tretinoin and tazarotene

Acne vulgaris is a chronic disfiguring inflammatory disease of adolescents and adults affecting up to 90% of the population around the world. The sequence of etiopathogenesis in acne is not completely understood but involves abnormalities in sebum production, follicular plugging, proliferation of propionibacterium acnes, and chronic inflammation.. This review aims to summarize the features of the topical selective RAR agonists in treating acne vulgaris with a special emphasis on the 4th generation topical retinoid trifarotene.. Studies were identified by searching electronic databases (MEDLINE and PubMed) till August 2019 and reference lists of respective articles. Only articles published in English language were included.. Topical retinoids have been first line of treatment for more than 30 years now in treating mild to moderate acne vulgaris. Third generation retinoids like adapalene and tazarotene are selective RAR and γ agonists, having an additional anti-inflammatory action along with their comedolytic effects and work well in combinations with topical antibiotics, due to the stability of chemical composition.. Trifarotene is a new 4th generation retinoid with selective action on RAR-γ receptor alone, which is specific for skin, and it is safe for long-term maintenance therapy with good efficacy and tolerability.

Topics: Acne Vulgaris; Adapalene; Administration, Cutaneous; Dermatologic Agents; Humans; Nicotinic Acids; Randomized Controlled Trials as Topic; Receptors, Retinoic Acid; Retinoids; Treatment Outcome; Tretinoin

Topics: Administration, Cutaneous; Dermatologic Agents; Humans; Isotretinoin; Keratosis; Laser Therapy; Nicotinic Acids; Randomized Controlled Trials as Topic; Skin Aging; Skin Diseases; Sunlight; Tretinoin

Skin, being exposed directly to the environment, represents a unique model for demonstrating the synergistic effects of intrinsic and extrinsic factors on the ageing process. Ultraviolet radiation (UVR) is the major factor among exogenous stressors responsible for premature skin ageing. The problem of skin ageing has captured public attention and has an important social impact. Different therapeutic approaches have been developed to treat cutaneous ageing and to diminish or prevent the negative effects of UVR. Topical retinoids represent an important and powerful class of molecules in the dermatologist's hands for the treatment of photodamaged skin. Since their introduction more than 20 years ago, topical retinoids have shown beneficial efficacy and good safety profiles in the management of photodamaged skin, and as therapeutic anti-ageing agents. This review provides a brief retrospective of the development of topical retinoids in the treatment of photodamaged skin, elucidates their mechanism of action, delineates their use and addresses clinical, pharmaceutical and regulatory issues in connection with their intended use.

Topics: Administration, Topical; Dermatologic Agents; Evidence-Based Medicine; Humans; Isotretinoin; Nicotinic Acids; Retinoids; Skin Aging; Tretinoin; Ultraviolet Rays; Vitamin A

Topical retinoids represent a mainstay of acne treatment because they expel mature comedones, reduce microcomedone formation, and exert anti-inflammatory effects. The first-generation retinoid tretinoin (all-trans retinoic acid) and the synthetic third-generation polyaromatics adapalene and tazarotene are approved for acne treatment by the US FDA, whereas topical tretinoin, isotretinoin (13-cis retinoic acid), and adapalene are accredited in Canada and Europe. Topical retinoids have a favorable safety profile distinct from the toxicity of their systemic counterparts. Local adverse effects, including erythema, dryness, itching, and stinging, occur frequently during the early treatment phase. Their impact varies with the vehicle formation, skin type, frequency and mode of application, use of moisturizers, and environmental factors such as sun exposure or temperature. The broad anti-acne activity and safety profile of topical retinoids justifies their use as first-line treatment in most types of non-inflammatory and inflammatory acne. They are also suitable as long-term medications, with no risk of inducing bacterial resistance, for maintenance of remission after cessation of initial combination therapy.

Topics: Acne Vulgaris; Adapalene; Administration, Topical; Anti-Inflammatory Agents, Non-Steroidal; Drug Therapy, Combination; Humans; Isotretinoin; Naphthalenes; Nicotinic Acids; Retinoids; Safety; Tretinoin

Chronic sun exposure leads to photodamage, which is characterized clinically by fine and coarse wrinkles, dyspigmentation, telangiectasia, laxity, roughness and a sallow appearance. Many treatments claim to reduce the signs of photodamage, however evidence from randomized controlled trials (RCT) to support these claims is limited. The use of topical retinoids, particularly tretinoin, isotretinoin and tazarotene, has been shown to significantly reduce signs of photodamage both clinically and histologically. Over recent years a number of RCTs, have affirmed that topical tazarotene is an effective and safe treatment for photodamaged skin.

Topics: Drug Therapy, Combination; Humans; Keratolytic Agents; Nicotinic Acids; Retinoids; Skin Aging; Treatment Outcome; Tretinoin

A Cochrane systematic review of 30 randomised clinical trials assessed the effects of current treatments for adults with mild-to-severe changes in facial and forearm skin that occurred as a result of prolonged exposure to the sun ('photodamage'). Topical tretinoin > or = 0.02% improved the appearance of mild-to-severe photodamage. Tazarotene 0.01-0.1% and isotretinoin 0.1% provided benefit to patients with moderate photodamage. The treatment duration was 4-11 months. Adverse effects were pain and redness. Both the efficacy and adverse effects were dose-dependent. Other treatments, such as polysaccharides, hydroxy acids, surgical procedures and laser, cannot be recommended.

