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Birth Control Methods01:22

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Vasectomy is a surgical form of male sterilization that involves severing and sealing the vasa deferentia, preventing sperm from mixing with semen during ejaculation. Because a vasectomy does not impact the testes' ability to produce testosterone, hormone levels, libido, and sexual function generally remain unchanged. While vasectomy is highly effective in preventing pregnancy, with a success rate near 99.85%, rare cases of recanalization (spontaneous reconnection) can occur. Although...
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Hormonal Control of the Ovarian Cycle01:30

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The ovarian cycle is meticulously regulated by the hypothalamic-pituitary-gonadal axis. This cycle orchestrates the release of a mature oocyte, essential for reproduction.
Before puberty, the hypothalamus releases GnRH in a low frequency, low amplitude pulsatile manner. This along with the immature hypothalamic-pituitary-gonadal axis activity, results in low estrogen levels and the absence of a fully functional ovarian cycle.  At puberty, GnRH secretion increases in both frequency and...
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Combined Effects of Drugs: Synergism01:27

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Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
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Hormonal Regulation of the Menstrual Cycle01:22

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The ovarian cycle regulates endometrial changes throughout a single menstrual cycle via the coordinated action of gonadotrophin-releasing hormone (GnRH) and gonadotrophins.
At puberty, GnRH begins a pulsatile release pattern, which triggers the anterior pituitary gland to secrete follicle-stimulating hormone (FSH) and luteinizing hormone (LH). The frequency and amplitude of GnRH pulses vary across the menstrual cycle, with faster pulses favoring LH release and slower pulses favoring FSH...
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Factors Influencing Drug Absorption: Presystemic Elimination01:24

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The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
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Oral Hypoglycemic Agents: Sulfonylureas01:17

Oral Hypoglycemic Agents: Sulfonylureas

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Sulfonylureas are oral hypoglycemic agents utilized in treating type 2 diabetes. They are characterized by their unique sulfonylurea chemical structure. The family of sulfonylureas is divided into generations. First-generation sulfonylureas, including tolbutamide (Orinase), chlorpropamide (Diabinese), and tolazamide (Tolinase), trigger insulin release from pancreatic β cells and enhance peripheral tissues' insulin sensitivity. The second-generation members, such as glipizide...
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Related Experiment Video

Updated: Jun 16, 2025

Fertility Preservation Through Oocyte Vitrification: Clinical and Laboratory Perspectives
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Hormonal contraception, past, present, and future part 2: optimizing combined oral contraceptives to decrease risks

Manuela Farris1, Carlo Bastianelli2, Marwan Habiba3

  • 1Obstetrics and Gynaecology, Unicamillus. Saint Camillus International University of Health and Medicine, Rome, Italy.

Expert Review of Clinical Pharmacology
|June 10, 2025
PubMed
Summary
This summary is machine-generated.

Oral contraceptives evolved from natural progesterone to synthetic progestins and estrogens due to clinical limitations. Research continues to balance efficacy and safety, considering various progestin properties for combined oral contraceptives (COC).

Keywords:
Hormonal contraceptionadverse effectscontraceptive pillestrogensethinyl estradiolpill scareprogestinsvenous thromboembolism

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Area of Science:

  • Reproductive endocrinology
  • Pharmacology of hormonal contraception

Background:

  • Initial hormonal contraception research focused on progesterone, but its poor oral availability and side effects necessitated synthetic progestins.
  • Combined oral contraceptives (COC) were developed with estrogen (ethinyl estradiol) for cycle control, but early concerns about thromboembolism arose.
  • Adverse events have been reported for newer progestins, prompting comparisons with established options like levonorgestrel.

Purpose of the Study:

  • To review the historical development and pharmacological considerations of combined oral contraceptives (COC).
  • To discuss the evolution of progestin and estrogen components in COC formulations.
  • To highlight the challenges in comparing different COC preparations due to varied progestin activity profiles.

Main Methods:

  • Literature review of historical research and clinical use of hormonal contraceptives.
  • Analysis of pharmacological properties of different progestins and estrogens.
  • Examination of reported adverse events and risk-benefit profiles of various COC formulations.

Main Results:

  • The shift from natural progesterone to orally active progestins and the addition of ethinyl estradiol (EE) marked significant advancements in contraception.
  • Concerns regarding EE-induced thromboembolism led to reduced EE content in COCs.
  • Different progestins exhibit unique androgenic, antiandrogenic, antiestrogenic, and mineralocorticoid activities, influencing their risk-benefit profiles.

Conclusions:

  • The development of COCs involved overcoming challenges with natural compounds, leading to synthetic alternatives with improved efficacy and cycle control.
  • Ongoing research and formulation changes aim to minimize side effects, particularly thromboembolism associated with the estrogenic component.
  • The diverse pharmacological profiles of progestins necessitate careful consideration when selecting COC formulations for individual patient needs.