Norethisterone enanthate Injection 200mg Taj Pharma

 

  1. Name of the medicinal product

Norethisterone enanthate injection 200mg Taj Pharma

  1. Qualitative and quantitative composition

Each ml contains 200mg norethisterone enanthate in oily solution.

Excipient with known effect:

333.8mg benzyl benzoate in 1 ml ampoule.

For the full list of excipients, see Section 6.1.

  1. Pharmaceutical form

Solution for Injection

  1. Clinical particulars

4.1 Therapeutic indications

Norethisterone enanthate is a depot contraceptive. It is intended for short-term use when a high level of efficacy independent of possible errors by the patient is required. It has been licensed for short-term use by women whose partners undergo vasectomy, until the vasectomy is effective, and women immunised against rubella, to prevent pregnancy during the period of activity of the virus.

Use after delivery or abortion: Norethisterone enanthate can generally be used immediately after delivery or abortion (but see Section 4.6 ‘Use during lactation’).

4.2 Posology and method of administration

200mg Norethisterone enanthate intramuscularly provides contraception for eight weeks. The first injection should be given within the first five days of a menstrual cycle (the first day of menstruation counting as day 1), unless it is given so soon after delivery or abortion that no possibility of pregnancy exists. Provided the injection is carried out according to these instructions, no additional contraceptive cover is required. The injection may be repeated once, after eight weeks. Norethisterone enanthate must always be injected deep into the gluteal muscles, care being taken that no liquid runs back from the injection site, which could result in loss of efficacy. The viscosity of the liquid at low temperatures is high, necessitating considerable pressure of injection. Therefore it is suggested that the ampoule be immersed in warm water before injection. A needle of at least medium bore should be used, and care taken to ensure that the needle is securely attached to the syringe. The injection must be administered extremely slowly (see Section 4.4 Special Warnings and Precautions for use).

4.3 Contraindications

– Known or suspected pregnancy.

– Current or severe hepatic disease as long as liver function values have not returned to normal.

– Previous or existing liver tumours.

– Severe diabetes with vascular changes.

– Pathologically increased blood pressure.

– Current thromboembolic disease.

– Disturbances of lipid metabolism.

– Suspected, existing or treated breast or endometrial cancer.

– Porphyria

– Hypersensitivity to the active substance(s) or to any of the excipients listed in section 6.1.

4.4 Special warnings and precautions for use

Medical Examination

Assessment of women prior to starting Norethisterone enanthate (and at regular intervals thereafter) should include a personal and family medical history of each woman. Physical examination should be guided by this and by the contraindications (section 4.3) and warnings (section 4.4) for this product. The frequency and nature of these assessments should be based upon relevant guidelines and should be adapted to the individual woman, but should include measurement of blood pressure and, if judged appropriate by the clinician, breast, abdominal and pelvic examination including cervical cytology.

Before starting treatment, pregnancy must be excluded.

Women should be advised that progestogen-only contraceptives do not protect against HIV infections (AIDS) and other sexually transmitted diseases.

Gynaecological considerations

Norethisterone enanthate should not be used in patients with abnormal uterine bleeding until a definite diagnosis has been established and the possibility of genital tract malignancy eliminated. Undiagnosed vaginal bleeding that is suspicious for underlying conditions should be investigated prior to first injection and endometrial pathology should be excluded if it occurs in women over 40 after prolonged amenorrhoea.

If there is a history of ectopic pregnancy or one fallopian tube is missing, the use of Norethisterone enanthate should be decided on only after carefully weighing the benefits against the risks.

If obscure lower abdominal complaints occur together with an irregular cycle pattern (above all amenorrhoea followed by persistent irregular bleeding), an extrauterine pregnancy must be considered.

The patient should be informed before starting Norethisterone enanthate that her menstrual pattern is likely to alter during the entire exposure period. Menstrual changes in the form of spotting, breakthrough bleeding and delayed menstruation are relatively frequent, and generally do not require treatment.

Amenorrhoea: if, when the second injection is due, bleeding has not occurred in the preceding eight weeks the second injection should not be given until pregnancy has been ruled out.

