Usage
Diclofenac + Rabeprazole is a combination medication prescribed for the management of pain and inflammation in musculoskeletal and joint conditions, such as osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. It is also used for acute musculoskeletal pain, postoperative pain, migraine attacks, and primary dysmenorrhea (painful menstruation). The addition of Rabeprazole, a proton pump inhibitor (PPI), helps protect the stomach lining from potential damage caused by Diclofenac, a non-steroidal anti-inflammatory drug (NSAID).
Pharmacological Classification:
- Diclofenac: Non-Steroidal Anti-inflammatory Drug (NSAID)
- Rabeprazole: Proton Pump Inhibitor (PPI)
Mechanism of Action: Diclofenac works by inhibiting cyclooxygenase (COX) enzymes, which are responsible for producing prostaglandins, mediators of pain and inflammation. Rabeprazole reduces stomach acid production by inhibiting the H+/K+-ATPase enzyme system in gastric parietal cells.
Alternate Names
While “Diclofenac + Rabeprazole” is the standard generic name, several brand names exist depending on the manufacturer and region. Some examples include Rclonac, Drab, Rabin-DFX, Safediclo, and Samurai. International variations may also exist.
How It Works
Pharmacodynamics: Diclofenac reduces pain and inflammation by blocking COX enzymes and decreasing prostaglandin synthesis. Rabeprazole suppresses gastric acid secretion, protecting the stomach lining from NSAID-induced damage.
Pharmacokinetics:
- Diclofenac: Rapidly absorbed, extensively protein-bound, short half-life. Usually administered in divided doses. Metabolized by the liver and excreted primarily through the kidneys.
- Rabeprazole: Administered once daily. Acid-labile with approximately 58% oral bioavailability. Food can delay time to peak plasma concentration but generally does not affect overall absorption. Metabolized by CYP enzymes, primarily CYP2C19 and CYP3A4, with renal excretion of metabolites.
Mode of Action: Diclofenac inhibits COX-1 and COX-2 enzymes. Rabeprazole irreversibly binds to the H+/K+-ATPase pump in gastric parietal cells.
Elimination Pathways: Diclofenac: primarily renal excretion. Rabeprazole: primarily renal excretion of metabolites.
Dosage
Standard Dosage
Adults: Diclofenac 100mg SR + Rabeprazole 20mg once daily.
Children: Contraindicated. This combination is not recommended for use in children.
Special Cases:
- Elderly Patients: Initiate therapy at the lowest dose due to potentially decreased renal and hepatic function. Monitor closely for adverse events.
- Patients with Renal Impairment: Dose adjustment may be necessary. Consult current guidelines for specific recommendations.
- Patients with Hepatic Dysfunction: Dose adjustment may be necessary. Close monitoring is recommended.
- Patients with Comorbid Conditions: Use with caution in patients with hypertension, heart disease, or history of gastrointestinal diseases.
Clinical Use Cases
The provided sources primarily focus on the use of Diclofenac + Rabeprazole for managing pain and inflammation in musculoskeletal conditions. Dosage in specialized settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations is not explicitly addressed in the sources and should be determined on a case-by-case basis under the guidance of a specialist.
Dosage Adjustments
Dosage adjustments should be made based on individual patient characteristics, including renal function, hepatic function, age, and the presence of other medical conditions. Monitor patients closely for adverse events and adjust the dose accordingly.
Side Effects
Common Side Effects: Dyspepsia, abdominal pain, nausea, headache, dizziness.
Rare but Serious Side Effects: Gastrointestinal bleeding, peptic ulcers, nephrotoxicity, hepatic dysfunction, cardiovascular events (heart attack, stroke).
Long-Term Effects: Potential long-term side effects include osteoporosis, gastric cancer.
Adverse Drug Reactions (ADR): Severe allergic reactions (anaphylaxis), Stevens-Johnson syndrome, toxic epidermal necrolysis.
Contraindications
- Hypersensitivity to diclofenac, rabeprazole, or any components of the formulation.
- Active gastric or duodenal ulcers.
- Severe liver or kidney disease.
