Summary of product characteristics

Name of the medicinal product

Diclofenac sodium 4% Spray Gel (DicloFlex®) w/w Cutaneous Spray, Solution

Qualitative and quantitative composition

ach 1g of solution contains 40 mg of diclofenac sodium. Excipient: 150 mg propylene glycol (E1520) / gram solution For a full list of excipients, see section 6.1.

Pharmaceutical form

Cutaneous spray, solution. A golden-yellow, transparent solution, which turns to a gel-like consistency after administration.

 

Clinical particulars

Therapeutic indications

For the local symptomatic relief of mild to moderate pain and inflammation following acute blunt trauma of small and medium-sized joints and periarticular structures.

Posology and method of administration

For cutaneous use only.

Adults

Sufficient solution of Diclofenac sodium 4% Spray Gel (DicloFlex®) should be sprayed onto the skin of the affected site. Depending on the size of area to be treated 4-5 pump strokes (0.8-1.0 g of spray containing 32-40 mg of diclofenac sodium) should be applied 3 times daily in regular intervals. A maximum single dose of 1.0 g of the product should not be exceeded. The maximum daily dose is 15 pump strokes (3.0 g of spray containing 120 mg of diclofenac sodium).

Diclofenac sodium 4% Spray Gel (DicloFlex®) should be massaged gently into the skin. After this the hands should be washed unless they are the site to be treated. After application some minutes for drying should be allowed before dressing or binding the treated area.

The treatment may be discontinued when the symptoms (pain and swelling) have subsided. Treatment should not be continued beyond 7-8 days without review. The patient is requested to consult the doctor if no improvement is seen after 3 days.

Elderly

The posology is the same as for adults.

Children

There is no experience in children, therefore Diclofenac sodium 4% Spray Gel (DicloFlex®) is not recommended for use in children below 15 years of age. Patients with hepatic or renal insufficiency For the use of Diclofenac sodium 4% Spray Gel (DicloFlex®) in patients with hepatic or renal insufficiency see section 4.4.

Contraindications

Special warnings and precautions for use

Contact with eyes and mucous membranes as well as oral use should be avoided. Diclofenac sodium 4% Spray Gel (DicloFlex®) should only be administered onto intact skin, not on open wounds or diseased skin areas.

Patients should be warned against excessive exposure to sunlight in order to reduce the incidence of photosensitivity. Discontinue if any rash develops. Not for use with occlusive dressings.

The concomitant use of Diclofenac sodium 4% Spray Gel (DicloFlex®) with oral NSAIDs should be cautioned as the incidence of systemic side effects may increase (see section 4.5). Where Diclofenac sodium 4% Spray Gel (DicloFlex®) is applied to a relatively large area of skin (i.e. more than 600 square centimetres of the body surface) and over a prolonged period (i.e. more than 4 weeks), the possibility of systemic side-effects cannot be completely excluded. If such usage is envisaged, the data sheet on diclofenac oral dosage forms should be consulted (for example, there is the potential for hypersensitivity, asthmatic and renal adverse reactions).

Bronchospasm may be precipitated in patients suffering from or with previous history of bronchial asthma or allergenic disease.

Diclofenac sodium 4% Spray Gel (DicloFlex®) should only be used with caution in patients with a history of peptic ulcer, hepatic or renal insufficiency, bleeding diathesis or inflammatory bowel disease as isolated cases with topical diclofenac have been reported.

Diclofenac sodium 4% Spray Gel (DicloFlex®) contains propylene glycol which may cause skin irritation. Diclofenac sodium 4% Spray Gel (DicloFlex®) contains peppermint oil which may cause allergic reactions.

Interaction with other medicinal products and other forms of interaction

The systemic availability of diclofenac from this pharmaceutical presentation is very low. Hence the risk of interactions with other medicinal products is small. Concurrent aspirin or other NSAIDs may result in an increased incidence of adverse reactions (see section 4.4).

Pregnancy and lactation

There are no adequate data from the use of Diclofenac sodium 4% Spray Gel (DicloFlex®) in pregnant and nursing women. Therefore the use is not recommended.

Use in pregnancy:

No evidence of a malformative effect was observed with diclofenac. However, additional epidemiological data is necessary to assess safety. During the last trimester of pregnancy, the use of prostaglandin synthetase inhibitors may result in:

Therefore, during the first six months of pregnancy, Diclofenac sodium 4% Spray Gel (DicloFlex®) should not be used unless clearly necessary and must not be applied to a large area of the skin (i.e. more than 600 square centimetres of the body surface). It must not be used for long-term treatment (> three weeks). Diclofenac sodium 4% Spray Gel (DicloFlex®) is contraindicated (see 4.3) during the last trimester of pregnancy.

