Orilissa

Orilissa is a prescription medication used to treat moderate to severe pain caused by endometriosis. Endometriosis is a painful disorder in which tissue similar to that which forms the lining of your uterus grows outside of your uterine cavity. These growths are sometimes called lesions.

During your menstrual cycle, when estrogen levels rise, these lesions can grow. And later, during your period, the lesions can break down and shed. This can cause pain throughout the month. 

Orilissa belongs to a group of drugs called gonadotropin releasing hormone (GnRH) receptor antagonists. By blocking GnRH receptors, Orilissa decreases signals to your ovaries to produce estrogen. This leads to reduced estrogen levels.

This medication comes in tablet form and is usually taken once or twice a day, with or without food.

Common side effects of Orilissa include hot flashes, night sweats, and nausea.

Orilissa is a prescription medication used to treat moderate or severe pain caused by endometriosis, a condition causing growth of the tissue lining the womb in other places in the body.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with Orilissa. See the “Orilissa Precautions” section.

Common side effects of Orilissa include the following:

• hot flashes or night sweats
• headache
• nausea
• joint pain
• difficulty sleeping
• absence of periods
• anxiety
• mood changes
• depression

This is not a complete list of Orilissa side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effects that bother you or that do not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• medications that use the p-glycoprotein transporter such as digoxin (Lanoxin), loperamide (Imodium), quinidine (Cardioquine, Quinact, Duraquin), vinblastine (Velban), fexofenadine (Allegra), indinavir (Crixivan), colchicine (Colcrys), topotecan (Hycamtin), and paclitaxel (Abraxane, Onxol, Taxol)
• medications that use the enzyme CYP3A4 such as budesonide (Entocort), cyclosporine (Neoral, Gengraf, Sandimmune), darifenacin (Enablex), dihydroergotamine (Migranal), fentanyl (Abstral, Fentora, Onsolis, Actiq), pimozide (Orap), quinidine (Cardioquin, Duraquin, Quinact), sirolimus (Rapamune), tacrolimus (Prograf), terfenadine (Seldane), fluticasone (Flovent HFA, Flonase), eletriptan (Relpax), lovastatin (Mevacor), quetiapine (Seroquel), sildenafil (Viagra, Revatio), and simvastatin (Zocor)
• medications that block a protein in the body (CYP3A4) such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), delavirdine (Rescriptor), and nefazodone
• medications that increase the activity of the enzyme CYP3A4 such as carbamazepine (Tegretol, Equetro, Carbatrol), phenobarbital, phenytoin (Dilantin), rifampin (Rifadin), and St John's wort
• medications that inhibit OATP transporters such as atazanavir (Reyataz), clarithromycin (Biaxin), cyclosporine (Neoral), erythromycin, gemfibrozil (Lopid), lopinavir/ritonavir (Kaletra), ritonavir/lopinavir (Kaletra), saquinavir (Invirase), simeprevir (Olysio), telithromycin (Ketek), tipranavir (Aptivus), rifampin, and velpatasvir (Epclusa)

This is not a complete list of Orilissa drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with Orilissa including the following:

• Bone Loss (decreased Bone Mineral Density [BMD]). While you are taking Orilissa, your estrogen levels will be low. This can lead to BMD loss. Your BMD may improve after stopping Orilissa, but may not recover completely. It is unknown if these bone changes could increase your risk for broken bones as you age. Your healthcare provider (HCP) may order a DXA scan to check your BMD.
• Effects on Pregnancy. Do not take Orilissa if you are trying to become or are pregnant, as your risk for early pregnancy loss may increase. If you think you are pregnant, stop taking Orilissa right away and call your HCP. Orilissa may change your menstrual periods (irregular bleeding or spotting, a decrease in menstrual bleeding, or no bleeding at all), making it hard to know if you are pregnant. Watch for other signs of pregnancy, such as breast tenderness, weight gain, and nausea. Orilissa does not prevent pregnancy. You will need to use effective hormone-free birth control (such as condoms or spermicide) while taking Orilissa and for one week after stopping Orilissa. Birth control pills that contain estrogen may make Orilissa less effective. It is unknown how well Orilissa works while on progestin-only birth control.
• Suicidal thoughts, actions, or behavior, and worsening of mood. Call your HCP right away, or call 911 if an emergency, if you have any of these symptoms, especially if they are new, worse, or bother you: thoughts about suicide or dying, try to commit suicide, new or worse depression or anxiety, or other unusual changes in behavior or mood. You or your caregiver should pay attention to any changes, especially sudden changes in your mood, behaviors, thoughts, or feelings.
• Abnormal liver tests. Call your HCP right away if you have any of these signs and symptoms of liver problems: yellowing of the skin or the whites of the eyes (jaundice), dark amber-colored urine, feeling tired, nausea and vomiting, generalized swelling, right upper stomach area pain, or bruising easily.

Do not take Orilissa if you:

• are allergic to Orilissa or to any of its ingredients
• are or may be pregnant
• have osteoporosis
• have severe liver disease
• are taking medicines known as strong OATP1B1 inhibitors such as cyclosporine or gemfibrozil. Ask your healthcare provider if you are not sure if you are taking one of these medicines.

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of Orilissa, there are no specific foods that you must exclude from your diet when receiving this medication.

Before taking Orilissa, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to Orilissa or to any of its ingredients
• have or have had broken bones
• have other conditions or take medicines that may cause bone problems
• have or have had depression, mood problems or suicidal thoughts or behavior
• have liver problems
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed

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

Tell your doctor if you are pregnant or plan to become pregnant.

Do not take Orilissa if you are trying to become or are pregnant, as your risk for early pregnancy loss may increase. If you think you are pregnant, stop taking Orilissa right away and call your HCP. Orilissa may change your menstrual periods (irregular bleeding or spotting, a decrease in menstrual bleeding, or no bleeding at all), making it hard to know if you are pregnant. Watch for other signs of pregnancy, such as breast tenderness, weight gain, and nausea. Orilissa does not prevent pregnancy. You will need to use effective hormone-free birth control (such as condoms or spermicide) while taking Orilissa and for one week after stopping Orilissa. Birth control pills that contain estrogen may make Orilissa less effective. It is unknown how well Orilissa works while on progestin-only birth control.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if Orilissa crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using Orilissa.

• Take Orilissa exactly as your healthcare provider tells you to take it. 
• Your healthcare provider will give you a pregnancy test before you start taking Orilissa or will have you start taking Orilissa within 7 days after you start your period.
  • If your healthcare provider prescribes: Orilissa 150 mg (a pink tablet), take it 1 time each day
  • Orilissa 200 mg (an orange tablet), take it 2 times each day 
• Take Orilissa at about the same time each day with or without food.
• If you miss a dose of Orilissa:
  • 150 mg (1 time each day), take it as soon as you remember as long as it is on the same day. Do not take more than 1 tablet each day.
  • 200 mg (2 times each day), take it as soon as you remember as long as it is on the same day. Do not take more than 2 tablets each day.
  • If you take too much Orilissa, call your healthcare provider or go to the nearest hospital.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• other medical conditions you have
• other medications you are taking
• how you respond to this medication

The recommended dose of Orilissa for the treatment of endometriosis pain is 150 mg once daily or 200 mg twice daily.

If you take too much Orilissa, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If Orilissa is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

• Store Orilissa between 36°F to 86°F (2°C to 30°C).
• Do not keep medicine that is out of date or that you no longer need. Dispose of unused medicines through community take-back disposal programs when available or place Orilissa in an unrecognizable closed container in the household trash. Do NOT flush Orilissa down the toilet. 
• Keep Orilissa and all medicines out of the reach of children.