Exlutena

What Is Exlutena and What Is It Used For?

Exlutena is a progestogen-only oral contraceptive (mini-pill) that contains a low dose of the synthetic progestogen lynestrenol (0.5 mg). It is used to prevent unwanted pregnancy and works primarily by thickening the cervical mucus and, in most women, by also suppressing ovulation.

Exlutena belongs to a category of hormonal contraceptives known as progestogen-only pills (POPs), commonly referred to as mini-pills. Unlike combined oral contraceptives (COCs), which contain both an oestrogen and a progestogen, Exlutena contains only one type of female sex hormone – a progestogen called lynestrenol. This important distinction makes Exlutena a suitable contraceptive option for women who cannot or prefer not to use oestrogen-containing birth control.

The contraceptive effect of Exlutena relies on two main mechanisms. First, lynestrenol causes the mucus in the cervix (the neck of the womb) to become thick and viscous, creating a barrier that is difficult for sperm to penetrate. This prevents sperm from reaching and fertilising an egg. Second, in approximately 70% of women taking Exlutena, ovulation (the release of an egg from the ovary) is suppressed. This dual mechanism provides reliable protection against pregnancy when the pill is taken correctly.

When taken as directed – at the same time every day without missing any tablets – the risk of becoming pregnant while using Exlutena is very low. The typical-use failure rate for progestogen-only pills is approximately 7–9%, while perfect-use rates are considerably lower, at approximately 0.3–0.5% per year. The difference between typical and perfect use highlights the importance of strict adherence to daily timing with this type of contraceptive.

Exlutena is particularly recommended for women in the following situations:

• Breastfeeding mothers: Because it does not contain oestrogen, Exlutena will not reduce milk supply or affect milk quality, making it a preferred choice during lactation
• Women who cannot tolerate oestrogen: Those who experience oestrogen-related side effects such as headaches, nausea, or mood changes with combined pills may benefit from switching to Exlutena
• Women with oestrogen-related contraindications: Those with a history of migraine with aura, certain cardiovascular risk factors (such as smoking over age 35), or a history of venous thromboembolism may be advised against oestrogen-containing contraceptives but can often safely use a progestogen-only pill

What Should You Know Before Taking Exlutena?

Before starting Exlutena, inform your doctor about all your medical conditions, particularly any history of blood clots, liver disease, hormone-sensitive cancers, or unexplained vaginal bleeding. Exlutena does not protect against sexually transmitted infections including HIV/AIDS.

Contraindications

You should not take Exlutena if any of the following apply to you. If any of these conditions apply, tell your doctor or midwife before starting Exlutena. You may be advised to use a non-hormonal method of contraception instead:

• Active venous thromboembolism (blood clot) – either deep vein thrombosis (a clot in the legs) or pulmonary embolism (a clot in the lungs)
• Jaundice (yellowing of the skin) or severe liver disease – since lynestrenol is metabolised by the liver, impaired liver function can affect the drug's safety profile
• Known or suspected hormone-sensitive tumours – including certain types of breast cancer that are stimulated by hormonal exposure
• Unexplained vaginal bleeding – any abnormal genital bleeding must be investigated before starting hormonal contraception
• Allergy (hypersensitivity) to lynestrenol or any of the other ingredients in Exlutena, including lactose monohydrate, potato starch, amylopectin, and magnesium stearate

If any of these conditions develop for the first time, worsen, or recur while you are using Exlutena, you should stop taking it and contact your doctor or midwife promptly.

