Megestrol acetate NEW

Specification of Megestrol acetate CAS 595-33-5:

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Megestrol Acetate is a synthetic progestin, which is a man-made version of the natural female hormone, progesterone. It is significantly more potent than natural progesterone when taken orally.

It is primarily used in medicine for two distinct purposes: treating certain cancers and stimulating appetite in wasting syndromes.

1. Chemical Structure and Classification

• Chemical Class: It is a synthetic steroid hormone, specifically a 17α-hydroxyprogesterone derivative.

  Key Feature: Its chemical structure is a modified version of the progesterone molecule. These modifications (including an additional double bond and an acetyl group) make it more potent and effective when taken orally, as it resists being broken down by the liver.

2. Mechanism of Action (How it Works)

How Megestrol Acetate works depends on its intended use:

• As an Anticancer Agent (for Breast/Endometrial Cancer):

1. Hormone Blocker: It binds to the progesterone receptor in hormone-sensitive cancer cells.

2. Alters Gene Expression: This binding changes the cell's gene activity, ultimately counteracting the growth-stimulating effects of estrogen.

3. Suppresses Ovulation: It can suppress the release of hormones from the pituitary gland that stimulate the ovaries to produce estrogen. This "starves" estrogen-dependent tumors of the fuel they need to grow.

• As an Appetite Stimulant (for Cachexia):
  The exact mechanism is not fully understood but is believed to involve:

1. Brain Appetite Center: It is thought to stimulate appetite by affecting the hypothalamus, the part of the brain that controls hunger. It may increase the production of Neuropeptide-Y, a potent appetite stimulant.

2. Reduces Inflammation: It may help by inhibiting inflammatory cytokines that contribute to the wasting process.

3. Promotes Fat Storage: Through its progestational activity, it can lead to weight gain, primarily as body fat.

3. Common Uses

1. Palliative Treatment of Cancer:

• Breast Cancer: Used as a second-line therapy for advanced, hormone-sensitive breast cancer.

• Endometrial Cancer: Used for the treatment of advanced endometrial cancer.

2. Treatment of Cachexia (Wasting Syndrome):

• AIDS

• Cancer (Cancer Cachexia)

• This is one of its most common uses today. It is prescribed to treat severe, unintentional weight loss and loss of appetite in patients with:

4. Important Considerations and Side Effects

• Formulations: It is available as an oral tablet and an oral suspension (liquid). The suspension is often preferred for appetite stimulation as it's easier for debilitated patients to swallow.

  Common Side Effects:

• Weight Gain: This is an intended effect for cachexia but can be an undesirable side effect in other contexts.

  Adrenal Suppression: This is a serious side effect. Long-term use can suppress the body's natural production of cortisol, a critical stress hormone. Abruptly stopping the drug can be dangerous and may require a slow, supervised dose reduction.

  Increased Risk of Blood Clots: Such as deep vein thrombosis (DVT) or pulmonary embolism (PE).

  Breakthrough Uterine Bleeding.

  Nausea, diarrhea, gas.

• Black Box Warning (US FDA): The label carries the FDA's strongest warning due to several serious risks:

• Increased risk of blood clots.

  It must not be used during pregnancy as it can cause birth defects.

Summary

In essence, Megestrol Acetate is a potent synthetic progestin. Its primary clinical value lies in its dual ability to act as a hormonal anti-cancer agent and as a powerful appetite stimulant to counteract severe weight loss in conditions like AIDS and cancer. Its use requires careful medical supervision due to significant potential side effects, particularly its impact on the adrenal gland and the risk of blood clots.

Package of Megestrol acetate CAS 595-33-5:

Application of Megestrol acetate CAS 595-33-5:

Intermediate of medroxyprogesterone.