Fulvestrant
Indications
Fulvestrant is used for:
Metastatic breast cancer, in postmenopausal women w/ oestrogen-receptor positive tumours.
Adult Dose
Intramuscular
Metastatic breast cancer in postmenopausal women with oestrogen-receptor positive tumours
Adult: 500 mg (250 mg into each buttock) on days 1, 15, and 29, then once monthly thereafter.
Moderate (Child-Pugh Class B): 250 mg (into 1 buttock) on days 1, 15, and 29, then once monthly thereafter.
Severe: Contraindicated.
Child Dose
Renal Dose
Renal impairment
Negligible amounts of fulvestrant are eliminated in urine
In clinical trials, fulvestrant concentrations in women with eCrCl ?30 mL/min were similar to women with normal creatinine
Administration
Contra Indications
Pregnancy and lactation.
Precautions
Patient w/ bleeding diatheses, thrombocytopenia. Admin at dorsogluteal inj site. Mild to moderate hepatic and severe renal (CrCl <30 mL/min) impairment.
Pregnancy-Lactation
Interactions
Increased risk of bleeding when taken concomitantly w/ anticoagulants.
Adverse Effects
Side effects of Fulvestrant :
>10%
Nausea (26%)
Asthenia (23%)
Pain (19%)
Vasodilatation (18%)
Pharyngitis (16%)
HA (15%)
Back pain (14%)
Constipation (13%)
Vomiting (13%)
Abd pain (12%)
Diarrhea (12%)
Inj site pain (11%)
1-10%
Cough (10%)
Anorexia (9%)
Peripheral edema (9%)
Chest pain (7%)
Flu-like syndrome (7%)
Rash (7%)
Depression (6%)
Fever (6%)
UTI (6%)
Anemia (5%)
<1%
Angioedema
Leukopenia
Myalgia
Thrombosis
Osteoporosis
Mechanism of Action
Fulvestrant competitively binds to oestrogen receptors, forming a nuclear complex, leading to down-regulation of oestrogen receptor protein levels and inhibition of tumour growth.