Diclofenac + Thiocolchicoside

Usage

• Diclofenac + Thiocolchicoside is prescribed for the relief of pain and muscle spasms associated with musculoskeletal conditions such as:
  • Degenerative vertebral disorders
  • Torticollis (neck muscle contractions)
  • Upper and lower back pain
  • Sprains and strains
  • Post-operative pain and inflammation
  • Other acute or chronic painful musculoskeletal conditions.
• Pharmacological Classification:
  • Diclofenac: Non-Steroidal Anti-inflammatory Drug (NSAID)
  • Thiocolchicoside: Muscle Relaxant
• Mechanism of Action: Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing pain and inflammation. Thiocolchicoside acts centrally on GABA-A and glycine receptors in the spinal cord and brain, leading to muscle relaxation and spasm reduction.

Alternate Names

• No widely recognized alternate names exist for this specific combination. However, the individual components may have different names internationally.
• Brand Names: Thioact D, Myospas TH, Thiorok D, and various others depending on the manufacturer and region.

How It Works

• Pharmacodynamics: Diclofenac exerts its analgesic and anti-inflammatory effects by inhibiting COX-1 and COX-2 enzymes, reducing prostaglandin production. Thiocolchicoside’s muscle relaxant effect is mediated by its action on GABAergic and glycinergic pathways in the central nervous system, although the precise mechanism is not fully elucidated. It acts as a competitive GABA-A receptor antagonist and inhibits glycine receptors.
• Pharmacokinetics:
  • Diclofenac: Well absorbed orally and intramuscularly. Metabolized primarily in the liver by CYP2C9. Excreted renally and in bile.
  • Thiocolchicoside: Primarily metabolized in the liver, with significant first-pass metabolism, reducing oral bioavailability. Excreted primarily via the kidneys.
• Mode of Action: Diclofenac reduces pain and inflammation by targeting COX enzymes and inhibiting prostaglandin production. Thiocolchicoside facilitates muscle relaxation via central effects on GABAergic and glycinergic neurotransmission.
• Elimination Pathways:
  • Diclofenac: Renal and hepatic excretion.
  • Thiocolchicoside: Primarily renal excretion.

Dosage

Standard Dosage

Adults:

• Oral: The typical dose is one tablet containing 50mg Diclofenac and 4mg Thiocolchicoside twice a day, although different formulations might contain slightly different doses. The maximum daily dose of Diclofenac is generally 150mg.
• Intramuscular: 75mg Diclofenac and 4mg Thiocolchicoside, once or twice daily, for up to 2 days, followed by oral administration.
• Dosage and duration should be tailored to the individual patient and the specific condition being treated.

Children:

• Not recommended for use in children and adolescents below 18 years of age, as safety and efficacy have not been established.

Special Cases:

• Elderly Patients: Start with the lowest effective dose and monitor closely for adverse effects.
• Patients with Renal Impairment: Dose adjustment may be necessary.
• Patients with Hepatic Dysfunction: Dose reduction is advised and close monitoring is essential.
• Patients with Comorbid Conditions: Caution should be exercised in patients with cardiovascular disease, gastrointestinal disorders, or a history of hypersensitivity to NSAIDs.

Clinical Use Cases

• Intubation: Not typically used during intubation.
• Surgical Procedures: Used for post-operative pain management and muscle spasm reduction. Dosage is determined by the nature of the surgery.
• Mechanical Ventilation: Not typically used during mechanical ventilation.
• Intensive Care Unit (ICU) Use: May be considered for post-operative pain and spasm management in ICU settings. Close monitoring for adverse events is required.
• Emergency Situations: Not a first-line drug in most emergency situations.

Dosage Adjustments

• Dose modifications are often necessary based on patient-specific factors, including renal/hepatic dysfunction, age, and other medical conditions. Consult current guidelines.

Side Effects

Common Side Effects

• Nausea, vomiting
• Diarrhea
• Stomach pain, heartburn
• Dizziness, headache
• Drowsiness

Rare but Serious Side Effects

• Gastrointestinal bleeding
• Allergic reactions
• Cardiovascular events (myocardial infarction, stroke) with prolonged use.
• Renal impairment, hepatic dysfunction

Long-Term Effects

• Chronic use of NSAIDs can increase the risk of gastrointestinal bleeding, peptic ulcers, and cardiovascular events.

