Description

Androcur 50 mg Tablets in Pakistan

Manufacturer

• Androcur is produced by Bayer.

Dosage

• The typical starting dose for adults is one tablet taken twice daily, ideally after meals.
• The treatment duration is tailored to individual needs, and the dosage may be adjusted based on therapeutic response.

Indications

• Men: Control of libido in severe hypersexuality and sexual deviations.
• Women: Treatment of severe hirsutism, androgen-dependent hair loss, and severe acne.

Side Effects and Precautions

• Common side effects include decreased libido and erectile dysfunction.
• More serious risks involve hepatic toxicity and potential development of liver tumors.
• Patients are advised to monitor for symptoms such as fatigue and should avoid driving or operating machinery if affected.
  

  Key Benefits of Androcur 50 mg Tablets

  • Used to treat advanced prostate cancer by blocking the effects of testosterone, which can help slow or stop cancer growth
  • Reduces abnormal sex drive and libido in men
  • Treats severe hirsutism (excessive hair growth), hair loss, acne, and oily skin in women by blocking androgen effects

  Key Ingredients

  • Androcur 50 mg tablets contain 50 mg of the active ingredient cyproterone acetate
  • Other ingredients include lactose, corn starch, povidone, magnesium stearate, and aerosil

  Mechanism of Action of Androcur (Cyproterone Acetate)

  Androcur, containing cyproterone acetate, functions primarily as a steroidal anti-androgen. Its mechanism of action involves several key processes:

  1. Androgen Receptor Blockade

  Cyproterone acetate competes with natural androgens, such as testosterone, for binding to androgen receptors. By blocking these receptors, it inhibits the physiological effects of androgens, which can contribute to the growth of certain cancers, particularly prostate cancer.

  2. Progestogenic Activity

  In addition to its anti-androgenic properties, cyproterone acetate exhibits progestogenic activity. This means it can exert a negative feedback effect on the hypothalamic-pituitary-gonadal axis, leading to decreased secretion of gonadotropins (LH and FSH) from the pituitary gland. This reduction in gonadotropins subsequently lowers testosterone production from the testes, further contributing to its anti-androgen effects.

  3. Clinical Applications

  • Prostate Cancer: By blocking androgens, Androcur can slow or stop the growth of prostate cancer cells that rely on these hormones for proliferation.
  • Sexual Drive Control: It is also used to manage abnormal sexual drive in men by reducing testosterone levels and its effects.
  
  

  Cyproterone acetate

  Antiandrogen and progestin medication

  More

  Uses

  Treatment of acne, excessive body hair growth, early puberty, prostate cancer, feminizing hormone therapy for transgender women, and in birth control pills

  Trade Names

  Androcur, Diane, Diane-35, among others

  Side Effects

  Gynecomastia, feminization, low sex hormone levels, reversible infertility, sexual dysfunction, fatigue, depression, weight gain, elevated liver enzymes

  Chemical Structure of Cyproterone Acetate (Androcur)

  Chemical Name

  • 6-chloro-17α-hydroxy-1α,2α-methylene-pregna-4,6-diene-3,20-dione acetate

  Molecular Formula

  • C24H29ClO4

  Molecular Weight

  • 416.95 g/mol

  Structural Representation

  Cyproterone acetate has a complex steroid structure characterized by a cyclopentanoperhydrophenanthrene core. The presence of a chlorine atom and a methylene group contributes to its unique properties as an anti-androgen.

  

  Synthesis of Cyproterone Acetate

  Cyproterone acetate is synthesized through a multi-step process that involves several key reactions to modify steroid precursors. Here is an overview of the synthesis based on recent methods:

  1. Starting Material

  The synthesis often begins with 17α-acetoxyprogesterone or solasodine as the primary starting material.

  2. Key Steps in Synthesis

  • Formation of Chlormadinone Acetate: The initial step involves converting the starting material into 6,7α-oxido-4-pregnene-17α-ol-3,20-dione-17-acetate using anhydrous hydrogen chloride gas. This intermediate is then transformed into chlormadinone acetate.
  • Dehydrogenation: A dehydrogenation step is performed using 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) to introduce a double bond at position 1 of the chlormadinone acetate.
  • Methylene Group Introduction: The next step involves introducing a methylene bridge between positions 1 and 2 of the resulting compound, yielding cyproterone acetate.

  3. Improved Methods

  Recent advancements have streamlined the synthesis process, reducing the number of steps from the conventional 18 to about 14 or 16 steps. This includes more efficient reaction conditions and the use of solvents like dioxane and reagents such as selenium dioxide for specific transformations.

  Key Precautions and Dietary Restrictions with Androcur (Cyproterone Acetate)

  Precautions

  • Liver problems: Androcur may cause severe or even fatal liver problems. Regular liver function tests are required before and during treatment, and the medication may need to be stopped if issues arise.
  • Tumor risks: Androcur has been linked to the development of benign liver tumors and in rare cases, malignant liver tumors. These tumors can lead to life-threatening abdominal bleeding.
  • Meningioma risk: Long-term use of Androcur, especially at high doses (25 mg/day or more), has been associated with an increased risk of developing a generally benign brain tumor called meningioma. If diagnosed, treatment must be stopped.
  • Fertility effects: In men, Androcur normally prevents sperm production, which is usually reversible within a few months of discontinuing therapy. It can also cause impotence.
  • Adrenal gland problems: Rarely, Androcur may cause improper functioning of the adrenal glands, especially in times of stress like surgery, injury or severe infection.

