norgestimate

Action and Spectrum

Actions and spectrum: 

norgestimate is a synthetic progestin that is commonly used in combination with an estrogen component in oral contraceptives. It acts by preventing ovulation, thickening cervical mucus to impede the passage of sperm, and altering the lining of uterine to make it less receptive to a fertilized egg. 

The spectrum of norgestimate is primarily related to its use in combination with estrogen in birth control pills, where it helps prevent pregnancy by inhibiting fertilization and changing the uterine environment. It is not used as a standalone medication but as a part of combination oral contraceptives. 

Drug Interaction

Adverse Reaction

Frequency not defined 

GI discomfort 

fluid retention 

acne 

skin rashes 

mental depression 

hair loss 

fatigue 

fever 

Headache 

drowsiness  

insomnia 

hirsutism 

libido 

urticaria 

Chloasma 

oedema 

appetite 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with norgestimate. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Pregnancy: norgestimate-containing oral contraceptives should not be used during pregnancy. They are intended for contraception and should not be taken if a woman is already pregnant. 
• Hypersensitivity: Women who have a known hypersensitivity or allergy to norgestimate, other progestins, estrogen, or any components of the contraceptive should not use these products. 
• History of Blood Clots: Women with a history of venous thromboembolic disorders should avoid norgestimate-containing contraceptives due to the increased risk of blood clots. 
• Severe Hypertension: Uncontrolled or severe hypertension (high blood pressure) is a contraindication. Women with hypertension should have their blood pressure well-managed before considering these contraceptives. 
• Severe Liver Disease: Conditions such as liver tumors, acute viral hepatitis, or severe liver disease are contraindications for norgestimate-containing oral contraceptives.

Caution: 

• Age: Adolescents and women over 35 years of age may have different risks and benefits associated with norgestimate-containing oral contraceptives. It is important to discuss age-related considerations with a healthcare provider. 
• Cigarette Smoking: Smoking, especially in women over 35 years of age, increases the risk of serious cardiovascular side effects, such as blood clots and stroke. Women who smoke while using oral contraceptives should be advised to quit smoking. 
• Obesity: Obesity may increase the risk of certain side effects, such as blood clots. Healthcare providers may need to consider alternative contraceptive options or closely monitor individuals who are obese. 
• Migraines: Women who experience migraines, particularly migraines with aura, may have an increased risk of stroke when using combined oral contraceptives. They should discuss these risks with their healthcare provider. 
• Vaginal Bleeding: Women should be aware of any changes in their menstrual pattern or unexplained vaginal bleeding while using these contraceptives and should promptly consult a healthcare provider.

Comorbidities: 

• Cardiovascular Disease: Women with a history of cardiovascular disease, including heart disease, hypertension, or a previous heart attack or stroke, may need special attention when considering the use of norgestimate-containing contraceptives. These conditions can increase the risk of cardiovascular side effects. 
• Thromboembolic Disorders: Individuals with a history of blood clots, deep vein thrombosis, or pulmonary embolism should use norgestimate-containing contraceptives with caution, as there is an increased risk of clot formation associated with some oral contraceptives. 
• Diabetes: Women with diabetes should be closely monitored while using norgestimate-containing contraceptives. These contraceptives can affect blood glucose levels, and adjustments in diabetes management may be necessary. 
• Epilepsy and Anticonvulsant Use: Some anticonvulsant medications can interact with norgestimate-containing contraceptives, potentially reducing their effectiveness. Adjustments or alternative contraceptive methods may be necessary for individuals with epilepsy. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

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: norgestimate is a synthetic progestin commonly used in combination with an estrogen component in oral contraceptives to prevent pregnancy. As a progestin, norgestimate exerts its contraceptive effects primarily by suppressing ovulation, preventing the release of eggs from the ovaries.

It thickens the cervical mucus, making it more difficult for the sperm to penetrate and fertilize an egg. Additionally, norgestimate can affect the endometrial lining of uterus, making it less receptive to a fertilized egg.

While norgestimate shares these contraceptive mechanisms with other progestins, its specific pharmacokinetic properties, including its absorption, distribution, metabolism, and excretion, can vary, influencing its overall efficacy and side effect profile.

Norgestimate-containing contraceptives are typically taken in a 28-day cycle, with 21 active pills containing hormones and seven inactive or placebo pills. The combination of norgestimate and an estrogen component is designed to provide reliable contraception with proper use while minimizing side effects and menstrual irregularities.  

Pharmacodynamics: 

• Suppression of Ovulation: norgestimate, as a progestin, primarily acts by suppressing ovulation, preventing the release of eggs from the ovaries. It does this by inhibiting the secretion of gonadotropins, specifically luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are essential for ovulation. 
• Cervical Mucus Changes: norgestimate thickens cervical mucus, making it more viscous and difficult for sperm to penetrate. This hinders their ability to reach and fertilize the egg in the fallopian tube. 
• Endometrial Changes: norgestimate can also alter the endometrial lining of uterus, making it less receptive to implantation of a fertilized egg. This change in the endometrium helps to prevent pregnancy. 
• Effect on Menstrual Cycle: norgestimate, when taken in a combined oral contraceptive, regulates and stabilizes the menstrual cycle. It reduces the severity of menstrual bleeding and can help manage conditions such as heavy or irregular periods.

Pharmacokinetics: 

Absorption 

norgestimate is administered orally, typically in combination with an estrogen component, as part of birth control pills (oral contraceptives). It is absorbed in the gastrointestinal tract. 

Distribution 

norgestimate is distributed throughout the body after absorption, and it binds to serum proteins like albumin. Its distribution is influenced by its lipophilicity and affinity for binding proteins. 

Metabolism 

norgestimate is a prodrug, meaning it undergoes metabolic conversion to its active form, norelgestromin. This conversion primarily occurs in the liver. Cytochrome P450 enzymes, especially CYP3A4, play a significant role in the metabolic conversion of norgestimate. Enzymes in the intestinal wall are also involved. 

Elimination and excretion 

norgestimate and its metabolites are excreted primarily in urine and feces. The metabolites of norgestimate, including norelgestromin and its derivatives, are excreted in both urine and feces. 

Adminstartion

Administration: 

The dosage of norgestimate can vary depending on the specific combination oral contraceptive product you are prescribed. Common regimens include 21-day or 28-day cycles, with most pills containing both norgestimate and an estrogen component. Take one pill at the same time each day, preferably with a meal or at bedtime. Consistency in the timing of administration is crucial for the effectiveness of the contraceptive. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: norgestimate 

Pronounced: (nor-JES-ti-mate)  

Why do we use norgestimate? 

The primary use of norgestimate is as a contraceptive. When combined with an estrogen, it prevents pregnancy by suppressing the ovulation, thickening of cervical mucus, and altering endometrial lining (making it less receptive to implantation). It is an effective and reversible method of birth control. norgestimate-containing birth control pills can help regulate irregular menstrual cycles.

They often lead to more predictable and lighter menstrual periods. Some individuals experience relief from common menstrual symptoms like premenstrual syndrome (PMS) and dysmenorrhea (painful periods) when using norgestimate-containing contraceptives. The hormone regulation can alleviate symptoms like bloating, mood swings, and cramps.