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Max-gainz
wtf?! det här har jag missat helt kan du linka studie? vill verkligen läsa!
Citat:
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HeadOfBoo
Jag vill också gärna veta hur denna utvärdering går och hur det känns.
AROMASIN – Exemestane
Type-I Aromatase Inhibitor
Aromasin (Exemestane) is a Type-I aromatase inhibitor, or suicidal aromatase inhibitor. It’s called this because it lowers estrogen production in the body by attaching to the aromatase enzyme, and permanently deactivating it. It averages 90% rate of estrogen suppression, which equals a reduction in estradiol levels of about 50%, as well as significantly raising testosterone .(up to 60%)
Aromasin not only increases testosterone and lowers estrogen, but it also increases levels of insulin -like growth Factor (IGF). And Aromasin is not too harsh on lipid panel (cholesterol), unlike some of the other AIs’ like Letrozole .(Femara) Aromasin reaches steady blood plasma levels of after a week of administration, and this is also when we see it begin its maximal effect on reducing circulating estrogen levels. It has a terminal half life of 9 hours in MEN, so taking it once per day will build up blood plasma levels to a very effective level.
Also, there have been some additional researches related to Aromasin in men in pharmacokinetics. The results of the research are the following:
24 hours after one 25mg dose, estrogen levels are reduced by 70-80%;
72 hours later estrogen levels are still 40% below the baseline;
120 hours after initial dose, estrogen levels return to baseline.
Additionally, the University of Florida conducted a study in healthy young men:
Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males.
Nemours Children’s Clinic and Research Programs (N.M., J.L., A.R.), Jacksonville, Florida 32207; and University of Florida Health Sciences Center (D.P.) and Amersham Pharmacia Biotech (E.d.S., A.K., B.L.), Peapack, New Jersey 07977
To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14–26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg Aromasin daily, orally, for 10 days with a 14 day washout period. Blood was withdrawn before and 24 hours after the last dose of each treatment period. A PK study was performed using a 25mg dose. Aromasin suppressed plasma estradiol comparably with either dose [25 mg, 38%; 50 mg, 32%], with a reciprocal increase in testosterone concentrations (60% and 56%; for both).
The following observations were made:
Plasma lipids and IGF-I concentrations were unaffected by treatment.
The PK properties of the 25-mg dose showed the highest concentrations 1 h after administration, indicating rapid absorption.
Maximal estradiol suppression of 62 ± 14% was observed at 12 h.
The drug was well tolerated.
The terminal half-life was 8.9 hours in the male subjects.
In conclusion, Aromasin (Exemestane) is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.
References and Supporting Data:
A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation.Br J Clinical Pharmacology. 2005 Mar, 59(3):355-64.
Eur. J. Cancer. 2000, May;36(8):976-82
The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956Copyright © 2003 by The Endocrine Society
Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S
Anticancer Res. 2003 Jul-Aug;23(4):3485
J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.