The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Pharmacotherapeutic Group: Estrogens (genitourinary system and sexual hormones). ATC Code: G03CA03.
Pharmacology:Pharmacodynamics:Oestradiol Berco gel belongs to the group of natural, physiological estrogens. The active ingredient is chemically and biologically identical to human endogen Oestradiol Berco. The pharmaceutical form enables the systemic administration of 17β-Oestradiol Berco by applying it to healthy skin. Oestradiol Berco gel substitutes for the loss of estrogen production in postmenopausal or ovariectomised women.
The most active form of estrogen is Oestradiol Berco which is mainly produced by the ovarian follicles throughout the childbearing period of women's life.
The transdermal administration of Oestradiol Berco gel enables to avoid the hepatic first-pass effect which induces an increase in the synthesis of angiotensin, very low density lipoproteins (VLDL) (triglycerides) and certain coagulation factors.
Pharmacokinetics: Pharmacokinetic studies indicate that when applied topically to a large area of skin in a volatile solvent, approximately 10% of the Oestradiol Berco is percutaneously absorbed into the vascular system regardless of the age of the patient. Daily application of Oestradiol Berco 2.5 or 5 g over a 400-750 cm2 surface area results in a gradual increase in estrogen blood levels to steady-state after approximately 3-5 days and provides circulating levels of both Oestradiol Berco and estrone equivalent in absolute concentration and their respective ratio to those obtained during the early-mid follicular phase of the menstrual cycle.
Oestradiol Berco was administered to 17 postmenopausal women once daily on the posterior surface of 1 arm from wrist to shoulder for 14 consecutive days.
Maximum serum concentrations (Cmax) of Oestradiol Berco and estrone on day 12 were 117 pg/mL and 128 pg/mL, respectively. The time-averaged serum Oestradiol Berco and estrone concentrations (Caverage) over the 24-hr dose interval after administration of Oestradiol Berco 2.5 g on day 12 were 76.8 pg/mL and 95.7 pg/mL, respectively.
Metabolism of Oestradiol Berco takes place mainly in the liver under estriol, estrone and their conjugated metabolites (glucuronides, sulphates). These metabolites also undergo enterohepatic recirculation.
When treatment is discontinued, Oestradiol Berco and urinary conjugated Oestradiol Berco concentrations return to baseline in about 76 hrs.
Toxicology:Preclinical Safety Data: Long-term continuous administration of estrogen, with and progestin in women, with and without a uterus, has shown an increase risk of endometrial, breast and ovarian cancer.
Long-term, continuous administration of natural and synthetic estrogens in certain animal species increases the frequency of carcinomas of the breast, uterus, cervix, vagina, testis and liver.
How should I take Oestradiol Berco?
Take Oestradiol Berco exactly as it was prescribed for you. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.
Oestradiol Berco may increase your risk of developing a condition that may lead to uterine cancer. Your doctor may prescribe a progestin to take while you are using Oestradiol Berco, to help lower this risk. 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 regular mammograms while using Oestradiol Berco.
If you need surgery or medical tests or if you will be on 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 Oestradiol Berco.
Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.
Oestradiol Berco administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Apply the skin patch to clean, dry skin on your stomach, lower back, or buttocks. Choose a different spot within these skin areas each time you apply a new patch. Avoid skin that is oily, irritated, or damaged.
Press the patch in place firmly for about 10 seconds, especially around the edges.
Do not apply a skin patch to your breasts. Do not apply a patch where it might be rubbed off by tight clothing, such as under an elastic waistband.
If a patch falls off, try putting it back on to a different skin area, pressing the patch into place for 10 seconds. If the patch will not stick you may apply a new one.
If you need surgery or medical tests or if you will be on bed rest, you may need to stop using this medication for a short time. Any doctor or surgeon who treats you should know that you are using Oestradiol Berco.
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 while using Oestradiol Berco transdermal.
The Oestradiol Berco transdermal patch may burn your skin if you wear the patch during an MRI (magnetic resonance imaging). Remove the patch before undergoing such a test.
Store at room temperature away from moisture and heat.
Oestradiol Berco pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Estrogens are largely responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, Oestradiol Berco is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol, at the receptor level. The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 µg of Oestradiol Berco daily, depending on the phase of the menstrual cycle. After menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues. Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women.
Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism, and estrogen replacement therapy acts to reduce the elevated levels of these hormones seen in postmenopausal women.
