scholarly journals Safety aspects of 36 months of administration of long-acting intramuscular testosterone undecanoate for treatment of female-to-male transgender individuals

2009 ◽  
Vol 161 (5) ◽  
pp. 795-798 ◽  
Author(s):  
J W Jacobeit ◽  
L J Gooren ◽  
H M Schulte
Keyword(s):  
Side Effects ◽  
Plasma Cholesterol ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Serum Testosterone ◽  
Lipoprotein Cholesterol ◽  
Testosterone Undecanoate ◽  
Internal Genitalia ◽  
Long Acting ◽  
Observation Period

DesignTestosterone treatment is essential for the induction and maintenance of virilization of female-to-male (FTM) transsexuals.AimTo test the safety of a novel testosterone preparation for this purpose.MethodsParenteral long-acting testosterone undecanoate (TU) was administered to 17 FTM transsexuals over 36 months. Observations were made while subjects received treatment.ResultsSerum testosterone rose from 0.50±0.25 to 6.2±1.3 ng/ml at 6 months and remained stable thereafter. The testosterone profiles were largely identical with those in hypogonadal receiving TU. There were no side effects. Over the 36 months of the study, there was a small but significant decrease in plasma cholesterol (from 218±47 to 188±42 mg/dl) and low-density lipoprotein-cholesterol (from 139±48 to 139±48 mg/dl), while plasma levels of high-density lipoprotein-cholesterol and triglycerides did not change significantly. Liver enzymes did not change during treatment. There was an increase of both levels in hemoglobin (from 13.6±1.2 to 16.0±1.5 g/dl) and hematocrit (from 41±4 to 46±4) upon administration but they remained almost without exception within the physiological range. No special measures were needed. Breast and gonads/internal genitalia did not show pathological changes over the observation period.ConclusionThis study reports that TU is suited for induction of virilization in FTM transsexuals without significant side effects over a longer term.

scholarly journals Study on the influence of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on the lipid metabolism in experiment

2021 ◽  
Vol 23 (3) ◽  
pp. 411-416
Author(s):  
I. M. Bilai ◽  
M. I. Romanenko ◽  
D. H. Ivanchenko
Keyword(s):  
Side Effects ◽  
Total Cholesterol ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Hdl Cholesterol ◽  
Lipoprotein Cholesterol ◽  
Atherogenic Index ◽  
Low Density ◽  
Low Density Lipoprotein Cholesterol ◽  
Xanthine Derivatives

Statin side effects are not a rare occurrence, in particular dyspeptic disorders, insomnia, headache, skin erythema, rash are often noted. All of this determines scientists to find new effective and low-toxic hypolipidemic agents. Various natural and synthetic xanthine derivatives have been recognized as therapeutically potential compounds and reported to control various diseases. Therefore, the study of new xanthine derivatives and their hypolipidemic effects, which would have a significant therapeutic effect with minimal side effects, is relevant. The aim of the study was to examine the effect of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives on lipidogram parameters in experimental laboratory rats. Materials and methods. The objects of the study were 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkanic acid derivatives. The experiments were performed in white laboratory Wistar rats weighing 180–220 g. Experimental modeling of hyperlipidemia – tween model: intraperitoneal administration of tween-80 at a dose of 200 mg/100 g body weight. The test compounds were administered orally, simultaneously with tween, at a dose of 1/10 of LD50 (previously calculated by Prozorovsky express method) for 6 days. The following indicators of lipidogram were determined: total cholesterol (TC), high-density lipoprotein cholesterol (HDL cholesterol), low-density lipoprotein cholesterol (LDL cholesterol), triglycerides (TG) and atherogenic index of plasma: TC – HDL cholesterol / HDL cholesterol. The experiments were carried out with respect to Bioethical rules and norms. Results. The studies have shown data on the hypolipidemic activity of 7-β-hydroxy-γ-aryloxypropylxanthinyl-8-thioalkane acid derivatives. According to the conditional efficiency index Ʃ, which included the overall percentage of the following indicators – total cholesterol, low-density lipoprotein cholesterol and triglycerides, the leading compounds were 2439 (87.47 %), 6047 (82.30 %). The reference drug atorvastatin had a value of 82.98 %. Conclusions. The major compound was 2439 identified among all compared to the control group. The prospect of further research is a more detailed study on the ability of xanthine derivatives to exhibit hypolipidemic effects and to influence oxidative stress in various hyperlipidemic models.

