Usage
This combination medication is primarily prescribed for managing pain and inflammation associated with musculoskeletal disorders such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, tendinitis, bursitis, and soft tissue injuries (sprains and strains). It’s also used for post-operative and post-traumatic inflammation, dental pain, and pain in the ear and throat.
Its pharmacological classifications include:
- Analgesic: Relieves pain.
- Anti-inflammatory: Reduces inflammation.
- Proteolytic enzyme combination: Facilitates the breakdown of proteins involved in inflammation.
The mechanism of action involves multiple pathways:
- Aceclofenac (NSAID): Inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby diminishing pain and inflammation.
- Bromelain and Trypsin: These proteolytic enzymes break down proteins in damaged tissues, reducing swelling and promoting healing. They also enhance blood flow to the inflamed areas.
- Rutoside (Flavonoid): Exerts antioxidant effects, protecting cells from free radical damage, and contributes to reducing inflammation.
- Beta-cyclodextrin: Improves the solubility and absorption of Aceclofenac, increasing its efficacy.
Alternate Names
- Bextrin Total Capsule
- Rutoheal
- Flammar 3D
How It Works
Pharmacodynamics:
- Aceclofenac: Exerts its analgesic and anti-inflammatory effects by inhibiting COX-1 and COX-2 enzymes, reducing prostaglandin production.
- Bromelain and Trypsin: Facilitate the breakdown of fibrin, a protein involved in inflammation and blood clotting, and decrease bradykinin levels, further contributing to pain reduction.
- Rutoside: Stabilizes cell membranes, reduces capillary permeability, and scavenges free radicals, mitigating inflammation.
- Beta-cyclodextrin: Through complexation with Aceclofenac, it improves its solubility, dissolution rate, and bioavailability.
Pharmacokinetics:
- Aceclofenac: Well-absorbed orally, reaching peak plasma concentrations in 1-3 hours. Metabolized in the liver, primarily by CYP2C9, and excreted mainly through the kidneys.
- Bromelain and Trypsin: Absorbed through the gastrointestinal tract, though the extent of absorption varies. Metabolized by proteases in the body.
- Rutoside: Undergoes limited absorption in the gut. Metabolized in the liver and intestines.
- Beta-cyclodextrin: Minimally absorbed, primarily excreted unchanged in feces.
Mode of Action:
The combined action of these components provides synergistic effects in reducing pain and inflammation. Aceclofenac targets the COX enzymes, while bromelain, trypsin, and rutoside modulate various inflammatory pathways and reduce oxidative stress. Beta-cyclodextrin’s role is to improve the delivery of Aceclofenac.
Dosage
Dosage should be individualized based on patient condition, age, and other factors. Always refer to specific product labeling.
Standard Dosage
Adults:
The typical adult dose is one tablet or capsule twice daily, taken orally, although this can vary.
Children:
Generally not recommended for children under 12. For adolescents (over 12 years), dosage should be determined by a physician.
Special Cases:
- Elderly Patients: Initiate with a lower dose and monitor closely for adverse effects.
- Patients with Renal Impairment: Dose adjustment is usually necessary, with careful monitoring of renal function.
- Patients with Hepatic Dysfunction: Lower doses are advised with hepatic function monitoring.
- Patients with Comorbid Conditions: Careful evaluation and potential dose adjustments are essential, especially for those with cardiovascular disease, diabetes, or gastrointestinal disorders.
Clinical Use Cases
Dosage for specific clinical settings (intubation, surgical procedures, mechanical ventilation, ICU use, emergencies) isn’t explicitly defined and requires clinical judgment based on patient needs.
Dosage Adjustments
Dose modifications may be required based on individual factors, such as renal or hepatic function, concurrent medications, and response to therapy. Genetic polymorphisms affecting drug metabolism may also influence dosing.
Side Effects
Common Side Effects:
- Nausea
- Vomiting
- Diarrhea
- Indigestion
- Abdominal pain
- Headache
- Dizziness
- Drowsiness
- Fatigue
Rare but Serious Side Effects:
- Gastrointestinal bleeding or ulceration
- Allergic reactions (rash, itching, swelling)
- Liver damage
- Kidney impairment
- Cardiovascular events (thrombotic events)
Long-Term Effects:
- Increased risk of gastrointestinal issues with prolonged NSAID use.
