Usage
Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID), is prescribed for the management of pain and inflammation associated with various conditions, including:
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis
- Acute articular and periarticular disorders (e.g., bursitis, capsulitis, synovitis, tendonitis)
- Fibrositis
- Cervical spondylitis
- Low back pain (e.g., strain, lumbago, sciatica)
- Gout
- Dysmenorrhea
- Post-operative pain
- Mild to moderate pain
Pharmacological Classification: Non-steroidal anti-inflammatory drug (NSAID), analgesic.
Mechanism of Action: Ketoprofen inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing the production of prostaglandins, which are mediators of pain and inflammation.
Alternate Names
Ketoprofen is also known as di-ketoprofen lysine salt. Brand names include Orudis, Oruvail, Actron, Kiprofen, Nexcede, Orudis KT.
How It Works
Pharmacodynamics: Ketoprofen exerts its analgesic and anti-inflammatory effects by inhibiting prostaglandin synthesis. It also has antipyretic properties.
Pharmacokinetics:
- Absorption: Ketoprofen is rapidly and almost completely absorbed after oral administration. Food may delay absorption but does not affect the extent of absorption.
- Metabolism: Primarily metabolized in the liver by glucuronidation.
- Elimination: Excreted mainly in the urine as ketoprofen glucuronide.
Mode of Action: Ketoprofen inhibits COX-1 and COX-2 enzymes, thereby blocking the conversion of arachidonic acid to prostaglandins.
Receptor Binding/Enzyme Inhibition: Ketoprofen acts through non-selective inhibition of COX enzymes.
Elimination Pathways: Primarily renal excretion.
Dosage
Standard Dosage
Adults:
- Immediate-release capsules: 25-50 mg every 6-8 hours as needed, up to a maximum of 300 mg/day.
- Extended-release capsules: 200 mg once daily for osteoarthritis and rheumatoid arthritis. Not recommended for acute pain.
Children:
Use and dose must be determined by a doctor. Not recommended for children under 12 years old.
Special Cases:
- Elderly Patients: Lower initial doses are recommended, typically starting at the lower end of the dosage range. Dose reductions may be necessary for patients over 75. Close monitoring for adverse effects is essential.
- Patients with Renal Impairment: Dose reduction is necessary for patients with moderate to severe renal impairment. Contraindicated in severe renal impairment.
- Patients with Hepatic Dysfunction: Dose reduction may be required in patients with hepatic impairment. Contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Dosage adjustments should be considered for patients with conditions like diabetes, cardiovascular disease, and bleeding disorders.
Clinical Use Cases
Ketoprofen is not typically recommended for use in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Other analgesics and anti-inflammatory agents are usually preferred in these scenarios.
Dosage Adjustments
Dosage modifications may be required based on patient-specific factors such as renal/hepatic function, age, and other medical conditions. Close monitoring of patient response and potential side effects is crucial.
Side Effects
Common Side Effects:
- Gastrointestinal upset (e.g., dyspepsia, nausea, diarrhea, constipation, abdominal pain)
- Headache
- Dizziness
- Drowsiness
- Rash
Rare but Serious Side Effects:
- Gastrointestinal bleeding or perforation
- Cardiovascular thrombotic events (e.g., myocardial infarction, stroke)
- Heart failure
- Renal impairment
- Hepatic dysfunction
- Severe allergic reactions (anaphylaxis)
- Severe skin reactions (e.g., Stevens-Johnson syndrome)
Long-Term Effects:
Chronic use of ketoprofen can increase the risk of gastrointestinal complications, cardiovascular issues, and renal damage.
Adverse Drug Reactions (ADR):
Any signs of gastrointestinal bleeding, cardiovascular events, or allergic reactions should be treated as medical emergencies.
Contraindications
- Hypersensitivity to ketoprofen or any other NSAIDs.
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
- Active peptic ulcer disease.
- History of gastrointestinal bleeding or perforation related to previous NSAID therapy.
- Severe heart failure.
- Severe renal impairment.
- Severe hepatic impairment.
- Coronary artery bypass graft (CABG) surgery.
- Third trimester of pregnancy.
