Usage
Lornoxicam is prescribed for short-term relief of mild to moderate acute pain, and for the symptomatic relief of pain and inflammation associated with osteoarthritis and rheumatoid arthritis. It is pharmacologically classified as a non-steroidal anti-inflammatory drug (NSAID). Lornoxicam works by inhibiting the cyclooxygenase (COX) enzymes, COX-1 and COX-2, which are responsible for producing prostaglandins, key mediators of pain and inflammation. By reducing prostaglandin production, lornoxicam diminishes pain and inflammation.
Alternate Names
While lornoxicam is the generic name, it’s marketed under various brand names, including Xefo and Xefocam.
How It Works
Pharmacodynamics: Lornoxicam exerts its analgesic and anti-inflammatory effects primarily through the inhibition of COX-1 and COX-2. This inhibition reduces the synthesis of prostaglandins, which play a crucial role in pain sensation, inflammation, and fever. The balanced inhibition of both COX isoforms contributes to its efficacy. Lornoxicam readily penetrates synovial fluid, further enhancing its effectiveness in joint-related conditions.
Pharmacokinetics:
- Absorption: Lornoxicam is well-absorbed orally, achieving peak plasma concentration within 1-2 hours after oral administration and approximately 25 minutes after intramuscular injection. Food can reduce absorption by about 20% and increase the time to peak concentration (Tmax).
- Metabolism: Lornoxicam is primarily metabolized in the liver, mainly by the cytochrome P450 2C9 (CYP2C9) enzyme, to inactive metabolites. This metabolic pathway can be influenced by drugs that induce or inhibit CYP2C9.
- Elimination: Lornoxicam and its metabolites are eliminated through both renal (urine) and hepatic (feces) routes. The mean elimination half-life is 3-4 hours.
Dosage
Standard Dosage
Adults:
- Pain: 8-16 mg daily, divided into 2 or 3 doses. Maximum daily dose: 16 mg for oral administration and 24 mg for parenteral administration.
- Osteoarthritis and Rheumatoid Arthritis: Initial dose: 12 mg daily, divided into 2 or 3 doses. Maintenance dose: Should not exceed 16 mg daily.
Children:
Lornoxicam is not recommended for use in children and adolescents below 18 years of age due to insufficient data on safety and efficacy.
Special Cases:
- Elderly Patients: No specific dosage adjustment is needed for elderly patients over 65 years unless there is renal or hepatic impairment. However, careful monitoring is recommended due to increased risk of gastrointestinal side effects.
- Patients with Renal Impairment: For mild to moderate renal impairment, the maximum daily dose is 12 mg, divided into 2 or 3 doses. In severe renal impairment (serum creatinine > 700 μmol/l), lornoxicam is contraindicated.
- Patients with Hepatic Dysfunction: For moderate hepatic impairment, the maximum daily dose is 12 mg, divided into 2 or 3 doses. In severe hepatic impairment, lornoxicam is contraindicated.
- Patients with Comorbid Conditions: Careful assessment and dose adjustments may be needed for patients with conditions such as diabetes, cardiovascular disease, hypertension, and heart failure due to potential drug interactions and increased risk of adverse events.
Clinical Use Cases
While lornoxicam is effective for post-surgical pain, there are no specific dosage guidelines for intubation, mechanical ventilation, or ICU use. Dosage should be tailored based on individual patient needs and pain assessment. For emergency situations, intravenous or intramuscular administration might be preferred for rapid pain relief, with a dose of 8 mg once or twice daily, not exceeding 24 mg daily.
Dosage Adjustments
Dose modification is necessary for patients with renal and hepatic impairment as detailed above. Metabolic disorders or genetic polymorphisms affecting drug metabolism (especially CYP2C9) may necessitate dosage adjustments. Close monitoring of patient response and potential adverse effects is crucial.
Side Effects
Common Side Effects
- Dizziness
- Diarrhea
- Nausea
- Headache
- Vomiting
- Dyspepsia
- Abdominal pain
- Indigestion
Rare but Serious Side Effects
- Gastrointestinal bleeding
- Perforation of the stomach or intestines
- Stevens-Johnson syndrome
- Toxic epidermal necrolysis
- Cardiovascular thrombotic events (myocardial infarction, stroke)
- Kidney impairment
Long-Term Effects
Chronic complications may include gastrointestinal issues, renal dysfunction, and cardiovascular risks with prolonged use.
Adverse Drug Reactions (ADR)
Clinically significant ADRs that necessitate immediate intervention include severe allergic reactions (anaphylaxis, angioedema), gastrointestinal bleeding or perforation, cardiovascular events, and serious skin reactions.
Contraindications
- Hypersensitivity to lornoxicam or any of its excipients.
- History of hypersensitivity reactions (asthma, rhinitis, angioedema, urticaria) to other NSAIDs, including aspirin.
- Active or history of recurrent peptic ulcer/hemorrhage.
- Severe hepatic impairment.
- Severe renal impairment.
