Active ingredients: Ethinylestradiol, Gestodene
GESTODIOL 20 micrograms / 75 micrograms coated tablets
GESTOSIOL Coated tablets of 30 micrograms / 75 micrograms
Indications Why is Gestodiol used? What is it for?
- GESTODIOL is a contraceptive pill used to prevent conception.
- Each tablet contains small amounts of two different female hormones, called ethinyl estradiol and gestodene.
- Birth control drugs such as GESTODIOL which contain two hormones are termed "combination" pills.
What you need to know before you take GESTODIOL
Before you start using GESTODIOL you should read the information on blood clots (thrombosis) in section 2. It is especially important that you read the symptoms of a blood clot (see section "Blood clots").
Before you can start taking GESTODIOL, your doctor will ask you questions about your medical history and family history. Your doctor will also measure your blood pressure and, depending on your personal situation, may also carry out other checks.
This leaflet describes situations where you must stop taking GESTODIOL or where the reliability of GESTODIOL may be compromised. In such situations you do not have sex or take extra non-hormonal contraceptive precautions, for example a condom or another barrier method. Do not use rhythm and basal temperature methods. These methods can be unreliable as GESTODIOL modifies changes in the menstrual cycle related to body temperature and cervical mucus.
GESTODIOL like other hormonal contraceptives, do not protect against HIV infection (AIDS) or other sexually transmitted infections.
Contraindications When Gestodiol should not be used
Do not use Gestodiol if you have any of the conditions listed below. If you have any of the conditions listed below, please contact your doctor. Your doctor will discuss with you other birth control methods that may be more suitable for you.
- if you have (or have ever had) a blood clot in a blood vessel of the leg (deep vein thrombosis, DVT), lung (pulmonary embolism, PE) or other organs;
- if you know you have a disorder that affects blood clotting, such as protein C deficiency, protein S deficiency, antithrombin-III deficiency, factor V Leiden or antiphospholipid antibodies;
- if you are going to have an "operation or if you will be lying down for a long time (see section" Blood clots (thrombosis and emboli) ");
- if you have ever had a heart attack or stroke;
- if you have (or have ever had) angina pectoris (a condition that causes severe chest pain and may be a first sign of a heart attack) or transient ischemic attack (TIA - temporary stroke symptoms);
- if you have any of the following diseases, which could increase the risk of blood clots in the arteries:
- severe diabetes with blood vessel damage
- very high blood pressure
- very high level of fat (cholesterol or triglycerides) in the blood
- a disease known as hyperhomocysteinemia
- if you have (or have ever had) a type of migraine called 'migraine with aura';
- if you have (or have ever had) an inflammation of the pancreas (pancreatitis)
- if you have or have suffered from liver disease and your liver function is not yet normalized
- if you have or have ever had liver cancer
- if your kidneys are not working well (kidney failure)
- if you have (or have ever had) or are suspected of having breast cancer or cancer of the genital organs
- if vaginal bleeding of unknown origin occurs
- if you are allergic to ethinyl estradiol or gestodene or any of the ingredients of this medicine (listed in section 6). This can be recognized by itching, rash or swelling.
Precautions for use What you need to know before taking Gestodiol
When should you see a doctor?
Contact a doctor urgently
- if you notice possible signs of a blood clot which may indicate that you are suffering from a blood clot in the leg (deep vein thrombosis), a blood clot in the lung (pulmonary embolism), a heart attack or a stroke (see section below " Blood clot (thrombosis) ").
For a description of the symptoms of these serious side effects go to the section "How to recognize a blood clot".
Tell your doctor if any of the following apply to you.
If this condition appears or worsens while you are using GESTODIOL you should tell your doctor.
In some situations you need to use caution while taking GESTODIOL or any other combined hormonal contraceptive, as you may need to be checked regularly by your doctor. If any of the following apply to you, tell your doctor before starting the intake of GESTODIOL.
- if you have Crohn's disease or ulcerative colitis (chronic inflammatory bowel disease);
- if you have systemic lupus erythematosus (SLE, a disease that affects the natural defense system);
- if you have haemolytic uremic syndrome (HUS, a blood clotting disorder causing kidney failure);
- if you have sickle cell anemia (an inherited disease of the red blood cells);
- if you have high levels of fat in the blood (hypertriglyceridaemia) or a "positive family history of this condition." Hypertriglyceridaemia has been associated with an increased risk of developing pancreatitis (inflammation of the pancreas);
- if you are going to have an "operation or if you are going to lie down for a long time (see section 2" Blood clots ");
- if you have just given birth, your risk of developing blood clots is higher. Ask your doctor how soon after having a baby you can start taking GESTODIOL;
- if you have "inflammation of the veins under the skin (superficial thrombophlebitis);
- if you have varicose veins.
- if a close relative has (or has suffered) from breast cancer or has been diagnosed with breast cancer;
- if you suffer from a disease affecting the liver or gallbladder;
- if you have diabetes;
- if you suffer from depression;
- if you suffer from epilepsy (see also "Other medicines and GESTODIOL");
- if you have a disease that first appeared during pregnancy or during previous use of sex hormones, such as hearing loss, porphyria (blood disease), gestational herpes (blistering skin rash that occurs during pregnancy ), Sydenham's chorea (a nerve disorder characterized by sudden body movements);
- if you suffer (or have suffered) from chloasma (patchy browning, especially of the face, the so-called "pregnancy spots"). If this concerns you, avoid direct exposure to sunlight or ultraviolet light;
- if you suffer from hereditary angioedema (severe allergic reaction), products containing estrogen can induce or worsen the symptoms of angioedema. If you experience symptoms of angioedema such as swelling of the face, tongue and / or pharynx and / or difficulty in swallowing or hives in combination with breathing difficulties, contact your doctor immediately.
Gestodiol and thrombosis BLOOD CLOTS
Using a combined hormonal contraceptive such as GESTODIOL increases your risk of developing a blood clot compared with not using one. In rare cases, a blood clot can block blood vessels and cause serious problems.
Blood clots can develop
- in veins (called "venous thrombosis", "venous thromboembolism" or VTE)
- in the arteries (referred to as 'arterial thrombosis', 'arterial thromboembolism' or ATE).
Recovery from blood clots is not always complete. Rarely, long-lasting severe effects can occur or, very rarely, they can be fatal.
It is important to remember that the overall risk of a harmful blood clot associated with GESTODIOL is low.
HOW TO RECOGNIZE A BLOOD CLOT
See a doctor immediately if you notice any of the following signs or symptoms.
