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:
Tmax: (IM) 33 to 44 minutes; (IV) 1.1 to 2.9 minutesbr>
Bioavailability: 100% Distribution:
1. Protein binding, Albumin: 99%
2. Vd: (IM) 0.175 L/kg; (IV, adults) 0.21 L/kg; (IV, pediatrics) 0.26 L/kg 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
1. 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
2. Bleeding risk (Cerebrovascular bleeding, Gastrointestinal bleeding/perforation, Hemostasis)
3. CABG surgery, perioperative pain treatment
4. Concomitant use with aspirin or NSAID, pentoxifylline, probenecid
5. Labor and delivery\; Nursing mothers
6. Peptic ulcer disease; Renal impairment
懷孕分類
C(AUS)C,D(FDA)
哺乳分類
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
IV; 17 to less than 65 years:
30 mg IV as a single dose OR 30 mg IV every 6 hours, MAX dose, 120 mg/day; MAX duration, 5 days IV; 65 years or older OR weight less than 50 kg:
15 mg IV as a single dose OR 15 mg IV every 6 hours; MAX dose, 60 mg/day; MAX duration, 5 days IM; 17 to less than 65 years:
60 mg IM as a single dose OR 30 mg IM every 6 hours; MAX dose, 120 mg/day; MAX duration, 5 days IM; 65 years or older OR weight less than 50 kg:
30 mg IM as a single dose OR 15 mg IM every 6 hours; MAX dose, 60 mg/day; MAX duration, 5 days
小兒調整劑量
Safety and efficacy of injectable ketorolac tromethamine have not been established in pediatric patients under 17 years of age
腎功能調整劑量
30 mg IM for 1 dose OR 15 mg IM every 6 hours, MAX 60 mg/day OR
15 mg IV for 1 dose OR 15 mg every 6 hours, MAX 60 mg/day