Active ingredients: Gestodene, Ethinylestradiol
ESTINETTE 75 micrograms / 20 micrograms coated tablets
Why is Estinette used? What is it for?
Estinette is a combined oral contraceptive pill and belongs to a group of medicines often called Pills. Estinette contains two types of hormones: an estrogen, ethinyl estradiol, and a progestin, gestodene. These hormones prevent the ovaries from producing an egg every month (ovulation). They also thicken the fluid (mucus) in the cervix ( cervix), making contact between sperm and egg more difficult. Finally, they alter the lining of the uterus to make it more difficult for a fertilized egg to settle.
Medical research and extensive experience show that, when taken correctly, the Pill is an effective and reversible method of contraception. Remember that combined oral contraceptive pills such as Estinette do not protect against sexually transmitted diseases (such as AIDS); only the condom can help protect you from these diseases.
YOU AND THE PILL
How your body prepares for pregnancy (the menstrual cycle).
You can usually get pregnant (ie conceive) from the time you start to menstruate (this usually happens during adolescence), until you stop having your period (ie go through menopause). Each menstrual cycle lasts approximately 28 days, and approximately In the middle of this cycle, one of the ovaries produces an egg, which passes into one of the two fallopian tubes.This procedure is called ovulation.
The egg travels down the tube to the uterus. When you have intercourse, millions of sperm come out of your partner's penis. From the vagina, these sperm pass through the uterus to the fallopian tubes, and if one tube contains an egg and a sperm reaches it, you can get pregnant. This process is called "conception." Once fertilized, the egg settles in the lining of the uterus and grows into a baby within nine months. Since eggs can live for up to two days, while sperm survive for up to five days, you can get pregnant by having intercourse for up to five days before ovulation, and for some time after ovulation. If the egg is not fertilized by a sperm, at the end of the menstrual cycle the body eliminates it together with the lining of the uterus, with "menstruation".
How do natural hormones work?
Your menstrual cycle is controlled by two sex hormones produced by the ovaries: estrogen and progesterone (a progestin). Estrogen levels rise in the first half of the menstrual cycle and cause the uterus to produce a thick, ready-to-wear lining. receive the egg if conception occurs. Progesterone acts later during the menstrual cycle and changes the lining of the uterus to prepare it for pregnancy.
If she does not get pregnant, she will produce less of these hormones and the lining of the uterus will break down. As mentioned above, the lining of the uterus is cleared from the body with menstruation. If instead she does conceive, the ovaries and placenta (which keeps the fetus connected to the uterus and feeds it) continue to produce progesterone and estrogen to prevent the ovaries from secreting more eggs. In other words, while you are pregnant you will not be able to ovulate or menstruate.
How does the pill work?
Combined contraceptive pills, such as Estinette, contain hormones similar to those produced by your body (estrogen and progestin). These hormones help her not to get pregnant, just like her natural hormones prevent her from conceiving again when she is already pregnant.
The combined contraceptive pill protects you in three ways from a possible pregnancy.
- There will be no fertilizable egg from the sperm.
- The fluid inside the cervix thickens, making it more difficult for sperm to penetrate.
- The lining of the uterus does not thicken enough to allow the egg to grow.
Contraindications When Estinette should not be used
Do not take Estinette
Do not use Estinette if you suffer from any of the conditions listed below. If you have any of these conditions you should tell your doctor, who may decide that Estinette is not suitable for you and recommend another method of birth control.
Tell your doctor
- if you have ever suffered from a blood circulation disorder called thrombosis (for example: having blood clots in the legs, lungs, heart, brain, eyes or other parts of the body);
- if you have ever had a heart attack or angina (severe chest pain), or a stroke (for example a sudden weakness or tingling on one side of the body);
- if you or a close family member have a medical condition that puts you at an increased risk of developing blood clots (see also section "The Pill and Thrombosis");
- if you suffer from diabetes with vascular disorders;
- if you have or have ever suffered from an eye disorder due to a circulatory disease;
- if you have high blood pressure (hypertension);
- if you have or have ever suffered from liver disease;
- if you have or have ever had liver cancer;
- if you have breast cancer or other cancers, for example of the ovaries, cervix or uterus;
- if you have unusual bleeding from the vagina;
- if you have or have ever suffered from migraines;
- if you are allergic (hypersensitive) to gestodene, ethinyl estradiol or any of the other ingredients of Estinette;
- if you are pregnant or think you are pregnant.
If you suffer from any of these while taking Estinette, stop taking the pills and contact your doctor immediately. In the meantime, use another method of contraception, such as a condom or diaphragm plus a spermicide.
Precautions for use What you need to know before taking Estinette
Regular checks
Before you start taking Estinette, your doctor will need to ask you about your medical history, asking you a few questions about yourself and other members of your family. In addition, your doctor will measure your blood pressure and rule out that you are pregnant. Your doctor may also have you examined. When you have started taking Estinette, you will need to go to your doctor again for regular check-ups, which will happen when you visit your doctor to request more packs of pills.
It is advisable to repeat this medical examination at least once a year while using Estinette.
The first follow-up visit should be performed 3 months after the prescription of Estinette. At each annual visit, the review should include the procedures that were performed at the initial visit, as described above.
Tell your doctor immediately ...
if you suffer from any of the following conditions while taking Estinette. Also, don't take any other pills before talking to your doctor. In the meantime, use another method of contraception, such as a condom or diaphragm plus a spermicide.
If you are suffering from migraines for the first time, or if you have suffered from it in the past but now the attacks are stronger or more frequent than before.
If you experience symptoms of a blood clot (see also section "The Pill and Thrombosis"). These symptoms include:
- unusual leg pain or swelling;
- sudden severe pain in the chest, which may radiate to the left arm;
- sudden shortness of breath or difficulty breathing;
- sudden fit of cough, for no apparent reason;
- unusual, severe or long-lasting headache;
- any sudden changes in vision (such as loss of vision, or blurred vision);
- indistinct words or any other difficulty in speaking;
- dizziness (spinning sensation);
- dizziness, fainting or convulsions;
- sudden weakness or numbness of only one side of the body;
- difficulty moving (also called motor disturbances), or
- severe abdominal pain (also called acute abdomen).
Surgery or hospitalization period (inability to move as usual). You must stop taking Estinette at least four weeks before a major scheduled surgery (for example a "stomach operation), or in the case of leg surgery. Also stop taking Estinette if you have to stay in bed for long periods. (for example after an accident or surgery, or if your leg is in a cast.) Taking the pill should not be resumed for 2 weeks after complete remobilization. Your doctor will tell you when to start taking Estinette again.
If you suspect you are pregnant.
Tell your doctor before you start taking Estinette ...
if you know you have any of the following ailments. In this case you should tell your doctor, as these problems may get worse when you take the pill. If any of these conditions get worse, or if it occurs for the first time, tell your doctor as soon as possible. Your doctor may ask you to stop using Estinette and recommend another method of contraception.
If you or a member of your family have a blood fat (lipid) disorder called hypertriglyceridaemia, as it may increase the risk of a pancreatic disease called pancreatitis.
