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Свидетельство о регистрации средства массовой информации Эл № ФС77-79153 выдано Федеральной службой по надзору в
сфере связи, информационных технологий и массовых коммуникаций (Роскомнадзор) 15 сентября 2020 года.
Copyright © Справочник Видаль «Лекарственные препараты в России»
Company: P.V.L.
DIN: 00345318
Active Ingredient(s): The sterile solution is available in 4 mg/mL concentration in cottonseed oil containing 5 mg anhydrous chlorobutanol (chloral deriv.), as a preservative.
Estradiol Cypionate in Oil Indications
ESTRADIOL CYPIONATE has a wide range of usefulness in veterinary practice as it offers all of the functional activity of natural estrogenic substances with prolonged action.
The indications in animal medicine include the following:
1. To correct anestrus (absence of heat period) in the absence of follicular cysts.
2. To treat cattle having a persistent corpus luteum.
3. To expel purulent material from the uterus in pyometra of cows.
4. As replacement therapy in spayed female dogs, particularly to treat those with urinary incontinence.
5. To stimulate uterine expulsion of retained placentas and mummified fetuses.
6. To prevent implantation of the fertilized ova in the mismated bitch.
Clinical evidence indicates value as palliative treatment for benign anal tumors in aged male dogs.
Pharmacology
The product is the oil-soluble 17β-cyclopentylpropionate ester of “alpha” estradiol. It provides estradiol-17β, believed to be the most potent of the naturally occurring estrogens, in the form of the cyclopentylpropionate ester, a highly fat-soluble derivative with profound estrogenic effects.
Comparative studies have demonstrated that estradiol cypionate produces estrogenic effects which are qualitatively the same as those produced by other estradiol esters. Estrus is usually induced in the majority of animals following injection of the preparation. Estrus may be maintained for variable periods, depending upon the status of the animal at the time of injection.
Dosage and Administration
ESTRADIOL CYPIONATE sterile solution is for intramuscular injection only. Recommended average doses are as follows and may be repeated, if necessary, in one (1) week.
Do not overdose.
|
mg |
4 mg per mL product |
|
|
Cows: |
||
|
Anestrus |
3-5 |
0.75-1.25 mL |
|
Pyometra |
10 |
2.5 mL |
|
Retained Placenta |
10 |
2.5 mL |
|
Persistent corpus luteum |
4 |
1 mL |
|
Mummified fetus |
10 |
2.5 mL |
|
Heifers: |
||
|
Anestrus |
3 |
0.75 mL |
|
Mares: |
||
|
Anestrus |
5-10 |
0.25-2.5 mL |
|
Ewes: |
||
|
Anestrus |
0.5-1 |
0.125-0.25 mL |
|
Bitches: |
||
|
Anestrus |
0.5-1 |
0.125-0.25 mL |
|
Urinary incontinence |
0.5-1 |
0.125-0.25 mL |
|
False pregnancy |
0.5-1 |
0.125-0.25 mL |
|
Mismating |
0.5-5 |
0.125-1.25 mL |
|
Pyometra |
1-2 |
0.25-0.5 mL |
|
Stud Dogs: |
||
|
Prostatic hypertrophy |
1-2 |
0.25-0.5 mL |
|
Anal Adenoma |
1-2 |
0.25-0.5 mL |
|
Cats: |
||
|
Anestrus |
0.25-0.5 |
0.06-0.12 mL |
|
Chinchillas: |
||
|
Anestrus |
0.2 |
0.05 mL |
Contraindication(s): As with all products of this nature, a complete examination to determine the status of the reproductive tract should be undertaken prior to administration of the drug. Pregnancy may be the prime reason for either anestrus or the persistence of the corpus luteum. Since pregnancy may be terminated by estrogens, estradiol cypionate is contraindicated where a desired pregnancy exists.
Caution(s): For veterinary use only.
Administration of an estrogenic substance to an animal may result in the development of follicular cysts.2
In the case of prolonged persistence of the corpus luteum, a thorough examination should also be made of the uterus to determine the presence of an endometritis or a fetus. The use of the appropriate antimicrobial agents, in addition to estradiol cypionate should be considered if endometritis exists.
