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Old 06-09-2011, 05:58 PM   #1
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The effects of anti-e's and AI's on the axis and gyno!

The effects of anti-e's and AI's on the axis and gyno!
Old 16-Oct-2005, 09:04 PM #1
Big'r

Clomid
Clomid increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone (C1-C16, C21, C22).
Clomid response decreases significantly with aging (C1, C7, C11, C13).
Long term treatment with Clomid is effective in normalising a suppressed axis:
-4 months Clomid for 178 men with secondary hypogonadism significantly increases lh - leutenizing hormone - and free testosterone in all patients (C1).
-2 months Clomid for 17 men with secondary hypogonadism significantly elevates lh - leutenizing hormone - , FSH - follicle stimulating hormone - and free testosterone levels (C4).
-12 months 25 mg/day Clomid for 23 men with fertility problems increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone levels during the treatment (C8).
-3 months 50 mg/day Clomid for 5 oligozoospermic men causes a significant rise in serum testosterone (C15).
Short term Clomid treatment is effective in normalising a suppressed axis:
-5 days Clomid for 45 men significantly increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and serum testosterone (C2).
-1 week 100 mg/day Clomid for 42 men with kidney problems increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone levels in all subjects (C6).
-1 week Clomid for 21 men with erectile complaints increases gonadotropin and testosterone levels (C7).
-3 weeks 100 mg Clomid/day for 5 men increases lh - leutenizing hormone - + FSH - follicle stimulating hormone - 3-fold, and circulating testosterone 2-fold (C10).
-11 days 100 mg Clomid for 10 normozoospermatic, 29 oligozoospermatic and 11 azoospermatic men significantly increases FSH - follicle stimulating hormone - , lh - leutenizing hormone - and testosterone (also androstenedione and sex hormone binding globulin ) (C14).
Clomid stimulates the axis in small amounts:
-25 mg/day Clomid for 12 months in 23 men with fertility problems increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone levels during the treatment. Clomid treatment also results in greater lh - leutenizing hormone - , FSH - follicle stimulating hormone - and T responses to GnRH (C8, C8b).
-25 mg/day Clomid for 25 days in 30 men with idiopathic male infertility increases lh - leutenizing hormone - 1,90 x, FSH - follicle stimulating hormone - 1,81 x and testosterone 1,89 x (C9).
Clomid increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone above basal levels:
-5 days Clomid for 45 men significantly increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and serum testosterone (C2).
-1 week 100 mg/day Clomid for 9 healthy males increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone levels in all subjects (C6).
-8 weeks 100 mg Clomid for 10 normal men significantly increases testosterone and non-sex hormone-binding globulin bound testosterone (C11).
-Clomid increases lh - leutenizing hormone - and testosterone and increases pulse amplitude in normal men (C12).
-Clomid for 7 days in 55 healthy men increases mean serum total T and non-sex hormone binding globulin -bound levels in young men (22-35 yr) by 100% and 304%. In older men (65-84 yr) these values increased by only 32% and 8%. (C13).
Clomid increases estrogen levels
-25 mg/day Clomid for 12 months in 23 men with fertility problems increases estradiol levels during the treatment (C8).
-3 weeks 100 mg Clomid/day for 5 men increases circulating estradiol levels 2-fold (C10).
-50 mg/day Clomid for 1-3 months in 5 boys increases estradiol significantly (C21).
-100 mg/day Clomid in 22 boys increases estradiol levels during therapy (C22).
-100 mg/day Clomid for 10 days in 21 normospermic and 36 oligozoospermic men increases estradiol (+60.8%) vs. (+58.8%-118.9%). A similar reaction of estradiol was shown in the hcg stimulation (C31).
-8 weeks 100 mg Clomid for 10 normal men significantly increases estradiol (C11).
-Clomid does not differ estradiol in normal men (C12).
-11 days 100 mg Clomid for 10 normozoospermatic, 29 oligozoospermatic and 11 azoospermatic men significantly increases estradiol (C14).
-3 months 50 mg/day Clomid for 5 oligozoospermic men causes a significant rise in serum E2 (C15).
-100-200 mg Clomid for 4 weeks, or 100 mg for 8 weeks increases estradiol (C16).
Clomid decreases suppression of chemically reduced lh - leutenizing hormone - levels:
-(Cetrorelix blocks the effects of Gonadotropin Releasing Hormone (GnRH). GnRH controls the release lh - leutenizing hormone - .)