Topics: Administration, Cutaneous; Dermatologic Agents; Dose-Response Relationship, Drug; Humans; Nicotinic Acids; Randomized Controlled Trials as Topic; Skin Aging; Skin Diseases; Sunlight; Tretinoin

The most widely used retinoids include topical tretinoin (Retin-A), adapalene (Differin), topical tazarotene (Tazorac), isotretinoin (Accutane), and acitretin (Soriatane). This article will review new uses and developments in tazarotene (its failure to secure FDA approval in oral form for psoriasis), adapalene (its new 0.3% gel form and use in rosacea), alitretinoin (its use in photoaging), bexarotene (its use for psoriasis and chronic hand dermatitis), isotretinoin (the IPledge program, its use for neuroblastoma and branded formulation pharmacological superiority to generics), and retinoic acid metabolism-blocking agents (RAMBAs) (liarazole use for ichthyosis and psoriasis).

Topics: Adapalene; Humans; Isotretinoin; Keratolytic Agents; Naphthalenes; Nicotinic Acids; Retinoids; Skin Diseases; Tretinoin

Aging of skin is an intricate biological process consisting of two types. While intrinsic or chronological aging is an inevitable process, photoaging involves the premature aging of skin occurring due to cumulative exposure to ultraviolet radiation. Chronological and photoaging both have clinically differentiable manifestations. Various natural and synthetic retinoids have been explored for the treatment of aging and many of them have shown histological and clinical improvement, but most of the studies have been carried out in patients presenting with photoaged skin. Amongst the retinoids, tretinoin possibly is the most potent and certainly the most widely investigated retinoid for photoaging therapy. Although retinoids show promise in the treatment of skin aging, irritant reactions such as burning, scaling or dermatitis associated with retinoid therapy limit their acceptance by patients. This problem is more prominent with tretinoin and tazarotene whereas other retinoids mainly represented by retinaldehyde and retinol are considerably less irritating. In order to minimize these side effects, various novel drug delivery systems have been developed. In particular, nanoparticles have shown a good potential in improving the stability, tolerability and efficacy ofretinoids like tretinoin and retinol. However, more elaborate clinical studies are required to confirm their advantage in the delivery of topical retinoids.

Topics: Adapalene; Dermatologic Agents; Dermis; Epidermis; Humans; Naphthalenes; Nicotinic Acids; Retinaldehyde; Retinoids; Skin Aging; Treatment Outcome; Tretinoin; Vitamin A Deficiency

Photodamage describes skin changes such as fine and coarse wrinkles, roughness, freckles and pigmentation changes that occur as a result of prolonged exposure to the sun. Many treatments are available to reverse the damage, but it is unclear which work and at what cost in terms of unwanted side effects.. To assess the effects of topically applied treatments, tablet treatments, laser and surgical procedures for photodamaged skin.. We searched the Cochrane Central Register of Controlled Trials (CENTRAL) in The Cochrane Library, Issue 1 2002, MEDLINE (1966-June 2002), EMBASE (1974-June 2002), Health Periodicals (1976-June 2002). We checked references of articles and communicated with authors and the pharmaceutical industry.. Randomised controlled trials which compared drug or surgical interventions with no treatment, placebo or another drug, in adults with mild, moderate or severe photodamage of the face or forearms.. Two reviewers independently extracted data and assessed trial quality.. Thirty studies of variable quality were included. Eight trials showed that topical tretinoin cream, in concentrations of 0.02% or higher, was superior to placebo for participants with mild to severe photodamage on the face and forearms (although losses to follow-up were relatively high in most studies). For example, the relative risk of improvement for 0.05% tretinoin cream, compared to placebo (three studies), at 24 weeks, was 1.73 (95% confidence interval 1.39 to 2.14). This effect was not seen for 0.001% topical tretinoin (one study) or 0.01% (three studies). A dose-response relationship was evident for both effectiveness and skin irritation. One small within-patient study showed benefit from topical ascorbic acid compared with placebo. Tazarotene (0.01% to 0.1%) and isotretinoin (0.1%) both showed significant improvement over placebo for moderate photodamage (one study each). There is limited evidence (one trial), to show that the effectiveness of 0.05% tretinoin, is equivalent to the effects of 0.05% and 0.1% tazarotene. One small study showed greater improvement in upper lip wrinkles with CO2 laser technique compared to Baker's phenol chemical peel, at 6 months. Three small RCTs comparing CO2 laser with dermabrasion found no difference in wrinkle score at 4 to 6 months, suggesting that both methods are equally efficacious, but more erythema was reported with the laser. The effectiveness of other interventions such as hydroxy acids and natural polysaccharides was not clear.. There is conclusive evidence that topical tretinoin improves the appearance of mild to moderate photodamage on the face and forearms, in the short term. However erythema, scaling/dryness, burning/stinging and irritation may be experienced initially. There is limited evidence that tazarotene and isotretinoin benefit patients with moderate photodamage on the face: both are associated with skin irritation and erythema. The effectiveness of other interventions remains uncertain.

