Overview Of Progesterone Cream
Progesterone Cream is a compounded preparation, made to the strength and directions your prescriber specifies.
Prescribers order preparations of this kind for hormone replacement therapy, at a strength and ratio matched to the individual rather than to a fixed commercial product.
All of our compounding is done at Brandon Pharmacy and Compounding and transferred to our other four Florida stores, so you can collect it wherever you normally go. A prescription is required. Compounded preparations are not FDA-approved.
Dosage Power Of Progesterone Cream
25 mg/mL 30 mL Topi-Click Dispenser
30 mg/mL 30 mL Topi-Click Dispenser
40 mg/mL 30 mL Topi-Click Dispenser
50 mg/mL 30 mL Topi-Click Dispenser
60 mg/mL 30 mL Topi-Click Dispenser
70 mg/mL 30 mL Topi-Click Dispenser
75 mg/mL 30 mL Topi-Click Dispenser
80 mg/mL 30 mL Topi-Click Dispenser
90 mg/mL 30 mL Topi-Click Dispenser
100 mg/mL 30 mL Topi-Click Dispenser
125 mg/mL 30 mL Topi-Click Dispenser
150 mg/mL 30 mL Topi-Click Dispenser
175 mg/mL 30 mL Topi-Click Dispenser
200 mg/mL 30 mL Topi-Click Dispenser
250 mg/mL 30 mL Topi-Click Dispenser
Generic Details
Progesterone is a derivative of cholesterol. After interaction with cellular membrane receptors and fusion with intracellular lysozymes, it is then transported to the mitochondria where it is then converted into pregnenolone. Through the mediating action of the Cytochrome P450 group of super enzymes, pregnenolone is then converted to progesterone within the corpus luteum or the placenta, depending on the presence or absence of pregnancy.
In addition to its role in pregnancy, progesterone also plays an essential role in the central as well as peripheral nervous system. It is a neurosteroid, meaning that it is synthesized in the nervous system; this synthesis occurs in neuronal cells located with the central nervous system (CNS). Within the CNS, the pathway for progesterone synthesis is similar to that found in the corpus luteum or placenta. In the central nervous system, progesterone aids in the production of the myelin sheath, which is the layer surrounding the nerves, and is responsible for the transmission of rapid impulses along the nerve cells.
MOA
- Thickening of the uterine endometrium, getting it ready for the implantation of a fertilized ovum. Progesterone is released by the corpus luteum from the granulosa cells in the ovary for this purpose.
- Maintenance of pregnancy, helping to ensure that a successfully implanted fertilized ovum is carried by the mother until delivery. After the development of the placenta, one of its roles is to continue the production of progesterone for the duration of the pregnancy, making sure that serum progesterone levels are sufficient to maintain the fetus within the uterus.
- In the female breast, progesterone stimulates the growth in number and size of the alveoli and lobes during pregnancy. In addition, progesterone inhibits the production of breast milk throughout the duration of the pregnancy. As progesterone levels fall after delivery, milk production within the breasts is triggered.
- In the central nervous system, progesterone plays a role in the development of the myelin sheath surrounding the nerves. It has also been shown to play role in the neurological recovery from after a traumatic brain injury or a hypoxic-ischemic injury within the brain.
In addition to the genomic mechanism, progesterone can also exert its effects through non-genomic means. The non-genomic pathway involves the activation of intracellular signaling pathways, which occurs through ion channels as well as second messenger cascades. This pathway normally occurs in the central nervous system; however, it can also take place in other areas of the body.
Clinical Pharmacokinetics
Progesterone metabolism occurs in the liver and intestine facilitated by the enzymes 5-alpha reductase and 5-beta reductase, part of the cytochrome P450 group of super enzymes. In the liver, progesterone is broken down into over 30 metabolites such as metabolites such as 6 beta hydroxyprogesterone, deoxycorticosterone, 11-deoxycorticosterone, 21-hydroxyprogesterone, 17-hydroxyprogesterone, 5 alpha-dihydroprogesterone, 20 alpha hydroxy-4 alpha-prenolone, and pregnanolone, among others. The main metabolites of progesterone metabolism, however, are allopregnanolone and pregnanolone.
