Dexibuprofen

Usage

• Dexibuprofen is prescribed for the symptomatic treatment of mild to moderate pain, including:
  • Osteoarthritis/arthrosis
  • Rheumatoid arthritis (short-term)
  • Primary dysmenorrhea (menstrual pain)
  • Musculoskeletal pain
  • Dental pain
  • Headache
  • Post-operative pain and inflammation
  • Fever (especially in children with upper respiratory tract infections)
• Pharmacological classification: Non-steroidal anti-inflammatory drug (NSAID), analgesic, antipyretic.
• Mechanism of Action: Dexibuprofen is the S(+)-enantiomer of ibuprofen. It inhibits cyclooxygenase (COX) enzymes, primarily COX-2, which are responsible for the production of prostaglandins, mediators of pain, inflammation, and fever. By reducing prostaglandin synthesis, dexibuprofen alleviates these symptoms.

Alternate Names

• S(+)-ibuprofen
• There are numerous brand names worldwide depending on the specific manufacturer and country. Common examples include Seractil, and various generic dexibuprofen formulations.

How It Works

• Pharmacodynamics: Dexibuprofen exerts its analgesic, anti-inflammatory, and antipyretic effects by inhibiting COX enzymes and reducing prostaglandin synthesis. It preferentially inhibits COX-2, although it also has some COX-1 inhibitory activity at higher doses. This preferential COX-2 inhibition is thought to be responsible for its analgesic and anti-inflammatory effects, while its COX-1 inhibition may lead to some side effects, such as gastrointestinal issues.
• Pharmacokinetics:
  • Absorption: Dexibuprofen is rapidly and almost completely absorbed after oral administration. Food may delay the rate but not the extent of absorption. Taking the medication with food is often recommended to minimize gastrointestinal side effects.
  • Metabolism: Dexibuprofen is extensively metabolized in the liver, primarily by CYP2C9 and CYP2C8 enzymes, into inactive metabolites.
  • Elimination: The metabolites are primarily excreted by the kidneys, with a small portion eliminated in the bile. The elimination half-life is approximately 1.8-3.5 hours.
• Mode of Action: Dexibuprofen binds to COX enzymes, preventing the conversion of arachidonic acid to prostaglandins. This inhibition of prostaglandin synthesis is responsible for its therapeutic effects.
• Elimination Pathways: Primarily renal excretion of metabolites, with some hepatic excretion via bile.

Dosage

Standard Dosage

Adults:

• Osteoarthritis/arthrosis, Rheumatoid arthritis: 600-900 mg daily, divided into 2-3 doses. May be increased up to a maximum of 1200 mg daily in acute conditions or exacerbations.
• Mild to moderate pain, Dysmenorrhea: Initially, 200 mg every 4-6 hours as needed. May increase up to 400 mg every 4-6 hours if necessary, not exceeding 1200 mg daily.

Children:

• Use in children under 12 years old is limited and should be guided by a doctor’s recommendation.
• Children 8 years and older: dosing will be based on their age and weight, following the doctors recommendations. For fever caused by upper respiratory tract infection, a dose of 5-7 mg/kg might be sufficient, administered every 6-8 hours. For pain, dose might be 4-10 mg/kg every 6-8 hours.
• Children less than 30 kg should not exceed 300 mg as dexibuprofen per day.

Special Cases:

• Elderly Patients: Start at the lower end of the dosage range and monitor closely for side effects. Dose adjustments may be necessary.
• Patients with Renal Impairment: Reduce initial dosage in mild to moderate renal impairment. Contraindicated in severe renal dysfunction (GFR < 30 mL/min).
• Patients with Hepatic Dysfunction: Start with reduced doses and monitor closely. Contraindicated in severe hepatic dysfunction.
• Patients with Comorbid Conditions: Careful monitoring is needed for patients with cardiovascular disease, hypertension, gastrointestinal disorders, or bleeding disorders.

Clinical Use Cases

Dosage in specific clinical settings should be determined by the treating physician based on patient factors, severity of condition, and response to therapy. The dosages mentioned above for adults and children under standard dosage can be used as reference, with possible adjustments for renal/hepatic dysfunction and other patient factors.

Dosage Adjustments

Dose modifications are necessary for elderly patients, patients with renal or hepatic dysfunction, and those with other comorbid conditions.

Side Effects

Common Side Effects:

• Dyspepsia, heartburn, nausea, vomiting, diarrhea, abdominal pain or discomfort, headache, dizziness, fatigue, skin rash.

Rare but Serious Side Effects:

• Gastrointestinal bleeding or ulceration, renal impairment, fluid retention, edema, hypertension, heart failure exacerbation, allergic reactions (including angioedema and anaphylaxis), blood dyscrasias (e.g., thrombocytopenia, anemia).

Long-Term Effects:

• With chronic use, particularly at higher doses, potential for gastrointestinal complications, renal dysfunction, cardiovascular events.

