Action and Clinical Pharmacology:
Similar to those of natural estrogens, i.e., stimulation of proliferative development of endometrium; development of secondary female sex characteristics; suppression of pituitary gonadotropin secretion; stimulation of protein synthesis; lowering of serum lipids; suppression of function of male target organs.
Indications And Clinical Uses:
The palliative treatment of advanced cancer of the prostate.
Diethylstilbestrol should not be administered to patients with active hepatic disease, especially of the obstructive type. The drug is also contraindicated in the following situations: children or young adults; a recent history of cerebrovascular accident or coronary thrombosis; thrombophlebitis and thromboembolic disease; partial or complete loss of vision or diplopia from ophthalmic vascular disease; porphyria; severe hypertension.
Warnings in Clinical States:
Before diethylstilbestrol is administered, the patient should have a complete physical examination, including a blood pressure determination.
If any surgical procedures are performed, the pathologist should be advised of the patient’s therapy when specimens are sent for examination.
Alternative therapy should be considered in patients who develop visual disturbances, classical migraine, transient aphasia, paralysis, loss of consciousness, or sudden elevation of blood pressure.
If the patient develops any sign of phlebitis or thrombo-embolic complications, medication should be discontinued.
Estrogen may cause fluid retention therefore particular caution is indicated in patients with cardiac or renal dysfunction, epilepsy, or asthma.:
Diabetic patients or those with a predisposition to diabetes should be observed closely to detect any alterations in carbohydrate metabolism. When liver or endocrine function tests are indicated, the results should not be considered reliable unless therapy has been discontinued for 2 to 4 months.
Elevation of blood pressure in previously normotensive or hypertensive patients may necessitate cessation of medication. Caution is indicated in patients with depression and in patients using contact lenses.
Although not all of the reactions listed below have been specifically associated with diethylstilbestrol tablets, they have been reported following estrogen therapy generally, and may be encountered when giving any product containing an estrogenic drug.
Gastrointestinal: nausea, anorexia, vomiting, abdominal cramps, bloating, cholestatic jaundice, cholelithiasis and increase or decrease in body weight.
Genitourinary: cystitis-like syndrome.
Endocrine and Metabolic: breast swelling and tenderness, testicular atrophy, increased blood sugar levels, and decreased glucose tolerance. Gynecomastia, reduced potency and feminization are expected adverse effects.
CNS: headaches, mental depression, increase or decrease of libido, nervousness, dizziness, fatigue, irritability.
Dermatologic: hypersensitivity reactions, loss of scalp hair, allergic reactions and rashes, hemorrhagic eruptions, itching, erythema nodosum, erythema multiforme, pigmentation of the skin.
Cardiovascular: sodium and water retention, increased blood pressure in susceptible individuals and aggravation of migraine headaches.
Hematologic: A statistically significant association has been demonstrated between the use of certain preparations containing estrogen and the following serious reactions: thrombophlebitis, pulmonary embolism and cerebral thrombosis.
Available evidence is suggestive of an association with the following reactions: coronary thrombosis and neuro-ocular lesions (e.g., retinal thrombosis and optic neuritis); altered coagulation tests (increase in prothrombin and Factors VII, VIII, IX, X).
Miscellaneous: precipitation or aggravation of porphyria cutanea tarda in predisposed individuals.
Symptoms And Treatment Of Overdose:
OverdoseExcessive doses may result in nausea, vomiting and abdominal cramps, headache, dizziness and general malaise. Gastric lavage may be considered if ingestion of the drug is recent and symptomatic treatment should be given. If the transient hyperestrogenic effects include severe sodium and water retention, administer diuretics.
Dosage And Administration:
Carcinoma of the prostate: Initial dose: 1 mg/day. Maximum dose: 3 mg/day. Maintenance dose: 1 mg/day.
Availability And Storage:
0.1 mg: Each round, white tablet contains: diethylstilbestrol 0.1 mg. Bottles of 100.
0.5 mg: Each round, light pink tablet contains: diethylstilbestrol 0.5 mg. Bottles of 100.
1 mg: Each round, dark pink tablet contains: diethylstilbestrol 1 mg. Bottles of 100.
STILBESTROL Roberts Diethylstilbestrol Estrogen