Partial metabolization of norethisterone to ethinylestradiol

Norethisterone is partly metabolised to ethinylestradiol (EE) after intramuscular administration in humans. This conversion results in a systemic EE exposure corresponding to an oral equivalent dose of about 4 µg EE per day, on average, over 8 weeks. Mean oral equivalent doses per day are about 10 μg EE during the first 2 weeks after Norethisterone enanthate administration and decline to about 5 μg EE in the 3rd week and about 2 μg EE from the 5th week onwards. Therefore, systemic estrogen effects cannot be excluded (see section 5.2). Post-marketing experience with Norethisterone enanthate indicates that the safety profile of Norethisterone enanthate does not resemble that of combined hormonal contraceptives.

Circulatory disorders:

There is a general opinion, based on statistical evidence, that users of hormonal contraceptives experience, more often than non-users, venous thromboembolism, arterial thrombosis, including cerebral and myocardial infarction, and subarachnoid haemorrhage. Full recovery from such disorders does not always occur, and it should be realised that in a few cases they are fatal.

The relative risk of arterial thrombosis (e.g. stroke and myocardial infarction) appears to increase further when heavy smoking, increasing age and the use of hormonal contraceptives coincide.

Although there have been so far no observations of thromboembolic disease during the use of Norethisterone enanthate, as a precaution it is recommended that this preparation should not be used where there is a history of thromboembolic processes.

No further injection should be given if symptoms of an arterial or venous thrombotic event occur during treatment, e.g.

  • new onset or exacerbation of migraine-type headaches,
  • sudden disturbances of vision or hearing perceptual disorders occur,
  • significant rise in blood pressure,
  • first signs of thrombosis or blood clots.

Liver Function

Porphyria and existing impairment of liver function might theoretically be exacerbated by Norethisterone enanthate.

In rare cases benign, and in even rarer cases malignant, liver tumours leading in isolated cases to life-threatening intra-abdominal haemorrhage, have been observed after the use of hormonal substances such as the one contained in Norethisterone enanthate. If severe upper abdominal complaints, liver enlargement or signs of intra-abdominal haemorrhage occur, a liver tumour should be considered in the differential diagnosis.

Women with a history of disturbed liver function or any disease that is prone to worsen during pregnancy such as idiopathic jaundice or severe pruritus of pregnancy should be carefully observed during medication.

Recurrence of cholestatic jaundice which occurred first during pregnancy or previous use of sex steroids necessitates the discontinuation of Norethisterone enanthate.

Other conditions

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 Norethisterone enanthate. In the case of diabetes, it may be necessary to reassess the required doses of antidiabetics or insulin.

In rare cases coughing, dyspnoea and circulatory irregularities may occur during or immediately after the injection. Experience has shown that these reactions can be avoided by injecting Norethisterone enanthate very slowly.

Women with a history of severe depressive states should be carefully observed during medication. No further injection should be given, if during treatment, recurrence of earlier depression is experienced.

Depressed mood and depression are well-known undesirable effects of hormonal contraceptive use (see section 4.8). Depression can be serious and is a well-known risk factor for suicidal behaviour and suicide. Women should be advised to contact their physician in case of mood changes and depressive symptoms, including shortly after initiating the treatment.

Effect on blood chemistry: No influence of Norethisterone enanthate on basal plasma cortisol, the ACTH test or the metyrapone test has been observed. In the acute dexamethasone suppression test, however, a higher plasma cortisol value than expected was found in 4 out of 10 women, although there were no clinical indications of disturbed adrenocortical function. A shortening of the recalcification time and of the thromboplastin time (Quick’s test) were observed in studies of the blood coagulation system.

Information about excipients

This medicine contains 333.8mg benzyl benzoate in each 1 ml ampoule.

Benzyl benzoate may increase jaundice in newborn babies (up to 4 weeks old).

4.5 Interaction with other medicinal products and other forms of interaction

Note: The prescribing information of concomitant medications should be consulted to identify potential interactions.

There are no data on progestogen-only injectables drug interactions.

Effects of other medicinal products on Norethisterone enanthate

Direct clinical evidence for reduced effectiveness of Norethisterone enanthate has not been obtained. However, theoretical interactions based on findings with combined oral contraceptives include the following, which have been shown to have clinically important interactions:

Anticonvulsants: phenytoin, barbiturates, primidone, carbamazepine, phenylbutazone, oxcarbazepine, topiramate, felbamate.

