ethinylestradiol + drospirenone


Laboratorios Leon Farma


Masa Lab
Full Prescribing Info
Drospirenone, ethinylestradiol.
Each film-coated tablet contains two active ingredients: Drospirenone 3 mg, Ethinylestradiol 0.03 mg.
Excipients/Inactive Ingredients: Lactose.
Pharmacology: Pharmacodynamics: Justima is a combined oral contraceptive ("the combined Pill"). Each tablet contains a small amount of two different female hormones. These are drospirenone (a progestogen) and ethinylestradiol (an estrogen). Because of the small amounts of hormones, Justima is considered a low-dose oral contraceptive. As all tablets in the pack combine the same hormones in the same dose, it is considered a monophasic combined oral contraceptive.
Justima act to suppress gonadotropins. This is achieved through inhibition of ovulation and alterations to both the cervical mucus and the endometrium. Improvement in symptoms like bloating, swelling or weight-gain, related to fluid retention. Improvement in acne and reduction in greasiness of the skin and hair.
Pharmacokinetics: The absolute bioavailability of drospirenone is 76% and ethinyl estradiol is 40%.
Volume of distribution is 4 liters per kilogram for drospirenone, 4-5 liters for ethinyl estradiol.
Drosperinone bind to serum proteins 97% and ethinyl estadiol bind to serum proteins highly but non-specifically.
Half-life: Drospirenone 30 hours and ethinyl estradiol 24 hours.
Drospirenone and ethinyl estradiol are well metabolized in the liver and conjugated with glucuronide and sulfate.
Drospirenone excretion is nearly complete after 10 days and amounts excreted were slightly higher than in feces compared to urine.
Ethinyl estradiol is excreted in the urine and feces as glucuronide and sulfate conjugates and undergoes enterohepatic circulation.
Prevention of pregnancy.
Dosage/Direction for Use
One pack (blister) contains 21 tablets. The day of the week to take the tablet is printed at the side of each tablet. If, for example, the patient start on Wednesday, the patient should take a tablet with "WED" at the side. Follow the arrow on the pack until the patient have used the 21 tablets.
The patient should then not take any tablet for 7 days. During theses 7 days when the patient do not take any tablets (called drug-free interval), the patient should menstruate. Menstruation. which can also be called withdrawal bleeding, usually starts on the 2nd or 3rd days of the drug-free interval.
On the eight day from taking the last Justima tablet (that is after 7 days drug-free interval), start the following pack, even if you have not stopped menstruating. This means that the patient should start the following package on the same day which the patient started the previous week and menstruation should occur during the same dates of every month.
If the patient used Justima as described, the patient is protected against pregnancy during the 7 days the patient does not take any tablet.
When can the patient start the first pack: If the patient have not taken any hormonal contraceptive in the previous month: Start taking Justima on the first day of cycle (that is the first day of menstruation). If the patient start taking Justima on the first day of menstruation, the patient will be immediately protected against pregnancy. The patient can also start from the second to the fifth day of the cycle, but the patient should use additional contraceptives (a condom for example) for the first 7 days.
Changing from another combined hormonal contraceptive, combined contraceptive vaginal ring or patch: The patient can start taking Justima the next day after the drug-free interval of the previous contraceptive vaginal ring or patch, follow the physician's recommendations.
Changing from a method based exclusively on progestogens (progestogen only tablets, injection, progestogen-releasing intrauterine device or implant): The patient can change from the progestogen only tablet whatever the patient like (if the patient had an implant or an intrauterine device, use the new tablet the day the patient remove it; if the patient used injections, use the new tablet on the day when the patient would have injected again), but it is recommended in all cases, to use additional protection (a condom for example) for the first 7 days of taking the tablets).
After Abortion: Follow the physician's recommendations.
After having a Child: The patient can start taking Justima between 21 and 28 days after having a child. If the patient start later, the patient should use a barrier contraceptive (a condom for example) for the first 7 days the patient take Justima.
If, after having a child, and have already had sexual relations before starting Justima (again), the patient must be sure that the patient is not pregnant or wait for the next period.
If the patient forgets to take Justima: If the patient forget to take a tablet in the 1st, 2nd or 3rd rows, the patient should follow these instructions: If less than 12 hours late in taking a tablet, the protection from pregnancy is not reduced. Take the tablet as soon as remembered and the following tablets at the usual time.
If more than 12 hours late in taking a tablet, protection from pregnancy may be reduced. The more tablets forgotten to take, the greater risk of reducing the contraceptive effect.
The risk of reduced protection against pregnancy is highest if the patient forgets to take the tablet at the beginning of 1st row and end of week 3-3rd row in the pack. Consequently, the patient should adopt the following measures.
Forgetting to take more than one tablet in a pack: Consult the physician.
Forgetting to take one more tablet in week 1: Take the tablet forgotten as soon as the patient realized, even if this means taking two tablets at the same time. Continue taking the following tablets at the usual time and take additional precautions, for example a condom, for the next 7 days. If the patient has had sexual relations in the week before the patient forgot to take the tablet, there is a risk of becoming pregnant. In this case, consult the physician.