Studies in animals have shown reproductive toxicity (see 5.3). The potential risk for humans is unknown.

Use during lactation:

It is not expected that any measurable amount of diclofenac will occur in breast milk following topical application. However, NSAIDs are excreted in human milk. Therefore Diclofenac sodium 4% Spray Gel (DicloFlex®) is not recommended for use in nursing mothers. An application to the breast area of nursing mothers is contraindicated.

Effects on ability to drive and use machines

Patients who experience dizziness or other central nervous disturbances while taking NSAIDs should refrain from driving or operating machinery, but this would be very unlikely using topical preparations.

Undesirable effects

Skin disorders are commonly reported. Skin: Application site reactions, rashes, pruritus and urticaria, drying, reddening, burning sensations, contact dermatitis. In a clinical trial 236 patients with ankle distortions were treated with 4-5 pump strokes of Diclofenac sodium 4% Spray Gel (DicloFlex®) t.i.d. (120 patients) or placebo (116 patients) for 14 days. The following adverse drug reactions were reported:

very common (≥1/10);
common (≥1/100 to <1/10);
uncommon (≥1/1,000 to ≤1/100);
rare (≥1/10,000 to ≤1/1,000);
very rare (≤1/10,000),
not known (cannot be estimated form the available data).

Undesirable effects may be reduced by using the minimum effective dose for the shortest possible duration. The total single dose of product should not exceed 1.0 g (equivalent to 5 pump strokes) of spray.

Nevertheless during long term treatment (> three weeks) and/or when treating large areas (i.e. more than 600 square centimetres of the body surface) there is a possibility of systemic adverse reactions. Reactions like abdominal pain, dyspepsia, gastric and renal disorders may occur.

In patients using topical NSAID preparations asthma has been reported rarely. In isolated cases generalised skin rash, hypersensitivity reactions such as angioedema and photosensitivity reactions have been reported.

Overdose

During recommended use there is practically no risk due to overdosage. It is recommended to wipe off the surplus Diclofenac sodium 4% Spray Gel (DicloFlex®). If, accidentally, Diclofenac sodium 4% Spray Gel (DicloFlex®) has been administered orally symptomatic treatment should be given.

Pharmacological properties

Pharmacodynamic properties

Pharmacotherapeutic group: Antiinflammatory preparations, non-steroids for topical use. ATC code: M02AA 15 Sodium diclofenac is a non-steroidal anti-inflammatory drug (NSAID) which has also analgesic properties. The inhibition of prostaglandin synthesis is considered to be an essential part of its mode of action.

Pharmacokinetic properties

After cutaneous application of 1.5 g Diclofenac sodium 4% Spray Gel (DicloFlex®) a rapid onset of diclofenac absorption can be observed leading to measurable plasma levels of about 1 ng/ml as early as 30 minutes and to maximum levels of about 3 ng/ml at about 24 hours after application.

The achieved systemic concentrations of diclofenac are about 50 times lower than those achieved following oral administration of equivalent amounts of diclofenac. Systemic plasma levels are not supposed to contribute to the efficacy of Diclofenac sodium 4% Spray Gel (DicloFlex®).

Diclofenac is extensively bound to plasma proteins (about 99 %).

Preclinical safety data

In rabbit skin, Diclofenac sodium 4% Spray Gel (DicloFlex®) is classified as non-irritant. Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential of diclofenac.

In rats and rabbits oral doses of diclofenac were not teratogenic but caused embryotoxicity at maternally toxic doses.

Diclofenac did not affect fertility in rats but inhibited ovulation in rabbits and reduced implantation in rats.

In rats, diclofenac resulted in dose-dependent constriction of the fetal ductus arteriosus, dystocia and delayed parturition.

Pharmaceutical particulars

List of excipients

Incompatibilities

Not applicable.

Shelf life

Unopened bottle (25g solution in 30 ml bottle and 12.5g solution in 15 ml bottle): 3 years
Unopened bottles (7.5g solution in 10 ml bottle): 2 years In-use: 6 months

Special precautions for storage

Store in the original package.

Nature and contents of container

Glass bottle with metering pump/nozzle/spray valve and cap. Pack sizes of 7.5 g (10 ml bottle), 12.5 g (15 ml bottle) and 25 g (30 ml bottle) solution. Not all pack sizes may be marketed.

Special precautions for disposal

No special requirements.

Revised Final Day 90 SmPC (UK_H_562-563_01_E01) Revision Date: 09.11.2007