- Third trimester of pregnancy.
- History of gastrointestinal bleeding or perforation related to previous NSAID therapy.
Drug Interactions
Lornoxicam can interact with a variety of medications, including:
- Anticoagulants: Increased risk of bleeding when combined with warfarin, heparin, or other anticoagulants.
- Antihypertensives: May reduce the effectiveness of diuretics, ACE inhibitors, and angiotensin II receptor antagonists.
- Lithium: May increase the risk of lithium toxicity.
- Methotrexate: Enhanced effects of methotrexate.
- CYP2C9 Inhibitors/Inducers: Drugs that inhibit or induce CYP2C9 can alter the metabolism of lornoxicam, leading to increased or decreased serum levels.
- Ciclosporin: May increase the risk of nephrotoxicity.
Alcohol consumption should be avoided while taking lornoxicam due to increased risk of gastrointestinal bleeding and other adverse effects.
Pregnancy and Breastfeeding
Lornoxicam is contraindicated during the third trimester of pregnancy. It should be avoided during the first and second trimesters as well, as it may increase the risk of miscarriage and fetal complications. Lornoxicam should not be used during breastfeeding.
Drug Profile Summary
- Mechanism of Action: NSAID inhibiting COX-1 and COX-2, reducing prostaglandin synthesis.
- Side Effects: Common: Dizziness, diarrhea, nausea, headache, vomiting. Serious: GI bleeding, Stevens-Johnson syndrome, cardiovascular events.
- Contraindications: Hypersensitivity to NSAIDs, peptic ulcer, severe hepatic/renal impairment, third trimester of pregnancy.
- Drug Interactions: Anticoagulants, antihypertensives, lithium, methotrexate, CYP2C9 inhibitors/inducers.
- Pregnancy & Breastfeeding: Contraindicated in third trimester, avoid during pregnancy and breastfeeding.
- Dosage: Adults: 8-16 mg/day for pain, 12-16 mg/day for arthritis. Adjust for renal/hepatic impairment. Not recommended for children under 18.
- Monitoring Parameters: Renal function, liver function, blood pressure, signs of GI bleeding.
Popular Combinations
Lornoxicam is sometimes used in combination with other analgesics for enhanced pain relief, but caution is advised due to increased risk of side effects. Combinations should be carefully considered and monitored by a healthcare professional.
Precautions
- General Precautions: Screen for allergies, history of peptic ulcer, bleeding disorders, renal/hepatic impairment, cardiovascular disease, and other relevant medical conditions before initiating treatment.
- Specific Populations: Avoid in pregnancy and breastfeeding. Exercise caution in elderly patients and children.
- Lifestyle Considerations: Avoid alcohol. Caution with driving or operating machinery due to potential dizziness or drowsiness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Lornoxicam?
A: For adults, the recommended dose for pain is 8-16 mg/day divided into 2-3 doses. For osteoarthritis and rheumatoid arthritis, the initial dose is 12 mg/day divided into 2-3 doses, with a maximum of 16 mg/day. Dosage adjustments are necessary for patients with renal or hepatic impairment. It is not recommended for children under 18 years.
Q2: How does Lornoxicam compare to other NSAIDs?
A: Lornoxicam exhibits a balanced inhibition of both COX-1 and COX-2, offering potent analgesic and anti-inflammatory effects. Its efficacy and safety profile are comparable to other NSAIDs like diclofenac.
Q3: What are the serious side effects to watch out for with Lornoxicam?
A: Serious side effects include gastrointestinal bleeding, peptic ulcer perforation, cardiovascular events (heart attack, stroke), severe skin reactions (Stevens-Johnson syndrome), and renal impairment.
Q4: Can Lornoxicam be used during pregnancy or breastfeeding?
A: Lornoxicam is contraindicated during the third trimester of pregnancy and should be avoided during the first and second trimesters. It should also be avoided during breastfeeding.
Q5: What are the common drug interactions with Lornoxicam?
A: Lornoxicam can interact with anticoagulants, antihypertensives, lithium, methotrexate, and drugs that affect CYP2C9 enzyme activity.
Q6: What precautions should be taken before prescribing Lornoxicam?
A: Patients should be screened for allergies, history of peptic ulcer, bleeding disorders, renal/hepatic impairment, cardiovascular disease. Caution should be exercised in elderly patients.
Q7: How long can Lornoxicam be used for?
A: Lornoxicam is generally prescribed for short-term use due to the potential for long-term side effects. The duration of treatment should be determined by the patient’s condition and response to therapy.
Q8: What should patients do if they experience side effects while taking Lornoxicam?
A: Patients should inform their doctor immediately if they experience any side effects, especially gastrointestinal discomfort, signs of allergic reaction, or cardiovascular symptoms.
Q9: Are there any dietary restrictions while taking Lornoxicam?
A: While no specific dietary restrictions are associated with lornoxicam, alcohol should be avoided due to increased risk of gastrointestinal complications. Taking lornoxicam with food can slightly reduce its absorption.
