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PubMed2003

The efficacy of calcipotriol + acitretin combination therapy for psoriasis: comparison with acitretin monotherapy.

BACKGROUND: Although the use of an oral retinoid as monotherapy is an effective treatment for psoriasis, it is usually used in combination with other topical or systemic therapies including topical corticosteroids, UVB phototherapy, psoralens + UVA (PUVA) chemotherapy and cyclosporine mainly in an effort to reduce or avoid adverse effects. AIM: To compare the efficacy of the calcipotriol + acitretin combination treatment with acitretin alone over a long period in Korean patients with psoriasis. METHODS: A randomized, bilateral paired comparison was conducted involving 40 patients with psoriasis who received calcipotriol + acitretin combination therapy and 20 psoriasis patients who received acitretin alone. The initial dose of acitretin was 10 or 20 mg/day. The dose was adjusted at each visit (2, 4 and 6 weeks) in steps of 10mg according to patient responsiveness and adverse effects. The maximum dose was 40 mg/day. The treatment duration for all patients ranged from 4-52 weeks. After 12 weeks, the efficacy of therapy, according to Psoriasis Area and Severity Index scores, was assessed. At the end of the study (52 weeks), we selected patients who had achieved complete clearance and compared the duration of treatment and total dose of acitretin used in both groups. RESULTS: After 12 weeks, 16 patients (40%) achieved complete clearance in the calcipotriol + acitretin group and 3 patients (15%) in the acitretin monotherapy group (p < 0.05). After 52 weeks, 24 patients (60%) in the calcipotriol + acitretin group and 8 patients (40%) in the acitretin monotherapy group achieved complete clearance. The duration of treatment and total dose of retinoid required to achieve clearance were slightly lower in the calcipotriol + acitretin combination group, however, this was not statistically significant. With the exception of liver enzyme elevation (which affected more patients in the acitretin monotherapy group than in the combination group), adverse effects were not significantly different. DISCUSSION: Our results showed that calcipotriol might enhance the clinical outcome of systemic acitretin therapy. More large, well-controlled, long-term studies need to be conducted to determine whether there is indeed a beneficial effect of the addition of calcipotriol to acitretin treatment and whether this effect is maintained over long-term periods.

Acitretin↗
PubMed1994

Inability to detect plasma etretinate and acitretin is a poor predictor of the absence of these teratogens in tissue after stopping acitretin treatment.

1. Concentrations of etretinate, acitretin and its main metabolite 13-cis-acitretin were measured in plasma and subcutaneous fat samples from 37 women of childbearing age exposed to acitretin before November 1990. Twenty of the women still used acitretin and 17 had stopped therapy for a period ranging from 1 to 29 months. 2. The prevalences of detectable etretinate concentrations were 45% and 83% in plasma and subcutaneous tissue, respectively, among current acitretin users and 18% and 86% among those who had stopped acitretin therapy. Thus, inability to detect plasma etretinate is a poor predictor of the absence of etretinate in fat. 3. Acitretin and/or etretinate were detectable in fat and in some cases in plasma from women who had ceased acitretin therapy for up to 29 months. 4. We suggest that (cis)-acitretin and etretinate should be monitored in subcutaneous tissue when plasma measurements are negative. The recommended contraception period of 2 years after cessation of acitretin therapy should be reconsidered to avoid the risk of teratogenicity.

Acitretin↗
PubMed1993

Skin, adipose tissue and plasma levels of acitretin with rare occurrence of esterified acitretin during long-term treatment.

In a previous study acitretin and its 13-cis-metabolite were monitored in the plasma and epidermis of healthy volunteers. They were given 50 mg of trans-acitretin daily. No drug accumulation was observed in the skin, nor in the plasma. The purpose of the present study was to extend the data from non-psoriatic to psoriatic (n = 11) subjects, treated for at least 1 month with 25 mg acitretin. Plasma, skin biopsies and subcutaneous fat samples were analysed using HPLC. Trough levels of acitretin in skin were below the quantification limit, increasing to 28 +/- 16 ng/g within 5 h after dosing. Fat tissue levels exceeded those of skin, with values of 98 +/- 71 ng/g within 5 h after drug intake. In 2 patients, additional samples were taken 3 days post-therapy. Here, concentrations were below the quantification limit in adipose tissue, confirming that acitretin is not stored in subcutaneous fat. Esterification of acitretin into etretinate was observed in 2 subjects. This observation illustrates the recently described new metabolic pathway for acitretin. On both occasions, the unexpected ethylester metabolite was extensively stored in fat tissue.

