promegestone

Action and Spectrum

Actions and spectrum: 

Action: 

• Progestational Activity: promegestone primarily acts as a progestin, binding to progesterone receptors in various tissues, including the uterus and the lining of the uterus (endometrium).  
• Contraception: promegestone is used as a component in birth control pills and intrauterine devices (IUDs). Its progestational activity helps to inhibit ovulation, thicken cervical mucus to impede sperm penetration, and alter the endometrial lining to prevent implantation. 
• Hormone Replacement Therapy (HRT): In some cases, promegestone may be used as part of hormone replacement therapy in postmenopausal women. It helps to alleviate symptoms of menopause and provide the progestin component necessary when estrogen is also being administered as part of HRT. 

Spectrum:  

• Contraception: promegestone is used in combination with other hormones to create contraceptive formulations, offering women a reliable means of birth control. 
• Hormone Replacement Therapy: In HRT regimens, promegestone can be employed to balance the effects of estrogen therapy, reducing the risk of endometrial hyperplasia and cancer. 
• Menstrual Disorders: In some cases, promegestone may be used to treat irregular menstrual cycles or heavy menstrual bleeding. 

Drug Interaction

Adverse Reaction

Frequency not defined 

GI disturbances 

edema 

chloasma 

hirsutism 

insomnia 

breakthrough bleeding 

changes in appetite 

acne 

breast changes 

headache 

altered menstrual cycles 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with promegestone. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Known Hypersensitivity: promegestone should not be used in hypersensitivity or allergy to the medication or any of its components. 
• Liver Disease: Individuals with severe liver disease or impairment may have an increased risk of adverse effects when using promegestone. It is essential to assess liver function before prescribing this medication. 
• Thromboembolic Disorders: promegestone, like other hormonal contraceptives, may increase the risk of thromboembolic disorders such as deep vein thrombosis (DVT) & pulmonary embolism (PE). It should be used with caution in individuals with a history of these conditions. 
• Breast Cancer: There might be an increased risk of breast cancer with use of hormonal contraceptives, including those containing promegestone. The use of such medications may not be advisable in individuals with a history of breast cancer or certain risk factors. 
• Undiagnosed Vaginal Bleeding: If a woman is experiencing undiagnosed vaginal bleeding, it is important to determine the cause before using promegestone or any hormonal contraceptive. 
• Active Liver Tumors: If a person has active liver tumors, promegestone should be avoided. 
• Porphyria: promegestone should be used with caution in individuals with a history of porphyria, a group of rare genetic disorders that affect the skin or nervous system.

Caution: 

• Cardiovascular Risk: Like other hormonal contraceptives, promegestone may have an increase the risk of cardiovascular diseases in patients with smoking, obesity, hypertension, or a history of cardiovascular disease. Healthcare providers should carefully assess a person’s cardiovascular risk before prescribing promegestone. 
• Breast Health: Women using hormonal contraceptives, including those containing promegestone, should be advised to perform regular breast self-examinations and have routine breast examinations by a healthcare provider. Any unusual changes in breast tissue should be reported promptly. 
• Interactions with Other Medications: promegestone may interact with other medications, including those that induce liver enzymes. These interactions can affect the effectiveness of promegestone and may require adjustments in dosage or the choice of contraceptive method. 
• Migraines: Women with a history of migraines, especially those with aura, should be cautious when using hormonal contraceptives, as they may increase the risk of stroke. 
• Bone Health: Prolonged use of hormonal contraceptives, including promegestone-containing products, may have an impact on bone density. Regular evaluation of bone health may be recommended, particularly in women with risk factors for osteoporosis. 
• Menstrual Irregularities: While promegestone is used to regulate menstrual cycles, some individuals may experience irregular bleeding or spotting during the first few months of use. This is typically temporary, but healthcare providers should counsel patients on what to expect. 
• Pregnancy and Breastfeeding: promegestone should not be used during pregnancy. If pregnancy occurs while using this medication, it should be discontinued. Additionally, women should be advised not to use hormonal contraceptives during breastfeeding unless recommended by a healthcare provider.

Comorbidities: 

• Hypertension: High blood pressure can be exacerbated by hormonal contraceptives, including promegestone-based products. Blood pressure should be well-controlled before starting this medication, and regular monitoring is advisable. 
• Diabetes: Women with diabetes may need adjustments in their diabetes management plan when using hormonal contraceptives, as these medications can affect blood glucose levels. Close monitoring of blood sugar is essential. 
• Migraines: Individuals with a history of migraines, especially those with aura (visual disturbances), should be cautious when using hormonal contraceptives, as they may increase the risk of stroke. 
• Breast Health: Women with a personal or family history of breast cancer should discuss the potential risks and benefits of hormonal contraceptives with their healthcare provider.  
• Depression and Mood Disorders: Hormonal contraceptives, including progestin-only options like promegestone, can affect mood in some individuals. Women with a history of depression or mood disorders should be monitored for changes in mood while using these contraceptives. 
• Osteoporosis: Prolonged use of hormonal contraceptives may affect bone density. Women with risk factors for osteoporosis should have their bone health assessed regularly. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast 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: 

promegestone is a synthetic progestin with pharmacological actions like the hormone progesterone. As a progestin, it primarily acts on the female reproductive system. promegestone exerts its effects by binding to progesterone receptors in the body’s tissues, including the uterus and cervix.

