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Tazorac
Overview
What is Tazorac?
TAZORAC Gel is a translucent, aqueous gel
and contains the compound tazarotene, a member of the acetylenic class of
retinoids. It is for topical dermatologic use only. The active ingredient is
represented by the following structural formula:
Chemical Name:
Ethyl 6-[2-(4,4-dimethylthiochroman-6-yl) ethynyl] nicotinate
Contains:
Inactives:
What does Tazorac look like?
What are the available doses of Tazorac?
Sorry No records found.
What should I talk to my health care provider before I take Tazorac?
Sorry No records found
How should I use Tazorac?
TAZORAC (tazarotene) Gel 0.05% and 0.1%
are indicated for the topical treatment of patients with stable plaque psoriasis
of up to 20% body surface area involvement.
TAZORAC (tazarotene) Gel 0.1% is also indicated for
the topical treatment of patients with facial acne vulgaris of mild to moderate
severity.
The efficacy of TAZORAC Gel in the treatment of acne
previously treated with other retinoids or resistant to oral antibiotics has not
been established.
Application may cause excessive irritation in the skin of certain
sensitive individuals. In cases where it has been necessary to temporarily
discontinue therapy, or the dosing has been reduced to a lower concentration (in
patients with psoriasis) or to an interval the patient can tolerate, therapy can
be resumed, or the drug concentration or frequency of application can be
increased as the patient becomes able to tolerate the treatment. Frequency of
application should be closely monitored by careful observation of the clinical
therapeutic response and skin tolerance. Efficacy has not been established for
less than once daily dosing frequencies.
For psoriasis:
For acne:
What interacts with Tazorac?
Retinoids may cause fetal harm when administered to a pregnant woman.
In rats, tazarotene 0.05% gel, administered during gestation days 6 through 17 at 0.25 mg/kg/day (1.5 mg/m/day) resulted in reduced fetal body weights and reduced skeletal ossification. Rabbits dosed with 0.25 mg/kg/day (2.75 mg/m total body surface area/day) tazarotene gel during gestation days 6 through 18 were noted with single incidences of known retinoid malformations, including spina bifida, hydrocephaly, and heart anomalies. Systemic daily-exposure (AUC) to tazarotenic acid at topical doses of 0.25 mg/kg/day tazarotene in a gel formulation in rats and rabbits represented 0.62 and 6.7 times, respectively, the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.78 and 8.4 times, respectively, the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
As with other retinoids, when tazarotene was given to experimental animals, developmental delays were seen in rats, and teratogenic effects and post-implantation loss were observed in rats and rabbits at AUC values that were 0.55 and 13.2 times, respectively, the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.68 and 16.4 times, respectively, the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
In a study of the effect of oral tazarotene on fertility and early embryonic development in rats, decreased number of implantation sites, decreased litter size, decreased numbers of live fetuses, and decreased fetal body weights, all classic developmental effects of retinoids, were observed when female rats were administered 2 mg/kg/day from 15 days before mating through gestation day 7. A low incidence of retinoid-related malformations at that dose was reported to be related to treatment. This dose produced an AUC that was 1.7 times the AUC observed in psoriatic patients treated with 2 mg/cm tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area) and 2.1 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
SYSTEMIC EXPOSURE TO TAZAROTENIC ACID IS DEPENDENT UPON THE EXTENT OF THE BODY SURFACE AREA TREATED. IN PATIENTS TREATED TOPICALLY OVER SUFFICIENT BODY SURFACE AREA, EXPOSURE COULD BE IN THE SAME ORDER OF MAGNITUDE AS IN THESE ORALLY TREATED ANIMALS. ALTHOUGH THERE MAY BE LESS SYSTEMIC EXPOSURE IN THE TREATMENT OF ACNE OF THE FACE ALONE DUE TO LESS SURFACE AREA FOR APPLICATION, TAZAROTENE IS A TERATOGENIC SUBSTANCE, AND IT IS NOT KNOWN WHAT LEVEL OF EXPOSURE IS REQUIRED FOR TERATOGENICITY IN HUMANS (SEE ).
