Important Safety Information
Letrozole is contraindicated in women who are or may become pregnant, as it can cause fetal harm. It is also contraindicated in patients with known hypersensitivity to letrozole or any excipients.
Letrozole may cause decreases in bone mineral density (BMD). Consideration should be given to monitoring BMD. In the adjuvant setting, the incidence of bone fractures at any time after randomization was 14.7% for letrozole and 11.4% for tamoxifen at a median follow-up of 96 months.
Important
Non-Medical Use
Non-medical use of letrozole falls outside approved indications. Letrozole is the most potent aromatase inhibitor available, and its use carries substantial risk of estrogen over-suppression. Product purity does not establish that non-medical use is safe or appropriate for an individual.
Potential Adverse Effects
Common adverse reactions reported in clinical trials include bone mineral density decreases, hot flashes, arthralgia, fatigue, hypercholesterolemia, and increased sweating. In the extended adjuvant setting, patients receiving letrozole had a median decrease from baseline of 3.8% in hip BMD compared to 2.0% in the placebo group.
In non-medical contexts, crashed estrogen from letrozole over-dosing presents as joint pain and crunching knees within 10–14 days, libido crash and erectile dysfunction, low mood and anhedonia, and serum estradiol under 15 pg/mL. These symptoms indicate that the dose is too high and require immediate correction.
Conditions Requiring Medical Evaluation
Letrozole is not appropriate for everyone. Contraindications include pregnancy and hypersensitivity to the drug. Caution is advised in patients with pre-existing osteoporosis, high cholesterol, or hepatic impairment.
In patients with cirrhosis and severe hepatic dysfunction, the dose should be reduced by 50%. No dosage adjustment is required for patients with renal impairment if creatinine clearance is greater than or equal to 10 mL/min.
Monitoring During Therapy
Medically supervised letrozole therapy may involve monitoring of bone mineral density, serum cholesterol, and liver function. In clinical settings, the BMD substudy demonstrated the need for bone density monitoring in patients receiving letrozole.
In non-medical contexts, experienced users recommend baseline and periodic bloodwork including sensitive estradiol (LC-MS/MS), total testosterone, free testosterone, SHBG, full lipid panel, and liver function tests to guide dosing and detect complications.
Product Care
Storage & Handling
Store tablets in a cool, dry place in the original packaging. Keep out of reach of children. Inspect tablets before use and do not use if they appear damaged or compromised.
Further Safety Information