Drug Interactions
Ketoprofen can interact with numerous medications, including:
- Anticoagulants (e.g., warfarin)
- Antihypertensives
- Lithium
- Methotrexate
- Other NSAIDs
- Corticosteroids
Pregnancy and Breastfeeding
- Pregnancy: Ketoprofen is contraindicated during the third trimester of pregnancy. Use in the first and second trimesters should be avoided unless the potential benefit outweighs the risk to the fetus.
- Breastfeeding: Ketoprofen is excreted in breast milk in small amounts. While generally considered compatible with breastfeeding, alternative agents may be preferred, particularly when nursing a newborn or preterm infant.
Drug Profile Summary
- Mechanism of Action: Inhibits COX-1 and COX-2 enzymes, reducing prostaglandin synthesis.
- Side Effects: GI upset, headache, dizziness, rash. Serious side effects include GI bleeding, cardiovascular events, and renal impairment.
- Contraindications: Hypersensitivity to NSAIDs, active peptic ulcer, severe heart failure, renal/hepatic impairment, third trimester of pregnancy, CABG surgery.
- Drug Interactions: Anticoagulants, antihypertensives, lithium, methotrexate, other NSAIDs, corticosteroids.
- Pregnancy & Breastfeeding: Contraindicated in third trimester. Use with caution during breastfeeding.
- Dosage: Adults: 25-50 mg every 6-8 hours or 200 mg ER once daily. Pediatric: Use with caution. Dosage to be determined by physician. Elderly: Start with lower doses.
- Monitoring Parameters: Renal function, liver function, blood pressure, signs of GI bleeding.
Popular Combinations
Ketoprofen is not typically used in combination with other drugs for synergistic effects due to the increased risk of side effects.
Precautions
- Pre-existing medical conditions should be carefully evaluated before prescribing ketoprofen.
- Renal and hepatic function should be monitored, especially in elderly patients.
- Patients should be advised to report any signs of GI bleeding or allergic reactions.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ketoprofen?
A: Adults: Immediate-release: 25-50 mg every 6-8 hours as needed, up to 300 mg/day. Extended-release: 200 mg once daily for osteoarthritis and rheumatoid arthritis. Children: Dosage should be determined by a doctor. Elderly: Start at the lower end of the dosage range.
Q2: What are the common side effects of ketoprofen?
A: Common side effects include gastrointestinal issues (dyspepsia, nausea, diarrhea, constipation, abdominal pain), headache, dizziness, drowsiness, and rash.
Q3: What are the serious side effects of ketoprofen?
A: Serious side effects can include gastrointestinal bleeding or perforation, cardiovascular thrombotic events (heart attack and stroke), heart failure, renal impairment, and severe allergic reactions.
Q4: Can ketoprofen be used during pregnancy?
A: Ketoprofen is contraindicated during the third trimester. Use in the first and second trimesters should be avoided unless the potential benefits outweigh the risks.
Q5: Can ketoprofen be used during breastfeeding?
A: Ketoprofen is excreted in breast milk in small amounts. While generally considered compatible with breastfeeding, alternative medications may be preferred.
Q6: What are the contraindications to ketoprofen use?
A: Contraindications include hypersensitivity to ketoprofen or other NSAIDs, history of NSAID-induced asthma or allergic reactions, active peptic ulcer, severe heart failure, severe hepatic or renal impairment, third trimester of pregnancy, and recent CABG surgery.
Q7: How does ketoprofen interact with other medications?
A: Ketoprofen can interact with various medications, including anticoagulants, antihypertensives, lithium, methotrexate, and corticosteroids. It is important to inform your doctor about all other medications you are taking.
Q8: What precautions should be taken when prescribing ketoprofen?
A: Renal and hepatic function, as well as cardiovascular health and history of GI issues should be assessed before prescribing ketoprofen. Patients should be monitored for adverse effects, and the lowest effective dose should be used for the shortest possible duration.
Q9: What is the mechanism of action of ketoprofen?
A: Ketoprofen inhibits COX-1 and COX-2 enzymes, leading to a reduction in prostaglandin synthesis. Prostaglandins are mediators of pain, inflammation, and fever.