scholarly journals Melatonin Improves Fatty Liver Syndrome by Inhibiting the Lipogenesis Pathway in Hamsters with High-Fat Diet-Induced Hyperlipidemia

Nutrients ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 748 ◽  
Author(s):  
Tzu-Hsuan Ou ◽  
Yu-Tang Tung ◽  
Ting-Hsuan Yang ◽  
Yi-Wen Chien
Keyword(s):  
High Fat Diet ◽  
Fatty Acid Synthase ◽  
Plasma Cholesterol ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Lipogenic Enzymes ◽  
High Fat ◽  
Syrian Hamsters ◽  
Hepatic Lipid

The aim of this study was to investigate the effect of melatonin on hepatic lipid metabolism in hamsters with high-fat diet (HFD)-induced dyslipidemia. Male Syrian hamsters were kept on either a chow control (C) or HFD for four weeks. After four weeks, animals fed the HFD were further randomly assigned to four groups: high-fat only (P), melatonin low-dosage (L), medium-dosage (M), and high-dosage (H) groups. The L, M, and H groups, respectively, received 10, 20, and 50 mg/kg/day of a melatonin solution, while the P and C groups received the ethanol vehicle. After eight weeks of the intervention, results showed that a low dose of melatonin significantly reduced HFD-induced hepatic cholesterol and triglycerides; decreased plasma cholesterol, triglycerides, and low-density lipoprotein cholesterol; and increased plasma high-density lipoprotein cholesterol (p < 0.05). In addition, melatonin markedly decreased activities of the hepatic lipogenic enzymes, acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS) (p < 0.05), and elevated the relative hepatic carnitine palmitoyltransferase-1α expression in hamsters with HFD-induced hyperlipidemia. Consequently, melatonin reduced activities of the hepatic lipogenic enzymes, ACC and FAS. In summary, chronic melatonin administration improved HFD-induced dyslipidemia and hepatic lipid accumulation in Syrian hamsters with HFD-induced dyslipidemia, which might have occurred through inhibiting the lipogenesis pathway.

scholarly journals The efficacy of evolocumab in the management of hyperlipidemia: a systematic review

2017 ◽  
Vol 11 (5-6) ◽  
pp. 155-169 ◽  
Author(s):  
Lamia AlHajri ◽  
Asma AlHadhrami ◽  
Shama AlMheiri ◽  
Yalwah AlMutawa ◽  
Zainab AlHashimi
Keyword(s):  
Systematic Review ◽  
Side Effects ◽  
Lipid Profile ◽  
Data Extraction ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Pcsk9 Inhibitors ◽  
Lipid Management ◽  
Highly Effective

Background: Hyperlipidemia or dyslipidemia has been a concern for a long time, with various guidelines emphasizing the importance of managing the lipid profile to prevent cardiac incidences. Although statins have been found to be highly effective, resistance and intolerability to side effects will continue to be a stumbling block for certain patients. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors tackle lipid profile via a novel mechanism and therefore provide an additional effective option for managing lipid profile. The overarching aim of this systematic review was to evaluate the efficacy of evolocumab among various populations with hypercholesterolemia. Methods: A comprehensive search was conducted in ProQuest Health & Medical Complete, Google Scholar, ScienceDirect, and PubMed to identify potential records; then titles, abstracts, and full texts were screened using the inclusion criteria to filter out irrelevant studies. Data extraction and quality assessment were undertaken using standardized tools and the results were narratively synthesized and presented in tables. Results: Eight studies were included in this systematic review after screening 1191 records. All studies demonstrated a statistically significant reduction in low-density lipoprotein cholesterol (LDL-C) values in the groups that received evolocumab compared with the comparator groups ( p < 0.05). The decline in LDL-C levels from baseline in the majority of studies ranged from 40% to 80%, whether used alone or in combination with other agents. Also, high-density lipoprotein cholesterol, lipoprotein (a) and apolipoprotein B were improved with the use of evolocumab. Conclusions: This study helped to collate evidence from studies that tested the effectiveness of evolocumab in the management of hyperlipidemia. Evolocumab seems to be highly effective in reducing LDL-C and other lipid parameters. Hence, it provides an excellent alternative for patients with refractory disease or patients who develop intolerable side effects, therefore helping to overcome the stumbling block to achieving optimal lipid management.

scholarly journals Rutin ameliorates carbon tetrachloride (CCl4)-induced hepatorenal toxicity and hypogonadism in male rats

