Peringatan Keamanan

Data regarding overdoses of norgestimate are rare.L11845,L11848 However, the majority of patients overdosing on oral contraceptives do not become seriously ill.A191080 Treat overdoses with symptomatic and supportive care.A191080,L11845,L11848

Norgestimate

DB00957

small molecule approved investigational

Deskripsi

Norgestimate was first described in the literature in 1977.A191068 It was developed by Ortho Pharmaceutical Corporation as part of an effort to develop new hormonal contraceptives with reduced adverse effects.A191068 It is commonly formulated with ethinylestradiol as a combined oral contraceptive that can also be used to treat moderate acne vulgaris.L11845,L11848

Norgestimate was granted FDA approval on 29 December 1989.L11842

Struktur Molekul 2D

Berat 369.4971
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Norgestimate is rapidly deacetylated.[A190981,A35883] The active metabolites of norgestimate, 17-desacetyl norgestimate, has a half life of 12-30h,[A190981] while norgestrel has a half life of 36.4±10.2h.[L11848]
Volume Distribusi Data regarding the volume of distribution of norgestimate are not readily available.[L11845,L11848]
Klirens (Clearance) Data regarding the clearance of norgestimate is not readily available.[L11845,L11848]

Absorpsi

Oral norgestimate has a Tmax of 0.5-2h.A190981 On day 21 of cycle 3, 17-desacetylnorgestimate reaches a Cmax of 1.82ng/mL, with a Tmax of 1.5h, and an AUC of 16.1h\*ng/mL.L11848 At the same time, norgestrel reaches a Cmax of 2.79ng/mL, with a Tmax of 1.7h, and an AUC of 49.9h\*ng/mL.L11848

Metabolisme

Norgestimate is rapidly deacetylated to the active 17-desacetylnorgestimate, which is deoximated to the active norgestrel.A190981,A35883 17-desacetylnorgestimate is metabolized to a number of undefined hydroxylated metabolites, mainly by CYP3A4 and to a lesser extend by CYP2B6 and CYP2C9.A35883 Norgestrel is O-glucuronidated by UGT1A1 or oxidized to a number of undefined hydroxylated metabolites by CYP3A4.A35883

Rute Eliminasi

Norgestimate is 45-49% eliminated in urine and 16-49% eliminated in feces.L11845 Unchanged norgestimate is not detected in urine.L11845

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food.

Interaksi Obat

1047 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Norgestimate.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Norgestimate.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Norgestimate.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Norgestimate.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Norgestimate.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Norgestimate.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Norgestimate.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Norgestimate.
Silodosin The excretion of Silodosin can be decreased when combined with Norgestimate.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Norgestimate.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Norgestimate.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Norgestimate.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Norgestimate.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Norgestimate.
Acitretin The therapeutic efficacy of Norgestimate can be decreased when used in combination with Acitretin.
Aprepitant The serum concentration of Norgestimate can be decreased when it is combined with Aprepitant.
Atazanavir The serum concentration of Norgestimate can be increased when it is combined with Atazanavir.
Boceprevir The serum concentration of Norgestimate can be increased when it is combined with Boceprevir.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Norgestimate.
Sugammadex The serum concentration of Norgestimate can be decreased when it is combined with Sugammadex.
Thalidomide Norgestimate may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Norgestimate can be decreased when used in combination with Ulipristal.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Norgestimate.
Perampanel The metabolism of Perampanel can be increased when combined with Norgestimate.
Warfarin The metabolism of Warfarin can be increased when combined with Norgestimate.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Norgestimate.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Norgestimate.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Norgestimate.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Norgestimate.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Norgestimate.
Zidovudine The metabolism of Norgestimate can be increased when combined with Zidovudine.
Testosterone propionate The metabolism of Norgestimate can be increased when combined with Testosterone propionate.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Norgestimate.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Norgestimate.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Norgestimate.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Norgestimate.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Norgestimate.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Norgestimate.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Norgestimate.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Norgestimate.
cis-Diamminechlorocholylglycinateplatinum(II) The therapeutic efficacy of cis-Diamminechlorocholylglycinateplatinum(II) can be decreased when used in combination with Norgestimate.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Norgestimate.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Norgestimate.
Aramchol The therapeutic efficacy of Aramchol can be decreased when used in combination with Norgestimate.
Ox bile extract The therapeutic efficacy of Ox bile extract can be decreased when used in combination with Norgestimate.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Norgestimate.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Norgestimate.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Norgestimate.
Vincristine The excretion of Vincristine can be decreased when combined with Norgestimate.
Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Norgestimate.
Tranexamic acid Norgestimate may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Norgestimate can be decreased when it is combined with Clobazam.
Colestipol Colestipol can cause a decrease in the absorption of Norgestimate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Norgestimate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Norgestimate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Norgestimate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Griseofulvin The metabolism of Norgestimate can be increased when combined with Griseofulvin.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Norgestimate.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Norgestimate.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Norgestimate.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Norgestimate.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Norgestimate.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Norgestimate.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Norgestimate.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Norgestimate.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Norgestimate.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Norgestimate.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Norgestimate.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Norgestimate.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Norgestimate.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Norgestimate.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Norgestimate.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Norgestimate.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Norgestimate.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Norgestimate.
Hydrocortisone acetate The serum concentration of Hydrocortisone acetate can be increased when it is combined with Norgestimate.
Hydrocortisone succinate The serum concentration of Hydrocortisone succinate can be increased when it is combined with Norgestimate.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Norgestimate.
Prednisolone hemisuccinate The serum concentration of Prednisolone hemisuccinate can be increased when it is combined with Norgestimate.
Methylprednisolone hemisuccinate The serum concentration of Methylprednisolone hemisuccinate can be increased when it is combined with Norgestimate.
Prednisone acetate The serum concentration of Prednisone acetate can be increased when it is combined with Norgestimate.
Clocortolone acetate The serum concentration of Clocortolone acetate can be increased when it is combined with Norgestimate.
Melengestrol acetate The serum concentration of Melengestrol acetate can be increased when it is combined with Norgestimate.
Betamethasone phosphate The serum concentration of Betamethasone phosphate can be increased when it is combined with Norgestimate.
Cortisone The serum concentration of Cortisone can be increased when it is combined with Norgestimate.
Budesonide The serum concentration of Budesonide can be increased when it is combined with Norgestimate.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Norgestimate.
Fludrocortisone The serum concentration of Fludrocortisone can be increased when it is combined with Norgestimate.
Trilostane The serum concentration of Trilostane can be increased when it is combined with Norgestimate.
Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Norgestimate.
Paramethasone The serum concentration of Paramethasone can be increased when it is combined with Norgestimate.
Ciclesonide The serum concentration of Ciclesonide can be increased when it is combined with Norgestimate.
Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Norgestimate.
Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Norgestimate.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Norgestimate.
Fluprednisolone The serum concentration of Fluprednisolone can be increased when it is combined with Norgestimate.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Norgestimate.
Melengestrol The serum concentration of Melengestrol can be increased when it is combined with Norgestimate.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Norgestimate.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Norgestimate.

