Overview
Levonorgestrel (LNG) is a synthetic progestogen similar to Progesterone used in contraception and hormone therapy. Also known as Plan B, it is used as a single agent in emergency contraception, and as a hormonal contraceptive released from an intrauterine device, commonly referred to as an IUD. Some of these devices are known as Jaydess, Kyleena, and Mirena. A subdermal implant of levonorgestrel that slowly releases the hormone over a long-term period is also available. In addition to the above uses, levonorgestrel is used as a component of long-term combination contraceptives. Globally, levonorgestrel is the most commonly used emergency contraceptive. It was initially granted FDA approval in 1982 and was the first emergency contraceptive containing only progesterone, showing high levels of efficacy and a lack of estrogenic adverse effects when compared to older emergency contraceptive regimens.
Indication
Emergency contraception Levonorgestrel, in the single-agent emergency contraceptive form, is indicated for the prevention of pregnancy after the confirmed or suspected failure of contraception methods or following unprotected intercourse. It is distributed by prescription for patients under 17, and over the counter for those above this age. This levonorgestrel-only form of contraception is not indicated for regular contraception and must be taken as soon as possible within 72 hours after intercourse. It has shown a lower efficacy when it is used off label within 96 hours. Long-term contraception or nonemergency contraception In addition to the above indication in emergency contraception, levonorgestrel is combined with other contraceptives in contraceptive formulations designed for regular use, for example with ethinyl estradiol. It is used in various hormone-releasing intrauterine devices for long-term contraception ranging for a duration of 3-5 years. Product labeling for Mirena specifically mentions that it is recommended in women who have had at least 1 child and can be indicated for the prevention of pregnancy for up to 8 years. A subdermal implant is also available for the prevention of pregnancy for up to 5 years. Hormone therapy and off-label uses Levonorgestrel is prescribed in combination with estradiol as hormone therapy during menopause to manage vasomotor symptoms and to prevent osteoporosis.Off-label, levonorgestrel may be used to treat menorrhagia, endometrial hyperplasia, and endometriosis.
Associated Conditions
- Endometrial Hyperplasia
- Endometriosis
- Heavy Menstrual Bleeding
- Hypermenorrhea
- Postmenopausal Osteoporosis
- Pregnancy
- Moderate Menopausal Vasomotor Symptoms
- Severe Vasomotor Symptoms Associated With Menopause
Research Report
Levonorgestrel (DB00367): A Comprehensive Monograph on its Chemistry, Pharmacology, Clinical Utility, and Development
Executive Summary
Levonorgestrel is a second-generation synthetic progestin that stands as a cornerstone of modern hormonal therapy and contraception. As the biologically active levorotatory enantiomer of norgestrel, it exerts potent progestational and androgenic effects, primarily by inhibiting ovulation through the suppression of the mid-cycle luteinizing hormone (LH) surge. Its remarkable versatility is demonstrated by its incorporation into a vast array of formulations, each tailored to a specific clinical need. These range from high-dose oral tablets for emergency contraception (EC) to low-dose daily oral pills (both combination and progestin-only), and long-acting reversible contraceptives (LARCs) such as subdermal implants and intrauterine devices (IUDs). Beyond contraception, levonorgestrel-releasing IUDs are approved for treating heavy menstrual bleeding and are used off-label for managing conditions like endometriosis and endometrial hyperplasia.
The pharmacological profile of levonorgestrel is well-characterized, but its clinical performance is significantly influenced by patient-specific factors, most notably body mass index (BMI). Pharmacokinetic studies have definitively shown that in women with obesity, increased volume of distribution and metabolic clearance lead to substantially lower plasma concentrations, providing a clear mechanistic basis for the observed reduction in EC efficacy in this population. This has highlighted a critical unmet need for evidence-based dosing strategies in individuals with high BMI.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2024/12/11 | Phase 3 | Not yet recruiting | |||
2024/10/01 | Not Applicable | Not yet recruiting | Zhang Jian | ||
2024/07/22 | Phase 1 | Active, not recruiting | |||
2024/07/09 | Phase 2 | Not yet recruiting | Gynuity Health Projects | ||
2024/06/14 | Phase 1 | Completed | |||
2024/03/12 | Phase 2 | Recruiting | |||
2023/10/10 | Phase 2 | Not yet recruiting | |||
2023/10/06 | Phase 1 | Completed | |||
2023/06/23 | N/A | Not yet recruiting | |||
2023/01/25 | Phase 2 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Home Health Brands, LLC | 85506-100 | ORAL | 1.5 mg in 1 1 | 4/23/2025 | |