- Potential for renal or hepatic dysfunction with chronic use.
Adverse Drug Reactions (ADR):
- Anaphylaxis
- Stevens-Johnson syndrome
- Toxic epidermal necrolysis
Contraindications
- Hypersensitivity to any component
- Active gastrointestinal bleeding or ulceration
- Severe hepatic or renal impairment
- History of asthma, urticaria, or allergic reactions to NSAIDs or aspirin
- Coronary artery bypass graft surgery
- Hemophilia
Drug Interactions
- Other NSAIDs (ibuprofen, naproxen): Increased risk of gastrointestinal side effects
- Corticosteroids (prednisone): Increased risk of GI bleeding
- Anticoagulants (warfarin): Increased bleeding risk
- Antiplatelet agents (clopidogrel): Increased bleeding risk
- Diuretics (furosemide): Reduced diuretic effect and increased risk of renal impairment
- ACE inhibitors (lisinopril): Reduced antihypertensive effect and increased risk of renal impairment
- Lithium: Increased lithium levels
- Methotrexate: Increased methotrexate toxicity
- Cyclosporine: Increased cyclosporine levels
- Alcohol: Increased risk of GI bleeding
Pregnancy and Breastfeeding
Use during pregnancy, especially the third trimester, and breastfeeding is generally not recommended due to potential risks to the fetus or infant.
Drug Profile Summary
- Mechanism of Action: Aceclofenac inhibits prostaglandin synthesis; bromelain and trypsin break down proteins and reduce inflammation; rutoside is an antioxidant; beta-cyclodextrin enhances Aceclofenac’s effects.
- Side Effects: Nausea, vomiting, diarrhea, indigestion, abdominal pain, headache, dizziness, allergic reactions, GI bleeding.
- Contraindications: Hypersensitivity, active GI bleeding, severe liver/kidney disease, history of asthma/urticaria/NSAID allergy.
- Drug Interactions: Other NSAIDs, anticoagulants, corticosteroids, alcohol.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: Varies, typically one tablet/capsule twice daily for adults. Consult product information.
- Monitoring Parameters: Liver and kidney function tests, signs of GI bleeding.
Popular Combinations
This medication itself is a combination product. Additional combinations are not typically recommended without careful consideration.
Precautions
- Pre-existing cardiovascular, hepatic, and renal disease
- Asthma or other respiratory conditions
- Coagulation disorders
- Gastrointestinal disorders
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aceclofenac + Beta-Cyclodextrin + Bromelain + Rutoside + Trypsin?
A: The usual adult dosage is one tablet or capsule twice daily. However, dosage should be individualized based on the patient’s condition. Pediatric dosages should be determined by a physician.
Q2: What are the common side effects?
A: Common side effects include nausea, vomiting, diarrhea, indigestion, abdominal pain, headache, and dizziness.
Q3: What are the serious side effects?
A: Serious side effects include GI bleeding, allergic reactions, liver damage, kidney impairment, and cardiovascular events.
Q4: What are the contraindications for this medication?
A: Contraindications include hypersensitivity to any component, active GI bleeding, severe hepatic or renal impairment, history of asthma/urticaria/NSAID allergy, coronary artery bypass graft surgery, and hemophilia.
Q5: Can this medication be used during pregnancy or breastfeeding?
A: It is generally not recommended during pregnancy, especially in the third trimester, or breastfeeding, due to potential risks to the fetus or infant.
Q6: What are the key drug interactions?
A: Significant interactions can occur with other NSAIDs, corticosteroids, anticoagulants, antiplatelet agents, some antihypertensives, lithium, methotrexate, cyclosporine, and alcohol.
Q7: What conditions does this medication treat?
A: Primarily used to treat pain and inflammation associated with musculoskeletal disorders like osteoarthritis, rheumatoid arthritis, and soft tissue injuries.
Q8: How should this medication be taken?
A: Orally, with or without food, but preferably at a fixed time each day. Tablets or capsules should be swallowed whole and not crushed or chewed.
Q9: What should patients be monitored for while taking this medication?
A: Monitor for liver and kidney function, any signs of gastrointestinal bleeding, and any allergic reactions.
