fulvestrant

(redirected from ICI 182,780)

fulvestrant

Faslodex

Pharmacologic class: Estrogen receptor antagonist

Therapeutic class: Antineoplastic

Pregnancy risk category D

Action

Inhibits cell division by binding with and downgrading estrogen receptor protein in breast cancer cells

Availability

Prefilled syringes: 125 mg/2.5 ml, 250 mg/5 ml

Indications and dosages

Hormone receptor-positive advanced metastatic breast cancer in postmenopausal women with disease progression who have received antiestrogen therapy

Adults: 250 mg I.M. q month as a single 5-ml injection or two concomitant 2.5-ml injections

Contraindications

• Hypersensitivity to drug

• Pregnancy

Precautions

Use cautiously in:

• bleeding disorders, hepatic dysfunction, thrombocytopenia

• breastfeeding patients.

Administration

• Expel air bubble from syringe before giving injection.

• Administer I.M. injection slowly.

Adverse reactions

CNS: depression, light-headedness, dizziness, headache, hallucinations, vertigo, insomnia, paresthesia, anxiety, weakness

CV: chest pain, vasodilation, peripheral edema

EENT: pharyngitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, anorexia

GU: urinary tract infection, pelvic pain

Hematologic: anemia

Musculoskeletal: back pain, bone pain, arthritis

Respiratory: dyspnea, increased cough

Skin: flushing, rash, diaphoresis

Other: food distaste, fever, hot flashes, injection site reactions, pain, flulike symptoms

Interactions

Drug-drug. Anticoagulants: increased bleeding risk

Patient monitoring

• Monitor CBC.

• Assess liver function test results.

Patient teaching

• Advise patient to report signs and symptoms of infection, especially urinary tract infection.

• Caution patient to avoid driving and other hazardous activities until she knows how drug affects concentration and alertness.

Tell patient to notify prescriber immediately if she thinks she is pregnant.

• Teach patient comfort measures to minimize hot flashes and rash.

• Instruct patient to minimize GI upset and sore throat by eating frequent, small servings of healthy food and drinking adequate fluids.

• Tell patient that drug may cause headache, muscle aches, or bone pain. Encourage her to discuss activity recommendations and pain management with prescriber.

• Advise patient to establish effective bedtime routine to minimize sleep disorders.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs mentioned above.

fulvestrant

(ful-vess-trant) ,

Faslodex

(trade name)

Classification

Therapeutic: antineoplastics
Pharmacologic: estrogen receptor antagonists
Pregnancy Category: D

Indications

Treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with progressive disease that has not responded to antiestrogen therapy.

Action

Competitively binds to estrogen receptors. Binding results in down-regulation of estrogen receptor protein in cancerous breast tissue.

Therapeutic effects

Decreased progression of hormone receptor-positive breast cancer.

Pharmacokinetics

Absorption: Well absorbed following IM administration.
Distribution: Rapidly and extensively distributed.
Protein Binding: 99%.
Metabolism and Excretion: Mostly metabolized by the liver; negligible renal elimination.
Half-life: 40 days.

Time/action profile (effect on estrogen receptors)

ROUTEONSETPEAKDURATION
IMrapid7 days30 days

Contraindications/Precautions

Contraindicated in: Obstetric / Lactation: Pregnancy or lactation; Pediatric: Children; Hypersensitivity; Bleeding disorders, thrombocytopenia, concurrent anticoagulant therapy.
Use Cautiously in: Moderate to severe hepatic impairment.

Adverse Reactions/Side Effects

Central nervous system

  • headache (most frequent)
  • weakness (most frequent)
  • anxiety
  • depression
  • dizziness
  • insomnia

Ear, Eye, Nose, Throat

  • pharyngitis (most frequent)

Respiratory

  • cough (most frequent)
  • dyspnea (most frequent)

Cardiovascular

  • vasodilation (hot flushes) (most frequent)
  • chest pain
  • edema

Gastrointestinal

  • abdominal pain (most frequent)
  • constipation (most frequent)
  • diarrhea (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)
  • anorexia

Genitourinary

  • pelvic pain
  • urinary tract infection

Dermatologic

  • rash
  • sweating

Local

  • pain/inflammation at injection site (most frequent)

Hematologic

  • anemia

Musculoskeletal

  • back pain (most frequent)
  • bone pain (most frequent)
  • arthritis

Neurologic

  • paresthesia

Miscellaneous

  • fever
  • flu syndrome

Interactions

Drug-Drug interaction

None known.

