Cyclobenzaprine + Diclofenac diethylamine + Linseed Oil + Menthol + Methyl Salicylate

Usage

This combination medication is primarily prescribed for topical relief of acute musculoskeletal pain and localized inflammation associated with conditions like sprains, strains, and osteoarthritis.

• Pharmacological Classification: This is a combination product encompassing several classifications:

  • Cyclobenzaprine: Skeletal Muscle Relaxant
  • Diclofenac: Nonsteroidal Anti-inflammatory Drug (NSAID)
  • Methyl Salicylate: Counterirritant, NSAID
  • Menthol: Counterirritant
  • Linseed Oil: Anti-inflammatory agent (due to its omega-3 fatty acid content)

• Mechanism of Action: This combination targets multiple pain pathways: Cyclobenzaprine acts centrally to reduce muscle spasms, possibly via serotonin (5-HT2) receptor antagonism. Diclofenac and Methyl salicylate inhibit cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and thus inflammation and pain. Menthol acts as a counterirritant by activating TRPM8 receptors, creating a cooling sensation, and may improve local circulation. Linseed oil, with its omega-3 fatty acids, may help reduce inflammation by inhibiting inflammatory mediators.

Alternate Names

This combination doesn’t have a universally recognized non-proprietary name. It is often referred to by the combination of its components.

• Brand Names: Flexabenz, Ultrabenz, Diclobenz, Broflez, Rlxbenz are among the common brand names for this combination product in India.

How It Works

• Pharmacodynamics: This combination exerts its therapeutic effect through a synergistic mechanism involving muscle relaxation, analgesia, and anti-inflammatory action. Cyclobenzaprine reduces muscle spasms; Diclofenac and Methyl Salicylate decrease pain and inflammation; Menthol provides a cooling sensation and potential circulatory benefits; and Linseed Oil adds to the anti-inflammatory effect.

• Pharmacokinetics: Topical administration leads to localized absorption through the skin. The extent of absorption is affected by factors like skin integrity and application site. Diclofenac is metabolized in the liver. Methyl salicylate is metabolized to salicylic acid. Cyclobenzaprine is also metabolized in the liver, with renal excretion being the primary elimination pathway. The topical application minimizes systemic exposure, compared to the oral route of these substances.

• Mode of Action: Cyclobenzaprine’s muscle relaxant effect likely involves serotonin (5-HT2) receptor antagonism in the brainstem. Diclofenac and Methyl salicylate inhibit COX enzymes. Menthol activates TRPM8 receptors, causing a cooling sensation, and may dilate blood vessels locally. Linseed oil’s alpha-linolenic acid may inhibit leukotrienes, contributing to anti-inflammatory action.

• Elimination Pathways: Primarily renal excretion for all components after metabolism, particularly hepatic metabolism for Diclofenac and Cyclobenzaprine and conversion to salicylic acid for Methyl Salicylate.

Dosage

The dosage is usually determined by the physician based on the patient’s specific condition and response to therapy. Since this combination is typically available as a topical gel, cream, or spray, the following applies to topical application:

Standard Dosage

Adults:

A thin layer should be applied to the affected area and gently massaged until absorbed. Frequency and duration of application should be as directed by the physician. Generally, this is 3-4 times daily. Do not exceed the maximum recommended daily dose as per the product packaging and physician advice.

Children:

Safety and efficacy haven’t been established in children under 14 years. Use in pediatric patients is not generally recommended unless specifically directed by a physician.

Special Cases:

• Elderly Patients: Use with caution due to potential age-related changes in hepatic and renal function.
• Patients with Renal Impairment: Use with caution. Close monitoring is essential. Dose adjustment may be required.
• Patients with Hepatic Dysfunction: Use with caution. Careful monitoring is necessary. Dosage modification may be needed.
• Patients with Comorbid Conditions: Consider individual patient characteristics and concurrent medications. Close monitoring is recommended.

Clinical Use Cases

The combined formulation is not generally indicated for use in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary usage is topical, and systemic use of some of its components in these scenarios would have different dosing and formulations.

