Detection and effects on serum and urine steroid and LH of repeated GnRH analog (leuprolide) stimulation

Handelsman, David J.; Idan, Amanda; Grainger, Janelle; Goebel, Catrin; Turner, Leo; Conway, Ann J.

doi:10.1016/j.jsbmb.2014.01.011

Cited by 27 publications

(17 citation statements)

References 37 publications

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“…The nandrolone dosage was selected as known to transiently suppress endogenous testosterone for the study period without adverse effects (Minto et al, 1997;Handelsman et al, 2009Handelsman et al, , 2014Singh et al, 2014). The secondary endpoints were serum dihydrotestosterone (DHT) and estradiol (LC-MS) as well as tolerability.…”

Section: Methodsmentioning

confidence: 99%

“…They were administered two intramuscular injections of nandrolone decanoate (50 mg in 1 mL arachis oil vehicle) comprising 200 mg three days prior to and 100 mg four days after the first testosterone dose to suppress endogenous testosterone secretion throughout the study. The nandrolone dosage was selected as known to transiently suppress endogenous testosterone for the study period without adverse effects (Minto et al, 1997;Handelsman et al, 2009Handelsman et al, , 2014Singh et al, 2014). Each eligible, consenting participant was administered three single doses of testosterone cream in random sequence on different study days with at least 2 days wash-out period between studies.…”

Section: Methodsmentioning

confidence: 99%

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Pharmacokinetics of testosterone cream applied to scrotal skin

et al. 2017

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Scrotal skin is thin and has high steroid permeability, but the pharmacokinetics of testosterone via the scrotal skin route has not been studied in detail. The aim of this study was to define the pharmacokinetics of testosterone delivered via the scrotal skin route. The study was a single-center, three-phase cross-over pharmacokinetic study of three single doses (12.5, 25, 50 mg) of testosterone cream administered in random sequence on different days with at least 2 days between doses to healthy eugonadal volunteers with endogenous testosterone suppressed by administration of nandrolone decanoate. Serum testosterone, DHT and estradiol concentrations were measured by liquid chromatograpy, mass spectrometry in extracts of serum taken before and for 16 h after administration of each of the three doses of testosterone cream to the scrotal skin. Testosterone administration onto the scrotal skin produced a swift (peak 1.9-2.8 h), dose-dependent (p < 0.0001) increase in serum testosterone with the 25 mg dose maintaining physiological levels for 16 h. Serum DHT displayed a time- (p < 0.0001), but not dose-dependent, increase in concentration reaching a peak concentration of 1.2 ng/mL (4.1 nm) at 4.9 h which was delayed by 2 h after peak serum testosterone. There were no significant changes in serum estradiol over time after testosterone administration. We conclude that testosterone administration to scrotal skin is well tolerated and produces dose-dependent peak serum testosterone concentration with a much lower dose relative to the non-scrotal transdermal route.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics of testosterone cream applied to scrotal skin

et al. 2017

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“…The influence of pharmacological interventions on the serum and urine steroid profile was studied by Handelsman et al who investigated the effect of administrations of the superactive gonadotropin analogue leuprolide to men. [62] Serum T, dihydrotestosterone (DHT), and 5α-androstane-3α,17β-diol (Adiol) were significantly increased along with urinary T, EpiT, and androsterone (A) concentrations upon five days of leuprolide administration, resulting in modest (if any) changes in T/EpiT ratios. Urinary steroid levels returned to baseline values at day 10, and a detection strategy involving both the direct analysis of leuprolide and its main metabolite as well as using the ratio of luteinizing hormone (LH)/T were suggested.…”

Section: Initial Testing Proceduressteroid Profilingmentioning

confidence: 99%

Annual banned‐substance review: analytical approaches in human sports drug testing

Thevis

Kuuranne

Geyer

et al. 2014

Drug Testing and Analysis

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Within the mosaic display of international anti-doping efforts, analytical strategies based on up-to-date instrumentation as well as most recent information about physiology, pharmacology, metabolism, etc., of prohibited substances and methods of doping are indispensable. The continuous emergence of new chemical entities and the identification of arguably beneficial effects of established or even obsolete drugs on endurance, strength, and regeneration, necessitate frequent and adequate adaptations of sports drug testing procedures. These largely rely on exploiting new technologies, extending the substance coverage of existing test protocols, and generating new insights into metabolism, distribution, and elimination of compounds prohibited by the World Anti-Doping Agency (WADA). In reference of the content of the 2014 Prohibited List, literature concerning human sports drug testing that was published between October 2013 and September 2014 is summarized and reviewed in this annual banned-substance review, with particular emphasis on analytical approaches and their contribution to enhanced doping controls.

