dienogest

Action and Spectrum

Actions and Spectrum: 

dienogest is a progestin, a synthetic hormone that acts similarly to the natural hormone progesterone. It has a variety of actions and affects various organs and systems in the body. 

• Contraception: dienogest is used in combination with estrogen in oral contraceptive pills to prevent pregnancy. It works by thickening the cervical mucus and suppressing ovulation, hence blocking sperm entry into the uterus. 
• Endometriosis: dienogest is also used to treat endometriosis, which causes pain and other symptoms. dienogest helps reduce the growth of endometrial tissue and decreases pain associated with endometriosis. 
• Menstrual disorders: dienogest can be used to treat heavy or irregular periods by regulating the menstrual cycle. 
• Androgen-related conditions: dienogest can also be used to treat androgen-related conditions, such as acne, hirsutism (excessive hair growth), and androgenic alopecia (hair loss). 

Drug Interaction

Adverse Reaction

Frequency Defined 

>10% 

Irregular menstrual bleeding 

Ovarian cyst 

Chloasma 

Nausea 

Abdominal Pain 

Vomiting 

Spotting 

Vaginal hemorrhage 

Decreased libido 

Breast discomfort 

Weight gain 

Muscle weakness 

Alopecia 

Acne 

Hypersensitivity 

Greasy hair 

Hirsutism 

Black Box Warning

Black Box Warning: 

Cigarette smoking while taking hormonal contraceptives increases the risk of cardiovascular issues. 

Contraindication / Caution

Contraindication/Caution: 

dienogest, like any medication, has certain contraindications and precautions that should be considered before use. Some of the contraindications and precautions associated with dienogest are: 

• Hypersensitivity: dienogest should not be used in individuals who are hypersensitive to dienogest or any of the other components of the medication. 
• Thromboembolism: dienogest should not be used in individuals with a history of or current thromboembolic disorders, such as pulmonary embolism (PE), deep vein thrombosis (DVT), or stroke, as it may increase the risk of blood clots. 
• Liver disease: dienogest should be used with caution in individuals with liver disease, as it may affect liver function and exacerbate existing liver conditions. 
• Breast cancer: dienogest should not be used in individuals who previously had breast cancer or any other estrogen- or progestin-sensitive cancer. 
• Pregnancy: dienogest should not be used during pregnancy or by individuals who are trying to conceive, as it may harm the developing fetus. 
• Interaction with other medications: dienogest may interact with other medications, such as anticonvulsants, antibiotics, and herbal supplements, which may affect its efficacy or increase the risk of side effects. 

Pregnancy / Lactation

Pregnancy consideration:  

Category X 

Breastfeeding warnings:  

Secretion of dienogest in breastmilk is unknown 

Breastfeeding is contraindicated during its treatment 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

dienogest is a synthetic progestin, which means it has similar effects to the natural hormone progesterone. As a progestin, dienogest has a variety of pharmacological effects on the body: 

• Progestational activity: dienogest binds to and activates progesterone receptors in the body, leading to changes in the endometrium and inhibition of ovulation. 
• Anti-androgenic activity: dienogest has anti-androgenic effects, meaning it reduces the activity of androgens (male hormones) in the body. This makes it useful for treating androgen-related conditions, such as acne and hirsutism. 
• Anti-inflammatory activity: dienogest has anti-inflammatory effects, which may be useful in the treatment of conditions such as endometriosis, where inflammation is thought to play a role. 
• Inhibition of GnRH secretion: dienogest reduces the secretion of GnRH from the hypothalamus, leading to decreased levels of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) and suppression of ovulation. 
• Thinning of endometrial lining: dienogest may cause thinning of the endometrial lining, making it less receptive to implantation by a fertilized egg. 

