Gynodian Depot Actions

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Consists of Estradiol, Prasterone

Actions of Estradiol (Gynodian Depot) in details

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: Estradiol (Gynodian Depot) gel belongs to the group of natural, physiological estrogens. The active ingredient is chemically and biologically identical to human endogen Estradiol (Gynodian Depot). The pharmaceutical form enables the systemic administration of 17β-Estradiol (Gynodian Depot) by applying it to healthy skin. Estradiol (Gynodian Depot) gel substitutes for the loss of estrogen production in postmenopausal or ovariectomised women.

The most active form of estrogen is Estradiol (Gynodian Depot) which is mainly produced by the ovarian follicles throughout the childbearing period of women's life.

The transdermal administration of Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) is percutaneously absorbed into the vascular system regardless of the age of the patient. Daily application of Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) and estrone equivalent in absolute concentration and their respective ratio to those obtained during the early-mid follicular phase of the menstrual cycle.

Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) and estrone on day 12 were 117 pg/mL and 128 pg/mL, respectively. The time-averaged serum Estradiol (Gynodian Depot) and estrone concentrations (Caverage) over the 24-hr dose interval after administration of Estradiol (Gynodian Depot) 2.5 g on day 12 were 76.8 pg/mL and 95.7 pg/mL, respectively.

Metabolism of Estradiol (Gynodian Depot) 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, Estradiol (Gynodian Depot) and urinary conjugated Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot)?

It is very important that you use Estradiol (Gynodian Depot) exactly as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects.

Estradiol (Gynodian Depot) is to be used only in the vagina. Use at bedtime unless your doctor tells you otherwise.

Estradiol (Gynodian Depot) comes with a patient information leaflet. Read and follow the instructions carefully. Ask your doctor if you have any questions.

To use the vaginal ring:

To use the vaginal tablet:

Do not eat grapefruit or drink grapefruit juice while you are using Estradiol (Gynodian Depot). Grapefruit and grapefruit juice may change the amount of Estradiol (Gynodian Depot) that is absorbed in the body.

Dosing

The dose of Estradiol (Gynodian Depot) will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Estradiol (Gynodian Depot). If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Missed Dose

If you miss a dose of Estradiol (Gynodian Depot), take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Wrap the used vaginal ring in tissue and throw it in the trash can. Do not flush the vaginal ring down the toilet.

Estradiol (Gynodian Depot) 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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Consider the use of a progestin when administering estrogens to postmenopausal women with a uterus.

Injection formulation: IM use only.

Estradiol (Gynodian Depot) cypionate: Shake or gently warm vial to redissolve crystals that may have formed during storage.

Estradiol (Gynodian Depot) valerate: Inject into the upper outer quadrant of the gluteal muscle; administer with a dry needle (solution may become cloudy with wet needle).

Gel: Apply to clean, dry, unbroken skin at the same time each day. Wash hands after application. Gel is flammable; avoid fire or flame until skin is dry.

Divigel: Apply the entire contents of packet to right or left upper thigh each day (alternate sites) over a ~5 x 7-inch area. Do not apply to face, breasts, vaginal area, or irritated skin. Do not wash application site for 1 hour. Allow gel to dry before dressing.

Elestrin: Apply the entire dose to upper arm and shoulder area using 2 fingers to spread gel. Do not apply to breasts or vaginal area. Allow skin to dry for ≥5 minutes prior to dressing. Prior to first use, pump must be primed. After priming, the pump contains 30 metered doses; discard pump after 30 doses even though container may not be empty. If >1 dose is needed, wait 5 seconds before pumping next dose. To avoid secondary exposure, do not allow others to contact the application site for 2 hours after gel is applied. Allow at least 2 hours between applying gel and going swimming. Wait at least 25 minutes before applying sunscreen to application area. When sunscreen and gel are applied to the same site for >7 consecutive days, the absorption of Estradiol (Gynodian Depot) is increased; do not apply sunscreen to an area where the gel was applied for ≥7 consecutive days.

