Norgestrel (Opill) - Indication, Dosage, Precautions, Side Effects, and Pharmacological Aspects

Drug Overview:

Norgestrel tablets, Opill tablets, and other progestin-only oral contraceptives work to prevent conception by suppressing ovulation in about half of the users' cycles, thickening cervical mucus to prevent sperm penetration, lowering midcycle LH (luteinizing hormone) and FSH (follicle stimulating hormone) peaks, slowing the passage of the ovum through the fallopian tubes, and changing the endometrium. Opill (Norgestrel) became the first everyday-use oral contraceptive since the FDA (U.S. Food and Drug Administration) approved it as a nonprescription medication for preventing pregnancy on July 13, 2023.

For Patients

What Are the Clinical Indications for Norgestrel?

Norgestrel tablets are indicated for any female of conceivable age to prevent pregnancy. It is not meant for protection against unprotected sex and should not be used as emergency contraceptive pills.

What Is the Dosage of Norgestrel?

There are 28 pills in a blister packet of Opill. Each pill contains 0.075 mg (milligrams) of Norgestrel.

• One tablet is taken by mouth every day at the same time.

• The dosage should be noted, and there should be no gaps between pill packs.

• The first pack can be started any day.

• Suppose a person is transitioning from prior methods like a vaginal ring, patch, or other oral contraceptive. In that case, they must start using Norgestrel a day after ceasing these prior contraceptive methods.

• For each sexual encounter within the first two days after starting the medication, use a condom (or another barrier device) to prevent contraception along with the medicine.

What Are the Things to Inform the Doctor Before Taking the Drug?

The patient must inform the doctor if they are on other medications before starting this drug.

They should also inform them about the below-mentioned conditions:

• Pregnancy.

• Heart disease.

• Liver disease.

• Migraines.

• Seizures.

• Kidney diseases.

• Bleeding from the vagina.

• Stroke.

• Cancer (especially breast, cancer, or cervical).

• Depression.

• Breastfeeding.

• Diabetes.

How Is Norgestrel Administered?

Take this drug orally. One can take it with or without meals. Follow the instructions on the medication label. Take this medication as prescribed on the label simultaneously every day. Do not take the medicine more frequently than recommended. This medicine can be administered to children who have begun their menstrual period. To discuss the use of this drug in children, speak with the medical team. One might need to exercise extra caution while administering the drug to children.

What Are the Side Effects of Norgestrel?

• Headache and dizziness.

• Irregularity in the menstrual cycle.

• Appetite increases.

• Nausea and vomiting.

• Acne.

• Pain and discomfort in the breast.

• Tiredness.

• Discharge from the vagina.

• Pain in the stomach and cramps.

• Painful menstruation.

• Pain in the back.

Missed Dose:

Following the label's directions is crucial to guaranteeing the prescribed medications' efficacy in preventing pregnancy. The pregnancy risk might rise if a dosage is missed or taken after the recommended time.

Following are some suggestions:

• The individual should take the missing drug dose as soon as they remember it, even if it is just delayed by a few hours (3 hours). Continue taking one pill at the scheduled time every day. Additionally, during the next 48 hours, utilize a backup birth control technique (such as condoms).

• It is important to use a different method of birth control for the rest of the pill pack until the period comes if a person misses more than one dose. It is done to reduce the possibility of an unwanted pregnancy. It is also important to remember that, depending on the kind and brand of the birth control pill, the recommendations for missing doses may change. Always check the package insert or a healthcare team member for exact instructions.

• It is advised to speak with the healthcare provider if a person has missed more than one dose or is unsure what to do. Healthcare workers can advise and suggest the best course of action.

Overdose:

Opill (Norgestrel) tablet overdose may present with symptoms that include vomiting, nausea, pain or sensitivity in the breast region, lightheadedness, drowsiness, and an irregular bleeding pattern (withdrawal bleeding) in females. Remembering that an oral contraceptive overdose has no particular antidote is crucial. If an overdose occurs, additional therapy, if required, will concentrate on controlling the person's symptoms.

Storage:

Keeping the drug in its original package and container is necessary. It must be safely secured and out of the children's reach. This action ensures their safety. Since bathrooms have substantial moisture levels, never keep or store drugs there. It should always be kept for storage at the optimal room temperature.

For Doctors

Indication:

Norgestrel (Opill) tablets should not be used as an emergency method of contraception since they are designed for regular use by females of reproductive potential as an effective way of preventing pregnancy.

