Norethindrone (Estrostep)

Oral Contraceptive

Oral contraceptives containing norethindrone are available as a prescription oral treatment. It is available as a tablet or capsule however, only the tablet form is prescribed for the treatment of acne. 

  • Available forms:

    • Oral treatment: 

      • Tablet:
        Available as prescription
        Generic available (US)
    • Brand names: 

      • Estrostep Fe®
      • Tilia Fe®
      • Tri-legest Fe®

        (Other brand names are available but are usually not prescribed to treat acne)
  • Available in these doses:

    • Tablets:

      • Estrostep Fe (Triphasic; 3 different doses of Ethinyl estradiol and norethindrone):
        • Day 1-5: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [5 white triangular tablets]
        • Day 6-12: Ethinyl estradiol 0.03 mg and norethindrone acetate 1 mg [7 white square tablets]
        • Day 13-21: Ethinyl estradiol 0.035 mg and norethindrone acetate 1 mg [9 white round tablets]
        • Day 22-28: Ferrous fumarate 75 mg [7 brown tablets]
      • Tilia Fe (Triphasic; 3 different doses of Ethinyl estradiol and norethindrone):
        • Day 1-5: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [5 white triangular tablets]
        • Day 6-12: Ethinyl estradiol 0.03 mg and norethindrone acetate 1 mg [7 white square tablets]
        • Day 13-21: Ethinyl estradiol 0.035 mg and norethindrone acetate 1 mg [9 white round tablets]
        • Day 22-28: Ferrous fumarate 75 mg [7 brown tablets]
      • Tri-Legest Fe (Triphasic; 3 different doses of Ethinyl estradiol and norethindrone):
        • Day 1-5: Ethinyl estradiol 0.02 mg and norethindrone acetate 1 mg [5 light pink tablets]
        • Day 6-12: Ethinyl estradiol 0.03 mg and norethindrone acetate 1 mg [7 light yellow tablets]
        • Day 13-21: Ethinyl estradiol 0.035 mg and norethindrone acetate 1 mg [9 light blue tablets]
        • Day 22-28: Ferrous fumarate 75 mg [7 brown tablets]

Dosing information:

Oral contraceptives containing norethindrone come in packets of 28 tablets. A tablet needs to be take once day according to the corresponding days indicated on the packet. 

  • Who is it for?

    • Gender:
      • Females
    • Severity of acne:
      • Moderate-to-severe
    • Age:
      • Females of 15 years and older 
    • Other:
      • Females must have had their first menstrual period before they can be started on norethindrone. Oral contraceptives containing norethindrone must only be prescribed when contraception is also desired.
      • Females must also have a form of acne that is unresponsive to topical treatment, have no contraindications for oral contraceptives, and plan to use the oral contraceptive for a minimum of 6 months. 

How to use it:

Oral contraceptives containing norethindrone is an oral treatment and is available in tablet form. 

During the first few months, you may feel sick or nauseous because of the treatment. Consult your physician, if these symptoms do not disappear with continued treatment. Take the oral contraceptive with food or milk to avoid nausea. An oral contraceptive needs to be taken at the same time every day, with meals or at bedtime, to make sure that the oral contraceptive works best. Do not miss or skip a dose because you could get pregnant. If you do miss a dose, be sure to use another form of contraception for 7 to 9 days to ensure that you do not become pregnant. 

Do not eat grapefruit or drink grapefruit juice when you are taking your tablet because it may alter the absorption and effectiveness of the medication.  

Oral contraceptives containing norethindrone are available in many different brands however, usually only Estrostep Fe®, Tilia Fe®, and Tri-legest Fe® are prescribed to treat acne. Be sure you know which brand you use and exactly how to use it. Do not switch between brands without consulting your physician first.

Follow the instructions on your prescription carefully and use the oral contraceptive exactly as prescribed by your physician. Do not change the dose or the frequency of your medication. If you have any questions about the medication or the prescription, ask your physician or pharmacist. 

Tablets in 28-tablet packet (Estrostep Fe®, Tilia Fe®, and Tri-legest Fe®)

Take 1 tablet once a day for 28 days in the order following the packet. Start a new packet the day after you have finished the previous packet and continue following the order. The tablets may come in different colors or shapes corresponding to different amounts of estrogen and progestin hormones in the tablet.