If you suffer from:
- high blood pressure (hypertension);
- yellowing of the skin (jaundice);
- itching all over the body;
- gallstones;
- an inherited disease called porphyria;
- systemic lupus erythematosus - SLE (an inflammatory disease that can affect various parts of the body, including the skin, joints and internal organs);
- a blood disorder called hemolytic uremic syndrome - HUS (in which blood clots cause kidney failure);
- a movement disorder called Sydenham's chorea;
- the rash called gestational herpes;
- the hereditary form of deafness called otosclerosis;
- liver function disorders;
- diabetes;
- depression;
- Crohn's disease or ulcerative colitis (both chronic inflammatory bowel diseases);
- dark spots on the face and body (chloasma), which can be alleviated by not exposing yourself to the sun and not using sunbeds or sunlamps
The pill and thrombosis
Some studies have suggested a slightly higher risk for women who use the combined pills of various circulation disorders than for women who do not take these pills. These disorders can lead to thrombosis, which is the appearance of a blood clot that could block a blood vessel. It is possible for a clot to form in a vein (venous thrombosis) or in an "artery (arterial thrombosis). Most clots are treatable, with no long-term danger, however a thrombosis can cause serious permanent disability or death - although this happens in very rare cases.
Sometimes blood clots form in the deep veins of the legs (deep vein thrombosis). If the clot subsequently detaches from the veins in which it has formed, it could travel to the arteries of the lungs, occluding them and causing a "pulmonary embolism".
In very rare cases, blood clots also form in the blood vessels of the heart (resulting in a heart attack) or in the brain (resulting in a stroke). In extremely rare cases, blood clots can form in other parts of the body, such as the liver, intestines, kidneys or eyes.
Blood clots can also form in women who do not take the pill, and also when they become pregnant. The risk is higher among women who take the pill than those who do not, but it is still lower than the risk during pregnancy. Thrombosis is more likely to occur in the first year of taking combined contraceptive pills.
Among women who take Estinette, there are about 30 to 40 cases of thrombosis per 100,000 women each year.
Among pregnant women there are about 60 cases of thrombosis every year for every 100,000 pregnancies. Symptoms of a blood clot formation are listed in the "Tell your doctor immediately if ..." section.
If you notice possible signs of a thrombosis, stop taking the pill and contact your doctor immediately. In the meantime, use another method of contraception, such as a condom or diaphragm plus a spermicide.
Also remember that some factors can increase the risk of thrombosis. These factors include:
- age (the risk of heart attack or stroke increases with age);
- smoking (the risk of thrombosis increases if you smoke a lot, and also with progressive aging). If you use the pill, stop smoking, especially if you are over 35 years old;
- an illness suffered by a close family member caused by blood clots, or a heart attack or stroke;
- if you are very overweight (obese);
- if you have a disturbance in the metabolism of fats in the blood (lipids) or other very rare blood disorders;
- if you have high blood pressure (hypertension);
- if you have a cardiovalvular disorder, or a certain heart rhythm disorder;
- if you have recently had a baby (the risk of thrombosis increases after delivery);
- if you have diabetes mellitus;
- if you have systemic lupus erythematosus - SLE (an inflammatory disease which can affect various parts of the body, including the skin, joints and internal organs);
- if you have a blood disorder called haemolytic uremic syndrome - HUS (in which blood clots cause kidney failure);
- if you have Crohn's disease or ulcerative colitis (both chronic inflammatory bowel diseases);
- if you have sickle cell anemia (Mediterranean anemia);
- if you are suffering from migraines for the first time, or if the migraine that you used to have in the past gets worse or occurs more often than before;
- if you are undergoing major surgery, any operation on your legs, or if you are unable to move normally.
The risk of deep vein thrombosis increases temporarily after surgery or when you cannot move freely (for example if you have one or both legs in a cast or splint). If you take the Pill, the risk may be higher. Tell your doctor that you take the pill long before you plan to be hospitalized or have surgery. Your doctor may ask you to stop taking the pill several weeks before or after surgery. If you do not have time to do so, your doctor may give you a medicine to reduce the risk of thrombosis. Your doctor will also tell you when to start over. to take the pill when she has recovered her strength.
The pill and cancer
Some studies have found a possible increased risk of cervical cancer with long-term use of the pill. This increased risk may not be due to the pill, but rather to the effects of sexual behavior and other circumstances.
All women are at risk for breast cancer, even if they don't take the pill. This cancer rarely affects women under the age of 40, and has been found to a slightly greater extent in women who take the Pill than their peers who do not take the Pill. If you stop the pill this risk is reduced, and 10 years after stopping the pill there is an equal incidence of breast cancer among women who took the pill and those who never took it. Since breast cancer is rare in women under the age of 40, the increase in the number of diagnosed cases of breast cancer in women who take the Pill and who have taken it in the past is low compared to the risk of cancer. of the breast throughout the entire life.
In rare cases, the use of the Pill has resulted in liver disease, such as jaundice and benign liver tumors. In very rare cases the Pill has been associated with some forms of malignant liver tumors (cancer) in women who use it for a long time. liver tumors can cause life-threatening intra-abdominal haemorrhages (bleeding into the abdomen). If you experience pain in the upper abdomen that does not improve in a short time, please tell your doctor. Also see your doctor if you notice yellowing of the skin (jaundice).
Interactions Which drugs or foods can modify the effect of Estinette
Taking Estinette with other medicines
Tell your doctor or pharmacist if you are taking or have recently taken any other medicines, even those obtained without a prescription. Some medicines may interfere with how Estinette works. If you take any other medicines while using Estinette, be sure to tell your doctor (or your dentist if you are prescribed antibiotics.) Your doctor (or dentist) can tell you if and for how long you need to use additional contraceptive measures.
Medicines that can sometimes affect the way Estinette works are:
- antibiotics (such as ampicillin, tetracycline and rifampicin);
- medicines for epilepsy or other nervous system diseases, such as primidone, carbamazepine, oxcarbazepine, phenytoin, topiramate, hydantoins or barbiturates (such as phenobarbitone);
- ritonavir and nevirapine medicines used for HIV infection);
- griseofulvin (a medicine prescribed for fungal infections (mycosis));
- Medicines for the treatment of inflammation (phenylbutazone, dexamethasone, felbamate); the herbal remedy commonly called St. John's wort (Hypericum perforatum).
Some medicines can affect the levels of ethinylestradiol in the blood:
- atorvastatin (medicine to treat high levels of fat in the blood)
- C vitamin
You may also need to use an alternative method of birth control, such as a condom, while taking these medicines and for another seven days after you stop taking them. Your doctor may advise you to use these additional precautions for a longer period.
If you are taking antibiotics, always ask your doctor for advice about the need for extra precautions. Always say you are taking the combined pill when prescribed any medicine.
The herbal remedy called St John's Wort (Hypericum perforatum) may affect the action of oral contraceptives and should not be taken at the same time as this medicine. If you are already using a preparation based on St John's Wort, stop taking it and tell the doctor at the next visit.
Estinette can affect the effects of other medicines, such as cyclosporine and lamotrigine; in these cases, consult your doctor.
Taking Estinette with food and drink
The intake of food and drink has no influence on the contraceptive effect of the pill.
Warnings It is important to know that:
Pregnancy and breastfeeding
Pregnancy
If you suspect that you are pregnant, stop taking Estinette and contact your doctor immediately. Until you talk to your doctor, use a different method of contraception, such as a condom or diaphragm plus a spermicide. Ask your doctor or pharmacist for advice before taking any medicine.
Feeding time
Ask your doctor or pharmacist for advice before taking Estinette. Do not take Estinette while breastfeeding your baby.
