Ketorolac

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Pharmacokinetics 6 Monitor 7 Adverse-effects 8 Drug-interactions 9 Laboratory 10 Mechanism-of-action 11 More General Terms 12 Internet Database 13 References

Introduction

• Tradenames: Toradol, Acular. ketorolac tromethamine.

Indications

• management of moderate to severe acute pain-related syndrome
• not for chronic pain

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
  

• 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
• metablized 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 [5]
  
• 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 [2]

• 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 lithium carbonate with NSAIDs
• drug interaction(s) of NSAIDs with SSRIs
• drug interaction(s) of aspirin with NSAIDs
• drug interaction(s) of NSAIDs with beta blockers
• drug interaction(s) of NSAIDs with ARBs
• drug interaction(s) of NSAIDs with ACE inhibitors
• drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
• drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
• 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)

Internet Database

PubChem: 3826
PubChem: 84003

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
4. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
5. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: [1] (subscription needed) [2]

ketorolac (Toradol, Acular)