Actidex

Approved Indications:

• Acute Pain Management: Treatment of mild to moderate acute pain, including dental pain, musculoskeletal pain, and postoperative pain.
• Dysmenorrhea: Relief of primary dysmenorrhea (menstrual pain).
• Inflammatory Conditions: Management of pain and inflammation in conditions such as strains, sprains, and soft tissue injuries.
• Fever Reduction: Used in some regions for antipyretic purposes.

Off-label or Clinically Accepted Uses:

• Pain associated with osteoarthritis and rheumatoid arthritis (limited use depending on local approvals).
• Acute exacerbations of chronic musculoskeletal disorders.

Adults:

• Oral Tablets: 25 mg orally every 8 hours as needed. Maximum daily dose generally not to exceed 75 mg.
• Oral Solution: Dosage similar to tablets, adjusted per mg/kg in some cases.
• Intramuscular (IM) or Intravenous (IV) Injection: 50 mg as a single dose or divided doses; frequency based on clinical condition, not exceeding 150 mg/day.

Pediatrics:

• Safety and efficacy not well established in children under 16 years; use only if benefits outweigh risks and under specialist guidance.

Elderly:

• Use the lowest effective dose; increased risk of adverse effects; monitor renal function.

Renal Impairment:

• Use with caution in mild to moderate renal impairment; avoid in severe renal impairment or end-stage renal disease.

Hepatic Impairment:

• Use with caution in mild to moderate hepatic impairment; contraindicated in severe hepatic dysfunction.

Administration Notes:

• Oral: Swallow tablets whole with water, preferably after meals to reduce gastrointestinal irritation.
• Parenteral: Administer IM or IV as per product instructions by trained healthcare professionals.

Dexketoprofen is the active S-enantiomer of ketoprofen, classified as a nonsteroidal anti-inflammatory drug (NSAID). It works by reversibly inhibiting cyclooxygenase (COX) enzymes COX-1 and COX-2, which are responsible for the conversion of arachidonic acid to prostaglandins. Prostaglandins mediate inflammation, pain, and fever. By reducing prostaglandin synthesis, dexketoprofen exerts analgesic, anti-inflammatory, and antipyretic effects, thereby alleviating pain and reducing inflammation in affected tissues.

• Absorption: Rapidly absorbed after oral administration with peak plasma concentrations reached within 30 minutes to 1 hour. Oral bioavailability is high.
• Distribution: Widely distributed in body tissues; plasma protein binding is approximately 99%, primarily to albumin.
• Metabolism: Extensively metabolized in the liver mainly by conjugation and hydroxylation pathways.
• Half-life: Approximately 1 to 2 hours.
• Excretion: Primarily excreted via the kidneys as metabolites and unchanged drug (about 70% renal, 30% fecal).

• Pregnancy: Classified as FDA Category C. Use during the third trimester is contraindicated due to risk of premature closure of the fetal ductus arteriosus and other fetal complications. Use in the first and second trimesters only if clearly needed and under medical supervision.
• Lactation: Dexketoprofen is excreted into breast milk in small amounts. Caution is advised; breastfeeding mothers should avoid the drug or monitor infants for adverse effects.

• Primary Class: Nonsteroidal Anti-inflammatory Drug (NSAID)
• Subclass: Propionic acid derivative

• Known hypersensitivity to dexketoprofen, ketoprofen, other NSAIDs, or any excipients.
• History of bronchospasm, urticaria, or allergic-type reactions after aspirin or NSAID administration.
• Active or history of recurrent gastrointestinal bleeding or ulcers.
• Severe hepatic, renal, or cardiac impairment.
• Third trimester of pregnancy.
• Concurrent use with other NSAIDs or anticoagulants without medical supervision.

• High-Risk Patients: Elderly, patients with cardiovascular disease, hypertension, renal or hepatic impairment.
• Gastrointestinal Risk: Increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation, which can be fatal.
• Cardiovascular Risk: NSAIDs may increase the risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke.
• Renal Effects: Can cause renal toxicity, especially in patients with preexisting renal impairment or dehydration.
• Hypersensitivity: Monitor for signs of allergic reactions including anaphylaxis.
• Monitoring: Regular monitoring of renal, hepatic function and blood pressure is recommended during prolonged therapy.

Common:

• Gastrointestinal: Nausea, dyspepsia, abdominal pain, diarrhea, flatulence.
• Central Nervous System: Headache, dizziness.
• Skin: Rash, pruritus.

Serious/Rare:

• Gastrointestinal bleeding, ulceration, or perforation.
• Severe hypersensitivity reactions, including anaphylaxis and Stevens-Johnson syndrome.
• Renal impairment or failure.
• Elevated liver enzymes or hepatitis.
• Cardiovascular events (myocardial infarction, stroke).

• Anticoagulants/Antiplatelets: Increased risk of bleeding.
• Other NSAIDs or Corticosteroids: Increased risk of gastrointestinal toxicity.
• ACE Inhibitors/ARBs: Reduced antihypertensive effect and increased risk of renal impairment.
• Diuretics: Risk of renal toxicity increased.
• Lithium and Methotrexate: Increased plasma concentrations and potential toxicity.
• Alcohol: Concomitant use increases gastrointestinal irritation and bleeding risk.

• Current guidelines recommend using the lowest effective dose for the shortest duration necessary to minimize adverse effects.
• Emphasis on caution in cardiovascular and gastrointestinal risk patients.
• Avoid use in late pregnancy due to fetal risk.
• Ongoing review of NSAIDs for cardiovascular safety; dexketoprofen generally considered to have a safety profile similar to other NSAIDs.

• Store at controlled room temperature between 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep tablets in original packaging until use.
• Do not freeze.
• Keep out of reach of children.