Pharmacodynamics: 

Some of the pharmacodynamics of dienogest are: 

• Inhibition of ovulation: dienogest inhibits ovulation by suppressing the secretion of LH and FSH, which are responsible for triggering ovulation. This effect is transferred by the negative feedback on the hypothalamic-pituitary-ovarian (HPO) axis. 
• Changes in the endometrium: dienogest causes changes in the endometrium that make it less receptive to implantation by a fertilized egg. It reduces the proliferation of the endometrium and causes it to become thinner and less vascularized, which reduces the chances of implantation. 
• Anti-androgenic activity: dienogest has anti-androgenic effects that make it useful in the treatment of androgen-related conditions, such as acne and hirsutism. It competes with androgens for binding to the androgen receptor and reduces the activity of androgens in the body. 
• Anti-inflammatory activity: dienogest has been shown to have anti-inflammatory effects that may be useful in the treatment of conditions such as endometriosis, where inflammation is thought to play a role. It reduces the expression of pro-inflammatory cytokines and chemokines and decreases the infiltration of immune cells into the affected tissues. 
• Modulation of cervical mucus: dienogest thickens the cervical mucus, blocking the entry of sperm into uterus. 
• Feedback on the hypothalamic-pituitary-adrenal (HPA) axis: dienogest has been shown to modulate the activity of the HPA axis by reducing the secretion of corticotropin-releasing hormone (CRH), which is responsible for the activation of the stress response. 

Pharmacokinetics: 

Absorption 

dienogest is rapidly absorbed after oral administration, with peak plasma concentrations reached within 1-2 hours. The absolute bioavailability of dienogest is approximately 90%, and it is not affected by food intake. 

Distribution 

dienogest is highly bound to plasma proteins (over 95%), mainly to sex hormone-binding globulin (SHBG) and albumin. The volume of distribution of dienogest is approximately 4 L/kg. 

Metabolism 

dienogest is extensively metabolized in the liver by cytochrome P450 enzymes, primarily CYP3A4. The main metabolite is 3-ketodesogestrel, which has a similar pharmacological activity to dienogest. Other metabolites include hydroxylated and conjugated metabolites. 

Elimination and Excretion  

The elimination half-life of dienogest is approximately 9-11 hours. It is primarily eliminated in the feces (42%) and urine (27%) as metabolites, with less than 1% excreted unchanged. 

Adminstartion

Administration: 

dienogest is primarily administered orally in the form of tablets. It is available as a standalone medication or in combination with estrogen in oral contraceptive pills. 

The dosage of dienogest may vary depending on the condition being treated. It is taken as an oral tablet daily. The effect decreases with St John’s Wort and increases with grapefruit juice. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dienogest 

Pronounced: dye-EN-oh-jest 

Why do we use dienogest? 

dienogest is used for a variety of indications, mainly related to its ability to modulate the hormonal environment of the body. Some of the uses of dienogest are: 

• Contraception: dienogest is used as a component of combined hormonal contraceptives (CHCs), which also contain an estrogen component. These contraceptives work by suppressing ovulation, thickening cervical mucus, and altering the endometrium, making it less receptive to implantation. dienogest is a highly effective contraceptive, with a failure rate of less than 1% when used correctly. 
• Endometriosis: dienogest is used in the treatment of endometriosis, a condition where the endometrial tissue grows outside the uterus and causes pain and inflammation. dienogest works by suppressing the growth and proliferation of endometrial tissue, reducing pain and other symptoms associated with endometriosis. 
• Dysmenorrhea: dienogest is also used in the treatment of dysmenorrhea, which is severe menstrual pain. It reduces pain by suppressing the growth and proliferation of endometrial tissue, which is responsible for the pain associated with dysmenorrhea. 
• Acne: dienogest has anti-androgenic properties, which make it useful in the treatment of acne, a condition that is often related to excess androgen activity. By reducing androgen activity, dienogest can help to reduce sebum production and inflammation, which are major factors in the development of acne. 
• Hirsutism: dienogest is also used in the treatment of hirsutism, a condition characterized by excessive hair growth in women, often associated with excess androgen activity. By reducing androgen activity, dienogest can help to reduce the growth of unwanted hair.