Norethindrone

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Norethindrone
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Vignesh Ponnusamy, M.B.B.S. [2]

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Overview

Norethindrone is an oral contraceptive that is FDA approved for the {{{indicationType}}} of prevention of pregnancy. Common adverse reactions include nausea, headache, abnormal menstrual cycle, breast tenderness, irregular periods.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Prevention of Pregnancy
  • To achieve maximum contraceptive effectiveness, norethindrone tablets must be taken exactly as directed. One tablet is taken every day, at the same time. Administration is continuous, with no interruption between pill packs.
  • Efficacy
  • If used perfectly, the first-year failure rate for progestin-only oral contraceptives is 0.5%. However, the typical failure rate is estimated to be closer to 5%, due to late or omitted pills. Table 1 lists the pregnancy rates for users of all major methods of contraception.

t1

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Norethindrone in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Norethindrone in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Norethindrone in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Norethindrone in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Norethindrone in pediatric patients.

Contraindications

*Benign or malignant liver tumors

Warnings

  • Norethindrone tablets do not contain estrogen and, therefore, this insert does not discuss the serious health risks that have been associated with the estrogen component of combined oral contraceptives (COCs). The healthcare professional is referred to the prescribing information of combined oral contraceptives for a discussion of those risks. The relationship between progestin-only oral contraceptives and these risks is not fully defined. The healthcare professional should remain alert to the earliest manifestation of symptoms of any serious disease and discontinue oral contraceptive therapy when appropriate.
  • Delayed Follicular Atresia/Ovarian Cysts
  • If follicular development occurs, atresia of the follicle is sometimes delayed and the follicle may continue to grow beyond the size it would attain in a normal cycle. Generally these enlarged follicles disappear spontaneously. Often they are asymptomatic; in some cases they are associated with mild abdominal pain. Rarely they may twist or rupture, requiring surgical intervention.
  • Irregular Genital Bleeding
  • Some epidemiological studies of oral contraceptive users have reported an increased relative risk of developing breast cancer, particularly at a younger age and apparently related to duration of use. These studies have predominantly involved combined oral contraceptives and there is insufficient data to determine whether the use of POPs similarly increases the risk.
  • A meta-analysis of 54 studies found a small increase in the frequency of having breast cancer diagnosed for women who were currently using combined oral contraceptives or had used them within the past ten years.
  • This increase in the frequency of breast cancer diagnosis, within ten years of stopping use, was generally accounted for by cancers localized to the breast. There was no increase in the frequency of having breast cancer diagnosed ten or more years after cessation of use.
  • Women with breast cancer should not use oral contraceptives because the role of female hormones in breast cancer has not been fully determined.
  • Some studies suggest that oral contraceptive use has been associated with an increase in the risk of cervical intraepithelial neoplasia in some populations of women. However, there continues to be controversy about the extent to which such findings may be due to differences in sexual behavior and other factors. There is insufficient data to determine whether the use of POPs increases the risk of developing cervical intraepithelial neoplasia.

Precautions

  • General
  • Physical Examination and Follow-up
  • It is considered good medical practice for sexually active women using oral contraceptives to have annual history and physical examinations. The physical examination may be deferred until after initiation of oral contraceptives if requested by the woman and judged appropriate by the healthcare professional.
  • Carbohydrate and Lipid Metabolism
  • Some users may experience slight deterioration in glucose tolerance, with increases in plasma insulin but women with diabetes mellitus who use progestin-only oral contraceptives do not generally experience changes in their insulin requirements. Nonetheless, prediabetic and diabetic women in particular should be carefully monitored while taking POPs.
  • Lipid metabolism is occasionally affected in that HDL, HDL2, and apolipoprotein A-I and A-II may be decreased; hepatic lipase may be increased. There is usually no effect on total cholesterol, HDL3, LDL, or VLDL.
  • The onset or exacerbation of migraine or development of severe headache with focal neurological symptoms which is recurrent or persistent requires discontinuation of progestin-only contraceptives and evaluation of the cause.

Adverse Reactions

Clinical Trials Experience

  • Adverse reactions reported with the use of POPs include:
  • The following adverse reactions were also reported in clinical trials or during post-marketing experience:
Body as a Whole

fatigue, edema

Digestive

vomiting, abdominal pain, hepatitis, jaundice cholestatic

Musculoskeletal

pain in extremity

Neurologic

depression, nervousness

Skin and Hypersensitivy Reactions

anaphylactic/anaphylactoid reaction, hypersensitivity, alopecia, rash, rash pruritic.