Dosage Adjustments

Dose adjustments may be necessary based on the patient’s individual factors, including renal or hepatic dysfunction, other metabolic disorders, or genetic polymorphisms impacting drug metabolism. Consult product-specific prescribing information.

Side Effects

Common Side Effects:

• Itching, irritation, redness, or burning sensation at the application site.

Rare but Serious Side Effects:

• Allergic reactions (e.g., hives, difficulty breathing, swelling of the face, lips, tongue, or throat)
• Severe skin irritation or blistering

Long-Term Effects:

No specific long-term adverse effects have been uniquely identified with this combination product when used topically as directed.

Adverse Drug Reactions (ADR):

Contact dermatitis, skin rash, pruritus, eczema

Contraindications

• Hypersensitivity to any of the ingredients.
• Application to open wounds, infected skin, or mucous membranes.
• Patients with known hypersensitivity to aspirin or other NSAIDs.

Drug Interactions

• Other topical medications applied to the same area may interact.
• Concurrent use of oral NSAIDs may increase the risk of systemic side effects.
• Concurrent use with anticoagulants or antiplatelet agents may increase the risk of bleeding.
• Potential interaction with medications metabolized by CYP enzymes (e.g., some antidepressants, antifungals).

Pregnancy and Breastfeeding

Consult a physician before using during pregnancy or breastfeeding. Use during the third trimester is contraindicated. Safety in pregnancy and breastfeeding is not fully established. Although topical application limits systemic exposure, caution is warranted.

Drug Profile Summary

• Mechanism of Action: Combined topical analgesic, muscle relaxant, and anti-inflammatory.
• Side Effects: Skin irritation, allergic reactions.
• Contraindications: Hypersensitivity to components, open wounds, aspirin sensitivity.
• Drug Interactions: Other topical medications, oral NSAIDs, anticoagulants, CYP enzyme substrates.
• Pregnancy & Breastfeeding: Consult a physician. Avoid during the third trimester.
• Dosage: Topical application as directed by the physician.
• Monitoring Parameters: Observe the application site for local reactions like irritation, redness, or allergic manifestations.

Popular Combinations

This product itself is a multi-component formulation. No further combinations are generally recommended for topical application.

Precautions

• General Precautions: Apply to intact skin only. Avoid contact with eyes, nose, and mouth. Wash hands thoroughly after application.
• Specific Populations: Use with caution in pregnant/breastfeeding women, children, and the elderly.
• Lifestyle Considerations: Monitor for potential photosensitivity, especially with prolonged sun exposure. Advise patients to avoid using sunlamps or tanning beds.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Cyclobenzaprine + Diclofenac diethylamine + Linseed Oil + Menthol + Methyl Salicylate?

A: Dosage is determined by a physician based on individual patient needs, but typically involves applying a thin layer to the affected area 3-4 times daily. Follow the directions on the product packaging and physician’s instructions.

Q2: Can this combination be used in children?

A: Not generally recommended for children under 14 unless specifically directed by a physician due to limited safety and efficacy data.

Q3: What are the major contraindications for using this product?

A: Hypersensitivity to any component, open wounds, infected skin, hypersensitivity to aspirin or other NSAIDs.

Q4: Can pregnant or breastfeeding women use this medication?

A: Consult a physician before use during pregnancy or breastfeeding. Use is contraindicated during the third trimester of pregnancy.

Q5: What are the common side effects?

A: Local skin reactions like itching, irritation, redness, and a burning sensation.

Q6: Are there any drug interactions I should be aware of?

A: Yes, potential interactions exist with oral NSAIDs, anticoagulants, certain medications metabolized by CYP enzymes, and other topical agents applied to the same area.

Q7: What is the mechanism of action of this combination?

A: It combines muscle relaxant, analgesic, and anti-inflammatory mechanisms via its various components.

Q8: How long does it take for this medication to start working?

A: The onset of action can vary but patients may experience some relief shortly after application. Maximum benefit might take several days of regular use.

Q9: Can this product be used on broken skin?

A: No, it should not be applied to open wounds or broken skin.

Q10: Should I cover the area after applying the medication?

A: Covering the treated area with occlusive bandages is not recommended unless advised by a physician.