Solaraze Information
Solaraze (Diclofenac) Description
Solaraze (Diclofenac) (diclofenac sodium) Gel, 3%, contains the active ingredient, diclofenac sodium, in a clear, transparent, colorless to slightly yellow gel base. Diclofenac sodium is a white to slightly yellow crystalline powder. It is freely soluble in methanol, soluble in ethanol, sparingly soluble in water, slightly soluble in acetone, and partially insoluble in ether. The chemical name for diclofenac sodium is:
Sodium [-(2,6-dichloranilino) phenyl] acetate
Diclofenac sodium has a molecular weight of 318.13.
The CAS number is CAS-15307-79-6. The structural formula is represented below:
Solaraze (Diclofenac) Gel also contains benzyl alcohol, hyaluronate sodium, polyethylene glycol monomethyl ether, and purified water.
1 g of Solaraze (Diclofenac) (diclofenac sodium) Gel contains 30 mg of the active substance, diclofenac sodium.
Solaraze (Diclofenac) Clinical Pharmacology
The mechanism of action of diclofenac sodium in the treatment of actinic keratoses (AK) is unknown. The contribution to efficacy of individual components of the vehicle has not been established.
Solaraze (Diclofenac) Indications And Usage
Solaraze (Diclofenac) (diclofenac sodium) Gel is indicated for the topical treatment of actinic keratoses (AK). Sun avoidance is indicated during therapy.
Solaraze (Diclofenac) Clinical Studies
Clinical trials were conducted involving a total of 427 patients (213 treated with Solaraze (Diclofenac) and 214 with a gel vehicle). Each patient had no fewer than five AK lesions in a major body area, which was defined as one of five 5 cm X 5 cm regions: scalp, forehead, face, forearm and hand. Up to three major body areas were studied in any patient. All patients were 18 years of age or older (male and female) with no clinically significant medical problems outside of the AK lesions and had undergone a 60-day washout period from disallowed medications (masoprocol, 5-fluorouracil, cyclosporine, retinoids, trichloroacetic acid/lactic acid/peel, 50% glycolic acid peel) and hyaluronan-containing cosmetics. Patients were excluded from participation for reasons of known or suspected hypersensitivity to any Solaraze (Diclofenac) ingredient, pregnancy, allergies to aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs), or other dermatological conditions which might affect the absorption of the study medication. Application of dermatologic products such as sunscreens, cosmetics, and other drug products was not permitted. Patients were instructed to apply a small amount of Solaraze (Diclofenac) Gel (approximately 0.5 g) onto the affected skin, using their fingers, and gently smoothing the gel over the lesion. In addition, all patients were instructed to avoid sun exposure. Complete clearing of the AK lesions 30 days after completion of treatment was the primary efficacy variable. No long-term patient follow-ups, after the 30-day assessments, were performed for the detection of recurrence.
Solaraze (Diclofenac) Contraindications
Solaraze (Diclofenac) (diclofenac sodium) Gel is contraindicated in patients with a known hypersensitivity to diclofenac, benzyl alcohol, polyethylene glycol monomethyl ether 350 and/or hyaluronate sodium.
Solaraze (Diclofenac) Warnings
As with other NSAIDs, anaphylactoid reactions may occur in patients without prior exposure to diclofenac. Diclofenac sodium should be given with caution to patients with the aspirin triad. The triad typically occurs in asthmatic patients who experience rhinitis with or without nasal polyps, or who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.
Solaraze (Diclofenac) Precautions
Solaraze (Diclofenac) (diclofenac sodium) Gel should be used with caution in patients with active gastrointestinal ulceration or bleeding and severe renal or hepatic impairments. Solaraze (Diclofenac) should not be applied to open skin wounds, infections, or exfoliative dermatitis. It should not be allowed to come in contact with the eyes.
The safety of the concomitant use of sunscreens, cosmetics or other topical medications and Solaraze (Diclofenac) is unknown.
In clinical studies, localized dermal side effects such as contact dermatitis, exfoliation, dry skin and rash were found in patients treated with Solaraze (Diclofenac) at a higher incidence than in those with placebo.
Patients should understand the importance of monitoring and follow-up evaluation, the signs and symptoms of dermal adverse reactions, and the possibility of irritant or allergic contact dermatitis. If severe dermal reactions occur, treatment with Solaraze (Diclofenac) may be interrupted until the condition subsides. Exposure to sunlight and the use of sunlamps should be avoided.
Safety and efficacy of the use of Solaraze (Diclofenac) together with other dermal products, including cosmetics, sunscreens, and other topical medications on the area being treated, have not been studied.