- swelling in one leg or along a vein in the leg or foot, especially when accompanied by:
- pain or tenderness in the leg that may only be felt when standing or walking;
- increased sensation of heat in the affected leg;
- change in color of the skin on the leg, such as turning pale, reddish or bluish;
- sudden and unexplained shortness of breath or rapid breathing;
- sudden cough with no obvious cause, possibly causing blood to be emitted;
- sharp chest pain which may increase with deep breathing;
- severe light headedness or dizziness;
- rapid or irregular heartbeat;
- severe pain in the stomach
- immediate loss of vision or
- painless blurring of vision which can progress to loss of vision
- chest pain, discomfort, feeling of pressure or heaviness;
- sensation of squeezing or fullness in the chest, arm or below the breastbone;
- feeling of fullness, indigestion or choking;
- upper body discomfort radiating to the back, jaw, throat, arms and stomach;
- sweating, nausea, vomiting or dizziness;
- extreme weakness, anxiety, or shortness of breath;
- rapid or irregular heartbeats
- sudden numbness or weakness of the face, arm or leg, especially on one side of the body;
- sudden confusion, difficulty speaking or understanding;
- sudden difficulty seeing in one or both eyes;
- sudden difficulty walking, dizziness, loss of balance or coordination;
- sudden, severe or prolonged migraine with no known cause;
- loss of consciousness or fainting with or without seizures.
- swelling and pale blue discoloration of one extremity;
- severe stomach pain (acute abdomen)
BLOOD CLOTS IN A VEIN
What can happen if a blood clot forms in a vein?
- The use of combined hormonal contraceptives has been linked to an increased risk of blood clots forming in the veins (venous thrombosis). However, these side effects are rare. In most cases they occur in the first year of using a combined hormonal contraceptive.
- If a blood clot forms in a vein in the leg or foot, it can cause a deep vein thrombosis (DVT).
- If a blood clot travels from the leg and lodges in the lung, it can cause a "pulmonary embolism."
- Very rarely, a clot can form in another organ such as the eye (retinal vein thrombosis).
When is the risk of developing a blood clot in a vein highest?
The risk of developing a blood clot in a vein is highest during the first year of taking a combined hormonal contraceptive for the first time. The risk may be even higher if you restart taking a combined hormonal contraceptive (the same drug or a different drug) after a break of 4 or more weeks. After the first year, the risk is reduced but is always slightly higher than if you were not using a combined hormonal contraceptive. When you stop taking GESTODIOL, the risk of developing a blood clot returns to normal within a few weeks.
What is the risk of developing a blood clot?
The risk depends on your natural risk of VTE and the type of combined hormonal contraceptive you are taking.
The overall risk of developing a blood clot in the leg or lung (DVT or PE) with GESTODIOL is low.
- Out of 10,000 women who are not using any combined hormonal contraceptive and who are not pregnant, about 2 will develop a blood clot in a year.
- Out of 10,000 women who are using a combined hormonal contraceptive that contains levonorgestrel, norethisterone or norgestimate, about 5-7 will develop a blood clot in a year.
- Out of 10,000 women who are using a combined hormonal contraceptive that contains gestodene, such as GESTODIOL, about 9-12 will develop a blood clot in a year.
- The risk of a blood clot forming depends on your medical history (see under "Factors that increase the risk of a blood clot forming").
Factors that increase the risk of developing a blood clot in a vein
The risk of developing a blood clot with GESTODIOL is low but some conditions increase the risk. Its risk is greater:
- if you are severely overweight (body mass index or BMI over 30 kg / m2);
- if a member of your immediate family has had a blood clot in the leg, lung or other organ at a young age (less than about 50 years). In this case you could have an inherited blood clotting disorder;
- if you are going to have an operation or if you have to lie down for a long time due to an injury or illness or if you have a leg in a cast. You may need to stop taking GESTODIOL a few weeks before the surgery or in the period in which you are less mobile. If you have to stop taking GESTODIOL, ask your doctor when you can start taking it again;
- as you get older (especially over the age of 35);
- if you gave birth less than a few weeks ago.
The risk of developing a blood clot increases the more conditions you have of this type
Air travel (lasting> 4 hours) may temporarily increase the risk of a blood clot, especially if you have some of the other risk factors listed.
It is important that you tell your doctor if any of these apply to you, even if you are not sure. Your doctor may decide that GESTODIOL needs to be stopped.
If any of the above conditions change while you are using GESTODIOL, for example if a close relative has a thrombosis for no known reason or if you gain a lot of weight, contact your doctor.
BLOOD CLOTS IN AN ARTERY
What can happen if a blood clot forms in an "artery?"
Like blood clots in a vein, clots in an artery can cause serious problems, for example, they can cause a heart attack or stroke.
Factors that increase the risk of developing a blood clot in an artery
It is important to note that the risk of heart attack or stroke associated with the use of GESTODIOL is very low but can increase:
- with increasing age (over 35 years);
- if you smoke. When using a combined hormonal contraceptive such as GESTODIOL you are advised to stop smoking. If you are unable to stop smoking and are over the age of 35, your doctor may advise you to use a different type of contraceptive;
- if you are overweight;
- if you have high blood pressure;
- if a member of your immediate family has had a heart attack or stroke at a young age (less than about 50 years). In this case, you may also be at high risk of having a heart attack or stroke;
- if you or a close relative have a high level of fat in the blood (cholesterol or triglycerides);
- if you suffer from migraines, especially migraines with aura;
- if you have any heart problems (valve defect, a heart rhythm disorder called atrial fibrillation);
- if you have diabetes
If you have more than one of these conditions or if any of them are particularly severe, the risk of developing a blood clot may be even higher.
If any of the above conditions change while you are using GESTODIOL, for example if you start smoking, if a close relative has a thrombosis for no known reason or if you gain a lot of weight, contact your doctor.
Gestodiol and cancer
Breast cancer has been seen slightly more often in women taking the combined pill but it is not known whether it is caused by the treatment. For example, there may be an increased occurrence of breast cancer in women on combined contraceptives because they are checked more often by their doctor. Breast cancer development gradually decreases after stopping combined hormonal contraceptives. It is important that you have regular breast checks and see your doctor if you feel unwell.
Benign liver tumors and in even fewer cases malignant liver tumors have been reported in rare cases among pill users. Consult your doctor if you feel unusually severe pain in your abdomen.
Intra-menstrual bleeding
During the first months of taking GESTODIOL you may experience unexpected bleeding (outside the week of suspension). If this bleeding continues for several months or if it starts after a few months, your doctor needs to investigate the cause.