There were thirteen reported pregnancies in patients who participated in clinical trials for topical tazarotene. Nine of the patients were found to have been treated with topical tazarotene, and the other four had been treated with vehicle. One of the patients who was treated with tazarotene cream elected to terminate the pregnancy for non-medical reasons unrelated to treatment. The other eight pregnant women who were inadvertently exposed to topical tazarotene during clinical trials subsequently delivered apparently healthy babies. As the exact timing and extent of exposure in relation to the gestation times are not certain, the significance of these findings is unknown.
TAZORAC Gel is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, treatment should be discontinued and the patient apprised of the potential hazard to the fetus. Women of child-bearing potential should be warned of the potential risk and use adequate birth-control measures when TAZORAC Gel is used. The possibility that a woman of childbearing potential is pregnant at the time of institution of therapy should be considered. A negative result for pregnancy test having a sensitivity down to at least 50 mIU/mL for human chorionic gonadotropin (hCG) should be obtained within 2 weeks prior to TAZORAC Gel therapy, which should begin during a normal menstrual period (see also ).
TAZORAC Gel is contraindicated in individuals who have shown hypersensitivity to any of its components.
What are the warnings of Tazorac?
Array
What are the precautions of Tazorac?
TAZORAC Gel should be applied only to the
affected areas. For external use only. Avoid contact with eyes, eyelids, and
mouth. If contact with eyes occurs, rinse thoroughly with water. The safety of
use of TAZORAC Gel over more than 20% of body surface
area has not been established in psoriasis or acne.
Retinoids should not be used on eczematous skin, as they may cause severe
irritation.
Because of heightened burning susceptibility, exposure to sunlight (including
sunlamps) should be avoided unless deemed medically necessary, and in such
cases, exposure should be minimized during the use of TAZORAC Gel. Patients must be warned to use sunscreens (minimum SPF
of 15) and protective clothing when using TAZORAC Gel.
Patients with sunburn should be advised not to use TAZORAC Gel until fully recovered. Patients who may have considerable
sun exposure due to their occupation and those patients with inherent
sensitivity to sunlight should exercise particular caution when using
TAZORAC Gel and ensure that the precautions outlined in
the Information for Patients subsection are observed.
TAZORAC Gel should be administered with caution if
the patient is also taking drugs known to be photosensitizers (e.g., thiazides,
tetracyclines, fluoroquinolones, phenothiazines, sulfonamides) because of the
increased possibility of augmented photosensitivity.
Some individuals may experience excessive pruritus, burning, skin redness or
peeling. If these effects occur, the medication should either be discontinued
until the integrity of the skin is restored, or the dosing should be reduced to
an interval the patient can tolerate. However, efficacy at reduced frequency of
application has not been established. Alternatively, patients with psoriasis who
are being treated with the 0.1% concentration can be switched to the lower
concentration.
Weather extremes, such as wind or cold, may be more irritating to patients
using TAZORAC Gel.
See attached .
Concomitant dermatologic medications and cosmetics that have a
strong drying effect should be avoided. It is also advisable to "rest" a
patient's skin until the effects of such preparations subside before use of
TAZORAC Gel is begun.
A long-term study of tazarotene following oral administration of
0.025, 0.050, and 0.125 mg/kg/day to rats showed no indications of increased
carcinogenic risks. Based on pharmacokinetic data from a shorter-term study in
rats, the highest dose of 0.125 mg/kg/day was anticipated to give systemic
exposure (AUC) in the rat equivalent to 0.32 times the
AUC observed in psoriatic patients treated with 2
mg/cm of tazarotene gel 0.1% (extrapolated for topical
application over 20% body surface area), and 0.38 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface
area.
In evaluation of photo co-carcinogenicity, median time to onset of tumors was
decreased, and the number of tumors increased in hairless mice following chronic
topical dosing with intercurrent exposure to ultraviolet radiation at tazarotene
concentrations of 0.001%, 0.005%, and 0.01% in a gel formulation for up to 40
weeks.
A long-term topical application study of up to 0.1% tazarotene in a gel
formulation in mice terminated at 88 weeks showed that dose levels of 0.05,
0.125, 0.25, and 1.0 mg/kg/day (reduced to 0.5 mg/kg/day for males after 41
weeks due to severe dermal irritation) revealed no apparent carcinogenic effects
when compared to vehicle control animals; untreated control animals were not
completely evaluated. Systemic exposure (AUC) at the
highest dose was 2.0 times the AUC observed in
psoriatic patients treated with 2 mg/cm of tazarotene
gel 0.1% (extrapolated for topical application over 20% body surface area), and
2.5 times the maximum AUC in acne patients treated
with 2 mg/cm of tazarotene gel 0.1% over 15 %
(targeted) body surface area.
