scholarly journals Toward a lowest effective dose of cyproterone acetate in trans women: Results from the ENIGI study

Author(s):  
Suzanne M E Kuijpers ◽  
Chantal M Wiepjes ◽  
Elfi B Conemans ◽  
Alessandra D Fisher ◽  
Guy T’Sjoen ◽  
...  

Abstract Context Cyproterone acetate (CPA) is a competitive inhibitor of the androgen receptor and exerts negative hypothalamic feedback. It is often used in combination with estrogens in trans women to achieve feminization. However, CPA has been associated with side effects such as changes in liver enzyme concentrations and increases in prolactin concentrations. The question is whether testosterone lowering, as well as these side effects, are dose-dependent. Objective To assess the lowest effective dose of CPA in trans women to prevent side effects. Design This longitudinal study is part of the European Network for the Investigation of Gender Incongruence (ENIGI), a multicenter prospective cohort study. Setting Gender identity centers in Amsterdam, Ghent, and Florence Participants Trans women (n = 882) using estrogens only or in combination with 10mg, 25mg, 50mg, or 100mg CPA daily. Intervention Different doses of CPA. Main Outcome measure The concentration of testosterone at 3 and/or 12 months of hormone therapy. Results Using estrogens only (without CPA) led to testosterone concentrations of 5.5nmol/L (SEM 0.3). All doses of CPA resulted in testosterone concentrations below the pre-defined threshold of suppression of 2nmol/L (10mg: 0.9nmol/L, SEM 0.7; 25mg: 0.9nmol/L, SEM 0.1; 50mg: 1.1nmol/L, SEM 0.1; 100mg: 0.9nmol/L, SEM 0.7). Higher prolactin and lower high-density lipoprotein concentrations were observed with increasing doses of CPA. No differences in liver enzyme concentrations were found between the doses. Conclusions Compared to higher doses of CPA, a daily dose of 10mg is equally effective in lowering testosterone concentrations in trans women, while showing fewer side effects.

LGBT Health ◽  
2017 ◽  
Vol 4 (5) ◽  
pp. 328-336 ◽  
Author(s):  
Justine Defreyne ◽  
Nienke Nota ◽  
Cecilia Pereira ◽  
Thomas Schreiner ◽  
Alessandra D. Fisher ◽  
...  

Author(s):  
Justine Defreyne ◽  
Nienke Nota ◽  
Cecilia Perreira ◽  
Schreiner Thomas ◽  
Fisher Alessandra Daphne ◽  
...  

2017 ◽  
Vol 14 (4) ◽  
pp. e162
Author(s):  
J. Defreyne ◽  
N. Nota ◽  
C. Pereira ◽  
T. Schreiner ◽  
A. Fisher ◽  
...  

1977 ◽  
Vol 37 (01) ◽  
pp. 154-161 ◽  
Author(s):  
B. A Janik ◽  
S. E Papaioannou

SummaryUrokinase, streptokinase, Brinase, trypsin, and SN 687, a bacterial exoprotease, have been evaluated in an ex vivo assay system. These enzymes were injected into rabbits and the fibrinolytic activity as well as other coagulation parameters were measured by in vitro techniques. Dose-response correlations have been made using the euglobulin lysis time as a measure of fibrinolytic activity and the 50% effective dose has been determined for each enzyme. Loading doses, equal to four times the 50% effective dose, were administered to monitor potential toxicity revealing that Brinase, trypsin, and SN 687 were very toxic at this concentration.Having established the 50% effective dose for each enzyme, further testing was conducted where relevant fibrinolytic and coagulation parameters were measured for up to two days following a 50% effective dose bolus injection of each enzyme. Our results have demonstrated that urokinase and streptokinase are plasminogen activators specifically activating the rabbit fibrinolytic system while Brinase, trypsin and SN 687 increase the general proteolytic activity in vivo.The advantages of this ex vivo assay system for evaluating relative fibrinolytic potencies and side effects for plasminogen activators and fibrinolytic proteases have been discussed.


