Robenacoxib
**Robenacoxib** is a highly selective coxib-class non-steroidal anti-inflammatory drug (NSAID) licensed specifically for use in dogs and cats. Key clinical features include: * **Tissue Selectivity**: It exhibits a unique pharmacokinetic profile where it clears rapidly from the central blood compartment but persists at higher concentrations and for longer durations at sites of active inflammation (such as inflamed joints). This "tissue-sparing" effect helps maximize efficacy while minimizing systemic adverse effects. * **High COX-2 Specificity**: It is approximately 140 times more selective for COX-2 in dogs and 500 times more selective in cats compared to COX-1, making it one of the most COX-2 specific NSAIDs available in veterinary medicine. * **Indications**: Primarily used for the management of chronic osteoarthritis pain in dogs, acute musculoskeletal pain in cats, and perioperative pain associated with soft tissue or orthopedic surgeries in both species.
Mecanismo: Robenacoxib exerts its anti-inflammatory and analgesic effects by selectively inhibiting the **Cyclooxygenase-2 (COX-2)** enzyme. **Arachidonic Acid** → **COX-2 Enzyme** → **Prostaglandin E2 (PGE2)** and other inflammatory mediators. By specifically targeting the inducible **COX-2** isoform, robenacoxib effectively blunts the production of prostaglandins responsible for pain, inflammation, and fever. Because it largely spares the constitutive **COX-1** enzyme, it preserves the homeostatic prostaglandins that are crucial for maintaining gastrointestinal mucosal integrity, renal blood flow, and normal platelet function.
Dosificación por especie
- Acute pain and inflammation associated with musculoskeletal disorders · 1 mg/kg; with a range of 1-2.4 mg/kg · PO · once daily · up to 6 days · Equates to 1 tablet for cats weighing 2.5-<6 kg and 2 tablets for cats weighing 6 kg-<12 kg. Give either without food or with a small amount of food; tablets should not be divided or broken.
- Pain and inflammation associated with chronic osteoarthritis (Note: Label likely intended for surgical pain based on injection formulation) · 2 mg/kg · SC · once · Administer approximately 30 minutes before the start of surgery.
- Perioperative analgesia · 2 mg/kg · SC · q24h · Maximum of 2 doses · Administer approximately 30 minutes before the start of surgery.
- Acute and chronic musculoskeletal pain and inflammation · 1-2 mg/kg · PO · q24h · As directed by veterinarian · May be mixed with a small amount of food. Monitoring is recommended for long-term treatment (>12 weeks).
- Pain and inflammation associated with chronic osteoarthritis · 1 mg/kg with a range of 1-2 mg/kg · PO · once daily · Discontinue after 10 days if no clinical improvement seen · Give at the same time every day. For long term treatment, can adjust to lowest effective dose.
- Pain and inflammation associated with orthopedic or soft tissue surgery · 2 mg/kg · SC · once · Administer approximately 30 minutes before the start of surgery.
- Perioperative analgesia (orthopaedic and soft tissue surgery) · 2 mg/kg · SC · q24h · Maximum of 2 doses · Administer approximately 30 minutes before the start of surgery.
Vías de administración
Contraindicaciones
- Patients with active gastrointestinal ulcers
- Hypersensitivity to robenacoxib or its excipients
- Dogs with hepatic disease
- Dehydrated, hypovolaemic, or hypotensive patients
- Patients with pre-existing gastrointestinal disease or ulceration
- Patients with blood clotting disorders
- Pregnant or lactating animals
- Dogs < 12 weeks of age or < 2.5 kg body weight
- Cats < 16 weeks of age or < 2.5 kg body weight
- Perioperative use in animals with renal disease (not advisable)
Efectos adversos
- Decreased appetite
- Vomiting
- Soft feces
- Diarrhea
- Blood in feces (melena/hematochezia)
- Mild gastrointestinal signs (vomiting, soft feces, diarrhea)
- Gastrointestinal ulceration or bleeding (rare but severe)
- Renal toxicity (especially if hypotensive or dehydrated)
- Hepatic accumulation (in patients with pre-existing liver disease)
Interacciones farmacológicas
- ACE Inhibitors (e.g., enalapril, benazepril) · Some NSAIDs can reduce effects on blood pressure
- Aspirin · May increase the risk of gastrointestinal toxicity (e.g., ulceration, bleeding, vomiting, diarrhea)
- Corticosteroids (e.g., prednisone) · May increase the risk of gastrointestinal toxicity (e.g., ulceration, bleeding, vomiting, diarrhea)
- Digoxin · NSAIDs may increase serum levels
- Fluconazole · Administration has increased plasma levels of celecoxib in humans and potentially could also affect robenacoxib levels in dogs
- Furosemide · NSAIDs may reduce the saluretic and diuretic effects
- Highly Protein Bound Drugs (phenytoin, valproic acid, oral anticoagulants, salicylates, sulfonamides, etc.) · As robenacoxib is highly bound to plasma proteins (>99%), it may displace other highly bound drugs or be displaced by them, potentially leading to increased serum levels and toxicity
- Methotrexate · Serious toxicity has occurred when NSAIDs have been used concomitantly; use together with extreme caution
- Nephrotoxic Drugs (e.g., aminoglycosides, amphotericin B) · May enhance the risk of nephrotoxicity development
- Other NSAIDs · Increased risk of severe gastrointestinal ulceration and renal toxicity. Require a 3-5 day wash-out period. · major
- Glucocorticoids · Increased risk of severe gastrointestinal ulceration and bleeding. · major
Monitoreo
- Baseline and periodic physical examinations to assess clinical efficacy and adverse effects
- Baseline and periodic CBC, serum biochemistry (liver and renal function), electrolytes, and urinalysis
- For long-term therapy in dogs: Monitor liver enzymes at the start of therapy, and after 2, 4, and 8 weeks; then every 3-6 months
- Discontinue therapy if liver enzymes increase markedly or if accompanied by clinical signs (anorexia, apathy, vomiting)
- Clinical response (reduction in pain and inflammation)
- Gastrointestinal signs (monitor for vomiting, diarrhea, or melena)
- Renal parameters (BUN, Creatinine, USG) and hepatic enzymes, especially prior to anesthesia or during long-term therapy (>12 weeks)
Sobredosis
Acute overdoses may potentially cause **gastrointestinal, kidney, or liver toxicity**. Interestingly, chronic toxicity studies in healthy young dogs (up to 10 mg/kg/day for 6 months) and cats (up to 10 mg/kg SC for 3 days) did not produce signs of toxicity. **Treatment**: If an acute overdose occurs, symptomatic and supportive therapy is recommended. This may include the administration of gastrointestinal protective agents (e.g., sucralfate, omeprazole), IV fluid therapy for forced diuresis and renal support, and contacting an animal poison control center for guided management.
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