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Logo ORTHO-EST
SCHEDULING STATUS:
Schedule 4

PROPRIETARY NAME
(and dosage form):

ORTHO-EST
0,625 mg tablets

COMPOSITION
Each tablet contains 0,75 mg estropipate equivalent to 0,625 mg sodium oestrone sulphate.

PHARMACOLOGICAL CLASSIFICATION
A 21.8.1 Oestrogens.

PHARMACOLOGICAL ACTION
Estropipate is a natural oestrogenic substance prepared from purified crystalline oestrone, solubilized as the sulphate and stabilized with piperazine. It owes its therapeutic action to the metabolites of oestrone sulphate, oestradiol (principal intracellular human oestrogen) and oestrone, to which it is hydrolysed in the body.
Metabolism is primarily hepatic and a certain portion of the oestrogen undergoes enterohepatic circulation during which degradation of oestrogen occurs. Elimination is primarily renal in the form of glucuronides and to a lesser extent biliary in the form of glucuronide and sulphate conjugates.

INDICATIONS
ORTHO-EST is indicated for:
– Signs and symptoms of the naturally occurring or surgically induced oestrogen deficiency states associated with menopausal and post-menopausal symptoms, eg. hot flushes, sleep disturbances and urogenital atrophy.
– Osteoporosis induced by oestrogen-deficiency states in conjunction with other pertinent measures.

CONTRA-INDICATIONS
Oestrogens should not be used in individuals with any of the following conditions:
– Known hypersensitivity to oestrogens
– Known or suspected cancer of the breast or genital tract
– Known or suspected pregnancy and lactation
– Abnormal and undiagnosed vaginal bleeding
– Known or suspected oestrogen-dependent neoplasia
– Active thrombophlebitis or thromboembolic diseases
– Cardiovascular disease
– Endometriosis
– Porphyria
– Severe liver dysfunction

WARNINGS
Oestrogens have been reported to increase the risk of endometrial carcinoma in post-menopausal women placed on unopposed oestrogen therapy for prolonged periods. There is however no such risk in patients who have undergone hysterectomies.
In post-menopausal women with an intact uterus oestrogen should be supplemented by sequential progestogen therapy.
Close clinical surveillance of all women taking oestrogens is important. Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding.

DOSAGE AND DIRECTIONS FOR USE
ADULT DOSE: The lowest dose and regimen that will control symptoms should be chosen. In general ORTHO-EST 0,625 mg is administered cyclically or continuously.
The usual starting dose is 0,75 mg estropipate daily, which may be adjusted upwards to 6 mg estropipate per day. If the patient has not menstruated within the last two months or more, cyclical administration is started arbitrarily. If the patient is menstruating, cyclical administration is started on day 5 of bleeding.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
Side-effects:
The following side-effects have been reported with oestrogen therapy: breast tenderness or enlargement, peripheral oedema. Amenorrhea, breakthrough bleeding, menorrhagia or spotting. Nausea, vomiting, diarrhoea, abdominal cramps or bloating, alteration in liver function, jaundice, increased incidence of gall bladder disease, gall stones.
Other side-effects include: skin reactions (chloasma, rashes, urticaria), erythema multiforme and erythema nodusum have been reported. Intolerance to contact lenses, headaches, migraine, dizziness, mental depression, chorea, increase in weight and changes in libido.
Precautions:
Oestrogens may cause sodium and fluid retention, thus should be used with care in patients with asthma, epilepsy, migraine or heart or kidney disease. Oestrogens may exacerbate diabetes mellitus because of a decrease in tolerance to glucose and thyrotoxicosis.
Studies have shown that administration of a progestin for 10 to 14 days of an oestrogen cycle, for women with an intact uterus, is associated with a lower incidence of endometrial hyperplasia and endometrial carcinoma than an oestrogen-only cycle. There is no documented need for concurrent progestin therapy in patients who have undergone hysterectomies.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Overdosage of oestrogen may cause nausea and vomiting, and withdrawal bleeding may occur in females. Treatment is supportive and symptomatic.

IDENTIFICATION
White, diamond-shaped tablets, scored on one side and imprinted with "WFHC 101" on the other side.

PRESENTATION
HDPE containers of 30 or 100 tablets.

STORAGE INSTRUCTIONS
Store well closed, below 25°C.
Protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
29/21.8.1/0247

NAME AND BUSINESS ADDRESS OF THE APPLICANT
JANSSEN - CILAG

JANSSEN PHARMACEUTICA (PTY) LTD
(Reg. No. 80/11122/07)
15th ROAD
HALFWAY HOUSE
1685

DATE OF PUBLICATION OF THIS PACKAGE INSERT
14 Jan 2003

                OE-03-018

Updated on this site: January 2005
Source: Community Pharmacy

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