Benzyl Alcohol + Diclofenac + Thiocolchicoside

Usage

• This combination is prescribed for the relief of pain and muscle spasm associated with musculoskeletal conditions such as low back pain, neck pain (e.g., torticollis), sprains, strains, frozen shoulder, and other musculoskeletal injuries. Topical formulations are used for localized relief, while injections are used for systemic delivery when needed.
• Pharmacological Classification: Nonsteroidal anti-inflammatory drug (NSAID) + Muscle relaxant + Antimicrobial preservative (benzyl alcohol, primarily in topical formulations).

Alternate Names

• Diclofenac + Thiocolchicoside + Benzyl Alcohol
• Brand names: Aquafast TH, Dicwed TH, Dolense Th, Serofin-TH, and others. Many different brand names exist depending on the manufacturer and specific formulation.

How It Works

• Pharmacodynamics: Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby diminishing inflammation and pain. Thiocolchicoside acts centrally to reduce muscle tone and spasm, likely by activating GABA inhibitory pathways. Benzyl alcohol provides additional local anesthetic and antiseptic effects in topical preparations.
• Pharmacokinetics:
  • Diclofenac: Well-absorbed orally and intramuscularly. Metabolized in the liver, primarily by CYP2C9. Excreted renally and in bile.
  • Thiocolchicoside: Metabolized in the liver. Excreted primarily in the urine.
  • Benzyl alcohol: Metabolized to benzoic acid and excreted in the urine.
• Mode of Action: Diclofenac’s principal mechanism of action is the inhibition of COX-1 and COX-2 enzymes. COX enzymes catalyze the conversion of arachidonic acid to prostaglandins, which play essential roles in pain and inflammation. Thiocolchicoside’s action is believed to be through modulation of GABAergic neurotransmission within the spinal cord, reducing muscle tone and spasm. In topical formulations, benzyl alcohol acts as a local anesthetic and antiseptic.

Dosage

Dosage varies significantly depending on the formulation (injection, gel, cream) and specific product. Always consult the specific product information and follow the prescribing physician’s directions.

Standard Dosage

Adults:

• Injection: A common dosage is Diclofenac 37.5 mg + Thiocolchicoside 2 mg + Benzyl alcohol 4% v/v, intramuscularly once or twice daily. However, other dosages exist.
• Topical: Apply a thin layer of gel/cream to the affected area 2-3 times per day.

Children:

• Not recommended for use in children below 18 years of age. Safety and efficacy have not been established.

Special Cases:

• Elderly Patients: Dose adjustment may be necessary. Start with the lowest effective dose and monitor for adverse effects.
• Patients with Renal Impairment: Caution advised. Dose adjustment may be necessary.
• Patients with Hepatic Dysfunction: Caution advised. Dose adjustment may be necessary.
• Patients with Comorbid Conditions: Use with caution in patients with cardiovascular disease, gastrointestinal disorders, or bleeding disorders.

Clinical Use Cases

• Intubation: Not typically used.
• Surgical Procedures: May be used post-operatively for pain and muscle spasm.
• Mechanical Ventilation: Not typically used.
• Intensive Care Unit (ICU) Use: May be used for pain management, but with caution due to potential side effects.
• Emergency Situations: Not typically used in emergency situations.

Dosage Adjustments

Dose adjustments are necessary for patients with renal or hepatic dysfunction. The elderly may also require a lower dose.

Side Effects

Common Side Effects

• Injection: Pain, redness, swelling at the injection site.
• Topical: Burning, itching, redness, or irritation at the application site.
• Systemic: Nausea, vomiting, stomach pain, diarrhea, headache, dizziness, drowsiness.

Rare but Serious Side Effects

• Allergic reactions
• Gastrointestinal bleeding or ulceration
• Renal dysfunction
• Hepatic dysfunction
• Cardiovascular events (rarely)

Long-Term Effects

Chronic use of NSAIDs can increase the risk of gastrointestinal complications.

Adverse Drug Reactions (ADR)

• Severe allergic reactions (anaphylaxis)
• Severe gastrointestinal bleeding
• Acute renal failure

Contraindications

• Hypersensitivity to any component of the formulation.
• Active peptic ulcer or gastrointestinal bleeding.
• Severe hepatic or renal impairment.
• Pregnancy (especially the third trimester).
• Breastfeeding.
• Use in children under 18 years of age.

Drug Interactions

• Other NSAIDs: Increased risk of gastrointestinal side effects.
• Anticoagulants (e.g., warfarin): Increased risk of bleeding.
• Lithium: Increased lithium levels.
• Methotrexate: Increased methotrexate toxicity.
• Alcohol: Increased risk of gastrointestinal bleeding.

Pregnancy and Breastfeeding

• Pregnancy: Contraindicated, especially in the third trimester. May cause premature closure of the ductus arteriosus in the fetus.
• Breastfeeding: Not recommended due to potential excretion in breast milk and adverse effects on the infant.

Drug Profile Summary (See information above)

Popular Combinations

This combination is itself a popular combination and is not typically combined with other active drugs. However, topical formulations may include other ingredients like linseed oil, menthol, or methyl salicylate for added local effects.

Precautions (See information above)

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Benzyl Alcohol + Diclofenac + Thiocolchicoside?

A: Dosage varies depending on the formulation (injection, topical) and product. Consult the specific product information for detailed dosing instructions. A common intramuscular injection dosage is Diclofenac 37.5 mg + Thiocolchicoside 2 mg + Benzyl alcohol 4% v/v, once or twice daily. Topical formulations are usually applied 2-3 times a day.

Q2: What are the main contraindications for this combination?

A: Contraindications include hypersensitivity to any of the components, active peptic ulcer or gastrointestinal bleeding, severe hepatic or renal impairment, pregnancy (especially the third trimester), breastfeeding, and use in children under 18 years.

Q3: Can this combination be used during pregnancy or breastfeeding?

A: No, it’s contraindicated during pregnancy, particularly in the third trimester, and is not recommended during breastfeeding.

Q4: What are the common side effects?

A: Common side effects include injection site reactions (pain, redness, swelling), topical irritation (burning, itching), and systemic effects like nausea, vomiting, stomach pain, diarrhea, headache, dizziness, and drowsiness.

Q5: What are the potential drug interactions?

A: Clinically significant interactions can occur with other NSAIDs, anticoagulants (e.g., warfarin), lithium, methotrexate, and alcohol.

Q6: How does thiocolchicoside contribute to this combination’s effects?

A: Thiocolchicoside is a muscle relaxant that works centrally to alleviate muscle spasms and improve muscle mobility, complementing diclofenac’s pain-relieving and anti-inflammatory actions.

Q7: Are there any specific monitoring parameters recommended during treatment?

A: Monitoring liver and kidney function is recommended, as well as watching for signs of gastrointestinal bleeding, especially in patients with risk factors.

Q8: What is the role of benzyl alcohol in this medication?

A: Benzyl alcohol primarily serves as an antimicrobial preservative in topical formulations, and can provide mild local anesthetic effects. It’s not typically a component of injectable formulations.

Q9: What are the available dosage forms?

A: This combination is commonly available as intramuscular injections and topical gels or creams.

Q10: Can this medicine be used long-term?

A: Long-term use, especially of diclofenac, can increase the risk of gastrointestinal complications. The lowest effective dose should be used for the shortest duration necessary.