(40 patients) Clomid in combination with gonadotropins and 0.25 mg of Cetrorelix provides significantly higher lh - leutenizing hormone - concentrations than only gonadotropins and 0.25 mg of Cetrorelix (C3).
Combined Clomid and hcg administration:
-A single dose of (5000 i.u. i.m.) hcg was administrated before and after 3 months of 50 mg Clomid/day in 5 oligozoospermic men. Before the CC-treatment normal responses to hcg were seen (significantly elevated E2 levels at 1 day and T levels at 4 days). After CC, only the concentrations of 17-OHP4 rose significantly following hcg administration (C15).
Following Clomid administration a single dose of (5000 i.u. i.m.) hcg (C15).
Clomid not fit enough to treat gynecomastia. At least in small doses.
-12 boys with persistent gynecomastia used 50 mg Clomid for 1-3 months. Only 5 boys experienced a reduction of > 20% (C21).
-22 boys with gynecomastia used 100 mg Clomid/day. 14 (64%) responded within 6 months (C22).



C1) http://www.ncbi.nlm.nih.gov/entrez/q...801&query_hl=1
C2) http://www.ncbi.nlm.nih.gov/entrez/q...089&query_hl=1
C3) http://www.ncbi.nlm.nih.gov/entrez/q...125&query_hl=1
C4) http://www.ncbi.nlm.nih.gov/entrez/q...597&query_hl=1
C5) http://www.ncbi.nlm.nih.gov/entrez/q...694&query_hl=1
C6) http://www.ncbi.nlm.nih.gov/entrez/q...872&query_hl=1
C7) http://www.ncbi.nlm.nih.gov/entrez/q...138&query_hl=1
C8) http://www.ncbi.nlm.nih.gov/entrez/q...318&query_hl=1
C8b) http://www.ncbi.nlm.nih.gov/entrez/q...318&query_hl=1
C9) http://www.ncbi.nlm.nih.gov/entrez/q...618&query_hl=1
C10) http://jcem.endojournals.org/cgi/con...e2=tf_ipsecsha
C11) http://www.ncbi.nlm.nih.gov/entrez/q...692&query_hl=1
C12) http://www.ncbi.nlm.nih.gov/entrez/q...207&query_hl=1
C13) http://www.ncbi.nlm.nih.gov/entrez/q...649&query_hl=1
C14) http://www.ncbi.nlm.nih.gov/entrez/q...739&query_hl=1
C15) http://www.ncbi.nlm.nih.gov/entrez/q...381&query_hl=1
C16) http://www.ncbi.nlm.nih.gov/entrez/q...529&query_hl=1
C21) http://www.ncbi.nlm.nih.gov/entrez/q...910&query_hl=1
C22) http://www.ncbi.nlm.nih.gov/entrez/q...752&query_hl=1
C31) http://www.ncbi.nlm.nih.gov/entrez/q...734&query_hl=1



Nolvadex
The way Nolvadex works:
Nolvadex can activate neural timing mechanism(s) that govern the intermittent release of endogenous GnRH. 20 mg Nolvadex/day for 7 days in 6 normal men attenuates the ability of exogenous GnRH to increase the bio/immuno lh - leutenizing hormone - ratio further, which suggests the attainment of maximal enrichment in endogenous lh - leutenizing hormone - bioactivity in the presence of antiestrogen (N4).
Nolvadex increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone values (N1-N4, N24, N29)
Long term treatment with Nolvadex is effective in normalising a suppressed axis:
-6 months 20 mg Nolvadex/day for 220 men with oligozoospermia increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone (N1).
-5,5 months 5-20 mg Nolvadex/day for 12 men with oligozoospermia increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone (N3).
-2-4 months Nolvadex for 6 men increases lh - leutenizing hormone - levels significantly (N24).
-2-12 months Nolvadex for 8 boys increases testosterone. lh - leutenizing hormone - showed an increased response to lh - leutenizing hormone - -RH (N29).
Short term Nolvadex treatment is effective in normalising a suppressed axis:
-1 week 20 mg Nolvadex/day for 4 men causes a moderate increase in lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone (N2).
