Cismadinone

Cismadinone is a synthetic progestogen, a type of hormone that plays a key role in the menstrual cycle and in maintaining the early stages of pregnancy. It is a derivative of progesterone, the natural female sex hormone, and is used in various contraceptive and hormone replacement therapies. Cismadinone is known for its high progestational activity, making it effective in treating conditions related to hormone imbalance.

Medical Uses[edit | edit source]

Cismadinone is primarily used in combined oral contraceptives and in hormone replacement therapy (HRT) for menopausal symptoms. It is also used in the treatment of Endometriosis, a condition where tissue similar to the lining inside the uterus is found outside the uterus, causing pain and infertility. Additionally, it may be prescribed for Amenorrhea (absence of menstruation), Dysmenorrhea (painful menstruation), and to counteract the effects of estrogen in conditions such as Estrogen Dominance.

Mechanism of Action[edit | edit source]

Cismadinone acts by binding to the progesterone receptors in the uterus, breast, and other parts of the body. This binding inhibits the secretion of Gonadotropin-releasing hormone (GnRH) from the hypothalamus and the subsequent release of Follicle-stimulating hormone (FSH) and Luteinizing hormone (LH) from the pituitary gland. As a result, ovulation is prevented, making cismadinone effective as a contraceptive. Additionally, it thickens the cervical mucus, making it difficult for sperm to enter the uterus, and alters the endometrium, preventing implantation of a fertilized egg.

Side Effects[edit | edit source]

Like all medications, cismadinone can cause side effects, although not everybody gets them. Common side effects include Nausea, Headache, Breast tenderness, and mood changes. Less common but more serious side effects may include Venous thromboembolism, Stroke, and Liver problems. Patients are advised to consult their healthcare provider if they experience any adverse effects.

Pharmacokinetics[edit | edit source]

Cismadinone is well absorbed from the gastrointestinal tract and is subject to first-pass metabolism in the liver. It binds extensively to plasma proteins, particularly Sex hormone-binding globulin (SHBG) and Albumin. The elimination half-life of cismadinone is relatively long, allowing for once-daily dosing in most therapeutic applications.

History[edit | edit source]

Cismadinone was developed in the 1960s as part of the search for more potent progestogens with improved pharmacokinetic properties. It was introduced for medical use in the 1970s and has since been used in various formulations for contraception and hormone replacement therapy.