Acitretin↗
PubMed2006

Low-dose acitretin is associated with fewer adverse events than high-dose acitretin in the treatment of psoriasis.

OBJECTIVE: In practice, lower dose acitretin therapy (25 mg/d) seems to be better tolerated and associated with fewer abnormalities found after laboratory testing. Here we revisit the original phase 3 trials for acitretin to evaluate the evidence for low-dose therapy producing fewer adverse effects than the 50 mg/d dosage. DESIGN: We retrospectively analyzed pooled data from 2 large pivotal trials, each including a randomized, placebo-controlled, 8-week double-blind phase followed by a 16-week open-label phase. SETTING: Multicenter pivotal trial of subjects in referral centers and private practice. PARTICIPANTS: Subjects with severe psoriasis requiring systemic therapy were recruited according to inclusion/exclusion criteria. INTERVENTION: During the double-blind phase, subjects received placebo or one of several fixed acitretin doses. Dose adjustment was allowed during the open-label phase, during which high-dose treatment was defined as a mean dosage of 50 mg/d and low-dose treatment was defined as a mean dosage of 25 mg/d. MAIN OUTCOME MEASURES: The frequency of anomalies found after laboratory testing and clinical adverse events were the outcomes of interest. RESULTS: Common adverse effects (dry skin, alopecia, rhinitis, etc) were 2 to 3 times more frequent in subjects receiving 50-mg/d acitretin than in those receiving 25 mg/d. Increases in hepatic enzymes and triglycerides in subjects receiving low-dose therapy were minimal compared with levels in those receiving high-dose therapy. CONCLUSIONS: We have shown low-dose therapy (25 mg/d) to be an effective strategy for substantially reducing acitretin-associated adverse effects. Many adverse effects associated with acitretin therapy are dose dependent and can limit the usefulness of this potentially beneficial therapy.

Acitretin↗
PubMed1989

Combined treatment of psoriasis with acitretin and UVB phototherapy compared with acitretin alone and UVB alone.

The administration of UVB phototherapy and low-dose acitretin (0.34-0.44 mg/kg body weight) was compared with the effect of acitretin alone and UVB phototherapy alone in 41 patients with plaque-type psoriasis. Of these patients, 32 received standard UVB phototherapy without acitretin. The other nine were treated with acitretin and the effect of UVB irradiation (Sylvania UV 21-tubes), applied to one half of the body, was assessed. Clearance was defined as 80-100% improvement and this occurred in eight out of the nine patients (89%) treated with acitretin-UVB (ReUVB) and, in two of them (23%), on the untreated side. Clearance occurred in 20 of the 32 (62.5%) patients given UVB alone. The improvement score was significantly higher for the ReUVB side than the acitretin side. Patients treated with ReUVB showed a statistically higher therapeutic score (95-100% clearance) than those receiving UVB alone. However, taking 80-100% improvement as the criterion, no significant difference was found. The number of treatments to clearance was significantly less for the patients treated with ReUVB than for the UVB (19.3 as compared with 24.9). The total UVB dose and the number of minimal erythema doses (MEDs) could be reduced by approximately 20% in the ReUVB group relative to the UVB group.

Acitretin↗
PubMed1989

Determination of acitretin and 13-cis-acitretin in skin.

The aim of the study was to investigate the concentrations of Ro 10-1670 (acitretin) and its isomeric metabolite Ro 13-7652 (cis-acitretin) after multiple oral dosing of acitretin. We used a highly sensitive HPLC method for simultaneous determination of the 2 retinoids with a quantification limit of 2 ng/ml in plasma and 10 ng/g in total skin (epidermis and dermis). In hairless rats receiving orally 8 mg/kg acitretin once daily during 8 days, blood and skin samples were taken at different time points between 5 and 96 h after the last dose. After 96 h, appreciable concentrations of Ro 10-1670, but not Ro 13-7652 could be measured in the skin, whereas both isomers were below the quantification limit in plasma. In psoriatic patients treated with a once daily dose of 30 mg acitretin, blood samples and biopsies were taken after 1 month of treatment (i.e. under steady state conditions). 24 h after the last drug intake, skin concentrations of acitretin were approximately 10 times higher than those observed in plasma. Ro 10-1670 concentrations in the skin were approximately 3-5 times higher than for Ro 13-7652 and concentrations of both isomers were higher in lesional compared to uninvolved skin.

