Exemestane 250 Manufacturer: Hilma Biocare Pack: 30 tabs/pack ( 25 mg/tab ) Drug class: Aromatase Inhibitor Common names: Aromadex, Aromasin, Aromasine, Aromaxyl, Exemestane, Examestane Chemical structure: 6-methyleneandrosta-1,4-diene-3,17-dione DESCRIPTION Exemestane is a synthetic androgen analogue. It is a steroidal inhibitor of aromatase which binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgen precursors into estrogens. Exemestane has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury. This medication is used to treat certain types of breast cancer (such as hormone-receptor-positive breast cancer) in women after menopause. Exemestane is also used to help prevent the cancer from returning. Some breast cancers are made to grow faster by a natural hormone called estrogen. Exemestane decreases the amount of estrogen the body makes and helps to slow or reverse the growth of these breast cancers. Exemestane is usually not used in women of childbearing age. Exemestane is usually taken once a day after a meal. Take Exemestane at around the same time every day. You may need to take Exemestane for several years or longer. Continue to take Exemestane even if you feel well. Do not stop taking Exemestane without talking to your doctor. PHARMACODYNAMICS Effect On Estrogens Plasma estrogen (estradiol, estrone, and estrone sulfate) suppression is seen starting at a 5-mg daily dose of Exemestane, with a maximum suppression of at least 85% to 95% achieved at a 25-mg dose. Exemestane 25 mg daily reduces whole body aromatization (as measured by injecting radiolabeled androstenedione) by 98% in postmenopausal women with breast cancer. After a single dose of Exemestane 25 mg, the maximal suppression of circulating estrogens occurred 2 to 3 days after dosing and persisted for 4 to 5 days. Effect On Corticosteroids In multiple-dose trials of doses up to 200 mg daily, Exemestane selectivity was assessed by examining its effect on adrenal steroids. Exemestane did not affect cortisol or aldosterone secretion at baseline or in response to ACTH at any dose. Thus, no glucocorticoid or mineralocorticoid replacement therapy is necessary with Exemestane treatment. Other Endocrine Effects Exemestane does not bind significantly to steroidal receptors, except for a slight affinity for the androgen receptor (0.28% relative to dihydrotestosterone). The binding affinity of its 17dihydrometabolite for the androgen receptor, however, is 100 times that of the parent compound. Daily doses of Exemestane up to 25 mg had no significant effect on circulating levels of androstenedione, dehydroepiandrosterone sulfate, or 17- hydroxyprogesterone, and were associated with small decreases in circulating levels of testosterone. Increases in testosterone and androstenedione levels have been observed at daily doses of 200 mg or more. A dose-dependent decrease in sex hormone binding globulin (SHBG) has been observed with daily Exemestane doses of 2.5 mg or higher. Slight, non dose-dependent increases in serum luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels have been observed even at low doses as a consequence of feedback at the pituitary level. Exemestane 25 mg daily had no significant effect on thyroid function [free triiodothyronine (FT3), free thyroxine (FT4), and thyroid stimulating hormone (TSH). Absorption Exemestane is distributed extensively into tissues. Exemestane is 90% bound to plasma proteins and the fraction bound is independent of the total concentration. Albumin and a11-acid glycoprotein both contribute to the binding. The distribution of Exemestane and its metabolites into blood cells is negligible. Metabolism Exemestane is extensively metabolized. The initial steps in the metabolism of Exemestane are oxidation of the methylene group in position 6 and reduction of the 17-keto group with subsequent formation of many secondary metabolites. Each metabolite accounts only for a limited amount of drug-related material The metabolites are inactive or inhibit aromatase with decreased potency compared with the parent drug, One metabolite may have androgenic activity [see Pharmacodynamics]. Studies using human liver preparations indicate that cytochrome P 450 3A4 (CYP 3A4) is the principal isoenzyme involved in the oxidation of Exemestane. Exemestane is