The Breast ◽  
2021 ◽  
Vol 57 ◽  
pp. 118-122
Author(s):  
Christel JM. de Blok ◽  
Benthe AM. Dijkman ◽  
Chantal M. Wiepjes ◽  
Inge RHM. Konings ◽  
Koen MA. Dreijerink ◽  
...  
Keyword(s):  
In Trans ◽  

Metabolites ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 223
Author(s):  
Roberta D’Assante ◽  
Mariarosaria De Luca ◽  
Sergio Ferraro ◽  
Andrea Ferraro ◽  
Antonio Ruvolo ◽  
...  

Hypercholesterolemia represents a serious public health problem as it significantly increases the risk of developing cardiovascular diseases. Its treatment with statin is limited by costs, side effects, and drugs interactions. Nutraceuticals appear to have an important metabolic effect on cholesterol reduction as well as on body weight and glycemia. The aim of this study was to evaluate the effect of a nutraceutical combination (Melasterol) in eighty-seven patients with acquired hypercholesterolemia. Clinically relevant parameters were collected at baseline and after three and six months of Melasterol treatment, one tablet per day. The primary endpoint was the change in cholesterol and triglyceride levels. Six months of treatment resulted in a 19.2% decrease in total cholesterol, accompanied by a 19.8% decrease in low-density lipoprotein (LDL) and a 23% reduction in triglycerides (p < 0.001) but not in high-density lipoprotein (HDL) levels (p > 0.05). These results were paralleled by a significative blood glucose (108.3 ± 21.3 vs. 98.4 ± 18.6 mg/dL p < 0.001) and body mass index (BMI) reduction (27.8 ± 4.4 vs. 27.0 ± 4.2 mg/dL, p < 0.001). A subgroup of 12 patients performed flow-mediated dilation, with values increasing by 1.8% (p < 0.05). No significant side effects were reported. Besides its cholesterol-lowering effect, Melasterol was associated with a significant improvement in other relevant metabolic parameters such as BMI and glycemia.


1985 ◽  
Vol 110 (4) ◽  
pp. 433-439 ◽  
Author(s):  
D. Dewailly ◽  
P. Thomas ◽  
J. Buvat ◽  
J. L. Wemeau ◽  
J. C. Fourlinnie ◽  
...  

Abstract. CU 38085 (mesulergin) was given at doses ranging from 0.5 to 5 mg/day to 37 patients with pathological hyperprolactinaemia of varying aetiology. The effectiveness of this drug on the suppression of hyperprolactinaemia and on the recovery of gonadal functions was equivalent to that of bromocriptine previously given to a different group of 83 hyperprolactinaemic patients. Tumour shrinkage during treatment with CU 32085 was ascertained in two cases of macroprolactinoma. Histological examination after adenomectomy revealed extensive peri-vascular fibrosis in both cases. In most patients, the efficient doses of CU 32085 were 5-fold lower than those of bromocriptine. After acute oral administration in 10 previously untreated patients, 0.5 mg of CU 32085 had a more prolonged suppressive effect on Prl levels than 2.5 mg of bromocriptine (approximately 18 vs 12 h). According to this, 0.5 mg CU 32085 once a day was sufficient to maintain Prl levels within the normal range in 16 patients. Side-effects were similar in nature and frequency to those induced by bromocriptine and seemed to be dose-dependent. They can be avoided by slowly increases of dose at initiation of treatment.


1998 ◽  
Vol 336 (2) ◽  
pp. 381-386 ◽  
Author(s):  
Lothar GORETZKI ◽  
Barbara M. MUELLER