Topics: Administration, Cutaneous; Dermatologic Agents; Humans; Isotretinoin; Keratosis; Laser Therapy; Nicotinic Acids; Randomized Controlled Trials as Topic; Skin Aging; Skin Diseases; Sunlight; Tretinoin

Topics: Dermabrasion; Humans; Isotretinoin; Laser Therapy; Nicotinic Acids; Skin Aging; Sunscreening Agents; Tretinoin

Topics: Acne Vulgaris; Adapalene; Dermatologic Agents; Humans; Keratolytic Agents; Meta-Analysis as Topic; Multicenter Studies as Topic; Naphthalenes; Nicotinic Acids; Randomized Controlled Trials as Topic; Retinoids; Treatment Outcome; Tretinoin; United States

Topical tazarotene has shown superior efficacy over other topical retinoids, including adapalene and tretinoin, in the treatment of mild to moderate acne. A meta-analysis of data from 6 multicenter, double-blind, randomized comparative trials was performed to determine how patient characteristics influence the efficacy and tolerability of topical tazarotene. Data on 468 patients who used tazarotene 0.1% gel or cream once daily for 12 weeks were collected. Topical tazarotene was effective and well tolerated, regardless of patients' acne severity, skin type, sex, or ethnicity. In general, 'using the cream formulation rather than the gel formulation optimized tolerability. These results indicate that topical tazarotene 0.1% gel and cream are efficacious and well-tolerated treatment options for clearing acne vulgaris across a broad range of patients.

Topics: Acne Vulgaris; Adapalene; Administration, Cutaneous; Adult; Dermatologic Agents; Drug Administration Schedule; Female; Gels; Humans; Male; Multicenter Studies as Topic; Naphthalenes; Nicotinic Acids; Randomized Controlled Trials as Topic; Retinoids; Severity of Illness Index; Time Factors; Treatment Outcome; Tretinoin; United States

Adapalene (Differin) is a retinoid agent indicated for the topical treatment of acne vulgaris. In clinical trials, 0.1% adapalene gel has proved to be effective in this indication and was as effective as 0.025% tretinoin gel, 0.1% tretinoin microsphere gel, 0.05% tretinoin cream and 0.1% tazarotene gel once every two days; however, the drug was less effective than once-daily 0.1% tazarotene gel. It can be used alone in mild acne or in combination with antimicrobials in inflammatory acne and has proved efficacious as maintenance treatment. Adapalene has a rapid onset of action and a particularly favorable tolerability profile compared with other retinoids. These attributes can potentially promote patient compliance, an important factor in treatment success. Adapalene is, therefore, assured of a role in the first-line treatment of acne vulgaris.

Topics: Acne Vulgaris; Adapalene; Administration, Cutaneous; Anti-Inflammatory Agents, Non-Steroidal; Dermatologic Agents; Drug Administration Schedule; Gels; Humans; Multicenter Studies as Topic; Naphthalenes; Nicotinic Acids; Randomized Controlled Trials as Topic; Treatment Outcome; Tretinoin

Topics: Ascorbic Acid; Dermabrasion; Humans; Isotretinoin; Laser Therapy; Nicotinic Acids; Skin Aging; Sunscreening Agents; Tretinoin; Vitamin E

Precise classification methods are used to define acne according to type (comedonal, papulopustular, or nodular) and severity. The relative effectiveness of several topical and systemic agents has been established in clinical trials, making possible an algorithm of specific treatment decisions based on acne classification.

Topics: Acne Vulgaris; Adapalene; Administration, Oral; Administration, Topical; Algorithms; Anti-Bacterial Agents; Benzoyl Peroxide; Contraceptives, Oral; Controlled Clinical Trials as Topic; Cost-Benefit Analysis; Decision Trees; Dermatologic Agents; Dicarboxylic Acids; Humans; Isotretinoin; Macrolides; Naphthalenes; Nicotinic Acids; Salicylates; Tretinoin; United States

Topics: Antioxidants; Dermabrasion; Dermatologic Agents; Humans; Isotretinoin; Laser Therapy; Nicotinic Acids; Skin Aging; Sunscreening Agents; Tretinoin

Topical retinoic acid was introduced for acne treatment three decades ago. Since that time, researchers have discovered thousands of retinoids, originally defined as chemical analogs of vitamin A. After the identification of nuclear retinoid receptors in 1987, the definition of this class expanded to include molecules that bind to and activate such receptors. The receptor-selective retinoid agents, adapalene and tazarotene, were developed in the 1990s. Other innovations of the past decade include retinoid formulations and methods aimed at limiting retinoid absorption. Cutaneous irritation may be reduced without losing retinoid efficacy by inhibiting retinoid penetration into the deep epidermis and dermis. Examples include tretinoin in slow-release vehicles and the short-contact method of tazarotene gel therapy. Only trace amounts of adapalene are absorbed after topical application, perhaps explaining its relatively low irritancy. New formulations of existing agents, such as additional concentrations of tretinoin in microsphere gel and cream formulations of tazarotene, are now under investigation for acne. Current research focused on receptor selectivity holds the promise of yielding new retinoid molecules with improved benefits and safety.

