A review on elagolix sodium
an oral gonadotropin - releasing hormone (gnrh) receptor antagonist for endometriosis associated pain
Journal name: World Journal of Pharmaceutical Research
Original article title: A review on elagolix sodium
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Subtitle: an oral gonadotropin - releasing hormone (gnrh) receptor antagonist for endometriosis associated pain
Original source:
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Gaurav S. Mahalpure, Dr. Rajendra D. Wagh and Bhushan J. Mali
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: A review on elagolix sodium
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20229-24770
Download the PDF file of the original publication
Summary of article contents:
Introduction
Elagolix sodium is a novel, non-peptide oral gonadotropin-releasing hormone (GnRH) receptor antagonist approved by the US FDA in July 2018 for treating moderate to severe pain related to endometriosis. Developed by AbbVie and Neurocrine Biosciences, Elagolix is characterized by its ability to partially and reversibly suppress ovarian estrogen production, making it effective for managing endometriosis and uterine fibroids. This review article provides an in-depth look at the clinical pharmacology, mechanism of action, therapeutic trials, potential adverse effects, and ongoing research associated with Elagolix sodium.
Mechanism of Action
Elagolix sodium functions by competitively binding to GnRH receptors in the anterior pituitary gland, preventing the action of endogenous GnRH. This inhibition leads to a decrease in the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), subsequently reducing ovarian estrogen levels. The drug demonstrates a dose-dependent response, with lower doses leading to partial suppression of estradiol and higher doses achieving nearly complete suppression. This rapid, reversible action differentiates Elagolix from long-acting GnRH agonists, which often require a period of receptor downregulation before achieving similar effects.
Pharmacokinetics
Elagolix is rapidly absorbed following oral administration, reaching maximum plasma concentration (Tmax) within approximately one hour. It exhibits linear pharmacokinetics across the therapeutic dose range, and its bioavailability is not significantly affected by food. The drug is moderately bound to plasma proteins, and it primarily undergoes metabolism through cytochrome P450 enzymes, with a terminal elimination half-life of around 4-6 hours. Excretion is primarily through feces, with minimal renal excretion indicating a favorable pharmacokinetic profile for sustained dosing regimens.
Therapeutic Trials and Efficacy
In extensive clinical trials, Elagolix has shown significant efficacy in reducing endometriosis-associated pain measures such as dysmenorrhea and non-menstrual pelvic pain. In trials like ELARIS EM-I and EM-II, participants reported substantially higher response rates in pain reduction when treated with Elagolix compared to placebo. Further studies have indicated the drug's effectiveness in managing heavy menstrual bleeding associated with uterine fibroids, highlighting its capacity to improve patient quality of life while offering a non-surgical option for managing pain and symptoms related to these hormone-dependent conditions.
Conclusion
Elagolix sodium represents a significant advancement in the management of endometriosis and uterine fibroids, offering an effective oral treatment option that operates through a distinct mechanism compared to existing therapies. The favorable pharmacokinetic characteristics, along with demonstrated efficacy in clinical trials, underscore its utility in addressing endemic pain conditions. However, careful consideration of contraindications and potential adverse effects is essential for optimizing patient outcomes, warranting ongoing research to further elucidate its long-term safety and effectiveness.
FAQ section (important questions/answers):
What is Elagolix sodium used for in women’s health?
Elagolix sodium is an oral GnRH receptor antagonist used for treating moderate to severe pain associated with endometriosis and heavy menstrual bleeding related to uterine fibroids.
How does Elagolix sodium function in the body?
Elagolix sodium works by competitively inhibiting GnRH receptors in the pituitary gland, which suppresses the production of gonadotropins and reduces ovarian estrogen, ultimately alleviating endometriosis-related pain.
What are the common dosages of Elagolix sodium?
Elagolix sodium is typically administered at 150 mg once daily or 200 mg twice daily for managing endometriosis-associated pain, based on clinical trials.
What are the side effects associated with Elagolix sodium?
Common side effects of Elagolix include hot flushes, headache, nausea, mood swings, and potential bone loss, while serious adverse events may include appendicitis and abdominal pain.
Is Elagolix sodium safe for pregnant women?
No, Elagolix sodium is contraindicated in pregnant women as it may increase the risk of early pregnancy loss.
What ongoing studies are evaluating Elagolix sodium's effectiveness?
Ongoing clinical trials are assessing Elagolix sodium, both as monotherapy and in combination with hormone therapies, for managing endometriosis pain and uterine fibroids.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “A review on elagolix sodium”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Pain:
Pain is a significant symptom associated with conditions like endometriosis and uterine fibroids, impacting women's quality of life. The review emphasizes evaluating treatments like Elagolix sodium to alleviate moderate to severe pain, showcasing the importance of pain management in reproductive health issues.
