progesterone, natural

Action and Spectrum

Actions and Spectrum: 

The mechanism of action of progesterone involves binding to specific receptors in the target tissues, including the uterus, mammary glands, and brain. Once bound, it modulates the expression of genes, which results in a variety of physiological effects.  

In the uterus, progesterone stimulates the growth of the endometrial lining and inhibits contractions, preventing premature labor. It also stimulates cervical mucus production, making it thicker and less permeable to sperm. In the mammary glands, progesterone stimulates the growth of the alveoli, which produces milk after childbirth. 

The spectrum of activity of progesterone is mainly focused on the female reproductive system. Still, it also affects other tissues and organs, including the brain, bone, and immune system. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Rash 

Vaginal spotting 

Edema 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Pregnancy: progesterone is essential for maintaining pregnancy, but its use is contraindicated during pregnancy as it can increase the risk of congenital disabilities and other complications. 
• Breast cancer: progesterone can stimulate the growth of certain types of breast cancer, so its use is contraindicated in women with a history of breast cancer. 
• Liver disease: progesterone is metabolized by the liver, so its use is contraindicated in women with liver disease. 
• Abnormal vaginal bleeding: progesterone can cause abnormal vaginal bleeding, so its use is contraindicated in women with undiagnosed vaginal bleeding. 
• Blood clots: progesterone can increase the risk of blood clots, so its use is contraindicated in women with a history of blood clots or thromboembolic disorders. 
• Allergy: progesterone can cause allergic reactions in some people, so its use is contraindicated in those allergic to progesterone or any of its components. 

Caution: 

• Breastfeeding: progesterone is excreted in breast milk, so its use is cautioned during breastfeeding. 
• Asthma: progesterone can exacerbate asthma symptoms in some people, so its use is cautioned in those with asthma. 
• Diabetes: progesterone can affect blood sugar levels, so its use is cautioned in people with diabetes. 
• Depression: progesterone can affect mood and exacerbate depression symptoms in some people, so its use is cautioned in those with a history of depression. 
• Migraines: progesterone can trigger migraines in some people, so its use is cautioned in those with a history of migraines. 
• Hypertension: progesterone can increase blood pressure in some people, so its use is cautioned in those with hypertension. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A 

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 available 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: 

progesterone is a steroid hormone produced by the corpus luteum in the ovaries during the menstrual cycle and by the placenta during pregnancy. It is also produced in small amounts by the adrenal glands.  

progesterone works by binding to specific progesterone receptors in target tissues, including the uterus, mammary glands, and brain. Once bound, it modulates the expression of genes, which results in a variety of physiological effects.  

In the uterus, progesterone stimulates the growth of the endometrial lining and inhibits contractions, preventing premature labor. It also stimulates cervical mucus production, making it thicker and less permeable to sperm.  

In the mammary glands, progesterone stimulates the growth of the alveoli, which produces milk after childbirth. In the brain, progesterone affects mood, memory, and anxiety. 

Pharmacodynamics: 

The pharmacodynamics of natural progesterone involve its interactions with specific progesterone receptors in target tissues. When progesterone binds to these receptors, it initiates a series of cellular responses that lead to its various physiological effects.  

In the uterus, progesterone promotes the proliferation of the endometrial lining and inhibits its shedding, which is necessary for the implantation and maintenance of a fertilized egg. progesterone also inhibits the contractions of the uterine smooth muscle, which helps to prevent premature labor.  

In the mammary glands, progesterone stimulates the growth of the lobules and alveoli, which produce milk after childbirth.  

In the brain, progesterone affects mood, memory, and anxiety.  progesterone also modulates the activity of other neurotransmitters, such as dopamine, serotonin, and norepinephrine, which are involved in mood regulation. 

Pharmacokinetics: 

Absorption 

Natural progesterone is typically administered orally, topically, or vaginally. Oral administration results in variable absorption due to first-pass metabolism in the liver, while topical and vaginal administration results in higher bioavailability and more targeted effects in the reproductive system.  

Distribution 

progesterone is highly lipophilic, which allows it to cross cell membranes and distribute throughout the body. It binds to serum proteins such as albumin and transcortin, which help transport it to target tissues, including the uterus, mammary glands, and brain.  

Metabolism 

progesterone is metabolized primarily in the liver, where it is converted to pregnanediol and then conjugated with glucuronic acid or sulfate for excretion. Some progesterone is also metabolized in the uterus and mammary glands.  

Elimination and Excretion 

Most progesterone and its metabolites are excreted in the urine, with a small portion excreted in the feces. The half-life of progesterone is relatively short, ranging from 5-20 minutes, which means that it is rapidly cleared from the body. 

Adminstartion

Administration: 

Natural progesterone is available in various forms, including oral capsules, topical creams, vaginal suppositories, and injections. The choice of formulation depends on the indication and the individual’s preferences and needs.  

Oral administration: 

Oral progesterone is typically administered in the form of capsules or tablets. It is usually taken once daily at bedtime to mimic the natural circadian rhythm of progesterone production. Oral progesterone may have more systemic effects, as it is absorbed through the digestive system and undergoes first-pass metabolism in the liver.  

Topical administration: 

progesterone cream or gel is applied to the skin and absorbed through the dermis. It is usually applied to areas with high blood flow, such as the inner arms, inner thighs, or abdomen. Topical administration may have more targeted and less systemic effects on the reproductive system.  

Vaginal administration: 

progesterone can be administered vaginally in the form of suppositories, gels, or creams. Vaginal administration may have more localized effects on the reproductive system, making it a preferred route for women with menstrual disorders, infertility, or menopausal symptoms. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: progesterone, natural 

Why do we use progesterone, natural? 

natural progesterone is used for a variety of indications related to the female reproductive system, including: 

• Hormone replacement therapy (HRT): natural progesterone treats menopausal symptoms, such as hot flashes, night sweats, vaginal dryness, and mood changes. It is often used in combination with estrogen to provide balanced hormonal support. 
• Infertility: natural progesterone supports fertility by preparing the uterine lining for implantation and maintaining a pregnancy in women undergoing assisted reproductive technologies, such as in vitro fertilization. 
• Menstrual disorders: natural progesterone regulates the menstrual cycle and treats conditions such as irregular periods, heavy bleeding, and premenstrual syndrome (PMS). 
• Endometriosis: natural progesterone is used to treat endometriosis, where the tissue that lines the uterus grows outside, causing pain and discomfort. 
• Uterine fibroids: natural progesterone is used to shrink uterine fibroids and noncancerous uterine growths that can cause heavy bleeding and pain. 
• Prevention of preterm labor: natural progesterone is used to prevent preterm labor in women with a history of preterm birth or other risk factors for preterm delivery. 
• Breast cancer: natural progesterone may be used as part of the treatment for certain hormone-sensitive breast cancer types.