Peringatan Keamanan

The oral LD50 in rats is greater than 5000 mg/kg.L7790

An overdose of this drug, like other contraceptives, may cause nausea and withdrawal bleeding. Provide symptomatic treatment in the case of a levonorgestrel overdose and contact the local poison control center. There is no specific antidote for a levonorgestrel overdose.L7760,L7793,L7796

Levonorgestrel

DB00367

small molecule approved investigational

Deskripsi

Levonorgestrel (LNG) is a synthetic progestogen similar to Progesterone used in contraception and hormone therapy.A181988,T659 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.L7823 In addition to the above uses, levonorgestrel is used as a component of long-term combination contraceptives.A181991,L7760,L7778

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.A181976,A181994,L7760

Struktur Molekul 2D

Berat 312.4458
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of a 0.75 mg dose of 1.5 mg of levonorgestrel ranges between 20-60 hours post-administration.[A181976] A pharmacokinetic study of women with a normal BMI and BMI over revealed an elimination half-life of 29.7 h and 41.0-46.4 hours, respectively.[A181985] Another pharmacokinetic study revealed a mean elimination half-life of 24.4 hours after a 0.75 mg dose of levonorgestrel was administered to 16 patients.[A181979]
Volume Distribusi One pharmacokinetic study determined a mean steady-state volume of distribution of 1.5 mg of levonorgestrel to be 162.2 L in those with normal BMI and in the range of 404.7 L to 466.4 L in obese patients with a body mass index of at least 30.[A181985] Mean volume of distribution in 16 patients receiving 0.75 mg of levonorgestrel in another pharmacokinetic study was 260 L.[A181979] The Plan B one-step FDA label reports an apparent volume of distribution of 1.8 L/kg.[L7760]
Klirens (Clearance) Clearance was found to 4.8 L/h in healthy female volunteers with a normal BMI, and 7.70-8.51 L/h in obese patients after a single 1.5 mg dose.[A181985] After a 0.75 mg dose of levonorgestrel in 16 patients in another pharmacokinetic study, mean clearance was calculated at 7.06 L/h.[A181979] Following levonorgestrel implant removal, the serum concentration falls below 100 pg/mL within the first 96 hours and further falls below the sensitivity of detection within the range of 5 days to 2 weeks.[L7823]

Absorpsi

Orally administered levonorgestrel is absorbed in the gastrointestinal tract while levonorgestrel administered through an IUD device is absorbed in the endometrium. Levonorgestrel is absorbed immediately in the interstitial fluids when it is inserted as a subdermal implant.L7823 After insertion of the subdermal implant, the Cmax of levonorgestrel is attained within 2-3 days.L7823The Cmax following one dose of 0.75 mg of oral levonorgestrel is reached within the hour after administration, according to one reference.A181976 In a pharmacokinetic study of 1.5 mg of levonorgestrel in women with a normal BMI and those considered to be obese (BMI>30), mean Cmax was found to be 16.2 ng/mL and 10.5 ng/mL respectively. Tmax was found to be 2 hours for those with normal BMI and 2.5 hours for patients with increased BMI.A181985 The bioavailability of levonorgestrel approaches 100%.L7793 Mean AUC has been shown to be higher in patients with a normal BMI, measuring at 360.1 h × ng/mL versus a range of 197.28 to 208.1 h × ng/mL in an obese group of patients. Obesity may contribute to decreased efficacy of levonorgestrel in contraception.A181985

Metabolisme

After absorption of the oral emergency contraceptive preparation, levonorgestrel is conjugated and forms a large number of sulfate conjugates. In addition, glucuronide conjugates have been identified in the plasma.A182033 High levels of conjugated and unconjugated 3?, 5?-tetrahydrolevonorgestrel are found in the plasma. The entire metabolic pathway for levonorgestrel has not been studied, however, 16?-hydroxylation is one pathway that has been identified.L7823 Small quantities of 3?, 5?­ tetrahydrolevonorgestrel and 16?hydroxylevonorgestrel are also formed.L7760 No active metabolites have been identified.L7793 The rate of metabolism may be considerably different according to the patient and may explain a wide variation in levonorgestrel clearance.L7760 Liver CYP3A4 and CYP3A5 hepatic enzymes are reported to be involved in the metabolism of levonorgestrel.A182084,L7760

Rute Eliminasi

Approximately 45% of an oral levonorgestrel dose and its conjugated or sulfate metabolites are found to be excreted in the urine. Approximately 32% of an orally ingested dose is found excreted in feces, primarily in the form of glucuronide conjugates of levonorgestrel.L7760

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food. The effect of food on absorption has not been evaluated.