In the absence of normally developing follicles on the ovaries, estrus may be produced, but ovulation may not accompany estrus. Because it is impossible to determine exactly if and when ovulation may occur in treated females during an induced heat period, it may help to have the female bred frequently throughout the induced heat periods in order to improve the possibility of conception.
Repeat breeding will improve the chance of conception only if ovulation occurs. In the case of bitches, the prolonged action of estradiol cypionate may, in some instances, interfere with nidation.
When used in mismated bitches, injection should be made as soon as possible after mismating. After nidation of the fertilized ova has taken place, the regimen is ineffective.
Side Effects
Prolonged estrus, precocious development, genital irritation, follicular cysts, and a reduction of milk flow may occur following estrogen therapy, frequently as a result of overdosage. If any of these phenomena are observed, the dosage should be reduced accordingly.
Estrogens used in the canine in large doses may produce a gradual anaemia and a profound leukocytosis which is followed by leukopaenia. Thrombocytopaenia may result with a concomitant alteration in the clotting mechanisms. If marked overdosage occurs, it would be prudent to consider periodic hematology and supportive therapy as deemed necessary.1 Further estrogen therapy should not be undertaken.
Discussion: Anestrus in conjunction with a persistent corpus luteum probably reflects some interference with normal function of the uterine endometrium. As indicated earlier, pregnancy must be considered as a cause of the persistence of the corpus luteum. Prolonged maintenance of the corpus luteum has also occurred following hysterectomy or the experimental induction of endometritis.5-6 It is doubtful that corpora lutea are retained indefinitely in cattle with normal uterine function.4-6 It has been demonstrated that estrogens will cause regression of the corpus luteum in cycling, pregnant, or hysterectomized cattle.7 In the absence of a pregnancy or a detectable uterine malfunction, repeated rectal palpations will be required to establish a diagnosis of persistent corpus luteum. Although estrogens may produce luteal regression, consideration of proper uterine treatment should also be given.
The proper diagnosis of anestrus without frequent rectal palpation is difficult since normal ovarian cycles can occur without accompanying estrus. It has been reported that such “silent heat” is more frequent at the first post-partum estrus.4
Regression of the corpus luteum following estrogen treatment and noticed in cattle may not be noticed in all species; for example, in swine, a persistent corpus luteum may be a sequel of estrogen therapy.8
Trial Data: Recent research findings indicate the necessity for a reappraisal of the causes and effects of anestrus in cattle.
Two recent reports have suggested that frequently cows with a follicular cyst may be more inclined to be anestrual than nymphomaniac.3-4 Many cows will recover spontaneously from anestrus (if due to follicular cysts) if less than 60 days post-parturient.4 In cases of anestrus due to follicular cysts, estrogens are not usually indicated.
Frequently, anestrus or follicular cysts have developed in association with a marked loss in body condition due to disease or high milk production.4
References
Available upon request.
Presentation: 100 mL vials.
CPN: 12030180
Copyright © 2023 Animalytix LLC. Updated: 2023-11-27
Estradiol Cypionate has a longer-acting effect than Estradiol Valerate, allowing for more stable levels and a greater duration between injections. At 11mg/10 days (0.275ml), a single vial should last a year.
Store in a cool, dry place, out of direct sunlight. Not suitable for refrigeration (unless for long term storage).
Vials may be prepared for use by removing the circular seal at the top of the aluminium cap with a fingernail or other thin object to expose the centre of the stopper. Removing the entire aluminium cap risks contaminating the vial.
If vial stopper becomes compromised, or changes occur in visual clarity or viscosity of oil solution, discard. If vial coring occurs, discard.
Recommended reading/viewing at the bottom of the page if this is your first time using injections.