What to do if no bleeding occurs during the week off
If you have taken all the tablets correctly, have not had vomiting or severe diarrhea and have not taken any other medicines, it is highly unlikely that you are pregnant.
If the expected bleeding does not occur twice in a row you may be pregnant. Consult your doctor immediately. Do not start the next pack until you are sure you are not pregnant.
Interactions Which drugs or foods can modify the effect of Gestodiol
Always tell your doctor who prescribes GESTODIOL about which medicines or herbal products you are already taking. Also tell any other doctor or dentist who prescribes another medicine (or the pharmacist) that you are taking GESTODIOL. They can tell you if you need to take additional birth control precautions (e.g. condoms) and if so, for how long.
- Some drugs can compromise the contraceptive efficacy of GESTODIOL or cause unexpected bleeding. These include drugs for the treatment of epilepsy (eg hydantoin, topiramate, felbamate, lamotrigine, primidone, phenytoin, barbiturates, carbamazepine, oxcarbamazepine) and tuberculosis (e.g. rifampicin), immunomodulatory agents (cyclosporine), for the treatment of HIV infections (ritonavir) or other infectious diseases (griseofulvin, ampicillin, tetracyclines) and the herbal preparation St. John's wort (St. John's wort).
- If you want to use herbal preparations containing St. John's wort (St. John's wort) at the same time as a treatment with GESTODIOL you should first of all consult your doctor.
- GESTODIOL may affect the effectiveness of other drugs, eg drugs containing the immunomodulating agent cyclosporine) or the antiepileptic drug lamotrigine (which could cause an increase in the frequency of seizures).
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines
Lab test
If you need a blood test, tell your doctor or the laboratory staff that you are taking the pill. This is because oral contraceptives can affect the results of some tests.
Warnings It is important to know that:
Pregnancy and breastfeeding
If you are pregnant you should not take GESTODIOL. If you become pregnant while taking GESTODIOL you must stop taking it immediately and consult your doctor.
Feeding time
In general, it is not recommended to take GESTODIOL while breastfeeding. If you want to take the pill while you are breastfeeding, please contact your doctor.
Consult your doctor or pharmacist before taking any medication.
Driving and using machines
There is no information indicating that the use of GESTODIOL has an influence on the ability to drive and operate machines.
Gestodiol contains lactose and sucrose If you have been told by your doctor that you have "intolerance to some sugars, contact your doctor before taking this medicinal product.
Dose, Method and Time of Administration How to use Gestodiol: Posology
Take one GESTODIOL tablet every day, if needed together with a small amount of water. The tablets can be taken with or without food but should be taken around the same time each day.
The blister contains 21 tablets. Next to each tablet is printed the day of the week. For example, if you start the pack on a Wednesday, take the tablet next to which is marked "WED". Follow the direction of the arrow on the blister until you have taken all 21 tablets.
So do not take any tablets for 7 days. During these 7 tablet-free days (otherwise known as a break or gap week) you should experience some blood loss. The so-called "withdrawal bleeding" usually begins on the second or third day of the gap week.
On the eighth day after the last GESTODIOL tablet (ie after the 7-day interval) you start the new pack, even if the bleeding has not stopped. This implies that you must start the next pack on the same day of the week. and that withdrawal bleeding must take place during this time.
If you take GESTODIOL in this way, the contraceptive protection will be active even during the 7 days when you do not take any tablets.
When can the first blister pack start?
- If you have not used a hormonal contraceptive in the previous month.
Start taking GESTODIOL on the first day of your period (which is the first day of your period).
If you take GESTODIOL on the first day of your menstruation, the contraceptive protection will be active immediately. You can also start taking it on the second-fifth day of your cycle, but in this case you will need to take extra protective measures (eg use a condom) for the first 7 days.
- Changing from another combined hormonal contraceptive or a combined contraceptive vaginal ring or patch
You can start GESTODIOL the day after the end of your previous pill withdrawal period (or after the last inactive tablet of the previous pill). When changing from a combined contraceptive vaginal ring or patch you must follow the instructions of your doctor.
- Changing from a progestogen-only preparation (progestogen-only minipill, injection, implant, or progestogen-releasing IUD).
Switching can occur whenever from an injectable, on the day the next injection should be given, from a progestogen-only minipill, and from an implant or IUD on the same day of their removal. However, in all these cases you will need to take extra protective measures (e.g. use a condom) for the first 7 days of taking the tablet.
- After an abortion
Follow your doctor's instructions.
- After giving birth
After a birth, you can start taking GESTODIOL between the twenty-first and the twenty-eighth day after. If you start taking it after the 28th day you will need to use a so-called barrier method (for example a condom) during the first 7 days of treatment with GESTODIOL .
If, after having a baby, you have sexual intercourse before (re) starting GESTODIOL, you must first make sure that you are not pregnant or wait until your next period.
Ask your doctor for advice if you are not sure when to start.
- If you are breastfeeding and want to (re) start taking GESTODIOL after having a baby.
GESTODIOL should not be taken during breastfeeding. Read the section "Breastfeeding".
Overdose What to do if you have taken an overdose of Gestodiol
If you take more Gestodiol than you should
There are no reports of serious harmful consequences of taking too many GESTODIOL tablets.
If you take several tablets at once, symptoms such as nausea or vomiting may occur. Vaginal bleeding may occur in young girls.
If you have taken too many GESTODIOL tablets or if you find that a child has swallowed some tablets, ask your doctor or pharmacist for advice.
If you forget to take Gestodiol
- If you are less than 12 hours late in taking the tablet, there is no reduction in contraceptive protection. Take the tablet as soon as you remember and take the following tablets at the usual time.
- If the delay in taking the forgotten tablet is more than 12 hours, contraceptive protection may be impaired. The more tablets are missed, the greater the risk of contraceptive protection being impaired.
The risk of incomplete contraceptive protection is greater if you forget the tablet at the beginning and at the end of the blister pack. It is therefore advisable that you follow the rules set out below (see also the diagram below):
- More than one tablet forgotten in this blister pack
Contact your doctor.
- One tablet forgotten in the first week
Take the forgotten tablet as soon as you remember, even if that means that you have to take two tablets at the same time. Continue taking the tablets at the usual time and use extra precautions for the next 7 days, such as a condom. If you have had sexual intercourse in the week prior to the forgetfulness or if you have forgotten to start a new pack after the withdrawal period, you should be aware that there is a risk of pregnancy. In these cases, contact your doctor.