Tazarotene was found to be non-mutagenic in the Ames assay using Salmonella
and and did not produce structural
chromosomal aberrations in a human lymphocyte assay. Tazarotene was also
non-mutagenic in the CHO/HGPRT mammalian cell forward gene mutation assay and
was non-clastogenic in the mouse micronucleus
test.
No impairment of fertility occurred in rats when male animals were treated
for 70 days prior to mating and female animals were treated for 14 days prior to
mating and continuing through gestation and lactation with topical doses of
tazarotene gel up to 0.125 mg/kg/day. Based on data from another study, the
systemic drug exposure (AUC) in the rat would be
equivalent to 0.31 times the AUC observed in
psoriatic patients treated with 2 mg/cm of tazarotene
gel 0.1% (extrapolated for topical application over 20% body surface area), and
0.38 times the maximum AUC in acne patients treated
with 2 mg/cm of tazarotene gel 0.1% over 15 % (targeted)
body surface area.
No impairment of mating performance or fertility was observed in male rats
treated for 70 days prior to mating with oral doses of up to 1.0 mg/kg/day
tazarotene, which produced an AUC that was 0.95 times
the AUC observed in psoriatic patients treated with
2 mg/cm of tazarotene gel 0.1% (extrapolated for topical
application over 20% body surface area), and 1.2 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15 % (targeted) body surface
area.
No effect on parameters of mating performance or fertility was observed in
female rats treated for 15 days prior to mating and continuing through day 7 of
gestation with oral doses of tazarotene up to 2.0 mg/kg/day. However, there was
a significant decrease in the number of estrous stages and an increase in
developmental effects at 2.0 mg/kg/day (see ). This dose produced an AUC which was 1.7 times that observed in psoriatic patients
treated with 2 mg/cm of tazarotene gel 0.1%
(extrapolated for topical application over 20% body surface area), and 2.1 times
the maximum AUC in acne patients treated with 2
mg/cm of tazarotene gel 0.1% over 15% (targeted) body
surface area.
Reproductive capabilities of F1 animals, including F2 survival and
development, were not affected by topical administration of tazarotene gel to
female F0 parental rats from gestation day 16 through lactation day 20 at the
maximum tolerated dose of 0.125 mg/kg/day. Based on data from another study, the
systemic drug exposure (AUC) in the rat would be
equivalent to 0.31 times the AUC observed in
psoriatic patients treated with 2 mg/cm of tazarotene
gel 0.1% (extrapolated for topical application over 20% body surface area), and
0.38 times the maximum AUC in acne patients treated
with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted)
body surface area.
Teratogenic Effects: Pregnancy Category
X:
After single topical doses of C-tazarotene to the skin of lactating rats, radioactivity was
detected in milk, suggesting that there would be transfer of drug-related
material to the offspring via milk. It is not known whether this drug is
excreted in human milk. Caution should be exercised when tazarotene is
administered to a nursing woman.
The safety and efficacy of tazarotene have not been established
in pediatric patients under the age of 12 years.
Of the total number of subjects in clinical studies of tazarotene
gels, 0.05% and 0.1% for plaque psoriasis, 163 were over the age of 65. Subjects
over 65 years of age experienced more adverse events and lower treatment success
rates after 12 weeks of use of TAZORAC Gel compared with
those 65 years of age and younger. Currently there is no other reliable clinical
experience on the differences in responses between the elderly and younger
patients, but greater sensitivity of some older individuals can not be ruled
out. Tazarotene gel for the treatment of acne has not been clinically evaluated
in persons over the age of 65.
What are the side effects of Tazorac?
In human dermal safety studies, tazarotene 0.05% and 0.1% gels
did not induce allergic contact sensitization, phototoxicity or
photoallergy.
The most frequent adverse events reported with TAZORAC Gel 0.05% and 0.1% were limited to the skin. Those occurring
in 10 to 30% of patients, in descending order, included pruritus,
burning/stinging, erythema, worsening of psoriasis, irritation, and skin pain.
