Gestodene: Difference between revisions

Latest revision as of 14:15, 21 February 2025

Gestodene[edit]

Gestodene is a synthetic progestogen used in hormonal contraception. It is a third-generation progestin, which is often combined with an estrogen such as ethinylestradiol in combined oral contraceptive pills.

Pharmacology[edit]

Gestodene is known for its high progestogenic activity and low androgenic activity, making it a preferred choice in contraceptive formulations. It works primarily by inhibiting ovulation and altering the endometrium to prevent implantation.

Mechanism of Action[edit]

Gestodene binds to the progesterone receptor in the body, mimicking the effects of natural progesterone. This leads to suppression of the luteinizing hormone (LH) surge, thereby preventing ovulation. Additionally, it increases the viscosity of cervical mucus, making it more difficult for sperm to penetrate.

Clinical Use[edit]

Gestodene is primarily used in contraception. It is available in various formulations, often in combination with ethinylestradiol. These combinations are used to prevent pregnancy and can also regulate menstrual cycles, reduce menstrual pain, and treat acne.

Side Effects[edit]

Common side effects of gestodene include nausea, headache, breast tenderness, and mood changes. As with other hormonal contraceptives, there is a small increased risk of venous thromboembolism (VTE).

Chemistry[edit]

Gestodene is a derivative of 19-nortestosterone and is structurally related to other progestins such as levonorgestrel. It is characterized by the presence of a 17α-ethynyl group, which is crucial for its progestogenic activity.

History[edit]

Gestodene was developed in the 1980s and introduced for medical use in the early 1990s. It was part of the development of third-generation progestins aimed at reducing the androgenic side effects associated with earlier progestins.

Related Pages[edit]

@@ Line 1: / Line 1: @@
 == Gestodene ==
-'''Gestodene''' is a synthetic [[progestogen]] used in [[hormonal contraception]]. It is a third-generation progestin, which is often combined with [[estrogen]]s in [[combined oral contraceptive pill]]s. Gestodene is known for its high progestational activity and low androgenic activity, making it a popular choice in contraceptive formulations.
+[[File:Gestodene.svg|thumb|right|Chemical structure of Gestodene]]
-=== Chemical Properties ===
+'''Gestodene''' is a synthetic [[progestogen]] used in [[hormonal contraception]]. It is a third-generation progestin, which is often combined with an [[estrogen]] such as [[ethinylestradiol]] in [[combined oral contraceptive pill|combined oral contraceptive pills]].
-Gestodene is a derivative of [[19-nortestosterone]], which is a common structural basis for many synthetic progestins. It has the chemical formula C21H26O2 and a molecular weight of 310.43 g/mol. The compound is characterized by its high affinity for the [[progesterone receptor]], which contributes to its effectiveness in preventing ovulation.
-=== Mechanism of Action ===
+=== Pharmacology ===
-Gestodene works primarily by inhibiting [[ovulation]]. It achieves this by suppressing the secretion of [[gonadotropins]] from the [[pituitary gland]], specifically [[luteinizing hormone]] (LH) and [[follicle-stimulating hormone]] (FSH). This suppression prevents the mid-cycle surge of LH, which is necessary for ovulation. Additionally, gestodene induces changes in the [[endometrium]] that make it less suitable for [[implantation]] and thickens the [[cervical mucus]], hindering sperm penetration.
+Gestodene is known for its high [[progestogenic]] activity and low [[androgenic]] activity, making it a preferred choice in contraceptive formulations. It works primarily by inhibiting [[ovulation]] and altering the [[endometrium]] to prevent [[implantation (human embryo)|implantation]].
+==== Mechanism of Action ====
+Gestodene binds to the [[progesterone receptor]] in the body, mimicking the effects of natural [[progesterone]]. This leads to suppression of the [[luteinizing hormone]] (LH) surge, thereby preventing ovulation. Additionally, it increases the viscosity of [[cervical mucus]], making it more difficult for [[sperm]] to penetrate.
 === Clinical Use ===
-Gestodene is used in various formulations of combined oral contraceptives. It is often combined with [[ethinylestradiol]], a synthetic estrogen, to enhance contraceptive efficacy. The typical dosage in contraceptive pills ranges from 60 to 75 micrograms of gestodene, combined with 20 to 30 micrograms of ethinylestradiol.
+Gestodene is primarily used in [[contraception]]. It is available in various formulations, often in combination with ethinylestradiol. These combinations are used to prevent [[pregnancy]] and can also regulate [[menstrual cycle|menstrual cycles]], reduce [[menstrual pain]], and treat [[acne vulgaris|acne]].
 === Side Effects ===
-Like other hormonal contraceptives, gestodene-containing pills may cause side effects. Common side effects include [[nausea]], [[headache]], [[breast tenderness]], and [[mood changes]]. Rare but serious side effects include an increased risk of [[venous thromboembolism]] and [[myocardial infarction]], particularly in smokers and women over 35 years of age.
-=== Advantages ===
+Common side effects of gestodene include [[nausea]], [[headache]], [[breast tenderness]], and [[mood changes]]. As with other hormonal contraceptives, there is a small increased risk of [[venous thromboembolism]] (VTE).
-Gestodene is favored for its minimal androgenic effects, which reduces the risk of side effects such as [[acne]] and [[hirsutism]]. Its high progestational activity allows for lower doses, which can reduce the incidence of side effects associated with higher hormone levels.
+[[File:Gestodeno3D.png|thumb|left|3D model of Gestodene]]
+=== Chemistry ===
+Gestodene is a derivative of [[19-nortestosterone]] and is structurally related to other progestins such as [[levonorgestrel]]. It is characterized by the presence of a [[17α-ethynyl group]], which is crucial for its progestogenic activity.
-=== Pharmacokinetics ===
+=== History ===
-Gestodene is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It is extensively metabolized in the liver and excreted primarily in the urine. The elimination half-life of gestodene is approximately 12 to 14 hours.
-=== Images ===
+Gestodene was developed in the 1980s and introduced for medical use in the early 1990s. It was part of the development of third-generation progestins aimed at reducing the androgenic side effects associated with earlier progestins.
-[[File:Gestodene_structure.png|thumb|right|Chemical structure of gestodene]]
-=== Related Pages ===
+== Related Pages ==
 * [[Progestogen]]
 * [[Combined oral contraceptive pill]]
 * [[Ethinylestradiol]]
-* [[Hormonal contraception]]
+* [[Venous thromboembolism]]
-{{Hormonal contraception}}
+{{Hormonal contraceptives}}
-[[Category:Contraceptives]]
 [[Category:Progestogens]]
+[[Category:Contraception]]