- One tablet forgotten in the second week
Take the forgotten tablet as soon as you remember, even if that means that you have to take two tablets at the same time. Continue taking the tablets at the usual time. Contraceptive protection is not reduced and therefore you do not need to take additional precautions.
One tablet forgotten in week 3
You can choose between two possibilities:
1. Take the forgotten tablet as soon as you remember, even if that means that you have to take two tablets at the same time. Continue taking the tablets at the usual time. Instead of stopping taking the tablets in the scheduled withdrawal interval, move on to the next pack immediately. Most likely your period (withdrawal bleeding) will occur at the end of the second pack but you may still experience breakthrough bleeding or breakthrough bleeding while taking the tablets in the second pack. second pack.
2. You may also decide to stop taking the tablets in the pack and start the withdrawal period directly (do not forget to write down the day you forgot to take your tablet). If you want to start a new pack on the scheduled start day make sure that the suspension period last less than 7 days.
If you follow either of these recommendations, contraceptive protection will not be compromised.
- If you have forgotten to take more than one tablet in the pack and no bleeding occurs in the first withdrawal period, you may be pregnant. Contact your doctor before moving on to the next pack.
What to do in case of vomiting or severe diarrhea
If vomiting and / or severe diarrhea occurs within 3-4 hours of taking the tablet, there is a risk that the active substances in the pill will not be completely absorbed by the body. The situation is similar to that of forgetting to take the pill. After vomiting or diarrhea take an extra tablet from a reserve strip as soon as possible. If possible, take it within 12 hours of the time you normally take the pill. If this is not possible or 12 hours have elapsed, follow the instructions. instructions given in the paragraph "If you forget to take GESTODIOL".
Delayed menstruation: what you need to know
Although not recommended, it is possible to delay your period (withdrawal bleeding). This is achieved by switching directly to a new pack of GESTODIOL instead of stopping taking the tablets for the usual 7 days, after the first pack. Intermenstrual bleeding (drops or blood spots) or withdrawal bleeding may occur while taking the tablets. of the second pack At the end of the usual 7-day withdrawal interval, continue with the next pack.
Ask your doctor for advice before deciding to delay your period.
Change in the day you start your period: what you need to know
If you take the tablets as instructed, your period / withdrawal bleeding will start during the week when you do not take any tablets. If you need to change this day you can do it by shortening the withdrawal interval (but never lengthening it!) For example, if your withdrawal interval starts on a Friday and you want to move it to Tuesday (3 days earlier) you must start a new pack 3 days sooner than usual If you greatly shorten your withdrawal period (for example, 3 days or less) you may not have any bleeding, but you may experience breakthrough bleeding (drops or bloodstains) or withdrawal bleeding.
If you are not sure how to proceed, ask your doctor for advice.
If you want to stop Gestodiol
You can stop taking GESTODIOL when you want. If you do not want to become pregnant, ask your doctor for advice on other reliable methods of birth control.
If you are unsure about the use of this drug, ask your doctor or pharmacist.
Side Effects What are the side effects of Gestodiol
Like all medicines, GESTODIOL can cause side effects, although not everybody gets them.
If you get any side effects, especially if they are severe or persistent, or if there is any change in your health which you think might be due to GESTODIOL, please tell your doctor.
An increased risk of developing blood clots in the veins (venous thromboembolism (VTE)) or blood clots in the arteries (arterial thromboembolism (ATE)) is present in all women taking combined hormonal contraceptives. For more detailed information on the different risks from "taking combined hormonal contraceptives, see section" What you need to know before you use GESTODIOL ".
- Side effects common (may affect up to 1 in 10 people):
Headache, nervousness, poor tolerance to contact lenses, vision disturbances, nausea, acne, migraines, weight gain, fluid retention, bleeding and intermenstrual bleeding can sometimes occur in the first few months, and then disappear as soon as the body is adapted to GESTODIOL. Contact your doctor if these symptoms continue, worsen or recur. Absence or reduction of menstruation, breast ulceration, loss of interest in sex, depressive states, irritability.
- Side effects uncommon (may affect up to 1 in 100 people):
Excess of lipids in the blood, vomiting, hypertension.
- Side effects rare (may affect up to 1 in 1,000 people):
Harmful blood clots in a vein or artery, for example:
- in a leg or foot (DVT), lung (PE), heart attack, stroke. mini-stroke or temporary stroke-like symptoms, known as transient ischemic attack (TIA); blood clots in the liver, stomach / intestines, kidneys or eye.
The chance of developing a blood clot may be higher if you have any other conditions that increase this risk (see section 2 for more information on conditions that increase the risk of blood clots and the symptoms of a blood clot).
Liver disorders, skin and subcutaneous tissue disorders (lupus erythematosus,), middle ear disorders, gallstones, pigmentation disorders. This can happen even if you have been taking GESTODIOL for many months. The effect can be reduced by avoiding exposure to yourself. too much in sunlight. Altered vaginal discharge.
- Side effects very rare (may affect up to 1 in 10,000 people):
Motor disorders, pancreatic disease.
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. You can also report side effects directly via the national reporting system at https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse
By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Do not store above 30 ° C.
Keep this medicine out of the sight and reach of children.
Do not use Gestodiol after the expiry date which is stated on the blister and on the carton after EXP.
The expiry date refers to the last day of that month.
What Gestodiol contains
- Active principles:
GESTODIOL 20 micrograms / 75 micrograms coated tablets:
Each tablet contains 20 micrograms of ethinylestradiol and 75 micrograms of gestodene
GESTODIOL 30 micrograms / 75 micrograms coated tablets:
Each tablet contains 30 micrograms of ethinylestradiol and 75 micrograms of gestodene
- The excipients are:
Tablet core:
Magnesium stearate, povidone K-25, corn starch, lactose monohydrate
Tablet coating:
Povidone K-90, macrogol 6000, talc, calcium carbonate, sucrose, lignite wax
Description of what Gestodiol looks like and contents of the pack
GESTODIOL is available in the form of white, rounded, biconvex sugar-coated tablets with no imprint on both sides.
The pills are supplied in a blister pack containing 21 tablets. The blister packs are supplied in a cardboard box. Each carton contains 1, 3 or 6 blister packs.
