Peringatan Keamanan

Administration of large quantities of desogestrel has been shown to produce strong hormonal effects but to lack chronic toxicity. The reported LD50 in rats after oral administration of desogestrel is higher than 2000 mg/kg.T521 Overdose hasn't reported serious effects but only symptoms of nausea and withdrawal of bleeding.FDA label

Most reports haven't linked the administration of desogestrel with the increased risk of breast cancer. The increased risk has been reported to be related to the duration of use. However, several reports indicate a desogestrel-driven increased risk in cervical intra-epithelial neoplasia but the results are still not conclusive.FDA label

Desogestrel

DB00304

small molecule approved

Deskripsi

Desogestrel, a prodrug, is a third generation progestogenA176315 and hence, a member of the gonane family which was largely used in Europe before being approved in the US and Canada.A176339 It was firstly generated from a study that showed that 11-beta and 11-alkylidene substituent in nortestosterone can enhance the biological activity.T521 Desogestrel is now produced semi-synthetically from naturally occurred plant steroids.F4127 In the US, desogestrel is found only in combination with ethinyl estradiol.A176342 The first approved drug containing desogestrel was developed by Organon USA Inc in 1972 and FDA approved in 1992.L5762

Struktur Molekul 2D

Berat 310.473
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life of desogestrel is determined to be of 30 hours.[F4127]
Volume Distribusi The apparent volume of distribution of desogestrel is of 1.5 L/kg.[F4127]
Klirens (Clearance) The metabolic clearance rate of desogestrel is reported to be of about 2 ml/min/kg.[F4127]

Absorpsi

After oral administration, desogestrel is rapidly absorbed and it reaches a peak concentration of 2 ng/ml after 1.5 hours. The bioavailability of desogestrel is reported to be in the range of 60-80% and the reported AUC is of 3000 ng.h/ml.F4127 Almost all the administered dose is modified to the active metabolite, etonogestrel.A176423

Metabolisme

Desogestrel is rapidly metabolized in the intestinal mucosa and by first-pass hepatic metabolismT357 to form the major metabolite of desogestrel is etonogestrel which is the biologically active metabolite.A176333, A176336 This modification is described by the hydroxylation in C3 of the desogestrel molecule.A176423 Later, etonogestrel is metabolized following the normal pathways of steroid metabolism. On the other hand, due to the 11-methylene side chain, desogestrel cannot be metabolized to other progestins.F4127

Rute Eliminasi

The elimination of desogestrel is found to be mainly renal corresponding to about 6 times the dose eliminated in the bile.F4127 The elimination of desogestrel is only done as the metabolites and not as the unchanged drug and about 85% of the administered dose can be excreted as metabolites after 6-8 days.T521