Topics: Acne Vulgaris; Adapalene; Dermatologic Agents; Drug Combinations; Humans; Keratolytic Agents; Naphthalenes; Nicotinic Acids; Receptors, Retinoic Acid; Tretinoin; Vitamin A

The efficacy and tolerability of tazarotene 0.1% gel in the treatment of acne vulgaris have been compared with those of tretinoin 0.025% gel and adapalene 0.1% gel in multicenter, double-blind, randomized, parallel-group trials. Preliminary results from the tazarotene versus tretinoin trial suggest that once-daily tazarotene is more efficacious than once-daily tretinoin in reducing the numbers of papules and open comedones, and achieves a more rapid reduction in pustules. Both drugs appear to be equally efficacious against closed comedones. Preliminary results from the tazarotene versus adapalene trial suggest that, when tazarotene is applied only half as frequently as adapalene (every other day versus every day), the two drugs achieve comparable reductions in noninflammatory and inflammatory lesion counts. The results from these studies, and a separate split-face tolerability study, suggest that the tolerability of tazarotene gel is clinically comparable to that of tretinoin 0.025% gel, tretinoin 0.1% gel microsphere, and adapalene 0.1% gel.

Topics: Acne Vulgaris; Adapalene; Administration, Topical; Dermatologic Agents; Double-Blind Method; Gels; Keratolytic Agents; Multicenter Studies as Topic; Naphthalenes; Nicotinic Acids; Randomized Controlled Trials as Topic; Treatment Outcome; Tretinoin

Topics: Acne Vulgaris; Adapalene; Administration, Topical; Anti-Inflammatory Agents, Non-Steroidal; Gels; Humans; Keratolytic Agents; Naphthalenes; Nicotinic Acids; Ointments; Retinoids; Tretinoin

This 12-week, single-center, investigator-blinded, randomized, parallel-design study assessed the safety and efficacy of tretinoin microsphere gel 0.04% delivered by pump (TMG PUMP) to tazarotene cream 0.05% (TAZ) in mild-to-moderate facial acne vulgaris. Efficacy measurements included investigator global assessment (IGA), lesion counts, and subject self-assessment of acne signs and symptoms. Efficacy was generally comparable between treatment groups, although TMG PUMP provided more rapid results in several parameters. IGA showed a more rapid mean change from baseline at week 4 in the TMG PUMP group (-0.18 versus -0.05 in the TAZ subjects). TMG PUMP yielded more rapid improvement in papules. At week 4, the mean percentage change from baseline in open comedones was statistically significant at -64% in the TMG PUMP group (P=0.0039, within group) versus -19% in the TAZ group (not statistically significant within the group; P=0.1875). Skin dryness, peeling and pruritus were significantly less in the TMG PUMP group as early as week 4. Adverse events related to study treatment were rare in both groups and all resolved upon discontinuation of study medication.

Topics: Acne Vulgaris; Administration, Cutaneous; Adolescent; Adult; Child; Female; Gels; Humans; Keratolytic Agents; Male; Microspheres; Nicotinic Acids; Pilot Projects; Severity of Illness Index; Single-Blind Method; Treatment Outcome; Tretinoin; Young Adult

Topical retinoids are the cornerstone of therapy for acne vulgaris. Nevertheless, the adjunctive use of other anti-acne agents can help enhance the efficacy of topical retinoids still further. Given that tazarotene 0.1 percent gel has previously shown significantly greater efficacy than tretinoin 0.025 percent gel, it is likely that tazarotene plus clindamycin offers superior efficacy to tretinoin plus clindamycin, which has recently become available as a combination product. A total of 150 patients with facial acne vulgaris were randomly assigned to receive either tazarotene 0.1 percent cream plus clindamycin 1 percent gel, or tretinoin 0.025 percent gel plus clindamycin 1 percent gel. Each medication was applied once daily in the evening (clindamycin followed by the retinoid 5-10 minutes later) for up to 12 weeks. At week 12, the reduction from baseline in lesion counts was greater with tazarotene/clindamycin than tretinoin/clindamycin for both the non-inflammatory lesion count (71% vs. 52%, p< or =.01) and the inflammatory lesion count (77% vs. 67%, P=.053). Tazarotene/clindamycin also resulted in a significantly higher incidence of patients achieving > or = 50 percent global improvement (incidence of 88% vs. 75% at week 12; p< or =.05). Both regimens were similarly well tolerated. In the treatment of facial acne vulgaris, tazarotene plus clindamycin offers significantly greater efficacy than tretinoin plus clindamycin and has comparable tolerability.

