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Look Up > Drugs > Diethylstilbestrol
Diethylstilbestrol
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Administration
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(dye eth il stil BES trole)

U.S. Brand Names
Stilphostrol®

Generic Available

Yes


Canadian Brand Names
Honvol®

Synonyms
DES; Diethylstilbestrol Diphosphate Sodium; Stilbestrol

Pharmacological Index

Estrogen Derivative


Use

Palliative treatment of inoperable metastatic prostatic carcinoma and postmenopausal inoperable, progressing breast cancer


Pregnancy Risk Factor

X


Contraindications

Undiagnosed vaginal bleeding, during pregnancy; breast cancer except in select patients with metastatic disease


Warnings/Precautions

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


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


Overdosage/Toxicology

Symptoms of overdose include nausea


Drug Interactions

Decreased effect of oral anticoagulants

Increased effect of corticosteroids, succinylcholine, TCAs

Decreased DES levels: Barbiturates, phenytoin, rifampin


Stability

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


Mechanism of Action

Competes with estrogenic and androgenic compounds for binding onto tumor cells and thereby inhibits their effects on tumor growth


Pharmacodynamics/Kinetics

Metabolism: In the liver

Elimination: In urine and feces


Usual Dosage

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


Dietary Considerations

Should be administered with food to decrease GI distress


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


Test Interactions

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


Mental Health: Effects on Mental Status

May rarely cause anxiety or depression


Mental Health: Effects on Psychiatric Treatment

Barbiturates may lower levels of diethylstilbestrol


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

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.


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


Dosage Forms

Injection, as diphosphate sodium (Stilphostrol®): 0.25 g (5 mL)

Tablet: 1 mg, 2.5 mg, 5 mg

Tablet (Stilphostrol®): 50 mg


References

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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