Emulgel 1%: One gram of Voltaren Emulgel 1% contains 11.6 mg (1.16% w/w) of diclofenac diethylamine, which corresponds to 10 mg (1% w/w) of diclofenac sodium.
Emulgel 2%: One gram of Voltaren 12 Hours Emulgel 2% Gel contains 23.2 mg (2.32% w/w) of diclofenac diethylamine, which corresponds to 20 mg (2% w/w) of diclofenac sodium.
Excipients/Inactive Ingredients: Propylene glycol (50 mg/g gel), Butylhydroxytoluene (0.2 mg/g gel), Carbomer, Cocoyl caprylocaprate, Diethylamine, Isopropyl alcohol, Liquid paraffin, Macrogol cetostearyl ether, Oleyl alcohol, Perfume eucalyptus sting, Purified water.
ATC Code: M02AA15.
Pharmacology: Pharmacodynamics: Mechanism of action: Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with effective analgesic, anti-inflammatory and antipyretic properties. Diclofenac exerts its therapeutic effects primarily through inhibition of prostaglandin synthesis by cyclo-oxygenase 2 (COX-2).
Voltaren 12 Hours Emulgel 2% Gel and Emulgel 1% is an anti-inflammatory and analgesic preparation for topical application use. In inflammation and pain of traumatic or rheumatic origin, Voltaren 12 Hours Emulgel 2% Gel and Voltaren Emulgel 1% relieves pain and decreases swelling.
Pharmacokinetics: Absorption: The quantity of diclofenac absorbed through the skin is proportional to the size of the treated area, and depends on both the total dose applied and the degree of skin hydration.
Emulgel 1%: Absorption amouns to about 6% of the applied dose of diclofenac after topical application of 2.5g Voltaren Emulgel 1% on 500 cm2 skin, determined by total renal elimination, compared with Voltaren tablets. A 10-hour occlusion leads to a three-fold increase in the amount of diclofenac absorbed.
Emulgel 2%: Following topical application to an area of skin approximately 400 cm2 in size, the level of systemic exposure, determined on the basis of the plasma concentrations reached under Voltaren 12 Hours Emulgel 2% Gel (2 applications a day), was equivalent to that measured with Diclofenac 1.16 % Emulgel (4 applications/day). The relative bioavailability of diclofenac (AUC ratio) lay at 4.5% (with an equivalent diclofenac sodium dose) on day 7 for Voltaren 12 Hours Emulgel 2% Gel compared with the tablet formulation. Application of a moisture permeable and water-vapour permeable bandage did not alter absorption.
Distribution: Diclofenac concentrations have been measured from plasma, synovial tissue and synovial fluid after topical administration of a diclofenac diethylamine gel to hand and knee joints. Maximum plasma concentrations are approximately 100 times lower than after oral administration of the same quantity of diclofenac. 99.7% of diclofenac is bound to serum proteins, mainly albumin (99.4%). Diclofenac accumulates in the skin which acts as reservoir from where there is a sustained release of drug into underlying tissues. From the skin and underlying tissue, diclofenac preferentially distributes and persists in deep inflamed tissues (such as the joint), rather than in the bloodstream. Diclofenac is found in tissues at concentrations up to 20 times higher than in plasma.
Metabolism: The biotransformation of diclofenac involves single and multiple hydroxylation steps followed by glucuronidation, and glucuronidation of the intact molecule.
Elimination: The total systemic clearance of diclofenac from plasma is 263 ± 56 ml/min. The terminal plasma half-life is 1-2 hours. Four of the metabolites, including the two active ones, also have short plasma half-lives of 1-3 hours. One metabolite, 3'-hydroxy-4'-methoxy-diclofenac, has a longer half-life but is virtually inactive. Diclofenac and its metabolites are excreted mainly in the urine.
Special populations, Renal and hepatic impairment: No accumulation of diclofenac and its metabolites is to be expected in patients suffering from renal impairment. In patients with chronic hepatitis or non-decompensated cirrhosis, the kinetics and metabolism of diclofenac are the same as in patients without liver disease.
Toxicology: Preclinical safety data: Non-clinical data from acute and repeated dose toxicity studies, as well as from genotoxicity, and carcinogenicity studies with diclofenac revealed no specific hazard for humans at the intended therapeutic doses. Topical diclofenac was well tolerated in a variety of studies. There was no potential for phototoxicity and diclofenac containing gel caused no skin sensitisation.
Reproductive toxicology: Diclofenac demonstrated no evidence of impairment on the fertility of male or female rats. There was no evidence that diclofenac had a teratogenic potential in mice, rats or rabbits. The prenatal, perinatal and postnatal development of the offspring was not affected.
