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Pronunciation |
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(dye
eth il stil BES
trole) |
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U.S. Brand
Names |
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Stilphostrol® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Honvol® |
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Synonyms |
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DES; Diethylstilbestrol Diphosphate Sodium; Stilbestrol |
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Pharmacological Index |
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Estrogen Derivative |
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Use |
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Palliative treatment of inoperable metastatic prostatic carcinoma and
postmenopausal inoperable, progressing breast cancer |
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Pregnancy Risk
Factor |
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X |
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Contraindications |
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Undiagnosed vaginal bleeding, during pregnancy; breast cancer except in
select patients with metastatic disease |
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Warnings/Precautions |
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Use with caution in patients with a history of thromboembolism, stroke,
myocardial infarction (especially >40 years of age who smoke), liver tumor,
hypertension, cardiac, renal or hepatic insufficiency; estrogens have been
reported to increase the risk of endometrial carcinoma; do not use estrogens
during pregnancy |
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Adverse
Reactions |
|
>10%:
Cardiovascular: Peripheral edema
Endocrine & metabolic: Enlargement of breasts (female and male), breast
tenderness
Gastrointestinal: Anorexia, bloating
1% to 10%:
Central nervous system: Headache
Endocrine & metabolic: Increased libido (female), decreased libido (male)
Gastrointestinal: Vomiting, diarrhea
<1%: Hypertension, thromboembolism, myocardial infarction, edema, stroke,
depression, dizziness, anxiety, chloasma, melasma, rash, amenorrhea, alterations
in frequency and flow of menses, increased triglycerides, nausea, GI distress,
increased LDL, cholestatic jaundice, intolerance to contact lenses, decreased
glucose tolerance, increased susceptibility to Candida infection, breast
tumors |
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Overdosage/Toxicology |
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Symptoms of overdose include nausea |
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Drug
Interactions |
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Decreased effect of oral anticoagulants
Increased effect of corticosteroids, succinylcholine, TCAs
Decreased DES levels: Barbiturates, phenytoin, rifampin |
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Stability |
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Intravenous solution should be stored at room temperature and away from
direct light; solution is stable for 3 days as long as cloudiness or
precipitation has not occurred |
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Mechanism of
Action |
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Competes with estrogenic and androgenic compounds for binding onto tumor
cells and thereby inhibits their effects on tumor growth |
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Pharmacodynamics/Kinetics |
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Metabolism: In the liver
Elimination: In urine and feces |
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Usual Dosage |
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Adults:
Prostate carcinoma (inoperable, progressing): Oral: 1-3 mg/day
Diphosphate: (inoperable, progressing): Oral: 50 mg 3 times/day; increase up
to 200 mg or more 3 times/day; maximum daily dose: 1 g
I.V.: Administer 0.5 g, dissolved in 250 mL of saline or D5W,
administer slowly the first 10-15 minutes then adjust rate so that the entire
amount is given in 1 hour; repeat for greater than or equal to 5 days depending
on patient response, then repeat 0.25-0.5 g 1-2 times for one week or change to
oral therapy
Female: Postmenopausal (inoperable, progressing) breast carcinoma: Oral: 15
mg/day |
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Dietary
Considerations |
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Should be administered with food to decrease GI distress |
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Administration |
|
I.V. infusion: Dilute 0.5-1 g in 250-500 mL D5W or NS; give 1-2
mL/minute for 10-15 minutes, then infuse remaining solution over 1
hour |
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Test
Interactions |
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Increased prothrombin and factors VII, VIII, IX, X
Decreased antithrombin III
Increased platelet aggregability
Increased thyroid binding globulin
Increased total thyroid hormone (T4)
Decreased serum folate concentration
Increased serum triglycerides/phospholipids |
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Mental Health: Effects
on Mental Status |
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May rarely cause anxiety or depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Barbiturates may lower levels of diethylstilbestrol |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Use as directed with or after meals (sustained release may be taken at
midmorning - do not crush or chew). May cause breast tenderness or enlargement
(consult prescriber for relief). You may be more sensitive to sunlight; use
sunblock, wear protective clothing and dark glasses, or avoid direct exposure to
sunlight. If you are diabetic, monitor serum glucose closely; antidiabetic agent
may need to be adjusted. Discontinue use and report promptly any pain, redness,
warmth, or swelling in calves; sudden onset difficulty breathing; headache; loss
of vision; difficulty speaking; sharp or sudden chest pain; severe abdominal
pain; or unusual bleeding or speech. Pregnancy/breast-feeding
precautions: Inform prescriber if you are pregnant. Do not get pregnant
while taking this drug and for 1 month following therapy. Consult prescriber for
instruction on appropriate contraceptive measures. This drug may cause severe
fetal defects. Do not donate blood during or for 1 month following therapy (same
reason). Do not breast-feed. |
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Nursing
Implications |
|
Administer 0.5 g I.V., dissolved in 250 mL of saline or D5W,
administer slowly the first 10-15 minutes then adjust rate so that the entire
amount is administered in 1 hour |
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Dosage Forms |
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Injection, as diphosphate sodium (Stilphostrol®): 0.25
g (5 mL)
Tablet: 1 mg, 2.5 mg, 5 mg
Tablet (Stilphostrol®): 50 mg |
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References |
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Emens JM, "Continuing Problems With Diethylstilbestrol," Br J Obstet
Gynaecol, 1994, 101(9):748-50.
Emens M, "Vaginal Adenosis and Diethylstilbestrol," Br J Hosp Med,
1984, 31(1):42-8.
Giusti RM, Iwamoto K, and Hatch EE,
"Diethylstilbestrol Revisited: A Review of the Long-Term Health Effects," Ann
Intern Med, 1995, 122(10):778-88.
Henriksson P,
"Estrogen in Patients With Prostatic Cancer: An Assessment of the Risks and Benefits,"
Drug Saf, 1991, 6(1):47-53.
Mittendorf R and Williams MA,
"Stilboestrol Exposure In Utero and Risk of Pre-eclampsia,"
Lancet, 1995, 345(8944):265-6.
Wilcox AJ, Baird DD, Weinberg CR, et al,
"Fertility in Men Prenatally to Diethylstilbestrol," N Engl J Med, 1995,
338(21):1411-6. |
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