There did not appear to be any increase in drug-related neoplasms following daily topical applications of diclofenac sodium gel for 2 years at concentrations up to 0.035% diclofenac sodium and 2.5% hyaluronate sodium in albino mice. (Note: Solaraze (Diclofenac) contains 3% diclofenac sodium.) When administered orally for 2 years, diclofenac showed no evidence of carcinogenic potential in rats given diclofenac sodium at up to 2 mg/kg/day (3 times the estimated systemic human exposure*), or in mice given diclofenac sodium at up to 0.3 mg/kg/day in males and 1 mg/kg/day in females (25% and 83%, respectively, of the estimated systemic human exposure).
A photococarcinogenicity study with up to 0.035% diclofenac in the Solaraze (Diclofenac) vehicle gel was conducted in hairless mice at topical doses up to 2.8 mg/ kg/day. Median tumor onset was earlier in the 0.035% group (Solaraze (Diclofenac) contains 3% diclofenac sodium).
Diclofenac was not genotoxic in point mutation assays in mammalian mouse lymphoma cells and Ames microbial test systems, or when tested in mammalian assays including dominant lethal and male germinal epithelial chromosomal studies in mice, and nucleus anomaly and chromosomal aberration studies in Chinese hamsters. It was also negative in the transformation assay utilizing BALB/3T3 mouse embryo cells.
Fertility studies have not been conducted with Solaraze (Diclofenac) Gel. Diclofenac sodium showed no evidence of impairment of fertility after oral treatment with 4 mg/kg/day (7 times the estimated systemic human exposure) in male or female rats.
* Based on body surface area and assuming 10% bioavailability following topical application of 2 g Solaraze (Diclofenac) Gel per day (1 mg/kg diclofenac sodium).
Solaraze (Diclofenac) Adverse Reactions
Of the 423 patients evaluable for safety in adequate and well-controlled trials, 211 were treated with Solaraze (Diclofenac) drug product and 212 were treated with a vehicle gel. Eighty-seven percent (87%) of the Solaraze (Diclofenac) -treated patients (183 patients) and 84% of the vehicle-treated patients (178 patients) experienced one or more adverse events (AEs) during the studies. The majority of these reactions were mild to moderate in severity and resolved upon discontinuation of therapy.
Of the 211 patients treated with Solaraze (Diclofenac) , 172 (82%) experienced AEs involving skin and the application site compared to 160 (75%) vehicle-treated patients. Application site reactions (ASRs) were the most frequent AEs in both Solaraze (Diclofenac) -and vehicle-treated groups. Of note, four reactions, (scaling) were significantly more prevalent in the Solaraze (Diclofenac) group than in the vehicle-treated patients.
Eighteen percent of Solaraze (Diclofenac) -treated patients and 4% of vehicle-treated patients discontinued from the clinical trials due to adverse events (whether considered related to treatment or not). These discontinuations were mainly due to skin irritation or related cutaneous adverse reactions.
Solaraze (Diclofenac) Overdosage
Due to the low systemic absorption of topically-applied Solaraze (Diclofenac) Gel, overdosage is unlikely. There have been no reports of ingestion of Solaraze (Diclofenac) . In the event of oral ingestion, resulting in significant systemic side effects, it is recommended that the stomach be emptied by vomiting or lavage. Forced diuresis may theoretically be beneficial because the drug is excreted in the urine. The effect of dialysis or hemoperfusion in the elimination of diclofenac (99% protein-bound) remains unproven. In addition to supportive measures, the use of oral activated charcoal may help to reduce the absorption of diclofenac. Supportive and symptomatic treatment should be given for complications such as renal failure, convulsions, gastrointestinal irritation and respiratory depression.
Solaraze (Diclofenac) Dosage And Administration
Solaraze (Diclofenac) Gel is applied to lesion areas twice daily. It is to be smoothed onto the affected skin gently. The amount needed depends upon the size of the lesion site. Assure that enough Solaraze (Diclofenac) Gel is applied to adequately cover each lesion. Normally 0.5 g of gel is used on each 5 cm x 5 cm lesion site. The recommended duration of therapy is from 60 days to 90 days. Complete healing of the lesion(s) or optimal therapeutic effect may not be evident for up to 30 days following cessation of therapy. Lesions that do not respond to therapy should be carefully re-evaluated and management reconsidered.
Solaraze (Diclofenac) How Supplied
Available in tubes of 100 g (NDC 10337-803-01). Each gram of gel contains 30 mg of diclofenac sodium.
Solaraze (Diclofenac) Package Label – Principal Display Panel – G Container
NDC 10337-803-01
Net Wt. 100 g
Rx Only
Solaraze (Diclofenac) GEL
diclofenac sodium-3%
Solaraze (Diclofenac) Package Label – Principal Display Panel – G Carton
NDC 10337-803-01
Rx only
Solaraze (Diclofenac) GEL
diclofenac sodium-3%
Net Wt. 100 g
PharmaDerm
