(and dosage form):
Depot progestogen for
hormonal contraception (oily solution)
1 mL contains norethisterone enantate (17alpha-ethinyl-17beta-heptanoyloxy-4-estrene-3-one) 200 mg.
A. 21.8.2 Progesterones without estrogens.
Nur-Isterate is a depot progestogen for hormonal contraception. The contraceptive action of Nur-Isterate is achieved by the additive effects of several factors. Protection against conception is mainly effected by alterations of the cervical mucus which are present during the whole period of action. These impair sperm movement into the uterine cavity. Ovulation is suppressed by the antigonadotropic effect of norethisterone. In addition, Nur-Isterate effects morphological changes in the endometrium which render it less suitable for nidation.
Nur-Isterate is contra-indicated in pregnancy, phlebitis or thromboembolic diseases, pathologically increased blood pressure, acute and severe, chronic liver diseases, with and without jaundice (particularly primary biliary liver cirrhosis), existing or treated cancer of the breast or uterus, severe diabetes with vascular changes, disturbances of lipometabolism, previous or existing liver tumours, a history of herpes of pregnancy, a history of idiopathic jaundice of pregnancy or severe pruritus of pregnancy. Dubin-Johnson syndrome, Rotor syndrome, otosclerosis with deterioration in pregnancy, 12 weeks before planned operations and during immobilisation (eg after accidents).
No further injection should be given if, during treatment, migrainous headaches occur for the first time or recurrent, unusually severe headaches develop, if sudden perceptual disorders (eg disturbances of vision or hearing) occur, if first signs of thrombophlebitis or thromboembolic disease (eg unusual pain in the legs or swelling of the legs, stabbing pains on breathing, or coughing for no apparent reason) are noted, or if a feeling of pain and tightness in the chest, a significant rise in blood pressure, recurrence of earlier depression or pathological changes of liver function and hormone levels are experienced.
In porphyria and all forms of limited liver function, a history of phlebitis or thromboembolic disease, the risk/benefit ratio must be considered carefully.
If there is a history of extrauterine pregnancy, the use of Nur-Isterate should be decided on only after carefully weighing the benefits against the risks. This also holds true if one Fallopian tube is missing.
If obscure lower abdominal complaints occur together with an irregular cycle pattern (above all amenorrhoea following persistent bleeding), an extrauterine pregnancy must be considered.
Nur-Isterate should only be administered to women with a history of regular cycles.
DOSAGE AND DIRECTIONS FOR USE
Before starting Nur-Isterate a thorough general medical and gynaecological examination (including the breasts) should be carried out and pregnancy must be excluded.
Nur-Isterate must always be administered as a slow, deep intramuscular injection (preferably intragluteal, alternatively into the deltoid muscle). It is advisable to cover the site of injection afterwards with a plaster in order to prevent partial reflux of the injection solution.
The first intramuscular injection is given within the first five days of the cycle. The next three injections are to be given at intervals of 8 weeks, after which a further injection is required every 12 weeks (84 days). If the injection interval is extended beyond that time, contraceptive protection will be inadequate from the 13th week onwards.
Should practical reasons make it difficult to maintain the 84-day injection interval, a 2-month regimen can alternatively be adopted.
In each case, the next injection should only be given if bleeding has occurred within the preceding 10 weeks. Nur-Isterate must otherwise be withdrawn and pregnancy ruled out.
If it appears desirable to check the full recovery of ovarian function in young women, the preparation should be discontinued after 2 years of administration. Following discontinuation, normal ability to conceive usually returns about 7-8 months after the last injection.
SIDE EFFECTS AND SPECIAL PRECAUTIONS
The relatively frequent side effects are cycle disturbances in the form of spotting, breakthrough bleeding and amenorrhoea of short duration.
Additional symptoms reported are headaches, dizziness, depressive moods, and transient nausea. Mass gain may be associated with Nur-Isterate.
Regular concurrent use of other medicines (eg barbiturates, hydantoins, rifampicin) may impair the action of Nur-Isterate.
A reduction of glucose tolerance has been observed in some women using progestogens. Consequently, diabetics and women with a tendency to diabetes should be carefully supervised during the use of Nur-Isterate. In the case of diabetics, the requirement for oral antidiabetics or insulin can change.
An association between the use of hormonal contraceptives and an increased risk of venous and arterial thromboembolic diseases cannot be ruled out.
The relative risk of arterial thromboses (eg stroke, myocardial infarction) appears to increase further when heavy smoking, increasing age and the use of hormonal contraceptives coincide.
In sickle-cell anaemia, the full status of the red blood picture must be determined before the start of treatment and checked at monthly intervals during treatment. If the status deteriorates during use, no further injection of Nur-Isterate should be given. The use of Nur-Isterate is contra-indicated if these checks are not possible or cannot be assured.
In rare cases benign and in even rarer cases malignant liver tumours leading in isolated cases to life-threatening intraabdominal haemorrhage have been observed after the use of hormonal substances such as the one contained in Nur-Isterate. The doctor must therefore be informed of the occurrence of unusual upper abdominal complaints which do not disappear spontaneously within a short time as it may then be necessary to withdraw the preparation.
Regular gynaecological examinations should be carried out as a precaution during long-term use of Nur-Isterate.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
None. See "Side effects and special precautions". Treatment is supportive and symptomatic.
Clear, yellowish, oily solution.
1 ampoule of 1 mL.
100 ampoules of 1 mL each.
Store below 30°C. Protect from light. Keep out of reach of children.
NAME AND BUSINESS ADDRESS OF THE APPLICANT
Schering (Pty) Ltd
(Reg No: 1964/009072/07)
106 Sixteenth Road
P O Box 5278
Halfway House 1685
DATE OF PUBLICATION OF THIS PACKAGE INSERT
14 September 1992
SCHERING (PTY) LTD
(Reg No: 1964/009072/07)
Schering AG Germany
Updated on this site: April 2003
Current: January 2005
Source: Pharmaceutical Industry
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