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REVISTA DERMATOLÓGICA NOVIEMBRE 2003-2024, PIMECROLIMUS
(ELIDEL)
En este bloque de noticias destaca la CREMA PIMECROLIMUS (1.2.3.), lanzada al mercado por el laboratorio NOVARTIS en el año 2002, con el nombre de ELIDEL crema al 1%, para ser utilizada fundamentalmente en la DERMATITIS ATÓPICA leve a moderada, como medicamento de SEGUNDA LÍNEA.
El PIMECROLIMUS es un inhibidor de la CALCINEURINA (ICT) y es un derivado de la ASCOMICINA, sustancia que proviene de la bacteria STREPTOMYCES HYGROSCOPICUS.
Posteriormente comenzó a utilizarse en otros eccemas como la PSORIASIS (1), la DERMATITIS CRÓNICA de las manos (2), y DERMATITIS SEBORREICA (3. ).
Pocos años después comenzaron a reportarse casos de LINFOMA y CÁNCER DE PIEL con el uso de esta crema, y LA FDA en el año 2006, obligó al LABORATORIO A COLOCAR en el empaque una "ADVERTENCIA CAJA NEGRA O BLACK BOX", con las ADVERTENCIAS del uso de este medicamento y su "POSIBLE ASOCIACIÓN CON CÁNCER" al ser utilizada.
Se prohibió su uso en niños menores de 2 años, en pacientes adultos inmunocomprometidos, niños con problemas de inmunidad, y pacientes que estén utilizando inmunosupresores, tanto niños como adultos.
Para los QUE NO SABEN QUE ES LO QUE ES UNA CAJA NEGRA O BLACK BOX, es una etiqueta que se le coloca al empaque de la medicina con los riesgos que conlleva el uso de ese medicamento en particular.
EXISTE otra crema también utilizada para DERMATITIS ATÓPICA y OTROS ECCEMAS, lanzada al mercado el mismo año 2001-2002, denominada TACROLIMUS, con el nombre de PROTOPIC ungüento al 0.1%, del laboratorio LEO pharma, a la cual se le comprobó los mismos efectos adversos que el PIMECROLIMUS, riesgo de CÁNCER DE PIEL y LINFOMA. Ambas cremas son inhibidoras de la CALCINEURINA, y están asociadas a un mayor riesgo de cáncer al ser utilizadas tópicamente.
Este evento ocurre porque los inhibidores de la CALCINEURINA disminuyen la producción y actividad de las células T, por una inhibicion de la interleuquina-2 (IL-2), lo qué provoca una disminución de la vigilancia inmunologica.
Aqui te dejo el enlace: EL TACROLIMUS.
El PIMECROLIMUS (ELIDEL), hoy 2024 no está disponible en venezuela. EL TACROLIMUS está en venezuela bajo el nombre de CROMUS crema al 0.1%. y se relanzó al mercado en el año 2024.
Es de notar que ambas cremas TIENEN MÁS DE 20 AÑOS EN EL MERCADO, no son NUEVAS, ni grandes innovaciones !!!.
Los otros temas de esta publicación incluyen: TADALAFIL (4,5), SILDENAFIL (6,7), VARDENAFIL (8,9) y VITILIGO (10).
Saludos,,,
Dr. José Lapenta.
ENGLISH
This news block highlights PIMECROLIMUS CREAM (1.2.3.), launched on the market by the NOVARTIS laboratory in 2002, under the name ELIDEL 1% cream, to be used primarily in mild to moderate ATOPIC DERMATITIS, as a SECOND LINE medication.
PIMECROLIMUS is a CALCINEURIN inhibitor and is a derivative of ASCOMYCIN, a substance that comes from the STREPTOMYCES HYGROSCOPICUS bacteria.
Later it began to be used in other eczemas such as PSORIASIS (1), CHRONIC DERMATITIS of the hands (2), and SEBORRHEIC DERMATITIS (3).