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
GESTODIOL
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
Active principles:
GESTODIOL 20 mcg / 75 mcg coated tablets: each tablet contains
20 mcg of Ethinylestradiol and 75 mcg of Gestodene
GESTODIOL 30 mcg / 75 mcg coated tablets: each tablet contains
30 mcg of Ethinylestradiol and 75 mcg of Gestodene
Excipients:
GESTODIOL 20 mcg / 75 mcg coated tablets contain 38 mg of lactose monohydrate and 20 mg of sucrose
GESTODIOL 30 mcg / 75 mcg coated tablets contain 38 mg of lactose monohydrate and 20 mg of sucrose
For the full list of excipients, see section 6.1.
03.0 PHARMACEUTICAL FORM
Coated tablet: White, rounded, biconvex sugar-coated tablets without impressions on both sides.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Oral contraception.
04.2 Posology and method of administration
How to take GESTODIOL.
The tablets should be taken in the order indicated on the pack at approximately the same time each day. One tablet per day for 21 days. Each subsequent pack should be started after a 7-day tablet-free interval: during this period of time a "withdrawal bleed will occur."This bleeding usually starts on the second or third day after taking the last tablet and may continue even after the next pack is started.
How to start taking GESTODIOL.
In case there has been no hormonal contraceptive treatment in the previous month.
The first tablet should be taken on the first day of a woman's natural cycle (i.e. the first day of her menstrual cycle). It is possible to start taking the pills from the second to the fifth day but in these cases it is also recommended to use a barrier method of contraception for the first seven days of taking the tablets during the first cycle.
In case of switching from "another combined oral contraceptive pill.
The woman should start taking GESTODIOL the day after the last active tablet of her previous contraceptive - but no later than the day after completing the usual pill-free period or taking placebo as prescribed by the previous contraceptive drug.
When switching from a progestogen-only contraceptive (progesterone-only pill (mini-pill, injection, implant) or from a progestogen-releasing intrauterine system (IUS).
The woman can switch from the progesterone-only pill (POP) at any time during her period. The first tablet should be taken the day after taking any of the tablets in the POP pack. In the case of an implant or an IUS, the intake of GESTODIOL must begin on the same day in which the implant is removed. In the case of an injectable, GESTODIOL should be started on the day the next injection should be given. In all these cases it is recommended that the woman also use a barrier method of contraception for the first seven days of taking the pills.
After a first trimester abortion.
The woman can start taking the pills immediately. If you follow these instructions, no additional contraceptive measures are necessary.
After a birth or second-trimester abortion.
For use in breastfeeding women, see section 4.6. It is recommended that the woman start taking the tablets on the 21st - 28th day after delivery, if not breastfeeding, or after a second trimester abortion. starts later, the woman should also be advised to also use barrier contraception for the first seven days of taking the pills. If intercourse has occurred in the meantime, pregnancy must be ruled out before actually starting the pills. or the woman must wait for her first menstruation to appear.
Failure to take tablets .
Failure to take a tablet within 12 hours of the usual time does not affect contraceptive protection. The woman should take the tablet as soon as she remembers and continue taking the rest of the tablets as usual. Failure to take a tablet for more than 12 hours from the usual time may decrease contraceptive protection. The following two rules can be helpful in managing not taking tablets.
1. tablet-taking must never be discontinued for longer than 7 days.
2. It takes 7 days of uninterrupted ingestion of tablets to achieve sufficient suppression of the hypothalamus-pituitary-gonadal axis.
Therefore the following advice can be given in daily practice:
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 should continue taking the tablets at the usual time. At the same time she must use a barrier method, eg a condom. , for the next 7 days. If in the previous 7 days the woman has had sexual intercourse, she must take into consideration the possibility of being pregnant. the tablets are not taken, the greater the risk of becoming pregnant.
Week 2. 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. Then she should continue taking the tablets at the usual time. If the tablets have been taken correctly for 7 days before the forgotten no extra contraceptive precautions need to be taken If not, or if more tablets have been missed, the woman should still use a barrier method, eg a condom, for the next 7 days.
Week 3. As the withdrawal period approaches, the risk of reduced contraceptive protection is greater. However, it is possible to prevent the reduction in contraceptive protection by adjusting the intake of the tablets. There is therefore no need to take any extra contraceptive precautions by adhering to either of the following two options, unless the tablets have been taken correctly for 7 days prior to forgetting. Otherwise it is advisable to advise the woman to follow the first of the two options and to use a barrier method at the same time, eg. a condom, for the next 7 days.
1. The woman must take the last missed tablet as soon as possible, even if this means that she has to take 2 tablets at the same time. After that she must continue taking the tablets at the usual time. She will start the new pack immediately after taking the last tablet of the packaging in use; in this case there will be no suspension period between the packs. Menstruation is unlikely to occur until the second pack of tablets is finished, however you may notice breakthrough bleeding or breakthrough bleeding while taking the tablets.
2. The woman may be advised to stop taking the tablets from the current pack. In which case she will have a withdrawal period of up to 7 days, including the days the tablet is missed, after which the woman will start a new pack If, after the woman has forgotten to take tablets, she does not menstruate in the first usual tablet-free interval, the possibility that the woman is pregnant should be considered.
What to do in case of vomiting / diarrhea.
If you vomit within 3-4 hours of taking a tablet, the tablet may not be fully absorbed. In this case, follow the instructions above regarding forgotten tablets. Unless the diarrhea is extremely severe, it does not affect the absorption of COCs, so no additional contraceptive methods are required. If severe diarrhea persists for 2 days or more, follow the procedures for forgotten pills. If the woman does not want to change her usual tablet intake, she should take an extra tablet (or tablets) from another pack.
How to shift or delay your period.
To delay menstruation, the woman will have to continue taking GESTODIOL by switching from one blister pack to another, without a withdrawal period. Menstruation can be delayed as long as desired but not beyond the end of the second pack. When menstruation is delayed, episodes of withdrawal bleeding or intermenstrual bleeding may occur. The intake of GESTODIOL must be resumed regularly at the end of the usual interval in which no tablet is taken. To move the period to a day in the week different from that expected with the current tablets, the woman can be advised to shorten the next tablet-free interval of as many days as you wish. The shorter this interval, the greater the risk of not having menstrual bleeding but breakthrough bleeding and bleeding while taking the tablets from the next pack (this also occurs when you delay your period) .
04.3 Contraindications
Combined oral contraceptives (COCs) should not be used if any of the conditions listed below are present. If such a condition occurs for the first time during the use of COCs, their use must be immediately suspended.
• Venous thromboembolic disease in active phase or in anamnesis (deep vein thrombosis,
pulmonary embolism).
• Active arterial thromboembolism or history (myocardial infarction, cerebrovascular disease) or prodromal symptoms (angina pectoris and transient ischemic attack) (see section 4.4).