Progesterone elimination from the body occurs primarily through the kidneys though some metabolites are excreted in the bile. The main metabolite that is excreted through the kidneys is pregnanolone.
Clinical Indication
- Amenorrhea or oligomenorrhea: For some women with absent or decreased menstrual cycles, the administration of progesterone has been shown induce withdrawal bleeding in an estrogen-primed endometrium.
- Dysfunctional uterine bleeding: Usually occurring in adolescent or pre-menopausal women, dysfunctional uterine bleeding may be as a result of hormone imbalances and may be corrected by progesterone therapy.
- Endometrial hyperplasia: Progesterone or its analogues are commonly used in the management of endometrial hyperplasia. It works by promoting shedding of the uterine endometrium and preventing its subsequent buildup.
- Infertility: Progesterone is one of the key medications used in the management of infertility. As earlier stated, it helps to prepare the uterus for the implantation of a fertilized egg, and for the maintenance of an implanted fetus throughout the pregnancy duration.
- Preterm delivery: Studies have shown that progesterone administration during pregnancy has some benefits in preventing preterm labor and delivery. While still not totally clear, it is thought that progesterone exerts this effect by limiting the production of stimulatory prostaglandins as well as inhibiting the expression of contraction-associated protein genes in the walls of the uterus.
- Contraception: Progesterone can be used alone or in conjunction with estrogen as a contraceptive to prevent pregnancy. It acts by preventing ovulation and the altering the walls of the uterus as well as cervical mucus.
- Traumatic brain injury: Recently conducted phase 2 clinical trials indicate that progesterone may be of benefit in the aftermath of an acute traumatic brain injury. Progesterone administration serves to reduce neuronal loss and cerebral edema as well as enhance neuronal remyelination following a traumatic brain injury. However, progesterone is not currently widely administered for this purpose as further research is still required.
Precautions
- Hypersensitivity: Progesterone should not be administered to individuals who have a hypersensitivity to progesterone or any of its products.
- Hepatic disease: Due to the fact that progesterone is mainly metabolized in the liver, its administration to individuals with significant renal impairment should be avoided as much as possible.
- Ectopic pregnancy: Ectopic pregnancy as well as missed or incomplete abortions are absolute contraindications to exogenous progesterone administration.
- Breastfeeding: Caution should be exercised when administering progesterone to breastfeeding mothers as detectable amounts have been found in breast milk.
- Thromboembolic diseases: Individuals with a current or previous history of thromboembolic disease such as peripheral vascular disease, stroke, or myocardial infarction should not receive progesterone therapy. Individuals with high risk factors for thromboembolic diseases need to be closely monitored if they are given progesterone.
- Vaginal bleeding: Progesterone should not be administered to females presenting with vaginal bleeding of an unknown cause.
- Diabetes mellitus: Diabetics may receive progesterone therapy with caution as some individuals may experience a decrease in glucose tolerance and a resultant increase in blood sugar levels.
- Reproductive cancer: Progesterone therapy is contraindicated in females presenting with breast, cervical, endometrial, ovarian, uterine, or vaginal cancer. Since these cancers are usually hormonally dependent, progesterone administration may worsen these conditions.
- Hyperlipidemia: Progesterone therapy has been shown to impair lipid metabolism in some individuals and so should be administered cautiously to individuals with known or suspected cases of hyperlipidemia.
- Drug interactions: Care should be taken when administering progesterone with other drugs due to the likelihood of significant drug interactions. Some drugs such as barbiturates can stimulate the production of Cytochrome P450 enzymes in the liver and increase the rate of hepatic clearance of progesterone; this can result in decreased serum levels of progesterone as well as decreased effectiveness.
