What Is Ketorolac?

This product is a derivative of pyrrolic acid, which is a non-steroidal anti-inflammatory drug, which inhibits PG synthesis, has analgesic, anti-inflammatory, antipyretic effect and inhibits platelet aggregation. The analgesic effect is similar to aspirin, and the analgesic effect after intramuscular injection is approximately medium morphine.

Drug Name: Ketorolac
Alias: (+/-)-5-benzoyl-2,3-dihydro-1H-pyrrolopyrrolidine-1-carboxylic acid
Foreign name: Ketorolac

Whether prescription drugs: prescription
Dosage: 10mg each time, 1-4 times a day
Main medication contraindications: Avoid fasting or long-term use
Drug type: chemical

Ketorolac Basic Information

Chinese name: ketorolac

Chinese alias: (+/-)-5-benzoyl-2,3-dihydro-1H-pyrrolopyrrolidine-1-carboxylic acid

English name: Ketorolac

English alias: Acular; Tm-asyn; Ketoralac; Toratex; Fluoxetin; Lixidol; Dolac; KETOROLAC-D5;

CAS number: 74103-06-3

Molecular formula: C ₁₅ H ₈ D ₅ NO ₃

Molecular weight: 260.29900

Exact mass: 260.12100

PSA: 59.30000

LogP: 2.29100

Structural formula:

Ketorolac properties

Appearance and properties: white crystal or white powder

Density: 1.398 g / cm ³

Melting point: 160-161 ° C

Boiling point: 223.7ºC at 760 mmHg

Flash point: 89.1ºC

Refractive index: 1.659 ^[2]

Ketorolac Toxicology Data

Acutely toxic LD50 mice (mg / kg): about 200 orally.

Molecular structure data

1. Molar refractive index: 70.53

2. Molar volume (cm3 / mol): 191.2

3. Isometric ratio (90.2K): 520.2

4. Surface tension (dyne / cm): 54.8

5. Polarizability (10-24cm3): 27.96

Ketorolac calculated chemical data

1. Hydrophobic parameter calculation reference value (XlogP): 1.9

2. Number of hydrogen-bonded donors: 1

3. Number of hydrogen bond acceptors: 3

4. Number of rotatable chemical bonds: 3

5. Number of tautomers: 4

6. Topological molecular polar surface area 59.3

7. Number of heavy atoms: 19

8. Surface charge: 0

9. Complexity: 376

10. Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 0

12. Uncertain number of atomic stereocenters: 1

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0

15. Number of covalent bond units: 1

Ketorolac properties and stability

(+)-Configuration: Crystallized from hexane-ethyl acetate, melting point 174 ° C; melting point 154 156 ° C. [] D + 173 ° (C = 1, methanol).

(-)-Configuration: Crystallized from hexane-ethyl acetate. [] D-176 ° (C = 1, methanol).

Ketorolac Tromethamine: [74103-07-4]. Crystallized from ethyl acetate, melting point 169-170 ° C ^[1] .

Ketorolac Safety Information

Packing level: II

Hazard category: 6.1 (a)

Dangerous Goods Transport Code: 3249

Ketorolac Ketorolac Related Drug Sheet Information

Ketorolac Classification Name

Primary classification: Nervous system drugs Second classification: Antipyretic analgesics Third classification: Other

Ketorolac drug dosage form

1. Injection: 10mg (1ml), 30mg (1ml); 2. Tablet: 10mg; 3. Eye drops: 8ml (0.1%).

Ketorolac pharmacological effects

It is a prostaglandin synthase inhibitor with strong analgesic effect and moderate anti-inflammatory and antipyretic effect. It mainly works by blocking the epoxidase of arachidonic acid metabolism and reducing the synthesis of prostaglandin. In a standard animal model of analgesia, the analgesic activity of this product is 800 times that of aspirin, which is stronger than indomethacin and naproxen, which is equivalent to or better than that of bataxone. In many tests, its anti-inflammatory activity is equivalent to or stronger than indomethacin, stronger than naproxen, and significantly better than that of boutezone. Multiple tests on eye diseases have shown that this product has strong anti-inflammatory activity without worsening potential eye infections. In the rat model, the antipyretic activity of this product is stronger than that of aspirin and buta pine, which is equivalent to indomethacin and naproxen. This product seems to inhibit platelet aggregation caused by arachidonic acid and collagen, but does not inhibit platelet aggregation caused by adenosine diphosphate, which seems to prolong the average bleeding time. Topical application of this product can reduce the level of prostaglandin (PGE2) in aqueous humor, has anti-inflammatory and analgesic effects, has little effect on intraocular pressure, and can be combined with antibiotics, -receptor antagonists and mydriatics. The advantage of this medicine is that it has no toxic and side effects such as central nervous system damage and addiction, and no adverse reactions such as respiratory depression or constipation.

