Anastrozole

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Adverse-effects 5 Drug-interactions 6 Mechanism-of-action 7 More General Terms 8 Additional Terms 9 Internet Database 10 References

Introduction

• Tradename: Arimidex.

Indications

• treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy
• patients with estrogen receptor-negative breast cancer & patients who did not respond initially to tamoxifen rarely respond to anastrozole
• approved for 1st line therapy (alternative to tamoxifen)

• may be more effective than tamoxifen for treatment of early breast cancer [5,8] Warnings:

• use with caution in patients with hyperlipidemia

Dosage

• 1 mg PO QD

• Tabs: 1 mg.

Adverse-effects

• common (> 5%)

• flushing & hot flashes
• little to mild nausea (10%)
• vomiting
• increased bone & tumor pain

• less common (2-5%)

• hypertension, somnolence, confusion, insomnia, anxiety, nervousness, fever, malaise, hair thinning, pruritis, breast pain, weight loss, urinary tract infection, thrombophlebitis, myalgia, arthralgia, pathological fracture, neck pain, sinusitis, bronchitis, rhinitis, flu-like syndrome, infection

• other: weight gain
• does not cause osteoporosis [9]
  

• drug adverse effects of aromatase inhibitors

Drug-interactions

• inhibits activity of cytochromes P-450 1A2, 2C8/9, 3A4 at high concentrations
• it is unlikely to cause clinically significant effects on cyt P-450 mediated drug metabolism

Mechanism-of-action

• aromatase inhibitor
• suppresses estrogen synthesis

More General Terms

• aromatase inhibitor
• antineoplastic agent (chemotherapeutic agent)

Additional Terms

• breast cancer
• cytochrome P450 19A1 (aromatase, estrogen synthetase, CYP19A1)

Internet Database

PubChem: 2187

References

1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
2. The Prescriber's Letter, vol 6 #11, Nov 1999
3. The Prescriber's Letter, vol 7 #10, Oct 2000, pg 57
4. The Prescriber's Letter, vol 8 #2, Feb 2001, pg 10
5. The Prescriber's Letter, vol 9 #2, Feb 2002, pg 10
6. Journal Watch 22(17):136, 2002 The ATAC Trialists' Group, Lancet 359:2131, 2002 [1]
7. Prescriber's Letter 12(1): 2005 Arimidex (Anastrozole) for Early Breast Cancer; an Update Detail-Document#: [2] (subscription needed) [3]
8. Boccardo F, Rubagotti A, Puntoni M, Guglielmini P, Amoroso D, Fini A, Paladini G, Mesiti M, Romeo D, Rinaldini M, Scali S, Porpiglia M, Benedetto C, Restuccia N, Buzzi F, Franchi R, Massidda B, Distante V, Amadori D, Sismondi P. Switching to anastrozole versus continued tamoxifen treatment of early breast cancer: preliminary results of the Italian Tamoxifen Anastrozole Trial. J Clin Oncol. 2005 Aug 1;23(22):5138-47. Epub 2005 Jul 11. PMID: [4]
9. Eastell R et al, Effect of anastrozole on bone mineral density: 5-year results from the Anastrazole, Tamoxifen, Alone or in Combination trial 18233230. J Clin Oncol 2008, 26:1051 PMID: [5]

anastrozole (Arimidex)