VOLTAROL OPTHA MULTIDOSE Eye drops solution Ref.[6793] Active ingredients: Diclofenac

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2014  Publisher: Laboratoires Thea, 12, rue Louis-Blรฉriot, 63017 Clermont-Ferrand Cedex 2, France

Pharmacodynamic properties

Voltarol Ophtha Multidose contains diclofenac sodium, a non-steroidal compound with pronounced anti-inflammatory and analgesic properties. Inhibition of prostaglandin biosynthesis, which has been demonstrated experimentally, is regarded as having an important bearing on its mechanism of action. Prostaglandins play a major role in the causation of inflammation and pain.

In clinical trials, Voltarol Ophtha has been found to:

  • Inhibit miosis during cataract surgery.
  • Reduce inflammation following surgical interventions.
  • Reduce ocular pain and discomfort associated with corneal epithelial defects after excimer PRK surgery or accidental non-penetrating trauma.
  • Reduce the incidence of angiographic cystoid macular oedema after cataract surgery but clinical significance remains to be established.
  • Reduce ocular inflammation and discomfort more effectively than topical steroids after strabismus surgery whilst avoiding steroidal adverse effects such as delayed conjunctival wound healing and raised intraocular pressure.
  • Reduce ocular inflammation, pain and discomfort (photophobia, burning/stinging, foreign body sensation, deep headache-like ocular pain and itching) more effectively than placebo eye drops after corneal incisional surgery such as radial keratotomy.

The effective daily dose after ocular application of Voltarol Ophtha Multidose (approximately 0.25-0.5 mg diclofenac sodium) corresponds to less than 1% of the daily dose recommended for Voltarol in rheumatic indications.

Voltarol Ophtha Multidose Eye Drops contain a cyclodextrin, hydroxypropyl ฮณ-cyclodextrin (HPฮณ-CD). Cyclodextrins (CDs) increase the aqueous solubility of some lipophilic water-insoluble drugs. It is believed that CDs act as true carriers by keeping hydrophobic drug molecules in solution and delivering them to the surface of biological membranes.

Pharmacokinetic properties

In rabbits, peak concentrations of 14C-labelled diclofenac could be demonstrated in the cornea and conjunctiva 30 minutes after application. The highest amounts are found in these two tissues and in the choroid and retina. Elimination was fast and almost complete after 6 hours.

Penetration of diclofenac into the anterior chamber has been confirmed in humans. No measurable levels of diclofenac could be found in humans after ocular application of diclofenac sodium eye drops.

Preclinical safety data

Preclinical data of systemically applied diclofenac from acute and repeated dose toxicity studies, as well as from genotoxicity and carcinogenicity studies revealed no specific hazard for humans at the intended therapeutic doses.

In reproductive and developmental toxicity studies systemic diclofenac has been shown to cross the placental barrier in mice and rats. Whilst no teratogenic effects have been demonstrated, maternally toxic doses were associated with dystocia, prolonged gestation, decreased foetal survival, and intrauterine growth retardation. The effects of diclofenac on fertility and delivery as well as the constriction of the ductus arteriosus in utero are pharmacological consequences of this class of prostaglandin synthesis inhibitors

Local ocular tolerance and toxicity of Voltarol Ophtha and Voltarol Ophtha Multidose 0.1% eye drops (containing hydroxypropyl-gamma cyclodextrin) were investigated and no evidence of toxicity and local adverse effects was found.

Concentrations of HP-gamma-CD in plasma and aqueous humor were below detection limits (1 nMol/mL) in rabbits after single or four times daily (q.i.d.) ocular administration of Voltarol Ophtha Multidose 0.1% eye drops.

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