Class: Nonsteroidal Anti-inflammatory Agents
VA Class: DE900
Chemical Name: 2-[(2,6-dichlorophenyl)amino]-benzeneacetic acid monosodium salt
Molecular Formula: C₁₄H₁₀C_l2NNaO₂
CAS Number: 15307-79-6
Brands: Solaraze

Medically reviewed by Drugs.com. Last updated on Jan 20, 2020.

• Overview
• Side Effects
• Dosage
• Professional
• Interactions
• More

Introduction

Prototypical NSAIA; phenylacetic acid derivative.^{1 2 3 4 5}

Uses for Diclofenac (Topical)

Actinic Keratoses

Treatment of actinic keratoses.^{1 2 3 4}

Superficial Thrombophlebitis

Has been used topically or orally for the symptomatic treatment of infusion-related superficial thrombophlebitis†.^{8 9}

Diclofenac (Topical) Dosage and Administration

General

Complete healing of the lesions or optimal therapeutic response may not occur until 30 days after cessation of therapy.¹

Administration

Topical Administration

Apply to actinic keratosis lesions as a 3% gel.¹

Dosage

Adults

Actinic Keratoses

Topical

Apply a sufficient amount (usually 0.5 g for each 5 cm × 5 cm lesion) and rub gently onto the lesions twice daily for 60–90 days.¹

Cautions for Diclofenac (Topical)

Contraindications

• Known hypersensitivity to diclofenac or any ingredient in the formulation.¹

Warnings/Precautions

Warnings

Sensitivity Reactions

Sensitivity reactions, including anaphylaxis, possible in patients without prior exposure to diclofenac.¹ Avoid in patients with aspirin triad (aspirin sensitivity, asthma, nasal polyps).¹

General Precautions

GI Effects

Use with caution in patients with active GI ulceration or bleeding.¹

Topical Use

For external use only; avoid contact with eyes.¹ Do not apply to open skin wounds, infected lesions, or exfoliative dermatitis.¹

Safety and efficacy of concomitant use with other topical products (e.g., sunscreens, cosmetics, other topical medications) unknown.¹

Specific Populations

Pregnancy

Category B.¹ Avoid use in third trimester (possible premature closure of ductus arteriosus) or in late pregnancy (possible delay in labor or parturition).¹

Lactation

Discontinue nursing or the drug because of potential risk to nursing infants.¹

Pediatric Use

Safety and efficacy not established in children.¹ Actinic keratoses generally are not seen in the pediatric population; diclofenac sodium gel should not be used by children.¹

Geriatric Use

Actinic keratoses occur frequently in an older patient population.¹ No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.¹

Hepatic Impairment

Use with caution in patients with severe hepatic impairment.¹

Renal Impairment

Use with caution in patients with severe renal impairment.¹

Common Adverse Effects

Contact dermatitis, rash, dry skin, exfoliation (scaling).¹

Interactions for Diclofenac (Topical)

NSAIAs

Potential pharmacologic interaction with oral NSAIAs including analgesic/anti-inflammatory dosages of aspirin.¹

Diclofenac (Topical) Pharmacokinetics

Absorption

Bioavailability

Absorbed into epidermis after topical application to the skin.^{1 2}

Minimal systemic absorption following topical application (serum diclofenac concentrations averaged 20 ng/mL following topical application twice daily for up to 105 days versus 1417 ng/mL following a single 50-mg oral dose of diclofenac sodium).^{1 6}

Distribution

Plasma Protein Binding

Bound to albumin.¹

Elimination

Metabolism

Metabolized in the liver via hydroxylation and conjugation following oral administration; metabolism following topical administration is expected to be similar to that following oral administration.¹

Elimination Route

Mainly excreted in urine following oral administration.¹

Half-life

1–2 hours following oral administration.¹

Stability

Storage

Topical

Gel

20–25°C (may be exposed to 15–30°C).^a Protect from heat; do not freeze.^a

Actions

• Prototypical NSAIA.^{1 2 3 4 5}

• While the mechanism(s) of the topical effects has not been established,^{1 2 3} diclofenac has inhibited angiogenesis and induced neovascular regression in inflammatory tissue in animal models.^{2 3}

• NSAIAs, including diclofenac, may inhibit angiogenesis through inhibition of substance P or by blocking the angiogenic effects of prostaglandin E₂ (PGE₂).²

• For topical use in the treatment of actinic keratoses, diclofenac sodium is commercially available as a 3% gel with benzyl alcohol, hyaluronate sodium, polyethylene glycol monomethyl ether, and purified water.¹ The contribution of individual vehicle components to the efficacy of diclofenac sodium gel remains to be established.¹

Advice to Patients

• Risk of adverse effects, including irritant or allergic contact dermatitis.¹ Importance of reporting signs and symptoms of adverse dermal reactions.¹ Necessity of interrupting therapy if severe dermal reactions occur.¹

• Avoid exposure to sunlight and use of sunlamps.¹

• Importance of monitoring and follow-up evaluation.¹

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription, OTC, or herbal products, as well as any concomitant illness.¹ Safety and efficacy of use with other topical products (e.g., sunscreens, cosmetics, other topical medications) is unknown.¹

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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