Route/Dosage

Intramuscular (Adults) 500 mg on days 1, 15, and 29, and then once monthly (given as two injections of 250 mg (5 mL) each).

Hepatic Impairment

Intramuscular (Adults) Moderate hepatic impairment—250 mg on days 1, 15, and 29, and then once monthly (given as a single injection).

Availability

Solution for injection: 50 mg/mL in 5–ml prefilled syringes

Nursing implications

Nursing assessment

  • Assess patient for pain and other side effects periodically throughout therapy.

Potential Nursing Diagnoses

Acute pain (Adverse Reactions)
Deficient knowledge, related to medication regimen (Patient/Family Teaching)

Implementation

  • A negative pregnancy test should be determined prior to initiation of treatment.
  • Intramuscular: Follow proper technique for injection using the manufacturer's instructions for the use of the SAFETYGLIDE syringe and needle. Inject slowly over 1–2 min into the gluteus muscle as two 5–mL injections, one in each buttock.

Patient/Family Teaching

  • Inform patient that fulvestrant may cause mild pain and inflammation at injection site.
  • Advise patient to use contraception during treatment with fulvestrant. May cause teratogenic effects and fetal death.
  • Inform patient of potential for adverse reactions and advise her to notify health care professional.
  • Advise patient to report an increase in pain so treatment with analgesics can be initiated.

Evaluation/Desired Outcomes

  • Slowing of disease progression in women with advanced breast cancer.
References in periodicals archive ?
To examine whether the enhancement of LTP by 100 nM BPA involves ERs, we add a high-affinity nonselective ER antagonist ICI 182,780 (100 nM) into bath solution 30 min before BPA application.
The mechanism of action of these hormones was examined using anti-estrogen ICI 182,780 (hereinafter ICI).
(Newport, RI); fulvestrant (ICI 182,780; ICI) and Gen from Sigma-Aldrich (St.
macrophylla were used with a pure and well-characterized antiestrogen ICI 182,780 in a cotreatment regimen in vitro on cells transiently transfected with the estrogen [alpha] or [beta] receptor expression plasmids and in vivo in ovariectomized rats.
DNA content and chromatin texture of human breast epithelial cells transformed with 17-[beta]-estradiol and the estrogen antagonist ICI 182,780 as assessed by image analysis.
Daidzein (minimum 98%), ICI 182,780, 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT), Ham's F12 medium, Dulbecco's modified Eagle's medium (DMEM), fetal calf serum and hCG were purchased from Sigma-Aldrich (St.
The essential oil strongly stimulated the proliferation of MCF-7 cells, and this effect was significantly inhibited by the specific estrogen receptor antagonist ICI 182,780.
The steroidal antiestrogen ICI 182,780 is an inhibitor of cellular aromatase activity.
ICI 182,780, an estrogen receptor (ER) antagonist, was co-treated with E2 or BPA or NP to BG-1 cells to identify the relevance of ER signaling in EMT and migration.
ICI 182,780 (ICI), an ER antagonist; 2,3-bis(4-hydroxyphenyl)-propionitrile (DPN) and 4,4',4"-(4-propyl-[1//]-pyrazole-1,3,5 -triyl^mphenol (PPT), synthetic ER agonists with affinity for human ER[alpha] and ER[beta], respectively; and 1,3-bi's(4-hydroxyphenyl)4-methyl-5 - [4-(2-piperidinylethoxy) phenol]-1//-pyrazole dihydrochloride (MPP) and 4-[2-phenyl-5,7-bi's(trifluoromethyl) pyrazolo[1,5-a ]pyrimidin-3-yl]phenol (PHTPP), antagonists for ER[alpha] and ER[beta], respectively, were obtained from Tocris Biosciences (Bristol, UK), with purity of > 99%, except for MPP (purity > 98%).
To investigate whether the observed the regulatory effect of puerarin on OPG, RANKL and IL-6 expression are mediated through an ER pathway, MG-63 cells were cultured in 1% sFBS for 3 days or 48 h in the presence of 0.1 [micro]M puerarin together with 100 [micro]M ICI 182,780 (the pure ER antagonist).