Leuprolide and norethindrone (Intramuscular, Oral)

Leuprolide injection and norethindrone tablets are used together to treat pain from endometriosis. This combination also helps prevent the symptoms of endometriosis from coming back. You should not use this medicine for more than 12 months.

Leuprolide injection is a synthetic (man-made) hormone that works like a natural hormone produced in the brain. It lowers the amount of estrogen in the body, which helps treat endometriosis. Norethindrone is a synthetic (man-made) progestin hormone that is used to treat bone thinning caused by leuprolide.

This medicine is available only with a prescription from your doctor.

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly.

You should not receive this medicine if you are pregnant or may become pregnant. Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control (e.g., diaphragm with spermicide, condoms with spermicide, IUD) to prevent pregnancy. If you think you have become pregnant while using this medicine, tell your doctor right away.

This medicine may cause serious allergic reactions, including anaphylaxis, which can be life-threatening and require immediate medical attention. Call your doctor right away if you have a rash, itching, hoarseness, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth while you are using this medicine.

This medicine can cause your bone mineral density to decrease, which may lead to osteoporosis or weakened bones. Talk with your doctor about how this risk will affect you.

Using this medicine may increase your risk of having seizures. Check with your doctor right away if you start to have muscle spasms or jerking of the arms or legs, sudden loss of consciousness, or loss of bladder control.

This medicine may cause depression. Check with your doctor right away if you have feelings of discouragement, sadness or emptiness, irritability, lack of appetite, loss of interest or pleasure, tiredness, trouble concentrating, or trouble sleeping.

Call your doctor right away if you have sudden loss of vision, double vision, bulging eyes, or a migraine headache.

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 or vitamin supplements.

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

Allergies

Inform your physician if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also inform 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 have not been performed on the relationship of age to the effects of Lupaneta Pack® in the pediatric population. Safety and efficacy have not been established.

Geriatric

Lupaneta Pack® is not indicated in postmenopausal women and has not been studied in women 65 years of age and older.

Breast Feeding

Studies in women breastfeeding have demonstrated harmful infant effects. An alternative to this drug should be prescribed or you should discontinue breastfeeding while using this medicine.

Interactions with Medications

Although certain drugs should not be used together at all, in other cases two different drugs 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 receiving this medication, 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 this drug with any of the following drugs is not advised. Your physician may decide not to treat you with this medication or change some of the other drugs you take.

• Bepridil
• Cisapride
• Dronedarone
• Levoketoconazole
• Mesoridazine
• Pimozide
• Piperaquine
• Saquinavir
• Sparfloxacin
• Terfenadine
• Thioridazine
• Tranexamic Acid
• Ziprasidone