Adverse Drug Reactions (ADR)

• Any signs of gastrointestinal bleeding (e.g., bloody or black stools)
• Severe allergic reactions (e.g., anaphylaxis)
• Signs of hepatotoxicity (e.g., jaundice)
• Signs of nephrotoxicity (e.g., changes in urine output).

Contraindications

• Hypersensitivity to diclofenac, thiocolchicoside, or other NSAIDs.
• Active peptic ulcer or gastrointestinal bleeding
• Severe hepatic or renal impairment
• Pregnancy (especially third trimester)
• Breastfeeding
• Asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
• Severe heart failure

Drug Interactions

• Other NSAIDs (increased risk of gastrointestinal adverse effects)
• Anticoagulants (e.g., warfarin) - increased bleeding risk.
• Antihypertensives – May decrease effectiveness of antihypertensives.
• Lithium, methotrexate, digoxin – Increased levels in the blood with Diclofenac.
• CYP2C9 inhibitors or inducers - May alter the metabolism of diclofenac.
• Alcohol - Increases the risk of gastrointestinal side effects.

Pregnancy and Breastfeeding

• Pregnancy Safety Category: Not recommended during pregnancy, particularly in the third trimester due to risk of premature ductus arteriosus closure.
• Breastfeeding: Not recommended during breastfeeding. Diclofenac and thiocolchicoside are excreted into breast milk and may pose a risk to infants.

Drug Profile Summary

• Mechanism of Action: Diclofenac: COX inhibitor (NSAID); Thiocolchicoside: GABA-A receptor antagonist and glycine receptor inhibitor (muscle relaxant).
• Side Effects: Nausea, vomiting, diarrhea, stomach pain, dizziness, headache, drowsiness. Serious but rare: GI bleeding, allergic reactions, cardiovascular events.
• Contraindications: Hypersensitivity, peptic ulcer, GI bleeding, severe liver/kidney disease, pregnancy, breastfeeding, asthma, urticaria post-aspirin/NSAID, severe heart failure.
• Drug Interactions: Other NSAIDs, anticoagulants, antihypertensives, lithium, methotrexate, CYP2C9 inhibitors/inducers, alcohol.
• Pregnancy & Breastfeeding: Contraindicated.
• Dosage: Adults: Oral: 50mg/4mg twice daily (or as prescribed), IM: 75mg/4mg once/twice daily (max. 2 days); Children: Not recommended.
• Monitoring Parameters: Liver function tests, renal function tests, signs of GI bleeding, blood pressure monitoring with long-term use.

Popular Combinations

• Often used as a stand-alone combination. Addition of other analgesics may be warranted at the clinician’s discretion.

Precautions

• General Precautions: Monitor for gastrointestinal, cardiovascular, renal, and hepatic adverse effects. Use the lowest effective dose for the shortest duration possible.
• Specific Populations:
  • Pregnant Women: Contraindicated.
  • Breastfeeding Mothers: Contraindicated.
  • Children & Elderly: Not recommended for children under 18. Elderly patients require close monitoring and lower doses.
• Lifestyle Considerations: Avoid alcohol. Caution while driving or operating machinery due to potential drowsiness and dizziness.

FAQs (Frequently Asked Questions)

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

A: Oral: Typically 50mg Diclofenac/4mg Thiocolchicoside twice daily. IM: 75mg/4mg once or twice daily (up to 2 days). Dosage needs to be individualized. Not for children under 18.

Q2: What are the common side effects?

A: Nausea, vomiting, diarrhea, stomach pain, dizziness, headache, and drowsiness.

Q3: Is it safe during pregnancy and breastfeeding?

A: No, it’s contraindicated in both pregnancy and breastfeeding.

Q4: Can I drink alcohol while taking this medication?

A: No, alcohol should be avoided as it can increase the risk of gastrointestinal side effects.

Q5: What if I have kidney or liver problems?

A: Consult your doctor. Dose adjustments may be necessary.

Q6: Can I take it with other pain relievers?

A: Avoid taking other NSAIDs. Consult your physician before combining with other analgesics.

Q7: How long can I take this medication?

A: Use for the shortest duration necessary to control symptoms. Consult your doctor.

Q8: What should I do if I experience severe side effects?

A: Discontinue the medication and immediately contact your doctor.

Q9: Can this medication be used in children?

A: No, this medication is not recommended for children under 18.

Q10: Are there any drug interactions I should be aware of?

A: Yes, it interacts with several medications, including other NSAIDs, anticoagulants, lithium, and some antidepressants. Provide a complete medication history to your doctor.