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“…4,5 On the other hand, LH can also be used to recover suppressed testicular function after use of anabolic steroids. 4,5 On the other hand, LH can also be used to recover suppressed testicular function after use of anabolic steroids.…”

mentioning

confidence: 99%

“…However, it has been reported that administration of LH has only minor effects on testosterone levels in men. 4,5 On the other hand, LH can also be used to recover suppressed testicular function after use of anabolic steroids. Furthermore, elevated LH levels can be a sign of consumption of a substance that induce the release of endogenous LH, such as gonadotropin-releasing factors (gonadotropin-releasing hormone (GnRH) and its synthetic analogs, such as leuprolide 3,6 or estrogen blockers (anti-estrogens and aromatase inhibitors).…”

mentioning

confidence: 99%

Analysis of luteinizing hormone (LH): Validation of a commercial ELISA kit for LH analysis and quantification in doping control samples

Mäkelä

Leinonen

Suominen

2020

Drug Testing and Analysis

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Luteinizing hormone (LH) is a dimeric glycoprotein produced and secreted by the pituitary gland, with a molecular weight of approximately 30 000 Da. The main clinical use for exogenous LH-administration is typically linked to the treatment of infertility, in both men and women. The desired effect of LH misuse in sport is due to the enhancement of testicular production of testosterone. Elevated LH levels may also indicate the usage of gonadotropin-releasing factors or estrogen blockers. Therefore, LH is listed by the World Anti-Doping Agency (WADA) as a prohibited substance in male athletes, and according to the WADA technical document, laboratories should determine the the total LH concentrations in urine. The TD lists two different assays that are suitable for measuring total LH in urine, Delfia and Siemens Immulite. Other fit-for-purpose assays can be used, as long as they are capable of detecting total LH in urine. In case an assay not listed in the TD will be used, population-based reference values have to be determined in the validation procedure.In this study a new immunoassay was validated for the measurement of LH in urine.The assay (AccuBind ELISA Microwells, Luteinizing Hormone, Monobind Inc.), originally intended for serum, showed adequate sensitivity and was proven fit-forpurpose in routine doping control. Population-based distribution of the assay was in good agreement with the results of Delfia and Immulite assays, for which the method-specific cut-off-values are 40 IU/L (Delfia) and 60 IU/L (Siemens Immulite). K E Y W O R D SAccuBind, Doping, ELISA, LH βcore fragment, LH β-chain, Luteinizing hormone (LH), Monobind Inc, Urine | INTRODUCTIONLH is a dimeric glycoprotein consisting of αand β-subunits noncovalently linked together. The α-subunit is similar to other pituitary hormones (FSH, TSH and hCG), while the β-subunit is unique. The βsubunit confers the biological activity to the molecule. Like hCG, in addition to the intact molecule the total immunoreactivity of urinary LH is due to intact LH, as well as to smaller degradation products, such as the LH β chain and the LH β-core fragment. 1 In addition there are naturally occurring variants of LH, eg. a variant with an additional glycosylation site, as well as a less common LH variant with an amino acid substitution in the β chain, which has been linked to male infertility.LH and hCG bind to a common receptor, the LH/choriogonadotropin receptor, also known as the lutropin receptor. Despite of sharing a common receptor, both of these hormones triggers different cascades of events following receptor binding. 2 LH is primarily responsible for regulating the synthesis of gonadal steroid hormones. In women LH drives follicle maturation and

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Detection and effects on serum and urine steroid and LH of repeated GnRH analog (leuprolide) stimulation

Cited by 27 publications

References 37 publications

Pharmacokinetics of testosterone cream applied to scrotal skin

Pharmacokinetics of testosterone cream applied to scrotal skin

Annual banned‐substance review: analytical approaches in human sports drug testing

Analysis of luteinizing hormone (LH): Validation of a commercial ELISA kit for LH analysis and quantification in doping control samples

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