The low-density-lipoprotein-receptor-related protein (LRP) binds and internalizes numerous ligands, including lipoproteins, proteinase–inhibitor complexes and others. We have shown previously that LRP-mediated ligand internalization is dependent on cAMP-dependent protein kinase (PKA) activity. Here, we investigated whether ligation of LRP increases the intracellular cAMP level and PKA activity via a stimulatory GTP-binding protein. Treatment of LRP-expressing cell lines with the LRP ligands lactoferrin or urokinase-type plasminogen activator caused a significant elevation in cAMP and stimulated PKA activity in a dose-dependent manner. Addition of the 39 kDa receptor-associated protein (RAP), an antagonist for ligand interactions with LRP, blocked the lactoferrin-induced increase in PKA activity, demonstrating a requirement for ligand binding to LRP. Incubation of cell membrane fractions with lactoferrin increased GTPase activity in a time- and dose-dependent manner, and treatment with LRP ligands suppressed cholera-toxin-mediated ADP-ribosylation of the Gsα subunit of a heterotrimeric G-protein. Affinity precipitation of LRP with RAP resulted in co-precipitation of two isoforms of Gsα from detergent extracts. We thus conclude that LRP is a signalling receptor that associates directly with a stimulatory heterotrimeric G-protein and activates a downstream PKA-dependent pathway.


Author(s):  
Rachel Wamboldt ◽  
Shirley Shuster ◽  
Bikrampal S Sidhu

Abstract Context Breastfeeding is known to have many health and wellness benefits to the mother and infant; however, breastfeeding in trans women has been greatly under-researched. Objective To review potential methods of lactation induction in trans women wishing to breastfeed and to review the embryological basis for breastfeeding in trans women. Design This article summarizes a case of successful lactation in a trans woman, in which milk production was achieved in just over 1 month. Setting This patient was followed in an outpatient endocrinology clinic. Participant A single trans woman was followed in our endocrinology clinic for a period of 9 months while she took hormone therapy to help with lactation. Interventions Readily available lactation induction protocols for nonpuerpural mothers were reviewed and used to guide hormone therapy selection. Daily dose of progesterone was increased from 100 mg to 200 mg daily. The galactogogue domperidone was started at 10 mg 3 times daily and titrated up to effect. She was encouraged to use an electric pump and to increase her frequency of pumping. Main Outcome Measure Lactation induction Results At one month, she had noticed a significant increase in her breast size and fullness. Her milk supply had increased rapidly, and she was producing up to 3 to 5 ounces of milk per day with manual expression alone. Conclusions We report the second case in the medical literature to demonstrate successful breastfeeding in a trans woman through use of hormonal augmentation.


Medicina ◽  
2022 ◽  
Vol 58 (1) ◽  
pp. 94
Author(s):  
Ioana Cretu ◽  
Bogdan Cretu ◽  
Catalin Cirstoiu ◽  
Adrian Cursaru ◽  
Mihaela Milicescu ◽  
...  

Background and Objectives: The occurrence of rheumatological side effects in a patient after receiving immunotherapy for cancer is becoming increasingly common. Oncologists often fail to diagnose and refer affected patients to rheumatologists. This paper presents the various rheumatological adverse events that occur after immunotherapy in patients as well as their treatment and evolution. Materials and Methods: A total of 36 patients were monitored between November 2018 and March 2020. The oncologist monitoring the immunotherapy-treated patients identified the occurrence of musculoskeletal side effects. The grading of toxicities was performed by both the oncologist and the rheumatologist using common terminology criteria for adverse events (CTCAE). Rheumatological treatment was administered, and for some patients, immunotherapy was discontinued. Results: The clinical presentations of the patients varied. Mild side effects (grade 1–2) were reported in a higher proportion than severe side effects (grade 3–5). Therefore, thirty-one patients had mild-to-moderate side effects, and five patients had severe side effects. Adverse reactions occurred, on average, 10 weeks after the initiation of immunotherapy; this indicated that the severity of the toxicity was dose dependent. Patients were treated with NSAIDs or prednisone, depending on the severity of the side effects, and for patients with severe manifestations, immunotherapy was discontinued. The remission of rheumatic manifestations varied depending on the grade of the manifestations. Conclusions: The clinical, biological, and ultrasound presentations of the patients with adverse events followed by cancer treatments differed from classic rheumatological manifestations. Thorough examinations of these patients by both oncologists and rheumatologists are needed in order to correctly diagnose and treat rheumatological adverse events. Multiple studies that include a larger number of participants are needed in order to better understand the pathogenesis and clinical evolution of these patients under different treatment conditions.


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