Dovonex scalp solution 0.005%

In humans, the natural supply of vitamin D depends mainly on exposure to the ultraviolet rays of the sun for conversion of 7-dehydrocholesterol to vitamin D 3 (cholecalciferol) in the skin. Calcipotriene is a synthetic analog of vitamin D 3 .

Although the precise mechanism of calcipotriene's antipsoriatic action is not fully understood, in vitro evidence suggests that calcipotriene is roughly equipotent to the natural vitamin in its effects on proliferation and differentiation of a variety of cell types. Calcipotriene has also been shown, in animal studies, to be 100-200 times less potent in its effects on calcium utilization than the natural hormone.

Clinical studies with radiolabelled calcipotriene solution indicate that less than 1% of the applied dose of calcipotriene is absorbed through the scalp when the solution (2.0 mL) is applied topically to normal skin or psoriasis plaques (160 cm 2 ) for 12 hours, and that much of the absorbed calcipotriene is converted to inactive metabolites within 24 hours of application.

Vitamin D and its metabolites are transported in the blood, bound to specific plasma proteins. The active form of the vitamin, 1,25-dihydroxy vitamin D 3 (calcitriol), is known to be recycled via the liver and excreted in the bile. Calcipotriene metabolism following systemic uptake is rapid, and occurs via a similar pathway to the natural hormone. The primary metabolites are much less potent than the parent compound.

There is evidence that maternal 1,25-dihydroxy vitamin D 3 (calcitriol) may enter the fetal circulation, but it is not known whether it is excreted in human milk. The systemic disposition of calcipotriene is expected to be similar to that of the naturally occurring vitamin.

Avoid contact with the eyes or mucous membranes. Discontinue use if a sensitivity reaction occurs or if excessive irritation develops on uninvolved skin areas.

Drug product is flammable. Keep away from open flame.

In controlled clinical trials, the most frequent adverse reactions reported to be related to Dovonex Scalp Solution, 0.005%, use were transient burning, stinging and tingling, which occurred in approximately 23% of patients. Rash was reported in about 11% of patients. Dry skin, irritation and worsening of psoriasis was reported in 1-5% of patients. Skin atrophy, hyperpigmentation, hypercalcemia, and folliculitis were not observed in these studies, but cannot be excluded.

Topically applied calcipotriene can be absorbed in sufficient amounts to produce systemic effects. Elevated serum calcium has been observed with excessive use of topical calcipotriene. If elevation in serum calcium should occur, discontinue treatment until normal calcium levels are restored. (See PRECAUTIONS .)

Dovonex (calcipotriene solution) Scalp Solution, 0.005%, is available in 60 mL plastic bottles (NDC 0072-1160-06).

STORAGE:   Store at controlled room temperature 15°C - 25°C (59°F - 77°F). Avoid sunlight. Do not freeze

Manufactured by

Leo Pharmaceutical Products, Ltd.

Ballerup, Denmark

Distributed by

Bristol-Myers Squibb Company

Princeton, NJ 08543 U.S.A.

E6-B001C-04-01                                         J4686A

US Patent No. 4,866,048    Revised November 2000