Description

Aromasin (exemestane) 25mg Tablets in Pakistan

Availability

• Aromasin is available in Pakistan primarily in a 25 mg dosage
• Typically packaged in strips of 15 tablets

Pricing

• The cost of Aromasin 25 mg (15 tablets) ranges from approximately Rs. 7,398.75 to Rs. 7,788.15, depending on the retailer

Indications

• Adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received prior tamoxifen therapy
• Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen treatment

Mechanism of Action

• Exemestane is an irreversible aromatase inhibitor that reduces estrogen levels in the body
• Estrogen reduction is crucial for the growth of certain types of breast cancer

Prescription Requirement

• Aromasin requires a prescription for purchase in Pakistan
  

  Key Benefits of Aromasin (exemestane) 25mg Tablets

  • Treats early and advanced breast cancer in postmenopausal women
  • Indicated for hormone-receptor-positive breast cancer
  • Helps prevent breast cancer from returning after prior tamoxifen therapy
  • Significantly reduces estrogen levels in the body, slowing growth of estrogen-dependent breast tumors

  Key Ingredients

  The active ingredient in Aromasin is exemestane. The inactive ingredients include:

  • Mannitol
  • Crospovidone
  • Polysorbate 80
  • Hypromellose
  • Colloidal silicon dioxide
  • Microcrystalline cellulose
  • Sodium starch glycolate
  • Magnesium stearate
  • Simethicone
  • Polyethylene glycol 6000
  • Sucrose
  • Magnesium carbonate
  • Titanium dioxide
  • Methylparaben
  • Polyvinyl alcohol

  Mechanism of Action of Aromasin (exemestane)

  Aromasin (exemestane) functions primarily as an irreversible steroidal aromatase inhibitor. Its mechanism of action involves the following key processes:

  Aromatase Inhibition

  • Aromatase Enzyme Role: Aromatase is the principal enzyme responsible for converting androgens (such as testosterone and androstenedione) into estrogens (like estrone and estradiol) in postmenopausal women. This conversion occurs mainly in peripheral tissues, as ovarian estrogen production significantly decreases after menopause.
  • Irreversible Binding: Exemestane acts as a false substrate for the aromatase enzyme. It is processed into an intermediate form that binds irreversibly to the active site of the aromatase enzyme, leading to its inactivation. This process is known as “suicide inhibition,” effectively reducing the enzyme’s ability to produce estrogen.

  Reduction of Estrogen Levels

  • Impact on Estrogen Production: By inhibiting aromatase, exemestane significantly lowers circulating estrogen levels in the body, achieving a reduction of approximately 85% to 95%. This decrease in estrogen is crucial because many breast cancers are estrogen-dependent, meaning their growth is fueled by this hormone.

  Selective Action

  • Specificity: Exemestane selectively inhibits aromatase without affecting other enzymes involved in steroidogenesis, ensuring that it primarily targets estrogen production without disrupting the synthesis of other hormones such as corticosteroids or aldosterone.

  Clinical Relevance

  • Treatment of Breast Cancer: The reduction of estrogen levels helps slow down the growth of estrogen-dependent breast tumors, making exemestane an effective treatment option for postmenopausal women with hormone-receptor-positive breast cancer, both in early and advanced stages.

  Chemical structure of exemestaneExemestane is chemically described as 6-methylenandrosta-1,4-diene-3,17-dione. Its molecular formula is C20H24O2 and its structural formula is shown in the image.The active ingredient is a white to slightly yellow crystalline powder with a molecular weight of 296.41. Exemestane is freely soluble in N, N-dimethylformamide, soluble in methanol, and practically insoluble in water.                                                                                                                                 

