Rocimus

Rocimus

tacrolimus

Manufacturer:

Mega Lifesciences

Distributor:

Metro Drug
Full Prescribing Info
Contents
Tacrolimus.
Description
Rocimus contains immunosuppressant agent, tacrolimus. It is a macrolide lactone produced by Streptomyces tsukubaensis. Rocimus is a white ointment free from any gritty matter. It is for topical dermatologic use only.
Action
Pharmacology: Mechanism of Action: The mechanism of action of tacrolimus in atopic dermatitis is not known. 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 (eg, interleukin-2, γ-interferon). Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, GM-CSF and TNF-α, 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.
Pharmacokinetics: When applied to intact human skin, in vitro studies have demonstrated that tacrolimus is not readily absorbed. However, on inflamed or damaged skin, it is absorbed in sufficient amounts to be topically active. The drug is metabolized in the liver by cytochrome P-450 3A4 and is eliminated almost completely in the bile.
Clinical data have shown that tacrolimus concentrations in clinical circulation after topical administration are low and when measurable, transient.
Tacrolimus does not accumulate in tissues following repeated topical application.
After systemic administration of tacrolimus, bile represents the principal pathway of elimination with a total body clearance of 2.25 L/hr and a systemic elimination half-life (t½) of approximately 40 hrs. Cytochrome P-450 3A4 isoenzyme is responsible for the metabolism of tacrolimus. In vitro, 8 metabolites have been characterized, so far, 13-O-demethylated metabolite has been shown to dominate in vitro. However, it reveals a limit pharmacological activity of 6.4% compared with tacrolimus. In vitro studies on viable human skin report no evident cutaneous metabolism of tacrolimus.
Formal topical drug interaction studies with tacrolimus have not been conducted.
Tacrolimus is not metabolized in human skin, indicating that there is no potential for percutaneous interactions that could affect the metabolism of tacrolimus.
Indications/Uses
In addition to its beneficial effects in the management of atopic dermatitis, topical tacrolimus has also been reported to be of benefit in other immunologically mediated skin diseases including hand, contact and eyelid dermatitis; erosive lichen planus, steroid-induced rosacea, pyoderma gangrenosum and graft-versus-host disease.
Dosage/Direction for Use
Adult: A thin layer of ointment should be applied to the affected skin areas twice daily and rubbed in gently and completely. Treatment should be continued for 1 wk after clearing of signs and symptoms of atopic dermatitis.
Tacrolimus ointment may be used on any part of the body including face, neck and flexure areas, except on mucous membrane.
The safety of tacrolimus ointment under occlusion which may promote systemic exposure has not been evaluated. Tacrolimus ointment should not be used w/ occlusive dressings.
Children: Apply a thin layer of tacrolimus ointment to the affected area daily and rub in gently and completely. Treatment should be continued for 1 week after clearing of signs and symptoms of atopic dermatitis. The safety of tacrolimus ointment under occlusion which may promote systemic exposure has not been evaluated. Tacrolimus ointment should not be used with occlusive dressings.
Overdosage
Overdosage following topical administration is unlikely.
If ingested, general supportive measures may be appropriate. These may include monitoring of vital signs and observation of clinical studies.
Contraindications
Hypersensitivity to macrolides in general, to tacrolimus or to any other ingredient of Rocimus.
Special Precautions
Exposure of the skin to sunlight should be minimized and the use of ultraviolet (UV) light from a solarium, therapy with UVB or UVA in combination with psoralens (PUVA) should be avoided during use of tacrolimus ointment. Physicians should advise patients on appropriate sun protection methods eg, minimization.
Of the time in the sun, use of sunscreen product and covering of the skin with appropriate clothing. Emollients should not be applied to the same area within 2 hrs of applying tacrolimus ointment. Concomitant use of other topical preparations have not been assessed. There is no experience of concomitant use of systemic steroids or immunosuppressive agents.
