Drospirenone + Ethinylestradiol (0.03 mg)

Uses

This is indicated in oral contraception.

Drospirenone + Ethinylestradiol (0.03 mg) is also used to associated treatment for these conditions: Abnormal Uterine Bleeding, Acne Vulgaris, Endometriosis, Hypermenorrhea, Idiopathic Hirsutism, Menstrual Distress (Dysmenorrhea), Menstrual Irregularities, Osteoporotic Fractures, Pregnant State, Premenstrual Dysphoric Disorder, Vasomotor Symptoms Associated With Menopause, Vulvovaginal Atrophy, Hypoestrogenism, Folate supplementation therapy, Hormone Replacement Therapy, Oral Contraceptives

How Drospirenone + Ethinylestradiol (0.03 mg) works

Drospirenone and ethinyl estradiol in combination suppress the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH), preventing ovulation. Other changes induced by this drug which may aid in the prevention of pregnancy include alterations in cervical mucus consistency, hindering sperm movement, and lowering the chance of embryo implantation.

Drospirenone is an analog of the diuretic spironolactone, which exerts anti-mineralocorticoid activity, blocking aldosterone receptors, which increases sodium and water excretion. Studies in animals have demonstrated that drospirenone administration leads to antiandrogenic activity. This activity helps to oppose the effects of naturally occurring androgens, inhibiting the binding of dihydrotestosterone (DHT) to its receptor, and preventing androgen synthesis in the ovaries, helping to treat acne and hirsutism. Drospirenone may also decrease the level of edema in sebaceous follicle during the second half of the menstrual cycle, when acne often appears.