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

• Adagrasib
• Alfuzosin
• Amiodarone
• Amisulpride
• Amitriptyline
• Amobarbital
• Amoxicillin
• Ampicillin
• Amprenavir
• Anagrelide
• Apalutamide
• Apomorphine
• Aprepitant
• Aripiprazole
• Aripiprazole Lauroxil
• Armodafinil
• Arsenic Trioxide
• Artemether
• Asenapine
• Astemizole
• Atazanavir
• Azithromycin
• Bacampicillin
• Bedaquiline
• Belzutifan
• Betamethasone
• Bexarotene
• Boceprevir
• Bosentan
• Buprenorphine
• Buserelin
• Butabarbital
• Butalbital
• Carbamazepine
• Carbenicillin
• Cefaclor
• Cefadroxil
• Cefdinir
• Cefditoren
• Cefixime
• Cefpodoxime
• Cefprozil
• Ceftazidime
• Ceftibuten
• Cefuroxime
• Cenobamate
• Ceritinib
• Chloroquine
• Chlorpromazine
• Ciprofloxacin
• Citalopram
• Clarithromycin
• Clobazam
• Clofazimine
• Clomipramine
• Clothiapine
• Cloxacillin
• Clozapine
• Colesevelam
• Crizotinib
• Cyclacillin
• Cyclobenzaprine
• Cyclosporine
• Dabrafenib
• Darunavir
• Dasatinib
• Degarelix
• Delamanid
• Desipramine
• Deslorelin
• Deutetrabenazine
• Dexamethasone
• Dexmedetomidine
• Dicloxacillin
• Dipyrone
• Disopyramide
• Dofetilide
• Dolasetron
• Domperidone
• Donepezil
• Doxepin
• Doxycycline
• Droperidol
• Ebastine
• Efavirenz
• Elagolix
• Elvitegravir
• Encorafenib
• Entrectinib
• Enzalutamide
• Eribulin
• Erythromycin
• Escitalopram
• Eslicarbazepine Acetate
• Etrasimod
• Etravirine
• Famotidine
• Felbamate
• Fexinidazole
• Fingolimod
• Flecainide
• Fluconazole
• Fluoxetine
• Formoterol
• Fosamprenavir
• Fosaprepitant
• Foscarnet
• Fosphenytoin
• Fostemsavir
• Galantamine
• Gatifloxacin
• Gemifloxacin
• Gepirone
• Glasdegib
• Gonadorelin
• Goserelin
• Granisetron
• Grazoprevir
• Griseofulvin
• Guar Gum
• Halofantrine
• Haloperidol
• Histrelin
• Hydroquinidine
• Hydroxychloroquine
• Hydroxyzine
• Ibutilide
• Iloperidone
• Imipramine
• Indinavir
• Inotuzumab Ozogamicin
• Isotretinoin
• Itraconazole
• Ivabradine
• Ivosidenib
• Ketoconazole
• Lapatinib
• Lefamulin
• Lenvatinib
• Lesinurad
• Levofloxacin
• Lixisenatide
• Lofexidine
• Lopinavir
• Lorlatinib
• Lumacaftor
• Lumefantrine
• Macimorelin
• Mavacamten
• Mefloquine
• Mephobarbital
• Meropenem
• Methadone
• Methohexital
• Methotrimeprazine
• Metronidazole
• Mifepristone
• Minocycline
• Mirtazapine
• Mitapivat
• Mitotane
• Mizolastine
• Mobocertinib
• Modafinil
• Moricizine
• Moxifloxacin
• Mycophenolate Mofetil
• Mycophenolic Acid
• Nafarelin
• Nafcillin
• Nelfinavir
• Nevirapine
• Nilotinib
• Norfloxacin
• Octreotide
• Ofloxacin
• Olanzapine
• Ondansetron
• Osilodrostat
• Osimertinib
• Oxacillin
• Oxaliplatin
• Oxcarbazepine
• Oxytetracycline
• Ozanimod
• Pacritinib
• Paliperidone
• Panobinostat
• Papaverine
• Paroxetine
• Pasireotide
• Pazopanib
• Penicillin G
• Penicillin G Procaine
• Penicillin V
• Pentamidine
• Pentobarbital
• Perphenazine
• Phenobarbital
• Phenylbutazone
• Phenytoin
• Pimavanserin
• Pipamperone
• Pitolisant
• Ponesimod
• Posaconazole
• Prednisolone
• Prednisone
• Primidone
• Probucol
• Procainamide
• Prochlorperazine
• Promethazine
• Propafenone
• Protriptyline
• Quetiapine
• Quinidine
• Quinine
• Quizartinib
• Ranolazine
• Red Clover
• Relugolix
• Ribociclib
• Rifabutin
• Rifampin
• Rifapentine
• Rilpivirine
• Risperidone
• Ritonavir
• Rufinamide
• Saquinavir
• Secobarbital
• Selpercatinib
• Sertindole
• Sertraline
• Sevoflurane
• Simeprevir
• Siponimod
• Sodium Phosphate
• Sodium Phosphate, Dibasic
• Sodium Phosphate, Monobasic
• Solifenacin
• Sorafenib
• Sotalol
• St John's Wort
• Sugammadex
• Sulpiride
• Sultamicillin
• Sultopride
• Sunitinib
• Tacrolimus
• Tamoxifen
• Tazemetostat
• Telaprevir
• Telavancin
• Telithromycin
• Telotristat Ethyl
• Tetrabenazine
• Tetracycline
• Theophylline
• Thiopental
• Thioridazine
• Ticarcillin
• Tigecycline
• Tipranavir
• Tirzepatide
• Tizanidine
• Tolterodine
• Topiramate
• Toremifene
• Trazodone
• Triclabendazole
• Trimipramine
• Triptorelin
• Troglitazone
• Ulipristal
• Vandetanib
• Vardenafil
• Vemurafenib
• Venlafaxine
• Vilanterol
• Vinflunine
• Voclosporin
• Voriconazole
• Vorinostat
• Voxilaprevir
• Zotepine
• Zuclopenthixol

Using this medication with any of the following medications may cause an increased chance of certain adverse effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your clinician may change the dose or how often you use one or both of the medicines.

• Amitriptyline
• Atazanavir
• Atorvastatin
• Clomipramine
• Diazepam
• Doxepin
• Imipramine
• Lamotrigine
• Licorice
• Lorazepam
• Parecoxib
• Selegiline
• Temazepam
• Triazolam
• Troleandomycin
• Valdecoxib
• 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 this medicine with any of the following may cause an increased chance 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 this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Caffeine

Other Medical Problems

The presence of other medical issues may affect the use of this medicine. Make sure you inform your clinician if you have any other medical issues, especially:

• Abnormal uterine bleeding, not diagnosed or
• Blood clotting disorders, or history of or
• Breast cancer or other hormone-sensitive cancer, known, suspected, or history of or
• Heart attack, recent or
• Liver disease or tumors or
• Stroke—Should not be used in patients with these conditions.

