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.

• 14 mg/kg orally in three or four divided doses.
• The treatment may be continued for 30 to 90 days until toxicity or as long as the favorable response lasts.

Use in Children:

It is not indicated for use in children.

Pregnancy Risk Category: X

• It is not recommended for women.
• It can cause impotence in males, but it is possible to get pregnant. Male patients who are pregnant should use effective contraception.

Use of Estramustine during breastfeeding

• It is not recommended for use by women.

Use in renal disease:

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

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):

• Allergy to any component of the formulation, such as estradiol, nitro mustard, or the drug;
• Patients with active thrombophlebitis and thromboembolic disorders, except for patients in whom the benefits may outweigh any risks.
• Advanced cardiac or liver disease

Warnings and precautions

• Cardiovascular effects

  • Patients could develop hypertension or congestive heart failure.
  • Patients with prostatic carcinoma are at greater risk of developing thrombosis.
  • Patients could develop fatal thrombotic events, such as myocardial Infarction.
  • Patients with thromboembolic diseases, thrombosis or thrombophlebitis should be cautious.
  • Patients with cerebrovascular disease or coronary artery disease should be cautious.

• Endocrine effects

  • The estrogenic effects of the drug can cause gynecomastia or impotence in patients.

• Fluid retention

  • Fluid overload may lead to peripheral edema and congestive heart failure.
  • Patients with fluid accumulations in the body, such as cardiovascular disease, hypertension, and renal failure, should not take it.
  • Patients with seizure and migraine disorders should be cautious when using it.

• Gastrointestinal toxicities:

  • There is a slight chance that the drug could cause vomiting.
  • To prevent nausea or vomiting, patients may be advised to take the drug along with an antiemetic.

• Tolerance to glucose:

  • Impaired glucose tolerance may result from the drug. Patients with diabetes should have their blood sugars closely monitored.

• Hepatic effects

  • Monitor for abnormalities in liver enzyme or bilirubin levels during treatment and for two months afterwards.

• Hypersensitivity

  • Airway compromise can occur from allergic reactions and angioedema.

• Hypertension

  • It can cause hypertension.
  • Patients with hypertension should have their blood pressure checked.

• Hepatic impairment

  • Patients with hepatic impairment may not be able to process the drug properly. This is why patients with liver disease should be cautious.

• Metabolic bone disease

  • Patients suffering from metabolic bone disease should be cautious about taking the drug because it can affect calcium and phosphate homeostasis.

• Osteoblastic metastases

  • It is important to monitor serum calcium levels regularly.
  • Hypoglycemia is more common in patients with bony metastasis.

• Renal impairment

  • Patients with impaired renal function should be cautious when taking the drug.

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

Monitoring parameters:

• Monitor serum calcium levels and liver function tests at baseline, during the treatment, and for two months after the last dose.
• Monitor plasma glucose levels in patients with diabetes.
• Monitor fluid and volume status, blood pressure, and adherence to therapy.

How to administer Emcyt (Estramustine)?

• It is best to take the drug on an empty stomach, at least one hour before and two hours after eating. You should drink plain water.
• There is a slight risk of vomiting from the drug. To prevent nausea or vomiting, it can be taken together with antiemetic medications.

Mechanism of action of Estramustine:

It is an estrogen- ( estradiol-linked combination drug) that has antiandrogen- and antimicrotubule effects due to the estrogen and nornitrogen- mustard compounds. It raises blood estrogen levels and lowers plasma testosterone levels.

Absorption:

• Incomplete

Metabolism:

• It is initially dephosphorylated in the gastrointestinal tract followed by oxidation in the liver and hydrolyzed to estromustine, estramustine (an oxidized isomer of estromustine), estrone, and estradiol.

Bioavailability:

• Oral: 44% to 75%

Half-life elimination:

• Estramustine: 13.6 hours (ranging from 9 to 23 hours);
• Estrone: 16.5 hours.

Time to peak:

• 2 to 3 hours.

Excretion:

• Primarily excreted via feces;
• A trace amount is excreted via urine.

International Brand Names of Estramustine:

• Emcyt
• Estracyt
• Multosin
• X-Trant

Estramustine Brand Names in Pakistan:

No Brands Available in Pakistan.