Xicotil20 mg

Xicotil is a non-steroidal anti-inflammatory drug (NSAID) of the oxicam class, used for the symptomatic relief of pain and inflammation in the following conditions:

Established / Approved Uses

• Osteoarthritis - relief of joint pain, stiffness, and swelling.
• Rheumatoid arthritis - reduction of inflammatory joint pain and swelling.
• Ankylosing spondylitis - relief of spinal pain and stiffness.
• Acute musculoskeletal disorders - short-term relief of pain from sprains, strains, tendinitis, bursitis, and periarthritis of the shoulder or hip.

Xicotil provides symptomatic relief of pain and inflammation; it does not alter the underlying course of arthritic disease.

Each tablet contains Tenoxicam 20 mg as the active ingredient. Tenoxicam is also available in some markets as a powder/lyophilisate for injection for short-term use in acute pain, reconstituted with the supplied diluent before administration.

Xicotil is a long-acting non-steroidal anti-inflammatory drug (NSAID) belonging to the oxicam class, chemically related to piroxicam. It is used to relieve pain, swelling, and stiffness associated with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and acute musculoskeletal injuries.

A key feature of Xicotil is its long elimination half-life, which allows for convenient once-daily dosing while providing sustained anti-inflammatory and analgesic effect throughout the day.

Xicotil belongs to the Non-Steroidal Anti-Inflammatory Drug (NSAID) class, specifically the oxicam subgroup of NSAIDs, which also includes piroxicam and meloxicam.

Tenoxicam exerts its anti-inflammatory, analgesic, and antipyretic effects primarily through non-selective, reversible inhibition of cyclooxygenase (COX-1 and COX-2) enzymes, which reduces the synthesis of prostaglandins, key mediators of pain, inflammation, and fever.

Pharmacokinetics

• Absorption: Well absorbed orally, with peak plasma concentrations reached within a few hours; food may slightly delay but does not significantly reduce absorption.
• Distribution: Highly protein-bound (greater than 99%), with good penetration into synovial fluid.
• Metabolism: Extensively metabolized in the liver, largely via CYP2C9, into inactive metabolites.
• Elimination: Has an unusually long elimination half-life (approximately 60-75 hours), which permits once-daily dosing; excreted mainly via the kidneys and to a lesser extent in bile.
• Steady state: Because of its long half-life, steady-state plasma concentrations are reached only after approximately 10-15 days of regular once-daily dosing.

Xicotil tablets should be taken orally, swallowed whole with a full glass of water, preferably with or immediately after food or milk to minimize gastrointestinal upset. Tablets should not be crushed or chewed unless specifically formulated for that purpose. Because of its long half-life, Xicotil should be taken at approximately the same time each day.

Xicotil has clinically significant interactions with the following drug classes:

• Anticoagulants (e.g. warfarin) and antiplatelet agents: increased risk of gastrointestinal and other bleeding due to additive effects on hemostasis; concurrent use requires close monitoring.
• Other NSAIDs and aspirin: additive risk of gastrointestinal ulceration/bleeding and renal impairment; concurrent use should generally be avoided.
• ACE inhibitors, angiotensin receptor blockers (ARBs), and diuretics: Xicotil may reduce the antihypertensive effect of these agents and, particularly in combination with diuretics, increases the risk of acute renal impairment ("triple whammy" effect).
• Lithium: Xicotil can reduce renal clearance of lithium, leading to increased plasma lithium levels and toxicity; lithium levels should be monitored.
• Methotrexate: Xicotil can reduce renal clearance of methotrexate, increasing the risk of methotrexate toxicity, especially at higher methotrexate doses.
• Corticosteroids and SSRIs: concurrent use increases the risk of gastrointestinal ulceration and bleeding.
• Cyclosporine: increased risk of nephrotoxicity when used together.

Side effects of Xicotil are generally dose- and duration-related and consistent with the NSAID class.