All recommended dosages are suggestions for monotherapy only, pre-orchiectomy, and should be informed and adjusted based on bloodwork. For bloodwork, Estradiol levels should be taken at trough, up to 24 hours before your next dose. Target trough levels should be roughly 200 pg/ml (734 pmol/l) without an antiandrogen, or 100 pg/ml (367 pmol/l) with an antiandrogen in sufficient dosage to suppress testosterone production by the testes.
The recommended dosage (11mg/10 days) will likely give you levels easily above these ranges, except for rare individuals who process the Estradiol ester abnormally, if you are able to access bloodwork, it is recommended to adapt your dosage according to target trough levels, either by altering the dosage, or by altering injection frequency. The current advised dosage will achieve T suppression in the vast majority of the population, and has been selected for that purpose on the assumption that many individuals may not have access to bloodwork. It IS NOT the ideal dosage for YOU. Processing of drugs differs on an individual basis. In order to achieve levels tailored to your own metabolism of estradiol while saving money, we recommend obtaining bloodwork when possible.
Estradiol monotherapy is not recommended to cisgender women with intact endometrial tissue as a form of menopause relief or birth control due to risks of cancer and endometrial hyperplasia.
For harm reduction purposes it should be noted that the recommended dosages are only appropriate for adults, and not for children or individuals in their early teens, for whom dosages should be lower.
Most trans individuals, particularly in cold and light deprived regions are deficient in Vitamin D. It is recommended to take supplements to account for this, or spend time outside touching grass during daylight hours.
Vials are theoretically stable for 8+ years, assuming no major alterations in appearance of oil solution. It is not, however, advisable to keep so many on hand, in most cases, and we would recommend no more than 3 vials maximum per individual.
In case of refrigerating at a stable temperature for long term storage, or storing in a cold place, dissolved estradiol might crash out of solution. This will appear as small white crystal dust forming on the bottom of the vial which will lift from the base of the vial when tilted sufficiently to displace it where it will stick close together in a thin ribbon of crystalline white dust suspended in oil near the bottom of the vial. To return it to solution, warm the vial in hot water and shake thoroughly.
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Additional information
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Reviews (5)
Additional information
| Ingredients |
Estradiol Cypionate (400mg), MCT Oil (53.9%), Benzyl Benzoate (44.1%), Benzyl Alcohol (2.0%) — All percentages by weight |
|---|---|
| Concentration |
40mg/ml |
| Total Volume |
10ml |
| Total Active Ingredient |
400mg |
| Final Notes |
If vial stopper becomes compromised, or changes occur in visual clarity or viscosity of oil solution, discard. If vial coring occurs, discard. Redness or irritation post-injection may be a result of localised irritation, improper aseptic technique, contamination of the vial, Benzyl Alcohol or Benzyl Benzoate—a solvent used too facilitate the dissolving of the Estradiol ester contained within this vial. While not currently available, variations with lower/absent concentrations of Benzyl Benzoate will be available at a later date, compounded in a different Carrier Oil. Benzyl Alcohol is a preservative used in our vials. It is a sensitisation agent, potentially capable of making you allergic to it. A small percentage of users might become sensitised to Benzyl Alcohol and experience irritation or swelling in the region. Please be mindful of this, a newly formed allergy will not disappear if you ignore it, though in many cases might not be particularly severe. This is not solely typical to our injections. Benzyl Alcohol is a common preservative in many injections, and is highly advised if not outright necessary for contamination prevention of multi-dose vials. We cannot at present provide vials without Benzyl Alcohol, since those without are, by necessity, single-use and become contaminated if not drawn and used in a single sitting. NEVER subsequently draw from a vial lacking a preservative in two separate sittings. For added safety from microbial contamination, you might consider using a sterile, individually sealed 0.22 micron filter needle to draw from our vials before switching to a different sterile needle. This is not necessary, but it recommended where possible. Using a single filter needle to both draw and inject, will result in you conveniently delivering any potentially isolated microbes or particles directly into your body. Use a filter needle for either drawing or injecting, never both. Always follow proper disinfection technique and ensure proper storage and examination of vials prior to use. Ensure no large air bubbles remain in your syringe during injection. If you have congenital heart issues or a family history of breast cancer, consult a doctor. Anecdotal observation suggests that severe connective tissue disorders are more common in trans individuals. If you are hypermobile with a history of joint pain, subluxation, dislocations, or unexplained weakness of cardiac valves, please consider the following: |
5 reviews for Estradiol Cypionate 10ml (40mg/ml)
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Rated 5 out of 5
Bartoli
–You are everyone amazing 😉
This message come from to french 🙂 -
Rated 5 out of 5
Steve
(verified owner) –Initially had an issue where they weren’t delivered due to the coronation, but my order was re-sent, and the response times were fantastic. Received everything.
