Metrigen Fuerte Actions

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Actions of Metrigen Fuerte 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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Endogenous 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 (Metrigen Fuerte) 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 mcg of Estradiol (Metrigen Fuerte) 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 in the peripheral tissues. Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women.

Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. To date, two estrogen receptors have been identified. These vary in proportion from tissue to tissue.

Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH), and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.

Endogenous Progesterone (Metrigen Fuerte) is secreted by the ovary, placenta, and adrenal gland. In the presence of adequate estrogen, Progesterone (Metrigen Fuerte) transforms a proliferative endometrium into a secretory endometrium.

Progesterone (Metrigen Fuerte) enhances cellular differentiation and generally opposes the actions of estrogens by decreasing estrogen receptor levels, increasing local metabolism of estrogens to less active metabolites, or inducing gene products that blunt cellular responses to estrogen. Progesterone (Metrigen Fuerte) exerts its effects in target cells by binding to specific Progesterone (Metrigen Fuerte) receptors that interact with Progesterone (Metrigen Fuerte) response elements in target genes. Progesterone (Metrigen Fuerte) receptors have been identified in the female reproductive tract, breast, pituitary, hypothalamus, and central nervous system.

How should I take Metrigen Fuerte?

Take Metrigen Fuerte (Metrigen Fuerte) only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

Metrigen Fuerte (Metrigen Fuerte) should come with a patient information leaflet. Read and follow these instructions carefully. Ask your doctor if you have any questions.

Take Metrigen Fuerte (Metrigen Fuerte) with food.

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

Dosing

The dose of Metrigen Fuerte (Metrigen Fuerte) 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 Metrigen Fuerte (Metrigen Fuerte). 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.

  • For oral dosage form (capsules):
    • For moderate to severe hot flashes:
      • Adults—One capsule once a day, in the evening. Each capsule contains 1 milligram (mg) Estradiol (Metrigen Fuerte) and 100 mg Progesterone (Metrigen Fuerte).
      • Children—Use is not recommended.

Missed dose

If you miss a dose of Metrigen Fuerte (Metrigen Fuerte), 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.

If you miss a dose and it is more than 2 hours until your next dose, take the missed dose as soon as possible with food, then go back to your regular time.

If you miss a dose and it is within 2 hours of your next evening dose, skip the missed dose and go back to your regular dosing schedule.

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.

Metrigen Fuerte 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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Oral: Administer in the evening with food. In case of missed dose, administer with food as soon as possible, unless it is ≤2 hours until the next dose.

Metrigen Fuerte 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

Endogenous 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 (Metrigen Fuerte) 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 mcg of Estradiol (Metrigen Fuerte) 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 in the peripheral tissues. Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women.

Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. To date, two estrogen receptors have been identified. These vary in proportion from tissue to tissue.

Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH), and FSH, through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.

Endogenous Progesterone (Metrigen Fuerte) is secreted by the ovary, placenta, and adrenal gland. In the presence of adequate estrogen, Progesterone (Metrigen Fuerte) transforms a proliferative endometrium into a secretory endometrium.

Progesterone (Metrigen Fuerte) enhances cellular differentiation and generally opposes the actions of estrogens by decreasing estrogen receptor levels, increasing local metabolism of estrogens to less active metabolites, or inducing gene products that blunt cellular responses to estrogen. Progesterone (Metrigen Fuerte) exerts its effects in target cells by binding to specific Progesterone (Metrigen Fuerte) receptors that interact with Progesterone (Metrigen Fuerte) response elements in target genes. Progesterone (Metrigen Fuerte) receptors have been identified in the female reproductive tract, breast, pituitary, hypothalamus, and central nervous system.

Pharmacodynamics

No specific pharmacodynamic studies were conducted with Metrigen Fuerte (Metrigen Fuerte (Metrigen Fuerte)) capsules, 1 mg/100 mg.

Pharmacokinetics

Absorption

The oral absorption of both Metrigen Fuerte (Metrigen Fuerte) is subject to first pass metabolism. After multiple doses of Metrigen Fuerte (Metrigen Fuerte (Metrigen Fuerte)) capsules, 1 mg/100 mg, the tmax (the time at which the maximum concentration is attained) for Estradiol (Metrigen Fuerte) is approximately 5 hours and approximately 3 hours for Progesterone (Metrigen Fuerte) (Figure 1, Figure 2, and Table 2, below). Steady state for both Metrigen Fuerte (Metrigen Fuerte) components of Metrigen Fuerte, as well as Estradiol (Metrigen Fuerte)'s main metabolite, estrone, is achieved within seven days.

