Prefest 30 Day
Prefest 30 Day Uses, Dosage, Side Effects, Food Interaction and all others data.
Prefest 30 Day is a naturally occurring oestrogen. Oestrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. They modulate the pituitary secretion of gonadotrophins, LH and FSH through a negative feedback system.
Prefest 30 Day acts on the on the estrogen receptors to relieve vasomotor systems (such as hot flashes) and urogenital symptoms (such as vaginal dryness and dyspareunia).
Prefest 30 Day has also been shown to exert favorable effects on bone density by inhibiting bone resorption. Estrogen appears to inhibit bone resorption and may have beneficial effects on the plasma lipid profile. Estrogens cause an increase in hepatic synthesis of various proteins, which include sex hormone binding globulin (SHBG), and thyroid-binding globulin (TBG). Estrogens are known to suppress the formation of follicle-stimulating hormone (FSH) in the anterior pituitary gland.
A note on hyper-coagulable state, cardiovascular health, and blood pressure
Trade Name | Prefest 30 Day |
Availability | Prescription only |
Generic | Estradiol |
Estradiol Other Names | 17beta oestradiol, beta-Estradiol, cis-Estradiol, Estradiol, Estradiol-17beta, Estradiolum |
Related Drugs | alendronate, finasteride, tamoxifen, Fosamax, Premarin, testosterone, norethindrone, medroxyprogesterone, megestrol, raloxifene |
Type | |
Formula | C18H24O2 |
Weight | Average: 272.382 Monoisotopic: 272.177630012 |
Protein binding | More than 95% of estrogens are found to circulate in the blood bound to sex hormone binding globulin (SHBG) and albumin. |
Groups | Approved, Investigational, Vet approved |
Therapeutic Class | Female Sex hormones |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Treatment of moderate to severe vasomotor symptoms associated with the menopause.
Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with the menopause. When prescribing solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.
Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure.
Treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease.
Treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).
Prevention of osteoporosis. When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should only be considered for women at significant risk of osteoporosis and for whom non-estrogen medications are not considered to be appropriate.
Prefest 30 Day is also used to associated treatment for these conditions: Atrophic Vaginitis, Breast Cancer, Breast engorgement caused by Postpartum state, Hypogonadism female, Kraurosis Vulvae, Metastatic Breast Cancer, Osteoporosis, Postmenopausal Osteoporosis, Premature Ovarian Failure (POF), Prostate Cancer, Urogenital atrophy, Vasomotor Symptoms Associated With Menopause, Vulvovaginal Atrophy, Advanced androgen dependent Prostate cancer, Female castration, Hypoestrogenism, Contraception, Hormone Replacement Therapy, Palliation
How Prefest 30 Day works
Estrogen is found in the the breast, uterine, ovarian, skin, prostate, bone, fat, and brain tissues. The main source of estrogen in adult women during the reproductive period of life is the ovarian follicle, which secretes 70 to 500 mcg of estradiol each day. After menopause, however, the majority of endogenous estrogen is produced by transformation of androstenedione (which is secreted by the adrenal cortex) to estrone in the peripheral tissues. Both estrone and its sulphate conjugated form, estrone sulphate, represent the most abundant estrogens found in postmenopausal women.
Prefest 30 Day, however, is considerably more potent than estrone and estriol at the estrogen receptor (ER). As a result, the higher estrone concentration in postmenopausal population, can cause various undesirable effects. These effects may include hot flashes, chills, vaginal dryness, mood swings, irregular menstruation, and chills, in addition to sleep problems.
Prefest 30 Day workings by binding to subtypes of the estrogen receptor: estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). It also exerts potent agonism of G Protein-coupled estrogen receptor (GPER), which is recognized an important regulator of this drug's rapid effects. Once the estrogen receptor has bound to its ligand, it enters the nucleus of the target cell, regulating gene transcription and formation of of messenger RNA. This mRNA makes contact with ribosomes producing specific proteins that express the effect of estradiol upon the target cell. Agonism of estrogen receptors increases pro-estrogenic effects, leading to the relief of vasomotor and urogenital symptoms of a postmenopausal or low estradiol state.
Dosage
Prefest 30 Day dosage
Oral:
- Prostate cancer: 10 mg 3 times/day for at least 3 month.