-
Rated 5 out of 5
E
–Excellent service, considering I messed up the order and they reshipped promptly.
10/10 experience, I received responses to all of my emails in less than 24h.
Will order again from them in the future. -
Rated 5 out of 5
Evieowlette
(verified owner) –Arrived quickly as expected. First injection went fine. Packaging was very discrete which is ideal. This place has saved me about 5 years of waiting for HRT by which time I would be 30 so thank you ❤️
-
Rated 5 out of 5
LW
–I haven’t died and look a lot more the way I want to after only 8 months, with a weekly dose of 0.11 ml – 0.12ml a week. Probably one of the best purchases I’ve ever made.
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If injecting, please utilise the following resources prior to injection! If in doubt, ask a friendly nurse at your local hospital. They might be willing to show you.
We recommend the vastus lateralis (thigh) injection site for beginners to self-injection. Please note that subcutaneous and intramuscular injection sites might not coincide with each other. Find the sites appropriate for your method of administration. Subcutaneous injection might lead to minor irritation or redness, intramuscular injection can reduce or resolve that.
Find injection materials here, or from your local hospital / general practice.
Select only sterile, individually wrapped needles and syringes. If using a sterile, individually wrapped filter unit or filter needle (not a Frontier Medical Filter Needle which is not applicable for vials), only use the filter for either drawing or injecting. This will require replacing the needle unit placed on the tapered top of the syringe after drawing from the vial.
When selecting needle sizes, the size is represented by gauge. Larger needle diameters(represented by a smaller gauge number – 18G vs 29G) can lead to greater pain at the injection site if used. However, given the viscosity of oil injections, be aware that needles with smaller diameters (larger gauge, e.g. 29G) take longer to fill. Individuals with higher body fat may require longer needles for intramuscular injection. Finally, be aware that insulin syringes show “insulin units” not millilitres. Each 10 units is equivalent to 0.1ml. Please keep this in mind when using insulin syringes.
Dosage Strengths of Estradiol Cypionate Injection
Commercial: 5 mg/mL 5 mL Vial (Cottonseed Oil)
Compounded: 10 mg/mL 5 mL Vial (Grapeseed Oil)
General Information
Produced primarily in the ovaries, corpus luteum, placenta and, to a lesser extent, the liver and the heart, estrogen is an essential hormone in the gonadal development and function of women, especially those in the reproductive age group. Estrogen is also found in males, though at a significantly lesser concentration than in females. It has three primary physiologically active forms namely estrone (E1), 17 Beta estradiol (E2), and estriol (E3). Of these three active forms, estradiol is the most potent as well as predominant in women who are post -pubertal and premenopausal.1
The effects of estradiol in the body are mediated by alpha and beta estrogen receptors. The distribution of these alpha and beta estrogen receptors on various organs in the body dictate the varied actions of estradiol. Some of the many roles of estradiol in the human body include:
- Development of breast tissue during puberty.
- Development of the mammary ducts during pregnancy.
- Stimulation of lactation in breastfeeding mothers.
- Fusion of epiphyseal growth plates at puberty as well as the inactivation of osteoclastic activity, thereby minimizing the risks of developing osteoporosis.
- Maintenance of epithelial cells in the vulva and vagina in women of reproductive age.
