Usage
Ketoprofen + Thiocolchicoside is prescribed for the relief of pain and inflammation associated with musculoskeletal conditions, such as:
- Osteoarthritis
- Rheumatoid arthritis
- Gouty arthritis
- Ankylosing spondylitis
- Acute pain
- Chronic low back pain
- Muscle spasms
Pharmacological Classification:
This combination medication includes two classifications:
- Ketoprofen: Non-steroidal anti-inflammatory drug (NSAID)
- Thiocolchicoside: Muscle relaxant
Mechanism of Action: Ketoprofen works by inhibiting cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing pain and inflammation. Thiocolchicoside acts on the central nervous system, specifically GABA receptors in the spinal cord and brain, leading to muscle relaxation and reduced spasms.
Alternate Names
While “Ketoprofen + Thiocolchicoside” is the generic name, several brand names exist depending on the manufacturer and region. Some examples include Keyprofen Thio, Ketolice, and Myoril Plus. Refer to local pharmaceutical resources for a comprehensive list of brand names in India.
How It Works
Pharmacodynamics: Ketoprofen exerts analgesic, anti-inflammatory, and antipyretic effects by inhibiting COX enzymes, thus reducing prostaglandin synthesis. Thiocolchicoside’s muscle relaxant action is mediated through interaction with GABA receptors in the spinal cord and brain, alleviating muscle stiffness and spasms.
Pharmacokinetics:
- Ketoprofen: Absorbed well orally, reaching peak plasma concentrations in 1-2 hours. Metabolized in the liver and excreted primarily by the kidneys.
- Thiocolchicoside: Also well-absorbed orally. Metabolism and excretion pathways are not fully elucidated but involve both hepatic and renal routes.
Mode of Action: Ketoprofen targets COX-1 and COX-2 enzymes, inhibiting the production of inflammatory mediators. Thiocolchicoside binds to GABA receptors, modulating neuronal activity and leading to muscle relaxation. Specific elimination pathways for Thiocolchicoside are complex and involve both hepatic metabolism and renal excretion. Ketoprofen is metabolized by CYP enzymes in the liver and primarily eliminated by the kidneys.
Dosage
Standard Dosage
Adults: The usual dosage is one tablet containing 50mg Ketoprofen and 4mg Thiocolchicoside taken twice daily, preferably after meals. Dosages might vary based upon individual patient needs and the severity of the condition.
Children: Use in children is generally not recommended due to limited safety and efficacy data.
Special Cases:
- Elderly Patients: Initiate therapy with lower doses and monitor closely for adverse effects. Dose adjustment may be necessary.
- Patients with Renal Impairment: Use with caution and consider dose reduction in patients with moderate to severe renal impairment. Monitor renal function.
- Patients with Hepatic Dysfunction: Use with caution and consider dose reduction in patients with hepatic impairment. Close monitoring is required.
- Patients with Comorbid Conditions: Exercise caution in patients with a history of peptic ulcers, gastrointestinal bleeding, cardiovascular disease, or asthma.
Clinical Use Cases
The primary clinical use cases are outlined in the “Usage” section. Dosage adjustments in these settings are determined by the treating physician based on individual patient needs and clinical response. There is no information available regarding the use of ketoprofen + thiocolchicoside in clinical cases as: intubation, surgical procedures, mechanical ventilation, intensive care unit (ICU) use, emergency situations (e.g., status epilepticus, cardiac arrest).
Dosage Adjustments
Dose modifications are required in elderly patients, and those with renal or hepatic impairment. Start with lower doses and titrate upwards based on clinical response and tolerability.
Side Effects
Common Side Effects:
- Nausea
- Heartburn
- Indigestion
- Stomach pain
- Dizziness
- Sleepiness
- Nervousness
- Diarrhea
- Ringing in the ears
- Skin rash
Rare but Serious Side Effects:
- Gastrointestinal bleeding
- Peptic ulcer
- Severe allergic reactions (anaphylaxis)
- Cardiovascular events (heart attack, stroke)
Long-Term Effects: Chronic use of NSAIDs like ketoprofen can increase the risk of gastrointestinal and cardiovascular complications.
Contraindications
- Hypersensitivity to ketoprofen, thiocolchicoside, or any other NSAID.
