Drospirenone/estetrol

Last updated

Drospirenone/estetrol
Combination of
Drospirenone Progestogen
Estetrol (medication) Estrogen
Clinical data
Trade names Nextstellis, Drovelis, Lydisilka, others
Other namesE4/DRSP; FSN-013
AHFS/Drugs.com Monograph
License data
Pregnancy
category
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Identifiers
ChemSpider
  • None
KEGG

Drospirenone/estetrol, sold under the brand name Nextstellis, among others, is a fixed-dose combination medication containing drospirenone, a progestin, and estetrol, an estrogen, which is used as a combined birth control pill for the prevention of pregnancy in women. [2] [6] It is taken by mouth. [2] [6]

Contents

It was approved for medical use in Canada in March 2021, [3] and in the United States in April 2021. [6]

Medical uses

Drospirenone/estetrol is used as a combined birth control pill to prevent pregnancy in women. [2] [6]

Side effects

Estetrol-containing birth control pills, similarly to estradiol-containing birth control pills, may have a lower risk of venous thromboembolism (VTE) than ethinylestradiol-containing birth control pills based on studies of coagulation. [11] [12] However, it is likely that another decade will be required before post-marketing epidemiological studies of VTE incidence with these birth control pills are completed and able to confirm this. [13]

Pharmacology

Pharmacodynamics

Drospirenone/estetrol has a much lower impact on liver protein synthesis, including of sex hormone-binding globulin, angiotensinogen, and coagulation factors, than does ethinylestradiol/drospirenone. [14]

Society and culture

Drospirenone/estetrol is approved for the use of hormonal contraception in the European Union, [7] [8] the United States, [15] and Canada. [3]

Brand names

Drospirenone/estetrol in sold under the brand names Nexstellis, [3] Drovelis, [7] and Lydisilka. [8]

See also

Related Research Articles

<span class="mw-page-title-main">Combined oral contraceptive pill</span> Birth control method which is taken orally

The combined oral contraceptive pill (COCP), often referred to as the birth control pill or colloquially as "the pill", is a type of birth control that is designed to be taken orally by women. It is the oral form of combined hormonal contraception. The pill contains two important hormones: a progestin and estrogen. When taken correctly, it alters the menstrual cycle to eliminate ovulation and prevent pregnancy.

<span class="mw-page-title-main">Ethinylestradiol</span> Estrogen medication

Ethinylestradiol (EE) is an estrogen medication which is used widely in birth control pills in combination with progestins. In the past, EE was widely used for various indications such as the treatment of menopausal symptoms, gynecological disorders, and certain hormone-sensitive cancers. It is usually taken by mouth but is also used as a patch and vaginal ring.

<span class="mw-page-title-main">Drospirenone</span> Medication drug

Drospirenone is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy and in menopausal hormone therapy, among other uses. It is available both alone under the brand name Slynd and in combination with an estrogen under the brand name Yasmin among others. The medication is an analog of the drug spironolactone. Drospirenone is taken by mouth.

<span class="mw-page-title-main">Norethisterone acetate</span> Chemical compound

Norethisterone acetate (NETA), also known as norethindrone acetate and sold under the brand name Primolut-Nor among others, is a progestin medication which is used in birth control pills, menopausal hormone therapy, and for the treatment of gynecological disorders. The medication available in low-dose and high-dose formulations and is used alone or in combination with an estrogen. It is ingested orally.

<span class="mw-page-title-main">Activated protein C resistance</span> Medical condition

Activated protein C resistance (APCR) is a hypercoagulability characterized by a lack of a response to activated protein C (APC), which normally helps prevent blood from clotting excessively. This results in an increased risk of venous thrombosis, which resulting in medical conditions such as deep vein thrombosis and pulmonary embolism. The most common cause of hereditary APC resistance is factor V Leiden mutation.

<span class="mw-page-title-main">Mestranol</span> Chemical compound

Mestranol, sold under the brand names Enovid, Norinyl, and Ortho-Novum among others, is an estrogen medication which has been used in birth control pills, menopausal hormone therapy, and the treatment of menstrual disorders. It is formulated in combination with a progestin and is not available alone. It is taken by mouth.

<span class="mw-page-title-main">Drospirenone/ethinylestradiol/levomefolic acid</span> Pharmaceutical combination

Drospirenone/ethinylestradiol/levomefolic acid (EE/DRSP/LMF), sold under the brand name Beyaz among others, is a combination of ethinylestradiol (EE), an estrogen, drospirenone (DRSP), a progestogen, antimineralocorticoid, and antiandrogen, and levomefolic acid (LMF), a form of vitamin B9, which is used as a birth control pill to prevent pregnancy in women. The formulation contains folate as the calcium salt of levomefolic acid to lower the risk of complications such as fetal neural tube defects should the medication fail as a form of birth control. EE/DRSP/LMF was approved for use by the US Food and Drug Administration (FDA) in September 2010.