Topics: Acne Vulgaris; Administration, Topical; Adolescent; Adult; Anti-Bacterial Agents; Child; Clindamycin; Dose-Response Relationship, Drug; Double-Blind Method; Drug Therapy, Combination; Female; Follow-Up Studies; Gels; Humans; Keratolytic Agents; Male; Middle Aged; Nicotinic Acids; Ointments; Retinoids; Severity of Illness Index; Treatment Outcome; Tretinoin

To compare the efficacy and tolerability of tazarotene 0.1% cream and tretinoin 0.05% emollient cream in the treatment of photodamaged facial skin.. Subjects were eligible to enroll in this multicenter, double-blind, randomized, parallel-group study if they had at least mild levels of facial fine wrinkling and mottled hyperpigmentation, and at least moderate levels of one of these. Subjects were randomly assigned to apply either tazarotene cream or tretinoin emollient cream to their faces once each evening for 24 weeks.. A total of 173 subjects were enrolled, of whom 157 completed. All significant between-group differences in efficacy measures were in favor of tazarotene - for fine wrinkling at the study endpoint and, at earlier timepoints, for treatment success (> or =50% global improvement), and the overall integrated assessment of photodamage, mottled hyperpigmentation, and coarse wrinkling. Both products were comparable in terms of cosmetic acceptability and tolerability except that tazarotene was associated with a transiently higher incidence of a burning sensation on the skin (in the first week of treatment but not thereafter).. Tazarotene 0.1% cream can offer superior efficacy over tretinoin 0.05% emollient cream in the treatment of facial photodamage, particularly with respect to the speed of improvement.

Topics: Administration, Topical; Dermatologic Agents; Double-Blind Method; Emollients; Face; Female; Humans; Hyperpigmentation; Male; Middle Aged; Nicotinic Acids; Skin Aging; Treatment Outcome; Tretinoin

Forty-two subjects with normal skin were enrolled in a single-center study to assess the cumulative irritancy potential of adapalene (Differin gel 0.1% and Differin solution 0.1%) compared with tazarotene (Tazorac gels 0.05% and 0.1%), tretinoin (Retin-A Micro gel 0.1%, Avita cream 0.025%, and Avita gel 0.025%), and white petrolatum (negative control). All test materials were applied randomly, under occlusion, to sites located on either side of the midline--the mid thoracic area of the subjects' backs. All patches were applied daily, Monday through Friday, to the same sites, unless the degree of reaction to a test product or adhesive necessitated removal (grade 3). Thirty-eight of the 42 subjects (90.5%) completed the study. Thirty-four of those 38 subjects (89.5%) had to discontinue using both tazarotene concentrations due to intolerance. Patch discontinuations for the remaining test materials were as follows: 7 subjects discontinued use of tretinoin microsphere gel 0.1%, 3 discontinued tretinoin cream 0.025%, 1 discontinued tretinoin gel 0.025%, and 1 discontinued adapalene gel 0.1%. None of the subjects discontinued use of the white petrolatum or the adapalene solution 0.1%. Adapalene gel and solution 0.1% were statistically (P<.01) less irritating than both tazarotene gels 0.1% and 0.05%, tretinoin microsphere gel 0.1%, and tretinoin gel 0.025%, and they were not statistically different from tretinoin gel 0.025%.

Topics: Adapalene; Adult; Aged; Dermatologic Agents; Double-Blind Method; Drug Interactions; Erythema; Female; Gels; Humans; Male; Middle Aged; Naphthalenes; Nicotinic Acids; Probability; Sensitivity and Specificity; Skin Irritancy Tests; Tretinoin

The efficacy and tolerability of tazarotene 0.1% gel and tretinoin 0.1% microsponge gel were evaluated in a multicenter, double-blind, randomized, parallel-group study in patients with mild-to-moderate inflammatory facial acne vulgaris. A total of 169 patients were randomized to once-daily applications of one of these topical retinoids for 12 weeks. Both agents were associated with significant reductions from baseline in the noninflammatory and inflammatory lesion counts. Tazarotene treatment was associated with a significantly greater incidence of treatment success (defined as > or = 50% global improvement [67% vs 49%; P=.03]) and significantly greater reductions in overall disease severity (36% vs 26%; P=.02) and noninflammatory lesion count (60% vs 38% at week 12; P=.02) than tretinoin microsponge treatment. Both drugs were well tolerated, with mean levels of dryness, burning, pruritus, erythema, and peeling generally being no more than trace throughout the study. There were no clinically significant between-group differences in these measures of tolerability. Two patients in each group (2%) discontinued because of treatment-related adverse events. The mean amount of medication applied by the patients was 0.28 g per application with tazarotene and 0.41 g per application with tretinoin microsponge, resulting in cost-effectiveness ratios of $81.45 per treatment success with tazarotene and $108.24 per treatment success with tretinoin microsponge. Tazarotene was observed to have greater efficacy and comparable tolerability and to be a cost-effective alternative to tretinoin 0.1% microsponge gel.