A few years later, cases of LYMPHOMA and SKIN CANCER began to be reported with the use of this cream, and the FDA forced (in year 2006) the LABORATORY TO PLACE a "WARNING BLACK BOX" on the packaging, with WARNINGS about the use of this medicine and its "POSSIBLE ASSOCIATION WITH CANCER" when used.
Its use was prohibited in children under 2 years of age, in immunocompromised adult patients, children with immune problems, and patients who are using immunosuppressants, both children and adults.
For those WHO DO NOT KNOW WHAT A BLACK BOX IS, it is a label that is placed on the medicine packaging with the risks involved in the use of that particular medicine.
There is another cream also used for ATOPIC DERMATITIS and OTHER ECZEMAS, launched on the market in the same year 2001-2002, called TACROLIMUS, with the name of PROTOPIC ointment at 0.1%, from the LEO pharma laboratory, which was found to have the same adverse effects as PIMECROLIMUS, risk of SKIN CANCER and LYMPHOMA. Both creams are CALCINEURIN inhibitors, and are associated with an increased risk of cancer when used topically.
This event occurs because CALCINEURIN inhibitors decrease the production and activity of T cells, by an inhibition of the interleukin-2 (IL-2) which causes a decrease in immune surveillance.
Here is the link: TACROLIMUS.
PIMECROLIMUS (ELIDEL), today 2024 is not available in Venezuela. TACROLIMUS is in Venezuela under the name of CROMUS cream at 0.1%. and It was relaunched in the year 2024.
It should be noted that both creams HAVE BEEN ON THE MARKET FOR MORE THAN 20 YEARS, they are not NEW, nor great innovations !!!.
Other topics in this post include: TADALAFIL (4,5), SILDENAFIL (6,7), VARDENAFIL (8,9) and VITILIGO (10).
Greetings,,,
Dr. José Lapenta.
PSORIASIS, PIMECROLIMUS (ELIDEL), TADALAFIL (CIALIS), SILDENAFIL (VIAGRA), VARDENAFIL (LEVITRA), VITILIGO.
3.) Topical pimecrolimus in the treatment of seborrheic dermatitis.
4.) Review of tadalafil in the treatment of erectile dysfunction.
5.) Tadalafil, a further innovation in the treatment of sexual dysfunction.
6.) Acute electroretinography changes during sildenafil (Viagra) treatment for erectile dysfunction.
8.) Vardenafil: a review of its use in erectile dysfunction.
10.) [Clinical observation on treatment of vitiligo with xiaobai mixture].
1.) An experimental ointment formulation of pimecrolimus is effective in psoriasis without occlusion. (ELIDEL)
Acta Derm Venereol. 2003;83(5):351-3.
Mrowietz U, Wustlich S, Hoexter G, Graeber M, Brautigam M, Luger
T.
Department of Dermatology, University of Schleswig-Holstein,
Campus Kiel, Germany. umrowietz@dermatology.uni-kiel.de
Pimecrolimus (Elidel, SDZ ASM 981), a new macrolactam ascomycin
derivative, was highly effective in treating plaque-type psoriasis
when applied under Finn-chamber occlusion. A two-centre,
randomized, double-blind, vehicle- and positive-controlled
within-patient study was therefore conducted in 23 adult psoriasis
patients. Pimecrolimus 1% was applied, twice daily, in an
experimental ointment formulation, along with the corresponding
vehicle, 0.005% calcipotriol ointment and 0.05%
clobetasol-17-propionate ointment to test sites without occlusion
for 21 days. Erythema, induration and scaling (score: 0 [absent]
to 4 [severe]) were evaluated. The total sign score was defined as
the sum of the erythema, induration and scaling scores (range
0-12). Pimecrolimus 1% ointment was significantly (p = 0.03) more
effective than the corresponding vehicle, with an improvement in
total sign score of 51.4% compared with 36.7% for the
corresponding vehicle. Improvements with calcipotriol and
clobetasol-17-propionate were 71.5% and 88.3%, respectively. No
local or systemic drug-related side effects were observed in the
study. We conclude that pimecrolimus 1% in the experimental
ointment formulation was significantly more effective than its
corresponding vehicle, but less effective than calcipotriol and
clobetasol ointment. This is the first study reporting a
significant therapeutic effect of pimecrolimus in an ointment
formulation applied without occlusion to psoriatic plaques.