Follow the instructions of your physician on when to start your oral contraceptive, carefully. This is usually on the first or the fifth day of the menstrual period. Your physician may ask you to use an additional method of birth control during the first 7 to 9 days of taking the oral contraceptive to prevent pregnancy.

During the last week of the packet, you will have a withdrawal bleeding that looks like a menstrual period because these tablets do not contain any hormones. You have to start the new packet as scheduled even if you are still bleeding. 

Be aware of: 

  • Warning: The risk of serious side effects, such as heart attacks, strokes and blood clots, increases significantly when smoking cigarettes while using oral contraceptives. This is especially the case in women over 35 years old and heavy smokers (15 cigarettes or more per day). Do not use this medication if you smoke cigarettes or are over 35 years old. 
  • Before using oral contraceptives, let your physician or pharmacist know if you are allergic to estrogen, progestin, or any of the other ingredients in the tablets. 
  • Tell your physician that you are taking oral contraceptives before any medical tests. Oral contraceptives may affect the results of some medical tests.
  • Before using oral contraceptives, inform your physician about the prescription and non-prescription medications, vitamins, nutritional supplements, and herbal products, especially St. John’s wort, you are using/taking. You will find a complete list of drug interactions below.
  • Before using oral contraceptives, inform your physician if you currently suffer from or have ever suffered from blood clots in your legs, lungs, or eyes, coronary artery disease or a heart attack (clogged blood vessels around the heart), thrombophilia (a condition with high risk of blood clots), cerebrovascular disease or stroke (clogged blood vessels in and to the brain). Inform you physician if you have had surgery recently or were immobile for a while. Oral contraceptives may be contraindicated in this case. 
  • Before using oral contraceptives, inform your physician if you currently suffer from or have ever suffered from an irregular heartbeat, heart disease, or chest pain, diabetes causing problems with blood circulation, headaches accompanied by other symptoms such as changes in vision, weakness or dizziness, migraine, seizures, high blood pressure or toxemia (high blood pressure during pregnancy). Oral contraceptives may be contraindicated in this case. 
  • Before using oral contraceptives, inform your physician if you currently suffer from or have ever suffered from breast cancer, endometrial cancer (cancer of the uterus wall), cancer of the cervix (the lower end of the uterus) or the vagina, liver cancer, liver tumors, or other liver problems, jaundice (yellow coloring) of the eyes or skin during pregnancy or while using hormonal contraceptives (such as birth control pills, patches, rings, implants, or injections), unexplained vaginal bleeding, adrenal insufficiency (adrenal glands do not produce enough certain hormones), or kidney disease. Certain or any oral contraceptive may be contraindicated in this case. 
  • Before using oral contraceptives, inform your physician if you currently suffer from or have ever suffered from overweight, breast problems, such as lumps, fibrocystic breasts (non-cancer swollen breasts or breast lumps), or an abnormal mammogram, hypercholesterolemia (high blood cholesterol), diabetes, asthma, depression, gallbladder disease, or excessive weight gain or fluid retention during the menstrual cycle. 
  • Before using oral contraceptives, inform your physician if anyone in your family suffers from or has ever suffered from breast cancer.
  • Oral contraceptives may increase the risk of blood clots so contact your physician immediately when you experience a pain in the chest, groin, or legs, especially the calves or when you have difficulty breathing, slurred speech, sudden loss of coordination, vision changes, a sudden, severe headache, or unexplained shortness of breath. 
  • Oral contraceptives may increase the risk of certain cancers such as breast cancer, or cancer of the uterus, ovaries or cervix. Consult your physician when you experience abnormal vaginal bleeding. 
  • Consult your physician if you wear contact lenses, or if you experience a change in vision, including blurred vision, or difficulty reading. 
  • Consult your physician immediately when you have signs of a serious liver disease including stomach pain, dark urine or pale stools, yellow eyes or skin. 
  • Consult your physician immediately when you have signs of a gallbladder disease including stomach pain, nausea, and vomiting.  
  • Do not use oral contraceptives when you are pregnant, want to become pregnant, or are breastfeeding. Call your physician immediately if you become pregnant while using oral contraceptives. You may be pregnant if you miss your menstrual period. If you have taken the oral contraceptive as directed, you may continue taking the tablets as prescribed even if you miss one period. However, if you have miss two periods in a row or miss one period when you have not taken the tablets as prescribed, contact your physician. 
  • You should wait 4 weeks after giving birth before taking oral contraceptives. If you have had a miscarriage or an abortion, consult your physician about when to start oral contraceptives. 
  • Vaginal bleeding in between menstrual periods, called spotting, may occur during the first 3 months of treatment. Continue your normal schedule but contact your physician if the bleeding continues for more than 1 week or when it continues to occur after 3 months of treatment. 
  • Oral contraceptives should be taken regularly as prescribed in order to be effective. Continue using your oral contraceptive even if you are bleeding, spotting, or have an upset stomach. Consult your physician if you have questions or want to stop  using oral contraceptives.
  • Oral contraceptives may become less effective in case of vomiting or diarrhea so make sure you have a second, backup method of birth control in this case. Ask your physician how long you should use the backup method for. 
  • If you are about to undergo surgery (which includes dental surgery), inform your physician or dentist that you use oral contraceptives, prior to the procedure.
  • Oral contraceptives may cause dark spots on the skin, especially on the face. Avoid exposure to real or artificial sunlight and wear protective clothing, sunglasses, and sunscreen if you have seen dark spots appearing during pregnancy or while taking oral contraceptives in the past.
  • Inform you physician that you are wearing contact lenses and see an eye doctor if your ability to wear lenses or you vision changes while using oral contraceptives. 
  • If oral contraceptives was prescribed for acne, you can continue your regular diet, however, avoid grapefruit / grapefruit juice and caffeine when taking the oral contraceptive. 
  • Do not share your medication with anyone else. 
  • Keep your regular appointments with your physician to track your response to oral contraceptives. A complete physical examination is needed every year which includes checking your blood pressure, a breast and pelvic exam, and a Pap test (test for cervical cancer). Talk to your physician about self-examination of your breasts and report any lumps you may have noticed in your breast immediately. 