• Hereditary or acquired predisposition to venous or arterial thrombosis such as antithrombin deficiency, protein C deficiency, protein S deficiency, resistance to activated protein C (APC), antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant), hyperhomocysteinemia.
• Multiple or substantial risk factors for arterial thrombosis (see section 4.4).
• Severe hypertension.
• Diabetes complicated by micro- or macroangiopathy.
• Severe dyslipoproteinemia.
• Known or suspected hormone-dependent malignancies (eg affecting the genital organs or breast).
• Concurrent severe liver disease or in history until liver function values have returned to normal.
• Concurrent or history of benign or malignant liver tumors.
• Vaginal bleeding of an unknown nature.
• Migraine with focal neurological symptoms.
• Hypersensitivity to the active substances or to any of the excipients.
04.4 Special warnings and appropriate precautions for use
Evaluation and examination prior to initiation of COCs. Prior to initiation or resumption of COC treatment, the physician should review the patient's personal and family medical history and exclude pregnancy. Based on of the contraindications (see section 4.3) and warnings (see "Warnings" in this section) it is necessary to measure the blood pressure and subject the patient to a physical examination, if clinically indicated. The woman is asked to read the package leaflet carefully and to follow the instructions provided The frequency and nature of further periodic check-ups should be based on established practice guidelines and be tailored to the individual woman.
Warnings. In general. Advise women that hormonal contraceptives do not protect against HIV (AIDS) or other sexually transmitted infections. If any of the risk factors mentioned below are present, evaluate the benefits of using COC on a case-by-case basis with the possible risks for each individual woman and discuss this with the woman before starting COC. In the event of any aggravation, exacerbation or development of any of these conditions or risk factors, the woman should contact her doctor. Your doctor will decide whether to stop taking the COC.
1. Circulation disorders. Use of any CHC increases the risk of venous thromboembolism (VTE) compared with non-use. The excess risk of VTE is highest during the first year a woman uses a CHC for the first time. The increased risk is lower than the risk of VTE associated with pregnancy, which is estimated to be 60 in every 100,000 pregnancies. VTE is fatal in 1-2% of cases. In several epidemiological studies it has been found that in women using combined oral contraceptives containing ethinylestradiol, mostly at a dose of 30 micrograms, and a progestin such as gestodene the risk of VTE is increased compared to women using combined oral contraceptives containing less than 50 mcg of ethinylestradiol and the progestin levonorgestrel. For COCs containing 30 micrograms of ethinylestradiol in combination with desogestrel or gestodene compared to those containing less than 50 micrograms of ethinylestradiol and levonorgestrel, the overall relative risk of VTE has been estimated to range from 1.5 to 2.0. . In the case of combined oral contraceptives containing levonorgestrel with less than 50 mcg of ethinylestradiol the incidence of VTE is about 20 cases per 100,000 woman-years of use. As for GESTODIOL, the incidence varies from 30 to 40 cases per 100,000 years. -woman of use, ie 10-20 additional cases each
100,000 woman-years of use. The impact of relative risk on the number of additional cases
it would be highest in women during the first year of COC use when the risk of VTE with all COCs is highest. Thrombosis has been reported very rarely in other blood vessels, i.e. of the hepatic, mesenteric, renal or retinal veins and arteries in users of oral contraceptives. There is no consensus on the possibility that the occurrence of these cases is related to the use of COC. The risk of developing venous thromboembolism increases:
• with advancing age;
• in the case of a positive family history (eg venous thromboembolism which involved a relative or a blood relative plus relatively young people). In case of suspected hereditary predisposition, the woman should be referred to a specialist before being prescribed an oral contraceptive;
• in case of obesity (body mass index greater than 30 kg / m2);
• prolonged immobilization, major surgery, leg surgery or major trauma. In these cases, discontinuation of treatment with oral contraceptives is recommended (in the case of a surgical operation scheduled at least 4 weeks before) and should not be taken until 2 weeks after complete ambulation;
• there is no consensus on the possible role of varicose veins and superficial thrombophlebitis in venous thromboembolism. In general the use of COC was
associated with an increased risk of acute myocardial infarction (AMI) or stroke, this risk strongly influenced by the presence of other risk factors (e.g. smoking, high blood pressure and age) (see also below). These events rarely occur. The risk of thromboembolic events increases with:
• advancing age;
• smoking (with heavy smokers and with advancing age the risk increases further, especially in the case of women over 35 years of age);
• dyslipoproteinemia;
• obesity (body mass index greater than 30 kg / m2);
• hypertension;
• heart valve disease;
• atrial fibrillation;
• positive family history (eg arterial thrombosis involving a relative or relative of a relatively young age). If hereditary predisposition is suspected, the woman should be referred to a specialist before being prescribed an oral contraceptive.
Symptoms of venous and arterial thrombosis can include:
• unilateral pain and / or swelling in one leg;
• sudden severe chest pain, which may or may not extend to the left arm;
• sudden shortness of breath;
• sudden cough;
• unusual, severe, prolonged headache;
• sudden partial or complete loss of vision;
• diplopia;
• difficulty in speaking or aphasia;
• dizziness;
• collapse accompanied or not by focal seizures;
• weakness or sudden very marked numbness of one side or part of the body;
• motor disturbances;
• "acute" abdomen.
The increased risk of venous thromboembolism during the puerperium should be considered. Other medical conditions related to vascular disorders are: diabetes mellitus, systemic lupus erythematosus, haemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. An increase in the frequency and severity of migraine (which may be prodromal in the case of cerebrovascular disease) during the use of oral contraceptives should consider immediate discontinuation of oral contraceptives. Biochemical parameters 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). While evaluating the risk / benefit ratio, the physician should bear in mind that adequate treatment of a condition may reduce the associated risk of thrombosis and that the risk associated with pregnancy is greater than that associated with the use of COCs.
2. Tumors: Cancer of the cervix. In some epidemiological studies an increased risk of cervical uterine cancer has been reported in long-term users of COCs but it is not yet clear to what extent this finding could be influenced by the aggravating effects of sexual behavior and other factors such as human papillomavirus. (HPV).
Breast cancer. A meta-analysis of 54 epidemiological studies reported a slightly higher relative risk (RR = 1.24) of breast cancer diagnosis among women currently using COCs. The excess risk gradually disappears over the 10 years following discontinuation of COC use. Since breast cancer is rare in women under 40, the higher number of breast cancer diagnoses among current users and recent development of COC is limited in relation to the overall risk of breast cancer. These studies do not provide evidence of causality. The observed higher trend in risk may be due to an early diagnosis of breast cancer in COC users, biological effects of COCs or a combination of both.Breast cancer diagnosed in women who have used COCs tends to be less clinically advanced than the cancers found among women who have never taken COCs.
