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ketorolac (Toradol, Acular, Acuvail)
Tradenames: Toradol, Acular. ketorolac tromethamine.
Indications:
- management of moderate to severe acute pain-related syndrome
- renal colic
- not for chronic pain
- ophthalmic
- eye pain, eye inflammation
- allergic conjunctivitis
- photophobia [7]
Contraindications:
1) concurrent administration of probenecid
2) patients who have developed nasal polyps, angioedema or bronchospastic reactions to NSAIDs
3) cerebrovascular hemorrhage
4) hemorrhagic diathesis
5) high risk of bleeding
6) pre-operative prophylaxis
7) intra-operative use when hemostasis is critical
8) severe renal insufficiency
9) active peptic ulcer disease
10) history of gastrointestinal bleeding
11) chronic pain
Dosage:
1) 15-60 mg IM/IV every 6 hours, max 120 mg/day
- administer IV over at least 15 seconds
2) patients > 65 years or patients with renal insufficiency
- 15 to 30 mg IV/IM every 6 hours, max 60 mg/day
3) 10 mg PO QID, max 40 mg/day
4) should NOT be used for > 5 days
5) do NOT administer intrathecally or epidurally
Tabs: 10 mg.
Injection: 15 mg, 30 mg, 60 mg (single-dose syringes).
Ophthalmic: (Acular) 1 drop QID (0.5%)
Pharmacokinetics:
1) rapidly absorbed with IM administration
2) peak levels 30-60 minutes after IM administration
3) peak levels 1-3 minutes after IV administration
4) metabolized by liver
5) excreted by kidneys
6) terminal 1/2life is approximately 6 hours, prolonged with renal impairment
Monitor:
- liver function tests periodically [5]
Adverse effects:
1) not common (1-10%)
- drowsiness, bruising or burning at site of injection, dyspepsia, abdominal pain, edema, diarrhea, dizziness, headache, increased sweating
2) uncommon (< 1%)
- purpura/ecchymosis, aphthous stomatitis, rectal bleeding, GI bleed/ulceration, dyspnea, blurred vision, oliguria, mental depression
3) other [2]
- nausea
- anaphylaxis
- renal impairment
- elevated serum transaminases
- inhibition of platelet adhesion
Drug interactions:
1) warfarin in combination prolong bleeding times
2) ketorolac decreases clearance & increases toxicity of:
a) methotrexate
b) Li+
3) probenecid
a) competes for elimination
b) contraindicated
4) glucocorticoids in combination increases risk of GI & renal damage
5) salicylates
6) ketorolac may enhance activity of non-depolarizing muscle relaxants
Laboratory:
1) specimen: serum, plasma
2) methods: HPLC
Mechanism of action:
1) acetic acid class NSAID with anti-inflammatory, analgesic & antipyretic properties
2) inhibits prostaglandin synthesis
Interactions
drug interactions
drug adverse effects of NSAIDs
monitor with non steroidal anti-inflammatory agents (NSIADs)
General
non-steroidal anti-inflammatory agent (NSAID)
Properties
INHIBITS: cyclooxygenase
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 4-10 HOURS
protein-binding >99%
elimination by hemodialysis -
peritoneal dialysis -
pregnancy-category C
D <3rd trimester>
safety in lactation -
?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed,
WB Saunders, Philadelpha 1995
- Prescriber's Letter 17(7): 2010
Recommended Lab Monitoring for Common Medications
Liver Function Test Scheduling
Detail-Document#: 260704
(subscription needed) http://www.prescribersletter.com
- Prescriber's Letter 19(6): 2012
COMMENTARY: Common Questions About Ketorolac
GUIDELINES: Guidelines for Prevention of NSAID-Related Ulcer Complications (2009)
Detail-Document#: 280607
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference
Component-of
isopropanol/ketorolac/lidocaine/povidone iodine
ketorolac/phenylephrine