Acitretin↗
PubMed1991

Acitretin plus UVB therapy for psoriasis. Comparisons with placebo plus UVB and acitretin alone.

UVB radiation is beneficial for the treatment of psoriasis vulgaris. Patients with recalcitrant disease, however, are slow to respond to UVB phototherapy with and without the use of coal tars or emollients. Etretinate and, more recently, acitretin have proved useful, but clinical improvement is slow when they are used as monotherapy in plaque psoriasis. Each drug also produces side effects, some of which are dose related. This study was designed to compare results of treatment with UVB combined with either acitretin (50 mg/day) or placebo to determine if psoriasis would respond faster and to less cumulative exposure to UVB and acitretin. The psoriatic disease cleared to a greater degree in patients treated with acitretin-UVB with fewer treatments and smaller amounts of UVB radiation than in patients treated with either placebo-UVB or acitretin alone.

Acitretin↗
PubMed2003

Acitretin treatment of premalignant and malignant skin disorders in renal transplant recipients: clinical effects of a randomized trial comparing two doses of acitretin.

INTRODUCTION: After renal transplantation, the incidence of premalignant and malignant skin lesions is high. Treatment with acitretin improves the number and aspect of actinic keratoses and appears to reduce the incidence of squamous cell carcinomas, but treatment is hampered by frequent side effects. No optimal long-term dosing advice is available. METHODS: A total of 26 long-term renal transplant recipients were randomized to 1-year treatment with acitretin, either 0.4 mg/kg/d throughout the whole year or 0.4 mg/kg/d during the first 3 months followed by 0.2 mg/kg/d for the remaining 9 months. At 9 different time points, the number of actinic keratoses and tumors was counted, and erythema and thickness of the lesions, and severity of side effects were scored. Patient's judgment was recorded using visual analog scores. RESULTS: In both groups, the number of actinic keratoses decreased by nearly 50%, but the number of new malignant tumors during the study year was similar to the number of tumors in the year before the study. Thickness of the keratoses decreased significantly in both groups. Acitretin dose had to be reduced in most patients because of the frequent occurrence of mucocutaneous side effects, such as cheilitis, excessive peeling of the skin, and hair disorders. In the 14 patients randomized to continuous treatment with a dose of 0.4 mg/kg/d, this dose could be maintained in 3 of 14 patients only. Temporary interruption of acitretin therapy was necessary in 7 of 26 patients. Patients' contentment about the aspect of their skin increased significantly, with no differences between groups. CONCLUSIONS: Acitretin therapy decreased the number of actinic keratoses in renal transplant recipients at a low maintenance dose of 0.2 mg/kg/d and significantly decreased the degree of thickness of the lesions. However, the incidence of new skin malignancies remained unchanged. Despite the high incidence of mucocutaneous side effects, patient's contentment with the aspect of their skin increased significantly.

Acitretin↗
PubMed1988

Acitretin (Ro 10-1670) in the treatment of severe psoriasis. A randomized double-blind parallel study comparing acitretin and etretinate.

A randomized double-blind parallel trial comparing acitretin and etretinate was performed in 20 patients with severe psoriasis during a treatment period of 12 weeks. The initial dose was 30 mg/day for 4 weeks, and the mean dose at the end of the study was slightly lower in the acitretin group when compared to the etretinate group (30.7 mg/day and 33.4 mg/day, respectively). Follow-up examinations were carried out every 2 weeks, and the efficacy of treatment was evaluated by using the PASI score. Percentage improvement in the PASI score was 50% at week 10 in both groups, and the difference between them at week 12 was insignificant. Both quantitatively and qualitatively, acitretin and etretinate do not significantly differ.

Acitretin↗
PubMed1992

Use of direct injection precolumn techniques for the high-performance liquid chromatographic determination of the retinoids acitretin and 13-cis-acitretin in plasma.