Driving and using machines
The effects of Estinette on the ability to drive or use machines have not been studied.
Important information about some of the ingredients of Estinette
Estinette contains lactose and sucrose.
If in the opinion of your doctor you have an "intolerance to some sugars, talk to your doctor before taking this medicine.
Before undergoing blood tests
Tell your doctor or laboratory staff that you are taking the pill, as oral contraceptives can affect the results of some tests.
Dose, Method and Time of Administration How to use Estinette: Posology
Always take Estinette exactly as your doctor has told you. If in doubt you should consult your doctor.
This pack is designed to help you remember to take your pills.
How to start the first pack
You take the first pill on the first day of your period. This is the first day of your period, which is when bleeding begins.
If you start the pill between day 2 and day 5 of your period, also use a second method of contraception, such as a condom, for the first 7 days of using the pill. However, this only applies to the first pack.
You can take the pill at any time, but take it around the same time every day. Perhaps it will be easier to take it before bedtime, or when you wake up in the morning.
Take one pill every day, following the order indicated on the package, until the entire pack of 21 pills is finished.
After taking all 21 pills, stop for seven days. You will probably have bleeding in some of these seven days.
There is no need to use other methods of contraception during the 7 days of not taking the pill, as long as the 21 pills have been taken correctly and the next pack is started without delay.
Move on to the next pack
After seven days without taking any pills, start the next pack. Do this even if the bleeding hasn't stopped yet. A new pack should always be started on the same day of the week.
How to switch to Estinette from another combined hormonal contraceptive
Start taking Estinette the day after taking the last tablet from the current pack (or the day after taking the last active tablet, if the current pack also contains inactive tablets), but no more than one day after. the normal tablet-free interval, or after the period of inactive tablet-taking, with the previous pill.
How to switch to Estinette from a progestogen-only product (progestogen-only pills, injection, implant)
You can stop taking the progestogen-only pills (POPs) at any time and start Estinette the next day, at the same time. However, when switching from injections to Estinette, start taking Estinette on the day you should have given the next injection. When switching from contraceptive implant to Estinette, start Estinette on the day the implant is removed. In all these cases, also use an additional barrier method of contraception in the first 7 days of taking the pills.
How to start after childbirth, or after a spontaneous or surgical abortion
After childbirth or after a surgical or spontaneous abortion, the doctor will advise the suitability of using the pill.
You can start taking Estinette right after a miscarriage or surgical abortion that occurs in the first trimester of pregnancy. In this case, no additional contraceptive measures need to be taken.
In the event of delivery or abortion in the second trimester of pregnancy, use of Estinette may begin 21-28 days later. It is not recommended to take a combination pill while breastfeeding, as it may reduce milk. Use a different method of contraception (such as a condom) in the first 7 days of taking the pill. If you have had unprotected intercourse, do not start taking Estinette until the start of your period, or until pregnancy can be ruled out. If you are unsure about the use of Estinette after childbirth or after an abortion, consult your doctor or pharmacist.
Overdose What to do if you have taken an overdose of Estinette
If you take more Estinette than you should
If you take more Estinette than you should, it is unlikely that it will harm you, however you may feel nauseous, suffer from vomiting or have vaginal bleeding. If you get any of these symptoms, talk to your doctor, who will be able to tell you if anything needs to be done.
If you forget to take Estinette
If you forget to take a pill, please follow the instructions below.
If you have forgotten to take a pill for 12 hours or less
Contraceptive protection should not be reduced if you take the missed pill immediately and then continue taking the next ones as usual. This could mean taking two pills on the same day.
If you have forgotten to take a pill for more than 12 hours, or if you have forgotten more than one pill
If you have forgotten to take a pill for more than 12 hours, or if you have missed more than one pill, your contraceptive protection may be reduced and you need to use additional protection. The more pills you skip, the greater the risk of compromised contraceptive protection. In this case, follow the instructions for daily use:
What to do if you forget to take a pill in the first week
Take the last missed pill as soon as you remember, even if it means taking 2 pills together. Then continue taking the pills at the usual time. Also use a barrier method of contraception, eg a condom, for the next 7 days If you have had sexual intercourse in the previous 7 days, you should consider the possibility of pregnancy The more pills you forget and the closer you get to the withdrawal period, the higher the risk of pregnancy.
What to do if you forget to take a pill during the second week
Take the last missed pill as soon as you remember, even if it means taking 2 pills together. Then continue taking the pills at the usual time. As long as you have taken the pills correctly in the 7 days before the missed pill, do not you will need to use additional contraceptive measures If not, or if you have missed more than 1 pill, use another method of contraception for 7 days.
What to do if you miss a pill during the third week
The risk of missed contraceptive protection is greater due to the approaching no-tablet interval. However, reduced contraceptive protection can be prevented by following one of the two alternatives below. There is no need to follow additional contraceptive precautions, as long as all tablets have been taken correctly in the 7 days preceding the first missed tablet.
However, if Estinette has not been taken correctly in the 7 days preceding the first missed tablet, follow the first of the two alternatives and also use a barrier method (such as a condom) for the next 7 days.
- Take the last missed pill as soon as you remember, even if it means taking 2 pills together. Continue taking the pills at the usual time. Start the next pack immediately after taking the last pill in the current pack, ie without leaving any interval between packs. It is unlikely that you will have a withdrawal bleed before finishing the second pack, however you may notice a few drops of blood or bleeding on the days you take the pills.
- Stop taking the pills from the current pack. Thereafter, a tablet-free period of 7 days should be observed, including those in which the pills have been forgotten, before continuing with the next pack.
If you have missed any pills and no withdrawal bleeding starts during the first normal pill withdrawal interval, consider the possibility of pregnancy.
If you have forgotten to take a pill (or several pills) and have had unprotected intercourse, pregnancy is possible. Ask your doctor or pharmacist about emergency contraception.
If you stop using Estinette
If you stop taking Estinette, you could become pregnant. Discuss with your doctor other methods of contraception to avoid becoming pregnant.
What to do in case of vomiting or diarrhea
If you have vomiting or diarrhea within 3-4 hours of taking the pill, the active ingredients it contains may not be fully absorbed by the body. In this case, follow the above advice regarding forgotten tablets. In case of vomiting or diarrhea, use extra contraceptive precautions, such as condoms, for all intercourse while suffering from stomach pain, and for the next seven days.
What to do if you want to delay or move your period
If you want to delay or shift your period, contact your doctor for advice.
If you want to delay menstruation
Continue with the next pack of Estinette after taking the last tablet in the current pack, without interruption. You can take the desired number of tablets from the next pack, up to the end of the second blister. When using the second pack, you may notice bleeding or a few drops of blood. At the end of the usual 7-day no-intake interval, you start taking Estinette again in the normal way.
If you want to move your period to a different day of the week
If Estinette is taken correctly, your period will always occur on the same day of the month. If you want to move them to another day of the week, instead of the day you are used to with your current pill intake, you can shorten (but never extend) the upcoming no-tablet interval by the desired number of days. . For example, if your period normally starts on a Friday and you want to have it on a Tuesday (ie three days earlier), start the next pack of Estinette three days early. The shorter the tablet-free interval, the more likely you are to have a withdrawal bleed, as well as bleeding or a few drops of blood during the second pack.
