Usage
This combination medication is primarily prescribed for managing pain, inflammation, and edema associated with various musculoskeletal conditions, such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, tendonitis, bursitis, and soft tissue injuries (sprains, strains). It is also used to manage post-operative and post-traumatic swelling, sports injuries, and pain associated with dental procedures, muscle aches, back pain, earaches, throat pain and high fever.
It is classified pharmacologically as an analgesic, anti-inflammatory, and proteolytic enzyme combination.
The mechanism of action involves multiple pathways: Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, which are mediators of pain and inflammation. Bromelain and Trypsin are proteolytic enzymes that break down proteins involved in the inflammatory process, promoting tissue repair and reducing swelling. Rutoside, a flavonoid, acts as an antioxidant and anti-inflammatory agent by neutralizing free radicals and strengthening blood vessels.
Alternate Names
No internationally recognized alternate names exist for this specific combination. However, it is often referred to as a proteolytic enzyme and NSAID combination.
Brand names for this combination vary depending on the manufacturer. A few examples are: Kritheal-D, RutoMor-D, Chymoral BR
How It Works
Pharmacodynamics: Diclofenac reduces pain and inflammation by inhibiting COX enzymes and prostaglandin synthesis. Trypsin and Bromelain exert anti-inflammatory effects by breaking down inflammatory mediators and promoting tissue healing. Rutoside reinforces capillary walls, improves microcirculation, and provides antioxidant benefits.
Pharmacokinetics: Diclofenac is well-absorbed orally, metabolized primarily in the liver by CYP enzymes (mainly CYP2C9), and excreted mainly through the kidneys. Bromelain and Trypsin are absorbed to some extent in the gastrointestinal tract. Rutoside is also absorbed orally and metabolized in the liver. Elimination pathways for Bromelain, Trypsin, and Rutoside are not fully characterized but likely involve a combination of renal and hepatic routes.
Mode of Action: Diclofenac acts by inhibiting COX-1 and COX-2 enzymes, thereby reducing prostaglandin synthesis. Trypsin and Bromelain catalyze the breakdown of proteins involved in inflammation. Rutoside acts as an antioxidant and may also inhibit some inflammatory enzymes.
Receptor Binding/Enzyme Inhibition: Diclofenac inhibits COX enzymes. Trypsin and Bromelain are proteolytic enzymes. Rutoside does not have specific receptor binding but exhibits antioxidant effects.
Elimination Pathways: Diclofenac is mainly excreted renally. Bromelain, Trypsin, and Rutoside elimination pathways are not fully elucidated.
Dosage
Standard Dosage
Adults: The standard dose is one tablet two to three times daily, preferably after meals, or as directed by the physician.
Children: Not recommended for children below 12 years of age.
Special Cases:
- Elderly Patients: Dose adjustment may be necessary based on renal and hepatic function.
- Patients with Renal Impairment: Dose reduction or less frequent dosing may be needed.
- Patients with Hepatic Dysfunction: Dose reduction should be considered.
- Patients with Comorbid Conditions: Caution is advised in patients with a history of gastrointestinal ulcers, bleeding disorders, cardiovascular disease, or asthma.
Clinical Use Cases
Dosage in specific clinical scenarios like intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations should be determined by the treating physician based on individual patient needs. Generally, the standard dosage guidelines are followed, with adjustments if necessary.
Dosage Adjustments
Dose adjustments are necessary for renal or hepatic impairment, elderly patients, and those with comorbid conditions. Individualized dosing based on patient-specific factors is crucial.
Side Effects
Common Side Effects:
Nausea, vomiting, heartburn, indigestion, diarrhea, loss of appetite, stomach pain, headache, dizziness, skin rash.
Rare but Serious Side Effects:
Allergic reactions (e.g., anaphylaxis, angioedema), gastrointestinal bleeding, peptic ulcer, Stevens-Johnson syndrome, acute renal failure, hepatotoxicity.
