Climacteron (Testosterone – Estradiol)

CLIMACTERON®

Sabex

Testosterone – Estradiol

Estrogen Androgen Therapy

Indications And Clinical Uses: As replacement therapy for the control of menopausal symptoms and for estrogen deficiency-induced osteoporosis where estrogen deficiency is naturally or surgically induced. It should be used only in patients available for reevaluation at periodic intervals. Each reevaluation should determine the need for continued therapy and, if continuing therapy is required, whether a downward readjustment of dosage can be made.

Contra-Indications: Esterified estrogens should not be administered to patients with active hepatic dysfunction or disease, especially of the obstructive type; or a personal history of breast or endometrial cancer.

Endometrial hyperplasia is also a contraindication for estrogen therapy without accompanying progestogen. The drug is also contraindicated in the following situations: undiagnosed vaginal bleeding; a history of cerebrovascular accident, coronary thrombosis or in the presence of classical migraine; a history of thrombophlebitis or thromboembolic disease; partial or complete loss of vision or diplopia, from ophthalmic vascular disease; suspected pregnancy. (A statistically significant association has been reported between maternal ingestion of diethylstilbestrol during pregnancy and the occurrence of vaginal carcinoma in the offspring. This occurred with the use of diethylstilbestrol for the treatment of threatened abortion or high risk pregnancies. Whether or not such an association is applicable to all estrogens is not known at this time. In view of this finding, however, the use of any estrogen in pregnancy is not recommended.)

Precautions: Three independent retrospective studies have reported an association between postmenopausal estrogen therapy and an increased risk of endometrial carcinoma. These studies, however, lacked information regarding certain important intrinsic risk factors of the patients (especially pretreatment endogenous hormonal status) and the mode of administration of estrogen. The potential relationship of estrogen to endometrial carcinoma under clinical conditions has to be considered. However, a cause and effect relationship between estrogen administration and endometrial carcinoma cannot be established by these data at this time.

Before estrogens are administered, the patient should have a complete physical examination including blood pressure determination. Breasts and pelvic organs should be examined and a Papanicolaou smear should be taken.

The first follow up examination should be done within 6 months after initiation of treatment. Thereafter, examinations should be made once a year. At each examination, repeat those procedures outlined above.

If any surgical procedures are performed, advise the pathologist of the patient’s therapy when specimens are sent for examination. Liver function tests should be made periodically in subjects who have, or are suspected of having, hepatic disease.

If abnormal vaginal bleeding occurs during therapy, perform diagnostic aspiration biopsy or curettage to rule out the possibility of uterine malignancy.

Although the estrogen content of oral contraceptive therapy has been associated with an increased risk of various thromboembolic, thrombotic and vascular diseases, to date no such increased risk in postmenopausal users of estrogens has been detected. Nevertheless, the physician should be alert to the earliest manifestations of thrombotic disorders (thrombophlebitis, retinal thrombosis, cerebral embolism and pulmonary embolism). If these occur or are suspected, estrogen therapy should be discontinued immediately.

In patients with metastatic carcinoma and hypercalcemia, estrogen medication should be used with caution.

Development of sudden enlargement, pain, or tenderness of uterine fibroids requires discontinuation of medication.

Estrogen may cause sodium and water retention. Therefore, particular caution is indicated in cardiac or renal dysfunction, epilepsy, or asthma.

Elevation of blood pressure in previously normotensive or hypertensive patients necessitates cessation of medication.

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.

Adverse Reactions: Gastrointestinal: nausea, vomiting, anorexia, abdominal cramps, bloating.

Endocrine: Estrogenic effects: withdrawal and breakthrough bleeding; breast soreness.

Androgenic effect: If virilization occurs, discontinue therapy. Virilization appears to be reversible if detected early, except for some instances of voice changes.

Metabolic: Slight weight gain due to sodium retention or from increased appetite caused by the anabolic action of the preparation; alteration of carbohydrate metabolism.

Cardiovascular: High doses of estrogens may predispose the patient to the development of thrombophlebitis or thromboembolic disease (pulmonary embolism, cerebral thrombosis, coronary thrombosis, retinal thrombosis and optic neuritis). An increase in blood pressure in susceptible individuals has also been reported following use of estrogen.

Dermatologic: skin rash; hepatic cutaneous porphyria becoming manifest. There have been a few reported cases of a temporary growth of hair at the injection site. This adverse effect is believed caused by a direct stimulation of the hair follicle at the injection site. Since this may occur in either sex, it should not be considered as a masculinization symptom.

CNS: headache, aggravation of migraine headaches, nervousness.

Hematologic: Altered coagulation tests such as increase in prothrombin and Factor VII, VIII, IX, and X have been reported following use of preparations containing estrogen.

Miscellaneous: Cholestatic jaundice has been reported with estrogens and methyltestosterone. A few instances of coughing, dyspnea and chest constriction have been reported with preparations containing benzyl benzoate.

Climacteron should always be injected as a deep i.m. injection into the gluteus maximus. Reports of pain, redness, swelling and tenderness have been received following the injection into the deltoid muscle. This should be expected considering the relatively small size of this muscle for a depot injection.

Dosage And Administration: Climacteron should be used only in patients available for reevaluation at periodic intervals. Each reevaluation should determine the need for continued therapy and if continuing therapy is required, whether a downward dosage readjustment can be made. In making such reevaluation of long-term therapy, such reassessment should be based on an evaluation of the benefits of therapy versus risks.

Recommended Dose: 1 mL by deep i.m. injection into the gluteus maximus. Repeat every 4 to 8 weeks or less frequently as indicated by the patient’s response.

Maximal Dose: 1 mL every 4 weeks. The patient’s response should serve as a guide for the duration of use.

Availability And Storage: Each mL of injectable solution contains: testosterone enanthate benzilic acid hydrazone 150 mg (equivalent to testosterone 69 mg), estradiol dienanthate 7.5 mg and estradiol benzoate 1 mg. Nonmedicinal ingredients: benzyl alcohol 7.5% as preservative in benzyl benzoate and corn oil. Ampuls of 1 mL, boxes of 3. Vials of 5 mL, boxes of 1. Store between 15 and 30°C.

CLIMACTERON® Sabex Testosterone – Estradiol Estrogen Androgen Therapy

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