Topics: Acne Vulgaris; Administration, Cutaneous; Adolescent; Adult; Child; Cost-Benefit Analysis; Dermatologic Agents; Double-Blind Method; Drug Administration Schedule; Facial Dermatoses; Female; Gels; Humans; Male; Nicotinic Acids; Severity of Illness Index; Treatment Outcome; Tretinoin; United States

Tazarotene 0.1% gel and tretinoin 0.025% gel are both effective in the treatment of acne vulgaris. Results of a multicenter, double-blind, randomized, parallel-group study that compared the efficacy and tolerability of these drugs are presented here. A total of 143 patients with mild-to-moderate facial acne vulgaris were randomized to receive tazarotene 0.1% gel or tretinoin 0.025% gel once daily for 12 weeks. Tazarotene 0.1% gel was more effective than tretinoin 0.025% gel in reducing the open comedo count (P < or = .05), the total noninflammatory lesion count (P < or = .05), and the total inflammatory lesion count (not statistically significant). At some time points, tazarotene was associated with increased irritation, but peeling, erythema, dryness, burning, and itching never exceeded trace levels. We conclude that tazarotene 0.1% gel is more effective than tretinoin 0.025% gel in reducing noninflammatory lesions and similarly effective in reducing inflammatory lesions.

Topics: Acne Vulgaris; Adolescent; Adult; Child; Double-Blind Method; Female; Gels; Humans; Keratolytic Agents; Male; Nicotinic Acids; Retinoids; Treatment Outcome; Tretinoin

Two double-blind, randomized, split-face studies have been performed to compare the facial tolerability of topical retinoids in volunteers with sensitive skin. In one study, subjects applied tazarotene 0.1% gel to one side of their face and tretinoin 0.1% gel microsponge, tretinoin 0.025% gel, or adapalene 0.1% gel to the other side of their face, for up to 29 days. Increases in facial dryness and erythema were comparable among all retinoids. Some subjects in each treatment group experienced levels of retinoid-associated irritation that required temporary suspension of, or reduction in, treatment. Facial dryness and erythema tended to be greater in these subjects than in those who tolerated the regimen without change, suggesting that the need to discontinue or modify treatment depends more on the individual than on any major inherent differences in the irritant potential of these retinoids. A second study compared once-daily versus alternate-day tazarotene 0.1% gel therapy. Tolerability was superior when initiating therapy with the alternate-day regimen.

Topics: Acne Vulgaris; Adolescent; Adult; Child; Double-Blind Method; Gels; Humans; Keratolytic Agents; Nicotinic Acids; Retinoids; Tretinoin

To assess the safety and efficacy of 4 concentrations of tazarotene cream in the treatment of facial photodamage.. Prospective weekly multicenter, investigator-masked, randomized, parallel-group study.. University hospitals and clinical research centers.. Three hundred forty-nine subjects with facial photodamage.. Daily topical application of tazarotene cream (0.01%, 0.025%, 0.05%, and 0.1%) compared with its vehicle and with 0.05% tretinoin emollient cream.. Tazarotene cream and tretinoin cream significantly improved mottled hyperpigmentation and fine wrinkles. At week 24, treatment success rates based on global responses were 67% (39 of 58 subjects) with 0.1% tazarotene, 52% (30 of 58 subjects) with 0.05% tazarotene, 36% (21 of 58 subjects) with 0.025% tazarotene, 41% (24 of 59 subjects) with 0.01% tazarotene, 55% (32 of 58 subjects) with 0.05% tretinoin, and 22% (13 of 58 subjects) with vehicle. Local adverse events, although more frequent with tazarotene at higher concentrations, were generally mild to moderate.. Tazarotene in a cream formulation is safe and is associated with positive changes in the treatment of photodamaged facial skin.

Topics: Administration, Cutaneous; Adult; Dermatologic Agents; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Face; Female; Humans; Hyperpigmentation; Male; Nicotinic Acids; Prospective Studies; Retinoids; Skin Aging; Treatment Outcome; Tretinoin; United States

Currently available therapies for chronic hepatitis B virus (HBV) infection can efficiently reduce viremia but induce hepatitis B surface antigen (HBsAg) loss in very few patients; also, these therapies do not greatly affect the viral covalently closed circular DNA (cccDNA). To discover new agents with complementary anti-HBV effects, we performed a drug repurposing screen of 1,018 Food and Drug Administration (FDA)-approved compounds using HBV-infected primary human hepatocytes (PHH). Several compounds belonging to the family of retinoic acid receptor (RAR) agonists were identified that reduced HBsAg levels in a dose-dependent manner without significant cytotoxicity. Among them, tazarotene exhibited the most potent anti-HBV effect, with a half-maximal inhibitory concentration (IC

Topics: Acitretin; Adapalene; Antiviral Agents; Cell Line; Cell Survival; Dermatologic Agents; Drug Repositioning; Drug Synergism; Gene Expression; Guanine; Hep G2 Cells; Hepatitis B e Antigens; Hepatitis B Surface Antigens; Hepatitis B virus; Hepatocytes; High-Throughput Screening Assays; Host-Pathogen Interactions; Humans; Keratolytic Agents; Nicotinic Acids; Receptors, Retinoic Acid; Transcription, Genetic; Tretinoin; Virus Replication

Topical retinoids are currently approved by the US Food and Drug Administration for the treatment of acne vulgaris in nonpregnant, nonlactating patients 12 years of age and older. Their efficacy, safety, and tolerability are well documented for inflammatory and noninflammatory acne with studies repeatedly demonstrating a decrease in the number of lesions, significant improvement in acne severity, improvement in the cosmetic appearance of acne, and the prevention of acne lesions through microcomedone formation. There is some variability between prescription retinoid products regarding efficacy, safety, and tolerability; with erythema, peeling, and dryness being common, potential side effects. Due to their efficacious and safe profile, topical retinoids remain the first-line treatment for acne vulgaris.

