diclofenac topical

Action and Spectrum

Actions and Spectrum 

diclofenac topical works by inhibiting the synthesis of prostaglandins, which are substances that play a role in pain and swelling. diclofenac helps to lessen pain, edema, and inflammation in the area where it is applied by preventing prostaglandin synthesis. 

The spectrum of diclofenac topical is generally limited to the area of application. It mainly treats musculoskeletal problems like arthritis, sprains, strains, and other locally inflamed conditions. 

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Hypertension  

Asthma 

Conjunctivitis 

Hematuria 

Alepesia 

Photosensitivity 

Diarrhea   

Pneumonia 

Dyspepsia 

Edema 

Chest pain 

Skin ulcer 

>10% 

Contact dermatitis (19-33%) 

Pain (15-26%)  

Paresthesia (≤ 20%) 

Exfoliation (6-24%) 

Pruritus (≤ 52%) 

Dry skin (25-27%) 

Rash (20-35%) 

<1% 

Application site pruritus 

Post marketing reports 

Photoallergic reactions  

Adverse reactions: musculoskeletal stiffness hypoesthesia, gait disturbance 

Hypersensitivity 

Dermal allergic reactions  

Burning sensations 

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• People with history of known hypersensitivity to or allergy to diclofenac or any other ingredient in the formulation should not use diclofenac topical. 
• Patients with a history of asthma or other allergic reactions like allergic rhinitis or urticaria may experience bronchospasm after taking diclofenac topical. 

Caution: 

• Patients with a history of sensitive skin or allergic skin responses should use diclofenac topical with caution. Prior to applying it to larger portions of the skin, it is recommended to conduct a patch test on a tiny piece of the skin. 
• Applying topical diclofenac to open wounds, skin injury, or mucous membranes is not advised. 
• When applying topical diclofenac to people who have liver or kidney disease, use caution. These patients may have greater diclofenac systemic absorption, which could have negative effects. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

The enzyme cyclooxygenase (COX), specifically the COX-1 and COX-2 isoforms, are inhibited by diclofenac topical. The prostaglandins, which act as mediators of pain, inflammation, and fever, are produced by COX enzymes. diclofenac topical inhibits COX, which lowers prostaglandin production and lessens pain and inflammation when it is applied. 

Pharmacodynamics 

By preventing the synthesis of prostaglandins, which are involved in the experience of pain, diclofenac topical serves as an analgesic. 

The immunological reaction at the application site may be impacted by diclofenac. It might lessen the migration of inflammatory cells to the site of damage or inflammation, including neutrophils and macrophages. 

Pharmacokinetics 

Absorption   

When diclofenac is topically given as a gel or cream, it is absorbed through the skin and underlying tissues. diclofenac normally absorbs very little through the skin, exposing the body into very little amount.  

Distribution 

In the tissues close to the application site, diclofenac topical distributes locally. The medication works its anti-inflammatory and analgesic effects once it has reached therapeutic concentrations in the underlying tissues. 

Metabolism 

diclofenac topical undergoes a variety of metabolic processes, such as oxidation and conjugation. Both 4′- and 5-hydroxydiclofenac are the main metabolites produced.  

Elimination and excretion 

Approximately 65% of the diclofenac metabolites are eliminated in the urine and 35% in the feces, respectively. diclofenac topical elimination half-life can change, it typically lasts 1 to 2 hours.

Adminstartion

Administration 

diclofenac topical formulations, such as gels or creams, are typically applied directly to the skin at the site of pain or inflammation.

Patient Information Leaflet

Patient information leaflet 

Generic Name: diclofenac topical 

Why do we use diclofenac topical? 

diclofenac topical helps ease pain and reduce inflammation in osteoarthritis-affected joints. Joints like the knees, hands, or hips are frequently treated with it. For the treatment of rheumatoid arthritis symptoms such joint pain and swelling, diclofenac topical may be administered. 

diclofenac topical can be used to treat minor injuries to the muscles, tendons, or ligaments that result in sprains, strains, and accompanying pain and inflammation.