Tacrolimus ointment has not been evaluated for its efficacy and safety in the treatment of clinically infected atopic dermatitis. Before commencing treatment with tacrolimus ointment, clinical infections at treatment sites should be cleared. Patients with atopic dermatitis are predisposed to superficial skin infections. Treatment with tacrolimus will be associated with an increased risk of herpes viral infections. In the presence of these infections, the balance of risk and benefits associated with tacrolimus use should be evaluated. Beyond 4 years of treatment, the potential for local immunosuppression (possibly resulting in infections or cutaneous malignancies) is unknown. Care should be taken to avoid contact with eyes and mucous membranes. If accidentally applied to these areas, the ointment should be thoroughly wiped off and/or rinsed off with water. The use of tacrolimus ointment under occlusion has not been studied in patients. Occlusive dressings are not recommended.
As with any topical medicinal product, patients should wash hands after application if the hands are not indicated for treatment.
Tacrolimus is extensively metabolized in the liver and although blood concentration are low following topical therapy, the ointment should be used with caution in patients with generalized erythroderma.
Use in pregnancy & lactation: There no adequate and well-controlled studies of topically administered tacrolimus in pregnant women. The experience with tacrolimus ointment when used by pregnant women is limited.
Tacrolimus is transferred across the placenta. It is secreted also in milk.
Although clinical data have shown that systemic exposure from application of tacrolimus ointment is minimal relative to systemic administration, tacrolimus ointment should be used during pregnancy and in nursing mothers only if the potential benefit to the mother justifies a potential risk to the fetus.
Use in children:
The use of tacrolimus ointment has not been evaluated in children <2 years.
Use in the elderly: Twenty five (25) patients >65 years received tacrolimus ointment in phase III studies. The adverse event profile for these was consistent with that of adult patients.
Use In Pregnancy & Lactation
There no adequate and well-controlled studies of topically administered tacrolimus in pregnant women. The experience with tacrolimus ointment when used by pregnant women is limited.
Tacrolimus is transferred across the placenta. It is secreted also in milk.
Although clinical data have shown that systemic exposure from application of tacrolimus ointment is minimal relative to systemic administration, tacrolimus ointment should be used during pregnancy and in nursing mothers only if the potential benefit to the mother justifies a potential risk to the fetus.
Adverse Reactions
Adverse reactions with suspected relationship to treatment are listed by system organ class as follows. Frequencies are defined as very common (>1/10), common (>1/100, <1/10) and uncommon (>1/1,000, <1/100).
General Disorders and Administration Site Conditions: Very Common: Application site burning and pruritus. Common: Application site warmth, erythema, pain, irritation, paresthesia and rash.
Infections and Infestations: Common: Herpes viral infections [herpes simplex dermatitis (eczema herpeticum), herpes simplex (cold sores), Kaposi's varicelliform eruption].
Skin and Subcutaneous Tissue Disorders: Common: Folliculitis, pruritus. Uncommon: Acne.
Nervous System Disorders: Common: Paresthesias and dysesthesias (hyperesthesia, burning sensation).
Metabolism and Nutrition Disorders: Common: Alcohol intolerance (facial flushing or skin irritation after consumption of an alcoholic beverage).
Drug Interactions
Formal topical drug interaction studies with tacrolimus ointment have not been conducted.
Tacrolimus is not metabolized in human skin, indicating that there is no potential for percutaneous interactions that could affect the metabolism of tacrolimus.
A potential interaction between vaccination and application of tacrolimus ointment has not been investigated because of the potential risk of vaccination failure.
Vaccination should be administered prior to commencement of treatment or during a treatment free interval with a period of 14 days between the last application of tacrolimus and the vaccination. In case of attenuated vaccination, this period should be extended to 28 days or the use of alternative vaccines should be considered.
Storage
Store below 25°C in a dry place. Protect from light and moisture.
Shelf-Life: 24 months.
ATC Classification
D11AH01 - tacrolimus ; Belongs to the class of agents for atopic dermatitis, excluding corticosteroids. Used in the treatment of atopic dermatitis.
Presentation/Packing
Oint 0.03% w/w x 10 g x 1's.
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