norgestrel

Action and Spectrum

Actions and Spectrum: 

Action: 

Contraceptive action: norgestrel, as a progestin, works primarily by suppressing ovulation. It prevents the release of eggs from the ovaries, thereby preventing fertilization by sperm. Additionally, it thickens cervical mucus, making it more difficult for sperm to reach the egg. norgestrel also alters the lining of the uterus, reducing the likelihood of implantation in case fertilization does occur. 

Hormone regulation: norgestrel helps regulate the menstrual cycle by stabilizing the endometrial lining. This can result in lighter and more regular periods. 

Spectrum: 

Inhibiting ovulation: norgestrel suppresses the release of eggs (ovulation) from the ovaries, which is a crucial mechanism in preventing pregnancy. 

Thickening cervical mucus: norgestrel thickens the cervical mucus, creating a barrier that hinders sperm from reaching and fertilizing an egg. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Cramps or bloating 

Abdominal pain 

Increased appetite 

Nausea 

Dizziness 

Headaches 

Irregular bleeding 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: Individuals who have shown hypersensitivity or allergic reactions to norgestrel or any other progestin should avoid using products containing this hormone. 

Thrombosis and Cardiovascular Disease: norgestrel, like other hormonal contraceptives, could potentially elevate the likelihood of developing blood clots, thrombosis, and cardiovascular complications, particularly in individuals with a medical background of deep vein thrombosis (DVT), pulmonary embolism, stroke, heart attack, or other pre-existing cardiovascular conditions. 

Liver Disease: norgestrel is metabolized in the liver, so individuals with severe liver impairment or liver disease should avoid using this medication. 

Breast Cancer: norgestrel is not recommended for individuals with a history of breast cancer or current breast cancer. 

Undiagnosed Vaginal Bleeding: If a woman experiences unexplained vaginal bleeding, it is important to consult a healthcare professional before starting or continuing norgestrel-based contraceptives. 

Known or Suspected Pregnancy: norgestrel is not a medication for terminating an existing pregnancy and should not be used for this purpose. If a woman is pregnant or suspects she may be pregnant, she should not use norgestrel-containing contraceptives. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: use is Contraindicated 

Lactation: small amount of progestins excreted into human milk  

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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:  

norgestrel is a synthetic progestin, which is a type of synthetic hormone with progestogenic activity.  

Pharmacodynamics:  

norgestrel exerts its pharmacological effects by binding to progesterone receptors in the body. Once bound, it mimics the actions of natural progesterone, leading to changes in the reproductive system.    

Pharmacokinetics: 

Absorption 

norgestrel is usually administered orally in the form of birth control pills. After oral ingestion, it is absorbed from the gastrointestinal tract into the bloodstream. The absorption can be influenced by various factors, such as food in the stomach and the formulation of the drug. 

Distribution 

Once absorbed into the bloodstream, norgestrel is distributed throughout the body. It binds to plasma proteins, primarily albumin, and can also bind to sex hormone-binding globulin. 

Metabolism 

norgestrel is metabolized in the liver by the process of hydroxylation and reduction. The major metabolites include 3α, 5β-tetrahydrolevonorgestrel, which is pharmacologically active, and 3α, 5α-tetrahydrolevonorgestrel. 

Excretion and Elimination 

The metabolites of norgestrel are excreted primarily in the urine and feces. The elimination half-life of norgestrel is around 10 to 30 hours. 

Adminstartion

Administration:  

For regular birth control pills: 

• It is taken daily, at the same time each day, for 21 days in a 28-day cycle. 
• Adhering to the guidelines given by your healthcare provider or the instructions provided in the pill packet is of utmost significance 

Patient Information Leaflet

Patient information leaflet 

Generic Name: norgestrel 

Why do we use norgestrel?  

Oral Contraceptive: norgestrel is commonly used in combination with an estrogen hormone in oral contraceptive pills (birth control pills). It helps prevent pregnancy by inhibiting ovulation. 

Emergency Contraception: norgestrel is also used as an emergency contraceptive pill, commonly known as the morning-after pill. 

Hormone Replacement Therapy (HRT): norgestrel is sometimes used as part of hormone replacement therapy in postmenopausal women. It helps alleviate menopausal symptoms by supplementing the body with progestin, which is necessary when estrogen is used alone to prevent the risk of endometrial hyperplasia (overgrowth of the uterine lining). 

Treatment of Menstrual Disorders: norgestrel may be prescribed to treat various menstrual disorders, such as irregular or heavy menstrual bleeding, dysmenorrhea (painful periods), and amenorrhea (absence of menstruation). 

Contraceptive Implants: norgestrel, in the form of etonogestrel, is used in contraceptive implants such as Nexplanon. This small, flexible rod is placed under the skin and provides a long-acting and highly effective form of birth control. 

Endometriosis: norgestrel may be used in the management of endometriosis.