Target Protein

Progesterone receptor PGR
Estrogen receptor ESR1
Androgen receptor AR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29403920
    Saxena A, Gupta AK, Kumar VP, Nainar MS, Bob M, Kasibhatta R: Quantification of 17-desacetyl norgestimate in human plasma by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and its application to bioequivalence study. J Pharm Anal. 2015 Apr;5(2):93-100. doi: 10.1016/j.jpha.2014.09.004. Epub 2014 Sep 22.
  • PMID: 28283499
    Ahire D, Sinha S, Brock B, Iyer R, Mandlekar S, Subramanian M: Metabolite Identification, Reaction Phenotyping, and Retrospective Drug-Drug Interaction Predictions of 17-Deacetylnorgestimate, the Active Component of the Oral Contraceptive Norgestimate. Drug Metab Dispos. 2017 Jun;45(6):676-685. doi: 10.1124/dmd.116.073940. Epub 2017 Mar 10.
  • PMID: 12586319
    Hammond GL, Abrams LS, Creasy GW, Natarajan J, Allen JG, Siiteri PK: Serum distribution of the major metabolites of norgestimate in relation to its pharmacological properties. Contraception. 2003 Feb;67(2):93-9.
  • PMID: 17505938
    Paris F, Rabeolina F, Balaguer P, Bacquet A, Sultan C: Antiandrogenic activity of norgestimate in a human androgen-dependent stable-transfected cell line. Gynecol Endocrinol. 2007 Apr;23(4):193-7.
  • PMID: 201429
    Hahn DW, Allen GO, McGuire JL: The pharmacological profile of norgestimate, a new orally active progestin. Contraception. 1977 Nov;16(5):541-53. doi: 10.1016/0010-7824(77)90077-4.
  • PMID: 27006385
    Weerasinghe M, Konradsen F, Eddleston M, Pearson M, Agampodi T, Storm F, Agampodi S: Overdose of oral contraceptive pills as a means of intentional self-poisoning amongst young women in Sri Lanka: considerations for family planning. J Fam Plann Reprod Health Care. 2017 Apr;43(2):147-150. doi: 10.1136/jfprhc-2015-101171. Epub 2016 Mar 22.
  • PMID: 28613632
    Cooper DB, Mahdy H: Oral Contraceptive Pills .
  • PMID: 15548387
    Frohlich M, Albermann N, Sauer A, Walter-Sack I, Haefeli WE, Weiss J: In vitro and ex vivo evidence for modulation of P-glycoprotein activity by progestins. Biochem Pharmacol. 2004 Dec 15;68(12):2409-16. doi: 10.1016/j.bcp.2004.08.026.

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