54 - Diclofenac injectable  pp. 232-235

Diclofenac injectable

By Daniel B. Carr and Ryan Lanier

Image View Previous Chapter Next Chapter

Generic Name: diclofenac sodium for injection

Brand/Proprietary name: Dyloject®

Drug Class: nonsteroidal anti-inflammatory drug

Manufacturer: Javelin Pharmaceuticals, Inc., Cambridge, MA; Javelin was recently acquired by Hospira, Lake Forest, IL

Chemical Structure: see Figure 54.1

Chemical Name: 2-[(2,6-dichlorophenyl)amino]benzeneacetic acid, monosodium (diclofenac sodium)

Molecular Formula: C14H10Cl2NNaO2


Injectable diclofenac sodium (Dyloject™) was developed to provide a “ready to use” injectable dose in a small volume with prolonged stability at room temperature. Solubilization of diclofenac in this novel formulation is accomplished by the use of hydoxypropyl-β-cyclodextrin (“HPβCD”). HPβCD is a cyclic carbohydrate derivative that is pharmacologically inert and is considered ideal for intravenous (IV) applications due to its high water solubility, excellent solubilizing potential, and favorable safety profile. The new formulation of injectable diclofenac is available as a 37.5 mg/mL solution that can be administered as a rapid IV bolus to provide rapid pain relief. Unlike the earlier formulation of diclofenac for injection (marketed as Voltarol® in the UK), the new formulation does not employ organic solvents to solubilize diclofenac, does not contain sulfites, and has proven less irritating to veins when given IV. The new formulation of injectable diclofenac is provided in the form of a solution that is ready to use without buffering, mixing, or dilution. In contrast, the older formulation requires such preparation prior to IV administration and, even then, its potential for venous irritation requires it to be infused slowly over at least 30 minutes.

Bauer KA , Gerson W , Ruais K , Wang J , McNicol E , Lanier RK , Kramer W , Carr DB . Platelet function following administration of a novel formulation of intravenous diclofenac sodium versus active comparators: a randomized, single dose, crossover study in healthy male volunteers. J Clin Anesthesia (in press).
Colucci RD , Wright C , Mermelstein F , Gawarecki DG , Carr DB . Dyloject®, a novel injectable diclofenac solubilised with cyclodextrin: reduced incidence of thrombophlebitis compared to injectable diclofenac solubilised with polyethylene glycol and benzyl alcohol. Acute Pain 2009;11:15–21.
Gandhi M , Prosser D . Our experience of Dyloject™ (intravenous diclofenac) in children. Pediatric Anesthesia 2009;19:908–928.
Leeson RM , Harrison S , Ernst CC , Hamilton DA , Mermelstein FH , Gawarecki DG , Moshman M , Carr DB . Dyloject™, a novel injectable diclofenac formulation, offers greater safety and efficacy than Voltarol® for post-operative dental pain. Reg Anesth Pain Med 2007;32:303–310.
McCormack PL , Scott LJ . Diclofenac sodium (Dyloject®) in post-operative pain. Drugs 2008;68:123–130.