PeerJ ◽  
2019 ◽  
Vol 7 ◽  
pp. e7011 ◽  
Author(s):  
Hany Elsawy ◽  
Gehan M. Badr ◽  
Azza Sedky ◽  
Basem M. Abdallah ◽  
Abdullah M. Alzahrani ◽  
...  
Keyword(s):  
Carbon Tetrachloride ◽  
Sperm Quality ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Serum Testosterone ◽  
Lipoprotein Cholesterol ◽  
Male Rats ◽  
Low Density ◽  
Low Density Lipoprotein Cholesterol ◽  
Serum Triglycerides

Rutin, a food derived-polyphenolic bioflavonoid, has been acknowledged for several health benefits. This study aims to explore the ameliorative effects of rutin against carbon tetrachloride (CCl4) toxicity in male rats. Adult male rats were given either CCl4 (30% in olive oil, 3 ml/kg b.w. intraperitoneally) alone or in combination with rutin (70 mg/kg intragastrically) twice a week for 4 weeks. Our data showed that rutin mitigated CCl4 hepatorenal damage, as indicated by diagnostic markers (i.e., transaminases, alkaline phosphatase, total bilirubin, total protein, albumin, urea, uric acid and creatinine), and histopathological findings. In addition, CCl4 induced profound elevation of free radical generation and oxidative stress, as evidenced by increasing lipid peroxidation and reducing catalase, superoxide dismutase and glutathione peroxidase activities in liver, kidney and testicular tissues; these effects were suppressed by coexposure with rutin. Moreover, the increase in the levels of serum triglycerides, cholesterol, low-density lipoprotein cholesterol, and very-low-density lipoprotein cholesterol induced by CCl4 was effectively counteracted by rutin. The decrease in the level of high-density lipoprotein cholesterol in the CCl4 group was also counteracted by rutin treatment. Interestingly, the decreased levels of hormonal mediators associated with sperm production, including serum testosterone, luteinizing hormone and follicle-stimulating hormone, and the impaired sperm quality induced by CCl4 were reversed by rutin. Data from the current study clearly demonstrated that rutin supplementation could at least partly overcome CCl4-induced hepatotoxicity, nephrotoxicity and reproductive toxicity by antioxidant and antidyslipidemic effects.

Platelet Function and Lipoprotein Levels after Plasma-Exchange in Patients with Familial Hypercholesterolaemia

1983 ◽  
Vol 64 (6) ◽  
pp. 637-642 ◽  
Author(s):  
Gerald Brook ◽  
Giora Winterstein ◽  
Michael Aviram
Keyword(s):  
Plasma Exchange ◽  
Platelet Function ◽  
Familial Hypercholesterolaemia ◽  
Plasma Cholesterol ◽  
Low Density Lipoprotein ◽  
Young Patients ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Low Density ◽  
Lipoprotein Concentration

1. Repeated plasma exchange was carried out on three young patients with severe familial hypercholesterolaemia. There was a 3 week interval between each exchange. After a single exchange, plasma cholesterol, apolipoprotein B and low density lipoprotein-cholesterol levels decreased markedly, but pre-exchange levels were not achieved within 2 weeks. High density lipoprotein-cholesterol and apolipoprotein A-I levels also fell but returned to the original concentration after only 5 days. 2. Platelet aggregation and [14C]serotonin release were increased in all three patients and dropped by 20% and 13% respectively after a single plasma exchange. Platelet function in vitro returned to pre-exchange levels with similar kinetics to that observed with the low density lipoprotein concentration. On removal of 100 g of plasma cholesterol, after repeated exchanges, low density lipoprotein concentration and platelet function were significantly decreased in comparison with values before initiation of plasma exchange. in addition there was a marked regression of xanthoma in all three patients. 3. Since this procedure is instrumental in achieving a negative cholesterol balance as well as inhibiting hypersensitive platelets, it may well result in a downgrading of the atherosclerotic risk.