metabolized also by aldo keto reductases. CONTRAINDICATIONS EXEMESTANE 250 Exemestane is contraindicated in patients with a known hypersensitivity to the drug or to any of the excipients. PRECAUTIONS Reductions in bone mineral density (BMD) over time are seen with Exemestane 250 use. Concomitant use of bisphosphonates, vitamin D supplementation, and calcium was not allowed. It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood tests may be needed to check for unwanted effects. It is important for women to have regular gynecology check-ups while taking this medicine. It is unlikely that a postmenopausal woman may become pregnant. But, you should know that using this medicine while you are pregnant could harm your unborn baby. If you are a woman who can bear children, your doctor may give you a pregnancy test 7 days before you start using this medicine to make sure you are not pregnant. Use an effective form of birth control during treatment and for 1 month after the last dose f you think you have become pregnant while using this medicine, call your doctor right away. This medicine may decrease bone mineral density when used for a long time. A low bone mineral density can cause weak bones or osteoporosis. If you have any questions about this, talk to your doctor. Do not take this medicine if you are also using medicines that contain estrogen, birth control pills or patches, or other medicines used for hormone replacement therapy. Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter) medicines and herbal (eg, St. John’s wort) or vitamin supplements. ADVERSE REACTIONS EXEMESTANE 250 Most people using this medication do not have serious side effects. Typically observed side effects in some cases are: hot flashes, hair loss, joint/bone/muscle pain, tiredness, unusual sweating, nausea, diarrhea, dizziness, and trouble sleeping may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly. Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Tell your doctor right away if you have any serious side effects, including: bone fractures, mental/mood changes (such as depression, anxiety), vaginal bleeding. persistent nausea/vomiting, unusual tiredness, dark urine, yellowing eyes/skin. DRUG INTERACTION Exemestane does not inhibit any of the major CYP isoenzymes, including CYP 1A2, 2C9, 2D6, 2E1, and 3A4. In a clinical pharmacokinetic study, coadministration of ketoconazole, a potent inhibitor of CYP 3A4, has no significant effect on Exemestane pharmacokinetics. Although no other formal drug-drug interaction studies with inhibitors have been conducted, significant effects on Exemestane clearance by CYP isoenzyme inhibitors appear unlikely. Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines. Be careful using Exemestane together with Carbamazepine, Enzalutamide, Fosphenytoin, Mitotane, Phenytoin, Primidone, Rifabutin, St John’s Wort. DOSE RANGE AND DURATION OF USE EXEMESTANE 250 It is recommended to take Exemestan during meals or after meal. Common cycle length is 2-4 weeks (some getting only two to three doses per week) Beginners: 12.5mg / EOD (every other day) Hobby: 12.5 mg / ED (every day) Professional Range: 25 mg / ED (every day) Women: 12.5mg / ED or EOD Half-life: 25-27 hours (active life about 130 hours) Detection time: 2-3 weeks SIDE EFFECTS FROM EXEMESTANE 250 Weakness or Fatigue Headaches Hot Flashes High Blood Pressure Joint Pain Depression (rare) Nausea and/or Vomiting (rare) AFTER CYCLE THERAPY Exemestane can be part of your cycle. (Exemestane during steroid cycle prevents the side effects that steroids can cause – flavoring). Also Exemestane can be used as Post Cycle Therapy. STORAGE To be store in a dry place, protected from light, at a temperature of 15-25 ° C. Keep out of reach of children. MIX/COMBINE YOUR STEROIDS CYCLE Exemestan use is not limited to PCT only, it also can be a part of your steroid cycle. It outperform Arimidex with about 12 % when it comes to estrogen inhibition. And it will even cause an increase of testosterone level as well. But Exemestan is a steroidal drug, which mean it carry on androgenic effects too. That’s why the best will be to let ti for PCT time, when this trait would be even beneficial. More you can find on our website: hilmabioshop.com/shop
Q & A
Ask a question
There are no questions yet