Antifungal agents:griseofulvin.

Certain antibiotics: rifampicin and ampicillin (possibly due to changes in the intestinal flora).

Herbal remedies: products containing St John’s wort (Hypericum perforatum).

Antiviral agents: HIV/HCV protease inhibitors and non-nucleoside reverse transcriptase inhibitors can have variable effects on the plasma concentrations of sex hormones.

Substances decreasing the clearance of sex hormones (enzyme inhibitors)

Strong and moderate CYP3A4 inhibitors such as azole antifungals (e.g. fluconazole, itraconazole, ketoconazole, voriconazole) and macrolides (e.g. erythromycin) can increase plasma concentrations of the progestin.

Effects of Norethisterone enanthate on other medicinal products

Hormonal contraceptives may affect the metabolism of certain other drugs. Accordingly, plasma and tissue concentrations may be affected (e.g. increased ciclosporin plasma concentrations).

The requirement for oral antidiabetics or insulin can change as a result of the effect on glucose tolerance.

Other forms of interaction

Laboratory tests

The use of contraceptive steroids may influence the results of certain laboratory tests.

Pharmacodynamic interactions

Co-administration of ethinylestradiol-containing medicinal products with direct-acting antiviral (DAA) medicinal products containing ombitasvir, paritaprevir, or dasabuvir, and combinations of these has been shown to be associated with increases in ALT levels to greater than 20 times the upper limit of normal in healthy female subjects and HCV infected women. Since norethisterone is partly metabolised to ethinylestradiol after intramuscular Norethisterone enanthate administration in humans (see section 5.2) such an interaction cannot be excluded.

4.6 Pregnancy and lactation

Pregnancy

Norethisterone enanthate is contraindicated in pregnancy.

Like all nortestosterone derivatives used for contraception, Norethisterone enanthate has slight androgenic activity, and a virilising effect on the external genitalia of a female foetus exposed to Norethisterone enanthate after the first month of pregnancy cannot be totally ruled out on theoretical grounds. However, no such virilisation has been observed after the few pregnancies that have been reported during the use of Norethisterone enanthate.

Lactation

There appear to be no adverse effects on infant growth or development when using Norethisterone enanthate after six weeks postpartum. Norethisterone enanthate does not appear to affect the quantity or quality of breast milk, however, minute amounts of the active substance are excreted with the milk and although considered harmless to a healthy neonate, might theoretically, like other steroids, impair the degradation of bilirubin, especially during the first week of life. If the mother has received Norethisterone enanthate, breast-feeding should therefore be withheld from neonates with severe or persistent jaundice requiring medical treatment.

4.7 Effects on ability to drive and use machines

None known.

4.8 Undesirable effects

Undesirable effects that have been reported in users of Norethisterone enanthate (based on post-marketing data) are:

System Organ ClassVery common

≥ 1/10

Common

≥ 1/100 and < 1/10

Uncommon

≥ 1/1.000 and < 1/100

Immune system disordersHypersensitivity reaction
Metabolism and nutrition disordersWeight increase
Psychiatric disordersDepressed mood
Nervous system disordersDizziness

Headache

Gastrointestinal disordersNausea
Skin and subcutaneous tissue disordersSkin disorder
Reproductive system and breast disordersUterine / Vaginal bleeding including Spotting

Amenorrhoea (short lasting)

breast discomfort
General disorders and administration site conditionsInjection site reaction

Local skin reaction

Bloating

Administration-related events:

Experience has shown that the short-lasting reactions (urge to cough, paroxysmal cough, respiratory distress, dyspnoea and circulatory irregularities) may occur in isolated cases during or immediately after the injection of oily solutions if the solution is injected too rapidly (see Section 4.4).

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product.

4.9 Overdose

Presentation of a single use injectable and administration by a physician minimize the risk of overdose. There have been no reports of serious deleterious effects from overdose. There are no antidotes and further treatment should be symptomatic.

