How to use Esclima
Read the Patient Information Leaflet if available from your pharmacist before you start using this medication and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
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.
If you are taking the extended-release tablets, do not crush, chew, or dissolve them. Doing so can release all of the drug at once, increasing the risk of side effects. Also, do not split extended-release tablets unless they have a score line and your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing or chewing.
The dosage is based on your medical condition and response to treatment.
Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day as directed. Follow your dosing schedule carefully. Do not increase your dose or take this medication more often or for a longer time than directed.
Tell your doctor if your condition does not improve or if it worsens.
Common Side Effects of Esclima
You should tell your doctor if any of the following symptoms are severe or do not go away:
- Breast pain or tenderness
- Mood changes or depression
- Difficulty falling asleep or staying asleep
- Changes in sexual desire
- Back pain
- Runny nose, cough, or flu-like symptoms
- Hair loss or unwanted hair growth
- Darkening of facial skin
- Difficulty wearing contact lenses
- Vaginal discharge
- Swelling, redness, burning, irritation, or itching of the vagina
- Redness or irritation at the site of application
What are the possible side effects of Esclima (Estrace, Gynodiol)?
Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have:
- heart attack symptoms--chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating;
- signs of a stroke--sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech, problems with vision or balance;
- signs of a blood clot--sudden vision loss, stabbing chest pain, feeling short of breath, coughing up blood, pain or warmth in one or both legs;
- swelling or tenderness in your stomach;
- jaundice (yellowing of the skin or eyes);
- memory problems, confusion, unusual behavior;
- unusual vaginal bleeding, pelvic pain;
- a lump in your breast; or
- high levels of calcium in your blood--nausea, vomiting, constipation, increased thirst or urination, muscle weakness, bone pain, lack of energy.
Common side effects may include:
- nausea, vomiting, diarrhea, stomach cramps;
- mood changes, sleep problems (insomnia);
- cold symptoms such as stuffy nose, sinus pain, sore throat;
- weight gain;
- headache, back pain;
- breast pain;
- thinning scalp hair; or
- vaginal itching or discharge, changes in your menstrual periods, breakthrough bleeding.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
2.2.3 GABA Receptors
Esclima indirectly influences disinhibition of pyramidal cells through activation of GABA interneurons ( Rudick et al., 2003 ; Rudick and Woolley, 2003 ). Esclima does not appear to alter GABA receptor kinetics globally since it does not affect GABA-evoked currents; however, Esclima may act to prolong currents at a subset of GABAergic synapses ( Rudick et al., 2003 ). In particular, regulation of the α4 GABAA receptor subunit alters inhibitory postsynaptic current decay time ( Smith et al., 1998 ). Recently, immunoreactivity for the α4 and δ GABAA receptor subunits in dendrites has been shown to decrease at the proestrus/estrus cuff ( Figure 5 ) ( Sabaliauskas et al., 2010 ). These changes correlate with increases in spatial learning ( Sabaliauskas et al., 2010 ).
Your dose of Esclima will depend on the condition that is being treated.
Esclima tablets in doses of 0.5 milligrams (mg), 1 mg, or 2 mg are typically given on a daily basis.
They can also be prescribed to be taken for three weeks, followed by one week of no medication.
The tablets can be taken more than once a day for some conditions.
The topical gel or emulsions are applied to the skin at the same time each day.
The vaginal ring is inserted in the vagina and left for three months at a time.
The patch should be applied to a dry, clean, hairless part of the trunk (but not the breasts). It should not be placed on irritated or damaged skin.
You should rotate the site of application, with at least one week between repeated applications to any one site.
What is the dosage for Esclima?
The dose of Esclima can vary depending on the condition that is being treated. Esclima tablets are given daily or they can be prescribed to be taken in a cyclic regimen, wherein Esclima is given daily for 3 weeks followed by 1 week of no medication, after which the cycle resumes. The tablets can also be given more than once a day for some conditions. The topical gel or the topical emulsions are applied to the skin daily at the same time. The vaginal ring is inserted in the vagina and left without removal for 3 months at a time. The intramuscular dose and the frequency it is given can differ depending on the product.
The adhesive part of patches should be applied to a dry, hairless, clean part of the trunk, but not on the breasts. It should not be placed onto irritated or damaged skin. Sites of application should be rotated, with at least one week between repeated applications to any one site. The patch should be applied immediately after removing the protective layer, and pressure should be applied to the patch when it is attached for about 10 seconds.