2) Drug:
The term 'drug' refers to pharmacological substances used to treat diseases or alleviate symptoms. This review highlights Elagolix sodium as an oral GnRH receptor antagonist, assessing its safety and effectiveness in managing conditions linked to female reproductive health, such as endometriosis and uterine fibroids.
3) Study (Studying):
A study is a systematic investigation aimed at discovering or interpreting facts. The review cites numerous clinical trials investigating the efficacy and safety of Elagolix sodium. These studies provide critical data on the drug's mechanism of action, pharmacokinetics, and its role in treating endometriosis and uterine fibroids.
4) Bleeding:
Bleeding refers to the loss of blood, which can be a significant concern in conditions like uterine fibroids and endometriosis. The review highlights Elagolix sodium's use in treating heavy menstrual bleeding (HMB), demonstrating its importance in managing symptoms related to these reproductive health issues.
5) Dysmenorrhea (Dysmenorrhoea):
Dysmenorrhea is the medical term for painful menstrual cramps, a common symptom in women with endometriosis. The review discusses how Elagolix sodium effectively reduces dysmenorrhea, showcasing its therapeutic relevance in improving women's health and alleviating significant discomfort associated with menstrual cycles.
6) Disease:
Disease denotes a pathological condition that disrupts normal bodily functions, often associated with specific symptoms and signs. Endometriosis and uterine fibroids are addressed in the review as estrogen-dependent diseases that significantly impact women's health, warranting effective treatments like Elagolix to mitigate their symptoms.
7) Blood:
Blood is a vital fluid in the body, responsible for transporting oxygen, nutrients, and waste. In the context of this review, the analysis of blood parameters and menstrual blood loss is crucial for understanding conditions like endometriosis and uterine fibroids and the effects of treatments such as Elagolix.
8) Mud:
Mood refers to a temporary emotional state that can influence overall well-being. The review notes mood alterations and depressive symptoms as common side effects of Elagolix sodium. Recognizing these effects is essential in assessing treatment tolerability for women experiencing reproductive health issues.
9) Relative:
Relative refers to a comparative context. In the review, relative comparisons of clinical responses highlight the effectiveness of Elagolix sodium against placebo treatments. Understanding these relationships is vital for assessing the drug's efficacy in managing endometriosis-related pain and symptoms.
10) Life:
Life encompasses the condition and experiences of living beings. This review emphasizes improving the quality of life for women suffering from endometriosis and uterine fibroids. Effective management of associated symptoms through treatments like Elagolix sodium is essential for enhancing overall well-being and daily functioning.
11) Pharmacology:
Pharmacology is the study of drug action on biological systems. The review provides insights into the clinical pharmacology of Elagolix sodium, detailing its mechanism of action, pharmacokinetics, and pharmacodynamics, relevant for understanding its therapeutic application in managing endometriosis and uterine fibroids.
12) Maharashtra (Maharastra, Maha-rashtra):
Maharashtra is a state in India, highlighted here as the location of the research institution involved in the study. The inclusion of geographical context provides insight into the demographic and cultural factors that may influence the presentation and management of reproductive health issues in women.
13) Nausea:
Nausea is an unpleasant sensation often leading to vomiting. The review notes nausea as a common side effect associated with Elagolix sodium treatment. Understanding and managing side effects like nausea is critical in ensuring adherence to medication and overall patient satisfaction in clinical practice.
14) India:
India is a country that serves as the geographical context for the research conducted and discussed in the review. Understanding the healthcare landscape in India, including access to treatments like Elagolix sodium, is important for managing reproductive health issues in its population.
15) Dhule:
Dhule is a city in the state of Maharashtra, India. The review connects specific author affiliations and research activities to this location, emphasizing the importance of regional context in the evaluation and dissemination of research findings regarding women's health and reproductive disorders.
16) Accumulation (Accumulating, Accumulate):
Accumulate means to gather or pile up over time. The review mentions the accumulation of hormones influenced by Elagolix sodium treatment, striving to explain how controlling hormone levels plays a pivotal role in managing symptoms of reproductive health disorders like endometriosis.
17) Quality:
Quality pertains to the standard of something as measured against other things. The review underscores improving the quality of life for women affected by endometriosis and fibroids through effective treatments, aligning treatment goals with patients' aspirations for relief from debilitating symptoms.
18) Table:
A table presents data visually for easy reference and comparison. The review likely contains tables summarizing pharmacokinetic parameters or clinical outcomes, aiding in clarifying the effects and efficacy of Elagolix sodium, enhancing understanding and analysis for readers and practitioners alike.
19) Line:
Line, in the context of clinical research, often refers to a particular approach or understanding of treatment protocols. The review delineates treatment lines and their progression in managing endometriosis, indicating how various therapies fit into the broader therapeutic landscape for reproductive health.