EstroGel: Apply dose into the palm of hand and then apply gel to the other arm, from the wrist to the shoulder. Do not apply to breasts or vaginal area. Spread gel as thinly as possible over one arm but do not massage or rub in gel. Allow skin to dry for 5 minutes before dressing. Prior to first use, pump must be primed. After priming, the pump contains 32 daily doses (50 g canister) or 14 daily doses (25 g canister). Discard pump after allotted doses even though container may not be empty. To avoid secondary exposure, do not allow others to contact the application site for ≥1 hour after gel is applied. Wait as long as possible between applying gel and going swimming. When sunscreen was applied 1 hour after the gel to the same site for >7 consecutive days, the absorption of Estradiol (Gynodian Depot) was decreased; when moisturizing lotion was applied 1 hour after the gel to the same site for >7 consecutive days, the absorption of Estradiol (Gynodian Depot) was increased. The effect of applying sunscreen or lotion prior to the gel has not been studied.

Spray: Evamist: Prior to first use, prime pump by spraying 3 sprays with the cover on. To administer dose, hold container upright and vertical and rest the plastic cone flat against the skin while spraying. Spray to the inner surface of the forearm, starting near the elbow. If more than one spray is needed, apply to adjacent but not overlapping areas. Apply at the same time each day. Allow spray to dry for ~2 minutes; do not rub into skin; do not cover with clothing until dry. Do not wash application site for at least 60 minutes. Apply to clean, dry, unbroken skin. Do not apply to skin other than that of the forearm. Make sure that children do not come in contact with any skin area where the drug was applied. If contact with children is unavoidable, wear a garment with long sleeves that covers the site of application. If direct exposure occurs, wash the child in the area of exposure with soap and water as soon as possible. Solution contained in the spray is flammable; avoid fire, flame, or smoking until spray has dried. If needed, apply sunscreen ~1 hour prior to application of Evamist.

Transdermal patch: General administration instructions (also refer to product labeling): Apply patch immediately after removing from protective pouch to lower abdomen or buttocks. Apply to clean, dry, healthy skin that is free of oil, powder, or lotion. Avoid waistline or other areas where tight clothing may rub the patch off; do not apply to breasts. After application, hold patch in place using palm of hand for 10 seconds. Rotate application sites allowing a 1-week interval between applications at a particular site. In general, if patch falls off, the same patch may be reapplied or a new system may be used for the remainder of the dosing interval. When replacing patch, reapply to a new site. Remove patch slowly after use to avoid skin irritation. If any adhesive remains on the skin after removal, first allow skin to dry for 15 minutes, then gently rub area with an oil-based cream or lotion. Dispose of any used or unused patches by folding adhesive ends together, replace in pouch or sealed container, and discard properly in trash away from children and pets.

Climara, Menostar: Swimming, bathing, or wearing patch while in a sauna have not been studied

Vaginal ring: Exact positioning is not critical for efficacy; however, patient should not feel anything once inserted. In case of discomfort, push ring further into vagina. If ring is expelled prior to 90 days, it may be rinsed off with warm water and reinserted. Ensure proper vaginal placement of the ring to avoid inadvertent urinary bladder insertion. Femring may remain in place during local treatment of a vaginal infection.

Estradiol (Gynodian Depot) 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, Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) using Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) have been evaluated in a total of 138 healthy postmenopausal women in 9 clinical pharmacology and biopharmaceutic studies.

Absorption

Transdermal administration of Estradiol (Gynodian Depot) produces therapeutic serum concentrations of Estradiol (Gynodian Depot) with lower circulating concentrations of estrone and estrone conjugates and requires smaller total doses than does oral therapy.

The in vivo Estradiol (Gynodian Depot) daily delivery rate from Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) was estimated using the baseline adjusted average serum concentrations determined from pharmacokinetic studies and an Estradiol (Gynodian Depot) clearance value of 1600 L/day. The estimated mean in vivo transdermal delivery rates of Estradiol (Gynodian Depot) are 0.020 mg/day, 0.051 mg/day, and 0.101 mg/day for the 11 cm,number of subjects

Excretion

Estradiol (Gynodian Depot), estrone, and estriol are excreted in the urine along with glucuronide and sulfate conjugates. Serum concentrations of Estradiol (Gynodian Depot) and estrone returned to baseline values within 12 to 24 hours after removal of Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal).

Special Populations

No specific studies have been conducted using Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) in any special populations.

Drug Interactions

No specific drug interaction studies have been conducted using Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal).

Clinical Trials

In a 12-week, double-blind study evaluating the efficacy and safety of Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) 0.025 group, 9.2 and 10.2 in the Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) 0.05, and Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) 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 Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) 0.025 group, 10.4 in the Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) transdermal) 0.05 group, and 10.7 in the Estradiol (Gynodian Depot) (Estradiol (Gynodian Depot) 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)

Estradiol (Gynodian Depot) 0.025 mg/day (N=48)

Estradiol (Gynodian Depot) 0.05 mg/day (N=47)

Estradiol (Gynodian Depot) 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.