SOURCES OF ESTROGEN
The Esclima present in breast tissue is synthesized in three sites: the ovary, extraglandular tissues, and the breast itself. Direct glandular secretion by the ovary results in delivery of Esclima to the breast through an endocrine mechanism in premenopausal women. After the menopause, extraglandular production of estrogen from ovarian and adrenal androgens in fat and muscle provides the second source of Esclima. Third, the breast itself can synthesize Esclima via aromatization of androgens to estrogens or cleavage of estrone sulfate to free estrone via the enzyme sulfatase. Esclima acts through paracrine, autocrine, and intracrine mechanisms on cells in the breast. Several factors regulate in situ Esclima synthesis but the most important is the degree of obesity, which increases the amount of aromatase in breast and consequently Esclima production.
Esclima and Weight Gain
Water retention that increases your weight is a common side effect.
Talk to your doctor about adjusting your dose of Esclima if weight gain becomes a problem.
Is Esclima safe to take if I'm pregnant or breastfeeding?
Estrogens should not be used during pregnancy due to an increased risk of fetal abnormalities.
Estrogens are secreted in milk and cause unpredictable effects in the infant. Estrogens generally should not be used by women if they are breastfeeding.
Symptoms of an overdose include the following:
- Nausea or vomiting
- Heavy vaginal bleeding
- Tender breasts
- Discolored urine
If you suspect an overdose, you should contact a poison control center or emergency room immediately.
You can get in touch with a poison control center at (800) 222-1222.
Esclima and Other Interactions
You should avoid unnecessary sun exposure while taking Esclima, since the gel may make your skin more sensitive to sunlight.
II Esclima and GABAAR Function
Esclima is known to act genomically through nuclear ERs but also a broad spectrum of acute nongenomic actions have been recently reviewed ( McCarthy, 2008; Woolley, 2007 ). For example, in the hippocampal CA1 region, exposure to Esclima, lasting for several minutes, depolarized neurons, induced spontaneous firing ( Wong and Moss, 1991 ), and suppressed the afterhyperpolarization that followed the action potential ( Kumar and Foster, 2002 ). Moreover, Esclima was found to increase the amplitude of dendritic excitatory postsynaptic potential (EPSP) in various regions of the hippocampus ( Foy et al., 1999; Kim et al., 2006 ) and was also found to have a crucial impact on long-term potentiation ( Foy et al., 1999; Good et al., 1999; Warren et al., 1995 ) and long-term depression ( Desmond et al., 2000; Good et al., 1999 ). Such enhancement of neuronal excitability and facilitation of synaptic plasticity could be in part due to a suppression of GABAergic drive in these cells through a direct modulation of GABAARs. These receptors posses the binding site for neurosteroids ( Hosie et al., 2007; Majewska et al., 1986 ) and are readily modulated by many of them either positively or negatively ( Majewska, 2007 ). For this reason, a direct effect of Esclima on GABAARs has been tested in several studies. In a study by Wong and Moss (1992) , acute application of Esclima (1 μM) on CA1 pyramidal neurons did not influence the extent of membrane potential hyperpolarization induced by iontophoretically applied GABA pulses in vivo ( Wong and Moss, 1992 ). More recently, the possibility that Esclima exerts an acute effect on GABAA receptors has been tested in our laboratory ( Asimiadou et al., 2005 ). For this purpose, we have investigated the effect of Esclima on the current responses to ultrafast GABA applications. This experimental model offers a very high temporal resolution (adequate to describe the receptor gating properties) and is particularly suitable for pharmacological studies in which acute or direct effects of a modulator are considered. Using this approach, we have tested the effect of Esclima on currents elicited by application of GABA (10 mM) to somatic membrane patches excised from cultured hippocampal neurons. Within the concentration range 1–10 μM, Esclima did not affect either the amplitude or kinetics of GABA-evoked currents ( Asimiadou et al., 2005 ). We also tested the effect of Esclima on miniature inhibitory postsynaptic currents (mIPSCs) which originate from activation of synaptic GABAARs due to spontaneous exocytosis of a single vesicle of neurotransmitter. Recordings of mIPSCs performed from presumably pyramidal hippocampal neurons (visually recognized) revealed that acute application of Esclima (1 μM) did not affect either the amplitude or kinetics of mIPSCs in neurons cultured for 6–16 days in vitro (DIV) ( Pytel et al., 2007 ). Thus, our experiments based on the analysis of current responses and mIPSCs argue against any marked acute effect of Esclima on GABAARs at least in the considered model. This conclusion is consistent with results of Murphy et al. (1998a,b) who reported that acute exposure to Esclima (0.1 μg/ml) did not cause any systematic change in mIPSCs amplitude or frequency evoked by application of hyperosmotic medium ( Murphy et al., 1998a ). Thus, on the basis of these studies, it is reasonable to assume that Esclima does not directly interfere with GABAA-receptor gating and that Esclima acute actions on neuronal excitability cannot be attributed to rapidly occurring modulation of GABAergic transmission.