Dosage

Drospirenone + Ethinylestradiol (0.03 mg) dosage

When and how to take the tablets: The this tablet pack contains 21 tablets. On the pack, each tablet is marked with the day of the week on which it is to be taken. Take your tablet at about the same time each day, with some water if necessary. Follow the direction of the arrows until all 21 tablets have been taken. During the next 7 days don't take any tablet. A period should begin during these 7 days (the withdrawal bleed), unusually it will start on day 2-3 after the last this tablettablet. Start taking your next pack on the 8th day even if your period continues. This means that you will always start new packs on the same day of the week and also that you have your withdrawal bleed on about the same days each month. Starting your first pack of this tablet: When no hormonal contraceptive has been used in the past month. Start taking this tablet on the first day of your cycle, i.e. the first day of menstrual bleeding. Take a tablet marked with that day of the week. For example, if your period starts on a Sunday, take a tablet marked Sunday. Then follow thedaysin order. You may also start on days 2-5 of your cycle, but in that case make sure you also use an additional contraceptive method (barrier method) for the first 7 days of tablet-taking in the first cycle.When changing form another combined Pill: You can start taking this tablet the day after you have the last tablet from your present Pill pack (this means no tablet-free break). If your present Pill pack also contains inactive tablets you can start this tablet on the day after taking the first active tablet (if you are not sure which this is, ask your doctor or pharmacist). You can also start later, but never later than the day following the tablet free break of your present Pill (or the day after the last inactive tablet of your present Pill).When changing from progestogen-only Pill (Mini Pill): You can stop taking the mini pill any day and start taking this tablet the next day, at the same time. But make sure you also use an additional-contraceptive method (a barrier method) for the first 7 days of tablet-taking when having intercourse.When changing from an Injectable or Implant: Start using this tablet when your next injection is due or on the day that your implant is removed. But make sure you also use an additional contraceptive method (a barrier method) for the first 7 days of tablet-taking when having intercourse.After having a baby: If you have just had a baby, your doctor may tell you to wait until after your first normal period before you start taking this tablet. Sometimes it is possible to start sooner. Your doctor will advise you. If you are breast-feeding and want to take this tablet you should discuss this first with your doctor.After a miscarriage or an abortion: Your doctor will advise you.If too many this tablet tablets are taken (overdose): There have been no reports of serious harmful effects from taking too many this tablet tablets at one time. If you have taken several tablets at a time, you may have nausea, vomiting or vaginal bleeding. If you discover that a child has taken this tablet ask your doctor for advice.When you want to stop taking this tablet: You can stop taking this tablet at any time you want. If you do not want to become pregnant, ask your doctor about other methods of birth control. If you stop taking this tablet because you want to get pregnant, it is generally recommended that you wait until you have had a natural period before trying to conceive. If you forget to take tablets If you are less than 12 hours late in taking a tablet, the reliability of the Pill is maintained. Take the tablet as soon as you remember and take the next tablets at the usual times. If you are more than 12 hours late in taking any tablet, the reliability of the Pill may be reduced. The more consecutive tablets you have missed, the higher the risk that the contraceptive efficacy is decreased. There is a particularly high risk of becoming pregnant if you miss tablets at the beginning or at the end of the pack. Therefore, you should follow the rules given below. More than one tablet forgotten in a pack: Ask your doctor for advice. 1 tablet missed in week 1: Take the missed tablet as soon as your remember (even if this means taking two tablets at the same time) and take the next tablets at the usual time. Use extra contraceptive precautions (barrier method) for the next 7 days. If you had sexual intercourse in the week before missing the tablets, there is a possibility of becoming pregnant. So tell your doctor immediately. 1 tablet missed in week 2: Take the missed tablet as soon as you remember (even if this means taking two tablets at the same time) and take the next tablets at the usual time. The reliability of the Pill is maintained. You need not use extra contraceptive precautions. 1 tablet missed in week 3: You may choose either of the following options, without the need for extra contraceptive precautions. Take the missed tablet as soon as you remember (even if this means taking two tablets at the same time) and take the next tablets at the usual time. Start the next pack as soon as the current pack is finished so that no gap is left between packs. You may not have a withdrawal bleed until the end of the second pack but you may have spotting or breakthrough bleeding on tablet-taking days. OrStop taking tablets from your current pack, have a tablet-free break of 7 days or less (also count the day you missed your tablet) and continue with the next pack. When, following this method, you can always start your next pack on the same day of the week as you usually do.If you have forgotten tablets in a pack and you do not have the expected period in the first normal tablet-free break, you may be pregnant. Consult your doctor before you start with the next pack.you vomit: If you vomit within 3 to 4 hours after taking your this tablet tablet, the active ingredients may not have been completely absorbed. This is like missing a tablet. Therefore, follow the advice for missed tablets. you want to delay your period: you can delay your period if you start with your next pack of this tablet immediately after finishing your current pack. You can continue with this pack for as long as you wish, until this pack is empty. When you wish your period to begin, just stop tablet taking. While using the second pack you may have some breakthrough bleeding or spotting on tablet-taking days. Start with your next pack after the usual 7 days tablet free break.you want to change the starting day of your period: If you take your tablets as directed, you will have your period on about the same day every 4 weeks. If you want to change this, just shorten, (never lengthen) the next tablet- free break. For example, if your period usually starts on a Friday and in future you want it to start on Tuesday (3 days earlier) you should now start your next pack 3 days sooner than you usually do. If you make your tablet-free break very short (e.g. 3 days or less) you may not have bleeding during the break. You may have some breakthrough bleeding or spotting during the use of the next pack.you have unexpected bleeding: With all Pills, for the first few months, you can have irregular vaginal bleeding (spotting or breakthrough bleeding) between your periods. You may need to use sanitary protection, but continue to take your tablets as normal. Irregular vaginal bleeding usually stops once your body has adjusted to the Pill (usually after about 3 tablet-taking cycles). If it continues, becomes heavy or starts again, tell your doctor.you have missed a period: If you have taken all of your tablets at the right time and you have not vomited or used other medicines then you are very unlikely to be pregnant. Continue to take this tablet as usual. If you miss your period twice in row, you may be pregnant. Tell your doctor immediately. Do not start the next pack of this tablet until your doctor has checked you are not pregnant.

Side Effects

Like other contraceptives some undesirable effects may have seen with this tablet, these include venous and arterial thromboembolic disorders. The following undesirable effects have been reported in users of COCs and whether this association is causal has not been confirmed: Nausea, abdominal pain, Vomiting, diarrhoea, Weight increased, Fluid retention, Headache, Migraine, Depressed mood, mood altered, Breast pain, breast tenderness, Libido decreased, Breast hypertrophy, Rash, urticaria. In women with hereditary angioedema exogenous estrogens may induce or exacerbate symptoms of angioedema.

Toxicity

The oral LD50 of drospirenone in rats is >2000 mg/kg.

Overdose information An overdose of drospirenone, like other oral contraceptives, may lead to cause nausea or withdrawal bleeding. For drospirenone in particular, as an analog of spironolactone, may affect the levels of serum sodium and potassium. Their concentrations should be monitored in cases of overdose in addition to monitoring from metabolic acidosis and hyperkalemia, which may also result.