Nolvadex stimulates the axis in small amounts:
-5, 10 and 20 mg Nolvadex/day significantly increases basal testosterone levels and the responses of lh - leutenizing hormone - /FSH - follicle stimulating hormone - to LHRH infusion. Without significant differences between the lower (5-10 mg) or higher doses (20 mg) (N3).
Nolvadex increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone above basal levels:
-20 mg Nolvadex/day for 1 week increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone in 4 normal men (N2).
-40 mg Nolvadex/day for 10 days in 8 normal men increases basal bioactive lh - leutenizing hormone - concentrations from (42.7 +/- 6.9) to (97.6 +/- 19.4) mIU/ml. Total serum testosterone increases significantly (approx. 1.4-fold) (N4).
Nolvadex increases estrogen levels
-5,5 months Nolvadex for 12 men does not significantly influence estradiol levels or the E2 over testosterone ratio (N3).
-2-4 months Nolvadex for 6 men increases total estradiol levels significantly (N24).
-2-12 months Nolvadex for 8 boys increases estradiol (N29).
Nolvadex appears effective in treating gynecomastia. Raloxifene possibly is even more effective.
-(13 men with painful gynecomastia) 10 mg nolva/day for 3 months provided a good response in 10 patients (N21).
-(36 men) 20 mg nolva/day for 6-12 weeks resolved the mass in 30 patients (83,3%). Lump gynecomastia was more responsive than the fatty type (100% vs. 62.5%) (N22).
-(23 men) 20 mg nolva/day provided complete resolution of gynecomastia in 18 patients (78,2%). 400 mg danazol provided complete resolution in only 8 out of 20 patients (40%) (N23).
-(6 men with painful gynecomastia) nolva for 2-4 months provided only marginally significant size reduction (N24).
-(61 men with gynecomastia) 40 mg nolva/day for 2 months provided complete regression of breast swelling in 80% (N25).
-(38 boys with persistent gynecomastia) nolva for 3-9 months reduces breast nodule diameter 2,1 cm. For raloxifene this was 2,5 cm. nolva provided a significant decrease (<50%) in 41%, with raloxifene this was (86%) (N27).
-(10 boys with pubertal gynecomastia) 20-40 mg nolva/day for 2-12 months decreases gynecomastia totally in 8 boys (N29).
Effect Nolvadex on heart and cholesterol in "normal" people seems positive, in women with breast cancer conflicting:
-40 mg Nolvadex for 8 weeks in 16 men with coronory artery disease increases %ED-FMD and decreases several plasma cardiovascular risk factors (N11).
-10 mg Nolvadex for 1 and 3 months in 15 healthy boys effects blood lipids and hemostasis similar, but lesser than described in women (N12).
-Nolvadex for 6 months in 54 women treated for breast cancer increases HDL-C/total-Cholesterol ratio which might lead to an increased cardiovascular risk (N13).
-Nolvadex for 3 + 6 months in 80 women with breast cancer: 38 premenopausal women showed no significant variation in serum lipoprotein profiles, 42 postmenopausal women showed significant improvement in serum lipoprotein profiles (N14).
-Nolvadex for 2 months in 16 postmenopausal women with breast cancer shows marked hypertriglyceridemia in 3/16 patients (N15).
-20 mg Nolvadex for 2 years in 57 normal postmenopausal women reduces the levels of atherogenic lipids and fibrinogen which may substantially reduce the risk o cardiovascular disease (N16).
Side effects Nolvadex
-(13 men) 10 mg nolva/day for 3 months. One patient developed calf tenderness and stopped the medication. No other adverse effects were reported (N21).
-(61 men) 40 mg nolva/day. No long term side effects were observed over a 3 year follow-up period (N25).
-(38 boys) Nolvadex for 3-9 months did not show any side effects (N27).
-(8 boys) Nolvadex for 2-12 months did not show any side effects (N29).