  1. Pharmacological properties

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Progestogens ATC code: None assigned

Mechanism of action

Norethisterone enanthate is a depot contraceptive. The mode of action, following injection, is initially inhibition of ovulation.

Towards the end of the injection interval, the action is mainly local on the cervical mucus and endometrium. These latter effects prevent ascension of sperm into the uterine cavity and impede nidation.

5.2 Pharmacokinetic properties

Absorption

Norethisterone enantate was completely absorbed after intramuscular injection. The ester was quickly and eventually completely hydrolyzed to its pharmacologically active compound norethisterone once it was released from the depot.

Distribution

Maximum levels of norethisterone were measured about 3-20 days after i.m. administration. They amounted on average to 13.4 ± 5.4 ng/ml and 12.2 ± 2.7 ng/ml about 7 days (median) after i.m. administration of 200mg norethisterone enanthate in 2 ml and 1 ml oily solution, respectively.

Plasma levels of norethisterone declined in two disposition phases with half-lives of 4-5 days and 15-20 days, respectively, which were due to a biphasical release of norethisterone enanthate from the depot.

Biotransformation

Norethisterone enantate is metabolised completely. Norethisterone enantate is split mainly in the liver by enzymatic hydrolysis into norethisterone and heptanoic acid.

While the fatty acid is metabolised by means of (β-oxidation, norethisterone is transformed mainly through the reduction of the C4 -C5 double bond and the C3 keto group. The majority of metabolites found in urine were present as conjugates, mainly as sulfates, which are expected to be inactive.

Norethisterone is partly metabolised to ethinylestradiol (EE) after intramuscular administration in humans. This conversion results in a systemic EE exposure corresponding to an oral equivalent dose of about 4 µg EE per day, on average, over 8 weeks. Mean oral equivalent doses per day are about 10 µg EE during the first 2 weeks after Norethisterone enanthate administration and decline to about 5 µg EE in the 3rd week and about 2 µg EE from the 5th week onwards. Therefore systemic estrogen effects cannot be excluded. The Cmax of EE after i.m. administration of 200mg NETE was significantly lower than after oral administration of 0.03mg EE/0.15mg LNG once daily for 21 days (approximately 68% lower). Post-marketing experience with Norethisterone enanthate indicates that the safety profile of Norethisterone enanthate does not resemble that of combined hormonal contraceptives.

Elimination

Up to 85% of the norethisterone enanthate dose were excreted within 30 days in urine (40%) and faeces (60%). No unchanged norethisterone enanthate was recovered in urine or faeces. In urine and faeces, similar excretion half-lives of 6 – 9 days were estimated for radioactive labelled substances during the observation period of 30 days and – in a further study – an excretion half-life of 20 – 30 days was measured in urine between day 30 and 80 after i.m. administration of 200mg 3H-norethisteteroneenantate. Based on animal studies, retention of the drug in the body is not to be expected.

In plasma of women, 96% of norethisterone are bound to proteins. The respective percentages bound to SHBG and albumin are approximately 35% and 61% as long as SHBG levels are within the normal range.

Due to the half-life of the terminal disposition phase from plasma (about 2.5 weeks) and the initial dose regimen (one injection every 2 months), a slight accumulation of the drug will be expected after multiple administrations. A steady state will already be reached after the second administration.

Transfer of norethisterone into mother’s milk was negligible. During the first week after i.m. injection of 200mg norethisterone enanthate, a daily intake of norethisterone with mother’s milk in the range of 0.5 μg to 2.4 μg was calculated from norethisterone concentrates in the milk, assuming that the infant ingests 600 ml milk daily.

Linearity/non-linearity

Although there is no direct investigation on bioavailability of norethisterone after i.m. administration of norethisterone enanthate reported, complete availability can be estimated by comparison of norethisterone AUC values determined in different studies after i.v. injection of norethisterone and after i.m. injection of norethisterone enanthate.

5.3 Preclinical safety data

Non-clinical data reveal no special risk for humans based on studies of repeated dose toxicity, genotoxicity, carcinogenicity and toxicity to reproduction which is not already included in other relevant sections.

Besides the studies with the active ingredient norethisterone enanthate, data recorded for norethisterone and norethisterone acetate were also taken into consideration for the toxicological evaluation of the risk from use of Norethisterone enanthate.