Side Effects What are the side effects of Estinette
Like all medicines, Estinette can cause side effects, although not everybody gets them.
The following serious side effects have been reported by women using COCs - see section 2 under "The Pill and Thrombosis" and "The Pill and Cancer".
- Venous thromboembolism (presence of a blood clot in the vessels)
- Arterial thrombotic disorders (occlusion of an "artery)
- Cervical cancer (cervical cancer)
REASONS TO IMMEDIATELY STOP THE USE OF EXTINETTE
If you suffer from any of the following while using Estinette, stop taking it and tell your doctor immediately. In the meantime, use another non-hormonal method of contraception, such as a condom.
- Migraine never suffered before, or attacks more frequent or stronger than the migraine you already suffered
- Unusually severe headache, or one that occurs more often than before
- Sudden changes in vision, or vision problems or difficulty speaking
- Unusual pain or swelling of the legs sharp twinges in the chest or sudden shortness of breath; very severe pain or tightness in the chest; persistent cough or bloody cough
- Numbness in an arm or leg
- Yellowing of the skin (jaundice)
- Significant increase in blood pressure
- Change in blood lipid (fat) levels
- Pregnancy
- A sharp worsening of ailments that had worsened during a previous pregnancy, or when she took the pill in the past
- Severe abdominal pain.
These side effects have been reported by women taking the Pill and can occur in the first few months after starting to use Estinette, although they usually go away as the body gets used to the pill. Very common side effects (more than 1 in 10 women) are: irregular menstruation, and headache Common (in 1 or more women in 100, but in less than 10 women in 100): depression, irritability, acne, absent or reduced menstruation, painful menstruation, inflammation vagina, fluid retention, changes in interest in sex (increase or decrease), nervousness, eye irritation, visual disturbance, dizziness, nausea, vomiting, abdominal pain, hypersensitive breasts, weight change, change in secretions vaginal and migraine.
Uncommon (in 1 or more in 1000 women, but less than 1 in 100 women) and rare (in 1 or more in 10,000 women, but less than 1 in 1000 women): appearance of brown spots on the face and body (chloasma), high blood pressure, breast cancer, cervical cancer, blood clot, increased fat levels in the blood, decreased folate levels in the blood, hearing problems (otosclerosis), intolerance to contact lenses, liver, systemic lupus erythematosus (SLE, a disease affecting the connective tissue, allergic reactions (angioedema), changes in appetite, sugar intolerance (increased blood sugar level), stomach cramps, excessive hair growth (for e.g. on the chest, face and shoulders), jaundice (yellowing of the skin and whiteness in the eyes), skin irritation, swelling, hair loss.
In case of very severe allergic reactions with very rare cases of hives, painful swelling of the skin and mucous membranes (angioedema) and respiratory and circulatory symptoms, contact your doctor immediately.
Very rare (less than one in 10,000 women): porphyria (hereditary disease in which the body cannot break down hemoglobin properly), chorea (a motor disease), eye disorders (for example, blood clot in the veins of the eyes) , varicose veins, inflammation of the pancreas, inflammation of the intestines, gallstones, colicyst disease, erythema multiforme (rash), haemolytic-uremic syndrome (blood disorder).
Frequency not known: inflammatory bowel disease (Crohn's disease), ulcerative colitis (inflammation of the bowel walls accompanied by the formation of ulcers), liver dysfunction, liver cell lesions.
If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.
Expiry and Retention
Keep Estinette out of the reach and sight of children.
Store below 25 C.
Store in the original package in order to protect from light and humidity
Do not use Estinette after the expiry date which is stated on the carton after the abbreviation EXP.
The expiry date refers to the last day of the month.
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.
Composition and pharmaceutical form
What Estinette contains
The active substances are: 75 micrograms of gestodene and 20 micrograms of ethinylestradiol in each coated tablet.
The excipients are:
Tablet: Sodium calcium edetate, Magnesium stearate, Silica colloidal anhydrous, Povidone K-30, Corn starch, Lactose monohydrate
Coating: Quinoline Yellow (E104), Povidone K-90, Titanium Dioxide (E171), Macrogol 6000, Talc, Calcium Carbonate (E170), Sucrose
Description of what Estinette looks like and contents of the pack
Light yellow, round, biconvex and sugar coated tablets, without imprint.
Packaging:
Blister: PVC / PVDC / aluminum.
Blister pack: PVC / PVDC / aluminum in PETP / aluminum / PE bag.
Sales formats: 1 x 21 tablets; 3 x 21 tablets; 6 x 21 tablets.
Not all pack sizes may be marketed.
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT
ESTINETTE GESTODENE 75 MCG / ETINYLESTRADIOL 20 MCG TABLETS
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains 75 micrograms of gestodene and 20 micrograms of ethinylestradiol.
For the full list of excipients, see section 6.1.
03.0 PHARMACEUTICAL FORM
Coated tablet.
Pale yellow, round, biconvex, sugar-coated tablets without imprint.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Oral contraception.
04.2 Posology and method of administration
How to take Estinette
The tablets should be taken in the order indicated on the pack, each day at approximately the same time. One tablet is taken every day, for 21 consecutive days. Each subsequent pack is started after a 7-day tablet-free period. and during which withdrawal bleeding occurs. Bleeding usually starts on the 2nd or 3rd day after taking the last tablet and may not finish before the next pack is started.
How to start taking Estinette
If you have not used hormonal contraceptives in the last month
The woman should take the first tablet on the 1st day of her normal cycle (i.e. the first day of her period). It is possible to start taking the tablets also between the 2nd and 5th day of the menstrual period, however during the first cycle it is recommended to use an additional barrier method of contraception in the first 7 days of taking the tablets.
If you were previously taking another combined hormonal contraceptive [COCJ
The woman should start taking Estinette the day after "taking" the last active hormone tablet from the previous pack, but in any case no later than the day after the usual no-active tablet interval, or the placebo tablet-taking period, with the previous oral contraceptive.
If you previously took a progestogen-only contraceptive (progestogen-only pills, injection, implant)
The woman can switch from progestogen-only pills [POP] to Estinette on any day. The first tablet should be taken the day after taking a tablet from the pack of POP pills. In the case of changing from an implant to Estinette, you should start Estinette on the same day as the implant is removed. In the case of switching from injections to Estinette, you must start Estinette on the date the new injection would be given. In any case, it is recommended to use an additional barrier method of contraception in the first 7 days of taking the tablets.
After spontaneous or procured abortion in the first trimester
The woman can start taking the tablets immediately. In this case, no additional contraceptive measures are necessary.
After childbirth, or after spontaneous or procured abortion in the second trimester
For breastfeeding women, see section 4.6.
It is advisable to start taking the tablets between the 21st and 28th day after delivery, in the case of women who are not breastfeeding, or following the miscarriage or procured in the second trimester. If taking it starts later, advise to use an additional barrier method of contraception in the first 7 days of taking the tablets. However, if the woman has already had sexual intercourse, rule out pregnancy before starting to take the tablets; alternatively, you will have to wait until your first menstrual cycle.
If you forget to take the tablets
If the woman forgets to take a tablet for less than 12 hours, there is no reduction in contraceptive efficacy. The woman should take the tablet as soon as she remembers, then continue taking the other tablets at the usual time.
If the delay exceeds 12 hours, contraceptive efficacy may be impaired. To take missed tablets, it may be helpful to rely on these two rules.
