PROTOPIC Tacrolimus 0.1% (1mg / g) Ointment 10g
RXDRUG-DR-XY30071
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Treatment of atopic dermatitis.
Tacrolimus ointment should be used for patients who are not adequately responsive to or are intolerant of conventional therapies.
Tacrolimus ointment should be used for patients who are not adequately responsive to or are intolerant of conventional therapies.
Dosage/Direction for Use
For adults apply 0.03% or 0.1% tacrolimus ointment.
For children aged 2 to 15 years apply only 0.03% tacrolimus ointment.
Treatment: Once or twice a day application to the affected areas.
If signs of a flare reoccur, twice daily treatment should be re-initiated.
Tacrolimus ointment is not recommended for children younger than two years of age.
Long term continuous use of tacrolimus ointment is not recommended.
For children aged 2 to 15 years apply only 0.03% tacrolimus ointment.
Treatment: Once or twice a day application to the affected areas.
If signs of a flare reoccur, twice daily treatment should be re-initiated.
Tacrolimus ointment is not recommended for children younger than two years of age.
Long term continuous use of tacrolimus ointment is not recommended.
Overdosage
No reports of adverse reactions associated with overdose of tacrolimus ointment have been received.
Contraindications
Tacrolimus ointment is contraindicated in patients with hypersensitivity to any component of this product.
Special Precautions
Patients with atopic dermatitis are predisposed to skin infections. In the presence of clinical skin infection, the use of tacrolimus ointment should be evaluated for relative risk and benefit.
Although causal relationship has not been established, rare cases of malignancies including skin malignancies and lymphomas have been reported in patients treated with tacrolimus ointment.
During the course of tacrolimus ointment use, exposure of skin to natural or artificial sunlight should be minimized.
Tacrolimus ointment is intended for dermal application without occlusive dressing. The use of tacrolimus ointment is not recommended in patients having skin conditions with a skin barrier defect in which there is the potential for increased systemic absorption of tacrolimus, for example Netherton's syndrome, lamellar ichthyosis, generalized erythroderma or cutaneous Graft Versus Host Disease. Oral application is also not recommended. Post-marketing cases of increased tacrolimus blood level have been reported in these conditions.
If signs or symptoms of atopic dermatitis do not improve, further treatment options should be considered.
The safety and efficacy of topical tacrolimus ointment has not been established in patients younger than two years of age.
Effects on Ability to Drive and Use Machines: Not applicable.
Although causal relationship has not been established, rare cases of malignancies including skin malignancies and lymphomas have been reported in patients treated with tacrolimus ointment.
During the course of tacrolimus ointment use, exposure of skin to natural or artificial sunlight should be minimized.
Tacrolimus ointment is intended for dermal application without occlusive dressing. The use of tacrolimus ointment is not recommended in patients having skin conditions with a skin barrier defect in which there is the potential for increased systemic absorption of tacrolimus, for example Netherton's syndrome, lamellar ichthyosis, generalized erythroderma or cutaneous Graft Versus Host Disease. Oral application is also not recommended. Post-marketing cases of increased tacrolimus blood level have been reported in these conditions.
If signs or symptoms of atopic dermatitis do not improve, further treatment options should be considered.
The safety and efficacy of topical tacrolimus ointment has not been established in patients younger than two years of age.
Effects on Ability to Drive and Use Machines: Not applicable.
Use In Pregnancy & Lactation
Pregnancy: The use of tacrolimus ointment has not been studied in pregnant women.
Tacrolimus ointment should be used only if the benefits outweigh the risks.
Lactation: Tacrolimus is excreted in human milk after systemic administration. Caution should be exercised when tacrolimus ointment is used by a nursing woman.
Tacrolimus ointment should be used only if the benefits outweigh the risks.
Lactation: Tacrolimus is excreted in human milk after systemic administration. Caution should be exercised when tacrolimus ointment is used by a nursing woman.
Adverse Reactions
See table.
Drug Interactions
Tacrolimus ointment is applied topically to the skin.
Concurrent use of tacrolimus ointment with other dermal preparations, and with UV therapy has not been studied.
Concurrent use of tacrolimus ointment with UVA, UVB, or in combination with psoralen (PUVA) therapy should be avoided.
Concurrent use of tacrolimus ointment with other dermal preparations, and with UV therapy has not been studied.
Concurrent use of tacrolimus ointment with UVA, UVB, or in combination with psoralen (PUVA) therapy should be avoided.
Caution For Usage
Incompatibility: Not applicable.
Instructions for Use and Handling: No special requirements.
Instructions for Use and Handling: No special requirements.
Storage
Store at temperatures not exceeding 25°C.
Action
Pharmacology: Pharmacodynamics: Mechanism of action and pharmacodynamic effects: The exact mechanism of action of topically applied tacrolimus in atopic dermatitis is unknown. Tacrolimus has been shown to inhibit calcineurin and subsequent calcium dependent signaling for transcription and synthesis of cytokines such as interleukins (IL-2, IL-3, IL-4, IL-5, IFN-gamma, TNF-alpha, and GM-CSF) that are involved in early T-cell activation. Clinical significance of these actions in atopic dermatitis is not known.
