Usage
- Aflapin, a standardized extract of Boswellia serrata gum resin, is primarily prescribed for the management of Osteoarthritis (OA), particularly OA of the knee. It is also used for other inflammatory conditions like rheumatoid arthritis.
- Pharmacological Classification: Nutritional supplement, anti-inflammatory agent.
- Mechanism of Action: Aflapin acts as a selective and potent 5-lipoxygenase (5-LOX) inhibitor. 5-LOX is an enzyme involved in the production of leukotrienes, which are inflammatory mediators that contribute to pain, swelling, and stiffness in joints. By inhibiting 5-LOX, Aflapin reduces the production of leukotrienes and thus, alleviates the symptoms of OA.
Alternate Names
- AprèsFlex®
- Boswellia serrata extract
How It Works
- Pharmacodynamics: Aflapin reduces joint pain, stiffness, and inflammation. It may also improve joint function and mobility. It shows potential in protecting cartilage.
- Pharmacokinetics: The specific pharmacokinetic parameters (absorption, distribution, metabolism, and excretion) of Aflapin have not been fully elucidated. However, it is known that administration with high-fat foods may enhance plasma levels of Boswellia serrata extracts. Boswellia serrata derived compounds demonstrate inhibition of several CYP enzymes, such as CYP1A2, 2C8, 2C9, 2C19, 2D6, and 3A4. More research is needed for complete pharmacokinetic profile.
- Mode of Action: Aflapin primarily inhibits 5-LOX, an enzyme responsible for leukotriene synthesis. It may also inhibit other inflammatory cytokines and enzymes like TNF-α and MMP-3.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Aflapin inhibits the 5-LOX enzyme. It may also modulate inflammatory cytokines (e.g., TNF-α) and cartilage-degrading enzymes (e.g., MMP-3). The full range of its molecular targets is still being investigated.
- Elimination Pathways: The elimination pathways are yet not fully understood, hepatic metabolism is possible.
Dosage
Standard Dosage
Adults:
- 100-250 mg/day of Aflapin, usually taken orally in capsule form. Some studies have used higher doses (up to 1000 mg/day) for non-proprietary Boswellia serrata extracts.
Children:
- Safety and efficacy in children have not been established. Use only if recommended by a doctor.
Special Cases:
- Elderly Patients: No specific dosage adjustments are available. Caution should be exercised.
- Patients with Renal Impairment: Data is limited, therefore caution should be exercised. Consult a nephrologist if required.
- Patients with Hepatic Dysfunction: Data is limited, therefore caution should be exercised. Consult a hepatologist if required.
- Patients with Comorbid Conditions: Caution advised; consult a doctor about potential interactions.
Clinical Use Cases
- Specific dosing for clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergencies has not been established.
Dosage Adjustments
- Dosage adjustments might be needed based on patient factors. However, limited specific guidelines are available.
Side Effects
Common Side Effects
- Nausea
- Diarrhea
- Heartburn
- Abdominal pain
- Headache
- Stomach upset
Rare but Serious Side Effects
- Allergic reactions (skin rash, itching, swelling)
- Liver injury is possible due to high paracetamol dose.
- Gastrointestinal bleeding/ulcer formation.
Long-Term Effects
- Data is limited and long-term effects are not well established.
Adverse Drug Reactions (ADR)
- Serious adverse reactions are rare but possibilities are skin reactions, hypersensitivity, gastrointestinal issues. Immediate medical attention needed.
Contraindications
- Hypersensitivity to Aflapin or any of its components.
- Pregnancy and breastfeeding (safety not established).
Drug Interactions
- May interact with drugs metabolized by CYP enzymes (CYP1A2, 2C8, 2C9, 2C19, 2D6, and 3A4). Caution is advised when using Aflapin with substrates of these enzymes.
- May interact with P-glycoprotein substrates.
- Interactions with commonly prescribed medications, OTC drugs, or food have not been extensively studied.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Not established. Avoid use as safety data is insufficient.
- Breastfeeding: Safety is not established. Avoid use.
Drug Profile Summary
- Mechanism of Action: 5-LOX inhibitor, reducing inflammation.
- Side Effects: Nausea, diarrhea, heartburn, abdominal pain, headache, stomach upset. Rare: Allergic reactions, liver injury, gastrointestinal bleeding/ulcer formation.
- Contraindications: Hypersensitivity, pregnancy, breastfeeding.
- Drug Interactions: CYP enzyme and P-gp substrates.
- Pregnancy & Breastfeeding: Avoid.
- Dosage: Adults: 100-250 mg/day. Children: Not established.
- Monitoring Parameters: Liver function, kidney function and gastrointestinal health.
Popular Combinations
- Often combined with other herbs or collagen in some formulations. Specific clinical data on combinations is limited.
Precautions
- General Precautions: Pre-existing medical conditions like liver or kidney disease should be assessed. Screening for allergies is important.
- Specific Populations: Pregnant and breastfeeding women should avoid use. Safety in children and the elderly needs more investigation.
- Lifestyle Considerations: Potential interactions with alcohol are unknown.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Aflapin?
A: The standard recommended dose for adults is 100-250 mg/day. Pediatric and special population dosing has not been established.
Q2: How does Aflapin work?
A: Aflapin inhibits 5-LOX, reducing inflammation in joints.
Q3: What are the common side effects of Aflapin?
A: Common side effects include nausea, diarrhea, heartburn, and abdominal pain.
Q4: Is Aflapin safe during pregnancy or breastfeeding?
A: No, its use is not recommended during pregnancy and breastfeeding due to limited safety data.
Q5: Can Aflapin be used with other medications?
A: It can interact with some medications, especially those metabolized by CYP enzymes or transported by P-gp. Consult a doctor before combining Aflapin with other medications.
Q6: How long does it take for Aflapin to work?
A: Some studies have shown improvements in pain and function as early as 5-7 days after starting Aflapin.
Q7: What are the contraindications for using Aflapin?
A: Contraindications include hypersensitivity to Aflapin and pregnancy/breastfeeding.
Q8: Are there any long-term effects of using Aflapin?
A: Long-term effects are not well-established due to a lack of extensive research.
Q9: Can Aflapin be used for other conditions besides osteoarthritis?
A: While primarily used for OA, Aflapin might be useful for other inflammatory conditions, but more research is needed. Always consult a physician.