2.) Occlusive treatment of chronic hand dermatitis with
pimecrolimus cream 1% results in low systemic exposure, is
well tolerated, safe, and effective. An open study.
(ELIDEL)
Dermatology. 2003;207(1):37-42.
Thaci D, Steinmeyer K, Ebelin ME, Scott G, Kaufmann R.
Department of Dermatology and Venereology, J.-W. Goethe University School of Medicine, Frankfurt, Germany. thaci@em.uni-frankfurt.de
BACKGROUND: Pimecrolimus cream 1% (Elidel, SDZ ASM 981) is a novel, non-steroid inflammatory cytokine inhibitor, effective in the treatment of atopic dermatitis. Here, we evaluate the treatment of chronic hand dermatitis with pimecrolimus cream 1%. OBJECTIVES: To determine pimecrolimus blood concentrations, and evaluate the safety, tolerability and efficacy following application of pimecrolimus cream 1% to subjects with chronic hand dermatitis. METHOD: In this open-label, multiple-topical-dose, non-controlled, pharmacokinetic study, pimecrolimus cream 1% was applied twice daily to dorsal and palmar areas (affected and unaffected) of both hands. Evening applications (except day 8) were immediately followed by overnight occlusion (> or =6 h). Full pharmacokinetic profile (days 1, 8 and 22), trough concentrations (days 3 and 15), physical examinations, laboratory measurements and adverse events were recorded. Efficacy was assessed via Investigators' Global Assessment (IGA), total key signs and symptoms and the subject's overall self-assessment. RESULTS: Twelve patients completed the study. The majority of pimecrolimus blood concentrations (73.6%) remained below the limit of quantitation (0.1 ng/ml). The maximum concentration observed was 0.91 ng/ml and the maximum area under the concentration-time curve from 0-12 h post dose was 7.6 ng.h/ml. Treatment was well tolerated locally and systemically. No serious adverse events occurred; 4/13 subjects showed a total of 6 adverse events at the application site: burning (n=4), and pruritus (n=2). No clinically relevant or drug-related changes were observed. Clear efficacy of the treatment was shown by all 3 assessment methods. Disease state at day 22 had improved in 11 (85%) subjects compared with baseline (IGA). CONCLUSION: Twice daily topical treatment of moderate to severe chronic hand dermatitis with pimecrolimus cream 1% results in low pimecrolimus blood levels, is well tolerated, safe, and effective. Copyright 2003 S. Karger AG, Basel
3.) Topical pimecrolimus in the treatment of seborrheic
dermatitis.(ELIDEL)
Dermatol Online J. 2003 Aug;9(3):13.
Brownell I, Quan LT, Hsu S.
Department of Dermatology, Baylor College of Medicine, Houston, TX, USA.
Seborrheic dermatitis is a chronic inflammatory disease that mainly affects seborrheic areas of skin. An inflammatory response to the yeast Pityrosporum ovale has been thought to be important in the etiology of the condition. Therefore, topical antifungals and corticosteroids have been the mainstay of treatment. The recent development of topical macrolactam immunomodulators has offered a useful, safe alternative to corticosteroids in the treatment of various inflammatory skin disorders. We report successful treatment of seborrheic dermatitis with pimecrolimus.
4.) Review of tadalafil in the treatment of erectile
dysfunction.(CIALIS)
Expert Opin Pharmacother. 2003 Nov;4(11):2049-56.
Meuleman EJ.
