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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Estrone, Sodium Chloride, Sepia Officinalis Juice
Brand Name
Cyclease Pms
Generic Name
Estrone, Sodium Chloride, Sepia Officinalis Juice
Active Ingredient
EstroneCategory
Non-Standardized Food Allergenic Extract [EPC]
Variants
1
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 15 [hp_C]/1 | TABLET | ORAL | 0220-9081 |
Detailed information about Cyclease Pms
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Cyclease Pms, you must consult a qualified healthcare professional.
Estrone is a naturally occurring steroidal estrogen, often used in hormone replacement therapy (HRT) to manage symptoms of menopause and estrogen deficiency. It belongs to the Estrogen [EPC] class and is vital for maintaining reproductive and bone health in women.
Dosage for Estrone must be highly individualized, using the lowest effective dose for the shortest duration consistent with treatment goals. For vasomotor symptoms (hot flashes), the typical starting dose of conjugated estrogens (containing estrone) is 0.3 mg to 1.25 mg daily. For atrophic vaginitis, localized vaginal creams are often preferred, typically administered at 0.5 g to 2 g daily for 3 weeks followed by a 1-week rest period.
In cases of female hypogonadism, the dose may range from 2.5 mg to 7.5 mg daily in divided doses for 20 days, followed by a 10-day rest period. If the patient has an intact uterus, a progestogen is usually added for the last 10-14 days of the cycle to prevent endometrial hyperplasia (overgrowth of the uterine lining).
Estrone is generally not approved for use in pediatric populations except in very specific cases of delayed puberty or primary ovarian failure under the strict supervision of a pediatric endocrinologist. Safety and efficacy in children have not been established for general use. If used, dosing is based on bone age and pubertal stage rather than weight.
There are no specific dosage adjustment guidelines for patients with renal impairment; however, since estrogen metabolites are excreted renally, these patients should be monitored closely for signs of estrogen excess.
Estrone is contraindicated in patients with acute liver disease or a history of hepatic impairment where liver function tests have not returned to normal. The liver is the primary site of estrogen metabolism, and impaired function can lead to dangerously high systemic levels.
Data from the Women's Health Initiative (WHI) suggest that women over age 65 starting estrogen therapy have an increased risk of developing probable dementia. Dosing in the elderly should be approached with extreme caution, focusing on the lowest possible dose.
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and resume your regular schedule. Do not double the dose to catch up, as this can increase the risk of side effects like breakthrough bleeding or breast tenderness.
Signs of an Estrone overdose may include severe nausea, vomiting, breast tenderness, abdominal pain, and withdrawal bleeding in females. In the event of a suspected overdose, contact your local poison control center or seek emergency medical attention immediately. Treatment is generally supportive, as there is no specific antidote for estrogen toxicity.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose or stop taking Estrone without medical guidance, as sudden discontinuation can cause a return of symptoms or withdrawal bleeding.
Patients taking Estrone frequently report the following symptoms, which are often dose-dependent and may subside as the body adjusts to the hormone therapy:
> Warning: Stop taking Estrone and call your doctor immediately if you experience any of these symptoms. These may indicate life-threatening complications.
Prolonged use of Estrone, especially without a progestogen in women with a uterus, significantly increases the risk of endometrial cancer. Long-term use (typically 5 years or more) is also associated with a slightly increased risk of breast cancer and ovarian cancer. Additionally, there is a risk of developing dementia in women who begin therapy after the age of 65. Regular screening and 'drug holidays' (periodic re-evaluation of the need for therapy) are essential for long-term safety.
Estrone-containing products carry the FDA's most serious warning regarding:
Report any unusual symptoms or persistent side effects to your healthcare provider immediately to ensure your treatment plan remains safe and effective.
Estrone is a potent hormone that affects multiple organ systems. It should never be used for the prevention of cardiovascular disease or dementia. Before starting Estrone, a complete medical and family history must be taken, including blood pressure, breast examination, and a pelvic exam (including a Pap smear). Periodic re-evaluations (at least every 6 months) are required to determine if therapy is still necessary.
Patients on Estrone require regular clinical monitoring:
Estrone generally does not interfere with the ability to drive or operate machinery. However, if you experience dizziness or severe headaches as a side effect, avoid these activities until you know how the medication affects you.
Alcohol consumption can increase circulating levels of Estrone and estradiol. Chronic heavy drinking may further increase the risk of breast cancer in women taking hormone replacement therapy. It is advised to limit alcohol intake while on Estrone.
When discontinuing Estrone, many physicians recommend a gradual taper (reducing the dose over several weeks) rather than stopping abruptly. Abrupt cessation can lead to a rapid return of vasomotor symptoms (hot flashes) and withdrawal bleeding. Always consult your doctor before stopping the medication.