- Menopausal vasomotor symptoms: 1-2 mg/day on a cyclical or continuous regimen
- Prevention of postmenopausal osteoporosis: 0.5 mg/day in cyclical regimen.
- Hypogonadism: 1-2 mg/day in a cyclic regimen.
Vaginal:
- Vulvular and vag atrophy: Insert 2-4 g/day for 2 wk. Maintenance: 1 g 1-3 times/wk.
- Postmenopausal vag atrophy; Urogenital symptoms: Insert a ring and keep in place for 90 days.
- Atrophic vaginitis: Insert 1 tab once daily for 2 wk. Maintenance: 1 tab twice wkly. Attempt to discontinue or taper medication at 3-6 monthly intervals.
Side Effects
GI disturbances, genitourinary changes, haematologic disorders, CV and CNS effects, endocrine and metabolic disorders, cholestatic jaundice, local skin reactions, chorea, contact lens intolerance, steeping of corneal curvature, pulmonary thromboembolism, carbohydrate intolerance.
Toxicity
The NOAEL (no-observed-adverse-effect-level) oral toxicity of estradiol after 90 day in rats was 0.003 mg/kg/day for blood, female reproductive, and male reproductive, endocrine, and liver toxicity. Oral TDLO of ethinyl estradiol is 21 mg/kg/21D intermittent, woman) with an oral LD50 of 960 mg/kg in the rat.
There is limited information in the literature regarding estrogen overdose. Prefest 30 Day overdose likely leads to the occurrence of estrogen-associated adverse effects, including nausea, vomiting, abdominal pain, breast tenderness, venous thrombosis, and vaginal bleeding. It is generally recommend to discontinue estradiol treatment and offer supportive care in the case of an overdose.
Precaution
Conditions exacerbated by fluid retention; hypercalcaemia, cerebrovascular diorders, coronary artery disease, gall bladder diseases; lipid effects; familial defects of lipoprotein metabolism. May increase BP, risk of venous thromboembolism, breast cancer, benign hepatic adenoma, endometrial cancer and size of preexisting uterine leiomyomata. Dosage should be reduced in hepatic impairment. Lactation. Child.
Interaction
CYP1A2 and CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, phenobarbital, and rifampin may decrease the effects of estradiol. May enhance the effects of hydrocortisone and prednisolone when used together.
Food Interaction
No interactions found.[Minor] Coadministration with grapefruit juice may increase the bioavailability of oral estrogens.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruits.
In a small, randomized, crossover study, the administration of ethinyl estradiol with grapefruit juice (compared to herbal tea) increased peak plasma drug concentration (Cmax) by 37% and area under the concentration-time curve (AUC) by 28%.
Based on these findings, grapefruit juice is unlikely to affect the overall safety profile of ethinyl estradiol.
However, as with other drug interactions involving grapefruit juice, the pharmacokinetic alterations are subject to a high degree of interpatient variability.
Also, the effect on other estrogens has not been studied.
Prefest 30 Day Cholesterol interaction
[Moderate] Although estrogens have generally favorable effects on plasma lipids, including increases in HDL and decreases in total cholesterol and LDL, they have also been associated with significant elevations in triglyceride levels, particularly when high dosages are used.
Severe hyperlipidemia is known to sometimes cause pancreatitis.
Patients with preexisting hyperlipidemia may require closer monitoring during estrogen therapy, and adjustments made accordingly in their lipid-lowering regimen.
Prefest 30 Day Hypertension interaction
[Major] The risk of myocardial infarction and strokes, including those associated with oral contraceptive use and some estrogen use, is increased in patients with hypertension.
Moreover, estrogens (and progestogens) may elevate blood pressure and worsen the hypertension, thus compounding the risk.
Clinically significant blood pressure increases have been reported during estrogen therapy, particularly in patients receiving high dosages or treated with oral contraceptive combinations having high progestational activity.
These effects also increase with duration of therapy and patient age.
Therapy with estrogens should be administered cautiously in patients with preexisting hypertension.
Patients should be monitored for changes in cardiovascular status, and their antihypertensive regimen adjusted or estrogen therapy withdrawn as necessary.
In patients requiring contraception, alternative methods should be considered for those who are hypertensive, over age 35, and smoke.