- Active peptic ulcer disease or gastrointestinal bleeding.
- Severe heart failure.
- Severe renal impairment.
- Pregnancy (especially third trimester).
- Breastfeeding.
Drug Interactions
- NSAIDs: Concurrent use with other NSAIDs increases the risk of gastrointestinal adverse effects.
- Anticoagulants: Ketoprofen can enhance the effects of anticoagulants, increasing bleeding risk.
- Corticosteroids: Combined use with corticosteroids may also increase the risk of gastrointestinal ulcers and bleeding.
- Antihypertensives: Ketoprofen can reduce the effectiveness of antihypertensive medications.
- Lithium: Ketoprofen can increase lithium levels, potentially leading to toxicity.
- Methotrexate: Ketoprofen can increase methotrexate levels, increasing the risk of toxicity.
- Alcohol: Concomitant alcohol consumption may increase the risk of gastrointestinal irritation and bleeding.
Pregnancy and Breastfeeding
Ketoprofen + Thiocolchicoside is contraindicated during pregnancy, particularly in the third trimester, due to potential adverse effects on the fetus. It is also contraindicated during breastfeeding as both drugs can pass into breast milk.
Drug Profile Summary
- Mechanism of Action: Ketoprofen inhibits COX enzymes, reducing prostaglandin synthesis. Thiocolchicoside acts as a muscle relaxant by modulating GABAergic neurotransmission.
- Side Effects: Nausea, heartburn, indigestion, stomach pain, dizziness, sleepiness, nervousness, diarrhea, ringing in ears, skin rash. Rare but serious: Gastrointestinal bleeding, peptic ulcer, allergic reactions, cardiovascular events.
- Contraindications: Hypersensitivity, active peptic ulcer, severe heart failure, severe renal impairment, pregnancy, breastfeeding.
- Drug Interactions: Other NSAIDs, anticoagulants, corticosteroids, antihypertensives, lithium, methotrexate, alcohol.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: One tablet (50mg ketoprofen + 4mg thiocolchicoside) twice daily after meals. Dose adjustments necessary for elderly patients and those with renal or hepatic dysfunction.
- Monitoring Parameters: Renal function, liver function, signs of gastrointestinal bleeding, cardiovascular status.
Popular Combinations
Ketoprofen + Thiocolchicoside is itself a popular combination. Additional combinations are generally avoided due to the risk of increased side effects.
Precautions
- General Precautions: Pre-existing medical conditions should be assessed, including cardiac, renal, and hepatic function. Screen for allergies and history of peptic ulcer disease.
- Specific Populations: See “Dosage - Special Cases” and “Pregnancy and Breastfeeding.”
- Lifestyle Considerations: Limit alcohol consumption during treatment. Avoid driving or operating heavy machinery if experiencing dizziness or drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ketoprofen + Thiocolchicoside?
A: The standard adult dose is one tablet (50mg Ketoprofen + 4mg Thiocolchicoside) twice daily, preferably after meals. Adjustments may be required in elderly patients and those with renal or hepatic impairment.
Q2: What are the common side effects?
A: Common side effects include nausea, stomach upset, dizziness, and drowsiness.
Q3: Can I take this medication if I am pregnant or breastfeeding?
A: No, it is contraindicated during pregnancy, especially the third trimester, and breastfeeding.
Q4: What are the serious side effects I should watch out for?
A: Serious side effects include gastrointestinal bleeding, allergic reactions, and cardiovascular events. Seek immediate medical attention if these occur.
Q5: Can I drink alcohol while taking this medicine?
A: It is advisable to limit alcohol consumption as it can increase the risk of stomach irritation and bleeding.
Q6: Can I drive while taking this medicine?
A: Use caution as the medication may cause dizziness or drowsiness. Avoid driving if these symptoms occur.
Q7: How does this medication work?
A: Ketoprofen reduces pain and inflammation, while thiocolchicoside relaxes muscles.
Q8: What conditions is this medication used for?
A: It’s used to manage pain and inflammation in musculoskeletal conditions like osteoarthritis, rheumatoid arthritis, and muscle spasms.
Q9: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it’s close to the time of your next dose. Do not double the dose.