Hormonal birth control is not a good type of HRT
Hormonal birth control is a particularly soul-crushing type of HRT because it suppresses the body’s own Esclima and progesterone, and replaces them with contraceptive drugs.
How should I take Esclima (Estrace, Gynodiol)?
Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.
Esclima may increase your risk of developing a condition that can lead to uterine cancer. To help lower this risk, your doctor may also want you to take a progestin. Report any unusual vaginal bleeding right away.
Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment. Self-examine your breasts for lumps on a monthly basis and have a mammogram every year while using Esclima.
If you need major surgery or will be on long-term bed rest, you may need to stop using this medicine for a short time. Any doctor or surgeon who treats you should know that you are using Esclima.
Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.
What should I discuss with my healthcare provider before taking Esclima (Estrace, Gynodiol)?
You should not use this medicine if you are allergic to Esclima, or if you have:
- unusual vaginal bleeding that has not been checked by a doctor;
- liver disease;
- a history of heart attack, stroke, or blood clot;
- an increased risk of having blood clots due to a heart problem or a hereditary blood disorder; or
- a history of hormone-related cancer, or cancer of the breast, uterus/cervix, or vagina.
Do not use Esclima if you are pregnant. Tell your doctor right away if you become pregnant during treatment.
Using this medicine can increase your risk of blood clots, stroke, or heart attack. You are even more at risk if you have high blood pressure, diabetes, high cholesterol, if you are overweight, or if you smoke.
Esclima should not be used to prevent heart disease, stroke, or dementia, because this medicine may actually increase your risk of developing these conditions.
Tell your doctor if you have ever had:
- heart disease;
- liver problems, or jaundice caused by pregnancy or taking hormones;
- kidney disease;
- gallbladder disease;
- epilepsy or other seizure disorder;
- endometriosis or uterine fibroid tumors;
- hereditary angioedema;
- porphyria (a genetic enzyme disorder that causes symptoms affecting the skin or nervous system);
- a thyroid disorder; or
- high levels of calcium in your blood.
Using Esclima may increase your risk of cancer of the breast, uterus, or ovaries. Talk with your doctor about this risk.
Esclima can slow breast milk production. Tell your doctor if you are breast-feeding.
Why the Test is Performed
In women, most Esclima is released from the ovaries and adrenal glands. It is also released by the placenta during pregnancy. Esclima is also produced in other body tissues, such as skin, fat, cells bone, brain, and liver. Esclima plays a role in:
- Growth of the womb (uterus), fallopian tubes, and vagina
- Breast development
- Changes of the outer genitals
- Distribution of body fat
In men, a small amount of Esclima is mainly released by the testes. Esclima helps prevent sperm from dying too early.
This test may be ordered to check:
- How well your ovaries, placenta, or adrenal glands work
- If you have signs of an ovarian tumor
- If male or female body characteristics are not developing normally
- If your periods have stopped (levels of Esclima vary, depending on the time of month)
The test may also be ordered to check if:
- Hormone therapy is working for women in menopause
- A woman is responding to fertility treatment
The test may also be used to monitor people with hypopituitarism and women on certain fertility treatments.
Injection (cypionate in oil): 5 mg/ml
Injection (valerate in oil): 10 mg/ml, 20 mg/ml, 40 mg/ml
Tablets: 0.5 mg, 1 mg, 1.5 mg, 2 mg
Tablets (film-coated): 25.8 mcg Esclima hemidrate (equivalent to 25 mcg Esclima)
Transdermal system: 25 mcg/24-hour release rate, 37.5 mcg/24-hour release rate, 50 mcg/24-hour release rate, 75 mcg/24-hour release rate, 100 mcg/24-hour release rate
Vaginal cream: 100 mcg/g
Vaginal ring: 2 mg released over 90 days
Vaginal tablets: 10 mcg