1. Do not delay tablet-taking by more than 7 days.
2. To have adequate suppression of the hypothalamic-pituitary-ovarian axis it is necessary to take the tablets continuously for 7 days.
Based on the above, the following practical recommendation can be made:
Week 1
The woman should take the last missed tablet as soon as she remembers, even if this means that she has to take 2 tablets at the same time. After that, she will need to continue taking the tablets at the usual time each day. The woman will need to use an additional barrier method of contraception, such as a condom, for the next 7 days. If the woman has had sexual intercourse during the previous 7 days, pregnancy cannot be ruled out. The more tablets you forget and the closer you get to your monthly tablet-free interval, the higher the risk of pregnancy.
Week 2
The woman will need to take the last missed tablet as soon as she remembers, albeit
this means having to take 2 tablets at the same time. Thereafter, she will need to continue taking the tablets at the usual time each day. Provided that the woman has taken the tablets correctly in the 7 days preceding the missed tablet, she will not need to use additional contraceptive measures. If not, or if the woman has forgotten to take more than 1 tablet, it is recommended to additionally use a contraceptive method for a period of 7 days.
Week 3
The risk of reduced safety becomes imminent as the tablet-free interval approaches. However, it is possible to adjust the reduced contraceptive protection by adjusting the intake of the tablets. In other words, if you stick to one of the following two alternatives you will not need to take additional contraceptive measures, as long as you have taken all the tablets correctly within 7 days before the first missed tablet. If not, advise the woman on the first of the two alternatives. Also, recommend the simultaneous use of another contraceptive method for 7 days.
1. The woman should take the last missed tablet as soon as she remembers, even if this means that she has to take 2 tablets at the same time. Thereafter, she should continue to take the tablets at the usual time each day. The woman should start the next pack of tablets immediately after taking the last tablet in the current pack, ie without leaving any gap between packs. The woman is unlikely to have a period until the entire second pack is taken. However, you may notice spotting or withdrawal bleeding on the days you take the tablets.
2. The woman may also be advised to discontinue the tablets in the current pack. In this case, ask her to observe an interval of up to 7 days without tablets, including the days when she forgot to take them, and then continue with the next pack.
If the woman has forgotten to take tablets and does not menstruate in the first normal tablet-free interval, consider the possibility of pregnancy.
Advice in case of vomiting / diarrhea
If the woman vomits within 3-4 hours of taking a tablet, the tablet may not have been fully absorbed by the body. In this case, follow the precautions above for missed tablets. Diarrhea may also reduce. the effectiveness, preventing the total absorption of the contraceptive. If the woman does not wish to change her usual tablet intake, she will need to take the required tablet (s) from another pack.
How to anticipate or delay menstruation.
Only in exceptional cases, it is possible to delay menstruation in the way described below.
To delay her period, the woman will have to continue taking Estinette by switching from one pack to the other, with no tablet-free interval. You can continue to delay your period as desired, until the second pack is finished but no later than. during this period the woman may experience spotting or withdrawal bleeding. Estinette should be resumed regularly at the end of the usual 7-day no-dose interval.
To shift her period to a different day than expected with the current tablets, the woman can be advised to shorten the upcoming no-tablet interval as desired. The shorter this interval, the greater the risk of not having a period. but breakthrough bleeding or spotting while taking the tablets in the next pack (this also occurs when menstruation is delayed).
04.3 Contraindications
Do not use a combined oral contraceptive [COC] in the presence of the following conditions. If any of these disorders first appear while taking a CHC, stop taking it immediately:
- Current or previous venous thromboembolism (deep vein thrombosis, embolism
pulmonary), with or without risk factors (see section 4.4)
- Current or previous arterial thromboembolism, particularly myocardial infarction or cerebrovascular disorder (see section 4.4)
- Considerable or multiple risk factors for venous or arterial thrombosis (see section 4.4)
- symptoms Previous prodromal symptoms of thrombosis (e.g. transient cerebral ischemia, angina pectoris)
- Cardiovascular disorders, i.e. heart disease, valvulopathy, arrhythmic disorders
- Severe hypertension
- Diabetes complicated by micro- or macro-angiopathy
- Ocular disorder of vascular origin
- Known or suspected breast cancer
- Known or suspected malignant neoplasms involving the endometrium or other estrogen-dependent neoplastic disorders
- Recent or severe liver problems, if liver function tests are not brought to normal
- Benign or malignant hepatic neoplasms, current or previous
- Undiagnosed vaginal bleeding
- Migraine with focal neurological symptoms
- Known or suspected pregnancy (see section 4.6)
- Hypersensitivity to the active substances or to any of the excipients
04.4 Special warnings and appropriate precautions for use
Evaluation and physical examination before taking oral contraceptives
Before starting or resuming treatment with a COC, obtain a complete personal and family medical history and rule out that there is a current pregnancy. Measure blood pressure and perform a physical examination, if clinically indicated, on the basis of contraindications (see section 4.3) and warnings (see under "Warnings" in this section). Ask the woman to read the package leaflet carefully and follow the advice contained. Base the frequency and nature of further periodic checks on the lines guide of established practice and adapt them to the individual patient.
Warnings
General
Inform women that COCs do not protect against HIV (AIDS) or sexually transmitted infections (STIs).
Cigarette smoking increases the risk of serious cardiovascular effects with the use of COCs. This risk increases with age and the number of cigarettes smoked, particularly in women over the age of 35. Strongly advise all women taking COCs to refrain from smoking. For smokers over 35 years of age, consider other methods of contraception.
In the presence of any of the risk factors listed below, weigh the advantages of using the COC against the possible risks on a case-by-case basis. Discuss the situation with the woman before starting the oral contraceptive. In case of worsening of symptoms, or if one of the aforementioned disorders or risk factors arises, advise the woman to contact the doctor, who will decide if it is appropriate to stop taking the COC.
Circulatory disorders
The use of any COCs increases the risk of venous thromboembolism (VTE), compared to women who are not taking this type of contraceptive. The risk of excess VTE peaks in the first year of taking COCs. This increased risk is lower than the risk of VTE associated with pregnancy, which is estimated to be 60 in 100,000 pregnancies. VTE is fatal in 1-2% of cases.
Numerous epidemiological studies show an increased risk of VTE for patients taking combined oral contraceptives containing ethinylestradiol, particularly at doses of 30 micrograms, plus a progestin, such as gestagen, compared to patients taking combined contraceptives containing less than 50 micrograms of ethinyl estradiol and the levonorgestrel progestin.
For COCs containing 30mcg ethinylestradiol plus desogesrel or gestodene a total relative risk of between 1.5 and 2.0 for VTE is calculated compared to COCs containing less than 50mcg ethinylestradiol plus levonorgestrel. The approximate frequency of VTE with the combination of combined oral contraceptives containing levonorgestrel and ethinylestradiol less than 50 mcg is about 20 cases per 100,000 women / years of use. In the case of Estinette, this frequency is about 30-40 cases per 100,000. women / years of use, ie an increase of 10-20 cases per 100,000 women / years of use. The influence of relative risk on the number of additional cases will touch the maximum for patients using COC for the first time, in the first year of use, or when the risk of VTE reaches its maximum for any type of combined contraceptive pill.
Very rare cases of thrombosis affecting other vessels have been reported among women taking oral contraceptives, eg hepatic, mesenteric, renal or retinal veins and arteries. There is no consensus on the relationship between these cases and the use of COCs.