Topics: Acne Vulgaris; Adapalene; Administration, Cutaneous; Dermatologic Agents; Humans; Nicotinic Acids; Retinoids; Treatment Outcome; Tretinoin

To investigate the molecular mechanism of dermal damage in heat shock-induced skin aging by observing the expressions of metalloproteinase-1 (MMP-1) and tissue inhibitor of MMP-1 (TIMP-1) in retinoic acid-treated cultured human fibroblasts with heat shock.. Cultured human fibroblasts were treated with tazarotene or all-trans-retinioic acid (at-RA) after heat shock for 30 min in 43 degrees celsius; water bath. Twenty-four hours later, MMP-1 and TIMP-1 contents in the supernatant of the cell culture medium were measured using enzyme-linked immunosorbent assay (ELISA).. Both tazarotene and at-RA dose-dependently reduced the expression of MMP-1 and increased the expression of TIMP-1 in cultured human fibroblasts exposed to heat shock, and tazarotene produced stronger effect than at-RA.. Retinoic acid can reduce the expression of MMP-1 and increase the expression of TIMP-1 in cultured human fibroblasts, suggesting its therapeutic potential for heat shock-induced skin aging.

Topics: Cells, Cultured; Fibroblasts; Heat-Shock Response; Humans; Matrix Metalloproteinase 1; Nicotinic Acids; Skin Aging; Tissue Inhibitor of Metalloproteinase-1; Tretinoin

Oral acitretin is currently indicated for the treatment of severe psoriasis in adults, but its use is limited by systemic side effects and teratogenicity. Topical administration of acitretin may lessen the risk of systemic toxicity while increasing local bioavailability in the skin. The effects of topical acitretin on reconstructed human epidermis (RHE) and Rhino mice were investigated and compared to those of currently marketed topical retinoids: tretinoin and tazarotene. In acitretin-treated RHE cultures, there was a reduction in keratohyalin granules and filaggrin expression in the stratum granulosum, a loss of keratin 10 expression in the stratum spinosum, and an increase in keratin 19 expression in all viable cell layers. All retinoids showed similar signs of activity in RHE cultures. Furthermore, the release of pro-inflammatory cytokines IL-1alpha and IL-8 in RHE cultures was less pronounced with acitretin compared to tretinoin- and tazarotene-containing formulations, suggesting that acitretin may be less irritating. In Rhino mice, acitretin induced a local, dose-dependent reduction in utricle diameter after seven daily dermal doses. A similar effect was observed in tretinoin- and tazarotene-treated mice. Our data suggest that topical application of acitretin may have a therapeutic benefit in the local management of keratinization disorders.

Topics: Acitretin; Administration, Topical; Animals; Disease Models, Animal; Epidermis; Female; Filaggrin Proteins; Humans; Interleukin-1alpha; Interleukin-8; Keratin-10; Keratin-19; Keratolytic Agents; Male; Mice; Mice, Hairless; Nicotinic Acids; Psoriasis; Tretinoin

This article reports on recent studies and case reports that evaluated the stability, tolerability, and efficacy of clindamycin 1%-benzoyl peroxide 5% tube gel in combination with topical retinoids and oral antibiotics. Overall, these combinations appeared to be well-tolerated, effective, and, as reported in the case studies, adaptable to common clinical practice.

Topics: Acne Vulgaris; Adapalene; Administration, Cutaneous; Administration, Oral; Adolescent; Adult; Anti-Bacterial Agents; Benzoyl Peroxide; Clindamycin; Dermatologic Agents; Drug Combinations; Female; Gels; Humans; Keratolytic Agents; Male; Minocycline; Naphthalenes; Nicotinic Acids; Retinoids; Treatment Outcome; Tretinoin

To investigate the effects of all-trans retinoic acid (ATRA), acitretin and tazarotene on apoptosis and Bax/Bcl-2 protein expressions of human melanoma A375 cells.. The effects of retinoids on apoptosis and Bax/Bcl-2 protein expressions of A375 cells in vitro were examined. Apoptosis analysis with double staining with annexin V-FITC and PI was performed using flow cytometer. SABC immunocytochemistry was employed for detection of Bax/Bcl-2 protein expressions.. At the concentration of 1 x 10(-5) mol/L, ATRA, acitretin and tazarotene all induced apoptosis of A375 cells with apoptosis ratio of 5.03% (P<0.05), 13.42% (P<0.05) and 2.88% (P>0.05), respectively, and acitretin induced more significant apoptosis than the other two agents (P<0.05). In addition, all the three agents significantly increased the number of cells positive for Bax expression and decreased the number of cells expressing Bcl-2 (P<0.05), among which acitretin had the strongest effects.. ATRA, acitretin and tazarotene mediate apoptosis of A375 cells possibly through, at least partially, the mitochondrial pathway. Acitretin may be utilized as a valuable alternative for treating melanoma.