- Congestive heart failure (NYHA Class II-IV).
- Asthma, urticaria, or allergic reactions to aspirin or other NSAIDs.
- Third trimester of pregnancy.
Drug Interactions
Diclofenac + Rabeprazole can interact with several medications, including:
- Other NSAIDs (ketorolac, celecoxib, aspirin, ibuprofen).
- Anticoagulants (warfarin, apixaban).
- Anticancer drugs (methotrexate).
- Lithium.
- Antihypertensives (ramipril).
- CYP2C19 and CYP3A4 inhibitors/inducers (fluconazole, rifampin).
Alcohol should be avoided as it can increase the risk of drowsiness, dizziness, and stomach bleeding. Consult current drug interaction resources for a comprehensive list.
Pregnancy and Breastfeeding
Pregnancy: Diclofenac is contraindicated during the third trimester. Its use in earlier stages of pregnancy should be avoided unless the benefits outweigh the risks. Rabeprazole’s safety in pregnancy is not well-established. Consult alternative treatment options.
Breastfeeding: Diclofenac is generally considered compatible with breastfeeding. Rabeprazole’s excretion in breast milk is unknown, but it is likely to be in small amounts. Consult recommendations regarding the use of this combination during lactation.
Drug Profile Summary
- Mechanism of Action: Diclofenac: COX inhibitor, reducing prostaglandins; Rabeprazole: PPI, inhibits gastric acid secretion.
- Side Effects: Dyspepsia, abdominal pain, nausea, headache, dizziness, GI bleeding (rare).
- Contraindications: Hypersensitivity, peptic ulcer, severe liver/kidney disease, pregnancy (3rd trimester).
- Drug Interactions: NSAIDs, anticoagulants, lithium, CYP2C19/3A4 inhibitors/inducers.
- Pregnancy & Breastfeeding: Consult guidelines for specific recommendations.
- Dosage: Adults: Diclofenac 100mg SR + Rabeprazole 20mg once daily. Children: Contraindicated.
- Monitoring Parameters: Renal and liver function, blood pressure, signs of GI bleeding.
Popular Combinations
The primary focus is on the fixed combination of Diclofenac and Rabeprazole. Specific information on alternative combinations is not provided in the current source material.
Precautions
Screen patients for allergies, metabolic disorders, and organ dysfunction before initiating treatment. Use with caution in pregnant/breastfeeding women, children, and the elderly. Advise patients against driving or operating machinery if dizziness or drowsiness occurs.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Rabeprazole?
A: The standard adult dose is Diclofenac 100mg SR + Rabeprazole 20mg once daily. It is contraindicated in children.
Q2: What are the primary uses of this medication?
A: Primarily used to treat pain and inflammation associated with conditions like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and other musculoskeletal disorders.
Q3: What are the common side effects?
A: Common side effects include dyspepsia, abdominal pain, nausea, headache, and dizziness.
Q4: Are there any serious side effects?
A: Yes, although rare, serious side effects can include gastrointestinal bleeding, peptic ulcers, kidney problems, and liver damage.
Q5: Can this medicine be used during pregnancy?
A: It is contraindicated in the third trimester of pregnancy. Use in the first and second trimester should be limited and only when benefits clearly outweigh risks.
Q6: Is it safe to breastfeed while taking this medication?
A: Limited information is available regarding rabeprazole. Diclofenac is generally considered safe during breastfeeding. Consult guidelines and alternative options.
Q7: Does this medication interact with other drugs?
A: Yes, it can interact with several medications, including other NSAIDs, anticoagulants, and certain antidepressants. Provide a complete medication history before prescribing.
Q8: What precautions should be taken while using this drug?
A: Patients should be screened for pre-existing conditions. Avoid alcohol. Exercise caution while driving or operating machinery due to potential dizziness. Report any unusual symptoms to the physician.
Q9: Can I take this medication if I have a history of stomach ulcers?
A: No. Active peptic ulcers are a contraindication for this medication.
Q10: Should this medication be taken with food?
A: It can be taken with or without food. However, taking with food might help reduce some gastrointestinal side effects.