Ketorolac tromethamine, a nonsteroidal antiinflammatory drug, blocks prostaglandin complex formation and production through its S-enantiomeric form. It is a potent analgesic that does not possess any sedative or anxiolytic activities.
藥動學
Absorption:
1. Tmax: 44 minutes
2. Bioavailability: 100%
3. Effect of food: (high-fat meal) decreases Cmax and delays Tmax by about 1 hours Distribution:
1. Protein binding, Albumin: 99%
2. Vd: 13 L Metabolism:
Hepatic: extensive via hydroxylation and conjugation Excretion:
Fecal: approximately 6%; Renal: 92% (40% metabolites, 60% unchanged) Elimination Half Life:
1. Healthy adults: 5.2 to 5.6 hours
2. Healthy elderly subjects: 6.1 to 7 hours
3. Hepatic insufficiency: 4.5 to 5.4 hours
4. Renal insufficiency: 10.3 to 10.8 hours
5. Renal dialysis patients: 13.6 hours
6. Pediatrics: 5.8 hours
禁忌症
Allergic-type reaction, asthma, or urticaria in response to exposure to aspirin or other NSAIDs; severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported
Bleeding risk, suspected or confirmed
CABG surgery, perioperative pain treatment
Cerebrovascular bleeding, suspected or confirmed
Concomitant aspirin or NSAID use
Concomitant pentoxifylline use
Concomitant probenecid use
Gastrointestinal bleeding/perforation, recent or history
Hemorrhagic diathesis, suspected or confirmed
Hemostasis, incomplete, suspected or confirmed
Hypersensitivity or serious skin reactions ketorolac tromethamine or to any product component
Labor and delivery; increased risk of uterine hemorrhage and risk for adversely affecting fetal circulation
Nursing mothers; increased risk of adverse events in the neonate
Peptic ulcer disease, active or history
Renal impairment, advanced, or risk of renal failure due to volume depletion
Use of ketorolac tromethamine as a prophylactic analgesic prior to major surgery
懷孕分類
C(AUS)C,D(FDA)
哺乳分類
Evidence and/or expert consensus has demonstrated harmful infant effects when used during breastfeeding. An alternative to this drug should be prescribed or patients should be advised to discontinue breastfeeding.
副作用
Central nervous system: Headache
Gastrointestinal: Gastrointestinal pain, dyspepsia, nausea
Cardiovascular: Edema, hypertension
Central nervous system: Dizziness, drowsiness
Dermatologic: Diaphoresis, pruritus, skin rash
Gastrointestinal: Diarrhea, constipation, flatulence, gastrointestinal fullness, gastrointestinal hemorrhage, gastrointestinal perforation, gastrointestinal ulcer, heartburn, stomatitis, vomiting
Hematologic & oncologic: Anemia, prolonged bleeding time, purpura
Hepatic: Increased liver enzymes
Local: Pain at injection site
Otic: Tinnitus
Renal: Renal function abnormality
劑量和給藥方法
(Oral; 17 to 64 years) 20 mg once followed by 10 mg orally every 4 to 6 hours as needed, MAX 40 mg/day; MAX duration of use including oral and parenteral routes is 5 days
(Oral; 65 years of age or older OR weight less than 50 kg) 10 mg once followed by 10 mg orally every 4 to 6 hours as needed, MAX 40 mg/day; MAX duration of use including oral and parenteral routes is 5 days
小兒調整劑量
Safety and efficacy of oral ketorolac tromethamine have not been established in pediatric patients under 17 years of age
腎功能調整劑量
10 mg ORALLY every 4 to 6 hours as needed, MAX 40 mg/day