A previously developed highly sensitive high-performance liquid chromatographic method for the determination of retinoids, using direct injection of large plasma volumes, on-line solid-phase extraction and ultraviolet detection, was improved and fully validated for the determination of acitretin and 13-cis-acitretin in plasma samples. The addition of acetonitrile to improve the recovery was performed on-line by a T-piece, avoiding any cis-trans isomerization which could occur when acetonitrile was added prior to storage in the autosampler. About 30 injections could be made onto one precolumn despite the large injection volume (1 ml of plasma containing the internal standard). Full automation was attained by the use of automated precolumn replacement. In addition, forward- and back-flush purging of the precolumn enhanced the longevity of the analytical column. This consisted of three coupled C18 columns of 125 mm length each. The quantification limit was 0.3 ng/ml, using ultraviolet detection at 360 nm, and the mean inter-assay precision was 3.8% for the two compounds.

Acitretin↗
PubMed1988

Quantitative analysis of retinoids in biological fluids by high-performance liquid chromatography using column switching. II. Simultaneous determination of etretinate, acitretin and 13-cis-acitretin in plasma.

An automated gradient high-performance liquid chromatographic method for the determination of etretinate, acitretin and 13-cis-acitretin in plasma was developed, using a column-switching technique. After protein precipitation with ethanol, 0.5 ml of the supernatant was injected onto a precolumn (17 mm x 4.6 mm I.D.), filled with 37-53 microns C18 Corasil. Polar plasma components were washed out using 1% ammonium acetate and 1% acetic acid-acetonitrile (8:2, v/v); the retained retinoids were then transferred to the analytical column (125 mm x 4 mm I.D., filled with 5-microns ODS material) in the backflush mode, separated by gradient elution and detected at 360 nm by UV detection. The limit of quantification was 2 ng/ml and the inter-assay precision in the concentration range 20-1000 ng/ml was between 0.9 and 4.0% for all three compounds. To optimize the recovery for etretinate (greater than 60%), protein was precipitated from plasma with ethanol before injection, instead of direct injection of plasma samples, and a mobile phase containing 20% acetonitrile, instead of pure water or buffer, was used.

Acitretin↗
PubMed1990

[Pharmacokinetics of etretinate, acitretin and 13-cis-acitretin: new results and advantages of blood level oriented clinical use].

Plasma concentrations of etretinate (E), acitretin (A) and 13-cis-acitretin (13-cis A) were measured using a reverse phase HPLC assay in patients with psoriasis during 24h after the first dose (0.8 mg/kg) and after 3 weeks (group A), and in a second group with various skin diseases (B) under long-term treatment after 3 months. Group A (n = 8) showed median peak plasma concentration levels (Cmax) 578 ng/ml for E. and 161 ng/ml for A 4h after dosing (tmax). The plasma concentration profile of 13-cis A. was plateau-like with Cmax-levels of 138 ng/ml after 4 to 10 hours. In group B treated with 0.3 to 0.4 mg/kg etretinate a trend to increased Cmax-values with 123 ng/ml for E., 44 ng/ml for A. and, more pronounced, 210 ng/ml for 13-cis A. occurred (steady state). In a third group C (n = 17) it was found that after an eight month treatment free period measurements of the 13-cis A. plasma concentration are more sensitive than that of E. or A. Comparing the pharmacokinetics in two patients with the same clinical conditions under E. and A., resp., two fold higher Cmax-values of A. after A. were found than for A. after E. However, 13-cis A. values were higher after E. than after A. Our observations have shown that the metabolisation of A. to 13-cis A. may be disturbed and the clinical efficacy may appear only after dramatic increase of the oral doses. Routine monitoring of plasma concentration profiles of oral retinoids and their metabolites under short or long-term treatment enable us to early identify and understand better the so-called "non-responders", either due to a disturbed metabolism of retinoids or to non-compliance. Furthermore, monitoring of 13-cis A in plasma after cessation of treatment with E. or A. in women in childbearing age seems to be more sensitive than measurement of plasma levels of E. or A. These measurements are helpful for defining the strategy of oral retinoid therapy and for reliable information of females who wish to become pregnant after interrupting the drug.

Acitretin↗
PubMed1996

Response of the clinically uninvolved skin of psoriatic patients to tape stripping during acitretin treatment.

