Attention, chocolate lovers: You may not be able to help yourselves. Swiss and British scientists have linked the widespread love of chocolate to a chemical "signature" that may be programmed into our metabolic systems.
Read more health news
CUTIVATE®
(fluticasone propionate cream)
Cream, 0.05%
Rx only
For Dermatologic Use Only—Not for Ophthalmic Use.
DESCRIPTION
CUTIVATE® (fluticasone propionate cream) Cream, 0.05% contains fluticasone propionate [(6α,11β,16α,17α)-6,9,-difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid, S-fluoromethyl ester], a synthetic fluorinated corticosteroid, for topical dermatologic use. The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents.
Chemically, fluticasone propionate is C25H31F3O5S. It has the following structural formula:
Fluticasone propionate has a molecular weight of 500.6. It is a white to off-white powder and is insoluble in water.
Each gram of CUTIVATE® Cream contains fluticasone propionate 0.5 mg in a base of propylene glycol, mineral oil, cetostearyl alcohol, Ceteth-20, isopropyl myristate, dibasic sodium phosphate, citric acid, purified water, and imidurea as preservative.
CLINICAL PHARMACOLOGY
Like other topical corticosteroids, fluticasone propionate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Fluticasone propionate is lipophilic and has a strong affinity for the glucocorticoid receptor. It has weak affinity for the progesterone receptor, and virtually no affinity for the mineralocorticoid, estrogen, or androgen receptors. The therapeutic potency of glucocorticoids is related to the half-life of the glucocorticoid-receptor complex. The half-life of the fluticasone propionate-glucocorticoid receptor complex is approximately 10 hours.
Studies performed with CUTIVATE® Cream indicate that it is in the medium range of potency as compared with other topical corticosteroids.
INDICATIONS AND USAGE
CUTIVATE® Cream is a medium potency corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. CUTIVATE® Cream may be used with caution in pediatric patients 3 months of age or older. The safety and efficacy of drug use for longer than 4 weeks in this population have not been established. The safety and efficacy of CUTIVATE® Cream in pediatric patients below 3 months of age have not been established.
CONTRAINDICATIONS
CUTIVATE® Cream is contraindicated in those patients with a history of hypersensitivity to any of the components in the preparation.
PRECAUTIONS
ADVERSE REACTIONS
In controlled clinical trials of twice-daily administration, the total incidence of adverse reactions associated with the use of CUTIVATE® Cream was approximately 4%. These adverse reactions were usually mild; self-limiting; and consisted primarily of pruritus, dryness, numbness of fingers, and burning. These events occurred in 2.9%, 1.2%, 1.0%, and 0.6% of patients, respectively.
Two clinical studies compared once- to twice-daily administration of CUTIVATE® Cream for the treatment of moderate to severe eczema. The local drug-related adverse events for the 491 patients enrolled in both studies are shown in Table 1. In the study enrolling both adult and pediatric patients, the incidence of local adverse events in the 119 pediatric patients ages 1 to 12 years was comparable to the 140 patients ages 13 to 62 years.
Fifty-one pediatric patients ages 3 months to 5 years, with moderate to severe eczema, were enrolled in an open-label HPA axis safety study. CUTIVATE® Cream was applied twice daily for 3 to 4 weeks over an arithmetic mean body surface area of 64% (range, 35% to 95%). The mean morning cortisol levels with standard deviations before treatment (prestimulation mean value = 13.76 ± 6.94 mcg/dL, poststimulation mean value = 30.53 ± 7.23 mcg/dL) and at end treatment (prestimulation mean value = 12.32 ± 6.92 mcg/dL, poststimulation mean value = 28.84 ± 7.16 mcg/dL) showed little change. In 2 of 43 (4.7%) patients with end-treatment results, peak cortisol levels following cosyntropin stimulation testing were ≤18 μg/dL, indicating adrenal suppression. Follow-up testing after treatment discontinuation, available for 1 of the 2 subjects, demonstrated a normally responsive HPA axis. Local drug-related adverse events were transient burning, resolving the same day it was reported; transient urticaria, resolving the same day it was reported; erythematous rash; dusky erythema, resolving within 1 month after cessation of CUTIVATE® Cream; and telangiectasia, resolving within 3 months after stopping CUTIVATE® Cream.
| Adverse Events | Fluticasone Once Daily (n = 210) | Fluticasone Twice Daily (n = 203) | Vehicle Twice Daily (n = 78) |
| Skin infection | 1 (0.5%) | 0 | 0 |
| Infected eczema | 1 (0.5%) | 2 (1.0%) | 0 |
| Viral warts | 0 | 1 (0.5%) | 0 |
| Herpes simplex | 0 | 1 (0.5%) | 0 |
| Impetigo | 1 (0.5%) | 0 | 0 |
| Atopic dermatitis | 1 (0.5%) | 0 | 0 |
| Eczema | 1 (0.5%) | 0 | 0 |
| Exacerbation of | 4 (1.9%) | 1 (0.5%) | 1 (1.3%) |
| eczema | |||
| Erythema | 0 | 2 (1.0%) | 0 |
| Burning | 2 (1.0%) | 2 (1.0%) | 2 (2.6%) |
| Stinging | 0 | 2 (1.0%) | 1 (1.3%) |
| Skin irritation | 6 (2.9%) | 2 (1.0%) | 0 |
| Pruritus | 2 (1.0%) | 4 (1.9%) | 4 (5.1%) |
| Exacerbation of | |||
| pruritus | 4 (1.9%) | 1 (0.5%) | 1 (1.3%) |
| Folliculitis | 1 (0.5%) | 1 (0.5%) | 0 |
| Bulers | 0 | 1 (0.5%) | 0 |
| Dryness of skin | 3 (1.4%) | 1 (0.5%) | 0 |
*See div for additional detail. | |
† n = 41. | |
| Adverse Events | Fluticasone Twice Daily |
| Burning | 1 (2.0%) |
| Dusky erythema | 1 (2.0%) |
| Erythematous rash | 1 (2.0%) |
| Facial telangiectasia† | 2 (4.9%) |
| Non-facial telangiectasia | 1 (2.0%) |
| Urticaria | 1 (2.0%) |
The following local adverse reactions have been reported infrequently with topical corticosteroids, and they may occur more frequently with the use of occlusive dressings and higher potency corticosteroids. These reactions are uled in an approximately decreasing order of occurrence: irritation, folliculitis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, skin atrophy, striae, and miliaria. Also, there are reports of the development of pustular psoriasis from chronic plaque psoriasis following reduction or discontinuation of potent topical corticosteroid products.
OVERDOSAGE
Topically applied CUTIVATE® Cream can be absorbed in sufficient amounts to produce systemic effects (see PRECAUTIONS).
DOSAGE AND ADMINISTRATION
CUTIVATE® Cream may be used in adult and pediatric patients 3 months of age or older. Safety and efficacy of CUTIVATE® Cream in pediatric patients for more than 4 weeks of use have not been established (see PRECAUTIONS: Pediatric Use). The safety and efficacy of CUTIVATE® Cream in pediatric patients below 3 months of age have not been established.
CLINICAL STUDIES
HOW SUPPLIED
CUTIVATE® (fluticasone propionate cream) Cream 0.05% is supplied in:
Store between 2° and 30° C (36° and 86° F).
PharmaDerm®
a division ofALTANAInc
Duluth, GA 30096 USA
www.pharmaderm.com