This binding leads to changes in the endometrium (uterine lining), inhibits ovulation, and thickens cervical mucus, making it less permeable to sperm. These actions collectively help prevent pregnancy when used in contraceptives and can also be beneficial in hormone replacement therapy.

Additionally, promegestone does not have estrogenic effects, making it suitable for women who cannot tolerate estrogen-based contraceptives or hormone therapies.  

Pharmacodynamics: 

• Endometrial Changes: promegestone promotes changes in the endometrial lining of the uterus, making less receptive to the implantation of a fertilized egg. This action is crucial for its contraceptive effects, as it helps prevent the embryo from implanting in the uterus. 
• Inhibition of Ovulation: Like other progestins, promegestone can suppress ovulation in some individuals. This is an essential mechanism of action in hormonal contraception, as preventing ovulation reduces the chance of pregnancy. 
• Cervical Mucus: promegestone thickens cervical mucus, making it more viscous and less permeable to sperm. This change in cervical mucus quality inhibits the sperm to travel through cervix and into the uterus, further reducing the likelihood of fertilization. 
• Contraceptive Effect: By combining these actions on the endometrium, ovulation, and cervical mucus, promegestone provides effective contraception when used in birth control methods like progestin-only pills or contraceptive implants. 
• Hormone Replacement Therapy (HRT): In hormone replacement therapy for menopausal or postmenopausal women, promegestone can regulate menstrual cycle and alleviate symptoms associated with hormonal imbalances. 
• Minimal Estrogenic Activity: Unlike some other synthetic progestins, promegestone has minimal estrogenic activity, making it suitable for women who cannot tolerate or should avoid estrogen-based contraceptives or hormone therapies.

Pharmacokinetics: 

Absorption 

promegestone is typically administered orally, such as in the form of progestin-only birth control pills. After oral administration, it is absorbed through the gastrointestinal tract and enters the bloodstream. 

Distribution 

Once absorbed into the bloodstream, promegestone is distributed throughout the body’s tissues. It crosses the blood-brain barrier, allowing it to exert its effects on the central nervous system. promegestone binds to progesterone receptors in various tissues, including the endometrium (uterine lining), cervix, and brain. 

Metabolism 

promegestone is metabolized in the liver through various metabolic pathways, including hydroxylation and conjugation reactions. The specific metabolites produced during metabolism can vary. 

Elimination and excretion 

Metabolized promegestone and its metabolites are primarily excreted from the body through the urine and feces. The elimination half-life of promegestone can vary based on the individual and the specific formulation but typically ranges from a few hours to about a day. 

Adminstartion

Administration: 

promegestone is typically administered orally in the form of progestin-only birth control pills or as part of hormone replacement therapy (HRT) regimens. 

Progestin-Only Birth Control Pills: 

• Take one promegestone pill at the same time each day. 
• Swallow the pill whole with a glass of water, with or without food. 
• It’s essential to take the pills consistently and not miss doses to ensure contraceptive effectiveness. If you miss a dose or take it late, follow the instructions provided with the medication or consult your healthcare provider. 

Hormone Replacement Therapy (HRT):  

• HRT regimens may involve taking promegestone in combination with other hormones, such as estrogen. 
• Follow your healthcare provider’s instructions carefully regarding the timing and dosage of promegestone as part of your HRT regimen. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: promegestone 

Pronounced: (pro-MEG-es-tone)  

Why do we use promegestone? 

• Contraception: promegestone is used in progestin-only birth control pills, also known as mini-pills. These pills provide contraception by thickening cervical mucus, making difficult for the sperm to reach and fertilize an egg, and by altering the endometrial lining, making it less receptive to implantation. It is suitable for women who cannot use estrogen-containing contraceptives due to medical reasons or personal preferences. 
• Hormone Replacement Therapy (HRT): promegestone is sometimes included in hormone replacement therapy regimens for menopausal or postmenopausal women. When combined with estrogen, it can help alleviate hot flashes, vaginal dryness, and mood swings. This combination can also help regulate the menstrual cycle in perimenopausal women. 
• Dysfunctional Uterine Bleeding: promegestone may be prescribed to treat abnormal uterine bleeding caused by hormonal imbalances.  
• Endometrial Hyperplasia: In some cases, promegestone may be used to manage or prevent endometrial hyperplasia, characterized by abnormal thickening of the uterine lining. 
• Breast Disorders: promegestone has been investigated for its potential use in the treatment of certain breast disorders, such as benign breast disease and fibrocystic breast changes. It may help reduce breast pain and discomfort associated with these conditions.