<span class="mw-page-title-main">Nomegestrol acetate/estradiol</span> Combination drug

Nomegestrol acetate/estradiol (NOMAC-E2), sold under the brand names Naemis and Zoely among others, is a fixed-dose combination medication of nomegestrol acetate, a progestogen, and estradiol, an estrogen, which is used in menopausal hormone therapy and as a birth control pill to prevent pregnancy in women. It is taken by mouth.

Combined birth control pills that contain natural estradiol or an estradiol ester include:

<span class="mw-page-title-main">Estradiol (medication)</span> Steroidal hormone medication

Estradiol (E2) is a medication and naturally occurring steroid hormone. It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women. It is also used in hormonal birth control for women, in feminizing hormone therapy for transgender women, and in the treatment of hormone-sensitive cancers like prostate cancer in men and breast cancer in women, among other uses. Estradiol can be taken by mouth, held and dissolved under the tongue, as a gel or patch that is applied to the skin, in through the vagina, by injection into muscle or fat, or through the use of an implant that is placed into fat, among other routes.

<span class="mw-page-title-main">Combined hormonal contraception</span> Form of hormonal contraception combining both an estrogen and a progestogen

Combined hormonal contraception (CHC), or combined birth control, is a form of hormonal contraception which combines both an estrogen and a progestogen in varying formulations.

<span class="mw-page-title-main">Estetrol (medication)</span> Estrogen medication

Estetrol (E4) is an estrogen medication and naturally occurring steroid hormone which is used in combination with a progestin in combined birth control pills and is under development for various other indications. These investigational uses include menopausal hormone therapy to treat symptoms such as vaginal atrophy, hot flashes, and bone loss and the treatment of breast cancer and prostate cancer. It is taken by mouth.

<span class="mw-page-title-main">Estradiol valerate/dienogest</span> Combination drug

Estradiol valerate/dienogest (EV/DNG), sold under the brand names Lafamme, Natazia and Qlaira among others, is a combination product of estradiol valerate, an estrogen, and dienogest, a progestogen, which is used in menopausal hormone therapy in and as a birth control pill to prevent pregnancy in women. It is taken by mouth.

<span class="mw-page-title-main">Ethinylestradiol/cyproterone acetate</span> Combination drug

Ethinylestradiol/cyproterone acetate (EE/CPA), also known as co-cyprindiol and sold under the brand names Diane and Diane-35 among others, is a combination of ethinylestradiol (EE), an estrogen, and cyproterone acetate (CPA), a progestin and antiandrogen, which is used as a birth control pill to prevent pregnancy in women. It is also used to treat androgen-dependent conditions in women such as acne, seborrhea, excessive facial/body hair growth, scalp hair loss, and high androgen levels associated with ovaries with cysts. The medication is taken by mouth once daily for 21 days, followed by a 7-day free interval.

Ethinylestradiol/drospirenone/prasterone (EE/DRSP/DHEA), known under developmental code names like Androgen Restored Contraceptive (ARC), Female Balance Pill, Pill-Plus, and Triple Oral Contraceptive, is a combination of ethinylestradiol (EE), an estrogen, drospirenone (DRSP), a progestin, antimineralocorticoid, and antiandrogen, and prasterone, an androgen prohormone and neurosteroid, which is under development for use as a birth control pill to prevent pregnancy in women. Clinical studies of this formulation have been conducted and published. Estrogens and progestogens suppress testosterone levels in women, and the addition of 50 mg prasterone, an oral prohormone of testosterone, has been found to restore total testosterone levels to normal levels. However, free testosterone levels, although higher with the addition of prasterone, remain significantly lower than usual despite prasterone inclusion.

<span class="mw-page-title-main">Ethinylestradiol/megestrol acetate</span> Combination drug

Ethinylestradiol/megestrol acetate (EE/MGA), sold under the brand name Volidan among others, was a combination of ethinylestradiol (EE), an estrogen, and megestrol acetate (MGA), a progestin, which was used as a birth control pill to prevent pregnancy in women. It was taken by mouth and contained 50 to 100 μg EE and 1 to 5 mg MGA per tablet. MGA-containing birth control pills were withdrawn after reports in the early 1970s of a high incidence of venous thromboembolism in association with the preparations.