| Agile Therapeutics, Inc. | 71671-100 | TRANSDERMAL | 2.60 mg in 1 1 | 9/11/2020 | |
| Rebel Distributors Corp | 21695-973 | ORAL | 1.5 mg in 1 1 | 7/14/2009 | |
| Physicians Total Care, Inc. | 54868-4894 | ORAL | 0.75 mg in 1 1 | 4/23/2012 | |
| Physicians Total Care, Inc. | 54868-5570 | TRANSDERMAL | 1.39 mg in 1 1 | 12/15/2010 | |
| Teva Pharmaceuticals, Inc. | 0480-3472 | ORAL | 90 ug in 1 1 | 3/6/2023 | |
| Dispensing Solutions, Inc. | 68258-3029 | ORAL | 0.75 mg in 1 1 | 9/30/2011 | |
| Novel Laboratories, Inc. | 40032-620 | ORAL | 1.5 mg in 1 1 | 2/26/2013 | |
| Novel Laboratories, Inc. | 40032-622 | ORAL | 1.5 mg in 1 1 | 9/15/2017 | |
| Bayer HealthCare Pharmaceuticals Inc. | 50419-491 | TRANSDERMAL | 0.015 mg in 1 d | 11/1/2017 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| MIRENA LEVONORGESTREL INTRAUTERINE SYSTEM 20 mcg/24 hr | SIN07915P | INTRAUTERINE DEVICE | 52 mg | 11/15/1994 | |
| POSTINOR 2 TABLET 0.75 mg | SIN11836P | TABLET | 0.75 mg | 3/5/2002 | |
| MICROGYNON 30 TABLET | SIN04834P | TABLET, SUGAR COATED | 0.15 mg | 6/26/1990 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| ESTINOR-1 TAB 0.75MG | N/A | N/A | N/A | 7/10/2009 | |
| NORDETTE TAB | N/A | N/A | N/A | 11/10/1978 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| APO-LEVONORGESTREL-1 levonorgestrel 1.5 mg tablet blister pack | 231506 | Medicine | A | 12/5/2014 | |
| MIRENA levonorgestrel 52mg intrauterine drug delivery system sachet | 73027 | Medicine | A | 7/24/2000 | |
| Triquilar ED Tablets Blister Pack | 10722 | Medicine | A | 8/19/1991 | |
| MICRONELLE 30 ED levonorgestrel 150 microgram and ethinylestradiol 30 microgram film-coated tablet blister pack | 211155 | Medicine | A | 1/31/2014 | |
| POSTELLA-1 levonorgestrel 1.5 mg tablet blister pack (new formulation) | 231505 | Medicine | A | 12/5/2014 | |
| NOVELLA-1 levonorgestrel 1.5mg tablet blister pack | 427700 | Medicine | A | 11/10/2023 | |
| POSTRELLE-1 levonorgestrel 1.5 mg tablet blister pack | 221973 | Medicine | A | 4/3/2014 | |
| LOETTE ethinylestradiol / levonorgestrel tablet blister pack | 296338 | Medicine | A | 1/23/2018 | |
| LEVLEN ED tablet blister pack | 40193 | Medicine | A | 6/18/1992 | |
| LOGYNON ED tablet blister pack | 40192 | Medicine | A | 6/18/1992 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| JAYDESS | Bayer Inc | 02408295 | Insert (Extended-Release) - Intrauterine | 13.5 MG | 10/30/2013 |
| ALESSE 21 | 02236974 | Tablet - Oral | 100 MCG | 1/7/1998 | |
| PORTIA 21 | teva canada limited | 02295946 | Tablet - Oral | 0.15 MG | 8/14/2007 |
| SEASONALE | teva canada limited | 02296659 | Tablet - Oral | 0.15 MG | 1/3/2008 |
| PLAN B | foundation consumer healthcare, llc | 02241674 | Tablet - Oral | 0.75 MG | 2/24/2000 |
| MIN-OVRAL 28 TAB | wyeth ltd. | 00782440 | Tablet - Oral | .15 MG | 12/31/1989 |
| AUDRINA 21 | 02532174 | Tablet - Oral | 100 MCG | 6/9/2023 | |
| OPTION 2 | perrigo international | 02371189 | Tablet - Oral | 0.75 MG | 9/25/2013 |
| MIRENA | Bayer Inc | 02243005 | Insert (Extended-Release) - Intrauterine | 52 MG | 2/22/2001 |
| LAYLAA 28 | lupin pharma canada limited | 02424290 | Tablet - Oral | 100 MCG | 7/6/2023 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| LEVOSERT 0,02 MG CADA 24 HORAS SISTEMA DE LIBERACION INTRAUTERINO | 80021 | SISTEMA DE LIBERACIÓN INTRAUTERINO | Diagnóstico Hospitalario | Commercialized | |
| LINELLE 0,1mg/0,02mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | 71708 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized | |
| LEVONORGESTREL/ETINILESTRADIOL DURBAN 0,1 MG/0,02 MG COMPRIMIDOS RECUBIERTOS EFG | Laboratorios Francisco Durban S.A. | 82942 | COMPRIMIDO RECUBIERTO | Medicamento Sujeto A Prescripción Médica | Commercialized |
| LEVESIALLE DIARIO 0,10 MG/0,02 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Exeltis Healthcare S.L. | 80973 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized |
| JAYDESS 13,5 MG SISTEMA DE LIBERACION INTRAUTERINO | Bayer Hispania S.L. | 77169 | SISTEMA DE LIBERACIÓN INTRAUTERINO | Diagnóstico Hospitalario | Commercialized |
| LEVONORGESTREL STADA 1.5 MG COMPRIMIDO EFG | Laboratorio Stada S.L. | 78911 | COMPRIMIDO | Sin Receta | Commercialized |
| LEVONORGESTREL/ETINILESTRADIOL STADA 0,1 MG/0,02 MG COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Laboratorio Stada S.L. | 77458 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized |
| MICROGYNON 0,15 mg / 0,03 mg COMPRIMIDOS RECUBIERTOS | BE091235 | COMPRIMIDO RECUBIERTO | Medicamento Sujeto A Prescripción Médica | Commercialized | |
| TRIAGYNON COMPRIMIDOS RECUBIERTOS | Bayer B.V. | RVG08663 | COMPRIMIDO RECUBIERTO | Medicamento Sujeto A Prescripción Médica | Not Commercialized |
| LEVONORGESTREL SANDOZ 1,5 MG COMPRIMIDO EFG | Sandoz Farmaceutica S.A. | 78438 | COMPRIMIDO | Sin Receta | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
Help Us Improve
Your feedback helps us provide better drug information and insights.