University Medical Center St Radboud, Department of Urology, PO Box 9101, 6500 HB Nijmegen, The Netherlands. e.meuleman@uro.umcn.nl
Approximately 150 million men worldwide experience erectile dysfunction (ED) whereby they are unable to achieve and maintain an erection adequate for satisfactory sexual performance. ED has a considerable impact on quality of life. Tadalafil (Cialis( trade mark ), Eli Lilly & Co./ICOS) is a novel effective and safe phosphodiesterase type 5 inhibitor, a secondary messenger for the smooth muscle relaxing effects of nitric oxide, which plays a central role in the vasodilation of erectile tissues. It has a longer half-life than sildenafil. As head-to-head comparative trials are lacking, it is not clear what tadalafil offers over sildenafil. In terms of marketing, much is made of the 'spontaneity' achievable because of the (relatively) longer half-life of tadalafil.
5.) Tadalafil, a further innovation in the treatment of sexual dysfunction. (CIALIS)
Drugs Today (Barc). 2003 Feb;39(2):103-13.
Pomerol JM, Rabasseda X.
Fundacion Puigvert, Barcelona, Spain.
In recognition of the large number of sufferers of sexual dysfunction worldwide, and the variety of etiologies of the condition, investigation into effective pharmacological agents has been expanded. One method of intervention is inhibition of the phosphodiesterase type 5 (PDE5) enzyme, which has already been exploited with a considerable degree--though not complete--success. A number of new agents that inhibit PDE5 are under development. Notable among these is tadalafil, which has demonstrated a high level of selectivity for PDE5 over the other phosphodiesterases and has shown efficacy in improving erectile function and sexual satisfaction in phase III trials. Throughout the clinical development program for tadalafil, the drug has been well tolerated and without serious side effects. The manufacturer, Lilly ICOS, received an approvable letter from the US Food and Drug Administration for use of the drug as a treatment for erectile dysfunction on April 30, 2002. Lilly ICOS hopes to market tadalafil, with the trade name Cialis, in the USA in 2003. Copyright 2003 Prous Science. All rights reserved.
6.) Acute electroretinography changes during sildenafil
(Viagra) treatment for erectile dysfunction.
Doc Ophthalmol. 2003 Sep;107(2):111-4.
Balacco Gabrieli C, Regine F, Vingolo EM, Rispoli E, Isidori A.
Department of Ophthalmology, University of Rome La Sapienza, Rome, Italy. corrado.balacco@uniroma1.it
The authors describe their findings on 12 subjects who were treated with 50 mg of sildenafil (Viagra) and underwent ERG measurements prior to and 1 hour after ingestion. The Naka-Rushton equation was used to describe the b-wave luminance-response function of the scotopic ERG. Statistically significant differences were noted in the Vmax and K values. Sildenafil ingestion resulted in an increase in Vmax (higher rod response to light stimuli) and a decrease in K (higher sensitivity).
7.) Sexual psychophysiology and effects of sildenafil citrate
in oestrogenised women with acquired genital arousal disorder
and impaired orgasm: a randomised controlled trial.
(VIAGRA)
BJOG. 2003 Nov;110(11):1014-24.
Basson R, Brotto LA.
B.C. Center for Sexual Medicine, Vancouver Hospital, Canada.