The aromatic retinoids etretinate and acitretin are widely used in the systemic treatment of severe psoriasis. The purpose of the present investigation was to further elucidate the mode of action of acitretin on abnormal keratinization and epidermal hyperproliferation in an in vivo model. Studies on the interference of acitretin with epidermal hyperproliferation and abnormal keratinization in psoriatic plaques are difficult to interpret, as acitretin-induced changes might be due to direct effects of acitretin or be the indirect effect of retinoid-induced modulation of cutaneous inflammation. Using an immunohistochemical assessment, we examined the in vivo effect of systemic acitretin ( > 35 mg daily) on the expression of filaggrin, involucrin, and on the recruitment of cycling epidermal cells, in the tape-stripped uninvolved skin of psoriatic patients, a model which provides the opportunity to study epidermal regeneration in the absence of significant accumulation of T-lymphocytes. During acitretin therapy and 3 weeks after withdrawal of acitretin, we took biopsies from uninvolved skin following tape-stripping in 6 patients with psoriasis. Six patients with psoriasis who had never used acitretin served as controls. We did not observe a Koebner response in our patients after tape stripping. Filaggrin expression was decreased, while the recruitment of cycling epidermal cells and the involucrin expression were increased in the biopsies taken from patients who did not use acitretin. During acitretin treatment, however, the filaggrin expression was similar, whereas the Ki-67 positive nuclei and the involucrin expression showed a statistically significant decrease compared to those parameters in the patients who did not use acitretin. Our findings indicate that epidermal hyperproliferation and abnormal keratinization are modulated directly by acitretin.

Acitretin↗
PubMed1988

Acitretin versus etretinate in psoriasis. Clinical and pharmacokinetic results of a German multicenter study.

175 patients with severe psoriasis of different types were treated with 10, 25, or 50 mg acitretin and compared with patients receiving 50 mg etretinate over a period of 8 weeks in a randomized, double-blind multicenter study in the Federal Republic of Germany. Plasma concentrations of etretinate and its metabolite acitretin were measured during therapy and also 3 weeks after cessation of treatment. After 4 weeks of treatment, a trend toward clinical improvement was shown in all groups with increasing dosage. Those groups receiving the lower acitretin doses (i.e., 10 and 25 mg/day) had more dropouts than the groups taking 50 mg acitretin or 50 mg etretinate. Complete remissions before the end of therapy occurred only among those receiving higher doses. Enlargement of psoriatic lesions, however, could be observed during treatment with both retinoids, despite improvement of other parameters, as measured by psoriasis area and severity index (PASI) and psoriasis severity index (PSI). After 8 weeks, a significant improvement was calculated by the PASI score and by a newly defined, corrected PASI score for all four dose regimens compared with baseline levels. A greater than 50% PSI score improvement was seen in 50% of patients treated with 10 mg acitretin, 40.5% with 25 mg acitretin, 53.8% with 50 mg acitretin, and 61.1% with 50 mg etretinate. No statistical differences were found among these groups at any time during the 8-week period. No new or unexpected side effects occurred during acitretin treatment. Moreover, cholesterol levels did not significantly change. Three weeks after cessation of drug administration, the plasma concentrations of acitretin were below the sensitivity level of the assay, whereas etretinate was still quantifiable. It is interesting that acitretin plasma concentrations during therapy with 50 mg acitretin were markedly lower (means = 18 ng/ml) than were acitretin levels during treatment with 50 mg etretinate (means = 36 ng/ml).

Acitretin↗
PubMed2000

Acitretin is converted to etretinate only during concomitant alcohol intake.

BACKGROUND: Acitretin has replaced etretinate in the treatment of various disorders of keratinization due to a considerably shorter terminal half-life. Possible esterification of acitretin to etretinate in the presence of ethanol has been reported. OBJECTIVES: To determine the plasma concentrations of etretinate as a metabolite in patients with various disorders of keratinization after multiple acitretin dosing, and to assess the influence of alcohol consumption using a questionnaire. In addition, to study the influence of alcohol consumption on the risk of metabolic formation of etretinate. PATIENTS/METHODS: Eighty-six acitretin (Neotigason(R), Roche)-treated outpatients from three centres provided pre-dose (trough) samples for determining plasma concentrations of acitretin and its metabolites 13-cis-acitretin and etretinate. Patients received acitretin doses of between 0.1 and 1.3 mg kg-1 daily. The concentrations of etretinate, acitretin and 13-cis-acitretin were determined by reverse-phase high-performance liquid chromatography. RESULTS: Of the 86 patients, 30 had detectable plasma etretinate levels. No etretinate was found in 20 patients who reported that they never drank alcohol, while etretinate was found in all 16 patients with an average weekly alcohol consumption of > 200 g ethanol, corresponding to about 15 U (1 U equals half a pint of standard beer or a wine glass of non-fortified wine). Etretinate was detected in 14 of 50 patients with a moderate weekly alcohol intake of up to 200 g ethanol. A trend linking higher alcohol intake with both higher risk of etretinate formation and higher etretinate levels was observed. The study also revealed that the ethylesterification only relates to acitretin (13-trans-) and not to the main metabolite 13-cis-acitretin, although the latter compound showed higher plasma trough concentration levels at steady state. CONCLUSIONS: Owing to the teratogenic potential and possible side-effects of oral retinoids, fertile women especially should be informed about the importance of strict alcohol abstinence during treatment and for at least 2 months after stopping therapy. In case of non-compliance with alcohol abstinence a post-therapy contraceptive period of 2-3 years should be recommended.