Pregnancy / Breast-Feeding
Detectable levels of progesterone have been found in the milk of breastfeeding mothers. There have been no reported instances of developmental problems in neonates and toddlers of mothers with progesterone in their breast milk. As such, there are no restrictions for breastfeeding women receiving progesterone therapy. However, some degree of care should be exercised when administering progesterone to lactating females.
Progesterone Cream Side Effects & Reactions
- Thromboembolic disease: This is especially the case in individuals who have risk factors for thromboembolic disease.
- Emotional lability: Sudden onsets of depression, anxiety, irritability, and uncontrollable outbursts are some emotional changes that may occur in women on progesterone therapy.
- Fluid retention: Progesterone administration may cause fluid retention. In individuals with cardiac or renal disease, this may result in a worsening of their condition.
- Menstrual changes: Changes in menstrual flow and rhythm, dysmenorrhea, and amenorrhea are some of the changes that may be seen in women receiving progesterone therapy.
How To Store
Areas we serve
Progesterone Cream is compounded at Brandon Pharmacy and Compounding and transferred to our other stores, so you can collect it at whichever is closest to you: Cape Coral, Fort Myers, Brandon or Riverview. Local delivery is free.
References
- Taraborrelli, S., “Physiology, production and action of progesterone”, ACTA Obstetricia et Gynecologica, vol.94, pp. 8-16, 2015. Available: https://obgyn.onlinelibrary.wiley.com/doi/pdf/10.1111/aogs.12771
- Graham, J. D., Clarke, C.L., “Physiological Action of Progesterone in Target Tissues” Endocrine Reviews, vol.18, pp. 502-519, 1997. Available: https://academic.oup.com/edrv/article/18/4/502/2530774
- “Progesterone”, National Center for Biotechnology information, 2020. Available: https://pubchem.ncbi.nlm.nih.gov/compound/Progesterone
- Schumacher, M., Hussain, R., Gago, N., Oudinet, J. P., Mattern, C., Ghoumari, A. M., “Progesterone synthesis in the nervous system: implications for myelination and myelin repair”, Frontiers in neuroscience, Vol.6, issue 10, 2012. Available: https://doi.org/10.3389/fnins.2012.00010
- Singh, M, Su, C, Ng, S., “Non-genomic mechanisms of progesterone action in the brain”, Frontiers in Neuroscience, vol.7, 2013. Available: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3776940/#:~:text=The%al%E2%80%20by%20%20of%20target0genes%20to
- Gonzalez-Orozco, J.C., Camacho-Arroyo, I, “Progesterone Actions During Central Nervous System Development”, Frontiers in Neuroscience, vol.13, 2019. Available: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6533804/
- “Progesterone”. Available: https://go.drugbank.com/drugs/DB00396
- “Progesterone – Drug summary”, Prescribers’ Digital Reference. Available: https://www.pdr.net/drug-summary/progesterone?druglabelid=2388
- Chandra, V., Joo-Kim, J., Benbrook, D.M., Dwivedi, A., Raj, R., “Therapeutic options for management of endometrial hyperplasia”, Journal of Gynecologic Oncology, vol.27, issue 1, Jan. 2016. Available: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4695458/
- Norwitz, E.R., Caughey, A.B., “Progesterone Supplementation and the Prevention of Preterm Birth” Reviews in Obstetrics and Gynecology, vol.4 issue 2, pp. 60-72. 2011. Available: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3218546/
- Espinoza, T. R., Wright, D. W., “The Role of Progesterone in Traumatic Brain Injury”, The Journal of head trauma rehabilitation, vol.26, issue 6, pp. 497-499, Nov-Dec 2011. Available: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6025750/
- “Progesterone pregnancy and breastfeeding warnings” Available: https://www.drugs.com/pregnancy/progesterone.html#:~:text=US%20FDA%20pregnancy%20category%20B,controlled%20studies%20in%20pregnant%20women.