Events occurring in 1 to 10% of patients included rash, desquamation, irritant
contact dermatitis, skin inflammation, fissuring, bleeding and dry skin.
Increases in “psoriasis worsening” and “sun-induced erythema” were noted in some
patients over the 4th to 12th months as compared to the first three months of a
1 year study. In general, the incidence of adverse events with TAZORAC Gel 0.05% was 2 to 5% lower than that seen with TAZORAC Gel 0.1%.
The most frequent adverse events reported with TAZORAC Gel 0.1% in the treatment of acne occurring in 10 to 30% of
patients, in descending order, included desquamation, burning/stinging, dry
skin, erythema and pruritus. Events occurring in 1 to 10% of patients included
irritation, skin pain, fissuring, localized edema and skin discoloration.
What should I look out for while using Tazorac?
Retinoids may cause fetal harm when administered to a pregnant
woman.
In rats, tazarotene 0.05% gel, administered
during gestation days 6 through 17 at 0.25 mg/kg/day (1.5 mg/m/day) resulted in reduced fetal body weights and reduced
skeletal ossification. Rabbits dosed with
0.25 mg/kg/day (2.75 mg/m total body surface area/day)
tazarotene gel during gestation days 6 through 18 were noted with single
incidences of known retinoid malformations, including spina bifida,
hydrocephaly, and heart anomalies. Systemic daily-exposure (AUC) to tazarotenic acid at topical doses of 0.25 mg/kg/day
tazarotene in a gel formulation in rats and rabbits represented 0.62 and 6.7
times, respectively, the AUC observed in psoriatic
patients treated with 2 mg/cm of tazarotene gel 0.1%
(extrapolated for topical application over 20% body surface area), and 0.78 and
8.4 times, respectively, the maximum AUC in acne
patients treated with 2 mg/cm of tazarotene gel 0.1%
over 15% (targeted) body surface area.
As with other retinoids, when tazarotene was given to experimental animals, developmental delays were seen
in rats, and teratogenic effects and post-implantation loss were observed in
rats and rabbits at AUC values that were 0.55 and 13.2
times, respectively, the AUC observed in psoriatic
patients treated with 2 mg/cm of tazarotene gel 0.1%
(extrapolated for topical application over 20% body surface area), and 0.68 and
16.4 times, respectively, the maximum AUC in acne
patients treated with 2 mg/cm of tazarotene gel 0.1%
over 15% (targeted) body surface area.
In a study of the effect of oral tazarotene on fertility and early embryonic
development in rats, decreased number of implantation sites, decreased litter
size, decreased numbers of live fetuses, and decreased fetal body weights, all
classic developmental effects of retinoids, were observed when female rats were
administered 2 mg/kg/day from 15 days before mating through gestation day 7. A
low incidence of retinoid-related malformations at that dose was reported to be
related to treatment. This dose produced an AUC that
was 1.7 times the AUC observed in psoriatic patients
treated with 2 mg/cm tazarotene gel 0.1% (extrapolated
for topical application over 20% body surface area) and 2.1 times the maximum
AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface
area.
SYSTEMIC EXPOSURE TO TAZAROTENIC ACID IS DEPENDENT UPON THE EXTENT OF THE
BODY SURFACE AREA TREATED. IN PATIENTS TREATED TOPICALLY OVER SUFFICIENT BODY
SURFACE AREA, EXPOSURE COULD BE IN THE SAME ORDER OF MAGNITUDE AS IN THESE
ORALLY TREATED ANIMALS. ALTHOUGH THERE MAY BE LESS SYSTEMIC EXPOSURE IN THE
TREATMENT OF ACNE OF THE FACE ALONE DUE TO LESS SURFACE AREA FOR APPLICATION,
TAZAROTENE IS A TERATOGENIC SUBSTANCE, AND IT IS NOT KNOWN WHAT LEVEL OF
EXPOSURE IS REQUIRED FOR TERATOGENICITY IN HUMANS (SEE ).
There were thirteen reported pregnancies in patients who participated in
clinical trials for topical tazarotene. Nine of the patients were found to have
been treated with topical tazarotene, and the other four had been treated with
vehicle. One of the patients who was treated with tazarotene cream elected to
terminate the pregnancy for non-medical reasons unrelated to treatment. The
other eight pregnant women who were inadvertently exposed to topical tazarotene
during clinical trials subsequently delivered apparently healthy babies. As the
exact timing and extent of exposure in relation to the gestation times are not
certain, the significance of these findings is unknown.