  Common Uses of Aromasin

  • Early Breast Cancer: Aromasin is used as an adjuvant treatment for postmenopausal women who have hormone-receptor-positive early breast cancer. This means the cancer is localized and has not spread beyond the breast or nearby lymph nodes. It is typically prescribed after a course of tamoxifen therapy to lower the risk of cancer recurrence.
  • Advanced Breast Cancer: Aromasin is also indicated for the treatment of advanced breast cancer in postmenopausal women. This applies to cases where the cancer has spread beyond the breast and lymph nodes, especially in situations where previous treatments, such as tamoxifen, have failed or the cancer has progressed.
  • Hormone Receptor-Positive Breast Cancer: Aromasin is specifically effective for cancers that are estrogen-receptor positive (ER+), meaning they grow in response to estrogen. By lowering estrogen levels in the body, Aromasin helps slow or reverse the growth of these tumors.
  • Switch Therapy: It is often used as a switch therapy after initial treatment with tamoxifen, allowing for continued hormone therapy to maximize treatment efficacy over a total of five years.

  Key Precautions for Aromasin (exemestane)

  • Allergic Reactions: Patients with known hypersensitivity to exemestane or any of its ingredients should avoid using Aromasin.
  • Pregnancy and Breastfeeding: Aromasin is contraindicated during pregnancy due to potential fetal harm. It is also not recommended for breastfeeding mothers; women should avoid breastfeeding during treatment and for one month after the last dose.
  • Menstrual Status: Aromasin is approved only for postmenopausal women. Those who are still menstruating should consult their doctor for alternative treatments.
  • Bone Health: Long-term use of Aromasin may lead to decreased bone mineral density, increasing the risk of osteoporosis and fractures. Regular monitoring of bone health and vitamin D levels is advised.
  • Liver and Kidney Function: Patients with liver issues (like hepatitis or cirrhosis) or kidney problems should inform their doctor, as these conditions may affect the drug’s metabolism and increase its levels in the body.
  • Cardiovascular Health: Aromasin may increase the risk of ischemic cardiovascular diseases. Patients with a history of heart disease or high cholesterol should be closely monitored.
  • Interactions with Other Medications: Inform your doctor of all medications being taken, including non-prescription and herbal products, as interactions may occur.
  • Driving and Operating Machinery: Aromasin can cause dizziness or fatigue. Patients are advised not to drive or operate heavy machinery until they know how the medication affects them.

  Dietary Restrictions

  • Alcohol Consumption: Patients should limit alcohol intake, as it may exacerbate dizziness caused by Aromasin.
  • Dietary Supplements: Discuss any dietary supplements, especially those that may affect bone health (like calcium and vitamin D), with a healthcare provider to ensure they do not interfere with treatment.
  • Food Intake: Aromasin should be taken with food, preferably after a meal, to enhance absorption and reduce gastrointestinal side effects.

  Foods to Consider Limiting or Avoiding

  • Alcohol: Limit alcohol consumption, as it can exacerbate dizziness and fatigue, common side effects of Aromasin. Alcohol may also impact overall health, particularly if there are concerns about cardiovascular health.
  • High-Fat Foods: Foods high in saturated fats may contribute to increased cholesterol levels. Since Aromasin can affect lipid profiles, it’s advisable to consume these foods in moderation.
  • Caffeine: Excessive caffeine may worsen side effects like anxiety or insomnia. Moderating caffeine intake can help manage these symptoms.
  • Spicy Foods: If experiencing gastrointestinal discomfort, such as nausea or indigestion, it may be beneficial to limit spicy foods that can irritate the stomach.

  General Dietary Recommendations

  • Balanced Diet: Focus on a well-balanced diet rich in fruits, vegetables, whole grains, and lean proteins to support overall health and mitigate side effects.
  • Hydration: Staying well-hydrated can help alleviate some side effects, including nausea.
  • Bone Health: Since Aromasin may lead to decreased bone density, consider foods rich in calcium and vitamin D, such as dairy products, leafy greens, and fortified foods, to support bone health.