The risk of venous thromboembolism increases with:
- The advancing age.
- Positive family history (eg. Venous thromboembolism in siblings or parents, at a relatively early age). In case of suspected hereditary predisposition, the woman should be referred to a specialist before deciding whether or not to use the oral contraceptive .
- Obesity (body mass index over 30 kg / m2).
- Prolonged immobility, major surgery, lower limb surgical procedure or major trauma. In these cases it is advisable to stop the oral contraceptive (in the case of scheduled interventions, at least 4 weeks before the date of the intervention) and not to resume it until 2 weeks after complete walking.
- There is no consensus on the possible role of varicose veins and superficial thrombophlebitis in the onset of venous thromboembolism.
In general, the use of COCs has been associated with an increased risk of myocardial infarction (MI) or stroke. This risk is strongly influenced by the presence of other risk factors (such as smoking, hypertension, age) (see also below. ) These events are rare.
The risk of arterial thromboembolic events increases with:
- The advancing age
- Tobacco smoking (the more you smoke and the older the age, the greater the risk, particularly in women over 35 years of age)
- Dyslipoproteinemia
- Obesity (body mass index over 30 kg / m2)
- Hypertension
- Valvulopathy
- Atrial fibrillation
- Positive family history (eg arterial thromboembolism in siblings or parents, at a relatively early age). In case of suspected hereditary predisposition, the woman should be referred to a specialist before deciding whether or not to use oral contraceptive .
Symptoms of venous or arterial thrombosis can include:
- pain and / or swelling of only one lower limb
- sudden severe pain in the chest, with or without irradiation to the left arm
- sudden shortness of breath
- sudden onset of cough
- any unusual, severe and prolonged headache
- sudden partial or total loss of vision
- diplopia
- indistinct articulation of words or aphasia
- dizziness
- collapse, with or without focal seizures
- very pronounced weakness or numbness suddenly affecting one side or both sides of the body
- motor disorders
- "acute" abdomen.
Consider the increased risk of venous thromboembolism in the puerperal period.
Other diseases related to circulatory disorders include: diabetes mellitus, systemic lupus erythematosus, haemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia.
Faced with an increase in the frequency or severity of migraines while taking oral contraceptives (perhaps a prodrome of cerebrovascular disorders), consideration should be given to whether or not to discontinue use of the oral contraceptive immediately.
Biochemical factors indicative of hereditary or acquired predisposition to venous or arterial thrombosis include: resistance to activated protein C (APC), factor V Leiden mutation, hyperhomocysteinemia, antithrombin-III deficiency, protein C deficiency, protein deficiency S, antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant) and dyslipoproteinemia.
When weighing the risk / benefit ratio, the physician should consider that by properly treating a disorder it may be possible to reduce the risk associated with thrombosis, and that the risk of developing thrombosis during pregnancy exceeds that associated with the use of COCs.
Tumors:
Cervical cancer
Some epidemiological studies report an increased risk of cervical cancer in women using COCs over the long term, however it is not yet adequately clarified to what extent this finding may be influenced by the effects of sexual behavior and other factors such as the papilloma virus. human (HPV).
Breast cancer
A meta-analysis of 54 epidemiological studies shows that women taking COCs are at slightly increased relative risk of breast cancer (RR = 1.24). This increased risk gradually decreases over the 10 years following discontinuation of the COCs. Because breast cancer rarely occurs in women under the age of 40, the increase in diagnosed cases of this cancer in women who are currently using COCs, or who have used them before, is low compared to the risk of breast cancer in women. "span of the whole life.
These studies do not show any causal relationship. The observed pattern of elevated risk could be attributable to an earlier diagnosis of breast cancer in women taking COCs, the biological effects of COCs, or a combination of both.
Liver cancer
Benign and malignant hepatic neoplasms have been reported among women taking COCs. In isolated instances these neoplasms have led to potentially fatal intra-abdominal haemorrhage. Consider the possibility of hepatic neoplasia as a differential diagnosis in the presence of severe upper abdominal pain, in case of hepatomegaly or in the presence of signs of intra-abdominal haemorrhage in women taking COCs.
Disorders of other types
Women with hypertriglyceridaemia or a family history of this disorder may be at increased risk of pancreatitis if they take a CHC.
In the event of acute or chronic impairment of liver function, discontinue use of Estinette until functional tests have normalized. In patients with impaired liver function there may be inadequate metabolism of steroid hormones.
Closely monitor women with hyperlipidemia who decide to take COCs.
Although small increases in blood pressure have been reported in many women taking CHCs, clinically important increases are rare. If persistent hypertension occurs while taking COCs, discontinue them and treat the hypertensive state. Where relevant, it will be possible to resume use of COCs once normotensive values are obtained with antihypertensive therapy.
the following disorders or their aggravation have been reported, both during pregnancy and with the use of COCs, although there is no definitive evidence of a causal relationship: jaundice and / or itching related to cholestasis, gallstone formation, porphyria, systemic lupus erythematosus, hemolytic uremic syndrome, Sydeham's chorea, gestational herpes, hearing loss due to otosclerosis.
COCs may affect peripheral insulin resistance and glucose tolerance. Therefore, follow diabetic women closely while taking COCs.
Estinette contains lactose and sucrose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency and glucose-galactose malabsorption, as well as patients with rare hereditary problems of fructose intolerance, should not take this medicine.
Crohn's disease and ulcerative colitis have been associated with the use of combined oral contraceptives.
Chloasma may occur, particularly among women with a history of chloasma during pregnancy. Women prone to chloasma should avoid exposure to sunlight or ultraviolet radiation while taking COCs.
Cases of retinal thrombosis have been reported with the use of COCs. Discontinue their intake in the presence of unexplained partial or total loss of vision, onset of proptosis or diplopia, papilloedema or vascular lesions affecting the retina.
If severe depression occurs during COC use, ask women to stop taking and use a different method of contraception while determining whether symptoms may be due to COC use. Follow closely for women with short episodes of major depression and discontinue the use of COCs in case of relapsing depressive symptoms.
Do not take herbal remedies containing Hypericum perforatum (St. John's wort) while taking Estinette, due to the risk of reduced plasma concentrations and compromised clinical effects for Estinette (see section 4.5).
Impairment of efficacy
The efficacy of oral contraceptives may be reduced if tablets are forgotten or if vomiting occurs (see section 4.2), or with the concomitant use of other medicinal products (see section 4.5).
Reduction of cycle control
Irregular bleeding (spotting or metrorrhagia) is possible with any combined oral contraceptive, particularly in the first months of use. Therefore, it is advisable to evaluate any irregular bleeding only after an adaptation period of about 3 cycles.
In the presence of persistent irregular bleeding, the use of COCs with a higher hormone content may need to be considered. If irregular bleeding occurs after previous regular cycles, consider the possibility of non-hormonal causes and take adequate diagnostic precautions to rule out malignant neoplasms or a pregnancy.
Occasionally there is no withdrawal bleeding in the no-tablet interval. However, if the tablets have been taken according to the instructions in section 4.2, it is unlikely that the woman is pregnant. occurred according to the instructions before the first skipped withdrawal bleed, or if two consecutive withdrawal bleeds are missed, rule out the possibility of pregnancy before continuing to take the COC.