Urogenital

genital discharge; breast pain, menstruation delayed, suppressed lactation, vaginal hemorrhage, menorrhagia, withdrawal bleed when product is stopped

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Norethindrone in the drug label.

Drug Interactions

  • Concurrent use of bosentan and norethindrone containing products may result in decreased concentrations of these contraceptive hormones thereby increasing the risk of unintended pregnancy and unscheduled bleeding.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category
  • Many studies have found no effects on fetal development associated with long-term use of contraceptive doses of oral progestins. The few studies of infant growth and development that have been conducted have not demonstrated significant adverse effects. It is nonetheless prudent to rule out suspected pregnancy before initiating any hormonal contraceptive use.


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Norethindrone in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Norethindrone during labor and delivery.

Nursing Mothers

  • In general, no adverse effects have been found on breastfeeding performance or on the health, growth, or development of the infant. However, isolated post-marketing cases of decreased milk production have been reported. Small amounts of progestins pass into the breast milk of nursing mothers, resulting in detectable steroid levels in infant plasma.

Pediatric Use

  • Safety and efficacy of norethindronetablets have been established in women of reproductive age. Safety and efficacy are expected to be the same for postpubertal adolescents under the age of 16 and for users 16 years and older. Use of this product before menarche is not indicated.

Geriatic Use

There is no FDA guidance on the use of Norethindrone with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Norethindrone with respect to specific gender populations.

Race

There is no FDA guidance on the use of Norethindrone with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Norethindrone in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Norethindrone in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Norethindrone in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Norethindrone in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral

Monitoring

There is limited information regarding Monitoring of Norethindrone in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Norethindrone in the drug label.

Overdosage

Acute Overdose

  • There have been no reports of serious ill effects from overdosage, including ingestion by children.

Chronic Overdose

There is limited information regarding Chronic Overdose of Norethindrone in the drug label.

Pharmacology

Template:Px
Template:Px
Norethindrone
Systematic (IUPAC) name
(17β)-17-ethynyl-17-hydroxyestr-4-en-3-one;
(8R,9S,10R,13S,14S,17S)-17-ethynyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
Identifiers
CAS number 68-22-4
ATC code G03AC01 G03DC02 (WHO)
PubChem 6230
DrugBank DB00717
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 298.419 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 64%
Protein binding >95%
Metabolism ?
Half life 7 hours
Excretion ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes ?

Mechanism of Action

Structure

  • Norethindrone, USP is a white to creamy white, odorless, crystalline powder. It is stable in air. Practically insoluble in water; soluble in chloroform and in dioxane; sparingly soluble in alcohol; slightly soluble in ether. The chemical name for norethindrone is 17-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one. The structural formula is as follows:
This image is provided by the National Library of Medicine.
  • Each yellow tablet contains 0.35 mg norethindrone, USP and has the following inactive ingredients: anhydrous lactose, corn starch, D&C yellow no. 10 aluminum lake, ethylcellulose aqueous dispersion, lactose monohydrate, magnesium stearate, microcrystalline cellulose and povidone.
  • Meets USP Dissolution Test 2.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Norethindrone in the drug label.

Pharmacokinetics

  • Serum progestin levels peak about two hours after oral administration, followed by rapid distribution and elimination. By 24 hours after drug ingestion, serum levels are near baseline, making efficacy dependent upon rigid adherence to the dosing schedule. There are large variations in serum levels among individual users. Progestin-only administration results in lower steady-state serum progestin levels and a shorter elimination half-life than concomitant administration with estrogens.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Norethindrone in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Norethindrone in the drug label.

How Supplied

  • Errin® (norethindrone tablets, USP 0.35 mg) are packaged in cartons of six blister cards each containing 28 tablets. Each yellow, round, flat-faced, beveled-edge, unscored tablet is debossed with stylized b on one side and 344 on the other side.
  • Store at 20° to 25°C (68° to 77°F).
  • KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.

Storage

There is limited information regarding Norethindrone Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

{{#ask: Label Page::Norethindrone |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

  • Counseling Issues

1

2

Precautions with Alcohol

  • Alcohol-Norethindrone interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

There is limited information regarding Norethindrone Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ "ERRIN- norethindrone tablet".


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