Letrozole

Indications
Oral
Advanced or locally advanced breast cancer, Adjuvant therapy for postmenopausal women with hormone receptor positive early breast cancer
Adult: 2.5 mg once daily.
Hepatic impairment: Reduce dose by 50% in patients with cirrhosis and severe hepatic impairment; recommended dose: 2.5 mg on alternate days.

Special Populations: In renal failure: No dosage adjustment is required in patients with CrCl of at least 10 mL/min. In hepatic failure: No dosage adjustment is required in patients with mild to moderate hepatic impairment. Use with caution.
Contraindications
Premenopausal women and children; hypersensitivity.
Warnings / Precautions
Severe renal impairment; severe hepatic impairment; osteoporosis. Caution when driving or operating machinery.
Adverse Reactions
Hot flushes, arthralgia, nausea, vomiting, fatigue, dizziness, headache, dyspepsia, constipation, diarrhoea, anorexia, alopoecia, increased sweating, rash, peripheral oedema, osteoporosis, musculoskeletal pain, vaginal irritation.
Potentially Fatal: Thromboembolic events.
Drug Interactions
Plasma levels reduced by tamoxifen.
See Below for More letrozole Drug Interactions
Mechanism of Actions
Letrozole competitively binds to the heme group of aromatase, a cytochrome P450 enzyme which catalyzes conversion of androgen to oestrogen, leading to inhibition of the enzyme and a significant reduction in plasma oestrogen levels.
Absorption: Rapidly and completely absorbed from the GI tract.
Distribution: Weakly bound to plasma proteins and has a large volume of distribution of about 1.9 l/kg.
Metabolism: Slow hepatic metabolism to inactive metabolites.
Excretion: Via urine (6% as unchanged drug); elimination half life of about 2 days.
Administration
May be taken with or without food.
ATC Classification
L02BG04 - letrozole ; Belongs to the class of enzyme inhibitors. Used in endocrine therapy.
Available As
  • Letrozole 2.5 mg
  • Letrozole 5 mg
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