04.5 Interactions with other medicinal products and other forms of interaction
Drug interactions leading to increased clearance of sex hormones could result in withdrawal bleeding and contraceptive failure. These interactions have been demonstrated in the case of hydantoins, barbiturates, primidone, carbamazepine and rifampicin. Other substances suspected of reducing the efficacy of COCs include oxycarbazepine, topiramate, griseofulvin, felbamate and ritonavir. The mechanism of this interaction appears to be based on the hepatoenzymes inducing properties of these medicinal products. Maximum enzyme induction generally occurs only 2-3 weeks after initiation of dosing, but thereafter may continue for at least 4 weeks after discontinuation of treatment.
Failure of contraception has also been reported with antibiotics such as ampicillin and tetracyclines, although this mechanism of action remains to be elucidated.
In the case of women on short-term therapy with one of the above groups or individual medicinal products, it will be necessary to temporarily use a barrier method simultaneously with the contraceptive pills, i.e. during the period of taking contraceptive plus medicinal product and for 7 days following the cessation of the medicinal product. Women taking rifampicin should use a barrier method in conjunction with the contraceptive while taking rifampicin and also for 28 days after stopping it. Where the intake or concomitant medicinal product exceeds the number of tablets in the contraceptive pack, start the next pack of pills without observing the usual no-intake interval.
In the case of women who use long-term medicinal products with an inducing effect on hepatoenzymes, advise the use of other contraceptive measures.
Patients taking Estinette should not simultaneously use homeopathic products / preparations containing Hypericum perforatum (St. John's wort), as there is a risk of loss of contraceptive efficacy. Cases of withdrawal bleeding and unwanted pregnancies have been reported.
Hypericum perforatum(St. John's wort) increases the number of enzymes metabolizing medicinal products due to enzyme induction. This induction effect may persist for at least 1-2 weeks after cessation of treatment with Hypericum.
Effects of COCs on other medicinal products: oral contraceptives may interfere with the metabolism of other drugs, resulting in an effect on plasma and tissue concentrations (e.g. cyclosporine, lamotrigine).
Laboratory analysis
The use of contraceptive steroids may affect the results of certain laboratory tests, including biochemical parameters for liver, thyroid, adrenal and renal function; plasma (transport) protein levels, such as corticosteroid-binding globulin and fractions of lipids / lipoproteins, the parameters of carbohydrate metabolism and those for coagulation and fibrinolysis Usually the changes do not go beyond the normal laboratory reference values.
04.6 Pregnancy and lactation
Estinette is not indicated during pregnancy. If you become pregnant while taking Estinette, stop treatment immediately.
Data on gestodene exposed pregnancies are not adequate to draw conclusions about the adverse effects of gestodene on pregnancy and fetal or newborn health. To date, no relevant epidemiological data is available.
Animal studies did not indicate direct or indirect harmful effects with respect to pregnancy, embryonal / fetal development, parturition or postnatal development (see section 5.3).
Most epidemiological studies conducted so far have shown neither an increased risk of congenital defects due to COC intake before pregnancy, nor teratogenic effects following inadvertent COC intake in the early stages of gestation. hormonal action of the active ingredients, an adverse effect of the active ingredients on embryo-fetal development cannot be totally excluded.
The use of contraceptive steroids can affect breastfeeding as they may reduce the volume and alter the composition of breast milk. Therefore, the use of contraceptive steroids is generally not recommended until the baby is completely weaned. Small amounts of contraceptive steroids and / or their metabolites may be excreted into breast milk, but there are no indications of any deleterious effects. on the health of the child. Do not take Estinette while breastfeeding.
04.7 Effects on ability to drive and use machines
Estinette has no or negligible influence on the ability to drive or use machines.
04.8 Undesirable effects
The most frequently reported adverse drug reactions (ADRs) (> 1/10) are irregular bleeding, nausea, weight gain, breast tenderness and headache. These reactions arise predominantly at the start of therapy and are transient in nature.
The serious adverse events listed below in women taking CHCs - see sections 4.3 and 4.4.
• Venous thromboembolism, ie thrombosis involving the deep veins of the lower limbs or pelvis and pulmonary embolism
• Arterial thromboembolic disorders
• Cervical cancer
• Liver tumors
• Disorders of the skin and subcutaneous tissues: chloasma
Among women taking COCs, the frequency of breast cancer diagnosis is slightly increased. Since these cancers are rare in women under 40, the excess number is modest in relation to the overall risk of breast cancer. The causal relationship with COCs is unknown. For more information, see sections 4.3 and 4.4.
04.9 Overdose
No serious or dangerous effects have been reported following overdose. Symptoms possible with overdose are: nausea, vomiting and vaginal bleeding. There is no antidote and further treatment must be symptomatic.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: hormonal contraceptives for systemic use ATC code: G03 AA 10
The contraceptive effect of birth control pills is based on the interaction between various factors, the most important of which are the inhibition of ovulation and changes in cervical secretions. In addition to protecting against pregnancy, oral contraceptives possess numerous beneficial qualities that, when weighed against the negative aspects, are useful to know when deciding which birth control method to use. Contraceptive pills regulate the menstrual cycle, which often becomes less painful, and reduce the intensity of the flow. This latter attribute may contribute to fewer iron deficiencies. It has also been shown that high-dose contraceptive pills (50 mcg ethinylestradiol) have been shown to reduce the risk of fibrocystic breast neoplasms, ovarian cysts, adnexitis, ectopic pregnancies and endometrial and ovarian neoplasms. It has not yet been possible to confirm whether these benefits can also be obtained with low-dose contraceptive pills.
05.2 Pharmacokinetic properties
Gestodene
Absorption
Absorption of gestodene taken orally occurs rapidly and completely. Following a single dose, the maximum serum concentration of 4 ng / ml is reached within approximately one hour. Bioavailability is approximately 99%.
Distribution
Gestodene binds to serum albumin and sex hormone binding globulin (SHBG). Only 1-2% of the total volume in serum is represented by free steroid, while 50-70% is specifically bound to SHBG. The increase in SHBG caused by ethinylestradiol influences the distribution of serum proteins, resulting in an increase in SHBG-bound fraction and decrease in serum albumin-bound fraction The apparent volume of distribution of gestodene is 0.7 l / kg.
Metabolism
Gestodene is completely metabolised via the usual steroid metabolism mechanisms. The metabolic clearance rate from serum is 0.8 ml / min / kg. There are no interactions with the concomitant intake of gestodene and ethinylestradiol.
Elimination
The level of gestodene in serum is reduced according to 2 different rates, the second characterized by a "half-life of 12-15 hours. Gestodene is not subject to excretion. Its metabolites are excreted at a ratio of 6: 4 in the urine. and in the bile.
The half-life of metabolite excretion is approximately 1 day.
Steady state
The pharmacokinetic properties of gestodene are influenced by the levels of SHBG present in serum, which triple with the intake of ethinylestradiol. With the daily intake the serum level of gestodene is approximately four times the value for the single dose intake and reaches the steady state in the second half of the treatment course.
Ethinylestradiol
Absorption
Orally taken ethinylestradiol is rapidly and completely absorbed. Maximum serum concentration of approximately 80 pg / ml is reached within 1-2 hours. Complete bioavailability, possible with presystemic conjugation and first pass metabolism, is about 60%.