Liver tumors. Benign and malignant liver tumors have been reported among COC users. In isolated cases, these tumors have led to life-threatening intra-abdominal haemorrhages. Therefore, consider the possibility of liver cancer in the differential diagnosis when a COC user has severe upper abdominal pain, liver enlargement (hepatomegaly), or signs of intra-abdominal haemorrhage.
3. Other conditions. Women with hypertriglyceridaemia, or a family history thereof, may be at increased risk of pancreatitis while using CHCs. In case of acute or chronic disturbances of liver function, it may be necessary to discontinue GESTODIOL, until the markers of liver function are restored to normal values. Steroid hormones may be poorly metabolised in patients with impaired hepatic function. Although they have been reported to be small. Increases in blood pressure in many women taking COCs, clinically significant increases are rare. If "persistent clinical hypertension develops while taking a combined hormonal contraceptive," persistent clinical hypertension should be discontinued and the combined hormonal contraceptive should be treated. "hypertension. The use of the COC may be resumed if it is possible to obtain normotensive values through the therapy. If the doctor deems it appropriate, the use of the pill can be resumed when the blood pressure values return to normal following antihype therapy. rtensive. Both with pregnancy and with the use of COCs, the following conditions may appear or worsen. However, the evidence of an association with the use of COCs is not conclusive: jaundice and / or itching associated with cholestasis; development gallstone disease; porphyria; systemic lupus erythematosus; haemolytic uremic syndrome; Sydenham's chorea; herpes gestationis; hearing loss due to otosclerosis. COCs may have an effect on peripheral insulin resistance and glucose tolerance. Diabetic patients should therefore be carefully monitored while using COCs. GESTODIOL contains lactose and sucrose. Patients with rare hereditary problems of galactose intolerance, Lapp-lactase deficiency or glucose-galactose malabsorption or with rare fructose intolerance should not take this medicinal product. Worsening of endogenous depression, epilepsy (see section 4.5 Interactions), Crohn's disease and ulcerative colitis have been reported during COC use. Chloasma may occur, especially in users with a history of chloasma gravidarum. Women with a tendency to chloasma should avoid exposure to the sun or ultraviolet radiation while taking COCs. Herbal preparations containing St. John's wort or St. John's wort (Hypericum perforatum) should not be taken at the same time as GESTODIOL due to the risk of decreased plasma concentrations and clinical effects of GESTODIOL (see section 4.5).
Reduced effectiveness. The efficacy of oral contraceptives may be reduced if tablets are forgotten, in the presence of severe diarrhea or vomiting (see section 4.2) or in the case of concomitant use of other medicinal products (see section 4.5).
Irregular cycle. As with all combined hormonal contraceptives, irregular blood loss (breakthrough bleeding or breakthrough bleeding) may occur, particularly in the first months of use. For this reason, a medical opinion about irregular blood loss will only be useful after an adaptation period of approximately three cycles. If bleeding persists, consideration should be given to using CHCs with a higher hormone content. If bleeding occurs. verification after previous regular cycles non-hormonal causes should be considered and adequate diagnostic measures taken to rule out malignancy or pregnancy. Occasionally there may be no withdrawal bleeding in the interval in which tablets are not taken. If the tablets have been taken according to the instructions in section 4.2, it is unlikely that the woman is pregnant. However, if the tablets have not been taken according to these instructions prior to the first skipped withdrawal bleed, or if the woman misses two consecutive withdrawal bleeds, pregnancy must be ruled out before continuing to take the COC.
04.5 Interactions with other medicinal products and other forms of interaction
Interactions with medicinal products that lead to high clearance of sex hormones can lead to bleeding and failure of oral contraception. This effect was established in the case of hydantoins, barbiturates, primidone, carbamazepine and rifampicin, and was suspected in the case of oxcarbazepine, topiramate, griseofulvin, felbamate and ritonavir. The mechanism of these interactions appears to be based on the liver enzyme inducing properties of these medicinal products. In general, maximum enzyme induction does not occur in the first 2-3 weeks after starting treatment, but the effect can be sustained for at least 4 weeks after stopping therapy. There have also been reports of unsuccessful contraception with antibiotics such as ampicillin and tetracyclines. The mechanism of this effect has not been elucidated. Women on short-term treatment with any of the above drug groups or with individual drugs, should temporarily use a barrier method in addition to the birth control pill, which this must be done for as long as this medicine is taken at the same time as the pill as well as for seven days after stopping it. Women taking rifampicin should use a barrier method at the same time as oral contraceptives while taking rifampicin as well as in the 28 days following its suspension If administration c oncomitant of the medicine continues beyond the number of contraceptive tablets in the pack, the woman should start the next pack, without observing the usual withdrawal interval. For women on long-term therapy with hepatic enzyme inducers, another method of contraception should be considered. Patients taking GESTODIOL should not use alternative medicinal preparations / products containing concomitant Hypericum perforatum (St. John's wort or St. John's wort) as they may cause a loss of contraceptive effect. Bleeding and unwanted pregnancies have been reported. L "Hypericum perforatum (St. John's wort or St. John's wort) increases, by enzyme induction, the amount of enzymes that metabolize medicinal products. The enzyme induction effect may persist for at least 1-2 weeks after cessation of treatment with Hypericum. Effects of COCs on Other Drugs: COCs can interfere with the metabolism of other drugs. This may result in an increase (e.g. cyclosporine) or decrease (lamotrigine) in plasma and tissue concentrations.
Lab test.
The use of contraceptive steroids can affect the results of some laboratory tests including biochemical parameters of liver, thyroid, adrenal and renal function, plasma levels of (transport) proteins, for example of corticosteroid-binding globulin and fractions lipid / lipoprotein, the parameters of carbohydrate metabolism and the parameters of coagulation and fibrinolysis.The variations are generally within the limits of normal laboratory values.
04.6 Pregnancy and lactation
GESTODIOL is contraindicated during pregnancy. If you become pregnant while taking GESTODIOL, discontinue treatment immediately. Extensive epidemiological studies have shown neither an increased risk of congenital defects in children born to women who have taken COCs before pregnancy, nor teratogenic effects following inadvertent use of COCs during pregnancy. Breastfeeding can be influenced by contraceptive steroids as they can reduce the volume and alter the composition of breast milk. Small amounts of contraceptive steroids and / or their metabolites may be excreted in breast milk. Therefore, the use of contraceptive steroids is generally not recommended in mothers who are breastfeeding until the end of complete weaning.
