Taclonex Scalp Information
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Dosage Forms And Strengths
Suspension.
Each gram of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension contains 52.18 mcg of calcipotriene hydrate (equivalent to 50 mcg of calcipotriene) and 0.643 mg of betamethasone dipropionate (equivalent to 0.5 mg of betamethasone).
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Contraindications
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Warnings And Precautions
Systemic absorption of topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression with the potential for clinical glucocorticosteroid insufficiency. This may occur during treatment or upon withdrawal of the topical corticosteroid.
In a study of 32 subjects treated with Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension on the scalp and Taclonex Ointment on the body, adrenal suppression was identified in 5 of 32 subjects (15.6%) after 4 weeks of treatment and in 2 of 11 subjects (18.2%) who continued treatment for 8 weeks. []
Because of the potential for systemic absorption, use of topical corticosteroids may require that patients be periodically evaluated for HPA axis suppression. Factors that predispose a patient using a topical corticosteroid to HPA axis suppression include the use of more potent steroids, use over large surface areas, use over prolonged periods, use under occlusion, use on an altered skin barrier, and use in patients with liver failure.
An ACTH stimulation test may be helpful in evaluating patients for HPA axis suppression. If HPA axis suppression is documented, an attempt should be made to gradually withdraw the drug, to reduce the frequency of application, or to substitute a less potent steroid. Manifestations of adrenal insufficiency may require supplemental systemic corticosteroids. Recovery of HPA axis function is generally prompt and complete upon discontinuation of topical corticosteroids.
Cushing’s syndrome, hyperglycemia, and unmasking of latent diabetes mellitus can also result from systemic absorption of topical corticosteroids.
Use of more than one corticosteroid-containing product at the same time may increase the total systemic corticosteroid exposure.
Pediatric patients may be more susceptible to systemic toxicity from use of topical corticosteroids. []
The safety and efficacy of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension in patients with known or suspected disorders of calcium metabolism have not been evaluated.
The safety and efficacy of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension in patients with erythrodermic, exfoliative or pustular psoriasis have not been evaluated.
The safety and efficacy of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension in patients with severe renal insufficiency or severe hepatic disorders have not been evaluated.
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Adverse Reactions
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Use In Specific Populations
Teratogenic Effects: Pregnancy Category C
Animal reproduction studies have not been conducted with Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension. Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension contains calcipotriene that has been shown to be fetotoxic and betamethasone dipropionate that has been shown to be teratogenic in animals when given systemically. There are no adequate and well-controlled studies in pregnant women. Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension should be used during pregnancy only if the potential benefit to the patient justifies the potential risk to the fetus.
Teratogenicity studies with calcipotriene were performed by the oral route in rats and rabbits. In rabbits, increased maternal and fetal toxicity were noted at a dosage of 12 mcg/kg/day (144 mcg/m/day); a dosage of 36 mcg/kg/day (432 mcg/m/day) resulted in a significant increase in the incidence of incomplete ossification of the pubic bones and forelimb phalanges of fetuses. In a rat study, a dosage of 54 mcg/kg/day (324 mcg/m/day) resulted in a significantly increased incidence of skeletal abnormalities (enlarged fontanelles and extra ribs). The enlarged fontanelles were most likely due to the effect of calcipotriene upon calcium metabolism. The estimated maternal and fetal no-adverse effect levels (NOAEL) in the rat (108 mcg/m/day) and rabbit (48 mcg/m/day) derived from oral studies are lower than the maximum topical dose of calcipotriene in man (460 mcg/m/day).
Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. Betamethasone dipropionate has been shown to be teratogenic in mice and rabbits when given by the subcutaneous route at doses of 156 mcg/kg (468 mcg/m/day) and 2.5 mcg/kg (30 mcg/m/day), respectively. Those dose levels are lower than the maximum topical dose in man (about 5,950 mcg/m/day). The abnormalities observed included umbilical hernia, exencephaly and cleft palate.
Pregnant women were excluded from the clinical studies conducted with Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension.
Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects.
It is not known whether topically administered calcipotriene or corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk.
Because many drugs are excreted in human milk, caution should be exercised when Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension is administered to a nursing woman.
Safety and effectiveness of the use of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension in pediatric patients have not been studied. Because of a higher ratio of skin surface area to body mass, children under the age of 12 years may be at particular risk of systemic adverse effects when they are treated with topical corticosteroids. []
HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension have been reported in children receiving topical corticosteroids. Manifestations of adrenal suppression in children include low plasma cortisol levels and absence of response to ACTH stimulation. Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema.
Of the total number of patients in the controlled clinical studies of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension, 334 were 65 years or older, while 84 were 75 years or older.
No overall differences in safety or effectiveness of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension were observed between these patients and younger patients. All other reported clinical experience has not identified any differences in response between elderly and younger
patients.
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Overdosage
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension can be absorbed in sufficient amounts to produce systemic effects [ ].
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Description
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension contains calcipotriene hydrate and betamethasone dipropionate. It is intended for topical use on the scalp.
Calcipotriene hydrate is a synthetic vitamin D analogue.
