Skip to main content

The metabolism and pharmacokinetics of isotretinoin in patients with acne and rosacea are not influenced by ethanol.

Br J Dermatol. 2009 May 21; Grønhøj Larsen F, Jakobsen P, Grønhøj Larsen C, Heidenheim M, Held E, Nielsen-Kudsk FSummary Background Isotretinoin is effective in the treatment of severe acne and rosacea. Both parent drug and its main metabolite 4-oxo-isotretinoin are potentially teratogenic compounds and contain a carboxylic acid moiety. In the presence of ethanol, naturally occurring as well as synthetic retinoids also containing a carboxylic acid moiety are capable of undergoing an ethyl esterification with the metabolic formation of more lipophilic compounds with a much longer terminal half-life. Objectives To determine if isotretinoin (13-cis-RA), its main metabolite 4-oxo-isotretinoin (4-oxo-13-cis-RA), and other possible metabolites in the presence or absence of ethanol are converted to their corresponding ethyl derivatives in patients with severe acne or rosacea after multiple isotretinoin dosing. In addition, pharmacokinetic parameters of the parent drug and its 4-oxo metabolite were determined. Patients/methods Eleven patients with severe acne or rosacea were treated with isotretinoin daily for 3 months and investigated pharmacokinetically during 24 h after 1 month of treatment and for up to 28 days after discontinuation of therapy. A possible influence of ethanol was evaluated using a simple self-administered questionnaire and by measuring serum ethanol levels during treatment. The concentrations of isotretinoin, 4-oxo-isotretinoin and possible ethylated and nonethylated metabolites were measured by reverse-phase high-performance liquid chromatography. Results Although seven of 11 patients had a considerable weekly alcohol intake, no endogenous synthesis of ethyl derivatives of isotretinoin, the main 4-oxo metabolite or the all-trans compounds was chromatographically detectable in any of the patients' plasma samples during the treatment period. Multiple dose pharmacokinetic data for the parent drug and its main metabolite were comparable to previous studies. Conclusions The metabolism and pharmacokinetics of isotretinoin and its main metabolites are not influenced by ethanol during long-term isotretinoin treatment. After ceasing long-term isotretinoin therapy the recommended period of 1 month for using anticonceptive measures in fertile women seems adequate.

Popular posts from this blog

Before And After: A Gorgeous Zen Bathroom Remodel

Before And After: A Gorgeous Zen Bathroom Remodel " casacullen.com/2009/12/rwd-home-kitchen-redesign-before-and-after almost the same issue during my recent 1960s bath remodel, I house in prime vintage condition and wants to zen " We love when sustainability meets beauty in home renovations. And this Japanese-inspired bathroom remodel in by Weston Miles Architects is a prime example. These before photos show a pleasant enough bathroom with bright color and functional traditional cabinetry, though a small sink space, not-so eco-friendly materials, and dim lighting. This after photo shows an incredible remodel that makes use of traditional materials in a modern aesthetic. The focal point is this Japanese soaking tub that the client wanted, and the room grew around that. The room has been opened up for a step-in shower next to the tub, its warm lichen-green balanced against the natural wood of the tub and wood trim. This beautiful remodel exemplifie...
Read more

Prevalence Of And Associated Factors For Dry Eye In A Spanish adult population

To estimate the prevalence of dry eye and to investigate its relationship with lifestyle and systemic factors in a general adult population in north-western Spain. METHODS: A dry eye questionnaire was administered and objective tests were performed in 654 individuals [mean age (Standard deviation): 63.6 (14.4) years, range: 40-96, 37.2% males]. Subjects were considered symptomatic when one or more of the symptoms of the questionnaire were present often or all the time. Schirmer test or= 3 and fluorescein staining >or= 1 were considered indicative of signs. Dry eye was defined as the simultaneous presence of symptoms and at least one sign. A design based analysis was performed and all calculations were weighted to give unbiased estimates. RESULTS: Dry eye prevalence was 11.0% (95%confidence interval [CI] 8.6-13.3). Dry eye was found to be more frequent in women (11.9%, 95%CI 8.8-15.1) than in men (9.0%, 95%CI 5.3-12.6), and was significantly associated with aging (p autoimmune diseas...
Read more

Enhanced Skin Blood Flow And Sensitivity to Noxious Heat Stimuliin papulopustular rosacea

Although patients with rosacea often complain of increased skin sensitivity, there has been no quantitative sensory testing of this phenomenon. Furthermore, cutaneous blood flow in these patients has not been assessed using state-of-the-art laser Doppler imaging (LDI). OBJECTIVES: To assess heat pain thresholds and skin blood flow using quantitative thermal sensory testing and LDI in patients with untreated rosacea . METHODS: Of the total 24 subjects enrolled, 8 had papulopustular rosacea (PPR), 8 had erythematotelangiectatic rosacea (ETR) and 8 were control subjects. Subjective burning perception, heat pain threshold, skin blood flow, and skin temperature was assessed in all subjects. In the ETR and PPR groups, two areas were compared: affected and nonaffected. RESULTS: Heat pain thresholds of areas affected by rosacea were lower than those of nonaffected areas. In addition, subjective burning perception was increased in rosacea patients when compared with control subjects. Altho...
Read more