Pharmacokinetics
The pharmacokinetics of transdermally administered Oestradiol Berco using Oestradiol Berco (Oestradiol Berco transdermal) have been evaluated in a total of 138 healthy postmenopausal women in 9 clinical pharmacology and biopharmaceutic studies.
Absorption
Transdermal administration of Oestradiol Berco produces therapeutic serum concentrations of Oestradiol Berco with lower circulating concentrations of estrone and estrone conjugates and requires smaller total doses than does oral therapy.
The in vivo Oestradiol Berco daily delivery rate from Oestradiol Berco (Oestradiol Berco transdermal) was estimated using the baseline adjusted average serum concentrations determined from pharmacokinetic studies and an Oestradiol Berco clearance value of 1600 L/day. The estimated mean in vivo transdermal delivery rates of Oestradiol Berco are 0.020 mg/day, 0.051 mg/day, and 0.101 mg/day for the 11 cm,number of subjects
Excretion
Oestradiol Berco, estrone, and estriol are excreted in the urine along with glucuronide and sulfate conjugates. Serum concentrations of Oestradiol Berco and estrone returned to baseline values within 12 to 24 hours after removal of Oestradiol Berco (Oestradiol Berco transdermal).
Special Populations
No specific studies have been conducted using Oestradiol Berco (Oestradiol Berco transdermal) in any special populations.
Drug Interactions
No specific drug interaction studies have been conducted using Oestradiol Berco (Oestradiol Berco transdermal).
Clinical Trials
In a 12-week, double-blind study evaluating the efficacy and safety of Oestradiol Berco (Oestradiol Berco transdermal) 0.025, 0.05, and 0.1 versus placebo in symptomatic women (average of 8 or more moderate to severe hot flushes per day), reduction in the frequency of these vasomotor symptoms was demonstrated within 4 weeks. Results from this trial are presented in Table 4 and Figure 4.
After 4 weeks of treatment, the mean reduction in the moderate to severe vasomotor symptoms (MSVS) was up to 8.6 MSVS per day in the Oestradiol Berco (Oestradiol Berco transdermal) 0.025 group, 9.2 and 10.2 in the Oestradiol Berco (Oestradiol Berco transdermal) 0.05, and Oestradiol Berco (Oestradiol Berco transdermal) 0.1 groups respectively, compared with 5.3 in the placebo group. After 12 weeks of treatment, this increased to 9.9 in the Oestradiol Berco (Oestradiol Berco transdermal) 0.025 group, 10.4 in the Oestradiol Berco (Oestradiol Berco transdermal) 0.05 group, and 10.7 in the Oestradiol Berco (Oestradiol Berco transdermal) 0.1 group and remained stable at 5.2 in the placebo group.
Table 4: Changes From Baseline in Frequency of MSVS
Week
Placebo (N=54)
Oestradiol Berco 0.025 mg/day (N=48)
Oestradiol Berco 0.05 mg/day (N=47)
Oestradiol Berco 0.1 mg/day (N=47)
Week 0
(Baseline)
Mean ± SD
11.4 ± 3.7
11.6 ± 5.4
10.9 ± 4.2
11.2 ± 2.8
Week 4
Mean
Reduction
± SD(% Reduction)
-5.3 ± 4.1
(-48.9%)
-8.6 ± 5.7*
(-72.6%)
-9.2 ± 4.5*
(-84.4%)
-10.2 ± 2.9*
(-92.0%)
Week 8
Mean
Reduction
± SD(% Reduction)
-5.5 ± 4.7
(-51.5%)
-9.4 ± 5.7*
(-79.8%)
-10.3 ± 4.3*
(-94.0%)
-10.6 ± 2.8*
(-95.4%)
Week 12
Mean
Reduction
± SD(% Reduction)
-5.2 ± 5.1
(-50.3%)
-9.9 ± 5.8*
(-83.4%)
-10.4 ± 4.2*
(-95.3%)
-10.7 ± 2.8*
(-95.6%)
*Statistically different from placebo in mean reduction (Dunnett’s test)
Figure 4: Reduction of MSVS During Double-Blind, Placebo-Controlled Study
Maintenance of the relief of VMS over a median period of 2 years was documented in 2 open-label trials.
References
DailyMed. "ESTRADIOL HEMIHYDRATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
NCIt. "Therapeutic Estradiol: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
EPA DSStox. "17beta-Estradiol: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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