Drospirenone + Ethinylestradiol (0.02 mg)

Uses

This tablet is indicated for: As an oral contraceptive Treatment of moderate acne vulgaris Treatment of premenstrual dysphoric disorder (PMDD)

Drospirenone + Ethinylestradiol (0.02 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 (0.02 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 (0.02 mg) dosage

To achieve maximum contraceptive effectiveness tablets must be taken in the order directed on the package every day at about the same time. Tablet-taking should be started with the first pink tablet of the upper row & have to continue daily for 24 consecutive days. After completion of pink tablet, white tablet should be taken from 25th day to 28th day. Withdrawal bleeding usually starts on days 2-3 after starting the white tablets & don't stop taking white tablets though your menstruation is already started. Each subsequent new pack is started on the day after the last white tablet of the previous pack.No preceding hormonal contraceptive use in the past month: Tablet taking has to start on day 1 of the woman’s menstrual cycle. The woman should be instructed to take the first light pink active tablet from the upper row of this tabletaccording to the direction and in this case no additional methods of contraception are required. Starting on days 2-5 is allowed, but during the first cycle a barrier method is recommended in addition for the first 7 days of tablet-taking.Changing from another combined hormonal pill or vaginal ring or transdermal patch: In case of combined hormonal pill, woman should start with the first light pink tablet of upper row on the day after the last active tablet of her previous COC. In case of a vaginal ring or transdermal patch has been used, the woman should start using this tablet preferably on the day of removal. Changing from a progestogen-only-method (minipill, injection, implant) or from a progestogen-releasing intrauterine system (IUS): The woman may switch any day from the minipill (or from an implant or the IUS on the day of its removal, from an injectable when the next injection would be due), but should in all of these cases be advised to additionally use a barrier method (like-condom) for the first 7 days of tablet-taking.Following first-trimester abortion: The woman may start immediately and in this case no need to take additional contraceptive method.Following delivery or second-trimester abortion: Women are advised to start at day 21 to 28 after delivery or second-trimester abortion. When starting later, the woman are advised to additionally use a barrier method (like-condom) for the first 7 days of tablet-taking. Management of Missed Tablets: Missed white pills from the last row of the blister are placebo tablets and thus can be disregarded. But if you forgot to take a light pink tablet one day, take the missed tablet as soon as you remember. This may mean taking two tablets the very next day. Additionally you should use some other method of contraception (like a condom) until next 7 days. If you forget to take the tablets for two continuous days, then it is likely that you will no longer be protected against pregnancy. You should therefore discontinue taking the tablet and adopt some other temporary methods (condom/foam tablet) till your next menstruation. Discard the unfinished pack of tablets and start taking tablets from the light pink tablet of the top row of a fresh pack from the first day of next menstruation.If you have missed a period after taking tablet: If you have taken all of your pills at the right time and you have not vomited or used other medicines then you are very unlikely to be pregnant. Continue to take tablet as usual. If you miss your period twice in a 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. How to Delay a Period: To delay period women should continue with another new pack of this tablet just after finishing the light pink active tablet of the present pack (that is no need to take white placebo tablet of present pack). The extension can be carried on for as long as wished until the end of light pink color tablet of the second pack. When women wish their period to begin, just stop tablet taking. While using the second pack woman may have some breakthrough bleeding or spotting. Start with your next pack after the usual 4 day white inactive tablet interval.Advice in case of Vomiting: If vomiting occurs within 3-4 hours after light pink tablet taking, absorption may not be complete. In such an event, the advice concerning management of missed tablets is applicable. The woman must take the extra active tablet (light pink color) needed from a back up pack after vomiting.

Side Effects

Different types of tablet suit to different types of woman. At the initial stage some women may experience side-effects like dizziness, headache, breast pain, nausea or unscheduled uterine bleeding. These symptoms may occur in >3% of users. After starting one brand of oral contraceptive tablets, if you feel any inconvenience such as migraine, changes in eyesight or speech, unusual pain or swelling in your legs, sharp chest pains or shortness of breath, rash, yellow skin or a rise in blood pressure take immediate advice from your doctor.

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

If any circulatory disorder (like- myocardial infarction, deep venous thrombosis, pulmonary embolism, cerebrovascular injury etc) or other risk factors(like smoking, obesity, hypertension, dyslipidemia, migraine, atrial fibrillation etc) are present, the benefits of COC use should be weighed against the possible risks for each individual woman and discussed with the woman before she decides to start using it. In the event of aggravation, exacerbation or first appearance of any of these conditions or risk factors after taking pill, the woman should contact with her physician. The physician should then decide on whether its use should be discontinued.

Interaction

Interactions between ethinylestradiol and other drugs may lead to decreased or increased ethinylestradiol concentrations, respectively. Decreased ethinylestradiol serum concentrations may cause an increased incidence of breakthrough bleeding and menstrual irregularities and may possibly reduce efficacy of the oral contraceptive. Example of substances that may decrease serum ethinylestradiol concentrations include rifampicin, phenytoin, primidone, rifabutin, dexamethasone, griseofulvin, topiramate, some protease inhibitors, modafinil, ritonavir and barbiturates. Certain antibiotics including ampicillin, other penicillins and tetracyclines may reduce the efficacy of oral contraceptives. During concomitant use of this tablet & other drugs that may lead to decreased ethinylestradiol serum concentrations, it is recommended that a non hormonal back-up method of contraception to be used in addition to the regular intake of this tablet.

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

Use during pregnancy: This is contraindicated during pregnancy. Pregnancy must be excluded before starting this tablet. If pregnancy occurs during use of this tablet, the preparation must be withdrawn immediately. Women who discontinue oral contraceptives with the intent of becoming pregnant, a non-hormonal method of contraception is recommended for three months before attempting to conceive.Use during lactation: Lactation may be influenced by combined pill as they may reduce the quantity and change the composition of breast milk, therefore the use of estrogen containing combined pill should generally not be recommended until the nursing mother has completely weaned her child. Small amounts of the contraceptive steroids and/or their metabolites may be excreted with the milk.

Contraindication

This tablet should not be used: Known or suspected pregnancy If you have heart disease, clotting of blood in the vein If you suffer from liver disease or jaundice If you suffer from high blood pressure, migraine, feel something hard in your breast, diabetes with vascular involvement, experience excessive bleeding for which no reason has yet been ascertained The presence or a history of venous or arterial thromboembolic events (e.g. deep venous thrombosis, pulmonary embolism, myocardial infarction or of a cerebrovascular accident) History of migraine with focal neurological symptoms Pancreatitis or a history thereof if associated with severe hypertriglyceridaemia Severe renal insufficiency or acute renal failure Presence or history of liver tumours (benign or malignant) Undiagnosed vagina! bleeding Hypersensitivity to any of the components of this preparation.

Special Warning

Pediatric Use: This is only indicated after menarche. There is no data suggesting the need for a dosage adjustment.Use in the Elderly: This is not indicated after menopause.

Acute Overdose

Symptoms of oral contraceptive overdose may include nausea, vomiting, breast tenderness, dizziness, abdominal pain, drowsiness/fatigue; withdrawal bleeding may occur in females. There is no specific antidote and further treatment of overdose, if necessary, is directed to the symptoms.

Storage Condition

Do not store above 30°C. Keep away from light and out of the reach of children.

Innovators Monograph

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