Action And Clinical Pharmacology: Dienestrol is a synthetic, nonsteroidal estrogen. The degree of systemic absorption and the mode of action are undetermined. However, one should be aware of the potential for systemic estrogen activity and related risks.
Indications And Clinical Uses: The treatment of senile or atrophic vaginitis or other vaginal disturbances associated with hypoestrogenic conditions.
Ortho Dienestrol cream is an estrogen product for intravaginal use only.
Contra-Indications: Known or suspected cancer of the breast; known or suspected estrogen-dependent neoplasia; known or suspected pregnancy (see Warnings); undiagnosed abnormal genital bleeding; active thrombophlebitis or thromboembolic disorders; a history of thrombophlebitis, thrombosis, or thromboembolic disorders; known or suspected hypersensitivity to any of the active or inactive ingredients, e.g., peanut oil.
Manufacturers’ Warnings In Clinical States: Induction of Malignant Neoplasms: Estrogens have been reported to increase the risk of endometrial carcinoma in postmenopausal women exposed to exogenous estrogens for prolonged periods. The risk appears to depend on both duration of treatment and on estrogen dose.
Long-term continuous administration of natural and synthetic estrogens in certain animal species increases the frequency of carcinomas of the breast, cervix, vagina and liver.
Pregnancy: Estrogens should not be used during pregnancy. Several reports suggest an association between intrauterine exposure to female sex hormones and congenital anomalies.
If the cream is used during pregnancy, or if the patient becomes pregnant while using this drug, she should be apprised of the potential risks to the fetus.
Gallbladder Disease: A 2- to 3-fold increase in the risk of surgically confirmed gallbladder disease in postmenopausal women receiving estrogens has been reported.
The following adverse effects have been associated with the systemic administration of estrogen-containing products: thromboembolic disease, hepatic tumors, hypertension and decreased glucose tolerance.
Precautions: Estrogens may cause fluid retention. Conditions possibly affected by this factor, such as epilepsy, migraine and cardiac or renal dysfunction, require careful observation.
Estrogens should be administered with caution in patients with: metabolic bone diseases that are associated with hypercalcemia; impaired liver function: If jaundice develops in any patient receiving estrogen, the medication should be discontinued while the cause of the jaundice is investigated; a history of mental depression; diabetes and pre-existing uterine leiomyomata (they may increase in size during estrogen use).
Certain patients may develop manifestations of excessive estrogenic stimulation, such as abnormal or excessive uterine bleeding, mastodynia, etc.
Estrogens should be used judiciously in patients in whom bone growth is not complete.
Drug Interactions: Laboratory Tests: Certain endocrine and liver function tests may be affected by estrogen-containing products. These are:
1. Increased sulfobromophthalein retention.
2. Increased prothrombin and factors VII, VIII, IX and X; decreased antithrombin 3; increased norepinephrine-induced platelet aggregability.
3. Increased thyroid-binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T4 by column or T4 by radioimmunoassay. Free T3 resin uptake is decreased, reflecting the elevated TBG; free T4 is unaltered.
4. Impaired glucose tolerance.
5. Decreased pregnanediol excretion.
6. Reduced response to metapyrone.
7. Reduced serum folate concentration.
8. Increased serum triglyceride and phospholipid concentration.
Adverse Reactions: Ortho Dienestrol Cream is generally well tolerated. There have been occasional reports of burning, itching and irritation. The physician should also be aware of those adverse reactions reported to occur with systemic administration of estrogens. (See also Contraindications and Warnings.)
Symptoms And Treatment Of Overdose: Symptoms and Treatment: Overdosage of estrogen may cause nausea and, in females, withdrawal bleeding may occur.
Dosage And Administration: The lowest dose that will control symptoms should be chosen and medication should be discontinued as promptly as possible.
Attempts to discontinue or taper medication should be made at 3- to 6-month intervals.
The usual dosage range is 1 or 2 applicatorsful/day for 1 or 2 weeks, then gradually reduced to one-half initial dosage for a similar period. A maintenance dosage of 1 applicatorful, 1 to 3 times a week, may be used after restoration of the vaginal mucosa has been achieved.
Treated patients with an intact uterus should be monitored closely for signs of endometrial cancer and appropriate diagnostic measures should be taken to rule out malignancy in the event of persistent or recurring abnormal vaginal bleeding.
Availability And Storage: The contents of each applicator is 5 g. Each g of water miscible, soft, white cream contains: dienestrol 0.1 mg (0.01%) in a base compounded with glyceryl monostearate, peanut oil, glycerin, benzoic acid, glutamic acid, citric acid, butylated hydroxanisole, sodium hydroxide and water. pH is approximately 4.3. Tubes of 78 g with applicator. Store at controlled room temperature (15 to 30°C).
ORTHO® DIENESTROL Janssen-Ortho Dienestrol Vaginitis Therapy