Role Of Megestrol Acetate Tablet:

• Progestogens, particularly megestrol acetate, are commonly used to treat anorexia-cachexia.

• Considerable evidence demonstrates the efficacy of megestrol acetate in the treatment of cachexia, the key characteristics of which are decreased appetite and low bodyweight.

• Megestrol acetate significantly increases both appetite and bodyweight.

• In doses ranging from 40 to 320 mg/day, megestrol acetate has been shown to stimulate appetite, increase caloric intake, induce a sense of wellbeing, and produce weight gain. 

• Megestrol acetate appears to have direct ant cytokine properties.

• The drug significantly antagonizes the effects of cytokines such as TNFá, IL-6, and IL-1. 

• In patients with cancer, megestrol acetate has been shown to significantly reduce serum levels of IL-1and beta and reduce IL-6 production in peripheral blood mononuclear cells. 

• Megestrol acetate has significant orexigenic properties.

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Therapeutic indications:

• Oncostrol is a progestational agent, indicated for the treatment of certain hormone dependent neoplasms, such as breast cancer, endometrial cancer and some time in loss of appetite in cancer and HIV patients.

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Undesirable effects of Megestrol Acetate:

• The main side-effect experienced by patients while taking megestrol acetate, particularly at high doses, is weight gain, which is usually not associated with water retention, but which is secondary to an increased appetite and food intake. Weight gain is associated with an increase in fat and body cell mass.

• Constipation and urinary frequency have also been reported in patients who received high doses of megestrol acetate in clinical trials.

• A rarely encountered side effect of prolonged administration of megestrol acetate is urticaria, presumably an idiosyncratic reaction to the drug. The drug is devoid of the myelosuppressive activity characteristic of many cytotoxic drugs and it causes no significant changes in haematology, blood chemistry or urinalysis.

• Pituitary adrenal axis abnormalities including glucose intolerance, new onset diabetes, exacerbation of pre-existing diabetes with decreased glucose tolerance and Cushing's syndrome have been reported with the use of megestrol acetate.

• Clinically apparent adrenal insufficiency has been rarely reported in patients shortly after discontinuing megestrol acetate. The possibility of adrenal suppression should be considered in all patients taking or withdrawing from chronic megestrol acetate therapy.

• Replacement stress doses of glucocorticoids may be indicated.

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Pharmacodynamic properties of Megestrol Acetate:

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• Megestrol Acetate possesses pharmacological properties similar to those of natural progesterone.

• Its progestational activity is slightly greater than that of medroxyprogesterone acetate, norethindrone, norethindrone acetate and norethynodrel; slightly less than that of chlormadinone acetate; and substantially less than that of norgestrel.

• Megestrol acetate is a potent progestogen that exerts significant anti-oestrogenic effects. It has no androgenic or oestrogenic properties. It has anti-gonadotropic, anti-uterotropic and anti-androgenic/anti-myotropic actions. It has a slight but significant glucocorticoid effect and a very slight mineralocorticoid effect.

 

Pharmacokinetic properties of Megestrol Acetate:

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• Peak plasma levels of tritiated megestrol acetate and metabolites occur one to three hours after oral administration.

• When 4 to 91mg of c-labelled megestrol acetate were administered orally to women, the major route of drug elimination was in the urine.

• The urinary and fecal recovery of total radioactivity within 10 days ranged from 56.6% to 78.4% (mean 66.4%) and 7.7% to 30.3% (mean 19.8%), respectively.

• The total recovered radioactivity varied between 83.1% and 94.7% (mean 86.2%).

• Megestrol acetate metabolites, which were identified in the urine as glucuronide conjugates, were 17-alpha-acetoxy-2-alpha hydroxy-6-methylpregna-4, 6-diene-3, 20-dione; 17-alpha-acetoxy-6-hydroxymethylpregna-4, 6-diene-3, 20-dione; and 17-alpha-acetoxy-2 alpha-hydroxy-6-hydromethylpregna-4, 6-diene-3, 20-dione; these identified metabolites accounted for only 5-8% of the administered dose.

• Serum concentrations were measured after the administration of single and multiple oral doses of megestrol acetate.

• Adult male and post-menopausal female volunteers, no more than 65 years of age participated in the study.

• Megestrol acetate is readily absorbed following oral administration of 20, 40, 80 and 200 mg doses.

• Megestrol serum concentrations increase with increasing doses, the relationship between increasing dosage and increasing serum levels not being arithmetically proportional. Average peak serum concentrations for the four doses tested were 89, 190, 209 and 465 ng/ml.

• Mean peak serum concentrations are found three hours after single-dose administration for all dosage levels studied. The serum concentration curve appears biphasic, and the beta-phase half-life is 15 to 20 hours long.

• After multiple doses over a three-day period, serum levels increase each day and are estimated to reach 80% to 90% predicted steady-state levels on the third day.(Ref: https://www.medicines.org.uk/emc/product/11135)

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MECHANISM OF ACTION:

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• Megestrol shares the properties of the progestins.

• The drug induces endometrial secretory changes, increases basal body temperature, inhibits pituitary function, and precipitates bleeding when estrogen is present.