Actions of Prasterone (Gynodian Depot) in details

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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Prasterone (Gynodian Depot) is an inactive endogenous steroid and is converted into active androgens and/or estrogens. The mechanism of action of Prasterone (Gynodian Depot) in postmenopausal women with vulvar and vaginal atrophy is not fully established.

How should I take Prasterone (Gynodian Depot)?

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.

It is very important that you use Prasterone (Gynodian Depot) exactly as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects.

Prasterone (Gynodian Depot) comes with a patient information leaflet. Read and follow the instructions in the leaflet carefully. Ask your doctor if you have any questions.

Prasterone (Gynodian Depot) comes with a disposable applicator. Place the vaginal insert in the applicator and then insert it into your vagina. Use each applicator only once, and then throw it away.

Dosing

The dose of Prasterone (Gynodian Depot) will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Prasterone (Gynodian Depot). If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Missed Dose

If you miss a dose of Prasterone (Gynodian Depot), take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

You may also store the medicine in the refrigerator.

Prasterone (Gynodian Depot) 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.

Mechanism of Action

Prasterone (Gynodian Depot) is an inactive endogenous steroid and is converted into active androgens and/or estrogens. The mechanism of action of Prasterone (Gynodian Depot) in postmenopausal women with vulvar and vaginal atrophy is not fully established.

Pharmacokinetics

In a study conducted in postmenopausal women, administration of the Prasterone (Gynodian Depot) vaginal insert once daily for 7 days resulted in a mean Prasterone (Gynodian Depot) C max and area under the curve from 0 to 24 hours (AUC 0-24) at Day 7 of 4.4 ng/mL and 56.2 ng·h/mL, respectively, which were significantly higher than those in the group treated with placebo (Table 1). The C max and AUC 0-24 of the metabolites testosterone and Prasterone (Gynodian Depot) were also slightly higher in women treated with the Prasterone (Gynodian Depot) vaginal insert compared to those receiving placebo.

Table 1. Cmax and AUC0-24 of Prasterone (Gynodian Depot), Testosterone, and Prasterone (Gynodian Depot) on Day 7 Following Daily Administration of Placebo or Prasterone (Gynodian Depot) (mean ± SD).
1: N=8
Placebo (N=9) Prasterone (Gynodian Depot) (N=10)
Prasterone (Gynodian Depot) C max (ng/mL) 1.60 (±0.95) 4.42 (±1.49)
AUC 0-24 (ng·h/mL) 24.82 (±14.31) 56.17 (±28.27)
Testosterone C max (ng/mL) 0.12 (±0.04) 1 0.15 (±0.05)
AUC 0-24 (ng·h/mL) 2.58 (±0.94) 1 2.79 (±0.94)
Prasterone (Gynodian Depot) C max (pg/mL) 3.33 (±1.31) 5.04 (±2.68)
AUC 0-24 (pg·h/mL) 66.49 (±20.70) 96.93 (±52.06)

Figure 1. Serum Concentrations of Prasterone (Gynodian Depot) (A), Testosterone (B), and Prasterone (Gynodian Depot) (C) Measured Over a 24h Period on Day 7 Following Daily Administration of Placebo or Prasterone (Gynodian Depot) (mean ± SD).

In two primary efficacy trials, daily administration of Prasterone (Gynodian Depot) vaginal insert for 12 weeks increased mean serum C trough of Prasterone (Gynodian Depot) and its metabolites testosterone and Prasterone (Gynodian Depot) by 47%, 21% and 19% from baseline, respectively. This comparison based on C trough may underestimate the magnitude of increase in Prasterone (Gynodian Depot) and metabolites’ exposure because it does not take into account the overall concentration-time profile following administration of Prasterone (Gynodian Depot).

Metabolism

Exogenous Prasterone (Gynodian Depot) is metabolized in the same manner as endogenous Prasterone (Gynodian Depot). Human steroidogenic enzymes such as hydroxysteroid dehydrogenases, 5α-reductases and aromatases transform Prasterone (Gynodian Depot) into androgens and estrogens.



References

  1. 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).
  2. 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).
  3. 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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