Mikromol featured product: Diclofenac

Featured product 

Diclofenac 

API and impurity reference standards

Introduction

Diclofenac (sold under the brand names Voltaren, Solaraze, Cambia and Lofena, among many others) is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and anti-inflammatory properties. It is commercially available as tablets, capsules, dragees, suppositories, gels, patches, eye drops, and as a solution of injection. Diclofenac is used in the management of pain, various inflammatory conditions , and dysmenorrhea (menstrual cramps).

Diclofenac was patented in 1965, and first introduced in Switzerland in 1973, before coming into medical use in the United States in 1988. Also available as a generic medication, it was the US’s 72^nd most commonly prescribed medicine in 2020, with over nine million prescriptions. Diclofenac sodium was initially developed with the goal of improving the safety profile of diclofenac and providing convenient, once-daily dosing for the treatment of chronic pain. New drug products, using diclofenac potassium salt, are associated with faster absorption and rapid pain relief. These include diclofenac potassium immediate-release tablets, liquid-filled soft gel capsules, and powder for oral solution.

Mechanism of action

Diclofenac acts through the inhibition of the enzyme cyclooxygenase (COX-1 and -2) and the reduced synthesis of prostaglandins (PGs). PGs have broad activity in inflammation and pain signalling, and are  involved in modulation of nociception – mediating acute inflammation via their IP and EP₂ receptors. By limiting the production of these PGs at the site of injury, diclofenac can reduce inflammation and pain. In addition, PGE₂ can cross the blood-brain barrier and act on receptors on thermoregulatory neurons - triggering an increase in heat generation and reduction in heat loss, and resulting in a fever. By inhibiting PGE₂ generation, diclofenac can reduce the activity of these neurons. Diclofenac has a short half-life of one to three hours and is therefore also administered in sustained-release forms.

Why not browse our range of diclofenac API and impurity reference standards below?