Process and rules for using Letrozole
Letrozole is a drug that has gained popularity because of its more effective analogue for lowering estrogen levels in the blood. These aromatase inhibitors are also not steroids. Many athletes involved in strength training and bodybuilding prefer to buy Letrozole in Ukraine, but this medicine is recommended for both men and women. Initially, this tool was developed to fight cancer and gynecomastia in women.
Inhibition of letrozole aromatase is due to competitive interactions during cytochrome P450 binding.
What drugs are useful for women?
The amount of estrone and estradiol is reduced by 75% and 78% with the use of 0.1 mg, 0.5 mg or 2.5 mg of the active substance in the body of a healthy woman in the bloodstream. The amount of hormone is gradually reduced, reaching a minimum after 2-3 days.
The body of women with the usual form of postmenopausal breast cancer who used 0.1-5 mg of the drug per day, showed a 75-95% reduction in estrogen concentration compared to their initial values. Concomitant use of more than 0.5 mg of the drug often reduces estradiol and estrone levels beyond the sensitivity of the assay.
Indicators of adrenal steroid hormone synthesis remain unchanged and suppression of estrogen secretion is observed throughout the treatment period.
Letrozole is characterized by high absorption of the drug from the gastrointestinal tract and bioavailability up to 100% (99.9). If the drug is taken before or after a meal, the maximum concentration of the active substance in the blood is observed 1 hour after ingestion. Taking food increases the time to reach the maximum concentration up to 2 hours.
These changes do not affect the therapeutic efficacy of the medicine, so you can take the medicine no matter what the meal time.
More than 80% of ingested substances are excreted unchanged through the urinary system and intestines. Several components undergo biotransformation in the liver including the cytochrome P450 isoenzyme. This phenomenon leads to the formation of an inactive metabolite of carbinol.
The plasma concentration of the drug is gradually increased with regular daily use of the drug. And letrozole reaches steady-state concentrations (7 times higher than a single dose) within 15 to 45 days of starting treatment. It is observed to maintain a single level of concentration in steady state during long-term treatment.
The recommended dose of Letrozole-Teva for adults is 2.5 mg once daily. Treatment should be continued for 5 years (5 years or less) with prolonged adjuvant therapy.
Letrozole-Teva should be discontinued at any sign of disease progression.
Elderly patients do not need dose adjustment of this drug.
No dose adjustment is required for liver or kidney damage (CC ≥ 10 ml / min). However, patients with severe hepatic impairment (Child-Pugh class C) should be closely monitored.