Dienogest
Encyclopedia
Dienogest is an orally active synthetic progesterone
(or progestin
). It is available for use as an oral contraceptive
in combination with ethinylestradiol
. It has antiandrogen
ic activity and as a result can improve androgen
ic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone
. Dienogest given in isolation is available for the treatment of endometriosis
under the trade name Visanne.
, Germany
under the leadership of Prof. Kurt Ponsold, was initially referred to as STS 557. It was found that its potency was 10 times that of levonorgestrel
. The first product on the market to contain dienogest as a contraceptive pill Valette in 1995 made by Jenapharm
. It has been little used outside of Germany.
. It is given as a tablet containing 2 mg of dienogest and 30 μg of ethinylestradiol.
The minimum dose required to inhibit ovulation has been found to be approximately 1 mg
. It has been shown to be equally effective as leuprorelin, which is a second line
medication against endometriosis.
in human uterus tissue, in vitro
, about 10% that of progesterone.
is 1 mg/day. The inhibition of ovulation by dienogest occurs mainly via peripheral action as opposed to central action on gonadotrophin secretion.
Oral treatment of dienogest 2 mg/day in cyclical women reduced serum progesterone levels to anovulatory
levels, however serum levels of lutenising hormone
and follicle-stimulating hormone
are not significantly altered.
Progesterone
Progesterone also known as P4 is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy and embryogenesis of humans and other species...
(or progestin
Progestin
A progestin is a synthetic progestogen that has progestinic effects similar to progesterone. The two most common uses of progestins are for hormonal contraception , and to prevent endometrial hyperplasia from unopposed estrogen in hormone replacement therapy...
). It is available for use as an oral contraceptive
Birth control
Birth control is an umbrella term for several techniques and methods used to prevent fertilization or to interrupt pregnancy at various stages. Birth control techniques and methods include contraception , contragestion and abortion...
in combination with ethinylestradiol
Ethinylestradiol
Ethynylestradiol , also ethynyl estradiol , is a derivative of estradiol. Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills...
. It has antiandrogen
Antiandrogen
Antiandrogens, or androgen antagonists, first discovered in the 1960s, prevent androgens from expressing their biological effects on responsive tissues. Antiandrogens alter the androgen pathway by blocking the appropriate receptors, competing for binding sites on the cell's surface, or affecting...
ic activity and as a result can improve androgen
Androgen
Androgen, also called androgenic hormone or testoid, is the generic term for any natural or synthetic compound, usually a steroid hormone, that stimulates or controls the development and maintenance of male characteristics in vertebrates by binding to androgen receptors...
ic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...
. Dienogest given in isolation is available for the treatment of endometriosis
Endometriosis
Endometriosis is a gynecological medical condition in which cells from the lining of the uterus appear and flourish outside the uterine cavity, most commonly on the ovaries. The uterine cavity is lined by endometrial cells, which are under the influence of female hormones...
under the trade name Visanne.
History
Dienogest was synthesised in 1979 in JenaJena
Jena is a university city in central Germany on the river Saale. It has a population of approx. 103,000 and is the second largest city in the federal state of Thuringia, after Erfurt.-History:Jena was first mentioned in an 1182 document...
, Germany
Germany
Germany , officially the Federal Republic of Germany , is a federal parliamentary republic in Europe. The country consists of 16 states while the capital and largest city is Berlin. Germany covers an area of 357,021 km2 and has a largely temperate seasonal climate...
under the leadership of Prof. Kurt Ponsold, was initially referred to as STS 557. It was found that its potency was 10 times that of levonorgestrel
Levonorgestrel
Levonorgestrel is a second generation synthetic progestogen used as an active ingredient in some hormonal contraceptives.-Chemistry:...
. The first product on the market to contain dienogest as a contraceptive pill Valette in 1995 made by Jenapharm
Jenapharm
Jenapharm is a pharmaceutical company from Jena, Germany. Founded in 1950 in East Germany, the company focused from the beginning on the production and development of steroids...
. It has been little used outside of Germany.
Contraception
Dienogest is used primarily as a contraceptive in combination with ethinylestradiolEthinylestradiol
Ethynylestradiol , also ethynyl estradiol , is a derivative of estradiol. Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills...
. It is given as a tablet containing 2 mg of dienogest and 30 μg of ethinylestradiol.
The minimum dose required to inhibit ovulation has been found to be approximately 1 mg
Endometriosis
Dienogest is also approved in the European Union for the treatment of endometriosisEndometriosis
Endometriosis is a gynecological medical condition in which cells from the lining of the uterus appear and flourish outside the uterine cavity, most commonly on the ovaries. The uterine cavity is lined by endometrial cells, which are under the influence of female hormones...
. It has been shown to be equally effective as leuprorelin, which is a second line
Second line
Second line is a tradition in brass band parades in New Orleans, Louisiana. The "main line" is the main section of the parade, or the members of the actual club with the parading permit;...
medication against endometriosis.
Progestational activity
Dienogest has moderate affinity for the progesterone receptorProgesterone receptor
The progesterone receptor also known as NR3C3 , is an intracellular steroid receptor that specifically binds progesterone...
in human uterus tissue, in vitro
In vitro
In vitro refers to studies in experimental biology that are conducted using components of an organism that have been isolated from their usual biological context in order to permit a more detailed or more convenient analysis than can be done with whole organisms. Colloquially, these experiments...
, about 10% that of progesterone.
Inhibition of ovulation
The minimum effective dose of oral dienogest required to inhibit ovulationOvulation
Ovulation is the process in a female's menstrual cycle by which a mature ovarian follicle ruptures and discharges an ovum . Ovulation also occurs in the estrous cycle of other female mammals, which differs in many fundamental ways from the menstrual cycle...
is 1 mg/day. The inhibition of ovulation by dienogest occurs mainly via peripheral action as opposed to central action on gonadotrophin secretion.
Oral treatment of dienogest 2 mg/day in cyclical women reduced serum progesterone levels to anovulatory
Anovulation
An anovulatory cycle is a menstrual cycle during which the ovaries do not release an oocyte. Therefore, ovulation does not take place. However, a woman who does not ovulate at each menstrual cycle is not necessarily going through menopause...
levels, however serum levels of lutenising hormone
Luteinizing hormone
Luteinizing hormone is a hormone produced by the anterior pituitary gland. In females, an acute rise of LH called the LH surge triggers ovulation and development of the corpus luteum. In males, where LH had also been called interstitial cell-stimulating hormone , it stimulates Leydig cell...
and follicle-stimulating hormone
Follicle-stimulating hormone
Follicle-stimulating hormone is a hormone found in humans and other animals. It is synthesized and secreted by gonadotrophs of the anterior pituitary gland. FSH regulates the development, growth, pubertal maturation, and reproductive processes of the body. FSH and Luteinizing hormone act...
are not significantly altered.