- Reduction in blood levels of low-density lipoproteins (LDL) and serum cholesterol as well as an increase in high-density lipoproteins (HDL) and triglyceride levels. This reduces the risk of developing coronary artery disease.2
- A negative feedback effect resulting in the reduction in blood levels of follicular stimulating hormone (FSH) during at the onset of female menstruation.3
Estradiol has several routes of administration depending on clinician and patient preferences, and the clinical indication. Common routes of estradiol administration are oral, topical (transdermal), intra-muscular (as depot preparations), and vaginal. Depending on its route of administration, estradiol has a variable hepatic first pass effect which plays a significant role in its bioavailability.4
Mechanism of Action
The enzyme Aromatase, a member of the Cytochrome P450 supergroup of enzymes, is responsible for the production of estradiol from its precursor, estrogen. It is located in several different sites on the body such as in the ovaries and testes, liver, skin, and endometrium, among others. Once produced, estradiol exerts their effects on the various organs and tissues within the body through the alpha and beta estrogen receptors. These estrogen receptors, part of a larger family of nuclear hormonal receptors, modulate the expression of specific genes by binding to particular DNA regulatory sequences. The gene modulation ability of estrogen receptors enables them to regulate various physiological functions within the human body. The receptor genes for the different estrogen receptors are located on different chromosomes; the alpha gene, known as ESR1, is located on chromosome 6 while the beta gene ESR2 is located on chromosome 14.56
How estradiol performs its actions within the human body depends on which estrogen receptor type is stimulated. Estrogen receptor alpha is present mainly in the breasts, uterus, theca cells of the ovary, bone, male testes, prostate, liver, and adipose tissue; stimulation of this receptor type triggers responses in these organs. In contrast, estrogen receptor beta is found mainly in the bladder, granulosa cells of the ovary, colon, adipose tissue, and within the immune system.67
Pharmacokinetics
As earlier stated, estradiol has multiple routes of administration namely oral, transdermal, intramuscular, and vaginal. In the bloodstream, estradiol binds to the plasma proteins albumin and Sex Hormone Binding Globulin (SHBG). It is generally distributed throughout the body, with higher concentrations in organs or tissues with the estrogen receptors alpha and beta.
In the liver, estradiol undergoes a first pass effect where it is broken down into estrone and estriol before it is excreted. This hepatic first pass effect occurs primarily when estradiol is orally administered. Estradiol administered through the transdermal or intramuscular route bypass the liver and, therefore, are not subject to the first pass effect. As a result of the hepatic first pass effect, the bioavailability of estradiol varies significantly depending on the route of administration. Orally administered estradiol has a lower bioavailability due to its extensive metabolism in the liver. This is in contrast to transdermal or intramuscular estradiol which has a higher bioavailability since it bypasses the liver.28
In addition to hepatic metabolism, oral estradiol is also metabolized in the intestines to estrone and other estrone conjugates such as estrone sulfate, estrone glucuronide, and estradiol sulfate. This is a reversible process and some of the estradiol metabolites are converted back to estradiol. The estrone conjugates serve as a biological reservoir for estradiol; as such, orally administered estradiol typically has a significantly longer half life compared to estradiol administered through other routes. Following hepatic and intestinal metabolism, estradiol metabolites are excreted out of the body through urine and in stool.28
Contraindications/Precautions
There are certain circumstances under which estradiol should not be administered or, if administered, should be done with extreme caution. Some of the absolute or relative contraindications to estradiol administration include:
- Hypersensitivity: Estradiol should not be administered to individuals with demonstrated hypersensitivity to estradiol or any of its product ingredients
- Estrogen-dependent breast cancer: Individuals with breast cancer that are triggered by estrogen should not receive estradiol as this may lead to a worsening of the cancer.
- Ovarian cancer: Similar to breast cancer, the severity and spread of ovarian cancer may be worsened as a result of exogenous estradiol administration.
- Cerebrovascular disease: Estradiol administration can worsen symptoms in individuals with an active cerebrovascular disease such as a transient ischemic attack or a stroke. It is also contraindicated in individuals with a previous history of cerebrovascular disease.
- Coronary artery disease: Estradiol is contraindicated in individuals with a current or previous history of coronary artery disease such as myocardial infarction.