TAZORAC Gel is contraindicated in women who are or
may become pregnant. If this drug is used during pregnancy, or if the patient
becomes pregnant while taking this drug, treatment should be discontinued and
the patient apprised of the potential hazard to the fetus. Women of
child-bearing potential should be warned of the potential risk and use adequate
birth-control measures when TAZORAC Gel is used. The
possibility that a woman of childbearing potential is pregnant at the time of
institution of therapy should be considered. A negative result for pregnancy
test having a sensitivity down to at least 50 mIU/mL for human chorionic
gonadotropin (hCG) should be obtained within 2 weeks prior to TAZORAC Gel therapy, which should begin during a normal menstrual
period (see also ).
TAZORAC Gel is contraindicated in individuals who
have shown hypersensitivity to any of its components.
Pregnancy Category X
CONTRAINDICATIONS
®
®
What might happen if I take too much Tazorac?
Excessive topical use of TAZORAC Gel may
lead to marked redness, peeling, or discomfort (see ).
TAZORAC Gels 0.05% and 0.1% are not for oral use.
Oral ingestion of the drug may lead to the same adverse effects as those
associated with excessive oral intake of Vitamin A (hypervitaminosis A) or other
retinoids. If oral ingestion occurs, the patient should be monitored, and
appropriate supportive measures should be administered as necessary.
How should I store and handle Tazorac?
Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.PHARMACIST:Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.PHARMACIST:Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.PHARMACIST:Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Protect from light.Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.PHARMACIST:TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -TAZORAC (tazarotene) Gel is available in concentration of 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 gm and 100 gm sizes.NOTE:RX ONLY® Marks owned by Allergan, Inc.U.S. Patent Numbers 5,089,509; 5,914,334 and 6,258,830 Irvine, California 92612, USA©2004 Allergan, Inc.Printed in USA8606X, 8607XAJanuary 200471722US10PRelabeling of "Additional Barcode Label" by:Pharmacist: Please cut or tear at dotted line and provide this patient package insert to your customer- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Tazarotene is a retinoid prodrug which is converted to its active
form, the cognate carboxylic acid of tazarotene (AGN 190299), by rapid
deesterification in animals and man. AGN 190299 (“tazarotenic acid”) binds to
all three members of the retinoic acid receptor (RAR) family: RARα, RARβ, and
RARγ but shows relative selectivity for RARβ, and RARγ and may modify gene
expression. The clinical significance of these findings is unknown.
Psoriasis:
in
vitro
Acne
Following topical application, tazarotene undergoes esterase
hydrolysis to form its active metabolite, tazarotenic acid. Little parent
compound could be detected in the plasma. Tazarotenic acid was highly bound to
plasma proteins (>99%). Tazarotene and tazarotenic acid were metabolized to
sulfoxides, sulfones and other polar metabolites which were eliminated through
urinary and fecal pathways. The half-life of tazarotenic acid was approximately
18 hours, following topical application of tazarotene to normal, acne or
psoriatic skin.
The human studies described below were
conducted with tazarotene gel applied topically at approximately 2 mg/cm and left on the skin for 10 to 12 hours. Both the peak plasma
concentration (Cmax) and area under the plasma concentration time curve (AUC)
refer to the active metabolite only.
Two single, topical dose studies were conducted using C-tazarotene gel. Systemic absorption, as determined from
radioactivity in the excreta, was less than 1% of the applied dose (without
occlusion) in six psoriatic patients and approximately 5% of the applied dose
(under occlusion) in six healthy subjects. One non-radiolabeled single-dose
study comparing the 0.05% gel to the 0.1% gel in healthy subjects indicated that
the Cmax and AUC were 40% higher for the 0.1% gel.
After 7 days of topical dosing with measured doses of tazarotene 0.1% gel on
20% of the total body surface without occlusion in 24 healthy subjects, the Cmax
for tazarotenic acid was 0.72 ± 0.58 ng/mL (mean ± SD) occurring 9 hours after
the last dose, and the AUC for tazarotenic acid was
10.1 ± 7.2 ng·hr/mL. Systemic absorption was 0.91 ± 0.67% of the applied
dose.
