Drug Name

Ovral (Ethinyl Estradiol and Norgestrel)

 Drug Uses

Oral contraceptives (birth-control pills) are used to prevent pregnancy. Estrogen and progestin are two female sex hormones. Combinations of estrogen and progestin work by preventing the release of eggs from the ovaries (ovulation) and changing the cervical mucus and the lining of the uterus. Oral contraceptives are a very effective method of birth control, but they do not prevent the spread of AIDS and other sexually transmitted diseases.

Take Ovral exactly as it was prescribed for you. Do not take larger amounts, or take it for longer than recommended by your doctor. You will take your first pill on the first day of your period or on the first Sunday after your period begins (follow your doctor's instructions).

You may need to use back-up birth control, such as condoms or a spermicide, when you first start using Ovral. Follow your doctor's instructions.

The 28-day birth control pack contains seven "reminder" pills to keep you on your regular cycle. Your period will usually begin while you are using these reminder pills.

Take one pill every day, no more than 24 hours apart. When the pills run out, start a new pack the following day. Get your prescription refilled before you run out of pills completely.

If you need to have any type of medical tests or surgery, or if you will be on bed rest, you may need to stop using Lo Ovral for a short time. Any doctor or surgeon who treats you should know that you are using Lo Ovral.

Your doctor will need to see you on a regular basis while you are using Ovral. Do not miss any appointments.

 Drug Class and Mechanism

Ethinylestradiol and norgestrel are rapidly and almost completely absorbed from the gastrointestinal tract. Ethinylestradiol is subject to considerable first-pass metabolism with a mean bioavailability of 40-45%. Norgestrel does not undergo first-pass metabolism and is therefore completely bioavailable.

Norgestrel is extensively plasma protein bound both to sex hormone binding globulin (SHBG) and albumin. Ethinyl-estradiol, however, is bound in plasma only to albumin and enhances the binding capacity of SHBG. Following oral administration, peak plasma levels of each medicine occur within 1 to 4 hours.

The elimination half-life for ethinylestradiol is approximately 25 hours. It is primarily metabolised by aromatic hydroxylation but a wide variety of hydroxylated and methylated metabolites are formed, and these are present both free and as conjugates with glucuronide and sulphate. Conjugated ethinylestradiol is excreted in bile and subject to enterohepatic recirculation. About 40% of the medicine is excreted in the urine and 60% is eliminated in the faeces.

The elimination half-life for norgestrel is approximately 24 hours. The medicine is primarily metabolised by reduction of the A ring followed by glucuronidation. About 60% of norgestrel is excreted in the urine and 40% is eliminated in the faeces.

Missing a pill increases your risk of becoming pregnant.

If you miss one "active" pill, take two pills on the day that you remember. Then take one pill per day for the rest of the pack.

If you miss two "active" pills in a row in week one or two, take two pills per day for two days in a row. Then take one pill per day for the rest of the pack. Use back-up birth control for at least 7 days following the missed pills.

If you miss two "active" pills in a row in week three, or if you miss three pills in a row during any of the first 3 weeks, throw out the rest of the pack and start a new one the same day if you are a Day 1 starter. If you are a Sunday starter, keep taking a pill every day until Sunday. On Sunday, throw out the rest of the pack and start a new one that day.

If you miss three "active" pills in a row during any of the first 3 weeks, throw out the rest of the pack and start a new pack on the same day if you are a Day 1 starter. If you are a Sunday starter, keep taking a pill every day until Sunday. On Sunday, throw out the rest of the pack and start a new one that day.

If you miss any reminder pills, throw them away and keep taking one pill per day until the pack is empty. You do not need back-up birth control if you miss a reminder pill.

Store Ovral at room temperature away from moisture and heat.

 Warnings/Precautions

Concurrent use of antibiotics or anticonvulsants may reduce the effective concentrations of the steroids and hence impair the contraceptive effect (see INTERACTIONS ).

Diarrhoea or vomiting can jeopardise the contraceptive effect by affecting absorption.

A thorough history and physical examination should be performed before prescribing oral contraceptives with special attention given to blood pressure, breasts, abdomen, and pelvic organs. As a general rule, oral contraceptives should not be prescribed for longer than one year without another physical examination being performed.

Under the influence of estrogen-containing oral contraceptives, pre-existing uterine leiomyomata may increase in size.

Oral contraceptives may cause depression. Patients with a history of depression should be carefully observed and the medicine discontinued if depression recurs to a serious degree.

These agents may cause some degree of fluid retention. Women with cardiac or renal dysfunction, convulsive disorders, migraine, or asthma require careful observation since these conditions may be exacerbated by the fluid retention which may occur in users of oral contraceptives.

Cholestatic jaundice has been reported in users of oral contraceptives. If this occurs, the medicine should be discontinued. Patients with a history of jaundice during pregnancy should be carefully observed whilst taking oral contraceptives.

Steroid hormones may be poorly metabolised in patients with impaired liver function and should be administered with caution to such patients.

Users of oral contraceptives may have disturbances in normal tryptophan metabolism which may result in a relative pyridoxine deficiency. The clinical significance of this is yet to be determined.

Serum folate levels may be depressed by oral contraceptive use. Women who become pregnant shortly after discontinuing these medicines may have a greater chance of developing folate deficiency and its complications.

 Possible Side Effects

Oral contraceptives may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

- upset stomach
- vomiting
- stomach cramps or bloating
- diarrhea
- constipation
- gingivitis (swelling of the gum tissue)
- weight gain or weight loss
- brown or black skin patches
- acne
- swelling of the hands, feet, or lower legs (fluid retention)
- hair growth in unusual places
- bleeding or spotting between menstrual periods
- changes in menstrual flow
- painful or missed periods
- breast tenderness, enlargement, or discharge
- difficulty wearing contact lenses

Some side effects can be seious. The following symptoms are uncommon, but if you experience any of them, call your doctor immediately:

- severe headache
- shortness of breath
- severe vomiting
- partial or complete loss of vision
- double vision
- speech problems
- dizziness or faintness
- weakness or numbness of an arm or leg
- crushing chest pain or chest heaviness
- coughing up blood
- calf pain
- severe stomach pain
- yellowing of the skin or eyes
- severe depression
- unusual bleeding
- loss of appetite
- extreme tiredness, weakness, or lack of energy
- fever
- dark-colored urine
- light-colored stool
- rash

Oral contraceptives may increase the risk of developing endometrial and breast cancer, gallbladder disease, liver tumors, heart attack, stroke, and blood clots. Talk to your doctor about the risks of taking this medication.

Oral contraceptives may cause other side effects. Call your doctor if you have any unusual problems while taking Ovral.

 More Information

Keep all appointments with your doctor and the laboratory. You should have a complete physical examination every year, including blood pressure measurements, breast and pelvic exams, and a Pap test. Follow your doctor's directions for examining your breasts; report any lumps immediately.

Before you have any laboratory tests, tell the laboratory personnel that you take oral contraceptives, as this medication may interfere with some laboratory tests.

If you miss one menstrual period and have taken your tablets as directed, continue taking them. However, if you miss one period and have not taken your tablets as directed or if you miss two menstrual periods and have taken the tablets as directed, call your doctor and use another method of birth control until you have a pregnancy test.

If you wish to stop taking oral contraceptives and become pregnant, use another method of birth control for at least 3 months after you stop taking the tablets to be sure that the medication will not harm the fetus. It may take a long time for you to become pregnant after you stop taking oral contraceptives, especially if you have never had a baby or if you had irregular, infrequent, or complete absence of menstrual periods before taking oral contraceptives. Questions should be discussed with your doctor.

Do not let anyone else take your medication.