka3.49 ±0.02(at 25℃)
- Water Solubility 183mg/L(32 ºC)
- CAS DataBase Reference74103-06-3(CAS DataBase Reference)
- EPA Substance Registry System1H-Pyrrolizine-1-carboxylic acid, 5-benzoyl-2,3-dihydro- (74103-06-3)
- RIDADR 3249
- HazardClass 6.1(a)
- PackingGroup II
- ToxicityLD50 orally in mice: ~200 mg/kg (Rooks)
Ketorolac Usage And Synthesis
- Chemical propertiesIt is crystallized in ethyl acetate - ether with a melting point of 160~161 degrees centigrade.The maximum absorption of UV (methanol):245,312m (epsilon 7080,17400). PKa3.49 + 0.02.Acute toxic LD50 mice (mg/kg): about 200 of oral administration. .(+) - configuration: crystallized from hexane ethyl acetate with the melting point of 174 degrees centigrade;The melting point is 154 156 degrees centigrade. [α]D+173° (C=1, methanol).(-) - configuration: crystallizzed from hexane ethyl acetate with melting point at 169~170 degrees centigrade; melting point is 153~155 degrees centigrade. [α]D-176° (C=1, methanol).
- Pharmacological actionKetorolac is also called ketorolac, acular and Ketorolac Tromethamine. It is a non steroid analgesic and anti-inflammatory drug, a derivative of pyrrolidone.The chemical structure and pharmacological action is similar to Tolectin, Zoaesthetic acid and Indometacin. By inhibiting cyclooxygenase, it inhibits the synthesis and release of prostaglandins, and produces anti-inflammatory effects. It can reduce the temperature induced by heat source, which is related to the inhibition of the synthesis of prostaglandin in the central nervous system.It has strong analgesic and moderate anti-inflammatory antipyretic and inhibition of platelet aggregation, and has no inhibition of respiration and addiction. In animal experiments, the analgesic effect is stronger than aspirin, indomethacin and naproxen.It is equal to or better than the anti-inflammatory effect of naproxen and indomethacin, phenylbutazone,Its antipyretic effect on rats are stronger than aspirin and phenylbutazone and the same with indomethacin and naproxen.It inhibits the platelet aggregation induced by arachidonic acid and collagen.But it does not inhibit the induction of adenosine diphosphate(ADP) ..This product is quickly and completely absorbed after the intramuscular injection, and is almost completely absorbed after oral administration.Food can slow down the absorption speed, but it does not affect the degree of absorption, and the bioavailability is 80% ~ 100%. 10 minutes after intramuscular injection of 30mg, it usually relieves the pain obviously. After 50 minutes, the peak of plasma concentration is up to 2.2 g/mL.After 30~60 minutes of oral administration, the pain is obviously relieved and the concentration of plasma is peak at 1.5 to 4 hours.The plasma half-life of young people is about 5.3 hours, and for the elderly it is about 7 hours, and the analgesic effect could be maintained for 6~8 hours. 91.4% will be excreted from the urinary tract, the rest will be excreted from the excrement.In patients with renal insufficiency, the total plasma clearance rate decreases and the half-life prolongs, so the dosage should be reduced.
Clinical application: ketorolac is mainly used for short-term pain treatment including postoperative pain (such as the abdomen, chest, Urology, gynecology, Department of Stomatology, orthopedic surgery and pain) as well as the acute skeletal muscle pain caused by various causes, such as sprain, dislocation, fracture and soft tissue injury, and other pain caused by other diseases, such as postpartum pain, acute renal colic, toothache, sciatica, late cancer pain, wound pain, biliary colic, etc.. It can be used as a substitute for morphine and pethidine.
- Chemical PropertiesLight yellow solid
- Usesprostaglandin F2a analogue
- IndicationsKetorolac (Toradol), an NSAID chemically related to indomethacin and tolmetin, is mainly used as an analgesic, not for the treatment of inflammatory disease. It is available in oral, parenteral, and topical formulations.
- brand nameAcular (Allergan); Toradol (Roche).
- World Health Organization (WHO)Ketorolac is a nonsteroidal anti-inflammatory agent used in the management of moderate to severe acute post-operative pain. It remains on the market in many countries with restrictions on its use.
- Biological FunctionsKetorolac (Toradol) is an NSAID with very mild antiinflammatory and antipyretic activity. It is a potent analgesic for postoperative pain. Its efficacy is equivalent to that of low doses of morphine in the control of pain. For this reason it is often combined with opioids to reduce opioid dose and related side effects while providing adequate pain relief. It is also used to replace the opioids in some patients with opioid sensitivity. The mechanism of action of ketorolac involves the inhibition of COX and decreased formation of prostaglandins. However, some evidence exists that ketorolac may stimulate the release of endogenous opioids as a part of its analgesic activity.
- General DescriptionKetorolac tromethamine (Toradol), marketed as a mixture of(R)- and (S)-ketorolac enantiomers, is a potent NSAID analgesicindicated for the treatment of moderately severe, acutepain. It should be noted that the pharmacokinetic dispositionof ketorolac in humans is subject to marked enantioselectivity.Thus, it is important to monitor the individual blood levelsso an accurate assessment of its therapeutic action can bemade correctly. However, it should be noted that, beingone of the conventional NSAIDs with highest risk of GIcomplications, its administration should not exceed 5 days.
Ketorolac Preparation Products And Raw materials
- rac Ketorolac 6-Benzoyl IsoMer Ketorolac EP IMpurity F Ketorolac EP IMpurity I 1-Keto Ketorolac Ketorolac Related Compound A (20 mg) (5-benzoyl-N-(1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)-2,3-dihydro-1H-pyrrolizine-1-carboxamide) Ketorolac EP IMpurity H Ketorolac EP IMpurity D Ketorolac EP IMpurity G Pyrrole KETOROLAC TROMETAMOL FOR PEAK IDENTIFICATION Ketorolac tromethamine 4-HYDROXY KETOROLAC KETOROLAC TROMETAMOL Ketorolac Tromethamine Injection USP (R)-(+)-Ketorolac,(R)-Ketorolac Ketorolac KETOROLAC ACETOPHENONE-2',3',4',5',6'-D5
- Company Name:Shanghai Renshi Pharmatech Co., LTD Gold
- Tel:17721318029 021-26018649-
- Company Name:parabiochem Gold
- Company Name:INTATRADE GmbH
- Tel:+49 3493/605464
- Company Name:Shijiazhuang Sdyano Fine Chemical Co., Ltd.
- Company Name:LGM Pharma