Prefest 30 Day Drug Interaction
Moderate: levothyroxine, levothyroxineUnknown: duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, montelukast, montelukast, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam, cetirizine, cetirizine
Prefest 30 Day Disease Interaction
Major: abnormal vaginal bleeding, carcinomas (estrogenic), hypercalcemia in breast cancer, hypertension, thromboembolism/cardiovascular, hepatic neoplasmsModerate: angioedema, gallbladder disease, hypercalcemia, hyperlipidemia, liver disease, melasma, depression, fluid retention, glucose intolerance, retinal thrombosis, thyroid function tests
Volume of Distribution
Estrogens administered exogenously distribute in a similar fashion to endogenous estrogens. They can be found throughout the body, especially in the sex hormone target organs, such as the breast, ovaries and uterus.
Elimination Route
The absorption of several formulations of estradiol is described below:
Oral tablets and injections
First-pass metabolism in the gastrointestinal tract rapidly breaks down estradiol tablets before entering the systemic circulation. The bioavailability of oral estrogens is said to be 2-10% due to significant first-pass effects. The esterification of estradiol improves the administration (such as with estradiol valerate) or to sustain release from intramuscular depot injections (including estradiol cypionate) via higher lipophilicity. After absorption, the esters are cleaved, which leads to the release of endogenous estradiol, or 17β-estradiol.
Transdermal preparations
The transdermal preparations slowly release estradiol through intact skin, which sustains circulating levels of estradiol during a 1 week period of time. Notably, the bioavailability of estradiol after transdermal administration is about 20 times higher than after oral administration. Transdermal estradiol avoids first pass metabolism effects that reduce bioavailability. Administration via the buttock leads to a Cmax of about 174 pg/mL compared to 147 pg/mL via the abdomen.
Spray preparations
After daily administration, the spray formulations of estradiol reach steady state within 7-8 days. After 3 sprays daily, Cmax is about 54 pg/mL with a Tmax of 20 hours. AUC is about 471 pg•hr/mL.
Vaginal ring and cream preparations
Prefest 30 Day is efficiently absorbed through the mucous membranes of the vagina. The vaginal administration of estrogens evades first-pass metabolism. Tmax after vaginal ring delivery ranges from 0.5 to 1 hour. Cmax is about 63 pg/mL. The vaginal cream preparation has a Cmax of estradiol (a component of Premarin vaginal estrogen conjugate cream) was a Cmax of 12.8 ± 16.6 pg/mL, Tmax of 8.5 ± 6.2 hours, with an AUC of 231 ± 285 pg•hr/mL.
Half Life
The terminal half-lives for various estrogen products post oral or intravenous administration has been reported to range from 1-12 hours. One pharmacokinetic study of oral estradiol valerate administration in postmenopausal women revealed a terminal elimination half-life of 16.9 ± 6.0 h. A pharmacokinetic study of intravenous estradiol administration in postmenopausal women showed an elimination half-life of 27.45 ± 5.65 minutes. The half-life of estradiol appears to vary by route of administration.
Clearance
In one pharmacokinetic study, the clearance of orally administered micronized estradiol in postmenopausal women was 29.9±15.5 mL/min/kg. Another study revealed a clearance of intravenously administered estradiol was 1.3 mL/min/kg.
Elimination Route
Prefest 30 Day is excreted in the urine with both glucuronide and sulfate conjugates.
Pregnancy & Breastfeeding use
Pregnancy Category X. Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Contraindication
Hypersensitivity; undiagnosed vag bleeding; thrombophloebitis or thromboembolic disorders; breast carcinoma except in selected patients being treated for metastatic disease; oestrogen-dependent tumor; porphyria; pregnancy.
Storage Condition
Store at room temperature.
Innovators Monograph
You find simplified version here Prefest 30 Day
Prefest 30 Day contains Estradiol see full prescribing information from innovator Prefest 30 Day Monograph, Prefest 30 Day MSDS, Prefest 30 Day FDA label
FAQ
What is Prefest 30 Day used for?
Prefest 30 Day is a form of estrogen, a female sex hormone that regulates many processes in the body. Prefest 30 Day is used to treat menopause symptoms such as hot flashes and vaginal changes, and to prevent osteoporosis (bone loss) in menopausal women.
How safe is Prefest 30 Day?