Interaksi Obat

738 Data
Acitretin The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Acitretin.
Atazanavir The serum concentration of Levonorgestrel can be increased when it is combined with Atazanavir.
Boceprevir The serum concentration of Levonorgestrel can be increased when it is combined with Boceprevir.
Prucalopride The serum concentration of Levonorgestrel can be decreased when it is combined with Prucalopride.
Sugammadex The serum concentration of Levonorgestrel can be decreased when it is combined with Sugammadex.
Thalidomide Levonorgestrel may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Ulipristal.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Levonorgestrel.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Levonorgestrel.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Levonorgestrel.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Levonorgestrel.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Levonorgestrel.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Levonorgestrel.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Levonorgestrel.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Levonorgestrel.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Levonorgestrel.
cis-Diamminechlorocholylglycinateplatinum(II) The therapeutic efficacy of cis-Diamminechlorocholylglycinateplatinum(II) can be decreased when used in combination with Levonorgestrel.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Levonorgestrel.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Levonorgestrel.
Aramchol The therapeutic efficacy of Aramchol can be decreased when used in combination with Levonorgestrel.
Ox bile extract The therapeutic efficacy of Ox bile extract can be decreased when used in combination with Levonorgestrel.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Levonorgestrel.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Levonorgestrel.
Tranexamic acid Levonorgestrel may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Levonorgestrel can be decreased when it is combined with Clobazam.
Colestipol Colestipol can cause a decrease in the absorption of Levonorgestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Levonorgestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Levonorgestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Levonorgestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Griseofulvin The metabolism of Levonorgestrel can be increased when combined with Griseofulvin.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Levonorgestrel.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Levonorgestrel.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Levonorgestrel.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Levonorgestrel.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Levonorgestrel.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Levonorgestrel.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Levonorgestrel.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Levonorgestrel.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Levonorgestrel.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Levonorgestrel.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Levonorgestrel.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Levonorgestrel.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Levonorgestrel.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Levonorgestrel.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Levonorgestrel.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Levonorgestrel.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Levonorgestrel.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Levonorgestrel.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Levonorgestrel.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Levonorgestrel.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Levonorgestrel.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Levonorgestrel.
Mometasone furoate The serum concentration of Mometasone furoate can be increased when it is combined with Levonorgestrel.
Hydrocortisone acetate The serum concentration of Hydrocortisone acetate can be increased when it is combined with Levonorgestrel.
Hydrocortisone succinate The serum concentration of Hydrocortisone succinate can be increased when it is combined with Levonorgestrel.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Levonorgestrel.
Prednisolone hemisuccinate The serum concentration of Prednisolone hemisuccinate can be increased when it is combined with Levonorgestrel.
Methylprednisolone hemisuccinate The serum concentration of Methylprednisolone hemisuccinate can be increased when it is combined with Levonorgestrel.
Prednisone acetate The serum concentration of Prednisone acetate can be increased when it is combined with Levonorgestrel.
Clocortolone acetate The serum concentration of Clocortolone acetate can be increased when it is combined with Levonorgestrel.
Melengestrol acetate The serum concentration of Melengestrol acetate can be increased when it is combined with Levonorgestrel.
Betamethasone phosphate The serum concentration of Betamethasone phosphate can be increased when it is combined with Levonorgestrel.
Cortisone The serum concentration of Cortisone can be increased when it is combined with Levonorgestrel.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Levonorgestrel.
Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Levonorgestrel.
Fluticasone The serum concentration of Fluticasone can be increased when it is combined with Levonorgestrel.
Budesonide The serum concentration of Budesonide can be increased when it is combined with Levonorgestrel.
Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Levonorgestrel.
Paramethasone The serum concentration of Paramethasone can be increased when it is combined with Levonorgestrel.
Hydrocortisone cypionate The serum concentration of Hydrocortisone cypionate can be increased when it is combined with Levonorgestrel.
Fludrocortisone The serum concentration of Fludrocortisone can be increased when it is combined with Levonorgestrel.
Trilostane The serum concentration of Trilostane can be increased when it is combined with Levonorgestrel.
Ciclesonide The serum concentration of Ciclesonide can be increased when it is combined with Levonorgestrel.
Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Levonorgestrel.
Fluprednisolone The serum concentration of Fluprednisolone can be increased when it is combined with Levonorgestrel.
Melengestrol The serum concentration of Melengestrol can be increased when it is combined with Levonorgestrel.
Clobetasol propionate The serum concentration of Clobetasol propionate can be increased when it is combined with Levonorgestrel.
Fluocinonide The serum concentration of Fluocinonide can be increased when it is combined with Levonorgestrel.
Hydrocortisone butyrate The serum concentration of Hydrocortisone butyrate can be increased when it is combined with Levonorgestrel.
Desoximetasone The serum concentration of Desoximetasone can be increased when it is combined with Levonorgestrel.
Mometasone The serum concentration of Mometasone can be increased when it is combined with Levonorgestrel.
Fluocortolone The serum concentration of Fluocortolone can be increased when it is combined with Levonorgestrel.
Prednisolone acetate The serum concentration of Prednisolone acetate can be increased when it is combined with Levonorgestrel.
Fluorometholone The serum concentration of Fluorometholone can be increased when it is combined with Levonorgestrel.
Difluocortolone The serum concentration of Difluocortolone can be increased when it is combined with Levonorgestrel.
Flumethasone The serum concentration of Flumethasone can be increased when it is combined with Levonorgestrel.
Methylprednisolone aceponate The serum concentration of Methylprednisolone aceponate can be increased when it is combined with Levonorgestrel.
Vitamin A The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Vitamin A.
Bexarotene The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Bexarotene.
Alitretinoin The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Alitretinoin.
Tretinoin The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Tretinoin.
Tazarotene The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Tazarotene.
Etretinate The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Etretinate.
Isotretinoin The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Isotretinoin.
4-Oxoretinol The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with 4-Oxoretinol.
Fenretinide The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Fenretinide.
Ro 12-7310 The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Ro 12-7310.
Zuretinol acetate The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Zuretinol acetate.
Motretinide The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Motretinide.
Bosentan The serum concentration of Levonorgestrel can be decreased when it is combined with Bosentan.