In a 14-day study in five psoriatic patients, measured doses of tazarotene
0.1% gel were applied daily by nursing staff to involved skin without occlusion
(8 to 18% of total body surface area; mean ± SD: 13 ± 5%). The Cmax for
tazarotenic acid was 12.0 ± 7.6 ng/mL occurring 6 hours after the final dose,
and the AUC for tazarotenic acid was
105 ± 55 ng·hr/mL. Systemic absorption was 14.8 ± 7.6% of the applied dose.
Extrapolation of these results to represent dosing on 20% of total body surface
yielded estimates for tazarotenic acid with Cmax of 18.9 ± 10.6 ng/mL and
AUC of 172 ± 88 ng·hr/mL.
An percutaneous absorption study, using
radiolabeled drug and freshly excised human skin or human cadaver skin,
indicated that approximately 4 to 5% of the applied dose was in the stratum
corneum (tazarotene: tazarotenic acid= 5:1) and 2 to 4% was in the viable
epidermis-dermis layer (tazarotene: tazarotenic acid= 2:1) 24 hours after
topical application of the gel.
Non-Clinical Toxicology
Retinoids may cause fetal harm when administered to a pregnant woman.In rats, tazarotene 0.05% gel, administered during gestation days 6 through 17 at 0.25 mg/kg/day (1.5 mg/m/day) resulted in reduced fetal body weights and reduced skeletal ossification. Rabbits dosed with 0.25 mg/kg/day (2.75 mg/m total body surface area/day) tazarotene gel during gestation days 6 through 18 were noted with single incidences of known retinoid malformations, including spina bifida, hydrocephaly, and heart anomalies. Systemic daily-exposure (AUC) to tazarotenic acid at topical doses of 0.25 mg/kg/day tazarotene in a gel formulation in rats and rabbits represented 0.62 and 6.7 times, respectively, the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.78 and 8.4 times, respectively, the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
As with other retinoids, when tazarotene was given to experimental animals, developmental delays were seen in rats, and teratogenic effects and post-implantation loss were observed in rats and rabbits at AUC values that were 0.55 and 13.2 times, respectively, the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.68 and 16.4 times, respectively, the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
In a study of the effect of oral tazarotene on fertility and early embryonic development in rats, decreased number of implantation sites, decreased litter size, decreased numbers of live fetuses, and decreased fetal body weights, all classic developmental effects of retinoids, were observed when female rats were administered 2 mg/kg/day from 15 days before mating through gestation day 7. A low incidence of retinoid-related malformations at that dose was reported to be related to treatment. This dose produced an AUC that was 1.7 times the AUC observed in psoriatic patients treated with 2 mg/cm tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area) and 2.1 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
SYSTEMIC EXPOSURE TO TAZAROTENIC ACID IS DEPENDENT UPON THE EXTENT OF THE BODY SURFACE AREA TREATED. IN PATIENTS TREATED TOPICALLY OVER SUFFICIENT BODY SURFACE AREA, EXPOSURE COULD BE IN THE SAME ORDER OF MAGNITUDE AS IN THESE ORALLY TREATED ANIMALS. ALTHOUGH THERE MAY BE LESS SYSTEMIC EXPOSURE IN THE TREATMENT OF ACNE OF THE FACE ALONE DUE TO LESS SURFACE AREA FOR APPLICATION, TAZAROTENE IS A TERATOGENIC SUBSTANCE, AND IT IS NOT KNOWN WHAT LEVEL OF EXPOSURE IS REQUIRED FOR TERATOGENICITY IN HUMANS (SEE ).
There were thirteen reported pregnancies in patients who participated in clinical trials for topical tazarotene. Nine of the patients were found to have been treated with topical tazarotene, and the other four had been treated with vehicle. One of the patients who was treated with tazarotene cream elected to terminate the pregnancy for non-medical reasons unrelated to treatment. The other eight pregnant women who were inadvertently exposed to topical tazarotene during clinical trials subsequently delivered apparently healthy babies. As the exact timing and extent of exposure in relation to the gestation times are not certain, the significance of these findings is unknown.