Precaution

The clinical and epidemiological evidence for estrogen/progestogen combinations like this tablet is predominantly based on experience with COCs in general. Therefore, the following warnings related to the use of COCs apply also to the use of this tablet. Also, increased risk of arterial, venous thrombotic and thromboembolic diseases such as myocardial infarction, deep venous thrombosis, pulmonary embolism and of cerebrovascular accidents. These events occur rarely. Cervical cancer Hypertriglyceridemia Blood pressure Jaundice Erythematosus Haemolytic uraemic syndrome Sydenham's chorea Herpes gestationis Otosclerosis-related hearing loss. Hereditary angioedema Acute or chronic disturbances of liver or kidney Crohn's disease and ulcerative colitis Chloasma The Pill and other Medicines: Some medicines may stop the Pill from working properly. These include medicines used for the treatment of epilepsy (e.g. primidone, phenyton, barbiturates) and tuberculosis (e.g. rifampicin); and antibiotics (e.g. ampilicllin, tetracyclines, griseofulvin); for some other infectious diseases. Always tell the doctor, who prescribes the Pill, which medicines you are already using. Also tell other doctor/dentist who prescribes another medicine (or the dispensing pharmacist) that you use this tablet. They can tell you if you need to take additional contraceptive precautions and if so, for how long.The Pill and Ability to Drive: There are no observed effects.

Interaction

Drugs or herbal products that induce certain enzymes (for example, CYP3A4) may decrease the effectiveness of Drospirenone or increase breakthrough bleeding. Counsel patients to use a back-up or alternative method of contraception when enzyme inducers are used with Drospirenone.

Volume of Distribution

The volume of distribution of drospirenone is estimated to be 4 L/kg, according to the FDA label for Yaz. Prescribing information from a combination of estradiol and drospirenone estimates the volume of distribution to range from 3.7- 4.2 L/kg.

Elimination Route

The absolute bioavailability of drospirenone is approximately 76% due to first-pass effects. The maximum plasma concentration of drospirenone occurs within 1 to 2 hours after oral administration and is estimated to range between 60 and 87 ng/mL. A European prescribing monograph for the combination product of estradiol and drospirenone indicates that drospirenone is both completely and rapidly absorbed. It reports a Cmax of 21.9 ng/ml, achieved approximately 1-hour post-administration. The absolute bioavailability is reported to range between 76 to 85%.

Half Life

The serum half-life of drospirenone is estimated to be 30 hours. The half-life of drospirenone metabolite excretion in the urine and feces is approximately 40 hours.

Clearance

Drospirenone is rapidly cleared, typically within 2-3 days of administration of the last active tablet. The rate of clearance of drospirenone calculated in the serum ranges from 1.2-1.5 ml/min/kg, however, this value can vary by up to 25% according to the patient.

Elimination Route

Various metabolites of drospirenone are measured in the urine and feces. Drospirenone elimination from the body is almost after 10 days post-administration when negligible amounts of drospirenone are found unchanged in both the urine and feces. Between 38% to 47% of the metabolites are identified as glucuronide and sulfate conjugates in the urine. In the feces, approximately 17% to 20% of identifiable metabolites are found to be excreted as glucuronides and sulfates.

Pregnancy & Breastfeeding use

The Pill and Breastfeeding: This tablet is generally not recommended for use during breast feeding. If you wish to take the Pill while breastfeeding, please seek the advice of your doctor.The Pill and Pregnancy: This tablet must not be used by women who are pregnant or who think they may be pregnant.

Contraindication

Preparations containing estrogen/progestogen combinations should not be used in the presence of any of the conditions listed below. If any of the conditions appear for the first time during their use, the product should be stopped immediately. Thrombosis (venous or arterial) present or in history (e.g. deep venous thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular accident) Presence or history of prodromi of a thrombosis (e.g.transient ischaemic attack, angina pectoris) Presence or history of migraine with focal neurological symptoms Diabetes mellitus with vascular involvement Disturbed lipometabolism The presence of a severe or multiple risk factor(s) for venous or arterial thrombosis may also constitute a contraindication Pancreatitis or a history thereof if associated with severe hypertriglyceridemia Presence or history of severe hepatic disease as long as liver function values have not returned to normal Severe renal insufficiency or acute renal failure Presence or history of liver tumours (benign or malignant) Known or suspected malignant conditions of the genital organs or the breasts, if sex steroid-influenced Undiagnosed vaginal bleeding Known or suspected pregnancy Hypersensitivity to any of the components of this tablet.

Storage Condition

Store below 30°C. Store all drugs properly and keep them out of reach of children.

Innovators Monograph

You find simplified version here Drospirenone + Ethinylestradiol (0.03 mg)