FASTUM GEL

Indications

• Pain and inflammation in musculoskeletal disorders
• Rheumatoid arthritis
• Osteoarthritis
• Dysmenorrhea
• Moderate pain relief

Mechanism of action

Ketoprofen's anti-inflammatory effects are primarily due to the inhibition of cyclooxygenase-2 (COX-2), an enzyme crucial for prostaglandin synthesis in the arachidonic acid pathway. This leads to reduced levels of prostaglandins, which mediate pain, fever, and inflammation. Ketoprofen also inhibits cyclooxygenase-1 (COX-1), contributing to its side effects such as gastrointestinal discomfort and ulceration. Additionally, it exhibits anti-bradykinin activity and stabilizes lysosomal membranes. Its antipyretic effects may involve action on the hypothalamus, enhancing peripheral blood flow, vasodilation, and heat dissipation.

Pharmacodynamics

As a nonsteroidal anti-inflammatory agent (NSAIA), ketoprofen shares pharmacological actions with other typical NSAIDs by inhibiting prostaglandin synthesis. It is effective in treating various conditions, including rheumatoid arthritis, osteoarthritis, and dysmenorrhea, and is used to alleviate moderate pain, thus providing both analgesic and anti-inflammatory effects.

Pharmacokinetics

Ketoprofen is absorbed from the gastrointestinal tract, with peak plasma concentrations typically reached within 1 to 2 hours after oral administration. It is extensively metabolized in the liver, primarily through conjugation, and excreted mainly via the urine. The drug has a half-life of approximately 1.5 to 2 hours, but this may vary based on individual factors such as age and liver function. Caution is advised in patients with hepatic or renal impairment, as these conditions may alter the drug's pharmacokinetics and increase the risk of adverse effects.

Contra-indications

• History of gastrointestinal perforation or ulceration
• Severe heart failure
• History of hypersensitivity to aspirin or other NSAIDs

Adverse effects

• Gastrointestinal discomfort
• Nausea
• Constipation
• Dizziness
• Drowsiness
• Fatigue
• Headache
• Rash
• Paraesthesia
• Skin reactions
• Increased risk of infection
• Angioedema
• Renal impairment
• Hypersensitivity reactions
• Photosensitivity
• Hematologic disorders
• Stomatitis
• Tinnitus
• Vision disorders
• Weight increase

Interactions

• May affect performance of skilled tasks such as driving
• Other NSAIDs may increase the risk of adverse effects

Precautions

• Caution in patients with dehydration or renal impairment
• Use with caution in elderly patients due to increased risk of serious side effects
• Careful monitoring required for prolonged therapy
• Caution advised in patients with a history of gastrointestinal disorders

Pregnancy

Avoid unless the potential benefit outweighs the risk. Avoid during the third trimester due to risk of fetal ductus arteriosus closure.

Breast-feeding

Amount probably too small to be harmful, but use with caution and avoid large amounts.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Oral suspension
• Oral solution
• Suppositories

Mechanism of action

The anti-inflammatory effects of ketoprofen are believed to be due to inhibition cylooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. Ketoprofen is a non-specific cyclooxygenase inhibitor and inhibition of COX-1 is thought to confer some of its side effects, such as GI upset and ulceration. Ketoprofen is thought to have anti-bradykinin activity, as well as lysosomal membrane-stabilizing action. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

Pharmacodynamics

Ketoprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties. Ketoprofen has pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. Ketoprofen is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and alleviate moderate pain.