Dose:

The recommended daily dose is 0.75 mg per day, taken simultaneously every day.

Dosing Considerations:

Inform the patient before prescribing Norgestret (Opill) tablets:

• Opill tablets should always be taken simultaneously each day, regardless of bleeding episodes. To guarantee the success of this contraceptive technique, consistent daily ingestion is essential.

• It is crucial that women using Norgestrel tablets use a non-hormonal backup form of contraception (such as condoms or spermicides) for the following 48 hours if their pill intake is delayed by three hours or more or if they have vomiting or diarrhea within four hours of taking the pill. This cautious strategy reduces the possibility of an unplanned pregnancy while preserving the effectiveness of the contraceptive method.

• Women who use Norgestrel tablets may experience changes to their typical menstrual cycle. It is crucial to remember that a woman should immediately take a pregnancy test if she skips two periods or one period while simultaneously skipping doses of Norgestrel. This preventative measure aids in spotting probable pregnancies and enables prompt management and decision-making.

• If a woman using Opill tablets develops frequent vaginal postcoital bleeding, prolonged bleeding, amenorrhea (lack of menstruation), or severe stomach discomfort, she must immediately notify her healthcare physician. By promptly reporting such symptoms, thorough assessment and appropriate medical care may be provided to treat any potential underlying problems or concerns.

• Norgestrel tablets do not offer any protection against AIDS or other STIs (sexually transmitted infections), including HIV infection. People who use Norgestrel tablets as a form of contraception must take additional precautions, such as wearing condoms or other barrier techniques, to lower their risk of contracting sexually transmitted illnesses.

What Are the Pharmacological Aspects of Norgestrel?

Mechanism Of Action

Norgestrel tablets are progestin-only tablets that act according to the mechanism described below:

• Ovulation Suppression: Users of Norgestrel tablets experience ovulation suppression in about 50 percent of their menstrual cycles. This implies that the egg's ability to exit the ovary is hindered, which lowers the likelihood of fertilization.

• Cervical Mucus Thickening: Norgestrel tablets thicken cervical mucus, forming a barrier that prevents sperm from entering the uterus and fallopian tubes. This reduces the chance of fertilization even further.

• Lowering LH and FSH Levels: Luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are hormones involved in the regular menstrual cycle, are reduced by Norgestrel tablets. Further suppressing the ovulation process lowers the peaks of these hormones.

• Slowing the Ovum's Movement: Norgestrel tablets can reduce the speed at which the egg travels through the fallopian tubes. As a result, there are fewer odds of the sperm fertilizing the egg.

• Alteration of the Endometrium: Norgestrel tablets may also change the endometrium, which makes it less amenable to a fertilized egg's implantation. Even if fertilization takes place, this helps prevent pregnancy by blocking implantation.

Pharmacokinetics

• Serum progestin levels peak two hours after oral administration and are quickly distributed throughout the body and eliminated. Serum progestin levels are nearly back to baseline 24 hours after taking the prescription, showing that careful adherence to the recommended dose schedule is necessary for the medication to work as intended.

• Serum progesterone levels might differ significantly across users. Lower steady-state progestin levels and a shorter elimination half-life are attained when progestin is supplied alone without the simultaneous administration of estrogens.

• To ensure the effectiveness of Opill tablets, it is essential to maintain constant and prompt adherence to the recommended dose schedule. Furthermore, the differences in serum levels across users emphasize the importance of individualized medical supervision and monitoring to maximize the drug's efficacy.

Clinical Studies and Efficacy:

• 144 women with proven fertility received Norgestrel, a progestogen-only oral contraceptive, continuously at 75 mg/day for 30 months. It was found to be an effective contraceptive.

• The conception rates for the whole study period were 2.1 percent overall and 1.3 pregnancies per 100 women per year.

• About one-fifth of the cycles lasted fewer than 17 days due to Norgestrel's high percentage of irregular and often brief bleeding intervals.

• The observed irregularity in menstrual periods when using Opill Tablets is due more to differences in cycle duration between women than to irregularities between subsequent cycles.

• Importantly, throughout the trial, no verified cases of thromboembolism were linked to this contraception.

Norgestrel is an effective substitute for combination oral contraceptives for women who are unsuitable for or unable to take estrogen-containing preparations, despite its main clinical and laboratory properties as well as its simple route of administration. For some people looking for contraceptive options, its effectiveness and tolerability make it a viable choice.

What Are the Contraindications to Norgestrel?

Norgestrel is contraindicated for women with the following conditions:

• Pregnancy or suspected pregnancy, as it can lead to abortion.