In animal studies on systemic tolerance with repeated administration (including studies for evaluation of a tumorigenic activity), no systemic intolerance reactions were observed which would raise objections to the use of the preparation in dosages required for contraception.

On principle, however, it should be kept in mind that sex steroids might stimulate the growth of hormone-dependent tissues and tumours.

In reproduction toxicological studies no indication of a teratogenic potential was noted. This is in accordance with reports on clinical experience after accidental administration of Norethisterone enanthate during pregnancy or on the rare cases of pregnancies occurring during use of Norethisterone enanthate, where no indication of a teratogenic potential was noted.

Local tolerance was assessed in the course of systemic tolerance studies and indicated only a mild irritant potential of the drug substance. The good local tolerance has been confirmed by long-term clinical experience.

Experimental investigations into possible sensitising effects of norethisterone enanthate have not been carried out.

In vitro studies for evaluation of genotoxicity did not indicate that norethisterone or its esters possess a mutagenic potential.

  1. Pharmaceutical particulars

6.1 List of excipients

Castor oil for injection

Benzyl benzoate

6.2 Incompatibilities

In the absence of compatibility studies, this medicinal product should not be mixed with other medicinal products.

6.3 Shelf life

5 years.

6.4 Special precautions for storage

Store below 25°C.

Protect from light.

6.5 Nature and contents of container

Carton containing one 1ml glass ampoule.

6.6 Special precautions for disposal and other handling

Keep out of the reach of children.

 

  1. MANUFACTURED IN INDIA BY:
    TAJ PHARMACEUTICALS LTD.
    Mumbai, India
    Unit No. 214.Old Bake House,
    Maharashtra chambers of  Commerce Lane,
    Fort, Mumbai – 400001
    at:Gujarat, INDIA.
    Customer Service and Product Inquiries:
    1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
    Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
    E-mail: tajgroup@tajpharma.com

 

Norethisterone enanthate Injection 200mg Taj Pharma

Package leaflet: Information for the user

Norethisterone enanthate for Injection 200mg

Norethisterone enanthate

Read all of this leaflet carefully before you start using this medicine because it contains important information for you.

  • Keep this leaflet. You may need to read it again.
  • If you have any further questions, ask your doctor, family planning nurse or pharmacist.
  • Norethisterone enanthate is given by injection for contraception.
  • If you get any side effects, talk to your doctor, family planning nurse or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4.

Three important things to know about this medicine.

  • It will not protect you against sexually transmitted diseases.
  • This medicine can increase your risk of problems such as blood clots
  • Some women should not use this medicine because of current medical problems or illnesses. Please read this leaflet to make sure Norethisterone enanthate is right for you.

What is in this leaflet:

  1. What Norethisterone enanthate is and what it is used for
    2. Make sure Norethisterone enanthate is OK for you
    3. How to use Norethisterone enanthate
    4. Possible side effects
    5. How to store Norethisterone enanthate
    6. What is in Norethisterone enanthate and who makes it 
  2. What Norethisterone enanthate is and what it is used for

Norethisterone enanthate is an injectable (depot) contraceptive. It is intended as a short-term method of contraception, for example in women whose partners are undergoing vasectomy, until the vasectomy is effective. It is also for use in women immunised against rubella, to prevent pregnancy while the virus is active.

You use it to stop you getting pregnant.

Norethisterone enanthate contains a type of female sex hormone, called a progestogen.

This hormone stops you getting pregnant by working in three ways: by preventing an egg being released from your ovaries; by making the fluid (mucus) in your cervix thicker, which makes it more difficult for sperm to enter the womb; and by preventing the lining of your womb thickening enough for an egg to grow in it.

The benefits of using Norethisterone enanthate include:

  • it is one of the most reliable reversible methods of contraception if used correctly
  • you only have to remember to visit your doctor after 8 weeks for a second injection
  • it doesn’t interrupt sex

Norethisterone enanthate will not protect you against sexually transmitted infections, such as Chlamydia or HIV. Only condoms can help to do this.

