Usage
- Medical Conditions: Etoricoxib + Tolperisone is prescribed for the relief of pain and muscle spasms associated with musculoskeletal conditions such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, low back pain, neck pain, and post-surgical or injury-related pain. It is also used to manage chronic conditions like fibromyalgia and cervical spondylosis.
- Pharmacological Classification: This combination drug includes a Nonsteroidal Anti-inflammatory Drug (NSAID) - Etoricoxib, and a centrally acting Muscle Relaxant - Tolperisone.
- Mechanism of Action: Etoricoxib inhibits cyclooxygenase-2 (COX-2), reducing prostaglandin synthesis and thereby decreasing inflammation and pain. Tolperisone acts centrally to inhibit pain signal transmission, reducing muscle stiffness and spasms.
Alternate Names
- No widely recognized alternate names exist for the combination itself.
- Brand Names: A common brand name for Etoricoxib + Tolperisone is TOPERITIME EX.
How It Works
- Pharmacodynamics: Etoricoxib exerts its analgesic and anti-inflammatory effects by selectively inhibiting COX-2. Tolperisone’s muscle relaxant properties are mediated through central action, though the precise mechanism is not fully elucidated. It’s believed to involve modulation of spinal reflexes and interference with pain signal transmission.
- Pharmacokinetics: Etoricoxib is well-absorbed orally, reaching peak plasma concentrations within approximately one hour. It’s primarily metabolized in the liver via CYP3A4 enzymes and excreted mainly through the kidneys. Tolperisone is also well-absorbed orally. It is extensively metabolized in the liver, primarily by CYP2D6, and excreted in the urine.
- Mode of Action/Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Etoricoxib inhibits the COX-2 enzyme. Tolperisone’s mode of action is complex and not completely understood. It likely involves multiple pathways, including some influence on calcium channels and possibly neurotransmitter systems within the central nervous system.
- Elimination Pathways: Etoricoxib is eliminated mainly via hepatic metabolism followed by renal excretion. Tolperisone is also primarily eliminated through hepatic metabolism with subsequent urinary excretion.
Dosage
Standard Dosage
Adults:
- One tablet (containing 150mg Tolperisone and 60mg Etoricoxib) taken once or twice daily, preferably after meals.
Children:
- This combination is not generally recommended for children.
Special Cases:
- Elderly Patients: Dose adjustment may be necessary based on renal function and potential drug interactions.
- Patients with Renal Impairment: Dosage reduction may be required depending on the severity of renal impairment.
- Patients with Hepatic Dysfunction: Caution is advised, and dosage adjustment may be necessary, especially with moderate to severe hepatic impairment. Etoricoxib dose should not exceed 60mg daily in mild hepatic impairment and 30mg daily in moderate hepatic impairment.
- Patients with Comorbid Conditions: Caution is advised in patients with cardiovascular disease, hypertension, history of gastrointestinal bleeding, or other relevant comorbidities.
Clinical Use Cases
- Dosage in specific clinical settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations should be determined by the treating physician based on the individual patient’s condition and needs.
Dosage Adjustments
- Dose modifications should be considered in patients with renal or hepatic dysfunction, as mentioned above. The presence of other medical conditions or concomitant medications may also necessitate dosage adjustments.
Side Effects
Common Side Effects
- Dizziness, drowsiness, headache, nausea, gastrointestinal discomfort (indigestion, flatulence, abdominal pain), peripheral edema, and flu-like symptoms.
Rare but Serious Side Effects
- Allergic reactions (rash, itching, swelling, difficulty breathing), gastrointestinal bleeding or ulcers, severe skin reactions, liver dysfunction, cardiovascular events (e.g. myocardial infarction, stroke), and kidney issues.
Long-Term Effects
- Prolonged use, especially of Etoricoxib, may increase the risk of cardiovascular and gastrointestinal complications. Regular monitoring of liver and kidney function, as well as blood pressure, is recommended.
Adverse Drug Reactions (ADR)
- Clinically significant ADRs include severe allergic reactions, gastrointestinal bleeding, acute liver injury, and severe skin reactions like Stevens-Johnson syndrome.
Contraindications
- Hypersensitivity to either Etoricoxib or Tolperisone.
- Active peptic ulcer or gastrointestinal bleeding.
- Severe hepatic or renal impairment.
- Severe heart failure.
- Pregnancy (especially the third trimester) and breastfeeding.
- History of myocardial infarction, stroke, or peripheral arterial disease.
- Uncontrolled hypertension.
Drug Interactions
- Anticoagulants (e.g., warfarin), other NSAIDs, diuretics, ACE inhibitors, angiotensin receptor blockers, lithium, methotrexate, cyclosporine, rifampicin, and oral contraceptives.
Pregnancy and Breastfeeding
- Etoricoxib + Tolperisone is contraindicated during pregnancy and breastfeeding.
Drug Profile Summary
- Mechanism of Action: COX-2 inhibitor (Etoricoxib) and centrally acting muscle relaxant (Tolperisone).
- Side Effects: Dizziness, drowsiness, GI upset, headache, peripheral edema. Serious but rare: allergic reactions, GI bleeding, liver/kidney issues, cardiovascular events.
- Contraindications: Hypersensitivity, active peptic ulcer/GI bleeding, severe hepatic/renal impairment, pregnancy/breastfeeding.
- Drug Interactions: Anticoagulants, NSAIDs, diuretics, lithium, methotrexate, cyclosporine, rifampicin.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: one tablet once or twice daily. Adjustments needed for hepatic/renal impairment.
- Monitoring Parameters: Blood pressure, liver and kidney function.
Popular Combinations
- While the Etoricoxib + Tolperisone combination itself is common, further combining it with other drugs is less frequent and depends on the specific clinical situation.
Precautions
- Pre-existing cardiovascular, hepatic, or renal disease.
- History of GI bleeding.
- Concomitant use of anticoagulants or other NSAIDs.
- Elderly patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Etoricoxib + Tolperisone?
A: The usual recommended dosage is one tablet (Etoricoxib 60 mg + Tolperisone 150 mg) once or twice a day. However, the dosage may be adjusted depending on individual patient needs and the presence of specific medical conditions like renal or hepatic dysfunction.
Q2: What are the common side effects?
A: Common side effects include dizziness, drowsiness, headache, nausea, and gastrointestinal discomfort.
Q3: Is Etoricoxib + Tolperisone safe during pregnancy?
A: No. It is contraindicated in pregnancy and breastfeeding.
Q4: Can this combination be used in children?
A: It is not generally recommended for pediatric use.
Q5: What are the serious side effects I should watch for?
A: Serious side effects, though rare, include allergic reactions, gastrointestinal bleeding, liver dysfunction, cardiovascular events, and kidney problems.
Q6: Does this combination interact with other medications?
A: Yes. It can interact with medications like anticoagulants, other NSAIDs, diuretics, and certain antidepressants. Always inform your doctor about all other medications you are taking.
Q7: Can I take this medicine if I have a history of stomach ulcers?
A: No. Etoricoxib + Tolperisone is contraindicated in patients with active peptic ulcer or gastrointestinal bleeding history.
Q8: What precautions should be taken in elderly patients?
A: Dosage adjustments may be necessary based on renal function. Close monitoring for side effects and drug interactions is essential.
Q9: How should this medication be taken?
A: The tablets should be taken orally with water, preferably with or after meals to minimize potential gastrointestinal upset.
