Products
Progestogens are commercially available in the form of tablets, capsules, transdermal patches and gels, vaginal rings, injectables, and vaginal preparations, among others. They are contained in hormonal contraceptives, on the one hand in mono- and on the other hand in combination preparations.
Structure and properties
Progestins are steroid hormones. The lead substance is the female sex hormone progesterone. In drugs, progestins are often present as esters. Synthetic derivatives are also called progestins. They are structurally derived, for example, from progesterone, testosterone, and spironolactone.
Effects
Progestins (ATC G03D) have contraceptive properties. The effects are primarily due to inhibition of ovulation. Furthermore, they also increase the viscosity of cervical mucus. Progesterone causes the conversion of a proliferative to a secretory endometrium in the female cycle. It maintains pregnancy. Progestins can have various partial effects. This applies differently to different agents:
- Antimineralocorticoid
- Androgen or antiandrogen
- Glucocorticoid
- Estrogen
The progestogenic effects are due to binding to intracellular progesterone receptors. They interact with DNA and promote protein expression. In addition, membrane progesterone receptors exist. Progresterone release from the corpus luteum is regulated by the hypothalamus and anterior pituitary with luteinizing hormone (LH).
Indications
Indications for use of progestogens (selection):
- For hormonal contraception.
- For emergency contraception (“morning-after pill”).
- For hormone replacement therapy during menopause or after an ovariectomy.
- Disorders of the female cycle, bleeding disorders.
- Ovulation disorders and disorders of fertility.
- Pain in the female breast area due to local progesterone deficiency without breast tissue changes.
- Premenstrual syndrome.
- Endometriosis.
- Menstrual cramps (dysmenorrhea).
- In the context of artificial insemination.
Off-label use:
- For the prevention of preterm birth during pregnancy.
- For sex reassignment surgery in males.
Dosage
According to the SmPC. Progestins are administered perorally, transdermally, intramuscularly, vaginally, and topically. For some indications, combination with an estrogen is required.
Active Ingredients
- Chlormadinone acetate (e.g. Belara).
- Cyproterone acetate (e.g. Androcur, Diane-35).
- Desogestrel (Cerazette, generics).
- Dienogest (e.g. Qlaira)
- Drospirenone (Yasmin, Yasminelle, generics).
- Dydrogesterone (Duphaston)
- Etonogestrel (Implanon, NuvaRing)
- Gestodene (hormonal contraceptives, eg Gynera).
- Levonorgestrel (generic, “morning after pill”).
- Medroxyprogesterone acetate (three-month injection).
- Nomegestrol acetate (Zoely)
- Norethisterone (Primolut)
- Norgestimate (out of trade)
- Norgestrel (Cyclacur)
- Norelgestromin (Evra)
- Progesterone (e.g., Utrogestan, Progestogel).
- Ulipristal acetate (ellaOne, “morning after pill”).
Contraindications
Contraindications include (selection):
- Hypersensitivity
- Cancers of the breast or other sex hormone-sensitive malignancies
- Unexplained vaginal bleeding
- Liver tumors
- Severe liver disease
- Acute venous thromboembolic events
- Pregnancy (depending on the product)
Full precautions can be found in the drug label.
Interactions
Some progestins, such as progesterone, are substrates of CYP450 and susceptible to interactions with CYP inducers or inhibitors.
Adverse effects
The following is a list of possible adverse effects of progestogens. They may differ depending on the profile of action:
- Weight gain
- Mood swings, depressed mood, decreased libido.
- Headache, dizziness
- Nausea, vomiting, abdominal pain
- Acne
- Irregular bleeding, amenorrhea
- Liver dysfunction
- Chest pain