Adverse Drug Reactions (ADR):

• Any signs of gastrointestinal bleeding (e.g., hematemesis, melena), allergic reactions, severe skin reactions, signs of renal impairment should prompt immediate medical attention.

Contraindications

• Hypersensitivity to dexibuprofen or other NSAIDs.
• History of asthma, bronchospasm, urticaria, or angioedema triggered by NSAIDs.
• Active or history of recurrent peptic ulcer/gastrointestinal bleeding.
• Severe heart failure.
• Severe renal or hepatic impairment.
• Third trimester of pregnancy.
• Bleeding disorders.

Drug Interactions

• Anticoagulants (e.g., warfarin, heparin): Increased risk of bleeding.
• Antihypertensives (e.g., ACE inhibitors, beta-blockers, diuretics): Reduced antihypertensive effect.
• Other NSAIDs (including aspirin): Increased risk of gastrointestinal and cardiovascular side effects.
• Lithium, Digoxin, Methotrexate, Phenytoin: Increased plasma levels and risk of toxicity.
• Corticosteroids: Increased risk of gastrointestinal ulceration and bleeding.
• Immunosuppressants (e.g., cyclosporine, tacrolimus): Increased risk of nephrotoxicity.
• Alcohol: Can worsen gastrointestinal side effects.

Pregnancy and Breastfeeding

• Pregnancy Safety Category: Avoid during the third trimester. Use with caution during the first and second trimesters, if clearly needed, and at the lowest effective dose for the shortest duration. Consult a doctor before use.
• Breastfeeding: Small amounts of dexibuprofen are excreted in breast milk. Generally considered safe for short-term use at recommended doses. Monitor infant for any adverse effects.

Drug Profile Summary

• Mechanism of Action: COX-2 inhibitor, reducing prostaglandin synthesis.
• Side Effects: Dyspepsia, nausea, vomiting, GI bleeding (rare), renal impairment (rare).
• Contraindications: Hypersensitivity to NSAIDs, active peptic ulcer, severe heart failure, severe renal/hepatic impairment.
• Drug Interactions: Anticoagulants, antihypertensives, other NSAIDs.
• Pregnancy & Breastfeeding: Avoid in the 3rd trimester, use with caution during 1st and 2nd trimesters. Generally considered safe during breastfeeding if used short-term and at recommended doses.
• Dosage: Adults: 600-1200 mg daily divided; Children (8-12 years): consult a physician.
• Monitoring Parameters: Renal function, blood pressure, signs of GI bleeding.

Popular Combinations

Not applicable. Combination therapy with other analgesics or NSAIDs is generally avoided due to the increased risk of side effects.

Precautions

• Pre-existing medical conditions should be thoroughly evaluated before prescribing dexibuprofen.
• Specific Populations: Monitor elderly patients, and those with renal or hepatic impairments closely. Avoid use in the third trimester of pregnancy.
• Lifestyle Considerations: Limit alcohol consumption to minimize gastrointestinal irritation.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Dexibuprofen?

A: Adults: 600-900 mg daily for osteoarthritis/RA, up to 1200 mg daily for acute pain. Mild to moderate pain: 200-400 mg every 4-6 hours, not exceeding 1200 mg/day. Children: limited use and dose needs to be determined by the treating physician.

Q2: What are the common side effects of Dexibuprofen?

A: Dyspepsia, nausea, heartburn, diarrhea, headache, dizziness.

Q3: Is Dexibuprofen safe during pregnancy?

A: Avoid during the third trimester. Use with caution and under medical supervision during the first and second trimesters if benefits outweigh risks.

Q4: How does Dexibuprofen differ from Ibuprofen?

A: Dexibuprofen is the S(+)-enantiomer of ibuprofen, thought to be the more active form. It preferentially inhibits COX-2, which can potentially lead to a more favourable side effect profile.

Q5: What are the contraindications for Dexibuprofen use?

A: Hypersensitivity to NSAIDs, active peptic ulcer disease, severe heart failure, severe renal/hepatic impairment, bleeding disorders, third trimester of pregnancy.

Q6: Can Dexibuprofen be used in children?

A: It is generally recommended to use under a doctor’s recommendations. Dosage should be adjusted to the child’s weight and age.

Q7: What should I do if a patient experiences gastrointestinal bleeding while taking Dexibuprofen?

A: Discontinue the drug immediately and provide supportive care. Contact a gastroenterologist for further management.

Q8: Does Dexibuprofen interact with other medications?

A: Yes, it can interact with anticoagulants, antihypertensives, other NSAIDs, lithium, digoxin, and methotrexate. Consult with the patient’s medication list to identify potential interactions.

Q9: How should I counsel patients taking Dexibuprofen?

A: Advise patients to take the medication with food to minimize GI side effects, report any unusual symptoms (e.g., black stools, severe abdominal pain), and avoid concurrent use of other NSAIDs.

Q10: Are there any long-term risks associated with Dexibuprofen use?

A: Long-term use, especially at higher doses, can increase the risk of GI complications, renal dysfunction, and cardiovascular events. Monitor patients regularly.