OBJECTIVE: Some postmenopausal women lose genital sexual
responsivity despite preserved subjective sexual arousal from
non-genital stimuli. When oestrogen replacement is without
benefit, both the underlying pathophysiology and management of
this acquired genital female sexual arousal disorder are
unclear. We aimed to study the effect of sildenafil on sexual
arousal and orgasmic functioning of such women. Secondly, we
aimed to explore the concordance between a detailed historical
assessment of genital response in real life, with laboratory
vaginal photoplethysmographic assessment of genital
vasocongestion. DESIGN: Session one consisted of a
semi-structured clinical interview to assess real life sexual
arousal. Session two employed vaginal pulse amplitude and
self-report questionnaire assessment of erotica-induced sexual
arousal. Sessions three and four were a randomised,
double-blind, placebo-controlled crossover administration of
sildenafil on orgasm latency, intensity, perception of genital
congestion and subjective arousal to erotica plus clitoral
vibrostimulation. SETTING: University associated Sexual Medicine
Clinic and Psychophysiology Laboratory. SAMPLE: Volunteer sample
of 34 estrogenized postmenopausal women with acquired genital
female sexual arousal disorder and impaired orgasm. METHODS:
Sildenafil (50 mg) or placebo administered over two laboratory
sessions. MAIN OUTCOME MEASURES: Orgasm latency and intensity
during drug sessions; subjective and psychophysiological sexual
arousal during photoplethysmography session. RESULTS: The erotic
video significantly increased subjective sexual arousal in all
women. Vaginal pulse amplitude responses varied from robust to
absent. Although across all women, sildenafil improved neither
arousal nor orgasm, subsequent analyses comparing high versus
low vaginal pulse amplitude responders revealed significantly
reduced latency to orgasm, and increased subjective sexual
arousal and perception of genital arousal in the latter group of
women. CONCLUSION: The data suggest that estrogenized
postmenopausal women with genital female sexual arousal disorder
and orgasmic impairment based only on clinical assessment do not
benefit from sildenafil. However, the photoplethysmograph had
predictive value-those women showing low vaginal pulse amplitude
response benefited from sildenafil compared with women with a
higher response. Thus, estrogenized women diagnosed with
acquired genital female sexual arousal disorder may be a
heterogeneous group and the photoplethysmograph might be useful
in their further characterisation.
8.) Vardenafil: a review of its use in erectile dysfunction.
(LEVITRA)
Drugs. 2003;63(23):2673-703.
Keating GM, Scott LJ.
Adis International Limited, Auckland, New Zealand. demail@adis.co.nz
Vardenafil (Levitra) is a potent and highly selective oral phosphodiesterase type 5 (PDE5) inhibitor. Vardenafil improved erectile function in men with mild to severe erectile dysfunction (ED) of varying aetiology in two randomised, double-blind, multicentre, fixed-dose studies of 12 or 26 weeks' duration. Men receiving vardenafil 10 or 20 mg had significantly greater improvements in International Index of Erectile Function (IIEF) questionnaire erectile function domain scores than placebo recipients. Moreover, improvements in penetration and maintenance of erection (assessed using IIEF or Sexual Encounter Profile [SEP] questions) were significantly greater with vardenafil 5-20 mg than with placebo. Improvements in IIEF intercourse satisfaction and orgasmic function domain scores were significantly greater with vardenafil 10 or 20 mg than with placebo and the proportion of patients with a positive response to a Global Assessment Question (GAQ) concerning improvement in erections after 12 or 26 weeks' therapy was significantly higher with vardenafil 5-20 mg than with placebo. Vardenafil improved erectile function in men with ED associated with diabetes mellitus or ED following unilateral or bilateral nerve-sparing radical retropubic prostatectomy in two randomised, double-blind, multicentre, fixed-dose, 3-month studies. In both studies, improvements from baseline in the erectile function domain score of the IIEF and in positive responses to SEP questions were significantly greater with vardenafil 10 or 20 mg than with placebo. In addition, a significantly higher proportion of vardenafil 10 or 20 mg recipients than placebo recipients had positive GAQ responses. Vardenafil was generally well tolerated in men with ED; treatment-emergent adverse events were of mild to moderate intensity and transient in nature. The most commonly reported adverse events (typical of those seen with PDE5 inhibitors) in vardenafil 5-20 mg recipients included headache, flushing, rhinitis, dyspepsia and sinusitis. There were no reports of abnormal colour vision in men with ED taking vardenafil at clinically recommended doses (5-20 mg). CONCLUSION: Vardenafil is a potent and highly selective oral PDE5 inhibitor. It is effective and generally well tolerated in men with mild to severe ED of varying aetiology, as well as in men with ED associated with diabetes mellitus or ED after radical prostatectomy. Vardenafil should be considered a first-line treatment option in men with ED who are suitable candidates for oral PDE5 inhibitor therapy.