Results from clinical studies in patients: [Treatment]: Five large, multicenter, randomized, double-blind, parallel group Phase III comparative studies were conducted in patients with atopic dermatitis: 3 adult studies (1 in Europe and 2 in the U.S.) and 2 pediatric studies (1 in Europe and 1 in the U.S.).
European studies: The primary efficacy endpoint for the European reference therapy controlled studies was the mEASI AUC (modified Eczema and Severity Index area under the time-curve) as a percent of baseline and averaged over the treatment period. These studies show that the efficacy of 0.1% tacrolimus ointment is similar to that of the potent topical corticosteroid 0.1% hydrocortisone butyrate ointment and greater than that of 0.03% tacrolimus ointment, and that 0.03% tacrolimus ointment is more effective than 1% hydrocortisone acetate.
U.S. Studies: The 3 U.S. trials were vehicle-controlled, and the primary efficacy endpoint was the rate of treatment success (≥ 90% improvement) at the end of the 12-week treatment period. All 3 U.S. studies showed both 0.03% and 0.1% tacrolimus ointment to be more effective than vehicle (P ≤ 0.001).
Findings from the 2 reference therapy controlled studies and the 3 vehicle controlled studies are consistent and indicate that both 0.03% and 0.1% tacrolimus ointment are effective in the treatment of atopic dermatitis in adult and pediatric patients.
Pharmacokinetics: Absorption: Most atopic dermatitis patients (adults and children) treated with single or repeated application of tacrolimus ointment (0.03 – 0.1%) had blood concentrations less than 2 ng/mL.
Toxicology: Pre-clinical safety data: Mutagenicity: In vitro and in vivo tests did not indicate a genotoxic potential of tacrolimus.
Carcinogenicity: In a 24-month dermal carcinogenicity study of tacrolimus ointment at up to 0.1%, no skin tumors were observed, however, an increased incidence of lymphoma was detected in association with high systemic exposure.
In a 52-week photocarcinogenicity study, the median time to onset of skin tumor formation was decreased in albino hairless mice following chronic topical dosing with tacrolimus ointment at ≥ 0.1 % tacrolimus concurrent exposure to UV radiation (40 weeks of treatment followed by 12 weeks of observation).
Reproduction toxicity: Reproductive toxicology studies were not performed with topical tacrolimus. In the studies of oral tacrolimus, embryo/fetal toxicity was observed in rats and rabbits, but only at doses that caused significant toxicity in maternal animals.
Results from clinical studies in patients: [Treatment]: Five large, multicenter, randomized, double-blind, parallel group Phase III comparative studies were conducted in patients with atopic dermatitis: 3 adult studies (1 in Europe and 2 in the U.S.) and 2 pediatric studies (1 in Europe and 1 in the U.S.).
European studies: The primary efficacy endpoint for the European reference therapy controlled studies was the mEASI AUC (modified Eczema and Severity Index area under the time-curve) as a percent of baseline and averaged over the treatment period. These studies show that the efficacy of 0.1% tacrolimus ointment is similar to that of the potent topical corticosteroid 0.1% hydrocortisone butyrate ointment and greater than that of 0.03% tacrolimus ointment, and that 0.03% tacrolimus ointment is more effective than 1% hydrocortisone acetate.
U.S. Studies: The 3 U.S. trials were vehicle-controlled, and the primary efficacy endpoint was the rate of treatment success (≥ 90% improvement) at the end of the 12-week treatment period. All 3 U.S. studies showed both 0.03% and 0.1% tacrolimus ointment to be more effective than vehicle (P ≤ 0.001).
Findings from the 2 reference therapy controlled studies and the 3 vehicle controlled studies are consistent and indicate that both 0.03% and 0.1% tacrolimus ointment are effective in the treatment of atopic dermatitis in adult and pediatric patients.
Pharmacokinetics: Absorption: Most atopic dermatitis patients (adults and children) treated with single or repeated application of tacrolimus ointment (0.03 – 0.1%) had blood concentrations less than 2 ng/mL.
Toxicology: Pre-clinical safety data: Mutagenicity: In vitro and in vivo tests did not indicate a genotoxic potential of tacrolimus.
Carcinogenicity: In a 24-month dermal carcinogenicity study of tacrolimus ointment at up to 0.1%, no skin tumors were observed, however, an increased incidence of lymphoma was detected in association with high systemic exposure.
In a 52-week photocarcinogenicity study, the median time to onset of skin tumor formation was decreased in albino hairless mice following chronic topical dosing with tacrolimus ointment at ≥ 0.1 % tacrolimus concurrent exposure to UV radiation (40 weeks of treatment followed by 12 weeks of observation).
Reproduction toxicity: Reproductive toxicology studies were not performed with topical tacrolimus. In the studies of oral tacrolimus, embryo/fetal toxicity was observed in rats and rabbits, but only at doses that caused significant toxicity in maternal animals.
MedsGo Class
Other Dermatologicals
Features
Brand
Protopic
Full Details
Dosage Strength
1 mg / g (0.1%)
Drug Ingredients
- Tacrolimus
Drug Packaging
Ointment 10g
Generic Name
Tacrolimus
Dosage Form
Ointment
Registration Number
DR-XY30071
Drug Classification
Prescription Drug (RX)
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