• Alcohol abuse or
• Blood clotting issues, family history of or
• Cigarette smoking or
• Diabetes or
• Hypercholesterolemia (high cholesterol in the blood) or
• Hypertension (high blood pressure) or
• Obesity—Use with caution. May cause adverse effects to become worse.

• Asthma, history of or
• Depression, history of or
• Epilepsy (seizures) or
• Fluid retention (body swelling) or
• Heart or blood vessel disease or
• Kidney disease or
• Migraine headache or
• Papilledema (swelling of the optic disc of the eyes) or
• Osteoporosis (thinning of the bones) or
• Retinal vascular lesions (eye issue)—Use with caution. May make these conditions worse.

Along with its necessary effects, a medicine may cause some unwanted effects. Not all of these side effects may occur, but if they do, they may need medical attention.

Check with your doctor or nurse right away if any of the following side effects happen:

More common

• Crying
• depersonalization
• dysphoria
• euphoria
• feeling of warmth
• mental depression
• paranoia
• quick to react or overreact emotionally
• rapidly changing moods
• redness of the face, neck, arms, and sometimes, upper chest
• sudden sweating
• swelling

Incidence not known

• Anxiety
• bladder pain
• bloody or cloudy urine
• blurred vision
• chest pain or tightness
• confusion
• cough
• dark urine
• difficulty, burning, or painful urination
• difficulty speaking
• difficulty swallowing
• dizziness or lightheadedness
• double vision
• fainting
• fast heartbeat
• flu-like symptoms
• frequent urge to urinate
• headache
• hives or welts
• inability to move the arms, legs, or facial muscles
• increased sensitivity of the skin to sunlight
• itching
• joint or muscle pain or stiffness
• lower back or side pain
• nausea and vomiting
• numbness or tingling in the face, arms, or legs
• pain in the groin or genitals
• pain, redness, or swelling in the arm or leg
• pounding in the ears
• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
• redness of the skin
• seizures
• severe sunburn
• sharp back pain just below the ribs
• skin rash
• slow or fast heartbeat
• slow speech
• stomach tenderness
• sudden shortness of breath or trouble breathing
• sweating
• thoughts or attempts at killing oneself
• trouble breathing
• trouble sleeping
• trouble thinking or walking
• unusual tiredness or weakness
• yellow eyes or skin

Some side effects may happen that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or lessen some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome, or if you have any questions about them:

More common

• Acid or sour stomach
• being forgetful
• belching
• bleeding, blistering, burning, coldness, discoloration of the skin, feeling of pressure, hives, infection, inflammation, itching, lumps, numbness, pain, rash, redness, scarring, soreness, stinging, swelling, tenderness, tingling, ulceration, or warmth at the injection site
• blemishes on the skin
• bloated or full feeling
• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
• changes in appetite
• decreased interest in sexual intercourse
• diarrhea
• difficulty having a bowel movement (stool)
• excess air or gas in the stomach or intestines
• feeling of constant movement of self or surroundings
• hair loss or thinning of the hair
• headache, severe and throbbing
• heartburn
• inability to have or keep an erection
• indigestion
• lack or loss of strength
• loss in sexual ability, desire, drive, or performance
• pain or tenderness from the breasts
• passing gas
• pimples
• sensation of spinning
• stomach discomfort, upset, or pain
• weight gain

Less common

• Absent missed or irregular menstrual periods
• itching of the vagina or genital area
• pain during sexual intercourse
• stopping of menstrual bleeding
• thick, white vaginal discharge with no odor or with a mild odor

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

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

In the U.S.

• Lupaneta Pack

Available Dosage Forms:

• Powder for Suspension, 1 Month
• Tablet
• Powder for Suspension, 3 Month

Lupaneta Pack® is a kit that contains two medicines: leuprolide injection and norethindrone tablets.

Leuprolide injection is given as a shot into a muscle by a nurse or other trained health professional in a hospital or clinic. It is a long acting form (depot) that may be given once every month or once every 3 months for up to 6 months of treatment.

Norethindrone tablets are to be taken by mouth every day for up to 6 months after you receive your leuprolide injection.

This medicine usually comes with a patient information leaflet. Read the information carefully and make sure you understand them before receiving this medicine. If you have any questions, ask your doctor.

Dosing

The dose of this medicine 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 this medicine. 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 oral dosage form (tablets):For pain due to endometriosis: Adults—5 mg once a day, for up to 6 months. Children—Use is not recommended.

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

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.