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ketorolac + ropivacaine + epinephrine + triamcinolone acetonide extended-release
- Development stage
- Unknown
- Lead developer
- Walter Reed National Military Medical Center
- Modality
- Small Molecules
- Administration
- Periarticular
01
Overview
This drug is a multi-component periarticular injection (PAI) cocktail combined with Zilretta, an extended-release formulation of triamcinolone acetonide. It is being evaluated by the Walter Reed National Military Medical Center for the management of postoperative pain and reduction of opioid consumption following total knee arthroplasty (TKA). The combination includes ketorolac (a nonsteroidal anti-inflammatory drug), ropivacaine (a long-acting local anesthetic), epinephrine (a vasoconstrictor used to prolong the anesthetic effect), and Zilretta (a microsphere-based corticosteroid). The mechanism of action involves the inhibition of prostaglandin synthesis via COX-1 and COX-2 (ketorolac), the blockade of voltage-gated sodium channels to inhibit nerve conduction (ropivacaine), alpha- and beta-adrenergic stimulation for local vasoconstriction (epinephrine), and glucocorticoid receptor activation to reduce local inflammation (triamcinolone acetonide). This multimodal approach aims to provide superior and prolonged pain relief compared to standard injections.
- Brand names
- Toradol
- Other names
- PAI + ZilrettaPeriarticular Injection + ZilrettaStandard PAI + Zilretta
02
Targets
PGHS-1 (Prostaglandin G/H Synthase 1)NaV (Voltage-gated sodium channels)ADRA1A (α1A)GR (Glucocorticoid receptor)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ADRB1 (β1)
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