Elashine Actions

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Actions of Elashine 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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Progesterone/sex hormone.

Pharmacology: Pharmacodynamics: Mechanism of Action: Elashine acetate (17α-hydroxy-6α-methylprogesterone acetate) is a derivative of progesterone. Elashine acetate is a synthetic progestinic (structurally related to the endogenous hormone progesterone) which has been demonstrated to possess several pharmacologic actions on the endocrine system: Inhibition of pituitary gonadotropins (FSH and LH); decrease circulating ACTH and hydrocortisone blood levels; decrease circulating testosterone; decrease circulating estrogen level (as a result of both FSH inhibition and enzymatic induction of hepatic reductase, resulting in increased clearance of testosterone and consequent decreased conversion of androgens to estrogens).

All of these actions result in a number of pharmacological effects as described as follows.

Gynecology: Elashine acetate, administered orally or parenterally in the recommended doses to women with adequate endogenous estrogen, transforms proliferative into secretory endometrium. Androgenic and anabolic effects have been noted, but the drug is apparently devoid of significant estrogenic activity. While parenterally administered Elashine acetate inhibits gonadotropin production, which in turn prevents follicular maturation and ovulation, available data indicate that this does not occur when the usually recommended oral dosage is given as single daily doses.

Oncology: MPA demonstrates antitumor activity. When MPA is given to patients at high doses (either by the oral route or by IM injection) it is effective in the palliative treatment of hormone-response, malignant neoplasms.

Clinical Studies: Bone Mineral Density Studies: Women’s Health Initiative (WHI) Study: The WHI CEE (0.625mg)/Elashine acetate (2.5 mg) trial enrolled 16,608 postmenopausal women aged 50-79 years with intact uteri at baseline, to assess the risks and benefits of the combined therapy compared with placebo in the prevention of certain chronic diseases. The primary endpoint was the incidence of coronary heart disease (CHD) (nonfatal myocardial infarction and CHD death), with invasive breast cancer as the primary adverse outcome studied. The study was stopped early after an average follow-up of 5.2 years (planned duration 8.5 years) because, according to the predefined stopping rule, the increased risk of breast cancer and cardiovascular events exceeded the specified benefits included in the "global index".

The combination conjugated equine estrogens/ Elashine acetate therapy reported a significant decrease in osteoporotic (23%) and total (24%) fractures.

Million Women Study (MWS): The MWS 37 was a prospective cohort study enrolling 1,084,110 women in the UK aged 50-64 years of whom 828,923 with defined time since menopause were included in the main analyses of risk of breast cancer in relation to HT. Overall, 50% of the study population had used HT at some point. Most current users of HT at baseline reported using preparations containing estrogen only (41%) or estrogen-progestin combinations (50%). The average duration of follow-up was 2.6 years for analyses of cancer incidence and 4.1 years for analyses of mortality

Heart and Estrogen/Progestin Replacement Studies (HERS): HERS and HERS II studies were 2 randomized, prospective secondary prevention trials on the long-term effects of oral continuous combined CEE/MPA (0.625 mg CEE plus 2.5 mg MPA) regimen in postmenopausal women with CHD 2,763 postmenopausal women with a mean age of 66.7 years and with intact uteri were enrolled in this study.

The average duration of follow-up was 4.1 years for HERS and 2.7 additional years (for a total of 6.8 years) for HERS II.

Women’s Health Initiative Memory Study (WHIMS): The WHIMS, a substudy of WHI, enrolled 4,532 predominantly healthy postmenopausal women age 65-79 years to evaluate the effects of CEE/MPA (0.625 mg CEE plus 2.5 mg MPA) or CEE-alone (0.625 mg) on the incidence of probable dementia compared with placebo. The average duration of follow-up was 4.05 years for the CEE/MPA.

Pharmacokinetics:

Oral Formulations: Absorption:

Oral MPA is rapidly absorbed with maximum concentration obtained between 2-4 hrs. The half-life of oral MPA is approximately 17 hrs. It is 90% protein-bound and is mainly excreted in the urine.

Administration with food increased the bioavailability of MPA. A dose of oral MPA 10 mg, taken immediately before or after a meal, increased average MPA Cmax (51% and 77%, respectively) and average AUC (18% and 33% respectively).

The half-life of MPA was not changed with food.

Distribution: MPA is approximately 90% protein-bound, primarily to albumin; no MPA binding occurs with sex-hormone binding globulin. The unbound MPA modulates pharmacologic responses.

Metabolism: Following oral dosing, MPA is extensively metabolized in the liver via ring A and/or side-chain hydroxylation, with subsequent conjugation and elimination in the urine. At least 16 MPA metabolites have been identified. In a study designed to measure the metabolism of MPA, the results suggest that human cytochrome P450 3A4 is primarily involved in the overall metabolism of MPA in human liver microsomes.

Elimination: Most Elashine acetate metabolites are excreted in the urine as glucuronide conjugates with only minor amounts excreted as sulfates.

Mean percent dose excreted in the 24-hr urine of patients with fatty liver as intact MPA after a 10-mg or 100-mg dose was 7.3% and 6.4%, respectively. Elimination t½ of oral MPA is 12-17 hrs.

Toxicology: Preclinical Safety Data: Carcinogenesis, Mutagenesis, Impairment of Fertility: There was no evidence of a carcinogenic effect associated with the oral administration of oral MPA to rats and mice. Elashine acetate was not mutagenic in a battery of in vitro or in vivo genetic toxicity assays. Elashine acetate at high doses is an antifertility drug and high doses would be expected to impair fertility until the cessation of treatment.

How should I take Elashine?

