Docetaxel

From Anvita Health Wiki

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

Introduction

• Tradename: Taxotere.

Indications

• locally advanced or metastatic breast cancer with progression or relapse after anthracycline therapy
• ovarian cancer

Contraindications

• Caution:
• severe hypersensitivity in 25% of patients not receiving premedication docetaxel administration
  

• pregnancy category = d

Dosage

• premedication with dexamethasone 16 mg PO QD for 3 days starting 1 day prior to administration of docetaxel

• Injection: 40 mg/mL (0.5 mL, 2 mL)

Pharmacokinetics

• extensive extravascular distribution
• protein binding 94%, largely albumin, alpha-1 acid glycoprotein & lipoproteins
• metabolism by cyt P450 3A
• triphasic elimination: 1/2lives 4 min, 36 min & 11 hours
  

• elimination via liver
• 1/2life = 11 hours terminal-phase

Adverse-effects

• common (> 10%)

• fever, alopecia (nearly all patients), nausea/vomiting, diarrhea, stomatitis, neutropenia (dose-limiting), leukopenia, thrombocytopenia, anemia, myalgia

• not common (1-10%)

• fluid retention syndrome:

• pleural effusion, edema, ascites
• incidence & severity increase markedly at cumulative doses of > 400 mg/m2

• dyspnea at rest
• cardiac tamponade (due to ascites)

• uncommon (< 1%)

• hypersensitivity reactions

Drug-interactions

• possibly increased toxicity with:

• ketoconazole
• erythromycin
• terfenadine
• astemizole
• cisapride
• cyclosporine

More General Terms

• taxane
• antineoplastic agent (chemotherapeutic agent)

Internet Database

PubChem: 148123
PubChem: 64780
PubChem: 148124
PubChem: 657391
PubChem: 3143
PubChem: 363540

References

1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
2. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529

docetaxel (Taxotere)