> Important: Discuss all your medical conditions, especially any history of cancer, blood clots, or liver disease, with your healthcare provider before starting Estrone.
Estrone should NEVER be used in combination with:
Estrone can affect several laboratory test results:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. Even 'natural' products can cause dangerous interactions with hormone therapy.
Estrone must NEVER be used in patients with the following conditions:
Conditions requiring a careful risk-benefit analysis include:
Patients who have had allergic reactions to other steroidal hormones (such as estradiol, estriol, or certain progestogens) should use Estrone with caution, as cross-sensitivity is possible. Signs of an allergic reaction include skin rash, itching, and swelling of the extremities.
> Important: Your healthcare provider will evaluate your complete medical history, including family history of cancer and cardiovascular disease, before prescribing Estrone.
FDA Pregnancy Category X: Estrone is contraindicated during pregnancy. There is no therapeutic indication for Estrone during pregnancy, and exposure to estrogens during gestation has been associated with an increased risk of reproductive tract abnormalities in the offspring and potentially an increased risk of certain cancers later in the child's life. If pregnancy occurs while taking Estrone, the medication must be discontinued immediately.
Estrogens have been shown to be excreted in human breast milk and can decrease both the quantity and the quality of milk produced. Because of the potential for adverse effects in the nursing infant (including premature breast development), Estrone is generally not recommended for use during breastfeeding. Alternative methods of symptom management should be discussed with a healthcare provider.
Safety and effectiveness in pediatric patients have not been established. Use in children is limited to rare cases of hormonal replacement for primary ovarian failure or certain genetic conditions. In these cases, estrogens can accelerate epiphyseal closure (the end of bone growth), potentially resulting in shorter adult stature. Monitoring of bone age every 6 months is typically required.
Clinical studies, including the WHI, have shown that women over age 65 are at a higher risk of stroke and probable dementia when taking estrogen therapy. There is also an increased risk of gallbladder disease in this population. For women over 65, the necessity of continuing HRT should be re-evaluated annually, with a strong emphasis on the lowest possible dose.
While specific dose adjustments are not provided by manufacturers, the kidneys are responsible for excreting conjugated estrogen metabolites. Patients with end-stage renal disease or significant impairment should be monitored for signs of estrogen excess, such as severe fluid retention or hypertension.
Estrone is contraindicated in patients with active hepatic disease. In patients with stable, chronic liver impairment, estrogens should be used with extreme caution. The liver's reduced ability to metabolize estrogens can lead to accumulation, increasing the risk of serious side effects like blood clots and estrogen-dependent cancers.
> Important: Special populations require individualized medical assessment and more frequent monitoring to ensure the benefits of therapy outweigh the risks.
Estrone (E1) is a steroidal estrogen that acts primarily as a nuclear receptor agonist. It enters target cells and binds to the Estrogen Receptor (ER) subtypes, ER-alpha and ER-beta. This binding induces a conformational change in the receptor, allowing it to dimerize and translocate into the nucleus. The receptor-ligand complex then binds to Estrogen Response Elements (EREs) on the DNA, recruiting co-activators or co-repressors to modulate gene transcription. This results in the synthesis of proteins that regulate various physiological processes, including the growth of the uterine lining, the maintenance of bone density, and the regulation of the hypothalamic-pituitary-gonadal axis.
Estrone is less potent than estradiol but more potent than estriol. It has a higher affinity for the ER-alpha receptor than for ER-beta. In postmenopausal women, Estrone is the most abundant circulating estrogen. Its effects are systemic, influencing the cardiovascular system (by increasing HDL and decreasing LDL cholesterol), the skeletal system (by decreasing bone resorption), and the central nervous system (by modulating thermoregulation).
| Parameter | Value |
|---|---|
| Bioavailability | 3-5% (Oral due to high first-pass) |
| Protein Binding | 95-98% (to SHBG and Albumin) |
| Half-life | 10 - 24 hours (as part of conjugated complex) |
| Tmax | 4 - 10 hours (Oral) |
| Metabolism | Hepatic (CYP3A4, CYP1A2) |
| Excretion | Renal (>90% as conjugates) |
Estrone is classified as a Natural Estrogen within the broader therapeutic class of Hormone Replacement Therapy (HRT). It is often grouped with other estrogens like estradiol and estriol. Related medications include conjugated estrogens (Premarin) and esterified estrogens (Estratab).
Common questions about Cyclease Pms
Estrone is primarily used in hormone replacement therapy (HRT) to treat moderate to severe symptoms of menopause, such as hot flashes and night sweats. It is also prescribed for atrophic vaginitis, which involves the thinning and drying of vaginal tissues due to low estrogen levels. Additionally, healthcare providers may use Estrone to treat female hypogonadism or primary ovarian failure. In some cases, it is used to prevent postmenopausal osteoporosis in women at high risk for bone fractures. It may also be used as a palliative treatment for certain types of advanced cancers, such as prostate or breast cancer, under specific clinical conditions.