20) Menstrual blood:
Menstrual blood is shed during a woman's menstrual cycle. The review discusses significant issues related to pelvic pain and heavy menstrual bleeding in endometriosis, emphasizing the need for effective management strategies to address physical symptomatology in affected women.
21) Depression:
Depression is a mood disorder characterized by persistent sadness. The review indicates that depressive symptoms may arise as common adverse reactions to treatments like Elagolix sodium, which must be monitored and managed to mitigate risks and improve overall patient satisfaction and quality of life.
22) Pregnant:
Pregnant refers to the condition of carrying a developing embryo or fetus. The review indicates Elagolix sodium is contraindicated during pregnancy due to potential risks, stressing the importance of understanding the implications of drug treatments in reproductive-age populations seeking to conceive.
23) Anxiety:
Anxiety is an emotional condition characterized by feelings of worry and fear. The review mentions anxiety as a possible side effect of Elagolix sodium, necessitating awareness around mental health implications and the importance of supporting psychological well-being in patients undergoing treatment.
24) Reason:
Reason refers to a rational explanation for something. In this context, the review explores the reasons for developing treatments like Elagolix sodium specifically to target pain and other symptoms associated with endometriosis, highlighting the need for effective management strategies in women's health.
25) Medium:
Medium can refer to a method or a means of achieving something. In pharmacology, it may relate to how drugs are administered or absorbed; in this review, it may contextually emphasize the importance of Elagolix sodium's medium effectiveness in managing estrogen suppression.
26) Water:
Water is essential for biological processes, including drug absorption and metabolism. The review mentions that Elagolix sodium is freely soluble in water, indicating its pharmacokinetic properties, thus facilitating quick absorption necessary for its therapeutic efficacy in treating endometriosis-related symptoms.
27) Sweating (Sweat):
Sweat refers to the liquid secreted by sweat glands to regulate body temperature. In the context of the review, it may address side effects of treatments like Elagolix sodium, with hot flashes and excessive sweating noted, presenting challenges in managing the comfort of patients undergoing therapy.
28) Food:
Food can influence drug absorption, metabolism, and the overall effectiveness of treatment regimens. The review indicates that the bioavailability of Elagolix sodium is not significantly impacted by food, aiming to reassess dietary considerations for patients taking this medication for managing reproductive health issues.
29) Sign:
Sign refers to an indication or a symptom of a condition. In the medical context of the review, signs of endometriosis or treatment side effects need thorough monitoring. Understanding how these signs correlate with effective treatment responses is essential for optimizing patient care.
30) Inflammation:
Inflammation is an immune response often characterized by redness and swelling. In endometriosis, chronic inflammation is prevalent. The review emphasizes controlling inflammation as part of treatment with Elagolix sodium to mitigate associated pain and improve overall health outcomes in affected women.
31) Annihilation (Annihilated, Annihilate):
Annihilate refers to completely destroying or obliterating. In the context of this review, it could discuss the need to annihilate pain or symptoms associated with endometriosis through effective treatments like Elagolix sodium, thereby enhancing women's quality of life and functioning.
32) Composite:
Composite refers to something made from various parts or elements. In the context of the review, a composite score may be used to evaluate overall symptoms in clinical trials involving Elagolix sodium, allowing for comprehensive assessments of treatment efficacy across multiple parameters.
33) Mineral:
Mineral references essential inorganic substances necessary for various biological functions. The review notes concerns regarding bone mineral density (BMD) when using Elagolix sodium, highlighting the importance of monitoring mineral levels in conjunction with managing side effects associated with treatment.
34) Cancer:
Cancer is a group of diseases characterized by uncontrolled cell growth. The review shows awareness of cancer through its discussion of endometriosis, as the conditions linked to hormonal imbalances require monitoring and may raise concerns regarding potential relationships with reproductive cancers in women.
35) Nature:
Nature refers to the inherent characteristics or qualities of something. This review discusses the nature of endometriosis and uterine fibroids as estrogen-dependent conditions, emphasizing the biological underpinnings central to developing targeted treatments and therapeutic approaches.
36) Animal:
Animal may refer to specific models used in scientific research. The review indirectly relates this term to the context of pharmacokinetics and drug testing, emphasizing the importance of preclinical studies involving animal models to explore efficacy and safety before human trials.
37) Salt (Salty):
Salt may represent an ionic compound critical for various biological processes. In pharmacology, the term can indicate a drug's formulation, such as Elagolix sodium, where the salt form enhances solubility and bioavailability, impacting absorption and therapeutic efficacy.
38) Pur:
Poor refers to substandard conditions or outcomes. In the context of the review, poor health outcomes or inadequate treatment response in women suffering from endometriosis highlight the necessity for effective therapies like Elagolix sodium to improve overall reproductive health and manage debilitating symptoms.