TAZORAC Gel is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, treatment should be discontinued and the patient apprised of the potential hazard to the fetus. Women of child-bearing potential should be warned of the potential risk and use adequate birth-control measures when TAZORAC Gel is used. The possibility that a woman of childbearing potential is pregnant at the time of institution of therapy should be considered. A negative result for pregnancy test having a sensitivity down to at least 50 mIU/mL for human chorionic gonadotropin (hCG) should be obtained within 2 weeks prior to TAZORAC Gel therapy, which should begin during a normal menstrual period (see also ).
TAZORAC Gel is contraindicated in individuals who have shown hypersensitivity to any of its components.
Pregnancy Category X
CONTRAINDICATIONS
®
®
The hypoglycemic action of sulfonylureas may be potentiated by certain drugs including nonsteroidal anti-inflammatory agents and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, and beta-adrenergic blocking agents. When such drugs are administered to a patient receiving glipizide, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving glipizide, the patient should be observed closely for loss of control. binding studies with human serum proteins indicate that glipizide binds differently than tolbutamide and does not interact with salicylate or dicumarol. However, caution must be exercised in extrapolating these findings to the clinical situation and in the use of glipizide with these drugs.
Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving glipizide, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving glipizide, the patient should be observed closely for hypoglycemia.
A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical, or vaginal preparations of miconazole is not known. The effect of concomitant administration of Diflucan® (fluconazole) and Glucotrol has been demonstrated in a placebo-controlled crossover study in normal volunteers. All subjects received Glucotrol alone and following treatment with 100 mg of Diflucan® as a single daily oral dose for 7 days. The mean percentage increase in the Glucotrol AUC after fluconazole administration was 56.9% (range: 35 to 81%).
TAZORAC Gel should be applied only to the affected areas. For external use only. Avoid contact with eyes, eyelids, and mouth. If contact with eyes occurs, rinse thoroughly with water. The safety of use of TAZORAC Gel over more than 20% of body surface area has not been established in psoriasis or acne.
Retinoids should not be used on eczematous skin, as they may cause severe irritation.
Because of heightened burning susceptibility, exposure to sunlight (including sunlamps) should be avoided unless deemed medically necessary, and in such cases, exposure should be minimized during the use of TAZORAC Gel. Patients must be warned to use sunscreens (minimum SPF of 15) and protective clothing when using TAZORAC Gel. Patients with sunburn should be advised not to use TAZORAC Gel until fully recovered. Patients who may have considerable sun exposure due to their occupation and those patients with inherent sensitivity to sunlight should exercise particular caution when using TAZORAC Gel and ensure that the precautions outlined in the Information for Patients subsection are observed.
TAZORAC Gel should be administered with caution if the patient is also taking drugs known to be photosensitizers (e.g., thiazides, tetracyclines, fluoroquinolones, phenothiazines, sulfonamides) because of the increased possibility of augmented photosensitivity.
Some individuals may experience excessive pruritus, burning, skin redness or peeling. If these effects occur, the medication should either be discontinued until the integrity of the skin is restored, or the dosing should be reduced to an interval the patient can tolerate. However, efficacy at reduced frequency of application has not been established. Alternatively, patients with psoriasis who are being treated with the 0.1% concentration can be switched to the lower concentration.
Weather extremes, such as wind or cold, may be more irritating to patients using TAZORAC Gel.
See attached .
Concomitant dermatologic medications and cosmetics that have a strong drying effect should be avoided. It is also advisable to "rest" a patient's skin until the effects of such preparations subside before use of TAZORAC Gel is begun.
A long-term study of tazarotene following oral administration of 0.025, 0.050, and 0.125 mg/kg/day to rats showed no indications of increased carcinogenic risks. Based on pharmacokinetic data from a shorter-term study in rats, the highest dose of 0.125 mg/kg/day was anticipated to give systemic exposure (AUC) in the rat equivalent to 0.32 times the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.38 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
In evaluation of photo co-carcinogenicity, median time to onset of tumors was decreased, and the number of tumors increased in hairless mice following chronic topical dosing with intercurrent exposure to ultraviolet radiation at tazarotene concentrations of 0.001%, 0.005%, and 0.01% in a gel formulation for up to 40 weeks.