Drug interactions: 

Some drugs interact with oral contraceptives and should not be used together. However, your physician may prescribe other drugs together with oral contraceptives which may cause a slight interaction, and in this case precautions are necessary.

Inform your physician or pharmacist about all the prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan on taking before starting oral contraceptives. Also inform your physician or pharmacist of the skin products you use including soaps, cleansers, moisturizers, and cosmetics. 

Drugs that should not be used with oral contraceptives at all are:

  • Dasabuvir
  • Ombitasvir
  • Paritaprevir
  • Ritonavir
  • Tranexamic Acid
Full list of drug interactions (From PubMed and Medline Plus)
  • Alprazolam
  • Ampicillin
  • Amprenavir
  • Anagrelide
  • Aprepitant
  • Atazanavir
  • Atorvastatine
  • Bacampicillin
  • Betamethasone
  • Bexarotene
  • Boceprevir
  • Bosentan
  • Bupropion
  • Carbamazepine
  • Ceritinib
  • Cimetidine
  • Clarithromycin
  • Clofibrate
  • Colesevelam
  • Cyclosporine
  • Dabrafenib
  • Danazol
  • Darunavir
  • Delavirdine
  • Dexamethasone
  • Diltiazem
  • Donepezil
  • Efavirenz
  • Eliglustat
  • Enzalutamide
  • Erythromycin
  • Eslicarbazepine Acetate
  • Etorocoxib
  • Fluconazole
  • Fluoxetine
  • Fosamprenavir
  • Fosaprepitant
  • Fosphenytoin
  • Ginseng
  • Glecaprevir
  • Griseofulvin
  • Idelalisib
  • Indinavir
  • Isoniazid
  • Isotretinoin
  • Itraconazole
  • Ketoconazole
  • Lamotrigine
  • Lesinurad
  • Levothyroxine
  • Licorice
  • Lixisenatide
  • Lumacaftor
  • Metronidazole
  • Methylprednisolone
  • Minocycline
  • Mitotane
  • Modafinil
  • Morphine
  • Mycophenolate Mofetil
  • Mycophenolic Acid
  • Nefazodone
  • Nelfinavir
  • Oxcarbazepine
  • Paclitaxel
  • Paclitaxel Protein-Bound
  • Parecoxib
  • Phenytoin
  • Phenobarbital
  • Pibrentasvir
  • Piperaquine
  • Pitolisant
  • Prednisolone
  • Prednisone
  • Primidone
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Roflumilast
  • Rosuvastatin
  • Rufinamide
  • Selegiline
  • St John’s Wort
  • Sugammadex
  • Telaprevir
  • Temazepam
  • Tetracyclin
  • Theophylline
  • Tipranavir
  • Tizanidine
  • Topiramate
  • Troglitazone
  • Troleandomycin
  • Ulipristal
  • Valdecoxib
  • Valproic Acid
  • Verapamil
  • Vitamin C
  • Voriconazole
  • Warfarin
  • Zafirlukast