• The mechanism of its antineoplastic activity is not known, but it has been suggested that megestrol-induced suppression of luteinizing hormone release from the pituitary may have a negative effect on cancerous tissues of the breast and endometrial lining.

• Megestrol enhances estrogen metabolism, which suppresses estrogen-dependent tumors by lowering plasma estrogen concentrations. Megestrol also may change the actively growing cancer cell stroma into decidua.

• Because megestrol promotes the differentiation and maintenance of endometrial tissue, it is effective in the therapy of endometriosis and endometrial cancer.

• The reported weight gain associated with megestrol therapy is believed to be due to the drug's metabolic and appetite-stimulatory effects rather than to its glucocorticoid activity.

• Megestrol, or its metabolites, may interfere with cachexin, the hormone that inhibits adipocyte lipogenic enzymes and leads to the wasting syndrome of AIDS or cancer.

• Weight gain occurs within 3 weeks in most patients who receive megestrol for this purpose.(Ref: https://www.pdr.net/drug-summary/Megace-megestrol-acetate-890.343)

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Is Megestrol Acetate Health supplements or pain Killer?

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• No.

• Megestrol Acetate is a type of hormonal therapy that is used by oncology doctors and other medical professionals to treat a variety of medical conditions. 

• Megestrol acetate is not a any kind of health supplement, and it does not contain any vitamins or minerals.

• In addition, there is not a single study that demonstrates that Megestrol Acetate can alleviate any kind of pain that can occur in the human body.

• Megestrol acetate should only ever be used under the close supervision of a qualified medical professional.

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What is Oncostrol 160 tablets and its use?​

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• Megestrol Acetate is a pharmaceutical API that is included in Oncostrol 160 Tablet.

• This medication is analogous to the hormone progesterone, which is produced by your body on a natural basis.

• Cancers of the breast and endometrial that are dependent on hormones are treated with it (lining of the uterus).

• In addition to this, it can be used to stimulate appetite and help AIDS patients gain weight.

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Does Oncostrol 160mg cause weight gain?

• Yes.

• Weight gain is a common side effect of Oncostrol 160 Tablet.

• Weight gain could be the result of an increase in appetite, which leads to an increase in fat and body cell mass overall.

• If you are gaining a lot of weight, see your doctor. It is frequently used to treat malnutrition, appetite loss, and severe weight loss in patients with acquired immunodeficiency syndrome (AIDS).

• It is not, however, intended for use as a preventive measure to avoid weight loss.

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When is the best time to take Oncostrol 160 Tablet?

• Oncostrol 160 Tablet can be taken at any time of day.

• You should, however, take it exactly as directed by your doctor.

• With a glass of water, swallow it whole. It can be taken with or without food, preferably at the same time every day so that you remember to take it.

• If you are unsure, consult your doctor.

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Does Oncostrol 160 Tablet prevent menstruation?

• No,

• Oncostrol 160 Tablet does not prevent menstruation.

• It may, however, disrupt your normal menstrual cycle.

• It has limited use in HIV-infected women because it can cause break-through bleeding.

• Consult your doctor if you experience breakthrough bleeding while taking Oncostrol 160 Tablet.

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Is Oncostrol 160 Tablet a chemotherapy medication?

 

• No.

• Oncostrol 160 Tablet is not a chemotherapy medication, contrary to popular belief.

• It is an artificial analogue of the naturally occurring hormone progesterone. Breast cancer and endometrial cancer are two types of cancer that benefit from its use in treatment (cancer of the uterus).

• It achieves this by acting on the female hormones, which play a role in the development of cancer.

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Is it safe to take Oncostrol 160 Tablet acetate while pregnant?

• No.

• If you are pregnant or planning to become pregnant, you should not take Oncostrol 160 Tablet.

• However, if you become pregnant while taking Oncostrol 160 Tablet, contact your doctor immediately because Oncostrol 160 Tablet may harm your unborn baby.

• It is critical to notify your doctor because it may cause sex organ abnormalities in male and female babies if taken during the first three months of pregnancy.

• Before beginning treatment with Oncostrol 160 Tablet, your doctor may recommend a pregnancy test.

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Is Oncostrol 160 Tablet effective in preventing pregnancy?

 

• No

• Pregnancy is not prevented by Oncostrol 160 Tablet.

• Menstruation may be affected, but pregnancy is not prevented. As a result, if you want to avoid getting pregnant, you should use a proven method of birth control.

• If you're unsure or have any concerns, make an appointment with your doctor.

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Is Oncostrol 160 Tablet used for hot flashes?

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• The use of Oncostrol 160 Tablet in the treatment of hot flashes is not recommended.

• Before taking Oncostrol 160 Tablet, always talk to your doctor.

• For the treatment of hot flashes, oestrogen in women and androgen in men are commonly used, but these hormones cannot be used in breast cancer patients and prostate cancer patients.

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Difference Between Fulvestrant and Megestrol Acetate

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Chemical Structure of Megestrol Acetate:

                                                      Megestrol Acetate, also known as 17α-acetoxy-6-dehydro-6-methylprogesterone                                                        or as 17α-acetoxy-6-methylpregna-4,6-diene-3,20-dione, is a synthetic pregnane                                                        steroid and a derivative of progesterone.

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