Acitretin↗
PubMed2006

Influence of the retinoid acitretin on erythrocyte microrheology in vitro.

OBJECTIVE: To determine in vitro changes in the microrheology of red blood cells (RBCs) treated with acitretin (Ro 10-1670). VOLUNTEERS AND METHODS: Venous blood samples were obtained from 27 healthy donors. Washed erythrocytes (5 x 10(6) cells/ml) were incubated for 30 min at 37 degrees C in solutions of low (25 ng/ml) and high (400 ng/ml) acitretin concentration. The whole red cell deformability was measured using osmotic gradient ektacytometry. To assess the contribution of factors influencing changes in red cell deformability, the biophysical state of the phospholipid bilayer was determined using the cation osmotic hemolysis technique (COH) and the internal viscosity using electron paramagnetic resonance (EPR) spectroscopy. RESULTS: Osmotic deformability studies revealed that cells treated with acitretin at low concentration deformed almost normally in isotonic medium, but RBCs incubated with high acitretin concentration showed distinct loss of deformation. However, in hypotonic medium, cell deformability was reduced to abnormally low values and this change was most marked with high acitretin concentration. CHO measurements showed that incubation of red cells at low acitretin concentration caused a significant increase in hemolysis at ionic strengths from 123.2 - 154.0 mmol/1 NaCl in relation to the control (p < 0.001). A high concentration of acitretin caused a significant increase in COH with high ionic strengths in the range 107.8 - 154.0 mmol/l NaCl (p < 0.001) and at low ionic strengths in the range 15.4 mmol/l NaCl (p < 0.05). The measurement of RBC intracellular microviscosity showed no statistically significant differences between control (6.22+/-0.22 cP) and acitretin-treated (6.29+/-0.25 cP) cells. CONCLUSION: The data show that acitretin, even at low concentration, is capable of inducing the reduction of red cell deformability. A reduced tendency of acitretin-treated RBCs to deform might result from the ability of acitretin to perturb the cell shape and membrane viscoelastic properties.

Acitretin↗
PubMed1998

N-linked glycoside and glucuronide conjugates of the retinoid, acitretin, are biologically active in cornea and conjunctiva.

The purpose of this study was to test two water-soluble, synthetic retinoids, glucoseamido acitretin and glucuronamido acitretin, for biological activity in cells of the cornea and conjunctiva. Vitamin A-deficient, xerophthalmic rats were treated topically with these retinoids, and corneas were examined histologically for effects on epithelial keratinization. The effect of these retinoids on the proliferation of rabbit conjunctival fibroblasts in culture was also investigated. Glucoseamido acitretin treatment restored a normal cornea after eight to nine days of treatment, while no improvement was observed in the vehicle-treated corneas. Likewise, glucuronamido acitretin application restored a normal corneal surface and reversed keratinization after eight to ten days of treatment. These retinoids caused no irritation of the eye or ocular adnexa. In culture, exposure of conjunctival fibroblasts to glucoseamide acitretin inhibited cell proliferation. Cultures exposed to glucoseamido acitretin at 10(-8) M or 10(-6) M had cell densities 77.3% and 51.9% of control, respectively, after seven days. Glucuronamido acitretin also inhibited cell proliferation. Cultures exposed to glucuronamido acitretin at 10(-8) M had a cell density of 69.2% of control at day seven, while at 10(-6) M this retinoid completely inhibited cell proliferation. These results show that glucoseamide acitretin and glucuronamido acitretin are biologically active in the cornea and conjunctiva, and may be considered for ophthalmic use in diseases involving abnormalities of ocular surface cell differentiation or hyperproliferation of fibroblasts.

Acitretin↗