NERISONE 0.1% CREAM

Indications

• Psoriasis
• Eczema
• Dermatitis
• Allergic skin reactions
• Inflammatory skin conditions

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing.

Adults: Refer to the BNF for specific dosing instructions.

Mechanism of action

Diflucortolone performs its action by inducing lipocortins, which are phospholipase A2 inhibitory proteins, leading to the inhibition of arachidonic acid release. This inhibition results in the decreased formation, release, and activity of endogenous inflammatory mediators. Additionally, it binds to the glucocorticoid receptor, which migrates to the nucleus to stimulate the transcription of anti-inflammatory genes while suppressing pro-inflammatory genes.

Pharmacodynamics

Diflucortolone exhibits anti-inflammatory, antipruritic, and vasoconstrictive effects. Its vasoconstrictive activity reduces blood flow to the inflamed area, decreasing the release of inflammatory mediators and resulting in a soothing effect on the skin. This mechanism effectively alleviates symptoms associated with various inflammatory skin conditions.

Pharmacokinetics

The pharmacokinetics of diflucortolone involve absorption, distribution, metabolism, and excretion typical of corticosteroids. Following application, diflucortolone is absorbed through the skin, with its effects localized to the site of application. The exact metabolic pathways and elimination routes are not specified, but like other corticosteroids, it is likely metabolized by the liver and excreted in urine.

Pregnancy

Use in pregnancy only if the potential benefit justifies the potential risk to the fetus. Limited data on the use of diflucortolone in pregnant women.

Breast-feeding

It is unknown whether diflucortolone is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Topical cream
• Topical ointment

Indications

• Eczema
• Psoriasis
• Inflammatory skin disorders

Dosage

Children: For children aged 1–17 years, apply 1–2 times a day for up to 4 weeks, to be applied thinly.

Adults: Apply 1–2 times a day for up to 4 weeks, to be applied thinly.

Mechanism of action

Diflucortolone valerate exerts its effects by binding to glucocorticoid receptors, leading to the modulation of gene expression. This results in reduced synthesis of pro-inflammatory cytokines and mediators, thus alleviating inflammation and promoting vasoconstriction in the affected tissues.

Pharmacodynamics

As a potent anti-inflammatory agent, diflucortolone valerate inhibits the accumulation of inflammatory cells at the site of application and suppresses the inflammatory response. This results in decreased erythema, swelling, and itching, providing symptomatic relief in skin disorders.

Pharmacokinetics

Diflucortolone valerate is absorbed through the skin, with systemic absorption being minimal when used topically. The drug undergoes metabolism in the liver, and its effects are generally localized to the site of application. The duration and extent of action can vary based on the formulation and the condition being treated.

Adverse effects

• Burning sensation
• Itching
• Skin irritation
• Dryness
• Folliculitis
• Atrophy of the skin
• Striae
• Allergic contact dermatitis

Precautions

• Use with caution in patients with skin infections
• Not recommended for use on the face or in intertriginous areas
• Avoid prolonged use to minimize systemic absorption
• Monitor for potential side effects, especially in pediatric populations

Pregnancy

Diflucortolone valerate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult healthcare provider.

Breast-feeding

It is not known whether diflucortolone valerate is excreted in human milk. Caution should be exercised when administered to a nursing woman.

Storage

Store at room temperature, away from excess heat and moisture. Keep out of reach of children.

Formulations

• 0.1% cream
• 0.1% ointment
• 0.1% lotion

Mechanism of action

Diflucortolone performs its action by the induction of lipocortins which are phospholipase A2 inhibitory proteins and sequentially inhibiting the release of arachidonic acid. The absence of arachidonic acid translates to the inhibition of the formation, release and activity of endogenous chemical inflammatory mediators. Another mechanism of action is the transrepression in which diflucortolone binds to the glucocorticoid receptor which induces its migration to the nucleus where it stimulates the transcription of anti-inflammatory genes like tyrosine aminotransferase, phophoenolpyruvate carboxykinase, IL-10, etc. and suppress the expression of proinflammatory genes like cytokines, growth factors, adhesion molecules, etc.

Pharmacodynamics

Diflucortolone is a steroid with the properties of being an anti-inflammatory, antipruritic and vasoconstrictive. Its activity causes the vasoconstriction of the blood vessels and thus a decrease in the release of inflammatory substances. These actions produce the effect of skin soothed and elimination of the symptoms.