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Oud 11 juli 2009, 16:43   #1
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flutamide gel

Flutagel is an innovative novelty on the world market. It is a gel which contains 1% Flutamide.
Flutamide (3`-trifluoromethyl-4`-nitromethyl propionylanilide) is a nonsteroidal pure antiandrogen.

It acts by inhibiting the uptake and/or binding of dihydrotestosterone (DHT) to the target cell receptor, thus interfering with androgen action [1].

This drug, produced by Schering-Plough, was introduced as a new potent compound for treatment of prostatic carcinoma (Martindale, 1993).

Flutamide is well absorbed orally and extensively metabolized; its active metabolite, 2-hydroxyflutamide, is formed rapidly and excreted almost entirely by the kidneys.

The systemic administration of flutamide causes several unwanted side effects, such as mild diarrhea, gynecomastia, reducing libido and impairing spermatogenesis in men and feminizing male fetuses in pregnant women. Topical administration, therefore, is an important goal for such a drug, especially if indicated for skin disorders. Here, we want to point out that our product is only for men. Women aren`t allowed to use our product. The motivation for us to formulate this gel stems mainly from an article of Sintov et al. [2] and we also choose nearly the same formulation for our gel as he authors used in their work. Sintov et al. transplanted human scalp skin grafts from balding donors onto SCID mice (SCID=Severe combined immune deficient). They treated the balding transplanted hair follicles with a topical 1% flutamide gel in order to re-enlarge the miniaturized hair follicles.

Here are some quotes from the article of Sintov et al. [2] :

“Testosterone metabolites exert a significant hormonal influence on hair growth by interacting with receptors at the follicular papilla.
It has long been known that an increased susceptibility of scalp follicles to these androgens is the main cause of androgenetic alopecia (or male-pattern baldness) in genetically predisposed individuals (Imperato-McGinley et al., 1974; Ebling et al., 1991).

In this type of alopecia, scalp follicles exhibit increased levels and activity of scalp 5a-reductase isoenzyme, which converts testosterone (T) to dihydrotestosterone (DHT) (Bingham and Shaw, 1973; Schweikert and Wilson, 1974). Taken together, increased conversion of T to DHT and increased DHT binding capacity in bald scalp as compared to hairy scalp (Sawaya et al., 1989) provide a mechanistic explanation for androgenetic alopecia. DHT shortens the hair cycle and progressively miniaturizes scalp follicles. The miniaturized follicles all remain present and thus the possibility of reversal by re-enlargement exists.

It is reasonable, therefore, to suppose that by administration of 5a-reductase inhibitors andr non-steroidal antiandrogens, this reversal should occur.”

“Chen et al. (1995) showed that topical administration of finasteride (in ethanol:propylene glycol vehicle) caused local inhibition of androgen-controlled sebaceous gland growth in hamster flank organ and that had a similar action to that of the same doses of flutamide. To date, clinical studies have not been performed for testing the efficacy of topical flutamide in male-pattern baldness. It is likely that the success (i.e. effective with minimal systemic exposure) of this drug would be dependent on a well-designed vehicle that would increase skin accumulation and decrease percutaneous absorption.”

Their results were impressive :

“The two topical formulations, finasteride and flutamide gels, showed significantly greater efficacy (PB0.05) than the vehicle formulation in enlarging hair length and diameter as well as in increasing the number of hairs per graft. Fig. 1 presents the results after 60 days of graft treatment with the two antiandrogenic formulations and with the vehicle. For the grafts treated with flutamide and finasteride gels, the number of hairs were 1.22+-0.47 and 0.88+-0.95 hairs/0.5 mm2 graft, respectively, versus 0.35+-0.6 hairs/graft for the vehicle-treated graft. Hair lengths were 5.82+- 0.50 and 4.50+-0.32 mm for the flutamide and finasteride groups, respectively, compared to 2.83+-0.18 mm for the vehicle-treated grafts.

The diameter of the hair shafts for the two drug-treatment groups was approximately twice that for grafts treated with the vehicle alone. It should be noted that hair growth in the two treatment groups started as early as after 36 days post transplantation. It can been seen in Fig. 1 that the topical application of flutamide, representing the anti-androgenic mechanism of action, resulted in more hairs per graft and longer hair shafts than the topical finasteride (5a-reductase inhibition).

The difference was statistically significant (P<0.05). Histological examination of the grafts treated with finasteride and flutamide (Table 1) demonstrated relatively more hairs in the growth (anagen) phase than in regression (catagen) and rest(telogen) phases (see also photographs a–c of Fig. 4), with some superiority of the topical flutamide over finasteride. In the two drug groups, before the treatment and in the vehicle group most if not all the hairs were in the catagen and the telogen phases (100 and 85.5%, respectively) (Fig. 4, photograph d). These findings, as shown in Table 1, support the above-described clinical results for hair growth, as presented in Fig. 1. Table 2 presents the plasma monitoring of T and DHT.

The measurements show that there was no systemic effect that might change the androgenic balance as a consequence of the topical applications of either flutamide or finasteride.”

“According to the present study, the effective topical delivery of flutamide and finasteride for alopecia is thus feasible, giving similar (if not better) results to those obtained with oral finasteride, i.e. with no systemic side effects, as demonstrated by T/DHT monitoring. It should be noted that, although the reversal of the vellus to terminal hair can occur in both the human scalp-grafted mouse and in man, it is still difficult to predict the degree of efficacy of this treatment in clinical studies or to compare it with oral finasteride trials.”
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Oud 11 juli 2009, 17:25   #2
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wesley1982's schermafbeelding
Geregistreerd: 3 januari 2008
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Cool niet meer verkrijgbaar ?

de flutagel word toch niet meer gemaakt ?
omdat er toch kans is op aantasting van de lever enz...

als je topische flutamide wil gebruiken ga je de flutamide 2% moeten gebruiken van genhair...
minox 5% kirkland (10 en 15% geven geen extra boost)
- ru58841
- cb
- ahkcu
- redken scalp relief
- alpecin c1 cafeine
- dutasteride (avodart) 1x dag (01-02-08)
- kelp & visolie caps
- msm 5000mg / biotine / silicium
- 1x dag 5min elektrische acupunctuur
- 3x week laserhelm 200 diodes 900mw
- 2725 FUT transplantatie istanbul (25-01-08)
- stabiel + hergroei
- 3x fitnessen 1x zwemmen en joggen
- 2509 FUE prohair (06/07-04-2010)
op 5-08-2009 prp gedaan bij prohair

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Oud 12 juli 2009, 08:45   #3
Poster v/h Jaar 2008

kevin's schermafbeelding
Geregistreerd: 2 juni 2004
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Wordt niet meer gemaakt nee.
Experimentele aanpak:
-Topicals: nieuwste HW topical.
-Supplementen: gezondheidsblog o.a ter ondersteuning van haarverlies.
micellarin green shampoo.

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