• Breast cancer, which is known to exist or has previously existed, and any other progestin-sensitive malignancy.

• Liver tumors, both benign and malignant.

• Acute liver illness.

• Undiagnosed uterine hemorrhage that is abnormal.

• Allergic reactions to the constituents of the drug.

Warnings and Precautions:

• Ectopic Pregnancy - Approximately 5 ectopic pregnancies per 1000 woman-years occur among users of oral contraceptives that exclusively contain progestin. Up to 10 percent of reported pregnancies were discovered to be ectopic in clinical investigations of people using oral contraceptives containing progestin. Therefore, while treating women who become pregnant or experience lower abdominal discomfort while using Norgestrel (Opill) tablets, medical providers need to be alert for the likelihood of an ectopic pregnancy.

• Delayed Follicular Atresia and Ovarian Cysts- When follicular development takes place, there may be a delay in the atresia (degeneration) of the follicle, causing it to expand beyond the size it would normally attain in a regular menstrual cycle. However, these swollen follicles often go away on their own without treatment. Even though they are frequently asymptomatic, some people may suffer stomach pain. In rare cases, these swollen follicles might twist or burst, which calls for surgical intervention. It is crucial to remember that such problems only happen sometimes.

• Liver Cancer and Liver Disease - It is critical to stop using Norgestrel (Opill) tablets as soon as one notices jaundice or severe liver function changes while taking them. One should not start taking the pills again until the liver function markers are back to normal and the possibility that the pills have caused them has been eliminated. To evaluate the condition of the liver and choose the best course of action, it is crucial to speak with a healthcare practitioner. One should not think about starting to take Norgestrel (Opill) tablets again until it is certain that the liver function is returning to normal and the possibility of Norgestrel (Opill) tablets causing it has been ruled out.

• Alterations in the Bleeding Pattern - Women who use Norgestrel tablets may experience irregular menstrual cycles. It is, therefore, crucial to assess and identify any untreated irregular uterine bleeding before giving Opill.

  • In a clinical trial on 2575 patients, around half reported alterations to their menstrual cycles. According to the participants' assessments, these alterations were classified as vaginal bleeding that differed from the subjects' pre-treatment menstrual cycles regarding timing, volume, or appearance. Participants using Norgestrel or Opill tablets reported spotting in 47.3 percent of instances and unexpected (breakthrough) bleeding in 48.6 percent of cases. 6.1 percent of individuals in their first cycle and 28.7 percent of all subjects during the study had amenorrhea (an absence of menstruation).

  • A total of 2173 participants out of 2575 reached their first menstrual cycle. 379 people (17.4 percent) out of the 2,173 participants who completed at least one cycle of therapy did not continue it because of adverse effects; bleeding patterns were responsible for 67.6 percent of all discontinuations. Particularly, 2.7 percent of individuals stopped their therapy due to amenorrhea, while 6.4 percent of participants stopped because of breakthrough bleeding.

Specific Considerations

• Pregnancy - Women should not take Norgestrel tablets since they are contraindicated. This is because a woman who is already pregnant does not require pregnancy prevention. In published research, using oral progestins as a form of contraception for an extended period during pregnancy has not been linked to any negative effects on fetal development. Although studies have not revealed any negative consequences, especially those linked to progestin usage during pregnancy, it is nevertheless suggested to stop using Norgestrel tablets and seek the advice of a healthcare provider for proper prenatal care and assistance.

• Lactating Mothers - Progestin can be transmitted in trace amounts into breast milk, resulting in measurable steroid levels in the plasma of breastfed babies. Norgestrel tablets, which contain only progestin, have not been linked to any negative impacts on baby health or nursing effectiveness. When deciding whether to take these medications, it is critical to balance breastfeeding's positive effects on health and development with the mother's clinical need for Norgestrel tablets and any potential hazards to the breastfed child. This evaluation should consider any potential negative effects of using Norgestrel tablets or the underlying maternal condition.

• Pediatric Population - Norgestrel tablets are safe and effective in women of reproductive age, including teenagers as young as 15, and over 30 percent of participants in clinical studies under 20. It is not advised to use this product before menarche.

• Geriatric Population - Norgestrel tablets have not been examined in postmenopausal women and are not recommended for this group.

• Fertility Following Discontinuation - Following the cessation of oral contraceptives that contain solely progestin (Norgestrel tablets), the limited available information does not show a substantial delay in the recovery of normal ovulation and fertility.