  Aromasin (exemestane) can interact with several medications, which may affect how well it works or increase the risk of side effects. Here are some key interactions to be aware of:

  Medications That Contain Estrogen

  Aromasin should not be taken with medications that contain estrogen, as they can interfere with the effectiveness of Aromasin. Examples include:

  • Hormone replacement therapy
  • Birth control pills or patches
  • Estradiol (Climara, Estrace, Femring, Minivelle)
  • Ethinyl estradiol and drospirenone birth control (Yaz, Nikki, Ocella)
  • Ethinyl estradiol and norethindrone (Ortho-Novum 7/7/7, Lo Loestrin Fe)

  CYP 3A4 Inducers

  Medications that induce the CYP 3A4 enzyme, such as rifampicin, phenytoin, carbamazepine, phenobarbital, or St. John’s wort, may significantly decrease exemestane exposure. Dose modification may be required if a strong CYP 3A4 inducer is co-administered.

  Other Interactions

  Aromasin may also interact with:

  • Tamoxifen – if switching from tamoxifen to Aromasin, the warfarin dose may need adjustment
  • Certain supplements – discuss with your doctor before taking any vitamins, herbs or supplements while on Aromasin

  Use During Pregnancy

  • Contraindicated: Aromasin is contraindicated during pregnancy. Animal studies have shown that the drug can cause fetal harm, including embryotoxic and abortifacient effects. It is advised that women of reproductive potential use effective contraception during treatment and for at least one month after the last dose.
  • Pregnancy Testing: Women who are able to become pregnant should undergo a pregnancy test within seven days prior to starting Aromasin to ensure they are not pregnant before treatment begins.

  Use During Breastfeeding

  • Not Recommended: Breastfeeding is not recommended while taking Aromasin and for at least one month after the last dose. Although it is not known if Aromasin passes into breast milk, there is a potential risk to breastfeeding infants.
  • Consult Healthcare Provider: Women who are breastfeeding or planning to breastfeed should consult their healthcare provider for advice and alternative options.

  Risks of Aromasin During Pregnancy

  • Fetal Harm: Based on animal studies and its mechanism of action, Aromasin can cause fetal harm when administered to a pregnant woman. Animal studies have revealed exemestane to be embryotoxic, fetotoxic, and abortifacient.
  • Pregnancy Loss: If Aromasin is used during pregnancy, or if the patient becomes pregnant while taking Aromasin, there is a potential risk for pregnancy loss.
  • Contraindicated or Not Recommended: Some authorities consider Aromasin contraindicated during pregnancy, while others simply state it is not recommended.
  • Effective Contraception: Women of reproductive potential should be advised to use effective contraception during Aromasin therapy and for at least 1 month after the last dose.
  • Pregnancy Testing: Pregnancy testing is recommended for females of reproductive potential within seven days prior to initiating Aromasin treatment to confirm the patient is not pregnant before starting the medication.

  Dosage of Aromasin (exemestane)

  • Recommended Dose: The standard dosage of Aromasin is 25 mg taken once daily after a meal.
  • Duration of Treatment: Patients may need to continue taking Aromasin for up to 5 years, especially in the context of adjuvant therapy following tamoxifen treatment.

  Storage of Aromasin

  • Temperature: Store Aromasin tablets at room temperature (approximately 77°F or 25°C).
  • Container: Keep the medication in its original container, tightly sealed to protect it from moisture and heat.
  • Child Safety: Ensure that Aromasin is kept out of the reach of children.
  • Expiration: Check the expiration date provided by the pharmacist, which is typically 1 year from the date of dispensing.

  Reviews and General Feedback

  While specific reviews from patients are not provided in the search results, Aromasin is generally regarded as an effective treatment for hormone-receptor-positive breast cancer in postmenopausal women. Patients often report:

  • Efficacy: Many users find Aromasin effective in reducing estrogen levels and slowing the progression of breast cancer.
  • Side Effects: Common side effects may include hot flashes, fatigue, joint pain, and decreased bone density, which some patients find challenging to manage.
  • Overall Satisfaction: Overall, the satisfaction with Aromasin varies among individuals, often depending on how well they tolerate the side effects versus the benefits of treatment.