TIVORBEX
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TIVORBEX (TIVORBEX).
| Breastfeeding | No data on presence in human milk. M/P ratio unknown. As a bisphosphonate with potential for accumulation in bone and long half-life, breastfeeding is not recommended during treatment. |
| 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. |
■ 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 dexibuprofen or any NSAID","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs","Perioperative pain in CABG surgery","Active gastrointestinal bleeding or peptic ulcer disease","Severe renal impairment or renal failure","Advanced liver disease"]
| 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)"] |
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| 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. |