04.7 Effects on ability to drive and use machines
GESTODIOL has no, if any, effect on the ability to drive and use machines.
04.8 Undesirable effects
The most frequently reported adverse events (> 1/10) are irregular bleeding, nausea, weight gain, breast tenderness and headache. They usually occur at the start of therapy and are transient.
The following serious side effects have been reported in women taking COCs, see sections 4.3 and 4.4.
• Venous thromboembolism, ie deep vein thrombosis in the leg or pelvis and pulmonary embolism.
• Arterial thromboembolic events.
• Liver tumors.
• Skin and subcutaneous tissue pathology: chloasma. The frequency of breast cancer diagnoses among women taking COCs is slightly higher. Breast cancer is rare in women under 40. The higher number is limited in relation to the overall risk of breast cancer. The causal relationship with COCs is unknown. For further information see sections 4.3 and 4.4.
04.9 Overdose
No serious side effects have been reported following overdose. Symptoms that can occur following overdose are: nausea, vomiting and vaginal bleeding. There is no antidote, and treatment must be symptomatic.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: hormonal contraceptives for systemic use.
ATC code: G03AA10.
The contraceptive effect of birth control pills is based on the interaction of various factors, the most important of which are the inhibition of ovulation and changes in the endometrium. negative properties (illustrated in section 4.8 Warnings, Undesirable Effects), can help in choosing the method to be adopted for birth control. The menstrual cycle is more regular and the menstruation itself is often less painful and the bleeding is lighter. appearance can lead to a decrease in iron deficiency cases.
05.2 "Pharmacokinetic properties
Gestodene.
Absorption.
After oral administration, gestodene is rapidly and completely absorbed. After administration of a single dose the maximum serum concentration of 4 ng / ml is reached after approximately one "hour. Bioavailability is around 99%.
Distribution.
Gestodene is bound to serum albumin and sex hormone binding globulins (SHBG). Only 1-2% of total serum gestodene is found as a free steroid, while 50-70% is specifically bound to SHBG. The ethinylestradiol-induced increase in SHBG influences the distribution of serum proteins with consequent increase in the SHBG-bound fraction and decrease in the albumin-bound fraction. The apparent volume of distribution of gestodene is 0.7 l / kg.
Metabolism.
Gestodene is completely metabolised via the known steroid metabolism channels. The extent of metabolic clearance from serum is 0.8 ml / min / kg. No interactions occur when gestodene is taken together with ethinyl estradiol.
Elimination.
Serum levels of gestodene decrease in a biphasic manner. The terminal elimination phase is characterized by a "half-life of 12-15 hours. Gestodene is not excreted unchanged. Its metabolites are excreted in the urine and bile in a ratio of 6: 4. The" half-life of excretion of the metabolites is equal to about 1 day.
Steady-state.
The pharmacokinetics of gestodene are influenced by serum SHBG levels which increase three-fold with ethinylestradiol. Following daily dosing, serum gestodene levels increase approximately four-fold the single dose value and reach steady-state by second half of the course of treatment.
Ethinylestradiol.
Absorption.
After oral administration, ethinylestradiol is rapidly and completely absorbed. The peak plasma levels, equal to about 80 pg / ml, are reached in 1-2 hours. The absolute bioavailability, after presystemic conjugation and first pass metabolism, is at " approximately 60%.
Distribution.
During lactation 0.02% of the mother's daily dose passes
in milk. Ethinylestradiol is largely, but nonspecifically, bound to albumin (approximately 98.5%) and induces an increase in serum concentrations of SHBG. An apparent volume of distribution of approximately 5 l / kg has been determined. Metabolism. Ethinylestradiol is subject to presystemic conjugation at the level of both the mucosa of the small intestine and the liver. The main metabolic pathway of ethinylestradiol is aromatic hydroxylation but a wide variety of hydroxylated and methylated metabolites are also formed, present as free metabolites and conjugated with glucuronides and sulphates. The extent of metabolic clearance is approximately 5 ml / min / kg.
Elimination.
Serum levels of ethinylestradiol decrease in a biphasic manner, with a terminal elimination phase with a half-life of approximately 24 hours. Unchanged ethinylestradiol is not excreted, but its metabolites are excreted in a urine: bile ratio of 4: 6. The half-life of metabolite excretion is approximately 1 day.
S.tready-state.
Steady-state concentrations are reached after 3-4 days and serum levels of ethinylestradiol are 30-40% higher than single intake.
05.3 Preclinical safety data
Ethinylestradiol and gestodene are not genotoxic. Carcinogenicity studies with ethinylestradiol alone or in combination with various progestogens show no carcinogenic hazard in women using the drug as a contraceptive as indicated. However, it should be borne in mind that sex hormones can promote the growth of some hormone-dependent tissues and tumors. Reproductive toxicity studies on fertility, fetal development or reproductive performance conducted with ethinylestradiol alone or in combination with progestogens did not provide indications of a risk of adverse effects in humans resulting from the use of the preparation as recommended.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
Tablet core: magnesium stearate, povidone k-25, corn starch, lactose monohydrate.
Tablet coating: povidone k-90, macrogol 6000, talc, calcium carbonate, sucrose, lignite wax.
06.2 Incompatibility
Not relevant.
06.3 Period of validity
Three years.
06.4 Special precautions for storage
Do not store above 30 ° C.
06.5 Nature of the immediate packaging and contents of the package
Blister: PVC / Aluminum. Packaging: 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
Farmitalia s.r.l
Viale A. De Gasperi 165 / B - 95127 CATANIA.
08.0 MARKETING AUTHORIZATION NUMBER
GESTODIOL 20 mcg / 75 mcg coated tablets, 1X21 cpr A.I.C. n.037684014
GESTODIOL 20 mcg / 75 mcg coated tablets, 3X21 cpr A.I.C. n.037684026
GESTODIOL 20 mcg / 75 mcg coated tablets, 6X21 cpr A.I.C. n.037684038
GESTODIOL 30 mcg / 75 mcg coated tablets, 1X21 cpr A.I.C. n.037684040
GESTODIOL 30 mcg / 75 mcg coated tablets, 3X21 cpr A.I.C. n.037684053
GESTODIOL 30 mcg / 75 mcg coated tablets, 6X21 cpr A.I.C. n.037684065
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
2 October 2007
10.0 DATE OF REVISION OF THE TEXT
March 2010