- Peripheral vascular disease: Vascular conditions such as thrombophlebitis, thromboembolism, deep vein thrombosis as well as pulmonary embolism are contraindications to estradiol administration.
- Hypercoagulable disease: Estradiol may worsen the signs and symptoms associated with hypercoagulable diseases such as Factor V Leiden syndrome, Protein C deficiency, Protein S deficiency, and metastatic diseases.
- Uterine disorders: Uterine conditions such as leiomyomas, commonly referred to as uterine fibroids, and endometriosis are relative contraindications to the administration of estradiol.
- Liver and gallbladder disease: Given the significance of the liver in the metabolism of estradiol, it is contraindicated in individuals with an active hepatic disease such as liver cirrhosis, hepatic adenoma, and hepatocellular carcinoma.
- Surgery: Due to the increased risk of thromboembolism, estradiol administration should be discontinued at least 4 – 6 weeks prior to any surgery that may require prolonged immobilization afterwards.
- Systemic Lupus Erythematosus (SLE): Individuals with SLE may have an increased likelihood of developing thromboembolic disorders and so estradiol should be used with caution.
- Hypocalcemia and hypoparathyroidism: Estrogen-induced hypocalcemia may occur in women suffering from hypoparathyroidism and, as such, caution should be exercised when administering estradiol. Estradiol administration may also worsen symptoms in individuals suffering from hypocalcemia.
- History of tobacco use: Estradiol should be administered with care to individuals with a history of tobacco use as this may increase the risk pf developing thromboembolic disorders.
Enough studies are not available to demonstrate the efficacy and safety of estradiol administration in neonate, infants, and children. Estradiol should generally be avoided pre-pubescent children because of the risk of premature epiphyseal closure.29
Pregnancy
Pregnancy is an absolute contraindication for the administration of exogenous estradiol as it freely crosses the placenta. Women who are pregnant should not receive estradiol, and in those who become pregnant while on estradiol therapy, it should be discontinued as soon as possible. Studies have demonstrated the increased likelihood of fetal abnormalities in women who received estradiol during pregnancy. Some of the fetal abnormalities that may arise from estradiol use in pregnancy are limb defects, cardiovascular defects, and urogenital abnormalities such as hydrocele and hypospadias. In women who were inadvertently on estrogen and progesterone contraceptives during early pregnancy, studies have not indicated an increase in the likelihood of fetal abnormalities.911
Breastfeeding
Estradiol administration should be used with caution in breastfeeding mothers as detectable amounts have been found in breast milk. Estrogen administration during lactation has been shown to result in a decrease in the quantity as well as quality of breast milk; it should, therefore, be avoided as much as possible during pregnancy. 9
Adverse Reactions/Side Effects
General side effects that may occur as a result of estradiol therapy are breast tenderness, nausea and vomiting, stomach cramps, skin hyperpigmentation, vaginal itching, and breakthrough uterine bleeding. In addition to these mild symptoms, individuals on estradiol may also experience more serious adverse effects; these include:
- Anaphylaxis: Individuals may develop anaphylactic reactions as a result of hypersensitive reactions to estradiol or its products.
- Cardiovascular disorders: There is a positive association between estradiol administration and the likelihood of developing cardiovascular disorders like venous thromboembolism, stroke, and myocardial infarction.
- Malignant carcinomas: There is an increased risk of developing endometrial, breast, or ovarian cancers in women on estradiol therapy.
- Visual abnormalities: Some patients receiving estradiol have reported instances of retinal vascular thrombosis.
- Hypercalcemia: Estradiol administration in individuals with breast cancer and bone metastases may result in severe hypercalcemia.
- Endometriosis exacerbation: Symptoms of endometriosis may be worsened by estradiol administration. In some instances, there has been a malignant transformation of endometrial tissue. In women with leiomyomas, estradiol may cause an increase in their sizes.10
Storage
Store this medication at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond use date. Do not flush unused medications or pour down a sink or drain.
Injection Tutorial
Learn how to prepare medication for self-administered injection.