Warnings and Precautions

Exlutena can be used by most women, but certain medical conditions require closer monitoring. Talk to your doctor or midwife before taking Exlutena if you have or have had any of the following:

• Breast cancer – a personal or family history requires careful medical assessment
• Liver cancer – your doctor will assess whether Exlutena is appropriate
• Previous blood clots (thrombosis) – a history of venous or arterial thrombosis increases risk and requires evaluation
• Diabetes mellitus – progestogen-only pills may affect blood sugar control; monitoring may be needed
• Previous ectopic pregnancy – a pregnancy that developed outside the uterus increases vigilance for this risk during POP use
• History of fallopian tube infection or surgery – may increase the risk of ectopic pregnancy
• Epilepsy – certain anti-epileptic medications can reduce Exlutena's effectiveness
• Tuberculosis – rifampicin treatment can reduce contraceptive efficacy
• High blood pressure (hypertension) – regular blood pressure monitoring may be recommended
• Chloasma (brown pigmentation patches on the face) – if you have had or currently have chloasma, avoid excessive sun exposure and ultraviolet radiation while taking Exlutena

Contraceptive Pills and Breast Cancer

All women face some risk of developing breast cancer, regardless of whether they use contraceptive pills. Research has found that breast cancer is diagnosed slightly more often in women who use oral contraceptives compared to women of the same age who do not. After stopping the pill, the increased risk gradually decreases, and within 10 years of stopping, the risk returns to the same level as women who have never used the pill.

Breast cancer is rare in women under 40 years of age, but the risk increases with age. Among 10,000 women who have used oral contraceptives for up to 5 years but stop at age 20, there would be fewer than 1 extra case of breast cancer (in addition to the 4 normally expected). Among 10,000 women who stop at age 30, there would be 5 extra cases (in addition to the 44 normally expected). Among those who stop at age 40, there would be 20 extra cases (in addition to the 160 normally expected).

Breast cancers diagnosed in women who use oral contraceptives tend to be at an earlier, less advanced stage than those found in non-users. It is not known whether this difference is caused by the pills or because pill users tend to have more frequent medical check-ups, leading to earlier detection.

Contraceptive Pills and Thrombosis

Thrombosis is the formation of a blood clot that can block a blood vessel. Deep vein thrombosis (DVT) occurs when a clot forms in the deep veins of the legs. If such a clot breaks free, it can travel to the lungs and cause a pulmonary embolism, which can be life-threatening. DVT is uncommon and can occur regardless of whether you take contraceptive pills. It can also occur during pregnancy.

The risk of thrombosis is considered to be lower with progestogen-only pills like Exlutena compared to combined oral contraceptives that contain oestrogen. This is one of the key reasons why progestogen-only pills may be preferred for women with certain cardiovascular risk factors. Nevertheless, if you notice any signs of thrombosis, you should contact your doctor immediately.

Ovarian Cysts

Small, fluid-filled cysts (known as functional ovarian cysts) can develop on the ovaries when using progestogen-only pills. These cysts are usually harmless and disappear on their own without treatment. Occasionally, they may cause lower abdominal pain. In very rare cases, more significant complications can arise that require medical attention.

Mental Health

Some women using hormonal contraceptives, including Exlutena, have reported depressed mood or depression. Depression can be serious and may sometimes lead to suicidal thoughts. If you experience mood changes or symptoms of depression, contact your doctor for advice as soon as possible.

Pregnancy and Breastfeeding

Pregnancy: Exlutena must not be used by women who are pregnant or who suspect they may be pregnant. If you become pregnant while taking Exlutena, stop taking it immediately and consult your doctor.

Breastfeeding: Exlutena does not affect the quality or quantity of breast milk. Only very small amounts of the active substance (approximately 0.14% of the maternal dose) pass into breast milk, and there is no evidence of any risk to the breastfed infant. However, if you wish to use Exlutena while breastfeeding, you should consult your doctor or midwife first.

Driving and Operating Machinery

No effects on the ability to drive or use machines have been observed with Exlutena.

Lactose Content

Exlutena contains approximately 43 mg of lactose monohydrate per tablet. If you have been told by your doctor that you have an intolerance to certain sugars, contact your doctor or midwife before starting Exlutena.

How Does Exlutena Interact with Other Drugs?