N1) http://www.ncbi.nlm.nih.gov/entrez/q...572&query_hl=1
N2) http://www.ncbi.nlm.nih.gov/entrez/q...972&query_hl=1
N3) http://www.ncbi.nlm.nih.gov/entrez/q...502&query_hl=1
N4) http://www.ncbi.nlm.nih.gov/entrez/q...&dopt=Abstract
N11) http://www.ncbi.nlm.nih.gov/entrez/q...075&query_hl=1
N12) http://www.ncbi.nlm.nih.gov/entrez/q...091&query_hl=1
N13) http://www.ncbi.nlm.nih.gov/entrez/q...&dopt=Abstract
N14) http://www.ncbi.nlm.nih.gov/entrez/q...&dopt=Abstract
N15) http://jcem.endojournals.org/cgi/content/full/83/5/1633
N16) http://jcem.endojournals.org/cgi/con...act/80/11/3191
N21) http://www.ncbi.nlm.nih.gov/entrez/q...589&query_hl=1
N22) http://www.ncbi.nlm.nih.gov/entrez/q...718&query_hl=1
N23) http://www.ncbi.nlm.nih.gov/entrez/q...345&query_hl=1
N24) http://www.ncbi.nlm.nih.gov/entrez/q...557&query_hl=1
N25) http://www.ncbi.nlm.nih.gov/entrez/q...552&query_hl=1
N27) http://www.ncbi.nlm.nih.gov/entrez/q...910&query_hl=1
N29) http://www.ncbi.nlm.nih.gov/entrez/q...765&query_hl=1


Arimidex + Femara
Arimidex increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone values (A1-6)
-1 mg/day Arimidex for 2 weeks in 10 men with IHH normalises levels of testosterone, lh - leutenizing hormone - and estradiol (A4).
Arimidex response decreases significantly with aging (A2).
Arimidex increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone above basal levels:
-1,0 mg/day Arimidex for 10 weeks in 8 healthy young men (15-22 yr) increases serum T (58%), lh - leutenizing hormone - and FSH - follicle stimulating hormone - concentrations (A1).
-Arimidex for 1 day in 11 young and 9 older men elevates mean lh - leutenizing hormone - concentrations by 2.1-fold (A2).
-10 mg/day Arimidex for 5 days in 9 normal men increases testosterone levels (563 +/- 42 to 817 +/- 81 ng/dl) (A5).
Arimidex decreases estrogen levels (A1-A3, A5):
-1,0 mg/day Arimidex for 10 weeks in 8 young men (15-22 yr) decreases E2 by 48% (A1).
-Arimidex for 1 day in 11 young and 9 older men decreases serum estradiol concentrations by 50% (A2).
-10 mg Arimidex for 5 days in 9 normal men decreases E2 (33 +/- 3 to 14 +/- 1 pg/mL; P: < 0.0005) (A5).
0,5 mg Arimidex provides the same decrease (50%) in E2 concentrations as 1 mg/day (A1).
1 mg/day Arimidex increases testosterone significantly more than 1 mg/twice weekly, but provides no difference in estrogen levels (A3):
-1 mg/day Arimidex for 12 weeks in 12 elderly men increases mean bioavailable testosterone from (99 +/- 31) to (207 +/- 65 ng/dl).
-1 mg/twice weekly Arimidex for 12 weeks in 11 elderly men increases mean bioavailable testosterone (115 +/- 37) to (178 +/- 55 ng/dl).
Blocking of estrogen does not influence body composition or strength:
-1,0 mg/day Arimidex for 10 weeks in 8 young men (15-22 yr) does not significantly change body composition (body mass index, fat mass, and fat-free mass) or in rates of Protein synthesis or degradation; carbohydrate, lipid, or Protein oxidation; muscle strength; calcium kinetics; or bone growth factors concentrations (A1).
Arimidex opposes exogenous testosterone's suppression of lh - leutenizing hormone - and FSH - follicle stimulating hormone - secretion:
-KTCZ lowers serum testosterone concentration (423 +/- 57 ng/dL (15 +/- 2.0 nmo/L) to 58 +/- 8.6 ng/dL (2.0 +/- 0.3 nmol/L). Added transdermal testosterone increases testosterone levels to (607 +/- 57 ng/dL (21 +/- 2.0 nmol/L).
KTCZ alone increases lh - leutenizing hormone - 3-fold and FSH - follicle stimulating hormone - 2.5-fold. Added transdermal testosterone represses the elevated secretion of both lh - leutenizing hormone - and FSH - follicle stimulating hormone - to mid-normal baseline values.
When Arimidex is added to this, it completely opposes exogenous testosterone's suppression of 24-h lh - leutenizing hormone - and FSH - follicle stimulating hormone - secretion. It likewise abolished testosterone-dependent inhibition of 3-h GnRH-stimulated lh - leutenizing hormone - and FSH - follicle stimulating hormone - release (A6).
