TIVORBEX
Clinical safety rating
cautionComprehensive clinical and safety monograph for TIVORBEX (TIVORBEX).
TIVORBEX (dexibuprofen) is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis, which mediates inflammation, pain, and fever.
| Metabolism | Primarily hepatic via CYP2C9 and CYP2C8; minor pathways include glucuronidation. |
| Excretion | Approximately 50% renal excretion as unchanged drug and metabolites; 50% biliary/fecal elimination. |
| Half-life | Approximately 22 hours; allows once-daily dosing. |
| Protein binding | >99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.15 L/kg; indicates limited extravascular distribution, consistent with high protein binding. |
| Bioavailability | Oral: Approximately 87%. |
| Onset of Action | Oral: Clinical effect (analgesia) within 30-60 minutes. |
| Duration of Action | Approximately 24 hours; provides sustained analgesia with once-daily dosing. |
| Molecular Weight | 316.37 |
20 mg orally three times daily
| Dosage form | CAPSULE |
| Renal impairment | No adjustment necessary for GFR >=30 mL/min; avoid use in severe renal impairment (GFR <30 mL/min) or dialysis patients |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 10 mg three times daily; Child-Pugh C: not recommended |
| Pediatric use | Not established; safety and efficacy in pediatric patients under 18 years have not been studied |
| Geriatric use | Initiate at 10 mg three times daily; increase to 20 mg three times daily if tolerated; monitor renal function |
| 1st trimester | Avoid use during first trimester due to potential risk of cardiovascular malformations and miscarriage associated with NSAID use. Consider risks vs benefits; use lowest effective dose for shortest duration if necessary. |
| 2nd trimester | Use with caution during second trimester; avoid prolonged use due to possible oligohydramnios and fetal renal effects. May consider if benefit outweighs risk. |
| 3rd trimester | Contraindicated during third trimester due to risk of premature closure of ductus arteriosus, oligohydramnios, and fetal renal dysfunction. |
Clinical note
Comprehensive clinical and safety monograph for TIVORBEX (TIVORBEX).
| Placental transfer | Crosses placenta; degree of transfer is significant and increases with gestational age. Fetal concentrations may approach maternal levels. |
| Breastfeeding | Minimal excretion into breast milk; considered compatible with breastfeeding. However, due to potential adverse effects on infant's cardiovascular and renal systems, use lowest effective dose for shortest duration and monitor infant for signs of NSAID toxicity. |
| Lactation Rating | L2 (Limited data - probably compatible) |
| Teratogenic Risk | TIVORBEX (tiludronate disodium) is a bisphosphonate. Data from animal studies show developmental toxicity including skeletal and visceral malformations at doses similar to human exposure. In humans, limited data: avoid use during pregnancy, especially in the second and third trimesters due to potential fetal skeletal effects. First-trimester exposure may be associated with fetal anomalies but data are insufficient. |
| Fetal Monitoring | Monitor renal function (serum creatinine, BUN) and serum calcium, phosphate, magnesium. Fetal growth scan and skeletal survey if inadvertent exposure. Monitor for signs of hypocalcemia in neonate. |
| Fertility Effects | May impair fertility in women based on animal studies showing disruption of estrous cycles and reduced pregnancy rates at high doses. Human data on fertility are lacking. Reversible upon discontinuation. |
■ FDA Black Box Warning
NSAIDs cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. Risk may increase with duration of use and in patients with cardiovascular risk factors. TIVORBEX is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Known hypersensitivity to Tivorbex or any excipientSevere hepatic impairmentActive peptic ulcer disease or gastrointestinal bleedingSevere renal impairment (CrCl <30 mL/min)Third trimester of pregnancy
| Precautions | Cardiovascular thrombotic events, Gastrointestinal bleeding, ulceration, and perforation, Renal toxicity including papillary necrosis and fluid retention, Hypertension, Anaphylactoid reactions, Serious skin reactions (e.g., Stevens-Johnson syndrome) |
| Food/Dietary | Take with food or milk to minimize gastrointestinal irritation. Avoid alcohol as it increases risk of gastric bleeding. No specific food restrictions; however, high-fat meals may delay absorption. |
| Clinical Pearls | TIVORBEX (dexketoprofen trometamol) is a NSAID with rapid onset of action (15-30 minutes). Use lowest effective dose for shortest duration. Contraindicated in patients with active peptic ulcer, bleeding disorders, severe heart failure, or hypersensitivity to NSAIDs. Monitor renal function and blood pressure in elderly or dehydrated patients. Avoid concurrent use with other NSAIDs, anticoagulants, or high-dose methotrexate. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not exceed recommended dose or duration. · Avoid alcohol consumption while taking this medication. · Report signs of stomach bleeding (black/tarry stools, vomit with blood), swelling, or chest pain immediately. · Not suitable for children or during pregnancy (especially third trimester). |
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