Several medications can reduce Exlutena's contraceptive effectiveness by increasing the rate at which lynestrenol is broken down in the body. These include certain anti-epileptic drugs, antibiotics used for tuberculosis, HIV medications, antifungals, and herbal preparations containing St. John's Wort.

Exlutena's active ingredient lynestrenol is metabolised by liver enzymes. Drugs that induce (speed up) these enzymes can reduce lynestrenol blood levels, potentially decreasing contraceptive efficacy. If you are taking or have recently taken any other medications – including herbal remedies and over-the-counter products – tell your doctor, midwife, or pharmacist. They will advise you whether additional contraceptive precautions are needed and for how long.

Major Interactions – Reduced Contraceptive Efficacy

Moderate Interactions

Exlutena may also affect the action of other medicines. Always tell your doctor, midwife, or pharmacist about all medications you are taking, including any herbal or natural remedies. Your prescriber can advise whether additional contraceptive precautions are needed and for how long.

What Is the Correct Dosage of Exlutena?

Take one Exlutena tablet daily at approximately the same time every day, without any breaks between packs. Each blister pack contains 28 tablets. Swallow the tablet whole with water. Being more than 3 hours late taking your pill may reduce contraceptive protection.

Always take Exlutena exactly as prescribed by your doctor or midwife. The strict timing of progestogen-only pills is critical for maintaining reliable contraceptive protection. Unlike combined pills, there is no hormone-free interval – you take one tablet every day, continuously.

How to Take the Tablets

Starting Exlutena for the First Time

Missed Dose

The timing window for progestogen-only pills is narrow. If you are less than 3 hours late, take the missed tablet as soon as you remember and continue taking your pills at the normal time. Your contraceptive protection is maintained.

If you are more than 3 hours late, your contraceptive protection may be reduced. Take the missed tablet as soon as you remember and continue taking subsequent tablets at the normal time. In addition, use barrier contraception (e.g. condoms) for the next 7 days. If you missed one or more tablets during the very first week of use and had unprotected sex in the week before the missed tablets, there is a risk of pregnancy. Consult your doctor or midwife for advice.

Vomiting or Severe Diarrhoea

If you vomit or have used activated charcoal within 3–4 hours of taking your Exlutena tablet, or if you have severe diarrhoea, the active substance may not have been fully absorbed. In this case, follow the same advice as for a missed tablet: use additional barrier contraception for the next 7 days.

Overdose

Stopping Exlutena

You can stop taking Exlutena whenever you wish. If you stop because you want to try to become pregnant, it is generally recommended to wait until you have had your first normal menstrual period before attempting to conceive. This helps your doctor or midwife date the pregnancy more accurately. Use a non-hormonal method of contraception in the meantime if you wish to avoid pregnancy.

Unexpected Bleeding

Irregular vaginal bleeding is common when taking progestogen-only pills. This can range from light spotting to bleeding resembling a period. Some women may not have any bleeding at all. These bleeding irregularities do not mean that contraceptive protection is reduced. Usually, no action is needed – simply continue taking Exlutena as normal. If bleeding becomes heavy or prolonged, contact your doctor or midwife.

What Are the Side Effects of Exlutena?

The most common side effects of Exlutena include irregular menstrual bleeding, absence of periods, breast tenderness, headache, nausea, and mood changes. Most side effects are mild and tend to improve over the first few months of use.

Like all medicines, Exlutena can cause side effects, although not everybody experiences them. Serious side effects associated with oral contraceptives are described in the sections on breast cancer, thrombosis, and ovarian cysts above. If any side effect becomes severe or persistent, consult your doctor, midwife, or pharmacist.

If you experience any side effects not listed here, or if any side effect becomes severe or troublesome, contact your doctor, midwife, or pharmacist. Reporting suspected side effects after the medicine has been authorised is important, as it allows continuous monitoring of the medicine's benefit-risk balance.

How Should You Store Exlutena?

Store Exlutena tablets out of the sight and reach of children. Do not use after the expiry date printed on the carton. No special storage temperature is required.