Arimidex is not effective in the prevention or treatment of gynecomastia:
-Bicalutamide (150 mg/d) + placebo or in combination with (20 mg/d) Nolvadex or Anastrozole (1 mg/d) for 48 weeks was given to 114 men with prostate cancer. gynecomastia developed in 73% of patients in the bicalutamide group, 10% of the bicalutamide-Nolvadex group, and 51% of the bicalutmide-Anastrozole group (A11).
-1 mg Arimidex for 6 months in 80 boys with gynecomastia provided a 38,5% response vs. 31,4% in the placebo group (A12).
-Arimidex for 6 months in 5 boys with gynecomastia provided a decrease of breast size in 4/5 patients, but breast tissue did not dissappear in 4/5 boys (A13).
Side effects Arimidex
-1 mg Arimidex for 6 months in 80 boys was well tolerated (A12).
-Arimidex for 6 months in 5 boys did not show any adverse effects (A13).
Arimidex and lipid profiles:
-Some studies show Anastrozole as generally having little effect on lipids, while others have indicated adverse effects on lipid profiles/increased hypercholesterolaemia (F11).


Femara increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone values (F1-F3)
-7.5-17.5 mg Femara/week for 6 weeks in 10 men with hypogonadism increases lh - leutenizing hormone - (4.5 +/- 0.8 to 14.8 +/- 2.3 U/l) and total testosterone (7.5 +/- 1.0 to 23.8 +/- 3.0 nmol/l) (F2).
Femara increases lh - leutenizing hormone - , FSH - follicle stimulating hormone - and testosterone above basal levels:
-2,5 mg/day Femara for 28 days in 20 healthy men increases lh - leutenizing hormone - (323-339%) and testosterone (99-146%) (F1).
Femara decreases estrogen levels:
-2,5 mg/day Femara for 28 days in 20 healthy men lowers E2 by 46% in young men and 62% in elder men (F1).
-7.5-17.5 mg Femara/week for 6 weeks in 10 men with hypogonadism decreases serum estradiol (120 +/- 20 to 70 +/- 9 pmol/l) (F2).
Femara keeps estradiol levels basal and increases testosterone + GnRH-induced lh - leutenizing hormone - response during testosterone treatment:
-A low-dose testosterone treatment was given to 23 boys with constitutional delay of puberty. Femara keeps estradiol concentrations at pretreatment levels and increases testosterone > 5-fold higher than testosterone alone (F3).
-testosterone treatment was given to 25 boys with dela puberty for 5 months. T concentrations increased by 55% and 17beta-E2 increased by 130% and gonadotropin concentrations were suppressed. Femara keeps 17beta-E2 at pretreatment levels and increases T concentrations 606%. Basal gonadotropin concentration and the GnRH-induced lh - leutenizing hormone - response increased, and the GnRH-induced FSH - follicle stimulating hormone - response did not change (F4).
No studies can be found on the effect of Femara on gynecomastia!
Femara and lipid profiles:
-Letrozole has been associated with adverse effects on lipid profiles in some studies, including BIG 1-98, but short-term data from randomised trials do not show increased cardiovascular morbidity (F11).


A1)http://jcem.endojournals.org/cgi/content/full/85/7/2370
A2)http://www.ncbi.nlm.nih.gov/entrez/q...79&query_hl=14
A3)http://www.ncbi.nlm.nih.gov/entrez/q...05&query_hl=15
A4)http://www.ncbi.nlm.nih.gov/entrez/q...79&query_hl=16
A5)http://www.ncbi.nlm.nih.gov/entrez/q...78&query_hl=18
A6)http://www.ncbi.nlm.nih.gov/entrez/q...60&query_hl=17
A11)http://www.ncbi.nlm.nih.gov/entrez/q...678&query_hl=1
A12)http://www.ncbi.nlm.nih.gov/entrez/q...042&query_hl=1
A13)http://www.ncbi.nlm.nih.gov/entrez/q...427&query_hl=1
F1)http://www.ncbi.nlm.nih.gov/entrez/q...582&query_hl=1
F2)http://www.ncbi.nlm.nih.gov/entrez/q...136&query_hl=1
F3)http://www.ncbi.nlm.nih.gov/entrez/q...531&query_hl=1
F4)http://www.ncbi.nlm.nih.gov/entrez/q...558&query_hl=1
F11)http://www.ncbi.nlm.nih.gov/entrez/q...522&query_hl=3
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