Target Protein

Progesterone receptor PGR
3-oxo-5-alpha-steroid 4-dehydrogenase 1 SRD5A1
Estrogen receptor ESR1
Androgen receptor AR
Sex hormone-binding globulin SHBG
Glucocorticoid receptor NR3C1

Referensi & Sumber

Synthesis reference: Yu-Sheng Chang, Shu-Ping Chen, "Levonorgestrel Crystallization." U.S. Patent US20090069584, issued March 12, 2009.
Artikel (PubMed)
  • PMID: 10715364
    Edgren RA, Stanczyk FZ: Nomenclature of the gonane progestins. Contraception. 1999 Dec;60(6):313.
  • PMID: 16291771
    Sitruk-Ware R: New progestagens for contraceptive use. Hum Reprod Update. 2006 Mar-Apr;12(2):169-78. Epub 2005 Nov 16.
  • PMID: 25698840
    Kahlenborn C, Peck R, Severs WB: Mechanism of action of levonorgestrel emergency contraception. Linacre Q. 2015 Feb;82(1):18-33. doi: 10.1179/2050854914Y.0000000026.
  • PMID: 12169384
    Kook K, Gabelnick H, Duncan G: Pharmacokinetics of levonorgestrel 0.75 mg tablets. Contraception. 2002 Jul;66(1):73-6.
  • PMID: 16860047
    Sambol NC, Harper CC, Kim L, Liu CY, Darney P, Raine TR: Pharmacokinetics of single-dose levonorgestrel in adolescents. Contraception. 2006 Aug;74(2):104-9. doi: 10.1016/j.contraception.2006.01.011. Epub 2006 Jun 16.
  • PMID: 30703352
    Natavio M, Stanczyk FZ, Molins EAG, Nelson A, Jusko WJ: Pharmacokinetics of the 1.5 mg levonorgestrel emergency contraceptive in women with normal, obese and extremely obese body mass index. Contraception. 2019 May;99(5):306-311. doi: 10.1016/j.contraception.2019.01.003. Epub 2019 Jan 28.
  • PMID: 24708837
    Shohel M, Rahman MM, Zaman A, Uddin MM, Al-Amin MM, Reza HM: A systematic review of effectiveness and safety of different regimens of levonorgestrel oral tablets for emergency contraception. BMC Womens Health. 2014 Apr 4;14:54. doi: 10.1186/1472-6874-14-54.
  • PMID: 27525548
    Polis CB, Phillips SJ, Hillier SL, Achilles SL: Levonorgestrel in contraceptives and multipurpose prevention technologies: does this progestin increase HIV risk or interact with antiretrovirals? AIDS. 2016 Nov 13;30(17):2571-2576. doi: 10.1097/QAD.0000000000001229.
Menampilkan 8 dari 17 artikel.
Textbook
  • Christina Vrettakos; Tushar Bajaj (2019). Levonorgestrel. Stat Pearls NIH.

Contoh Produk & Brand

Produk: 367 • International brands: 10
Produk
  • Afirmelle
    Kit; Tablet • - • Oral • US • Generic • Approved
  • After Banger
    Tablet • 1.5 mg/1 • Oral • US • Generic • OTC • Approved
  • Aftera
    Tablet • 1.5 mg/1 • Oral • US • Generic • OTC • Approved
  • Aftera
    Tablet • 1.5 mg/1 • Oral • US • Generic • OTC • Approved
  • AfterPill
    Tablet • 1.5 mg/1 • Oral • US • Generic • OTC • Approved
  • AfterPill
    Tablet • 1.5 mg/1 • Oral • US • Generic • OTC • Approved
  • AfterPlan
    Tablet • 1.5 mg/1 • Oral • US • Generic • OTC • Approved
  • Alesse 21
    Tablet • - • Oral • Canada • Approved
Menampilkan 8 dari 367 produk.
International Brands
  • Jadelle — Bayer
  • Levonelle — Bayer
  • Medonor — Medopharm
  • Microlut — Bayer
  • Microluton
  • Microval — Wyeth
  • Neogest — Schering
  • Norgeston — Bayer
  • Norplant — Bayer
  • Postinor — Gedeon Richter

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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