Forgetting to take one tablet in week 2: Take the tablet forgotten as soon as realized, even if this means taking two tablets at the same time. Continue taking the following tablets at the usual time. The contraceptive effect will not be reduced and the patient does not need to take additional precautions.
Forgetting to take one tablet in week 3: The patient can choose one of two possibilities: 1.Take the tablet the patient have forgotten as soon as the patient realized, even if this means taking two tablets at the same time. Continue taking the following tablets as the usual time. Start taking the next pack as soon as the current pack is finished.
The patient will probably have period (withdrawal bleeding) at the end of the second pack, but could also have some spots or bleeding when taking the second pack.
2. The patient can stop taking tablets from the current pack, have a tablet-free interval of 7 days (taking note that of the day the patient forget to take the tablet) and start a new pack on the fixed start date.
If the patient follows one of these two recommendations, the patient will be protected against pregnancy: If the patient have forgotten to take tablets and does not have a period during the tablet-free interval, the patient may be pregnant. In this case, the patient should consult the physician before continuing with the second pack.
Patients in whom intentional overdose is known or suspected should be referred for psychiatric consultation.
The symptoms are nausea and vomiting. Serum concentrations of potassium and sodium, and evidence of metabolic acidosis, should be monitored. Nausea or vomiting is treated for symptomatic relief.
Hypersensitivity to drospirenone or ethinylestradiol.
Justima should not be used in the presence of any of the conditions listed as follows. Should any of the conditions appear for the first time during use, Justima should be stopped immediately.
Adrenal insufficiency; hepatic function or renal impairment or in patients with conditions that predispose to hyperkalemia; known or suspected breast carcinoma, or endometrium carcinoma; known or suspected estrogen-dependent neoplasia; cardiac insufficiency; active or history of cerebrovascular disease/coronary artery disease; cholestatic jaundice of pregnancy or jaundice with prior pill use; cholestatic hepatic disease; history of benign or malignant hepatic tumors; pregnancy; if the patient have (or have that in the past) thrombophlebitis, thrombosis or thromboembolic disorder; abnormal or undiagnosed uterine bleeding; hypertension; diabetes mellitus.
1. Do not use in the presence of thrombosis and hepatic disease.
2. Should not be used in women who have higher risk of thrombosis, such as a history of thrombophlebitis, obesity, diabetes and hypertension.
3. Use carefully in women smoking tobacco, especially women over 35 years of age should consult the physician before using Justima.
4. Consult the physician if any abnormal symptoms occur while using Justima.
Special Precautions
Regular visits to physician at least every 6 to 12 months to check progress.
Stop medication immediately and check with physician if pregnancy is suspected.
If schedules for laboratory tests, tell the physician if taking birth control pills; certain blood test may be affected by oral contraceptives.
Not refilling an old prescription for oral contraceptives without having a physical examination by physician, especially after pregnancy.
Stop using Justima and immediately go to the physician if the patient has possible signs of thrombosis, such as: Extreme pain and/or inflammation of one of the legs; intense and sudden chest pain, which may reach the left arm; sudden difficulty in breathing; sudden cough without clear cause; unusual headache, intense or prolonged, or worsening of a migraine; partial or complete vision loss, or double vision; difficulty or inability to speak; vertigo or fainting; weakness, abnormal sensations, or numbness of any part of the body.
Justima and Cancer: Women who take combined contraceptives have a slightly higher rate of breast cancer than women who don't, but it is not known if this is due to the medication. For example, it is possible that more tumors are detected in women who take contraceptives because they are examined by their physician more frequently. The breast cancer rate reduces gradually after the patient decide to stop taking combined hormonal contraceptives.
It is important to regularly examine the breast and go to the physician if the patient finds any lump.
Benign liver tumors have been found in women who use combined contraceptives on rare occasions and malignant tumors are even rarer. Go to the physician if the patient experiences sudden intense abdominal pain.
Use In Pregnancy & Lactation
Use in Pregnancy: If the patient is pregnant the patient should not take Justima. If the patient is pregnant when taking Justima the patient should stop taking it immediately and contact the physician.
Use in Lactation: It is generally not recommended to take Justima when the patient is breast-feeding. If the patient wants to use the contraceptive while breast-feeding, the patient should consult the physician.
Adverse Reactions
The following undesirable effects have been reported by users of the Pill, although they need not be caused by the Pill. These undesirable effects may occur in the first few months of using the Pill and usually lessens with time. (See Table.)

Click on icon to see table/diagram/image

If the patient has hereditary angioedema; exogenous estrogens may induce or exacerbate symptoms of angioedema.
If the patient notice any side effects not mentioned, please inform the physician or pharmacist.