Ketorolac pharmacokinetics

It can be absorbed after intramuscular injection or oral tromethamine salt. At physiological pH, the salt dissociates to form a cationic ketorolac molecule, which is less hydrophilic than the salt. Ketorolac peak in blood can be reached in about 30 to 60 minutes. In some individuals, intramuscular injection is slower than oral absorption. Ketorolac has a protein binding rate of 99%. Ketorolac does not easily penetrate the blood-cerebrospinal fluid barrier, but it can pass through the placenta, and a small amount of drug can be distributed into milk. The terminal t1 / 2 is about 4 to 6 hours, 6 to 7 hours in the elderly, and 9 to 10 hours in patients with renal insufficiency. Mainly combined with glucuronic acid and hydroxylated metabolism, about 90% of the original drug and metabolites are excreted with urine, and the rest are excreted with feces.

Ketorolac indication

This product is suitable for analgesia after short-term surgery, including moderate to severe pain caused by abdominal, gynecological, oral, orthopedic and urological surgery. It can also be used to relieve renal colic, toothache, trauma and cancer pain. The medicine eye drops can be used to treat inflammation and seasonal allergic conjunctivitis after ophthalmic surgery. (Foreign data)

Ketorolac contraindications

1. This product is contraindicated in patients who are allergic to it and this class of drugs, patients with active ulcer disease, and postoperative patients. 2. Allergic to other non-steroidal anti-inflammatory drugs, nasal polyps syndrome, neurovascular edema, bronchial asthma, renal insufficiency, pregnant women and children are prohibited from using this product. 3 Obstetric surgery and pain during delivery are contraindicated. 4. Prohibition of use with anticoagulants or other non-steroidal anti-inflammatory drugs. 5. Disable elderly and children. 6. Eye drops are forbidden for those who wear contact lenses. 7. Patients with active peptic ulcer. 8. Pregnant women. 9. Analgesia during childbirth. 10. Nasal polyps syndrome and angioedema. 11. Those with a high risk of bleeding. 12. Children under 18 years of age.

Ketorolac Notes

1. Since this product will increase the incidence of side effects of the digestive tract with the use of time, it should not be used for a long time. 2. For patients with prolonged bleeding time, history of peptic ulcer, history of liver and kidney disease, and elderly over 65 years, lactating women should use this product with caution. 3. Closely observe the occurrence of adverse reactions in patients during medication. This medicine should not be used orally for a long time to treat chronic pain.

Ketorolac adverse reactions

This product has more serious adverse reactions than similar drugs. Common neurological reactions are: lethargy, dizziness, and headache. Gastrointestinal reactions: nausea, vomiting, abdominal pain, indigestion. Others: dry mouth, muscle pain, palpitations, vasodilation. Long-term application can cause allergic reactions such as renal insufficiency and rash, bronchospasm, shock. Deaths caused by gastrointestinal bleeding, postoperative bleeding, acute renal insufficiency, and allergic reactions have been reported. Occasionally inhibits platelet function, prolongs bleeding time, and is reversible.

Ketorolac usage and dosage

1. Oral, adults, 10 mg each time, 1 to 4 times a day, increasing to 20 mg each time for severe pain. The duration of medication should not exceed 2 days. 2. Intramuscular injection, 30 ~ 60mg each time, daily maximum 90mg. The duration of medication should not exceed 3 days. 3. Renal insufficiency and dose reduction for the elderly over 65 years old. 4. Eye drops: Eye drops with 0.1% solution, 1 to 2 drops each time, 3 times a day.

The corresponding effects of ketorolac drugs

1. This medicine is used in combination with other non-steroidal anti-inflammatory drugs, and the adverse reactions increase, and it should be avoided. 2. Combination of diuretics can enhance the adverse reactions of this drug. 3. This drug is used in combination with morphine or pethidine in the treatment of postoperative pain without significant adverse interactions. 4. Combined with certain anti-infective drugs such as -lactam penicillin, cephalosporins and aminoglycoside antibiotics, antiemetics, laxatives, bronchodilators, etc., without drug interactions ^[3] .

Ketorolac reviews

This product is similar to other non-steroidal anti-inflammatory drugs. It has the strongest analgesic effect and moderate anti-inflammatory effect. It is suitable for severe pain after surgery and advanced cancer pain. Its analgesic effect is equivalent to or more than 6 to 12 mg of morphine. According to domestic reports, 62 patients with cancer pain (25 patients with moderate pain and 37 patients with severe pain) were randomly divided into two groups, and intramuscular injection of ketorolac 30mg once every 6 hours, or 100 mg of cinnarizine was injected once every 6 hours; the two groups were administered for 3 days each, and then exchanged for 3 days. Results The total effective rates of moderate to severe cancer pain in the two groups were 85% and 76%, respectively (P> 0.05). The former takes effect later than the latter, and the painless maintenance takes longer than the latter. This medicine has a strong analgesic effect at a lower dose, and can replace analgesics such as morphine and pethidine. Its analgesic activity is 800 times that of aspirin, its anti-inflammatory activity is stronger than that of indomethacin, and its antipyretic effect is stronger than that of boutezone. The medicinal product has the advantages of small side effects and no addiction.