Levonorgestrel

Kyleena is indicated to prevent pregnancy for up to 5 years. Replace the system after 5 years if continued use is desired.

Included as part of the PRECAUTIONS section.

Levonorgestrel can cause serious side effects including: 

• Pelvic inflammatory disease (PID). Some intrauterine device (IUD) users get a serious pelvic infection called pelvic inflammatory disease. PID is usually sexually transmitted. You have a higher chance of getting PID if you or your partner have sex with other partners. PID can cause serious problems such as infertility, ectopic pregnancy or pelvic pain that does not go away. PID is usually treated with antibiotics. More serious cases of PID may require surgery. A hysterectomy (removal of the uterus) is sometimes needed. In rare cases, infections that start as PID can even cause death.
  • Tell your healthcare provider right away if you have any of these signs of PID: long-lasting or heavy bleeding, unusual vaginal discharge, low abdominal (stomach area) pain, painful sex, chills, or fever.
• Life-threatening infection. Life-threatening infection can occur within the first few days after the IUD is placed. Call your healthcare provider if you develop severe pain within a few hours after the IUD is placed.
• Embedment. IUD may become attached to the uterine wall. This is called embedment. If embedment happens, this medication may no longer prevent pregnancy and you may need surgery to have it removed.
• Perforation. The IUD may go through the uterus. This is called perforation. If your uterus is perforated, this medication may no longer prevent pregnancy. It may move outside the uterus and can cause internal scarring, infection, or damage to other organs, and you may need surgery to have the IUD removed.

Common side effects of levonorgestrel include:

• Pain, bleeding or dizziness during and after placement. If these symptoms do not stop 30 minutes after placement, the IUD may not have been placed correctly. Your healthcare provider will examine you to see if the IUD needs to be removed or replaced.
• Expulsion. The IUD may come out by itself. This is called expulsion. You may become pregnant if the IUD comes out. If you notice the IUD has come out, use a backup birth control method like condoms and call your healthcare provider.
• Missed menstrual periods. About 2 out of 10 women stop having periods after 1 year of levonorgestrel use. If you do not have a period for 6 weeks during levonorgestrel use, call your healthcare provider. When the IUD is removed, your menstrual periods will come back.
• Changes in bleeding. You may have bleeding and spotting between menstrual periods, especially during the first 3 to 6 months. Sometimes the bleeding is heavier than usual at first. However, the bleeding usually becomes lighter than usual and may be irregular. Call your healthcare provider if the bleeding remains heavier than usual or if the bleeding becomes heavy after it has been light for a while.
• Cyst on the ovary. About 12 out of 100 women using this hormone-releasing system develop a cyst on the ovary. These cysts usually disappear on their own in a month or two. However, cysts can cause pain and sometimes cysts will need surgery.

• Levonorgestrel does not protect against HIV infection (AIDS) and other sexually transmitted diseases (STDs).
• Cigarette smoking increases the risk of serious cardiovascular (CV) events. Risk increases with age (>35 yrs) and with the number of cigarettes smoked.
• Should not be used by women who are >35 yrs of age and smoke.

Do not use this medication if you:

• might be pregnant
• have had a serious pelvic infection called pelvic inflammatory disease (PID) unless you have had a normal pregnancy after the infection went away
• have an untreated pelvic infection now
• have had a serious pelvic infection in the past 3 months after a pregnancy
• can get infections easily. For example, if you have:
  • more than one sexual partner or your partner has more than one partner
  • problems with your immune system
  • intravenous drug abuse
• have or suspect you might have cancer of the uterus or cervix
• have bleeding from the vagina that has not been explained
• have liver disease or liver tumor
• have breast cancer now or in the past or suspect you have breast cancer
• have an intrauterine device in your uterus already
• have a condition of the uterus that changes the shape of the uterine cavity, such as large fibroid tumors
• are allergic to levonorgestrel, silicone, or polyethylene

Before taking or using levonorgestrel, tell your doctor if you:

• have had a heart attack
• have had a stroke
• were born with heart disease or have problems with your heart valves
• have problems with blood clotting or take medicine to reduce clotting
• have high blood pressure
• recently had a baby or if you are breastfeeding
• have diabetes (high blood sugar)
• use corticosteroid medications on a long-term basis
• have severe migraine headaches

Tell your doctor about all of the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

• Birth Control Options (Types and Side Effects)
• Contraceptive Measures after Unprotected Sex

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For levonorgestrel, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to levonorgestrel or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of levonorgestrel in teenage females. levonorgestrel may be used for birth control in teenage females but is not recommended before the start of menstruation.