Common

• Dyspepsia, nausea, abdominal pain
• Diarrhea or constipation
• Headache, dizziness
• Peripheral edema
• Skin rash

Less Common / Serious

• Gastrointestinal ulceration, bleeding, or perforation
• Elevated liver enzymes
• Renal impairment, fluid retention, hypertension
• Tinnitus, vertigo

Rare but Serious

• Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
• Anaphylaxis, bronchospasm (especially in aspirin-sensitive individuals)
• Cardiovascular thrombotic events (myocardial infarction, stroke)

Pregnancy: Xicotil should be avoided during pregnancy unless clearly necessary. Use during the first and second trimesters should occur only if the potential benefit justifies the potential risk to the fetus, and only under medical supervision. Xicotil, like other NSAIDs, is contraindicated during the third trimester of pregnancy because of the risk of premature closure of the fetal ductus arteriosus, fetal renal impairment, and complications during labor and delivery.

Lactation: It is not established whether Xicotil is excreted in human breast milk; because many NSAIDs pass into breast milk, use during breastfeeding is not recommended unless a physician determines the benefit outweighs the potential risk to the infant.

Xicotil shares the cardiovascular and gastrointestinal risks common to the NSAID class:

• Cardiovascular risk: NSAIDs, including Xicotil, may increase the risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal; this risk may increase with duration of use and in patients with existing cardiovascular disease or risk factors.
• Gastrointestinal risk: NSAIDs increase the risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can occur at any time and without warning symptoms, especially in elderly patients.
• Renal effects: Long-term use may impair renal function, particularly in patients with pre-existing renal impairment, heart failure, liver dysfunction, or those on diuretics or ACE inhibitors/ARBs; adequate hydration should be maintained.
• Hepatic effects: Elevations of liver enzymes may occur; discontinue if signs of liver dysfunction develop.
• Delayed onset of full effect: Because of its long half-life, it may take 1-2 weeks of regular once-daily dosing for Xicotil to reach steady-state plasma levels and full anti-inflammatory effect.
• Fluid retention: Use with caution in patients with a history of hypertension or heart failure due to potential fluid retention and edema.
• Masking of infection signs: As an anti-inflammatory and antipyretic agent, Xicotil may mask the usual signs of infection.

For hypersensitivity, gastrointestinal bleeding, severe heart failure, severe renal/hepatic impairment, and third-trimester pregnancy, see Contraindications.

Symptoms of Xicotil overdose may include nausea, vomiting, abdominal pain, gastrointestinal bleeding, drowsiness, dizziness, headache, and in severe cases, hypotension, respiratory depression, seizures, or acute kidney injury.

There is no specific antidote for Xicotil overdose. In case of suspected overdose, seek immediate medical attention or contact emergency services / a poison control center. Treatment is supportive and symptomatic, and should be initiated promptly by qualified medical personnel; do not attempt to manage an overdose at home.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Elderly

Elderly patients are at greater risk for serious gastrointestinal, renal, and cardiovascular adverse effects with Xicotil. Use the lowest effective dose for the shortest duration and monitor closely.

Renal Impairment

Xicotil should be used with caution in patients with mild to moderate renal impairment, with close monitoring of renal function; it is contraindicated in severe renal impairment (see Contraindications).

Hepatic Impairment

Use with caution in mild to moderate hepatic impairment, with monitoring of liver function; Xicotil is contraindicated in severe hepatic impairment (see Contraindications).

Pediatric Use

Safety and efficacy of Xicotil in children have not been established; its use in the pediatric population is not recommended.

Pregnancy and Lactation

See Pregnancy and Lactation section for full details.

Xicotil should be used for the shortest duration consistent with the treatment goal. For acute musculoskeletal pain, treatment courses of about 7 days (including an initial higher-dose phase) are typical. For chronic conditions such as osteoarthritis, rheumatoid arthritis, or ankylosing spondylitis, treatment duration should be periodically reassessed by the prescribing physician to confirm continued need and to monitor for adverse effects.

Non-Steroidal Anti-Inflammatory Drug (NSAID), oxicam class

Tenoxicam works by non-selectively and reversibly inhibiting cyclooxygenase (COX-1 and COX-2) enzymes, thereby blocking the conversion of arachidonic acid to prostaglandins and thromboxanes. This reduction in prostaglandin synthesis underlies its analgesic, anti-inflammatory, and antipyretic effects, while inhibition of COX-1 in the gastric mucosa and platelets accounts for its gastrointestinal and bleeding-related adverse effects.

C (D in third trimester)

The safety and efficacy of Xicotil have not been established in children, and its use is not recommended in the pediatric population. Alternative analgesic/anti-inflammatory agents with established pediatric safety data should be used for children requiring NSAID therapy.