The activated protein C resistance (APCR) test is a coagulation test used in the evaluation and diagnosis of activated protein C (APC) resistance, a form of hypercoagulability. Hereditary APC resistance is usually caused by the factor V Leiden mutation, whereas acquired APC resistance has been linked to antiphospholipid antibodies, pregnancy, and estrogen therapy. APC resistance can be measured using either an activated partial thromboplastin time (aPTT)-based test or an endogenous thrombin potential (ETP)-based test.

Fibrin monomers are monomers of fibrin which are formed by the cleavage of fibrinogen by thrombin. Levels of fibrin monomers can be measured using blood tests and can serve as a marker of in vivo fibrinogenesis and coagulation activation. They may be useful in the evaluation of hypercoagulability, as reflected in research studies done using fibrin monomers.

Coagulation activation markers are biomarkers of net activation of coagulation and fibrinolysis. Examples include prothrombin fragment 1+2 (F1+2), thrombin–antithrombin complex (TAT), fibrinopeptide A (FpA), fibrin monomers (FMs), plasmin-α2-antiplasmin complex (PAP), activated protein C–protein C inhibitor (APC-PCI), and D-dimer (DD). These compounds are markers of thrombin generation, fibrin generation, and fibrinolysis. Coagulation activation markers, particularly D-dimer, are useful in the diagnosis of acute venous thromboembolism. They may also be useful in the assessment of hypercoagulability and venous thromboembolism risk.

References

  1. 1 2 "Nextstellis". Therapeutic Goods Administration (TGA). 6 December 2021. Archived from the original on 28 December 2021. Retrieved 28 December 2021.
  2. 1 2 3 4 "PRODUCT MONOGRAPH INCLUDING PATIENT MEDICATION INFORMATION NEXTSTELLIS" (PDF). 5 March 2021. Archived (PDF) from the original on 9 July 2022. Retrieved 4 July 2024.
  3. 1 2 3 4 "Nextstellis Product information". Health Canada. 25 April 2012. Archived from the original on 22 September 2021. Retrieved 4 November 2021.
  4. "Summary Basis of Decision (SBD) for Nextstellis". Health Canada . 23 October 2014. Archived from the original on 30 May 2022. Retrieved 29 May 2022.
  5. "Health product highlights 2021: Annexes of products approved in 2021". Health Canada . 3 August 2022. Archived from the original on 25 March 2024. Retrieved 25 March 2024.
  6. 1 2 3 4 5 "Nextstellis- drospirenone and estetrol kit". DailyMed. Archived from the original on 2 June 2021. Retrieved 1 June 2021.
  7. 1 2 3 "Drovelis EPAR". European Medicines Agency (EMA). 24 March 2021. Archived from the original on 4 November 2021. Retrieved 4 November 2021.
  8. 1 2 3 "Lydisilka EPAR". European Medicines Agency (EMA). 24 March 2021. Archived from the original on 4 November 2021. Retrieved 4 November 2021.
  9. "Drovelis Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
  10. "Lydisilka Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
  11. Morimont L, Haguet H, Dogné JM, Gaspard U, Douxfils J (2021). "Combined Oral Contraceptives and Venous Thromboembolism: Review and Perspective to Mitigate the Risk". Front Endocrinol (Lausanne). 12: 769187. doi: 10.3389/fendo.2021.769187 . PMC   8697849 . PMID   34956081.
  12. Douxfils J, Morimont L, Bouvy C (November 2020). "Oral Contraceptives and Venous Thromboembolism: Focus on Testing that May Enable Prediction and Assessment of the Risk". Semin Thromb Hemost. 46 (8): 872–886. doi:10.1055/s-0040-1714140. PMID   33080636. S2CID   224821517.
  13. Grandi G, Facchinetti F, Bitzer J (February 2022). "Confirmation of the safety of combined oral contraceptives containing oestradiol on the risk of venous thromboembolism". Eur J Contracept Reprod Health Care. 27 (2): 83–84. doi: 10.1080/13625187.2022.2029397 . PMID   35133236. S2CID   246651102. Moreover, the introduction of other new natural oestrogenic components, such as estetrol (E4) [12], could have a similar lower VTE impact; however, we will likely need another decade to obtain results from post-marketing studies.
  14. Farris M, Bastianelli C, Rosato E, Brosens I, Benagiano G (October 2017). "Pharmacodynamics of combined estrogen-progestin oral contraceptives: 2. effects on hemostasis". Expert Rev Clin Pharmacol. 10 (10): 1129–1144. doi:10.1080/17512433.2017.1356718. PMID   28712325. S2CID   205931204.
  15. "Drug Approval Package: Nextstellis". U.S. Food & Drug Administration (FDA). 12 May 2021. Archived from the original on 6 November 2021. Retrieved 30 November 2021.