Keep this medicine in its original packaging to protect it from light and moisture. Check the expiry date (marked “EXP” on the packaging) before taking any tablets. The expiry date refers to the last day of the stated month. Do not use Exlutena after this date.

Do not flush unused tablets down the toilet or throw them into household waste. Return any unused or expired medication to your pharmacy for safe disposal. These measures help protect the environment from pharmaceutical contamination.

What Does Exlutena Contain?

Each Exlutena tablet contains 0.5 mg of the active ingredient lynestrenol (a progestogen hormone) along with inactive ingredients including potato starch, amylopectin, lactose monohydrate, and magnesium stearate.

Active Ingredient

The active substance is lynestrenol, a synthetic progestogen hormone. Each tablet contains 0.5 mg of lynestrenol. Lynestrenol is a prodrug that is converted in the body to its active metabolite norethisterone, which exerts the progestogenic effects responsible for contraception.

Inactive Ingredients (Excipients)

The other ingredients are: potato starch, amylopectin, lactose monohydrate (approximately 43 mg per tablet), and magnesium stearate. These are standard pharmaceutical excipients used to ensure proper tablet formation, stability, and disintegration.

Tablet Appearance and Packaging

Appearance: White, round tablets marked with “TT2” on one side and “ORGANON” on the other.

Pack sizes: Each blister pack contains 28 tablets. Each box contains 1 or 3 blister packs.

Manufacturer: N.V. Organon, Oss, The Netherlands.

How Does Exlutena Work in the Body?

Exlutena works through a dual mechanism: it thickens the cervical mucus to prevent sperm penetration and suppresses ovulation in approximately 70% of women. Lynestrenol is converted to norethisterone in the liver, which is the active progestogenic metabolite responsible for these effects.

Lynestrenol, the active ingredient in Exlutena, is a 19-nortestosterone derivative that acts as a prodrug. After oral administration, it is rapidly absorbed from the gastrointestinal tract and converted in the liver to norethisterone (also known as norethindrone), which is the pharmacologically active metabolite. Norethisterone then exerts progestogenic effects throughout the body.

The primary contraceptive mechanism of Exlutena is its effect on the cervical mucus. Under the influence of the progestogen, the mucus produced by the cervix becomes thick, scanty, and highly viscous. This creates a physical barrier that is extremely difficult for sperm to penetrate, effectively preventing them from reaching the uterus and fallopian tubes where fertilisation would normally occur.

The secondary mechanism involves the suppression of ovulation. In approximately 70% of women taking Exlutena, the progestogen prevents the pituitary gland from releasing the surge of luteinising hormone (LH) that normally triggers ovulation. Without this LH surge, no egg is released from the ovary, making fertilisation impossible. This ovulation-suppressive effect is more consistent than with some other progestogen-only pills that use lower-potency progestogens.

Additionally, lynestrenol/norethisterone affects the endometrium (the lining of the uterus). The progestogen causes the endometrial lining to become thinner and less suitable for implantation of a fertilised egg. While this endometrial effect is considered a secondary mechanism, it provides an additional layer of contraceptive protection.

Pharmacokinetic Profile

After oral administration, lynestrenol is rapidly and almost completely absorbed from the gastrointestinal tract. It undergoes extensive first-pass metabolism in the liver, where it is converted to norethisterone by the cytochrome P450 enzyme system. Peak plasma concentrations of norethisterone are typically reached within 2–4 hours. The elimination half-life of norethisterone is approximately 8–11 hours, which necessitates strict daily dosing at the same time each day to maintain effective contraceptive blood levels.

Because of this relatively short half-life, the 3-hour window for late pills is critical. Beyond this window, progestogen blood levels may drop below the threshold needed to maintain the cervical mucus barrier, potentially allowing sperm penetration. This is why strict timing adherence is more important with progestogen-only pills than with combined oral contraceptives, which have a more forgiving 12-hour window.

Frequently Asked Questions About Exlutena