Estramustine is a medication that combines estradiol, a form of the hormone estrogen, with the nitrogen mustard compound nor-nitrogen mustard. This combination makes it a type of chemotherapy drug used in the treatment of advanced prostate cancer. It's primarily used when the cancer has spread beyond the prostate gland and other treatments like surgery or radiation therapy are no longer effective.

Emcyt (Estramustine) is an estrogen derivative that has potent antiandrogen activity. It is used in patients with metastatic or progressive prostatic carcinoma.

Emcyt (Estramustine) Use:

• It is used for the palliative treatment of metastatic prostatic carcinoma.

Emcyt (Estramustine) Dose in Adults:

It is indicated for the palliative treatment of patients with metastatic and/or progressive prostate carcinoma.

• Estramustine is a medicine used to help relieve symptoms for patients with advanced prostate cancer that has spread.
• Patients typically take it by mouth in divided doses that add up to 14 mg for every kg of their body weight.
• This treatment can last from 30 to 90 days, depending on how well a patient handles the medicine or how well it's working.

Use in Children:

It is not indicated for use in children.

Pregnancy Risk Category: X

• Estramustine is not for women.
• Some men who couldn't have sex while on other hormone treatments found they could when taking estramustine.
• So, men using this medicine should use birth control if their partners can still have children.

Use of Estramustine during breastfeeding

• Estramustine is not meant for women.

Estramustine Use in renal disease:

Use with caution in patients with kidney disease as it may cause fluid retention.

Estramustine Use in Liver disease:

Avoid using it in patients with liver disease.

Frequency not always defined.

Common Side Effects of Emcyt (Estramustine):

• Cardiovascular:
  • Edema
• Endocrine & Metabolic:
  • Gynecomastia
  • Increased Lactate Dehydrogenase
  • Decreased Libido
• Gastrointestinal:
  • Nausea
  • Diarrhea
  • Gastrointestinal Irritation
• Genitourinary:
  • Breast Tenderness
• Hepatic:
  • Increased Serum AST
• Respiratory:
  • Dyspnea

Less Common Side Effects Of Emcyt (Estramustine):

• Cardiovascular:
  • Cardiac Failure
  • Local Thrombophlebitis
  • Myocardial Infarction
  • Cerebrovascular Accident
  • Pulmonary Embolism
  • Chest Pain
  • Flushing
• Central Nervous System:
  • Lethargy
  • Insomnia
  • Emotional Lability
  • Anxiety
  • Headache
• Dermatologic:
  • Pruritus
  • Xeroderma
  • Exfoliation Of Skin
  • Skin Rash
  • Thinning Hair
• Endocrine & Metabolic:
  • Increased Thirst
• Gastrointestinal:
  • Anorexia
  • Flatulence
  • Gastrointestinal Hemorrhage
  • Sore Throat
  • Vomiting
• Hematologic & Oncologic:
  • Leukopenia
  • Bruise
  • Thrombocytopenia
• Hepatic:
  • Increased Serum Bilirubin
• Neuromuscular & Skeletal:
  • Leg Cramps
• Ophthalmic:
  • Lacrimation
• Respiratory:
  • Hoarseness
  • Rhinorrhea

Contraindications to Emcyt (Estramustine):

You shouldn't take Estramustine if you're allergic to it, estradiol, nitrogen mustard, or anything else in the drug. Don't take it if you have blood clot problems unless the cancer is causing it and the benefits outweigh the risks.

In Canada, people with serious liver or heart diseases shouldn't take it either.

Even though we're not sure if people allergic to other estrogens might be allergic to this, it's possible due to their similarities.

Warnings and precautions

Cardiovascular effects

• Taking Estramustine can raise blood pressure or cause heart problems.
• Men treated with estrogens for prostate cancer might have a higher risk of blood clots or heart attacks, sometimes fatal.
• If someone has had blood clot issues, especially with estrogen treatment, or has had strokes or heart problems, be very careful using Estramustine.

Endocrine effects

• Estramustine can act like estrogen, which might lower testosterone in the body.
• This can lead to breast growth in men and/or difficulty in having an erection.

Fluid retention

• Estramustine can cause swelling or worsen heart problems.
• Be careful using it in people who can't handle extra fluid, like those with heart issues, high blood pressure, migraines, seizures, or kidney problems.

Gastrointestinal toxicities:

• Estramustine can make people feel like throwing up.
• It's a good idea to take medicine to prevent nausea and vomiting when using it.

Tolerance to glucose:

• Estramustine might affect how the body handles sugar.
• Be careful when using it in people with diabetes.

Hepatic effects

• Estramustine can affect liver tests.
• Keep an eye on the liver while using it and for 2 months after stopping.

Hypersensitivity

• ome people have had allergic reactions, including swelling that can affect breathing, while using Estramustine.