  1. Make sure Norethisterone enanthate is OK for you

It’s important that you understand the benefits and risks of using Norethisterone enanthate before you are given it, or when deciding whether to have a second injection. Although Norethisterone enanthate is suitable for most healthy women it isn’t suitable for everyone.

  • Tell your doctor if you have any of the illnesses or risk factors mentioned in this leaflet.

Before you are given Norethisterone enanthate

  • Your doctor will ask about you and your family’s medical problems, check your blood pressure and exclude the likelihood of you being pregnant. You may also need other checks, such as a breast examination, but only if these examinations are necessary for you, or if you have any special concerns.

While you’re on Norethisterone enanthate

  • Check your breasts and nipples every month for changes – tell your doctor if you can see or feel anything odd, such as lumps or dimpling of the skin.
  • If you need a blood test or other laboratory tests, tell your doctor or the laboratory staff that you are using Norethisterone enanthate, because hormonal contraceptives can affect the results of some tests.
  • If you’re going to have an operation, make sure your doctor knows about it. You may need to avoid having a second injection of Norethisterone enanthate before the operation. This is to reduce the risk of a blood clot (see section 2.1).

2.1 Norethisterone enanthate and blood clots

Norethisterone enanthate may slightly increase your risk of having a blood clot (called a thrombosis), especially in the first year of using it.

A clot in a leg vein – a deep vein thrombosis (or DVT) – is not always serious. However, if it moves up the veins and blocks an artery in the lungs, it can cause chest pain, breathlessness, collapse or even death. This is called a pulmonary embolism and is very rare.

Very rarely, blood clots can also form in the blood vessels of the heart (causing a heart attack) or the brain (causing a stroke). In healthy young women the chance of having a heart attack or stroke is extremely small.

You are more at risk of having a blood clot:

  • as you get older
  • if you smoke
  • if you are seriously overweight
  • if you have some diseases of the heart and blood vessels
  • if you suffer from migraines
  • if you have recently had a baby
  • if you’re off your feet for a long time because of major surgery, injury or illness
  • Tell your doctor if any of these risk factors apply to you. Norethisterone enanthate may not be suitable for you.

Signs of a blood clot include:

  • migraine for the first time, a migraine that is worse than normal or unusually frequent or severe headaches
  • any sudden changes to your eyesight (such as loss of vision or blurred vision)
  • any sudden changes to your hearing, speech, sense of smell, taste or touch
  • pain or swelling in your leg
  • stabbing pain when you breathe
  • coughing for no apparent reason
  • pain and tightness in the chest
  • sudden weakness or numbness in one side or part of your body
  • dizziness or fainting.
  • See a doctor as soon as possible. Do not have a further injection until your doctor says you can. Use another method of contraception, such as condoms, in the meantime.

2.2 Norethisterone enanthate and cancer

Norethisterone enanthate has also been linked to liver diseases, such as jaundice and non-cancer liver tumours, but this is rare. Very rarely, Norethisterone enanthate has also been linked with some forms of liver cancer in women who have used it for a long time.

  • See a doctor as soon as possible if you get severe pain in your stomach, or yellow skin or eyes (jaundice). You may need to stop using Norethisterone enanthate .

2.3 Norethisterone enanthate should not be used by some women

  • Tell your doctor or family planning nurse if you have any medical problems or illnesses.

Do not use Norethisterone enanthate if you have any of the problems listed below. Using Norethisterone enanthate would put your health at risk.

  • If you are pregnant or might be pregnant
  • If you have ever had a problem with your blood circulation. This includes a blood clot (thrombosis) in the legs (deep vein thrombosis), lungs (pulmonary embolism), heart (heart attack), brain (stroke) or any other parts of the body
  • If you have or have ever had severe liver disease, and you have been told by your doctor that your liver function test results are not yet back to normal
  • If you have or have ever had liver tumours
  • If you have severe diabetes affecting your blood vessels
  • If you have very high blood pressure
  • If you have disorders of blood fat (lipidmetabolism
  • If you have or suspect you have cancer affected by sex hormones – such as some cancers of the breast or womb lining or have ever had either of these conditions
  • If you have an inherited disease called porphyria
  • If you are allergic (hypersensitive) to norethisterone enanthate or any of the other ingredients in Norethisterone enanthate (listed in section 6).
  • If you suffer from any of these, or get them for the first time while using Norethisterone enanthate, contact your doctor as soon as possible. It may not be suitable for you to have a second injection of Norethisterone enanthate.