In postmenopausal women, estrogens, taken with or without a Prefest 30 Day, increase the risk of cancer of the breast/ovaries, stroke, dementia, and serious blood clots. When used along with a Prefest 30 Day, estrogens also increase the risk of heart disease (such as heart attacks). Prefest 30 Day topical should not be used to prevent heart disease, stroke, or dementia.
How does Prefest 30 Day work?
Prefest 30 Day works by replacing Prefest 30 Day that your body normally produces.
What are the common side effects of Prefest 30 Day?
Common side effects of Prefest 30 Day are include:
- Abdominal cramping.
- Anxiety.
- Bloating.
- Breakthrough bleeding.
- Breast enlargement.
- Breast tenderness/pain/swelling.
- Freckles or darkening of facial skin (melasma)
- Changes in menstrual periods.
Is Prefest 30 Day safe during pregnancy?
Prefest 30 Day should not be used during pregnancy. There appears to be little or no increased risk of birth defects in children born to women who inadvertently used Prefest 30 Day during early pregnancy.
Is Prefest 30 Day safe during breastfeeding?
Prefest 30 Day is not recommended in nursing mothers. Prefest 30 Day pass into the breast milk and may decrease the amount and quality of breast milk. Caution should be exercised in mothers who are using estrogen and breast-feeding
Can I drink alcohol with Prefest 30 Day?
You should avoid smoking and drinking alcohol. You may also wish to not consume grapefruit or grapefruit juice while using Prefest 30 Day as it may result in increased levels in the blood.
What is the best time to take Prefest 30 Day?
Take this medication by mouth with or without food as directed by your doctor. You may take it with food or right after a meal to prevent stomach upset.
How many time can I take Prefest 30 Day daily?
One to three times a day for 3 to 6 months.
How long does Prefest 30 Day take to work?
It can take up to 4 months to see the full effect of the Prefest 30 Day. Your doctor may reconsider continuing your Prefest 30 Day treatment or may lower your dose several times within the first one or two months, and every 3 to 6 months after that.
Who should not take Prefest 30 Day?
You should not use Prefest 30 Day if you have: undiagnosed vaginal bleeding, liver disease, a bleeding disorder, or if you have ever had a heart attack, a stroke, a blood clot, or cancer of the breast, uterus/cervix, or vagina. Do not use Prefest 30 Day if you are pregnant.
What happen If I missed Prefest 30 Day?
If you miss a dose and it is more than 2 hours until your next dose, take the missed dose as soon as possible with food, then go back to your regular time. If you miss a dose and it is within 2 hours of your next evening dose, skip the missed dose and go back to your regular dosing schedule.
What happens if I overdose?
Seek emergency medical attention. Overdose can result in nausea, vomiting and vaginal bleeding. Symptoms of an Prefest 30 Day overdose include: Breast tenderness. Drowsiness. Excessive vaginal bleeding (2 to 7 days after overdose).
What happen If I stop taking Prefest 30 Day?
Most don't have any problems while they stop, however, stopping suddenly does increase the risk of menopausal symptoms returning, so you should not stop taking your HRT without consulting your doctor. Doctors may differ in how they taper their patients off HRT.
Will Prefest 30 Day affect my fertility?
Yes, and on either end of the spectrum. Prefest 30 Day is one of the hormones that keep our menstrual cycles going, so when levels are too low or too high, that can cause disruption.
Can Prefest 30 Day cause heart palpitations?
Another common symptom that women experience during menopause due to low Prefest 30 Day levels are heart palpitations. Lower Prefest 30 Day levels can overstimulate the heart and cause arrhythmias.
Can Prefest 30 Day cause liver problems?
Postmenopausal women are also reported to have a higher risk of liver fibrosis than premenopausal women, suggesting that Prefest 30 Day is associated with liver protection from fibrosis.
Can Prefest 30 Day affet my kidney?
One of the most important actions of the Prefest 30 Day is represented by the protective effect on the kidneys, Prefest 30 Day attenuating glomerulosclerosis and tubulo-interstitial fibrosis.
Does Prefest 30 Day make my gain weight?
Lower levels of Prefest 30 Day may lead to weight gain.
Can Prefest 30 Day cause hair loss?
Prefest 30 Day is related to hair growth — and hair loss.