Drug Interactions
Some medicines may stop the Pill from working properly. These include medicines used for the treatment of epilepsy (e.g. primidone, phenytoin, barbiturates, carbamazepine, oxcarbazepine, topiramate, felbamate); tuberculosis (e.g. rifampicin, rifabutin) and the infections (e.g. ritonavir, nevirapine); antibiotics (e.g. penicillins, tetracyclines, griseofulvin) for some other infectious diseases; and the herbal remedy St. John's wort (primarily used for the treatment of depressive moods). Some medicines (e.g. ketoconazole, erythromycin, cyclosporine) may inhibit the metabolism of Justima.
The Pill may also interfere with the working of other medicines. Accordingly, plasma and tissue concentrations may either increase (e.g. cyclosporine) or decrease (e.g. lamotrigine).
There is a theoretical potential for an increase in serum potassium if the patient is taking Justima with other drugs that may increase serum potassium levels. Such drugs include angiotensin-II-receptor antagonists. However in studies in women taking drospirenone (combined with estradiol) together with an ACE inhibitor or indomethacin no significant difference in the potassium blood level could be observed.
Please inform the physician or pharmacist if the patient is taking or have recently taken any other medicines or herbal products, even those not prescribed. Also tell any other physician or dentist who prescribes another medicine (or the dispensing pharmacist) that the patient use Justima. They can tell if there is need to take additional contraceptive precautions and if so, for how long.
Certain laboratory tests may be affected by oral contraceptives.
Store below 30°C.
Patient Counseling Information
What to do if: The patient suffers from gastro-intestinal disturbances (e.g. vomiting, severe diarrhea): If the patient vomits, or has severe diarrhea, the active ingredients of Justima may not have been completely absorbed. If there is vomiting within 3 to 4 hours after taking the tablet, this is like missing a tablet. Therefore, follow the advice for missed tablets. If the patient has severe diarrhea, please contact the physician.
The patient has unexpected bleeding: With all Pills, for the first few months, the patient can have irregular vaginal bleeding (spotting or breakthrough bleeding) between the patient's periods. The patient may need to use sanitary protection, but continue to take the tablets as normal. Irregular vaginal bleeding usually stops once the body has adjusted to the Pill (usually after about 3 tablet-taking cycles). If it continues, becomes heavy or starts again, tell the physician.
The patient has missed a period: If the patient has taken all the tablets at the right time, and have not vomited, nor had severe diarrhea or used other medicines then the patient is very likely to be pregnant.
Continue to take Justima as usual. If the patient misses period twice in a row, the patient may be pregnant. Tell the physician immediately. Do not start the next pack of Justima until the physician has checked that the patient is not pregnant.
Changing the period: Before deciding to change the period, the patient should consult the physician.
If the patient is unsure how to proceed, consult the physician for an examination.
The patient want to delay a period: If necessary, the patient can delay the period if the patient start with the next pack of Justima immediately after finishing the current pack. The patient can continue this pack for as long as the patient wish, until this pack is empty. When the patient wishes for the period to begin, just stop tablet-taking. While using the second pack the patient may have some breakthrough bleeding or spotting on tablet-taking days. Start with the next pack after the usual 7-day tablet-free break.
The patient want to change the starting day of the period: If the patient take the tablets as directed, the patient will have period on about the same day every 4 weeks. If the patient want to change this, just shorten, (never lengthen) the next tablet-free break. For example, if the period usually starts on a Friday and in the future the patient want it to be on Tuesday (3 days earlier) the patient should now start the next pack 3 days sooner than the patient usually do. If the patient make the tablet-free break very short (e.g. 3 days or less), the patient may not have a bleeding during the break. The patient may have some breakthrough bleeding or spotting during the use of the next pack.
The patient want to stop using Justima: The patient can stop using whenever the patient wants. If the patient does not want to be pregnant, should consult the physician about using other methods for prevention.If the patient has any questions, please contact the physician.
More about the Pill: The combined pill may also have non-contraceptive health benefits. The period may be lighter and shorter. As a result, the risk of anemia may be lower.
The period pains may become less severe or may completely disappear.
In addition, some serious disorders have been reported to occur less frequently in users of the Pills containing 50 micrograms of ethinylestradiol ('high-dose Pills').
These are benign breast disease, ovarian cysts, pelvic infections (pelvic inflammatory disease or PID), ectopic pregnancy (pregnancy in which the embryo implants outside the womb) and cancer of the endometrium (lining of the womb) and ovaries. This may also be the case for low-dose Pills but so far this has only been confirmed for endometrial and ovarian cancer.
One of the hormones in Justima, drospirenone, has special properties leading to beneficial effects in addition to contraception. Drospirenone can prevent weight-gain, and other symptoms like bloating and swelling, related to fluid retention caused by hormones both in oral contraceptives and at certain times in the menstrual cycle.
Drospirenone also has antiandrogenic activity which can help to reduce acne (pimples) and greasiness of the skin and hair. These special properties make drospirenone similar to the natural progesterone hormone produces by the body.
MIMS Class
ATC Classification
G03AA12 - drospirenone and ethinylestradiol ; Belongs to the class of progestogens and estrogens in fixed combinations. Used as systemic contraceptives.
Tab (round, yellow) 21's.
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