What if I overdose? 

In case of overdose, contact an emergency facility or call the American Association of Poison Control Centers at 1 (800) 222-1222 (available 24/7).

If immediate assistance is necessary because the victim has collapsed, had a seizure, has trouble breathing, or cannot be awakened, call 911 at once.

Information can also be found online at https://www.poisonhelp.org/help

Symptoms of overdose:

  • Nausea
  • Vaginal bleeding

What if I miss a dose?

Oral contraceptives have specific instructions on what to do when you miss a dose because you may not be protected from getting pregnant. Consult your physician when you miss a dose because you may need a backup method of birth control for 7 to 9 days or until the end of the cycle.

Do not increase the quantity or frequency of dosing to make up for the missed dose but continue taking the tablets as scheduled and use backup birth control until you receive further advice from your physician.

Storage:

Store your medication in the container that the pharmacist provided and keep it out of reach and out of sight of children. Many containers can be opened by children. Keep the container tightly closed. Always lock safety caps and immediately place the medication in a safe location that is up and away from the sight of young children, to prevent poisoning (www.upandaway.org).

Store the medication at room temperature. Keep the medication away from excessive heat and moisture – do not store in the bathroom. Do not freeze oral contraceptives.

Disposal:

Do not keep outdated medication and medication that you no longer use. Unneeded medications should be disposed of in a way that pets, children, and other people cannot consume them. Do not flush the medication down the toilet. Contact your pharmacist to learn about the availability of a medicine take-back program in your neighborhood, or get in touch with your local garbage/recycling department to ensure safe disposal. If you do not have access to a take-back program, you can find more information on safe disposal of medication on the FDA website: (https://www.fda.gov/Drugs/ResourcesForYou/Consumers/BuyingUsingMedicineSafely/EnsuringSafeUseofMedicine/SafeDisposalofMedicines/ucm186187.htm)

References
  1. Medlineplus.gov. (2018). Estrogen and Progestin (Oral contraceptives): MedlinePlus Drug Information. [online] Available at: https://medlineplus.gov/druginfo/meds/a601050.html.  [Accessed 4 June. 2018]
  2. PubmedHealth. (2018). Ethinyl Estradiol and Norethindrone (Oral route). [online] Avaliable at: https://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0060082/. [Accessed 4 June. 2018]
  3. Toxnet.nlm.nih.gov. (2018). Oral contraceptives (combined). [online] Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/search2/f?./temp/~1inLKx:4. [Accessed 4 June. 2018].
  4. Uptodate.com. (2018). Ethinyl estradiol and Norethindrone. [online] Available at: https://www.uptodate.com/contents/ethinyl-estradiol-and-norethindrone-drug-information?search=norethindrone%20ethinyl%20estradiol&source=search_result&selectedTitle=1~19&usage_type=default&display_rank=1. [Accessed 4 June. 2018].
  5. Epocrates.com. (2018). Norethindrone/ ethinyl estradiol. [online] Available at: https://online.epocrates.com/drugs/2453/norethindrone-acetate-ethinyl-estradiol. [Accessed 4 June. 2018].