TACROLIMUS ointment

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

TACROLIMUS (UNII: WM0HAQ4WNM) (TACROLIMUS ANHYDROUS - UNII:Y5L2157C4J)

Available from:

Padagis Israel Pharmaceuticals Ltd

INN (International Name):

TACROLIMUS

Composition:

TACROLIMUS ANHYDROUS 0.3 mg in 1 g

Administration route:

TOPICAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Tacrolimus Ointment, both 0.03% and 0.1% for adults, and only 0.03% for children aged 2 to 15 years, is indicated as second-line therapy for the short-term and non-continuous chronic treatment of moderate to severe atopic dermatitis in non-immunocompromised adults and children who have failed to respond adequately to other topical prescription treatments for atopic dermatitis, or when those treatments are not advisable. Tacrolimus Ointment is not indicated for children younger than 2 years of age (see boxed WARNING, WARNINGS and PRECAUTIONS: Pediatric Use). Tacrolimus Ointment is contraindicated in patients with a history of hypersensitivity to tacrolimus or any other component of the ointment.

Product summary:

NDC 45802-390-00 30 gram laminate tube NDC 45802-390-01 60 gram laminate tube NDC 45802-390-02 100 gram laminate tube NDC 45802-700-00 30 gram laminate tube NDC 45802-700-01 60 gram laminate tube NDC 45802-700-02 100 gram laminate tube Store at room temperature 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).

Authorization status:

New Drug Application

Patient Information leaflet

TACROLIMUS- TACROLIMUS OINTMENT
Padagis Israel Pharmaceuticals Ltd
----------
MEDICATION GUIDE
TACROLIMUS
OINTMENT 0.03%
OINTMENT 0.1%
Read the Medication Guide every time you or a family member gets
Tacrolimus Ointment. There may be
new information. This Medication Guide does not take the place of
talking to your doctor about your
medical condition or treatment. If you have questions about Tacrolimus
Ointment, ask your doctor or
pharmacist.
What is the most important information I should know about Tacrolimus
Ointment?
The safety of using Tacrolimus Ointment for a long period of time is
not known. A very small number of
people who have used Tacrolimus Ointment have had cancer (for example,
skin or lymphoma). However,
a link with Tacrolimus Ointment has not been shown. Because of this
concern:
•
Do not use Tacrolimus Ointment continuously for a long time.
•
Use Tacrolimus Ointment only on areas of your skin that have eczema.
•
Do not use Tacrolimus Ointment on a child under 2 years old.
Tacrolimus Ointment comes in two strengths:
•
Only Tacrolimus Ointment 0.03% is for use on children aged 2 to 15
years.
•
Either Tacrolimus Ointment 0.03% or 0.1% can be used by adults and
children 16 years and older.
Talk to your doctor for more information.
What is Tacrolimus Ointment?
Tacrolimus Ointment is a prescription medicine used on the skin
(topical) to treat eczema (atopic
dermatitis). Tacrolimus Ointment is in a class of medicines called
topical calcineurin inhibitors. It is for
adults and children 2 years of age and older who do not have a
weakened immune system. Tacrolimus
Ointment is used on the skin for short periods, and if needed,
treatment may be repeated with breaks in
between.
Tacrolimus Ointment is for use after other prescription medicines have
not worked for you, or if your
doctor recommends that other prescription medicines should not be
used.
Who should not use Tacrolimus Ointment?
Tacrolimus Ointment should not be used:
•
on children younger than 2 years of age.
•
if you are allergic to Tac

Summary of Product characteristics

TACROLIMUS- TACROLIMUS OINTMENT
PADAGIS ISRAEL PHARMACEUTICALS LTD
----------
TACROLIMUS
OINTMENT 0.03%
OINTMENT 0.1%
FOR DERMATOLOGIC USE ONLY
NOT FOR OPHTHALMIC USE
RX ONLY
PRESCRIBING INFORMATION
SEE BOXED WARNING CONCERNING LONG-TERM SAFETY OF TOPICAL CALCINEURIN
INHIBITORS
DESCRIPTION
Tacrolimus Ointment contains tacrolimus, a macrolide immunosuppressant
produced by
_Streptomyces tsukubaensis_. It is for topical dermatologic use only.
Chemically,
tacrolimus is designated as [3_S_-
[3_R_*[_E_(1_S_*,3_S_*,4_S_*)],4_S_*,5_R_*,8_S_*,9_E_,12_R_*,14_R_*,15_S_*,16_R_*,18_S_*,19_S_*,26a_R_*]]-
5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[2-
(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,
12,18-
tetramethyl-8-(2-propenyl)-15,19-epoxy-3H-pyrido[2,1-_c_][1,4]
oxaazacyclotricosine-
1,7,20,21(4H,23H)-tetrone,monohydrate. It has the following structural
formula:
Tacrolimus has an empirical formula of C
H
NO
∙H O and a formula weight of
822.03. Each gram of Tacrolimus Ointment contains (w/w) either 0.03%
or 0.1% of
tacrolimus in a base of mineral oil with all-_rac_-α-tocopherol,
paraffin, propylene
carbonate, white petrolatum with butylhydroxytoluene, and white wax.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
The mechanism of action of tacrolimus in atopic dermatitis is not
known. While the
44
69
12
2
following have been observed, the clinical significance of these
observations 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 (such as interleukin-2, gamma interferon). Tacrolimus also
inhibits the
tr