For the external treatment of pain, inflammation and swelling in the following situations: trauma of the tendons, ligaments, muscles and joints, e.g. sprains, contusions, strains and sport-related back pain or backache following accidents;
localised forms of soft tissue rheumatism such as tendinitis (tennis elbow), shoulder-hand syndrome, bursitis, periarthropathy;
and for the symptomatic treatment of osteoarthritis of small and medium-sized joints located close to the skin such as the finger joints or knee joints.
Emulgel 1%: Adults and adolescents aged 12 years and over: This medicine should be applied over the affected area 3 or 4 times daily and rubbed gently into the skin. The amount needed depends on the size of the painful area: 2 g to 4 g Voltaren Emulgel 1% (a quantity ranging in size from a cherry to a walnut) is sufficient to treat an area of about 400-800 cm2. The duration of treatment depends on the indication and clinical response.
Emulgel 2%: Adults and adolescents aged 12 years and over: Voltaren 12 Hours Emulgel 2% Gel provides lasting pain relief of up to 12 Hours (applied 2 times daily - morning and evening). It should be rubbed gently into the skin at the affected area. The amount needed depends on the size of the painful area: 2 g to 4 g (a quantity ranging in size from a cherry to a walnut) of gel is sufficient to treat an area of about 400-800cm2. The duration of treatment depends on the indication and clinical response.
Patients should consult doctor if the condition does not improve or worsens within 7 days of starting treatment.
Voltaren 12 Hours Emulgel 2% Gel and Emulgel 1% should not be used for more than 14 days.
Voltaren 12 Hours Emulgel 2% Gel and Emulgel 1% can also be used by as adjunctive therapy with other pharmaceutical forms of Voltaren.
After application, the hands should be washed, unless they are the site being treated.
Children under 12 years: The use and safety of Voltaren 12 Hours Emulgel 2% Gel and Emulgel 1% in children under 12 years has not been tested systematically and is not recommended.
Patients over 65 years of age: The usual adult dosage may be used.
Route of Administration: For cutaneous use only.
The low systemic absorption of topical diclofenac renders overdose very unlikely. However undesirable effects, similar to those observed following an overdose of diclofenac tablets, can be expected if topical diclofenac is ingested. In the event of accidental ingestion, resulting in significant systemic adverse effects, general therapeutic measures normally adopted to treat poisoning with non-steroidal anti-inflammatory medicines should be used. Further management should be as clinically indicated or as recommended by the national poisons centres where available.
Known hypersensitivity to diclofenac or to any of the excipients (see list of excipients); patients in whom asthma, angioedema, urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs); during the last trimester of pregnancy.
The possibility of experiencing systemic adverse events (those associated with the use of systemic forms of diclofenac) should be considered if topical diclofenac is used at a higher dosage or for a longer period of time than recommended (see Recommended Dosage). Topical diclofenac should be applied only to intact, non-diseased skin, and not to skin wounds or open injuries. It should not be allowed to come into contact with the eyes or mucous membranes and should not be ingested. Discontinue thetreatment if a skin rash develops after applying the product. Topical diclofenac can be used with non-occlusive bandages but should not be used with an airtight occlusive dressing.
Information concerning excipients: Emulgel 2% Gel: Contains propylene glycol, which may cause mild, localised skin irritation in some people, and butylhydroxytoluene, which may cause local skin reactions (e.g. contact dermatitis) or irritation to the eyes and mucous membranes. Emulgel 1%: Contains propylene glycol and benzyl benzoate, which may cause mild, localised skin irritation in some people.
Effects on ability to drive and use machines: Cutaneous application of Voltaren Emulgel 2% Gel and Emulgel 1% has no influence on the ability to drive and use machines.
Pregnancy: There are insufficient data on the use of diclofenac in pregnant women. Diclofenac should be used during the first two trimesters of pregnancy only if the expected benefit justifies the potential risk to the foetus. As with other NSAIDs, use of diclofenac during the third trimester of pregnancy is contraindicated owing to the possibility of uterine inertia, fetal renal impairment with subsequent oligohydramnios and/or premature closure of the ductus arteriosus.
Lactation: It is not known whether topical diclofenac is excreted in breast milk. Diclofenac should only be used during lactation if the expected benefit justifies the potential risk to the newborn. If there are compelling reasons for using it, it should not be applied to the breasts nor should it be used at a higher dosage or for a longer period of time than recommended.
Adverse reactions are listed as follows, by system organ class and frequency. Frequencies are defined as: 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). Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness. (See table.)
Click on icon to see table/diagram/image
Since systemic absorption of diclofenac from topical application is very low, such interactions are very unlikely.
M02AA15 - diclofenac ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.
Emulgel 1% (white to practically white, soft homogeneous, creamy-like gel) x 20 g, 50 g. 2% (white to practically white, soft, homogenous, cream-like gel) x 30 g, 50 g.