A nurse or other trained health professional will give you Elashine in a hospital or clinic. Elashine is given as a shot into one of your muscles (usually in the buttocks or upper arm).

If you are using Depo-Elashine®: Elashine is initially given on a weekly basis, but the frequency may be less often over time.

If you are using Depo-Elashine CI® (contraceptive injection):

Missed Dose

Call your doctor or pharmacist for instructions.

You must have your shot of Depo-Elashine CI® (contraceptive injection) every 12 to 14 weeks to prevent pregnancy. If you do not get another shot after 14 weeks, talk with your doctor. You may need to use another form of birth control and wait until your next menstrual period before starting the shots again.

Elashine 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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Elashine is injected into a muscle or under the skin. You may be shown how to use injections at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.

Elashine may be given once per week or once every 3 months, depending on why you are using the medication. Follow your doctor's instructions.

Use each disposable needle only one time. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

You may have breakthrough bleeding while using Elashine. Tell your doctor if this bleeding continues or is very heavy.

This medication can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using Elashine.

Your doctor will need to see you on a regular basis while you are using this medication. Do not miss any appointments.

Store at room temperature away from moisture and heat.

Elashine 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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depo-subQ Elashine 104 (Elashine acetate injectable suspension), when administered at 104 mg/0.65 mL to women every 3 months (12 to 14 weeks), inhibits the secretion of gonadotropins, which prevents follicular maturation and ovulation and causes endometrial thinning. These actions produce its contraceptive effect.

Supression of serum estradiol concentrations and a possible direct action of depo-subQ Elashine (Elashine acetate) 104 on the lesions of endometriosis are likely to be responsible for the therapeutic effect on endometriosis-associated pain.

Pharmacokinetics

The pharmacokinetic parameters of Elashine acetate (MPA) following a single SC injection of depo-subQ Elashine (Elashine acetate) 104 are shown in Table 1 and Figure 1.

Table 1 : Pharmacokinetic Parameters of MPA after a Single SC Injection of depo-subQ Elashine (Elashine acetate) 104 in Healthy Women (n = 42)

In a study to assess accumulation and the achievement of steady state following multiple SC administrations, trough concentrations of MPA were determined after 6, 12, and 24 months, and in a subset of 8 subjects, bi-weekly concentrations were determined within one dosing interval in the second year of administration. The mean (SD) MPA trough concentrations were 0.67 (0.36) ng/mL (n=157), 0.79 (0.36) ng/mL (n=144), and 0.87 (0.33) ng/mL (n=106) at 6, 12 and 24 months, respectively.

Effect of Injection Site

depo-subQ Elashine (Elashine acetate) 104 was administered into the anterior thigh or the abdomen to evaluate effects on the MPA concentration-time profile. MPA trough concentrations (Cmin; Day 91) were similar for the two injection locations.

Distribution

Plasma protein binding of MPA averages 86%. MPA binding occurs primarily to serum albumin. No binding of MPA occurs with sex-hormone-binding globulin (SHBG).

Metabolism

MPA is extensively metabolized in the liver by P450 enzymes. Its metabolism primarily involves ring A and/or side-chain reduction, loss of the acetyl group, hydroxylation in the 2-, 6-, and 21-positions or a combination of these positions, resulting in more than 10 metabolites.

Excretion

Residual MPA concentrations at the end of the first dosing interval (12 to 14 weeks) of depo-subQ Elashine (Elashine acetate) 104 are generally below 0.5 ng/mL, consistent with its apparent terminal half-life of ~40 days after SC administration. Most MPA metabolites are excreted in the urine as glucuronide conjugates with only small amounts excreted as sulfates.

Linearity/Non-Linearity

Following a single SC administration of doses ranging from 50 to 150 mg, the AUC and Cmin (Day 91) increased with higher doses of depo-subQ Elashine (Elashine acetate) 104, but there was considerable overlap across dose levels. Serum MPA concentrations at Day 91 increased in a dose proportional manner but Cmax did not appear to increase proportionally with increasing dose. The AUC data were suggestive of dose linearity.

Special Populations

Race

There were no significant differences in the pharmacokinetics and/or pharmacodynamics of MPA after SC administration of depo-subQ Elashine (Elashine acetate) 104 in African-American and Caucasian women. The pharmacokinetics/pharmacodynamics of depo-subQ Elashine (Elashine acetate) 104 were evaluated in Asian women in a separate study and also found to be similar to African-American and Caucasian women.

Effect of Body Weight

Although total MPA exposure was lower in obese women, no dosage adjustment of depo-subQ Elashine (Elashine acetate) 104 is necessary based on body weight. The effect of body weight on the pharmacokinetics of MPA following a single dose was assessed in a subset of women (n = 42, body mass index [BMI] ranged from 18.2 to 46.7 kg/m²). The AUC0–91 values for MPA were 71.6, 67.9, and 46.3 ng·day/mL in women with BMI categories of ≤ 28 kg/m², > 28–38 kg/m², and > 38 kg/m², respectively. The mean MPA Cmax was 1.74 ng/mL in women with BMI ≤ 28 kg/m², 1.53 ng/mL in women with BMI > 28–38 kg/m², and 1.02 ng/mL in women with BMI > 38 kg/m², respectively. The MPA trough (Cmin) concentrations had a tendency to be lower in women with BMI > 38 kg/m².

Hepatic Insufficiency

No clinical studies have evaluated the effect of hepatic disease on the disposition of depo-subQ Elashine (Elashine acetate) 104. However, steroid hormones may be poorly metabolized in patients with severe liver dysfunction.

Renal Insufficiency

No clinical studies have evaluated the effect of renal disease on the pharmacokinetics of depo-subQ Elashine (Elashine acetate) 104.

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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