9.) Safety and efficacy of vardenafil for the treatment of men with erectile dysfunction after radical retropubic prostatectomy. (LEVITRA)
J Urol. 2003 Oct;170(4 Pt 1):1278-83.
Brock G, Nehra A, Lipshultz LI, Karlin GS, Gleave M, Seger M, Padma-Nathan H.
St. Joseph's Medical Center, Lawson Research Institute, London, Ontario, Canada. gebrock@sympatico.ca
PURPOSE: More than one-third of men may experience erectile dysfunction (ED) after nerve sparing radical retropubic prostatectomy. The efficacy and safety of vardenafil, a potent, selective, phosphodiesterase 5 inhibitor, was assessed for the treatment of ED after radical prostatectomy. MATERIALS AND METHODS: In this double-blind study 440 men with ED after nerve sparing radical prostatectomy were randomized to take placebo, or 10 or 20 mg vardenafil. Efficacy was measured after 12 weeks using the erectile function domain of the International Index of Erectile Function, diary questions measuring vaginal penetration and intercourse success rates, and a global assessment question (GAQ) on erection. RESULTS: Of the intent to treat population 70% had severe ED (erectile function less than 11) at baseline. After 12 weeks both vardenafil doses were significantly superior to placebo (p <0.0001) for all efficacy variables. Improved erections (based on GAQ) were reported by 65.2% and 59.4% of patients on 20 and 10 mg vardenafil, respectively, and by only 12.5% of patients on placebo (p <0.0001). Among men with bilateral neurovascular bundle sparing, positive GAQ responses were reported by 71.1% and 59.7% of patients on 20 and 10 mg vardenafil, respectively, versus 11.5% of those on placebo (p <0.0001). The average intercourse success rate per patient receiving 20 mg vardenafil was 74% in men with mild to moderate ED and 28% in men with severe ED, compared to 49% and 4% for placebo, respectively. Few adverse events were observed. They were generally mild to moderate headache, flushing and rhinitis. CONCLUSIONS: In men with severe ED after nerve sparing radical retropubic prostatectomy, vardenafil significantly improved key indices of erectile function.
10.) [Clinical observation on treatment of vitiligo with
xiaobai mixture]
Zhongguo Zhong Xi Yi Jie He Za Zhi. 2003 Aug;23(8):596-8.
[Article in Chinese]
Liu ZJ, Xiang YP.
Department of Dermatology, First Affiliated Hospital, Nanhua
University, Hunan 421001. liuzj71@sohu.com
OBJECTIVE: To observe the therapeutic effect of Xiaobai Mixture
(XBM) in treating vitiligo. METHODS: Seventy-four patients with
vitiligo were randomly divided into the XBM group treated with XBM
and the control group treated with 8-MOP. The therapeutic effect,
nail-fold microcirculation, plasma endothelin-1, serum
immunoglobulin were observed and compared. RESULTS: The
therapeutic effect of XBM was better than that of 8-MOP (P <
0.05). XBM could also obviously improve the nail-fold
microcirculation, elevate the plasma endothelin-1 level and lower
the serum IgG (P < 0.01). CONCLUSION: XBM has superiority in
treating vitiligo.
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DATA-MÉDICOS/ DERMAGIC JOURNAL/ NOVEMBER 2.003-2024/ DR. JOSE
LAPENTA R.
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Produced by Dr. José Lapenta R. Dermatologist
Venezuela
1.998-2.024
Producido por Dr. José Lapenta R. Dermatólogo Venezuela 1.998-2.0024
Tlf: 0414-2976087 - 04127766810
