Ketoprofen

OVERVIEW

Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the propionic acid class. It is primarily used to relieve pain, inflammation, and stiffness associated with a variety of conditions, including arthritis and menstrual cramps.

DOSAGE

Pain Management

Immediate-release capsules:

Adults: 25–50 mg every 6 to 8 hours as needed. Maximum: 300 mg per day.

Extended-release capsules:

200 mg once daily. Not recommended for acute pain.

Rheumatoid Arthritis and Osteoarthritis

Immediate-release capsules:

Adults: 75 mg three times a day or
50 mg four times a day.
Maximum: 300 mg per day.

Extended-release capsules:

Adults: 200 mg once daily.

Menstrual Pain (Dysmenorrhea)

Adults: 25–50 mg every 6 to 8 hours as needed. Maximum: 300 mg per day.

ketoprofen- Dosage
Condition	Formulation	Dosage	Maximum Dosage
Pain Management	Immediate-release	25–50 mg every 6–8 hours as needed	300 mg per day
	Extended-release	200 mg once daily	200 mg per day
Rheumatoid Arthritis	Immediate-release	75 mg three times a day or 50 mg four times a day	300 mg per day
	Extended-release	200 mg once daily	200 mg per day
Osteoarthritis	Immediate-release	75 mg three times a day or 50 mg four times a day	300 mg per day
	Extended-release	200 mg once daily	200 mg per day
Dysmenorrhea (Menstrual Pain)	Immediate-release	25–50 mg every 6–8 hours as needed	300 mg per day
	Extended-release	Not recommended for acute pain	N/A

MECHANISM OF ACTION

Inhibition of Cyclooxygenase Enzymes

COX-1 and COX-2 inhibition: Ketoprofen inhibits both COX-1 and COX-2 enzymes. COX-1 is involved in the production of prostaglandins that protect the stomach lining and support platelet function, while COX-2 is induced during inflammation and is responsible for the production of prostaglandins that control pain and inflammation. By inhibiting these enzymes, ketoprofen reduces the synthesis of prostaglandins, thereby reducing inflammation, pain, and fever.

Anti-inflammatory Effects

Decreased prostaglandins: Decreasing prostaglandin levels results in decreased sensitivity of pain receptors and reduced vasodilation in inflamed tissues, thereby reducing symptoms associated with conditions such as arthritis and dysmenorrhea.

Additional Actions

Anti-Bradykinin Activity: Ketoprofen may also exhibit anti-bradykinin properties, which contribute to its analgesic effects by counteracting the action of bradykinin, a peptide that increases inflammation and pain.

Lysosomal membrane stabilization: It has been suggested that ketoprofen stabilizes lysosomal membranes, which may help prevent the release of inflammatory mediators from damaged cells.

Antipyretic Effects

Ketoprofen’s ability to reduce fever is thought to be due to its action on the hypothalamus, causing increased peripheral blood flow and vasodilation, which facilitates heat dissipation.

ADVERSE DRUG REACTIONS

Gastrointestinal Issues:

• Dyspepsia
• Abdominal pain
• Nausea
• Diarrhea
• Constipation
• Heartburn

Central Nervous System:

• Headache
• Dizziness
• Drowsiness

Cardiovascular Risks:

There is an increased risk of serious cardiovascular thrombotic events, including myocardial infarction (heart attack) and stroke, which can be fatal. This risk is increased in patients with pre-existing cardiovascular conditions or those who use the drug for a long period of time.

Gastrointestinal Risks:

Risk of serious gastrointestinal events such as bleeding, ulceration, and perforation of the stomach or intestines, which can occur without warning. Elderly patients are at particularly high risk.

Renal Effects:

Kidney problems, including decreased urine output and fluid retention.

Hepatic Effects:

Possible liver damage, indicated by symptoms such as jaundice (yellowing of the skin or eyes), dark urine, and loss of appetite.

Severe Allergic Reactions:

Serious skin reactions such as anaphylaxis or Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) that can be fatal. Symptoms may include rash, fever, swollen lymph nodes, and difficulty breathing.

DRUG-DRUG INTERACTIONS

Warfarin: Risk of gastrointestinal bleeding increases with concurrent use. Close monitoring is required.

Methotrexate: Ketoprofen may inhibit the elimination of methotrexate, resulting in increased serum levels and toxicity.

Probenecid: This combination may increase levels of ketoprofen in the body, potentially leading to more side effects. Co-administration is not recommended.

Lithium: Ketoprofen may increase plasma lithium levels, increasing the risk of lithium toxicity. Monitoring is essential.

Aspirin: Concomitant use may decrease ketoprofen protein binding, thereby increasing its clearance and possibly decreasing its efficacy.

ACE inhibitors: Ketoprofen may reduce the antihypertensive effect of ACE inhibitors, which can increase blood pressure.

Diuretics: Co-administration may decrease diuretic efficacy and increase blood pressure.

Alcohol: There are three known interactions with food and alcohol. Alcohol may increase the risk of gastrointestinal side effects.

USE

Pain Killer

Acute pain: Effective for managing mild to moderate pain, including postoperative pain and pain from injuries.

Chronic pain: Used for chronic conditions such as osteoarthritis and rheumatoid arthritis, helping to reduce pain, swelling, and stiffness.

Inflammatory Conditions

Arthritis: Ketoprofen is commonly prescribed for inflammatory arthritis, including rheumatoid arthritis and osteoarthritis, reducing inflammation and improving joint function.

Dysmenorrhea: It is also used to relieve menstrual pain, providing great relief from the discomfort experienced during menstruation.

Topical Applications

Musculoskeletal pain: Ketoprofen is available in topical formulations (gels, creams, patches) for the local treatment of musculoskeletal pain, such as back pain or tendonitis.

Other Indications

Nerve pain: It can be used to treat nerve pain conditions such as sciatica and postherpetic neuralgia.

Combination therapy: Ketoprofen is sometimes used in combination with other medications (eg, lidocaine or ketamine) to increase pain relief in specific cases.

Veterinary Use

Ketoprofen is also used in veterinary medicine to treat musculoskeletal pain and inflammation in animals, especially horses.