Long-Term Effects:
With prolonged use of NSAIDs like Diclofenac, potential long-term effects include cardiovascular risks (e.g., myocardial infarction, stroke), renal impairment, and gastrointestinal complications.
Adverse Drug Reactions (ADR):
Any severe or persistent side effects, including signs of allergic reactions or gastrointestinal bleeding, should be considered an ADR and reported to the treating physician immediately.
Contraindications
Absolute contraindications include hypersensitivity to any component of the drug, active peptic ulcer disease, severe hepatic impairment, severe renal impairment, aspirin triad (asthma, nasal polyps, and aspirin sensitivity). Relative contraindications include history of gastrointestinal bleeding, coagulation disorders, pregnancy, and breastfeeding.
Drug Interactions
Clinically significant interactions can occur with anticoagulants (warfarin, aspirin), other NSAIDs, corticosteroids, antihypertensives (ACE inhibitors, diuretics), lithium, methotrexate, and some antibiotics. Alcohol should be avoided as it may increase the risk of gastrointestinal bleeding.
Pregnancy and Breastfeeding
This combination is generally contraindicated during pregnancy, particularly in the third trimester, due to the risk of premature closure of the ductus arteriosus and other fetal complications associated with NSAID use. It is also advised to avoid this combination during breastfeeding, as Diclofenac is excreted in breast milk and may pose risks to the newborn.
Drug Profile Summary
- Mechanism of Action: Diclofenac: COX inhibitor; Bromelain and Trypsin: proteolytic enzymes; Rutoside: antioxidant and anti-inflammatory.
- Side Effects: Nausea, vomiting, gastrointestinal upset, headache, dizziness, allergic reactions.
- Contraindications: Hypersensitivity, active peptic ulcer, severe hepatic/renal impairment, pregnancy (third trimester).
- Drug Interactions: Anticoagulants, NSAIDs, corticosteroids, antihypertensives, lithium.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: One tablet two to three times daily after meals. Children: Not recommended.
- Monitoring Parameters: Renal function, liver function, signs of gastrointestinal bleeding.
Popular Combinations
This combination itself is a popular combination used in clinical practice to address inflammation, pain, and swelling in musculoskeletal conditions.
Precautions
- General Precautions: Evaluate renal and hepatic function before initiating therapy.
- Specific Populations: Avoid in pregnancy and breastfeeding. Use with caution in elderly patients and those with pre-existing medical conditions.
- Lifestyle Considerations: Avoid alcohol. Avoid driving or operating machinery if experiencing dizziness or drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Bromelain + Diclofenac + Rutoside + Trypsin?
A: The standard adult dose is one tablet two to three times a day, preferably after meals. Dosages should be adjusted for patients with renal or hepatic impairment. Not recommended for children under 12 years.
Q2: What are the common side effects?
A: Common side effects include nausea, vomiting, heartburn, indigestion, diarrhea, stomach pain, headache, and dizziness.
Q3: Is this medication safe during pregnancy?
A: No, this medication is contraindicated during pregnancy, particularly in the third trimester, due to potential risks to the fetus.
Q4: Can I take this medication if I have a history of stomach ulcers?
A: This medication is contraindicated in patients with active peptic ulcers. Caution is advised in those with a history of ulcers.
Q5: What are the potential drug interactions?
A: This drug may interact with anticoagulants, other NSAIDs, corticosteroids, antihypertensives, and lithium. Inform your doctor about all medications you are taking.
Q6: How does this combination medication work?
A: Diclofenac reduces pain and inflammation, Bromelain and Trypsin break down inflammatory proteins, and Rutoside protects against free radicals and strengthens capillaries.
Q7: Can I drink alcohol while taking this medication?
A: Alcohol should be avoided as it can increase the risk of gastrointestinal side effects and may interact with Diclofenac.
Q8: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.
Q9: Are there any long-term risks associated with this medication?
A: Long-term use of NSAIDs like Diclofenac carries potential cardiovascular and renal risks. Regular monitoring is important.