Hypertension

• Estramustine can raise blood pressure.
• Check blood pressure regularly when using it.

Hepatic impairment

• Be careful using Estramustine in people with liver issues, as their liver might not process the drug well.

Metabolic bone disease

• Be careful using Estramustine in people with bone diseases because it can affect calcium and phosphorus balance in the body.

Osteoblastic metastases

• People with cancer spread to the bones might have low calcium levels.
• Check their calcium often when using Estramustine.

Renal impairment

• Be careful using Estramustine in people with kidney issues.

Estramustine: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy)
Clodronate	May increase the serum concentration of Estramustine.
Coccidioides immitis Skin Test	Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test.
Denosumab	May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased.
Ocrelizumab	May enhance the immunosuppressive effect of Immunosuppressants.
Pidotimod	Immunosuppressants may diminish the therapeutic effect of Pidotimod.
Siponimod	Immunosuppressants may enhance the immunosuppressive effect of Siponimod.
Tertomotide	Immunosuppressants may diminish the therapeutic effect of Tertomotide.
Trastuzumab	May enhance the neutropenic effect of Immunosuppressants.
Risk Factor D (Consider therapy modification)
Baricitinib	Immunosuppressants may enhance the immunosuppressive effect of Baricitinib. Management: Use of baricitinib in combination with potent immunosuppressants such as azathioprine or cyclosporine is not recommended. Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted.
Calcium Salts	May decrease the absorption of Estramustine. Exceptions: Calcium Chloride.
Echinacea	May diminish the therapeutic effect of Immunosuppressants.
Fingolimod	Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections).
Leflunomide	Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly.
Lenograstim	Antineoplastic Agents may diminish the therapeutic effect of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy.
Lipegfilgrastim	Antineoplastic Agents may diminish the therapeutic effect of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy.
Nivolumab	Immunosuppressants may diminish the therapeutic effect of Nivolumab.
Palifermin	May enhance the adverse/toxic effect of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy.
Roflumilast	May enhance the immunosuppressive effect of Immunosuppressants.
Sipuleucel-T	Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Management: Evaluate patients to see if it is medically appropriate to reduce or discontinue therapy with immunosuppressants prior to initiating sipuleucel-T therapy.
Tofacitinib	Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants.
Vaccines (Inactivated)	Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation.
Risk Factor X (Avoid combination)
BCG (Intravesical)	Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical).
Cladribine	May enhance the immunosuppressive effect of Immunosuppressants.
Natalizumab	Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased.
Pimecrolimus	May enhance the adverse/toxic effect of Immunosuppressants.
Tacrolimus (Topical)	May enhance the adverse/toxic effect of Immunosuppressants.
Vaccines (Live)	Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants.

Monitoring parameters:

Bone Health:

• Check calcium levels in the blood.

Liver Health:

• Test liver function during treatment.
• Continue testing for 2 months after treatment ends.

Blood Sugar (For People with Diabetes):

• Check blood sugar levels.

Blood Pressure:

• Monitor blood pressure regularly.

Fluid Levels:

• Keep an eye on signs of fluid buildup.

Taking the Medicine:

• Make sure the medicine is taken as prescribed.

How to administer Emcyt (Estramustine)?

Nausea Potential:

• Estramustine can make people feel like throwing up.
• It's a good idea to take anti-nausea medicine to prevent this.

How to Take It:

• Take on an empty stomach: either 1 hour before eating or 2 hours after eating.
• Drink with water.
• Don't take with milk, milk products, or calcium products.

Mechanism of action of Estramustine:

Two-in-One Combo:

• Estramustine is a mix of estradiol and nornitrogen mustard carbamate.
• Estradiol has antiandrogen effects.
• Nornitrogen mustard has effects on microtubules.

Effects on Hormones:

• Lowers testosterone in the blood a lot.
• Raises estrogen levels.

Absorption:

• Not fully absorbed.
• Details: Incomplete absorption (Based on Bergeheim 1998's study).

Metabolism (How it's processed in the body):

• First, it's changed in the stomach and intestines.
• Then, in the liver, it's turned into various forms: estramustine, estromustine, estrone, and estradiol.

How much is available after taking:

• When taken by mouth: Between 44% to 75% of it is available for the body to use (Bergeheim 1998).

How long it stays in the body:

• Estromustine: About 13.6 hours, but it can range between 9 to 23 hours.
• Estrone: About 16.5 hours (Bergeheim 1998).

When it reaches its maximum level in the body:

• Between 2 to 3 hours after taking (Bergeheim 1998).

How it leaves the body:

• Mostly through feces.
• A very small amount is found in urine (Bergeheim 1998).

International Brand Names of Estramustine:

• Emcyt
• Estracyt
• Multosin
• X-Trant

Estramustine Brand Names in Pakistan:

Not available.