Distribution
Ethinylestradiol binds predominantly to albumin (approximately 98.5) non-specifically and leads to increased serum SHBG concentrations. The apparent volume of distribution is approximately 5 l / kg.
Metabolism
Ethinylestradiol is subject to presystemic conjugation both in the mucosa of the small intestine and in the liver. Its metabolism occurs mostly through aromatic hydroxylation, however there is the formation of various types of hydroxylated and methylated metabolites, found as free metabolites and as glucuronide and sulphate conjugates. The metabolic clearance rate is approximately 5 ml / min / kg.
Elimination
The level of ethinylestradiol in serum is reduced according to 2 different rates, the second characterized by a "half-life of 24 hours." Ethinylestradiol is not subject to excretion. However, its metabolites are excreted at a ratio of 4: 6 in the urine and bile. The half-life of metabolite excretion is approximately 1 day.
Steady state
Steady state is reached after 3-4 days, with serum levels of ethinylestradiol 30-40% higher than single dose.
05.3 Preclinical safety data
To assess the risk in humans, laboratory animal toxicity studies were conducted for both the active substances ethinylestradiol and gestodene, used separately or in combination. Systemic tolerance studies reveal the absence of any undesirable effects that could indicate unexpected risks for the man following the repeated assumption.
Longer repeated-dose toxicity studies conducted to investigate the risk of carcinogenic activity reveal no relevant risk to humans. However, it should be noted that sex hormones can promote the growth of certain hormone-dependent tissues and tumors.
The studies on the embryotoxicity and on the teratogenic potential of ethinylestradiol, and the evaluation of the effects of the combination on the fertility of the adult animals treated, on the development of the fetus, on the lactation and on the reproductive capacity, reveal no risk of undesirable effects for the " man with the use of the preparation as recommended.
Education in vitro And in vivo do not indicate a risk of mutagenicity.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
Tablet:
Sodium calcium edetate
Magnesium stearate
Anhydrous colloidal silica
Povidone K-30
Cornstarch
Lactose monohydrate
Coating:
Quinoline yellow (E 104)
Povidone K-90
Titanium dioxide (E171)
Macrogol 6000
Talc
Calcium carbonate (E170)
Sucrose
06.2 Incompatibility
Not relevant.
06.3 Period of validity
3 years.
06.4 Special precautions for storage
Store below 25 ° C. Store in the original package in order to protect from light and moisture.
06.5 Nature of the immediate packaging and contents of the package
Blister: PVC / PVDC / aluminum.
Blister packs: PVC / PVDC / aluminum in PETP / AL / PE bag.
Sales formats: 1 x 21 tablets; 3 x 21 tablets; 6 x 21 tablets.
Not all pack sizes may be marketed.
06.6 Instructions for use and handling
No special instructions.
07.0 MARKETING AUTHORIZATION HOLDER
Effik Italia S.p.A.
Via Lincoln 7 / A,
20092 Cinisello Balsamo (MI)
Italy
08.0 MARKETING AUTHORIZATION NUMBER
037136013 / M
037136025 / M
037136037 / M
037136049 / M
037136052 / M
037136064 / M
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
25/04/2005
10.0 DATE OF REVISION OF THE TEXT
April 2010
11.0 FOR RADIO DRUGS, COMPLETE DATA ON THE INTERNAL RADIATION DOSIMETRY
12.0 FOR RADIO DRUGS, FURTHER DETAILED INSTRUCTIONS ON EXEMPORARY PREPARATION AND QUALITY CONTROL
Please use this checklist together with the Summary of Product Characteristics during any consultation on Combined Hormonal Contraceptives (COCs).
• The thromboembolism (eg deep vein thrombosis, pulmonary embolism, heart attack and stroke) represents an important risk associated with the use of COCs.
• The risk of thromboembolism with a CHC is higher:
- during the first year d "employment;
- when you leave resume use after a break in intake of 4 or more weeks.
• COCs containing ethinylestradiol in combination with levonorgestrel, norgestimate or norethisterone have the lower risk to cause venous troembolism (VTE).
• The risk for a woman also depends on her baseline risk of thromboembolism. The decision to use a COC must therefore take into account the contraindications and individual risk factors, particularly those relating to thromboembolism - see the boxes below and the relevant Summary of Product Characteristics.
• The decision to use any CHC rather than one with the lowest risk of venous thromboembolism (VTE) should only be made after an interview with the woman to ensure she understands:
- the risk thromboembolism associated with its COC;
- the effect of any risk factor inherent in his risk of thrombosis;
- which must pay particular attention to signs and symptoms of a thrombosis.
Remember that a woman's risk factors can vary over time. It is therefore important to use this checklist at every consultation.
→ In these cases it would be better to reconsider whether or not to use a non-hormonal contraceptive until the risk returns to normal..
→ In such situations, your patient should pay particular attention to catch any signs and symptoms of thromboembolism.
Please strongly encourage women to read the Package Insert that accompanies each COC pack, including the symptoms of thrombosis which they should carefully watch out for.
Please report any suspected adverse reactions from COC to the territorially competent Pharmacovigilance Offices or to the AIFA as required by current legislation
All combined contraceptives increase the risk of having a blood clot. The overall risk of a blood clot from taking a combined hormonal contraceptive (COC) is small., but clots can represent a serious condition and in very rare cases even fatal.
It is very important that you recognize when you may be at a higher risk for a blood clot, what signs and symptoms to watch out for and what actions you need to take.
In which situations is the risk of a blood clot higher?
- during the first year of use of a COC (including when resuming use after an interval of 4 or more weeks)
- if you are overweight
- if you are over 35 years of age
- if you have a family member who has had a blood clot at a relatively young age (i.e. under 50)
- if you have given birth in the last few weeks
Self smokes and over 35 years of age, she is strongly advised to stop smoking or to use a non-hormonal method of contraception.
See a doctor immediately if you experience any of the following symptoms:
• Severe pain or swelling in one of the legs which may be accompanied by flaccidity, warmth or changes in the color of the skin such as the appearance of paleness, redness or bluish color. He could have deep vein thrombosis.
• The sudden and unexplained shortness of breath or onset of rapid breathing; severe chest pain which may increase with deep breathing; a sudden cough with no obvious cause (which can produce blood). It could be a serious complication of deep vein thrombosis called pulmonary embolism. This occurs if the blood clot migrates from the leg to the lung.
• A pain in the chest, often sharp, but which sometimes occurs such as malaise, a sense of pressure, weight, upper body discomfort radiating to the back, jaw, throat, arm with a feeling of fullness associated with indigestion or choking, sweating, nausea, vomiting or dizziness . It could be a heart attack.
• A numbness or a sense of weakness in the face, arm or leg, especially on one side of the body; a difficulty in speaking or understanding; a "sudden confusion of mind, a sudden loss of vision or blurred vision; a headache / migraine intense and worse than usual. This could be a stroke.
Look out for symptoms of a blood clot, especially if:
• has just had surgery
• you have been immobilized for a long time (such as due to an accident or illness, or because you have had your leg in a cast)
• has traveled a long way (for more than 4 hours)
Remember to tell your doctor, nurse or surgeon that you are taking a combined hormonal contraceptive if:
• You have had or are due to have surgery
• There is any situation where a healthcare professional asks you what medications you are taking
For more information, please read carefully the Package Leaflet accompanying the drug and immediately report any undesirable effects associated with the use of the combined hormonal contraceptive to your doctor or pharmacist.
