Comprehensive summary-the advantages, disadvantages and indications of different preparations of estradiol

1. What is estradiol?

Estradiol (E2) is an essential hormone for women and one of the main sex hormones in women. It is of great significance in maintaining women's reproductive and physiological needs. In addition to acting on the reproductive system, it also acts on other target organs, including bones, central nervous system, skin and its appendages, etc. It is mainly secreted by the follicles of the ovaries, and a small amount is produced by the adrenal glands.

A sudden drop or rise in estrogen levels in the body can cause a series of endocrine disorders. Excessive secretion of E2 will lead to precocious puberty, gynecomastia, fibroadenoma, etc. If secretion of E2 is too little, it will lead to primary and secondary amenorrhea, menopause, and unstable menstrual periods, which will affect the development and function of these target organs. Appropriate natural estrogen preparations should be used for supplementary treatment for appropriate groups under the guidance of a doctor. The following content summarizes the advantages, disadvantages, and indications of different preparation types to facilitate clinical selection and use!

2. What types of estradiol preparations are there?

There are currently 5 main types of estradiol preparations on the market, mainly the following 5 types:

①Oral preparation estradiol valerate;

②Transdermal delivery preparation: semihydrated estradiol patch/estradiol gel;

③Estradiol vaginal tablets for vaginal administration;

④Injection preparation estradiol benzoate;

⑤ Nasal mucosal preparation: estradiol hemihydroxide nasal solution.

Semi-hydrated estradiol patch (Songqi) and estradiol gel transdermal administration are estradiol absorbed through the skin. After entering the human body, it is decomposed into estradiol and water, which can effectively supplement E2.

① Advantages: Among various estrogen preparations, the estrogen absorbed through the skin is closer to the secretion mode of estrogen in the natural state. It avoids the first-pass effect of the liver and directly enters the systemic circulation without being destroyed. It has high bioavailability, so it can reduce the total dose taken by the patient and has little impact on hepatobiliary function. It is currently recognized as an estrogen supplement with good safety and few side effects.

②Indications: It is effective in relieving symptoms related to menopause and perimenopause and preventing postmenopausal osteoporosis. It can be used for patients with hepatobiliary dysfunction and high risk factors for thrombosis who are not suitable for oral estrogen.

③ Precautions: The absorption rate of estradiol through skin absorption is low, and administration over a large area may cause irritation and allergy to the skin, so skin reactions need to be closely monitored during use.

(2) Estradiol benzoate injection

Estradiol benzoate injection is a newly added injectable estrogen in the new guidelines. The specifications are 1 mg: 1 ml or 5 mg: 1 ml, intramuscular injection, 1 to 2 mg each time, 2 to 3 times a week.

① Advantages: Compared with other estradiol preparations, injections are absorbed quickly, have rapid efficacy and accurate dosage.

②Indications: It can be used to supplement estrogen deficiency, such as atrophic vaginitis, oophorectomy, advanced prostate cancer (disabled for patients with breast cancer and ovarian cancer), etc. It can be used in combination with progesterone drugs to inhibit ovulation.

③Precautions: However, regular gynecological examinations are required during medication. Use with caution in patients with uterine fibroids, heart disease, epilepsy, diabetes and high blood pressure. In addition, it should be shaken thoroughly before injection, or heated and shaken. It is forbidden for pregnant women and breastfeeding women. It should not be used by children as it may cause premature puberty.

(3) Estradiol valerate

Estradiol valerate is a drug that can be taken orally. Since everyone's constitution is different, the dosage needs to be adjusted according to the individual.

① Advantages: It can be used together with progesterone to establish an artificial menstrual cycle.

②Indications: It is used to treat patients with estrogen deficiency related to natural menopause or artificial menopause, as well as hot flashes, genitourinary tract nutritional diseases, mental diseases, etc. related to menopause.

③ Precautions: However, pregnant or lactating women cannot use estradiol valerate, and there are certain risks in taking the drug. If the patient develops migraine or severe headache after taking the drug for the first time, or has signs of cerebral vascular obstruction, the drug needs to be stopped immediately. In addition, if you have symptoms of blood clots, you should stop taking it.

(4) Estradiol hemihydroxide nasal solution

Estradiol hemihydroxide nasal solution (trade name Aerodiol), specifications: 150 g/spray, 60 sprays/bottle.

① Advantages: Compared with oral administration, drugs administered through the nasal cavity go directly to the site of action without passing through the gastrointestinal tract, thus avoiding drug degradation in gastrointestinal fluid and the first-pass effect of the liver. A very small amount of drug can reach a higher blood concentration.

②Indications: Nasal administration of estradiol provides another option for postmenopausal hormone replacement therapy. The efficacy of nasal administration of estradiol 300 μg/day in relieving postmenopausal symptoms and reducing the incidence of flushing is similar to that of estradiol sustained-release tablets 2 mg/day.

③ Precautions: However, due to the complex internal physiological structure of the nasal cavity, drug absorption varies greatly between individuals. As the nasal cavity is an important sensory organ, adverse reactions such as tingling or itching, sneezing, rhinorrhea and epistaxis may occur at the site of medication.

(5) Estradiol vaginal tablets

Estradiol vaginal tablets include proestradiol cream, prasterone vaginal suppository, chloroquinadol-proestren vaginal tablets, etc.

① Advantages: Estradiol is administered vaginally at a precise site of action, directly reaches the hospital, and has mild systemic adverse reactions.

②Indications: Suitable for symptoms such as vaginal dryness, itching, dyspareunia, recurrent atrophic vaginitis, recurrent lower urinary tract infections, frequent urination, urgency and nocturia.

③ Precautions: The reported adverse reactions of estradiol vaginal tablets are relatively mild. Mild vaginal bleeding and vaginal discharge may occur. Some patients may experience skin allergies, manifested as rashes.

Understand the advantages, indications, and medication precautions of the above different preparations of estradiol. You may have doubts about the use of estradiol vaginal tablets. The author below will introduce how to use vaginal tablets!

Attached: Detailed illustration of how to use estradiol vaginal tablets

First wash your hands, then hold the estradiol vaginal tablet with your fingers (disposable sterile gloves can be worn), use the drug delivery device in a squatting position, and insert the product deep into the vagina. Starting dose: one tablet daily for two weeks; maintenance dose: one tablet twice a week.

(1) Tear open the bubble wrap of the vaginal tablet and open it from the bottom as shown in the picture;

(2) Slowly insert the drug delivery device into the vagina until resistance is felt;

(3) Press the push button lightly to send out the tablets, and there should be a bouncing feeling in your hand;

At this time, the tablet can be immediately firmly attached to the vaginal wall and will not fall off when standing or walking.

(4) Take out and discard the medicine delivery device to complete the operation.

3. Summary

Since there are many types of estradiol dosage forms, for patients who need to use estrogen, under the premise of determining the purpose of treatment, different estrogen preparations should be selected based on the patient's age, whether they want to be pregnant, whether they are postmenopausal, and the length of time they need to treat. In addition, in order to reduce the impact on the development and maturation of the patient's hypothalamic-pituitary-ovarian axis, it is generally recommended that patients choose low-dose, natural estrogen to induce the maturation of the hypothalamic-pituitary-ovarian axis.