2.4 Norethisterone enanthate can make some illnesses worse

Some of the conditions listed below can be made worse by using Norethisterone enanthate. Or they may mean it is less suitable for you. You may still be able to be given Norethisterone enanthate but you need to take special care.

  • If you have had severe depression
  • If you have ever had liver problems, e.g. jaundice (yellow skin or eyes)
  • If you have any disease that tends to get worse during pregnancy
  • If you have an irregular menstrual pattern together with stomach pains
  • If you have abnormal vaginal bleeding
  • If you have diabetes
  • If you have ever had an ectopic pregnancy or fallopian tube removed.

The main ingredient of Norethisterone enanthate (the progestogen, norethisterone enanthate) is partly converted into the oestrogen, ethinylestradiol. The expected concentration of ethinylestradiol in your body is relatively low compared to taking combined hormonal contraceptives containing ethinylestradiol. This means that although effects similar to those after taking combined hormonal contraceptives containing ethinylestradiol cannot be completely ruled out, experience to date suggests that this may not be the case.

  • Tell your doctor or family planning nurse if any apply to you. Also tell them if you get any of these for the first time after being given Norethisterone enanthate, or if any get worse or come back, because it may not be suitable for you to have a second injection of Norethisterone enanthate.

2.5 Psychiatric disorders

Some women using hormonal contraceptives including Norethisterone enanthate have reported depression or depressed mood. Depression can be serious and may sometimes lead to suicidal thoughts. If you experience mood changes and depressive symptoms contact your doctor for further medical advice as soon as possible.

2.6 Taking other medicines

If you ever need to take another medicine or herbal products at the same time, always tell your doctor, pharmacist or dentist that you’ve been given Norethisterone enanthate. Also check the leaflets that come with all your medicines to see if they can be taken with hormonal contraceptives.

Some medicines can stop Norethisterone enanthate from working properly – for example:

  • certain sedatives (called barbiturates)
  • some medicines used to treat epilepsy
  • some medicines used to treat HIV and Hepatitis C virus infections (so-called protease inhibitors and non-nucleoside reverse transcriptase inhibitors)
  • griseofulvin (an anti-fungal medicine)
  • phenylbutazone (an anti-inflammatory medicine)
  • certain antibiotics
  • St. John’s Wort (a herbal remedy).

If you do need to take one of these medicines, you may need to use extra contraception (for example condoms) for a while. Your doctor, pharmacist or dentist can tell you if this is necessary and for how long.

Norethisterone enanthate can also affect how well other medicines work. For example, if you have diabetes, you may need to take more insulin or other anti-diabetic drugs after being given Norethisterone enanthate. Your doctor will tell you if this is necessary.

2.7 Using Norethisterone enanthate with food and drink

There are no special instructions about food and drink while on Norethisterone enanthate

2.8 Pregnancy and breast-feeding

Pregnancy

You should not be given Norethisterone enanthate if you are pregnant. If you think you might be pregnant, do a pregnancy test to confirm that you are and do not have your second injection.

Breast-feeding

Norethisterone enanthate has not been shown to reduce the amount of milk you produce which is an advantage if you wish to breastfeed your baby. Very small amounts of the hormone are found in breast milk. There is no evidence to suggest that the small amounts of the hormone that appear in the milk are harmful to a healthy baby. However, if your baby has severe or long-lasting jaundice that requires medical treatment you should not breast-feed your baby after having your injection.

2.9 Driving and using machines

Norethisterone enanthate has no known effect on the ability to drive or use machines.

2.10 Norethisterone enanthate contains benzyl benzoate

This medicine contains 333.8 mg benzyl benzoate in each 1 ml ampoule.

Benzyl benzoate may increase jaundice (yellowing of the skin and eyes) in newborn babies (up to 4 weeks old).

  1. How to use Norethisterone enanthate

3.1 How to start

Your doctor or family planning clinic will give you the first injection of Norethisterone enanthate within the first five days of your period (unless you start just after a pregnancy or an abortion). The injection is given into the muscle.