Figure 1: Mean Steady-State Serum Estradiol (Metrigen Fuerte) Concentrations Following Daily

Oral Administration of 1 mg Estradiol (Metrigen Fuerte)/100 mg Progesterone (Metrigen Fuerte) (Baseline Unadjusted, at Day 7)

Figure 2: Mean Steady-State Serum Progesterone (Metrigen Fuerte) Concentrations Following Daily

Oral Administration of 1 mg Estradiol (Metrigen Fuerte)/100 mg Progesterone (Metrigen Fuerte) (Baseline Unadjusted, at Day 7)

Table 2: Mean (SD) Steady-State Pharmacokinetic Parameters after Administration of Capsules Containing 1 mg Estradiol (Metrigen Fuerte)/100 mg Progesterone (Metrigen Fuerte) in Healthy Postmenopausal Women (Baseline Unadjusted, at Day 7)
Dosage Strength (Metrigen Fuerte) Metrigen Fuerte

1 mg/100 mg

Mean (SD)

*Effective t½. Calculated as 24•ln(2)/ ln(accumulation ratio/(accumulation ratio-1)) for subjects with accumulation ratio >1.

Abbreviations: AUC0-τ = area under the concentration vs time curve within the dosing interval at steady-state, Cavg = average concentration at steady-state, Cmax = maximum concentration, SD = standard deviation, tmax = time to maximum concentration, t½ = half-life

Estradiol (Metrigen Fuerte) N
AUC0-τ (pg·h/mL) 20 772.4 (384.1)
Cmax (pg/mL) 20 42.27 (18.60)
Cavg (pg/mL) 19 33.99 (14.53)
tmax (h) 19 4.93(4.97)
t½ (h)* 19 26.47 (14.61)
Estrone
AUC0-τ (pg·h/mL) 20 4594 (2138)
Cmax (pg/mL) 20 238.5 (100.4)
Cavg (pg/mL) 20 192.1 (89.43)
tmax (h) 20 5.45 (3.47)
t½ (h)* 19 22.37 (7.64)
Progesterone (Metrigen Fuerte)
AUC0-τ (ng·h/mL) 20 18.05 (15.58)
Cmax (ng/mL) 20 11.31 (23.10)
Cavg (ng/mL) 20 0.76 (0.65)
tmax (h) 20 2.64 (1.51)
t½ (h) 18 9.98 (2.57)

Food Effect

Concomitant food ingestion increased the AUC and Cmax of the Progesterone (Metrigen Fuerte) component of Metrigen Fuerte relative to a fasting state when administered at a dose of 100 mg. In a study where Metrigen Fuerte was administered to postmenopausal women at a dose of 1 mg Estradiol (Metrigen Fuerte)/100 mg Progesterone (Metrigen Fuerte) within 30 minutes of starting a high-fat meal, the Cmax and AUC of Progesterone (Metrigen Fuerte) were 162% and 79% higher, respectively, relative to the fasting state. Concomitant food ingestion had no effect on the AUC of the Estradiol (Metrigen Fuerte) component of Metrigen Fuerte but decreased Cmax by approximately 54% and delayed Tmax to 12 hours.

Distribution

Estradiol (Metrigen Fuerte)

The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Estrogens circulating in the blood largely are bound to SHBG and albumin.

Progesterone (Metrigen Fuerte)

Progesterone (Metrigen Fuerte) is approximately 96% to 99% bound to serum proteins, primarily to serum albumin (50% to 54%) and transcortin (43% to 48%).

Elimination

Following repeat dosing with Metrigen Fuerte (Metrigen Fuerte (Metrigen Fuerte)) capsules, 1 mg/100 mg, the half-life of Estradiol (Metrigen Fuerte) was approximately 26 hours. The half-life of Progesterone (Metrigen Fuerte), following repeat dosing was approximately 10 hours.

Metabolism

Estradiol (Metrigen Fuerte)

Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol (Metrigen Fuerte) is converted reversibly to estrone, and both can be converted to estriol, the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant portion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens.

Progesterone (Metrigen Fuerte)

Progesterone (Metrigen Fuerte) is metabolized primarily by the liver largely to pregnanediols and pregnanolones. Pregnanediols and pregnanolones are conjugated in the liver to glucuronide and sulfate metabolites. Progesterone (Metrigen Fuerte) metabolites, which are excreted in the bile, may be deconjugated and may be further metabolized in the intestine via reduction, dehydroxylation, and epimerization.

Excretion

Estradiol (Metrigen Fuerte)

Estradiol (Metrigen Fuerte), estrone, and estriol are excreted in the urine along with glucuronide and sulfate conjugates.

Progesterone (Metrigen Fuerte)

The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the bile and urine. Progesterone (Metrigen Fuerte) metabolites are eliminated mainly by the kidneys. Progesterone (Metrigen Fuerte) metabolites which are excreted in the bile may undergo enterohepatic recycling or may be excreted in the feces.


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References

  1. DailyMed. "PROGESTERONE: 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. 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).
  3. NCIt. "Therapeutic Progesterone: 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).

Reviews

The results of a survey conducted on ndrugs.com for Metrigen Fuerte are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Metrigen Fuerte. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

User reports

1 consumer reported administration

When best can I take Metrigen Fuerte, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Metrigen Fuerte should be taken Empty stomach. In any case, this may not be the right description on how you ought to take this Metrigen Fuerte. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Metrigen Fuerte can be taken.
Users%
Empty stomach1
100.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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