Fezol 2.5 mg (Tablet)

Title

• Letrozole Tablet

Categories

• Medicine
• Hormonal Chemotherapy

Description

• Adjuvant treatment of postmenopausal women with hormone receptor positive early breast cancer.
• Effective in early breast cancer cases
• First-line treatment in postmenopausal women with hormone-dependent advanced breast cancer
• Treatment of advanced breast cancer in women with postmenopausal status
• Pre-operative therapy in postmenopausal women with localized hormone receptor positive breast cancer

Dosage

• 2.5 mg once daily for 5 years in adjutant and extended adjutant setting
• Continue treatment for metastatic disease until tumor progression
• No dose adjustment for elderly patients or those with hepatic and/or renal impairment
• Not applicable in children

Mechanism of Action

• Potent and highly specific nonsteroidal aromatase inhibitor
• Competitively binds to the haem of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis
• Exerts antitumor effect by depriving estrogen-dependent breast cancer cells of their growth stimulus
• Suppression of estrogen biosynthesis in peripheral and malignant tissues

Pharmacokinetics

• Rapid and complete absorption from the gastrointestinal tract
• Plasma protein binding of letrozole is approximately 60%
• Metabolic clearance to a pharmacologically inactive carbinol metabolite
• Terminal elimination half-life in plasma is about 2 days
• Steady-state levels reached within 2 to 6 weeks after daily administration of 2.5mg

Interaction

• No clinically significant drug reactions observed with cimetidine and warfarin
• Cimetidine is a known inhibitor of one of the cytochrome P450 isoenzymes capable of metabolizing letrozole in vitro

Contraindications

• Known or suspected hypersensitivity to letrozole or other aromatase inhibitors
• Contraindicated during pregnancy, lactation, and in pre-menopausal women
• Contraindicated in severe hepatic dysfunction

Side Effects

• Common: Hot flashes, hypercholesterolemia, fatigue, increased sweating, arthralgia, skin rash, headache, gastrointestinal disorders, osteoporosis, edema, depression, weight increase, and more
• Rare: Nervous disorders, carpal tunnel syndrome, impairment of sensation, eye disorders, skin disorders, weight decrease, urinary tract infection, cough, and more

Pregnancy & Lactation

• Teratogenicity and maternal toxicity observed in pregnant rats
• No adequate and well-controlled studies in pregnant women
• Not recommended for nursing women due to possible excretion in human milk

Precautions & Warnings

• No dosage adjustment in breast cancer patients with moderate hepatic dysfunction
• Caution recommended for Fezol elimination depending on intrinsic metabolic clearance
• Renal impairment did not affect plasma Fezol concentration at a dose of 2.5 mg or 5 mg
• Potential risks and benefits should be considered carefully before prescribing Fezol
• Fatigue and dizziness observed in some cases

Overdose Effects

• No clinical experience of overdosage
• No specific antidote to Fezol
• Dialysis may be helpful due to low protein-binding nature
• Emesis may be induced if the patient is alert
• Supportive care and frequent monitoring of vital signs recommended

Therapeutic Class

• Hormonal Chemotherapy

Storage Conditions

• Keep below 30°C temperature
• Protect from light & moisture
• Keep out of the reach of children

Related Brands

• Arofrez 2.5 mg (Tablet) - healthcare-pharmaceuticals-ltd
• Letrozol 2.5 mg (Tablet) - drug-international-ltd