  Dietary Restrictions

  • Alcohol intake: Alcohol consumption should be limited while taking Androcur as it may reduce the effectiveness of the medication.
  • No specific dietary restrictions: There are no other specific dietary restrictions mentioned in the provided information. However, it is always best to discuss any dietary questions with your doctor or pharmacist.

  Dietary Restrictions

  • Alcohol Consumption: Limit alcohol intake while taking Androcur, as it may reduce the effectiveness of the medication and increase the risk of side effects.
  • Lactose Consideration: Androcur contains lactose. If you have lactose intolerance or any related conditions, consult your doctor before taking this medication.

  General Precautions

  • Regular Monitoring: Regular liver function tests are necessary, as Androcur can cause liver problems, including severe liver toxicity.
  • Medical Consultation: Always discuss any other medications or supplements you are taking with your healthcare provider, as interactions may occur.

  Androcur (cyproterone acetate) may interact with several medications:

  • Statins (medicines for reducing blood fats): The risk of statin-associated myopathy or rhabdomyolysis may be increased when statins metabolized primarily by CYP 3A4 are co-administered with high therapeutic cyproterone acetate doses, as they share the same metabolic pathway.
  • Ketoconazole, itraconazole, clotrimazole, ritonavir, and other strong inhibitors of CYP3A4: These medications may inhibit the metabolism of cyproterone acetate, as Androcur is metabolized by CYP3A4.
  • Inducers of CYP3A4 such as rifampicin, phenytoin, and products containing St. John’s wort: These may reduce the levels of cyproterone acetate.
  • Substrates of the P450 enzymes CYP2C8, 2C9, 2C19, 3A4, and 2D6: Caution should be exercised when co-administering Androcur with these medications, as inhibition of these enzymes is possible at high therapeutic doses of 300 mg daily.
  • Alcohol: Alcohol consumption should be limited while taking Androcur, as it may reduce the effectiveness of the medication.

  Medications to Avoid

  • Statins: The risk of statin-associated muscle problems may be increased when statins metabolized primarily by CYP 3A4 are co-administered with high therapeutic cyproterone acetate doses, as they share the same metabolic pathway.
  • Strong inhibitors of CYP3A4 like ketoconazole, itraconazole, clotrimazole, ritonavir: These medications may inhibit the metabolism of cyproterone acetate, as Androcur is metabolized by CYP3A4.
  • Inducers of CYP3A4 such as rifampicin, phenytoin, and products containing St. John’s wort: These may reduce the levels of cyproterone acetate.

  Use with Caution

  • Substrates of the P450 enzymes CYP2C8, 2C9, 2C19, 3A4, and 2D6: Caution should be exercised when co-administering Androcur with these medications, as inhibition of these enzymes is possible at high therapeutic doses of 300 mg daily.
  • Alcohol: Alcohol consumption should be limited while taking Androcur, as it may reduce the effectiveness of the medication.

  Pregnancy

  • Androcur should not be used by pregnant women, as it may affect the developing baby if taken during pregnancy.
  • Before starting Androcur, your doctor will check that you are not pregnant.
  • Women should use a reliable form of contraception while taking Androcur.

  Breastfeeding

  • Androcur should not be used by women who are breastfeeding, as the active ingredient passes into breast milk and there is a possibility that the baby may be affected.                                         
    

    Dosage of Androcur (Cyproterone Acetate)

    The dosage of Androcur varies depending on the condition being treated:

    • Men with prostate cancer: The usual daily dose is 50-300 mg of Androcur. The doctor may request taking Androcur with other medicines and/or change the dose during treatment.
    • Men for reduction of abnormal sex drive: Treatment is generally started with 50 mg of Androcur twice daily and may be increased to 100 mg twice daily or three times daily before reducing gradually to the lowest effective dose. The doctor may change the dose during treatment.
    • Women of childbearing age: If taking Androcur for 10 days starting from day 1 of the menstrual cycle, the dose is 50-100 mg daily as advised by the doctor. An appropriate contraceptive is also taken to provide contraceptive protection and stabilize the cycle.
    • Postmenopausal women or those who have had a hysterectomy: The usual dose is 25-50 mg of Androcur once daily for 21 days, followed by a 7-day tablet-free interval.

    Storage

    • Do not take Androcur after the expiry date printed on the pack and blister.
    • Do not take Androcur if the packaging is torn or shows signs of tampering.
    • If the packaging is damaged, return it to your pharmacist for disposal.

    Reviews

    No specific reviews were provided in the given search results. However, it is important to consult with a healthcare professional regarding the use of Androcur and to report any side effects or concerns.