Synthetic Approaches Towards Antihypercholesterolemic Drug Simvastatin

2019 ◽  
Vol 16 (5) ◽  
pp. 652-670
Author(s):  
Tanzeela A. Fattah ◽  
Aamer Saeed ◽  
Syeda A. Shehzadi
Keyword(s):  
Cardiovascular Diseases ◽  
Plasma Cholesterol ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Low Density ◽  
Experimental Conditions ◽  
High Cholesterol Level ◽  
Lowering Drug ◽  
High Yields

Cardiovascular diseases are among the most threatening problems being faced by twenty-first century humans. The core cause of these diseases is high cholesterol level. Simvastatin (1: Synvinolin) is a well-known cholesterol-lowering drug marketed under the trade name Zocor®, which significantly reduces the risk of cardiovascular diseases related to hypercholesterolemia and is effective in lowering the total plasma cholesterol, low-density and very low-density lipoprotein cholesterol. It also enhances the high-density lipoprotein cholesterol. This review article aims to provide an overview of several chemical and biological methods utilized for the production of simvastatin in high yields and purity. Many robust and scalable methods have been described using lovastatin (2: Mevinolin) as a starting material, produced by the fungal strain of Aspergelius terreus. Enzymatic synthesis of simvastatin is also highlighted in this review. In addition, detailed experimental conditions, as well as the compatibility for industrial-scale preparations of simvastatin are also discussed.

Balancing Efficacy and Tolerability Issues with Statin Therapy— Considerations for the Use of Pitavastatin in Special Patient Populations

2011 ◽  
Vol 07 (01) ◽  
pp. 30 ◽  
Author(s):  
James M Falko ◽  
Keyword(s):  
Side Effects ◽  
High Risk ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Asian Populations ◽  
Increased Risk ◽  
Mixed Dyslipidemia ◽  
High Risk Populations ◽  
History Of Use

One of the main objectives of cardiovascular care is to control elevated low-density lipoprotein cholesterol (LDL-C). Statins are the mainstay for managing LDL-C with proven high efficacy and satisfactory safety profiles. However, the most known side effects are muscle symptoms, which are particularly common in individuals who often have co-existing conditions and are taking multiple medications. The latest statin that has become available, pitavastatin, is not known to cause cytochrome P450-mediated drug–drug interactions, making it an ideal statin for individuals at a high risk for side effects. Pitavastatin will be particularly beneficial in treating patients with mixed dyslipidemia, as it is effective in reducing triglycerides and increasing high-density lipoprotein cholesterol (HDL-C). Pitavastatin has an established history of use, and has a safety and adverse event profile similar to that of other existing statins. Individuals at high risk from side effects with statins include older people (>65 years), individuals with diabetes, kidney disease, or metabolic syndrome and individuals taking multiple medications. South Asian populations that have migrated to Western countries are at particularly high risk for cardiovascular disease, and this population also has an increased risk for statin-related side effects. This article will summarize the factors that place individuals at high risk for dyslipidemia, treatment of high risk populations with statins, and the issues associated with treating high risk populations with statins. The benefits of treating these individuals with pitavastatin will be reviewed, as well as alternative forms of therapy.

scholarly journals Update on Inclisiran for Treatment of Hypercholesterolemia

2020 ◽  
pp. 1-3
Author(s):  
Nasser Mikhail ◽  
Keyword(s):  
Severe Renal Impairment ◽  
English Literature ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Lipoprotein Cholesterol ◽  
Apo B ◽  
Pubmed Search ◽  
Cv Disease ◽  
Long Acting ◽  
Meta Analyses

Background: Inclisiran is a drug under development that inhibits the hepatic synthesis of proprotein convertase subtilistin/Kexin type 9 (PCSK9) leading to reduction in plasma levels of low-density lipoprotein-cholesterol (LDL-C). Methods: Review of pertinent English literature by Pubmed search until June 12, 2020. Search terms are lipids, PCSK9, LDL-C, inclisiran, safety, efficacy. Studies included are randomized trials, meta-analyses, and review articles. Results: Inclisiran is administered by subcutaneous (SC) injection at day 1, day 90, then every 6 months. In patients with atherosclerotic cardiovascular (CV) disease and those with heterozygous familial hypercholesterolemia receiving maximally tolerated statins, the placebo-adjusted percent reduction in LDL-C levels was 48% to 52% after 6 months. Inclisiran also lowers other atherogenic lipoproteins such non-high-density lipoprotein-cholesterol (nonHDL-C) by 43 to 47%, apoprotein B (apo B) 39% to 43%, lipoprotein(a) by 18-25% compared with placebo. Efficacy of inclisiran in lowering LDL-C levels was similar in patients with and without diabetes, and patients with normal renal function compared with those with severe renal impairment. Inclisiran is overall well-tolerated. Most common adverse effects are injection site reactions. Conclusions: Inclisiran is an effective and long-acting drug for lowering LDL-C levels. Studies are underway to evaluate effects of inclisiran on CV events and mortality

Sign in / Sign up

Export Citation Format

Share Document