desogestrel

Action and Spectrum

Actions and spectrum: 

desogestrel is a synthetic progestin hormone that is used in various forms of hormonal contraception, including oral contraceptive pills. It acts primarily by inhibiting ovulation, preventing the release of eggs from the ovaries.

desogestrel also thickens the cervical mucus, makes it more difficult for sperm to reach uterus and fertilize an egg. Additionally, it alters the lining of the uterus, making it less receptive to implantation of a fertilized egg. The spectrum of desogestrel’s action is focused on preventing pregnancy and does not have additional therapeutic uses outside of contraception. 

Drug Interaction

Adverse Reaction

None

Black Box Warning

Black Box Warning: 

desogestrel does not have any black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: desogestrel should not be used in individuals with a known hypersensitivity or allergy to desogestrel or any of its components. 
• Thromboembolic Disorders: desogestrel is contraindicated in individuals with a history of or current thromboembolic disorders, such as deep vein thrombosis (DVT), pulmonary embolism (PE), or cerebrovascular accident (stroke). 
• Liver Disease: desogestrel is contraindicated in individuals with active liver disease or liver dysfunction. 
• Undiagnosed Vaginal Bleeding: desogestrel should not be used in individuals with undiagnosed abnormal vaginal bleeding. 
• Known or Suspected Pregnancy: desogestrel is contraindicated in individuals who are pregnant or suspect they may be pregnant.

Caution: 

• Cardiovascular Risk: Like other hormonal contraceptives, desogestrel may increase the risk of cardiovascular events, such as blood clots, heart attack, or stroke. This risk may be higher in individuals who smoke, have a history of blood clotting disorders. 
• Gallbladder Disease: desogestrel may increase the risk of developing gallbladder disease, especially in individuals with a history of gallbladder problems. 
• Liver Function: desogestrel is metabolized in the liver, so it should be used with caution in individuals with impaired liver function. Regular monitoring of liver function may be necessary. 
• Breast Cancer: Some studies have suggested a slight increase in the risk of breast cancer in users of hormonal contraceptives. However, the evidence is inconclusive, and the overall risk is considered small. 
• Drug Interactions: desogestrel may interact with certain medications, including those that induce liver enzymes, such as certain anticonvulsants and antiretrovirals. This can affect the effectiveness of desogestrel or increase the risk of side effects.

Comorbidities: 

• Cardiovascular Disease: Individuals with cardiovascular disease, such as heart attack, stroke, or blood clots, may need close monitoring while using desogestrel due to the potential increased risk of cardiovascular events associated with hormonal contraceptives. 
• Liver Disease: desogestrel is metabolized in the liver, so individuals with impaired liver function may need careful monitoring while using the medication. 
• Diabetes: desogestrel can affect glucose metabolism, so individuals with diabetes may require close monitoring of their blood sugar levels while using the medication. 
• Migraine: desogestrel may increase the frequency or severity of migraines in some individuals. It is important to discuss this with your healthcare provider if you have a history of migraines. 
• Depression or Mental Health Conditions: Hormonal contraceptives, including desogestrel, may have an impact on mood in some individuals. If you have a history of depression or other mental health conditions, it is important to discuss this with your healthcare provider. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: X 

Lactation: Excreted into human milk: Yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

desogestrel is a synthetic progestin, which is a type of female sex hormone. It acts primarily by binding to the progesterone receptors in the body, leading to various pharmacological effects. 

desogestrel is a progestin hormone used in hormonal contraceptives. It acts by binding to progesterone receptors in the body, resulting in the suppression of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) secretion.

This prevents ovulation and alters the cervical mucus, making it less favorable for sperm penetration. Additionally, desogestrel causes thinning of the endometrium, reducing the likelihood of implantation.  

Pharmacodynamics: 

• Progestogenic Activity: desogestrel binds to and activates the progesterone receptors in the body. This leads to a range of progestogenic effects, such as inhibition of ovulation, thickening of cervical mucus, and changes in the endometrium to make it less receptive to implantation. 
• Suppression of Follicle-Stimulating Hormone (FSH): desogestrel inhibits the release of FSH from the pituitary gland. This suppression of FSH levels helps to prevent the development and maturation of ovarian follicles, thereby inhibiting ovulation. 
• Inhibition of Luteinizing Hormone (LH) Surge: desogestrel can suppress the surge of LH that normally triggers ovulation. By preventing this LH surge, it further contributes to the inhibition of ovulation. 
• Stabilization of the Endometrium: desogestrel helps to stabilize the endometrium, reducing the risk of abnormal growth or shedding of the uterine lining.

Pharmacokinetics: 

Absorption 

desogestrel is well absorbed after oral administration. It undergoes rapid and extensive first-pass metabolism in the liver, resulting in a lower systemic bioavailability. 

Distribution 

desogestrel is highly protein-bound, primarily to albumin and sex hormone-binding globulin (SHBG). It has a large volume of distribution, indicating its extensive distribution into tissues. 

Metabolism 

desogestrel is extensively metabolized in the liver via hydroxylation and oxidation processes. The primary metabolite is etonogestrel, which is pharmacologically active and contributes to the contraceptive effects of desogestrel. 

Elimination and excretion 

Metabolites of desogestrel, including etonogestrel, are excreted in the urine and feces. The elimination half-life of desogestrel is approximately 24 hours, while that of etonogestrel is around 30 hours 

Adminstartion

Administration: 

desogestrel is typically administered orally in the form of a tablet. The specific administration instructions may vary depending on the brand and formulation of the medication. Generally, desogestrel tablets are taken once daily, preferably at the same time each day, with or without food.

It is recommended to swallow the tablet whole with a glass of water. It is important to adhere to the prescribed dosage and schedule for optimal effectiveness. If you have any questions or concerns about the administration of desogestrel, it is best to consult your healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: desogestrel 

Pronounced: des-oh-JES-trel  

Why do we use desogestrel? 

desogestrel is primarily used as a hormonal contraceptive, commonly known as a progestin-only pill or mini-pill. It is used to prevent pregnancy by inhibiting ovulation, thickening the cervical mucus to prevent sperm from reaching the egg, and altering the lining of the uterus to make it less receptive to implantation. desogestrel is also used to regulate menstrual cycles, reduce menstrual pain, and heavy bleeding, and treat conditions such as endometriosis and PCOS.