Tacrotopic Forte Ointment

TACROTOPIC

Each tube of 10 gm contains:
Tacrolimus ointment - 0.03 % w/w

TACROTOPIC FORTE
Each tube of 10 gm contains:
Tacrolimus ointment - 0.1% w/w

Tacrolimus is a macrolide immunosuppressant produced by Streptomyces
tsukubaensis . It is for topical dermatologic use only.

It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by
first binding to an intracellular protein, FKBP-12. A complex of
tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and
the phosphatase activity of calcineurin is inhibited.

This effect has been shown to prevent the dephosphorylation and
translocation of nuclear factor of activated T-cells (NF-AT), a nuclear
component thought to initiate gene transcription for the formation of
lymphokines (such as interleukin-2, gamma interferon).

Tacrolimus also inhibits the transcription of genes, which encode IL3, IL4,
IL5, GM-CSF, and TNF-alpha, all of which are involved in the early stages of
T-cell activation. Additionally, tacrolimus has been shown to inhibit the
release of pre-formed mediators from skin mast cells and basophils, and to
downregulate the expression of FcRI on Langerhans cells.

Tacrolimus is absorbed after the topical application of 0.1% ointment. Peak
tacrolimus blood concentrations ranged from undetectable to 20 ng/mL after
single or multiple doses of 0.1% ointment.

Tacrolimus ointment, both 0.03% and 0.1% for adults, and only 0.03% for
children aged 2 to 15 years, is indicated for short-term and intermittent long-term therapy in the treatment of patients with moderate to severe atopic
dermatitis in whom the use of alternative, conventional therapies are deemed
inadvisable because of potential risks, or in the treatment of patients who are
not adequately responsive to or are intolerant of alternative, conventional
therapies.

Also indicated in:

Tacrolimus Ointment is contraindicated in anyone with a hypersensitivity to
macrolides, tacrolimus or to any of the excipients.

The use of tacrolimus ointment may cause local symptoms such as skin burning or pruritus. Localized symptoms are most common during the first few days of tacrolimus ointment application and typically improve as the lesions of atopic dermatitis heal.

While using tacrolimus ointment, exposure of the skin to sunlight needs to be minimized and the use of ultraviolet light, therapy with UVA or UVB in combination with psoralens (PUVA) should be avoided.

Tacrolimus ointment should be used with caution in patients with hepatic failure.

Based on its minimal extent of absorption, interactions of tacrolimus ointment with systemically administered drugs are unlikely to occur but cannot be ruled out.

The concomitant administration of known CYP3A4 inhibitors in patients with widespread and/or erythrodermic disease should be done with caution. Some examples of such drugs are erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers and cimetidine

Pregnancy Category C: There are no adequate and well-controlled studies of topically administered tacrolimus in pregnant women.

The experience Tacrotopic Ointment when used by pregnant women is too limited to permit assessment of the safety of its use during pregnancy.

Although systemic absorption of tacrolimus following topical applications of tacrolimus ointment is minimal relative to systemic administration, it is known that tacrolimus is excreted in human milk. Because of the potential for serious adverse reactions in nursing infants from tacrolimus, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Tacrolimus ointment 0.03% may be used in pediatric patients 2 years of age and older. Since the safety and efficacy of tacrolimus ointment have not been established in pediatric patients below 2 years of age, its use in this age group is not recommended.

The adverse event profile for patients > 65 years was consistent with that for other adult patients.

Adverse events reported in decreasing order are: Skin Burning, Pruritus, Flu-like symptoms, Allergic Reaction, Headache, Herpes Simplex , Folliculitis, Rhinitis, Otitis Media, Sinusitis, Diarrhea, Bronchitis, Vomiting

Apply a thin layer of tacrolimus ointment 0.03% or 0.1% to the affected skin areas twice daily and rub in gently and completely. Treatment should be continued for one week after clearing of signs and symptoms. Tacrolimus ointment 0.03% and 0.1% should not be used with occlusive dressings.

Tacrolimus ointment is not for oral use. Oral ingestion of tacrolimus ointment may lead to adverse effects associated with systemic administration of tacrolimus.