The most common side effects experienced by patients taking Estrone include breast tenderness or enlargement, headaches, and mild fluid retention (edema). Many women also report nausea, especially when first starting the medication, and abdominal cramping or bloating. Changes in vaginal discharge or the development of a yeast infection (vaginal candidiasis) are also frequent. Some patients may notice mild weight fluctuations or mood swings. While these symptoms are often manageable, it is important to discuss them with a doctor if they become persistent or severe.
It is generally advised to limit or avoid alcohol while taking Estrone. Alcohol consumption can interfere with the way the liver processes estrogen, leading to higher-than-normal levels of the hormone in your bloodstream. This increase can heighten the risk of side effects and, according to some studies, may further increase the risk of breast cancer in women on hormone therapy. Chronic heavy drinking is particularly concerning as it can also strain the liver, which is the primary organ responsible for metabolizing Estrone. Always consult your healthcare provider regarding your specific alcohol consumption habits.
No, Estrone is not safe during pregnancy and is classified as FDA Pregnancy Category X. It is strictly contraindicated because there is no medical need for estrogen replacement during pregnancy, and exposure can cause significant harm to a developing fetus. Research has shown that prenatal exposure to high levels of estrogens can lead to reproductive abnormalities and an increased risk of certain cancers in the child later in life. If you suspect you are pregnant while taking Estrone, you must stop the medication immediately and contact your doctor. It is also not recommended for use while breastfeeding, as it can reduce milk supply and pass into the milk.
The time it takes for Estrone to show noticeable effects depends on the symptom being treated. For vasomotor symptoms like hot flashes, some women may feel improvement within the first 1 to 2 weeks, though it typically takes 4 to 8 weeks to reach the full therapeutic effect. For atrophic vaginitis, localized improvement in tissue health and comfort may take several weeks of consistent use. When used for osteoporosis prevention, the 'work' of the drug is internal and long-term, requiring ongoing therapy to maintain bone density. Your doctor will likely schedule a follow-up after 3 months to evaluate how well the medication is working for you.
Stopping Estrone suddenly is generally not recommended, as it can lead to a rapid return of menopausal symptoms like severe hot flashes and night sweats. Abrupt discontinuation can also trigger withdrawal bleeding, which may be mistaken for a menstrual period. Most healthcare providers suggest a gradual tapering process, where the dose is slowly reduced over several weeks or months to allow the body to adjust. This approach helps minimize the 'rebound' effect of hormonal fluctuations. Always talk to your doctor before making any changes to your dosing schedule to ensure a safe transition.
If you miss a dose of Estrone, you should take it as soon as you remember. However, if it is almost time for your next scheduled dose (within a few hours), it is better to skip the missed dose entirely and return to your normal schedule. You should never take two doses at once to make up for a missed one, as this can increase the risk of side effects like nausea or breast pain. Maintaining a consistent daily routine, perhaps by using a pill organizer or a phone alarm, can help you stay on track. If you miss multiple doses, contact your healthcare provider for specific instructions.
Estrone can cause changes in weight, but this is often due to fluid retention rather than an increase in body fat. Some women notice a 'bloated' feeling or swelling in the ankles and fingers, which can reflect on the scale as a few extra pounds. However, the hormonal changes associated with menopause itself often lead to a redistribution of body fat, particularly toward the abdominal area, which can be confused with drug-induced weight gain. If you notice sudden or significant weight gain while taking Estrone, it is important to report this to your doctor, as it could indicate a problem with fluid management or other underlying issues.
Estrone can interact with many other medications, so it is vital to provide your doctor with a full list of everything you take. It specifically interacts with blood thinners like warfarin, potentially making them less effective, and can interfere with thyroid medications, requiring a dose adjustment for levothyroxine. Drugs that induce or inhibit the CYP3A4 enzyme (like certain antibiotics, anti-seizure meds, or St. John's Wort) can also change how much Estrone stays in your system. Because of these complex interactions, you should not start any new prescription or over-the-counter products without first checking with your pharmacist or physician.
Estrone is available as a generic in certain formulations, though it is most commonly found as a component of 'conjugated estrogens' (like the brand Premarin) or 'esterified estrogens.' Pure estrone injections or tablets are less common today than they were in the past, as micronized estradiol has become the preferred form for many generic hormone therapies. However, generic versions of conjugated estrogen tablets and creams are widely available and are generally more cost-effective than brand-name products. Your pharmacist can help determine if a generic equivalent is available for the specific form of Estrone your doctor has prescribed.
Other drugs with the same active ingredient (Estrone)