Topics: Acitretin; Antineoplastic Agents; Apoptosis; bcl-2-Associated X Protein; Humans; Melanoma; Nicotinic Acids; Proto-Oncogene Proteins c-bcl-2; Skin Neoplasms; Tretinoin; Tumor Cells, Cultured

To investigate the effects of ATRA, acitretin and tazarotene on the growth and apoptosis of human tongue squamous cell carcinoma cell line Tca8113. The effect of retinoids on growth of Tca8113 cells in vitro was examined by MTT assay and Trypan blue exclusion assay. Cell cycle analysis, early apoptosis analysis with double staining with Annexin V-FITC and PI, and active caspase-3 analysis with the staining of FITC-conjugated monoclonal rabbit anti-active caspase-3 antibody were made by flow cytometer. Streptavidin-biotin complex (SABC) immunocytochemical assays were employed for the detections of Bax/Bcl-2 proteins expressions. Our results showed that the retinoids inhibited growth of Tca8113 cells in a dose- and time-dependent manner with maximal inhibition 24 h after treatment of 10(-5) mol/L. 10(-5) mol/L retinoids altered cell cycle distribution of Tca8113 cells, revealing an increase in G0/G1-phase population, a decrease in S-phase population and the inhibition of G1/S switching. 10(-5) mol/L retinoids significantly induced apoptosis of Tca8113 cells (all P < 0.05), elevated the cells population with detectable active caspase-3 (P < 0.05 for all), increased the number of cells forming Bax and decreased the number of cells forming Bcl-2 significantly (all P < 0.05). Acitretin played a most prominent role among the retinoids. It is concluded that the inhibition of cell cycle progress of Tca8113 cells by ATRA, acitretin and tazarotene is one of the possible mechanisms for proliferation arrest of Tca8113 cells elicited by the retinoids. The retinoids mediate apoptosis in Tca8113 cells that may be caspase-dependent through mitochondria pathway. High concentration retinoids inhibit growth of Tca8113 cells in vitro by interfering with proliferation and inducing apoptosis of cells. Acitretin may be an alternative medicine for the prevention and treatment of tongue squamous cell carcinoma.

Topics: Acitretin; Antineoplastic Agents; Apoptosis; Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Proliferation; Humans; Nicotinic Acids; Tongue Neoplasms; Tretinoin

Topics: Cryotherapy; Dermatologic Agents; Humans; Keratolytic Agents; Laser Therapy; Nicotinic Acids; Skin Aging; Tretinoin

Retinoids affect keratinocyte differentiation and modulate the expression of many epidermal proteins, among them cellular retinoic acid-binding protein II and the family of cytokeratins. The upregulation of the former protein is a well-known phenomenon, whereas the retinoid-induced regulation of epidermal keratin expression is more complex and only partially understood. We studied the effect of topical retinoids on the expression in healthy skin of cellular retinoic acid-binding protein II, tazarotene-induced genes 1 and 2, several epidermal keratins (K1, K2e, and K10), and two mucous keratins (K4 and K13) known to appear in epidermis under certain abnormal conditions. Reverse transcription-polymerase chain reaction experiments showed that the K4 expression was the one most overtly induced by 2 wk of open treatment with 0.05% of retinoic acid and tazarotene. Using real-time quantitative polymerase chain reaction (TaqMan) and normalization of the mRNA values to beta-actin, the increase in K4 was found to be 100-1000-fold. In comparison, the expression of K13 and cellular retinoic acid-binding protein II was increased 10-50-fold, the K1 and K10 mRNA levels remained unchanged, and the K2e level decreased by a factor of 100-1000. In parallel biopsies, immunohistochemistry showed no change in K1, K2e, or K10 staining, but a strong de novo appearance of K4 in the granular layer after retinoid treatment. In a separate study, occlusive application of 0.025% retinoic acid in four healthy subjects produced a maximal K4 mRNA signal after 48 h and strong K4 staining after 80 h. Finally, a dose-response study showed that the de novo appearance of K4 can be utilized as a sensitive test for retinoid bioactivity in epidermis in vivo.

Topics: Administration, Topical; Adult; Biomarkers; Dose-Response Relationship, Drug; Female; Gene Expression; Humans; Immunohistochemistry; Keratins; Male; Middle Aged; Nicotinic Acids; Receptors, Retinoic Acid; Retinoids; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Skin; Time Factors; Tretinoin; Up-Regulation

The inhibitory effect of tazarotene, an acetylenic retinoid, on human dermal fibroblast in vitro was compared to that of all-trans-retinoic acid. The proliferation of fibroblasts was inhibited by both retinoids at the concentration of 1 microM after 5 days of culture. Synthesis of DNA and collagen was inhibited by both retinoids concentration-dependently up to 10 microM, although tazarotene was weaker in the inhibition of collagen synthesis. These results suggest the possible usefulness of tazarotene in the treatment of fibrotic diseases.

Topics: Bromodeoxyuridine; Cell Division; Cells, Cultured; Collagen; Dermatologic Agents; DNA; Fibroblasts; Fibrosis; Humans; Nicotinic Acids; Receptors, Retinoic Acid; Retinoids; Skin; Tretinoin