Chemically, calcipotriene hydrate is 9,10-Secochola-5,7,10(19),22- tetraene-1,3,24-triol,24-cyclo-propyl-, monohydrate, (1α,3ß,5Z,7E,22E,24S) with the empirical formula CHO,HO, a molecular weight of 430.6, and the following structural formula:
Calcipotriene hydrate is a white to almost white, crystalline compound.
Betamethasone dipropionate is a synthetic corticosteroid.
Betamethasone dipropionate has the chemical name Pregna-1,4- diene-3,20-dione-9-fluoro-11-hydroxy-16-methyl-17,21-bis(1-oxypropoxy)-(11ß,16ß), with the empirical formula CHFO, a molecular weight of 504.6, and the following structural formula:
Betamethasone dipropionate is a white to almost white, crystalline powder.
Each gram of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension contains 52.18 mcg of calcipotriene hydrate (equivalent to 50 mcg of calcipotriene) and 0.643 mg of betamethasone dipropionate (equivalent to 0.5 mg of betamethasone) in a base of hydrogenated castor oil, PPG-15 stearyl ether and mineral oil.
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Clinical Pharmacology
Hypothalamic-Pituitary-Adrenal (HPA) Axis Suppression:
HPA axis suppression was evaluated in adult subjects (N=32) with extensive psoriasis involving at least 30% of the scalp and, in total, 15-30% of the body surface area. Treatment consisted of once daily application of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension on the scalp in combination with Taclonex Ointment on the body for 4 to 8 weeks. Adrenal suppression as indicated by a 30-minute post-stimulation cortisol level ≤ 18 mcg/dL was observed in 5 of 32 subjects (15.6%) after 4 weeks of treatment and in 2 of 11 subjects (18.2%) who continued treatment for 8 weeks.
Effects on Calcium Metabolism
In the study described above, the effects of once daily application of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension on the scalp in combination with Taclonex Ointment on the body for 4 to 8 weeks on calcium metabolism were also examined. Following once daily application of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension on the scalp in combination with Taclonex Ointment on the body, elevated urinary calcium levels outside the normal range were observed in two subjects (one at 4 weeks and one at 8 weeks).
Absorption
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension
The systemic effect of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension in extensive psoriasis was investigated in the study described above. In this study, the serum levels of calcipotriene and betamethasone dipropionate and their major metabolites were measured after 4 and 8 weeks of once daily application of Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension on the scalp in combination with Taclonex Ointment on the body. Calcipotriene and betamethasone dipropionate were below the lower limit of quantification in all serum samples of the 34 subjects evaluated.
However, one major metabolite of calcipotriene (MC1080) was quantifiable in 10 of 34 (29.4%) subjects at week 4 and in five of 12 (41.7%) subjects at week 8. The major metabolite of betamethasone dipropionate, betamethasone 17-propionate (B17P) was also quantifiable in 19 of 34 (55.9%) subjects at week 4 and seven of 12 (58.3%) subjects at week 8. The serum concentrations for MC1080 ranged from 20-75 pg/mL. The clinical significance of this finding is unknown.
Metabolism
Calcipotriene
Calcipotriene metabolism following systemic uptake is rapid and occurs in the liver. The primary metabolites of calcipotriene are less potent than the parent compound.
Calcipotriene is metabolized to MC1046 (the α,ß-unsaturated ketone analog of calcipotriene), which is metabolized further to MC1080 (a saturated ketone analog). MC1080 is the major metabolite in plasma. MC1080 is slowly metabolized to calcitroic acid.
Betamethasone dipropionate
Betamethasone dipropionate is metabolized to betamethasone 17-propionate and betamethasone, including the 6ß-hydroxy derivatives of those compounds by hydrolysis. Betamethasone 17-propionate (B17P) is the primary metabolite.
Taclonex scalp (Calcipotriene,betamethasone dipropionate) How Supplied/storage And Handling
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension is available in bottles of:
15 g (NDC 0430-3240-11)
30 g (NDC 0430-3240-13)
60 g (NDC 0430-3240-15)
2 x 60 g (NDC 0430-3240-17)
Store between 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F).
Do not refrigerate. Keep the bottle in the outer carton when not in use.
The product should be used within three months after it has been opened.
Keep out of reach of children.
Shake before use.
Rx only
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Patient Counseling Information
This information is intended to aid in the safe and effective use of this medication. It is not a disclosure of all possible adverse or intended effects.
Patients using Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension should receive the following information and instructions.
Taclonex scalp (Calcipotriene,betamethasone dipropionate)
Taclonex scalp (Calcipotriene,betamethasone dipropionate)
Taclonex scalp (Calcipotriene,betamethasone dipropionate) Principal Display Panel - Carton Label G
NDC 0430-3240-15
Each gram contains 52.18 mcg of calcipotriene hydrate (equivalent to 50 mcg of calcipotriene) and 0.643 mg of betamethasone dipropionate (equivalent to 0.5 mg of betamethasone) in a base of hydrogenated castor oil, PPG-15 stearyl ether and mineral oil.
Store Taclonex scalp (Calcipotriene,betamethasone dipropionate) Topical Suspension between 20-25°C (68-77°F). Excursions permitted between 15-30°C (59-86°F). Do not refrigerate. Keep the bottle in the outer carton when not in use. Shake before use.
Discard product three months after opening.
Keep out of the reach of children.
Usual dosage: Apply once daily, or as directed by physician. See insert for complete information.