A long-term topical application study of up to 0.1% tazarotene in a gel formulation in mice terminated at 88 weeks showed that dose levels of 0.05, 0.125, 0.25, and 1.0 mg/kg/day (reduced to 0.5 mg/kg/day for males after 41 weeks due to severe dermal irritation) revealed no apparent carcinogenic effects when compared to vehicle control animals; untreated control animals were not completely evaluated. Systemic exposure (AUC) at the highest dose was 2.0 times the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 2.5 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15 % (targeted) body surface area.
Tazarotene was found to be non-mutagenic in the Ames assay using Salmonella and and did not produce structural chromosomal aberrations in a human lymphocyte assay. Tazarotene was also non-mutagenic in the CHO/HGPRT mammalian cell forward gene mutation assay and was non-clastogenic in the mouse micronucleus test.
No impairment of fertility occurred in rats when male animals were treated for 70 days prior to mating and female animals were treated for 14 days prior to mating and continuing through gestation and lactation with topical doses of tazarotene gel up to 0.125 mg/kg/day. Based on data from another study, the systemic drug exposure (AUC) in the rat would be equivalent to 0.31 times the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.38 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15 % (targeted) body surface area.
No impairment of mating performance or fertility was observed in male rats treated for 70 days prior to mating with oral doses of up to 1.0 mg/kg/day tazarotene, which produced an AUC that was 0.95 times the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 1.2 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15 % (targeted) body surface area.
No effect on parameters of mating performance or fertility was observed in female rats treated for 15 days prior to mating and continuing through day 7 of gestation with oral doses of tazarotene up to 2.0 mg/kg/day. However, there was a significant decrease in the number of estrous stages and an increase in developmental effects at 2.0 mg/kg/day (see ). This dose produced an AUC which was 1.7 times that observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 2.1 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
Reproductive capabilities of F1 animals, including F2 survival and development, were not affected by topical administration of tazarotene gel to female F0 parental rats from gestation day 16 through lactation day 20 at the maximum tolerated dose of 0.125 mg/kg/day. Based on data from another study, the systemic drug exposure (AUC) in the rat would be equivalent to 0.31 times the AUC observed in psoriatic patients treated with 2 mg/cm of tazarotene gel 0.1% (extrapolated for topical application over 20% body surface area), and 0.38 times the maximum AUC in acne patients treated with 2 mg/cm of tazarotene gel 0.1% over 15% (targeted) body surface area.
Teratogenic Effects: Pregnancy Category X:
After single topical doses of C-tazarotene to the skin of lactating rats, radioactivity was detected in milk, suggesting that there would be transfer of drug-related material to the offspring via milk. It is not known whether this drug is excreted in human milk. Caution should be exercised when tazarotene is administered to a nursing woman.
The safety and efficacy of tazarotene have not been established in pediatric patients under the age of 12 years.
Of the total number of subjects in clinical studies of tazarotene gels, 0.05% and 0.1% for plaque psoriasis, 163 were over the age of 65. Subjects over 65 years of age experienced more adverse events and lower treatment success rates after 12 weeks of use of TAZORAC Gel compared with those 65 years of age and younger. Currently there is no other reliable clinical experience on the differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals can not be ruled out. Tazarotene gel for the treatment of acne has not been clinically evaluated in persons over the age of 65.
In human dermal safety studies, tazarotene 0.05% and 0.1% gels did not induce allergic contact sensitization, phototoxicity or photoallergy.
The most frequent adverse events reported with TAZORAC Gel 0.05% and 0.1% were limited to the skin. Those occurring in 10 to 30% of patients, in descending order, included pruritus, burning/stinging, erythema, worsening of psoriasis, irritation, and skin pain. Events occurring in 1 to 10% of patients included rash, desquamation, irritant contact dermatitis, skin inflammation, fissuring, bleeding and dry skin. Increases in “psoriasis worsening” and “sun-induced erythema” were noted in some patients over the 4th to 12th months as compared to the first three months of a 1 year study. In general, the incidence of adverse events with TAZORAC Gel 0.05% was 2 to 5% lower than that seen with TAZORAC Gel 0.1%.
The most frequent adverse events reported with TAZORAC Gel 0.1% in the treatment of acne occurring in 10 to 30% of patients, in descending order, included desquamation, burning/stinging, dry skin, erythema and pruritus. Events occurring in 1 to 10% of patients included irritation, skin pain, fissuring, localized edema and skin discoloration.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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