Geriatric

Appropriate studies on the relationship of age to the effects of levonorgestrel have not been performed in the geriatric population. levonorgestrel is not indicated for use in elderly women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking levonorgestrel, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using levonorgestrel with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Tranexamic Acid

Using levonorgestrel with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Aprepitant
• Bosentan
• Carbamazepine
• Ceritinib
• Dabrafenib
• Darunavir
• Dexamethasone
• Efavirenz
• Eliglustat
• Enzalutamide
• Fosphenytoin
• Griseofulvin
• Idelalisib
• Isotretinoin
• Lesinurad
• Lixisenatide
• Lumacaftor
• Mitotane
• Modafinil
• Oxcarbazepine
• Phenytoin
• Pitolisant
• Prednisone
• Rifabutin
• Rifampin
• St John's Wort
• Sugammadex
• Theophylline
• Tizanidine
• Topiramate
• Ulipristal

Using levonorgestrel with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acitretin
• Alprazolam
• Amprenavir
• Atazanavir
• Bacampicillin
• Betamethasone
• Bexarotene
• Colesevelam
• Cyclosporine
• Delavirdine
• Eslicarbazepine Acetate
• Fosamprenavir
• Fosaprepitant
• Lamotrigine
• Licorice
• Mycophenolate Mofetil
• Mycophenolic Acid
• Nelfinavir
• Perampanel
• Prednisolone
• Rifapentine
• Ritonavir
• Rosuvastatin
• Rufinamide
• Selegiline
• Tacrine
• Telaprevir
• Troglitazone
• Troleandomycin
• Voriconazole
• Warfarin

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using levonorgestrel with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use levonorgestrel, or give you special instructions about the use of food, alcohol, or tobacco.

• Caffeine

Use levonorgestrel exactly as directed by your doctor or follow the instructions on the package. levonorgestrel is for occasional use as emergency birth control. It should not replace your regular birth control method. You may use levonorgestrel at any time during your monthly period.

levonorgestrel comes with a patient information leaflet. Read and follow the instructions carefully. Ask your doctor if you have any questions.

Plan B One-Step® is available as an over-the-counter medicine for any woman of childbearing potential.

If you vomit within 2 hours after taking levonorgestrel, call your doctor right away. Your doctor may prescribe another tablet for you.

Dosing

The dose of levonorgestrel will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of levonorgestrel. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For emergency contraception:
  • For oral dosage form (Plan B One-Step® tablets):
    • Adults and teenagers—One tablet taken as soon as possible and not more than 72 hours (3 days) after unprotected sex or after failure of another birth control method.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

It is very important that your doctor check you closely to make sure levonorgestrel is working properly and does not cause unwanted effects.

Although you are using levonorgestrel to prevent pregnancy, you should know that using levonorgestrel while you are pregnant could harm the unborn baby. Your doctor may give you a pregnancy test before you start using levonorgestrel to make sure you are not pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away.

Call your doctor right away if you have severe lower abdominal or stomach pain 3 to 5 weeks after taking levonorgestrel. You may have a pregnancy outside of the uterus (womb), which is called an ectopic pregnancy. An ectopic pregnancy can be a serious and life-threatening condition. It can also cause problems that may make it harder for you to become pregnant in the future.

You may have some blood spotting a few days after taking levonorgestrel. If the bleeding continues for more than 1 week, check with your doctor right away.

levonorgestrel may make your next monthly period later than expected by a few days. If your next period after taking levonorgestrel is more than 1 week late, check with your doctor right away for a pregnancy test.

levonorgestrel will not protect you from getting HIV/AIDS or other sexually transmitted infections. If this is a concern for you, talk with your doctor.

Your regular birth control method such as birth control pills or patch may not work as well while you are using levonorgestrel. After using levonorgestrel, you must use two forms of birth control. Use birth control pills or patch together with another form of birth control, such as a condom, diaphragm, or contraceptive foam or jelly, during any other times that you have sex in the same monthly period you used levonorgestrel.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

Drugs or herbal products that induce enzymes, including CYP3A4, that metabolize progestins may decrease the plasma concentrations of progestins, and may decrease the effectiveness of progestin-only pills. Some drugs or herbal products that may decrease the effectiveness of progestin-only pills include:

• Barbiturates
• bosentan
• carbamazepine
• felbamate
• griseofulvin
• oxcarbazepine
• phenytoin
• rifampin
• St. John’s wort
• topiramate

Significant changes (increase or decrease) in the plasma levels of the progestin have been noted in some cases of co-administration with HIV protease inhibitors or with non-nucleoside reverse transcriptase inhibitors.

Consult the labeling of all concurrently used drugs to obtain further information about interactions with progestin-only pills or the potential for enzyme alterations.

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenicity: There is no evidence of increased risk of cancer with short-term use of progestins. There was no increase in tumorgenicity following administration of Levonorgestrel to rats for 2 years at approximately 5 µg/day, to dogs for 7 years at up to 0.125 mg/kg/day, or to rhesus monkeys for 10 years at up to 250 µg/kg/day. In another 7 year dog study, administration of Levonorgestrel at 0.5 mg/kg/day did increase the number of mammary adenomas in treated dogs compared to controls. There were no malignancies.

Genotoxicity: Levonorgestrel was not found to be mutagenic or genotoxic in the Ames Assay, in vitro mammalian culture assays utilizing mouse lymphoma cells and Chinese hamster ovary cells, and in an in vivo micronucleus assay in mice.

Fertility: There are no irreversible effects on fertility following cessation of exposures to Levonorgestrel or progestins in general.