By starting in this way you will have contraceptive protection at once.

3.2 Further injections of Norethisterone enanthate

One injection will give you contraception for 8 weeks. After 8 weeks a second injection can be given. You must make sure that you leave no longer than 8 weeks between injections or contraceptive protection will be lost.

3.3 Starting Norethisterone enanthate after having a baby

Norethisterone enanthate can normally be used straight after having a baby. Your doctor will advise you on when to start.

3.4 Starting Norethisterone enanthate after having a miscarriage or an abortion

You may be able to have an injection immediately. Your doctor will advise you.

3.5 Missed a period – could you be pregnant?

If, when the second injection is due, you have not had a further period since the first injection, it is unlikely that you are pregnant, but the second injection should not be given until pregnancy has been ruled out.

3.6 Being given more Norethisterone enanthate than you should

Overdosage is unlikely but if it does occur no serious ill-effects are expected.

  1. Possible side effects

Like all medicines, Norethisterone enanthate can cause side effects, although not everybody gets them.

  • Tell your doctor, pharmacist or family planning nurse if you are worried about any side effects which you think may be due to Norethisterone enanthate.

4.1 Serious side effects – see a doctor straight away

Signs of a blood clot:

  • migraine for the first time, a migraine that is worse than normal or unusually frequent or severe headaches
  • any sudden changes to your eyesight (such as loss of vision or blurred vision)
  • any sudden changes to your hearing, speech, sense of smell, taste or touch
  • pain or swelling in your leg
  • stabbing pain when you breathe
  • coughing for no apparent reason
  • pain and tightness in the chest
  • sudden weakness or numbness in one side or part of your body
  • dizziness or fainting.

Signs of a severe allergic reaction to Norethisterone enanthate:

  • swelling of the face, lips, mouth, tongue or throat.

Signs of severe liver problems include:

  • severe pain in your upper abdomen
  • yellow skin or eyes (jaundice)
  • inflammation of the liver (hepatitis)
  • your whole body starts itching.
  • If you think you may have any of these, see a doctor straight away. You may need to stop using Norethisterone enanthate.

4.2 Less serious side effects

  • irregular bleeding
  • bloating
  • tender breasts
  • headaches
  • depressive moods
  • dizziness
  • feeling sick
  • putting on weight
  • skin reactions (e.g. pain or itchy rash) at the injection site
  • rarely coughing for no apparent reason, shortness of breath and disturbances of the circulatory system may develop while you are having your injection, or immediately after.
  • Tell your doctor or family planning nurse if you are worried about any side effects which you think may be due to Norethisterone enanthate. Also tell them if any existing conditions get worse while you are using Norethisterone enanthate.

Reporting of side effects

If you get any side effects, talk to your doctor, family planning nurse or pharmacist. This includes any possible side effects not listed in this leaflet.

By reporting side effects you can help provide more information on the safety of this medicine.

  1. How to store Norethisterone enanthate

Keep this medicine out of the sight and reach of children.

Norethisterone enanthate should not be used after the expiry date which is stated on the packaging. The expiry date refers to the last day of that month.

Store below 25°C. Protect from light.

  1. What is in Norethisterone enanthate and who makes it

What is in Norethisterone enanthate

The active substance is norethisterone enanthate.

Each ampoule of Norethisterone enanthate contains 200mg of the progestogen norethisterone enanthate in 1ml of oily solution for injection into a muscle.

The other ingredients are benzyl benzoate and castor oil for injection.

What Norethisterone enanthate looks like and contents of the pack

Norethisterone enanthate is a solution for intramuscular injection; the injection is given into the muscle.

Norethisterone enanthate is supplied in single packs of 1 ampoule.

  1. MANUFACTURED IN INDIA BY:
    TAJ PHARMACEUTICALS LTD.
    Mumbai, India
    Unit No. 214.Old Bake House,
    Maharashtra chambers of  Commerce Lane,
    Fort, Mumbai – 400001
    at:Gujarat, INDIA.
    Customer Service and Product Inquiries:
    1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
    Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
    E-mail: tajgroup@tajpharma.com