C H A P T E R 1 4
Antineoplastic agents
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Adverse effects
Adverse effects frequently encountered with the use of
these drugs involve the effects that are seen when oes
trogen is blocked or inhibited. Menopause-associated
effects include hot flushes, vaginal spotting, vaginal
dryness, moodiness and depression. Other effects
include bone marrow suppression and GI toxicity,
including hepatic dysfunction. Hypercalcaemia is
also encountered as the calcium is pulled out of the
bones without oestrogen activity to promote calcium
deposition. Many of these drugs increase the risk for
cardiovascular disease because of their effects on the
body.
Clinically important drug–drug interactions
If hormones and hormone modulators are taken with
oral anticoagulants, there is often an increased risk of
bleeding. Care is also necessary when administering
these agents with any drugs that might increase serum
lipid levels.
TABLE 14.5
DRUGS IN FOCUS Hormones and hormone modulators (continued)
Drug name
Dosage/route
Usual indications
nilutamide (Anandron)
300 mg/day PO for 30 days, then
150 mg/day PO
With surgical castration for treatment of
metastatic prostate cancer
Actions:
antioestrogenic drug, inhibits androgen
uptake and binding on target cells
Special considerations:
may cause liver
toxicity, and liver function test results should
be monitored regularly; associated with
interstitial pneumonitis—baseline and periodic
chest radiographs should be obtained and drug
discontinued at first sign of dyspnoea
tamoxifen (Nolvadex,
Tamosin)
20–40 mg/day PO
In combination therapy with surgery to treat
breast cancer; treatment of advanced breast
cancer in men and women; first drug approved
for the prevention of breast cancer in women at
high risk
Actions:
antioestrogen, competes with oestrogen
for receptor sites in target tissues
Special considerations:
signs and symptoms
of menopause are common effects; CNS
depression, bone marrow depression and
GI toxicity are also common; can change
visual acuity and cause corneal opacities and
retinopathy—pretherapy and periodic ophthalmic
examinations are indicated
toremifene (Fareston)
60 mg/day PO
Treatment of advanced breast cancer in women
with oestrogen receptor–positive disease
Actions:
binds to oestrogen receptors and
prevents growth of breast cancer cells
Special considerations:
signs and symptoms
of menopause are common effects; CNS
depression and GI toxicity are also common
triptorelin (Diphereline)
3.75-mg IM depot monthly or 11.25-mg
IM depot every 3 months
Treatment of advanced prostatic cancer
Actions:
analogue of luteinising hormone–
releasing hormone; causes a decrease in follicle-
stimulating hormone and luteinising hormone
levels, leading to a suppression of testosterone
production
Special considerations:
monitor prostate-specific
antigen and testosterone levels regularly; sexual
dysfunction, urinary tract symptoms, bone pain
and hot flushes are common; schedule depot
injections and mark calendar for person
Prototype summary: Tamoxifen
Indications:
Treatment of metastatic breast cancer,
reduction of risk of invasive breast cancer in
women with ductal carcinoma in situ, reduction in
occurrence of contralateral breast cancer in people
