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Fulvestrant instruction manual
Common name: Fulvestrant
Trade name: Faslodex
All names: Faslodex, Fulvestrant, Fulvestrant, Fulvestrant, Fulzos
Indications:
For the treatment of estrogen receptor-positive locally advanced or metastatic breast cancer in postmenopausal (including natural menopause and artificial menopause) patients who relapse after or during adjuvant anti-estrogen therapy, or who progress during anti-estrogen therapy.
Usage and dosage:
Intramuscular injection once a month, 250mg each time, can be a single injection (1 time 5ml) or 2 injections (1 time 2.5ml), the injection should be slow.
Adverse reactions:
>10%:
Central nervous system: fatigue (8%-32%), headache (8%-15%)
Endocrine and metabolism: increased γ-glutamyl transferase (49%), decreased blood sugar (18%), hot flashes ( 7%-11%)
Gastrointestinal tract: nausea (10%-28%), diarrhea (6%-25%), abdominal pain (13%-16%), vomiting (6%-15%), stomatitis (10%-13%), decreased appetite (8%-13%), constipation (5%-12%)
Hematoma Tumors: anemia (4%-40%; grade 3: ≤2%), lymphopenia (35%; grade 3: 2%)
Liver: elevated serum aspartate aminotransferase (5%-48%), elevated serum alanine aminotransferase (5%-37%), elevated liver enzymes (>15%)
Infection: infection (25 %-31%)
Local reactions: injection site pain (12%)
Neuromuscular and skeletal: arthralgia (8%-17%)
Kidney: increased serum creatinine (≤74%)
Respiratory system: cough (5%-15%), dyspnea (4%-12%)
1% - 10%:
Cardiovascular: peripheral edema (7%)
Central nervous system: dizziness (6%-8%)
Dermatology: pruritus (6%-7%), rash (4%-7%), alopecia (2%-6%)
Endocrinology and metabolism: decreased serum albumin (8%), decreased serum phosphate Low (8%), weight loss (2%)
Gastrointestinal tract: anorexia (6%), anorexia (3%)
Hematology and neoplasms: leukopenia (≤5%; grade 3: 1%; grade 4: 1%), thrombocytopenia (3%; grade 4: <1%), neutropenia (2%; grade 3: 1%; grade 4 :<1%)
Neuromuscular and skeletal: bone pain (9%), back pain (8%-9%), myalgia (7%), limb pain (6%-7%), musculoskeletal pain (6%), fatigue (5%-6%)
Others: fever (5%-7%)
<1%:
Post-marketing or case reports : Hepatic failure, hepatitis, elevated serum bilirubin, vaginal bleeding, venous thromboembolism
Undefined frequency:
Central nervous system: neuralgia, peripheral neuropathy, sciatica
Contraindications:
Known hypersensitivity to fulvestrant or any component of the formulation.
Contraindicated for pregnant or lactating women.
Patients with severe liver damage.
Hypersensitivity: Anaphylaxis, including urticaria and angioedema, has been reported.
Injection site reactions: sciatica, neuralgia, neuropathic pain and peripheral neuropathy. Due to the proximity to the sciatic nerve, use caution if administering in the dorso-gluteal position.
Bleeding Disorders: Use with caution in patients with a history of bleeding disorders (including thrombocytopenia) or receiving anticoagulant therapy; intramuscular injection may cause bleeding or hematoma.
Hepatic Impairment: Patients with moderate impairment should have increased exposure and dose adjustment is recommended. Safety and effectiveness in serious injuries have not been established.
Benzyl alcohol and its derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) are associated with potentially fatal toxicity in neonates ("wheezing syndrome"); "wheezing syndrome" includes metabolic acidosis, respiratory distress, wheezing breathing, central nervous system dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular failure. Some data suggest that parabens displace bilirubin at protein binding sites; avoid or use with caution benzyl alcohol-containing dosage forms in neonates.
Fetal Toxicity: Based on results from animal reproduction studies and mechanism of action, fulvestrant may cause fetal harm during pregnancy.
Stored at 2-8℃ (in the refrigerator). Prefilled injections should be stored in their original packaging to protect them from light.
Mechanism of action:
Fulvestrant is a competitive estrogen receptor antagonist with an affinity similar to that of estradiol. Fulvestrant blocks the nutritional effects of estrogen without having any partial agonistic (estrogen-like) effects of its own. Its mechanism of action is related to down-regulation of estrogen receptor (ER) protein levels. In vitro studies have confirmed that fulvestrant is a reversible inhibitor of the growth of tamoxifen-resistant and estrogen-sensitive human breast cancer (MCF-7) cell lines. In in vitro tumor studies, fulvestrant can delay the engraftment of human breast cancer MCF-7 cell xenografts in nude mice. Fulvestrant inhibits the growth of implanted MCF-7 xenografts and tamoxifen-resistant breast tumor xenografts. Breast tumor xenografts that are resistant to fulvestrant may also be cross-resistant to tamoxifen.