ketorolac (Toradol, Acular, Acuvail)

Introduction

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

Contraindications

• concurrent administration of probenecid
• patients who have developed nasal polyps, angioedema or bronchospastic reactions to NSAIDs
• cerebrovascular hemorrhage
• hemorrhagic diathesis
• high risk of bleeding
• pre-operative prophylaxis
• intra-operative use when hemostasis is critical
• severe renal insufficiency
• active peptic ulcer disease
• history of gastrointestinal bleeding
• chronic pain

pregnancy category = c

pregnancy category = d

safety in lactation = -

safety in lactation = ?

Dosage

• 15-60 mg IM/IV every 6 hours, max 120 mg/day
  • administer IV over at least 15 seconds
• patients > 65 years or patients with renal insufficiency
  • 15 to 30 mg IV/IM every 6 hours, max 60 mg/day
• 10 mg PO QID, max 40 mg/day
• should NOT be used for > 5 days
• 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

• rapidly absorbed with IM administration
• peak levels 30-60 minutes after IM administration
• peak levels 1-3 minutes after IV administration
• metabolized by liver
• excreted by kidneys
• terminal 1/2life is approximately 6 hours, prolonged with renal impairment

elimination via liver

elimination via kidney

1/2life = 4-10 hours

protein binding = >99 %

elimination by hemodialysis = -

elimination by peritoneal dialysis = -

Monitor

• liver function tests periodically

• monitor with non steroidal anti-inflammatory agents (NSIADs)

Adverse effects

• not common (1-10%)
  • drowsiness, bruising or burning at site of injection, dyspepsia, abdominal pain, edema, diarrhea, dizziness, headache, increased sweating
• uncommon (< 1%)
  • purpura/ecchymosis, aphthous stomatitis, rectal bleeding, GI bleed/ulceration, dyspnea, blurred vision, oliguria, mental depression
• other
  • nausea
  • anaphylaxis
  • renal impairment
  • elevated serum transaminases
  • inhibition of platelet adhesion

• drug adverse effects of NSAIDs

Drug interactions

• warfarin in combination prolong bleeding times
• ketorolac decreases clearance & increases toxicity of:
  • methotrexate
  • Li+
• probenecid
  • competes for elimination
  • contraindicated
• glucocorticoids in combination increases risk of GI & renal damage
• salicylates
• ketorolac may enhance activity of non-depolarizing muscle relaxants

• drug interaction(s) of cholinesterase inhibitors with NSAIDs
• drug interaction(s) of lithium carbonate with NSAIDs
• drug interaction(s) of NSAIDs with oral contraceptive
• drug interaction(s) of NSAIDs with SSRIs
• drug interaction(s) of NSAIDs with antidepressants
• drug interaction(s) of aspirin with NSAIDs
• drug interaction(s) of apixaban with NSAIDs
• drug interaction(s) of warfarin with NSAIDs
• drug interaction(s) of NSAIDs with beta blockers
• drug interaction(s) of NSAIDs with ARBs
• drug interaction(s) of NSAIDs with aldosterone antagonis
• drug interaction(s) of NSAIDs with glucocorticoid
• drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
• drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
• drug interaction(s) of NSAIDs with ACE inhibitors
• drug interaction(s) of NSAIDs & antihypertensives
• drug interaction(s) of NSAIDs & loop diuretics
• drug interaction(s) of NSAIDs & aspirin

Laboratory

• specimen: serum, plasma
• methods: HPLC

Mechanism of action

• acetic acid class NSAID with anti-inflammatory, analgesic & antipyretic properties
• inhibits prostaglandin synthesis

More general terms

• non-steroidal anti-inflammatory agent (NSAID)

Component of

• ketorolac/phenylephrine
• isopropanol/ketorolac/lidocaine/povidone iodine

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3826
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=84003