Interaksi Obat

838 Data
Acitretin The therapeutic efficacy of Desogestrel can be decreased when used in combination with Acitretin.
Aprepitant The serum concentration of Desogestrel can be decreased when it is combined with Aprepitant.
Atazanavir The serum concentration of Desogestrel can be increased when it is combined with Atazanavir.
Boceprevir The serum concentration of Desogestrel can be increased when it is combined with Boceprevir.
Prucalopride The serum concentration of Desogestrel can be decreased when it is combined with Prucalopride.
Sugammadex The serum concentration of Desogestrel can be decreased when it is combined with Sugammadex.
Thalidomide Desogestrel may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Desogestrel can be decreased when used in combination with Ulipristal.
Deferasirox The metabolism of Deferasirox can be increased when combined with Desogestrel.
Estradiol The metabolism of Estradiol can be increased when combined with Desogestrel.
Propacetamol The metabolism of Propacetamol can be increased when combined with Desogestrel.
Tramadol The metabolism of Tramadol can be increased when combined with Desogestrel.
Liothyronine The metabolism of Liothyronine can be increased when combined with Desogestrel.
Morphine The metabolism of Morphine can be increased when combined with Desogestrel.
Indomethacin The metabolism of Indomethacin can be increased when combined with Desogestrel.
Minoxidil The metabolism of Minoxidil can be increased when combined with Desogestrel.
Raloxifene The metabolism of Raloxifene can be increased when combined with Desogestrel.
Zidovudine The metabolism of Zidovudine can be increased when combined with Desogestrel.
Diclofenac The metabolism of Diclofenac can be increased when combined with Desogestrel.
Labetalol The metabolism of Labetalol can be increased when combined with Desogestrel.
Losartan The metabolism of Losartan can be decreased when combined with Desogestrel.
Furosemide The metabolism of Furosemide can be increased when combined with Desogestrel.
Naltrexone The metabolism of Naltrexone can be increased when combined with Desogestrel.
Flurbiprofen The metabolism of Flurbiprofen can be increased when combined with Desogestrel.
Naproxen The metabolism of Naproxen can be increased when combined with Desogestrel.
Propofol The metabolism of Propofol can be increased when combined with Desogestrel.
Metronidazole The metabolism of Metronidazole can be increased when combined with Desogestrel.
Buprenorphine The metabolism of Buprenorphine can be increased when combined with Desogestrel.
Fulvestrant The metabolism of Fulvestrant can be increased when combined with Desogestrel.
Ezetimibe The metabolism of Ezetimibe can be increased when combined with Desogestrel.
Ketoprofen The metabolism of Ketoprofen can be increased when combined with Desogestrel.
Abacavir The metabolism of Abacavir can be increased when combined with Desogestrel.
Ibuprofen The metabolism of Ibuprofen can be increased when combined with Desogestrel.
Carvedilol The metabolism of Carvedilol can be increased when combined with Desogestrel.
Fusidic acid The metabolism of Fusidic acid can be increased when combined with Desogestrel.
Alvocidib The metabolism of Alvocidib can be increased when combined with Desogestrel.
Indacaterol The metabolism of Indacaterol can be increased when combined with Desogestrel.
Eltrombopag The metabolism of Eltrombopag can be increased when combined with Desogestrel.
Bazedoxifene The metabolism of Bazedoxifene can be increased when combined with Desogestrel.
Muraglitazar The metabolism of Muraglitazar can be increased when combined with Desogestrel.
Gavestinel The metabolism of Gavestinel can be increased when combined with Desogestrel.
Raltegravir The metabolism of Raltegravir can be increased when combined with Desogestrel.
Dolutegravir The metabolism of Dolutegravir can be increased when combined with Desogestrel.
Bictegravir The metabolism of Bictegravir can be increased when combined with Desogestrel.
Letermovir The metabolism of Letermovir can be increased when combined with Desogestrel.
Nintedanib The metabolism of Nintedanib can be increased when combined with Desogestrel.
Dexibuprofen The metabolism of Dexibuprofen can be increased when combined with Desogestrel.
Delafloxacin The metabolism of Delafloxacin can be increased when combined with Desogestrel.
Lumateperone The metabolism of Lumateperone can be increased when combined with Desogestrel.
Darolutamide The metabolism of Darolutamide can be increased when combined with Desogestrel.
Atorvastatin The metabolism of Atorvastatin can be increased when combined with Desogestrel.
Selumetinib The metabolism of Selumetinib can be increased when combined with Desogestrel.
Cabotegravir The metabolism of Cabotegravir can be increased when combined with Desogestrel.
Febuxostat The metabolism of Febuxostat can be increased when combined with Desogestrel.
Ponesimod The metabolism of Ponesimod can be increased when combined with Desogestrel.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Desogestrel.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Desogestrel.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Desogestrel.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Desogestrel.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Desogestrel.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Desogestrel.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Desogestrel.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Desogestrel.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Desogestrel.
cis-Diamminechlorocholylglycinateplatinum(II) The therapeutic efficacy of cis-Diamminechlorocholylglycinateplatinum(II) can be decreased when used in combination with Desogestrel.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Desogestrel.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Desogestrel.
Aramchol The therapeutic efficacy of Aramchol can be decreased when used in combination with Desogestrel.
Ox bile extract The therapeutic efficacy of Ox bile extract can be decreased when used in combination with Desogestrel.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Desogestrel.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Desogestrel.
Tranexamic acid Desogestrel may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Desogestrel can be decreased when it is combined with Clobazam.
Colestipol Colestipol can cause a decrease in the absorption of Desogestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Desogestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Desogestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Desogestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Griseofulvin The metabolism of Desogestrel can be increased when combined with Griseofulvin.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Desogestrel.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Desogestrel.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Desogestrel.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Desogestrel.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Desogestrel.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Desogestrel.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Desogestrel.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Desogestrel.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Desogestrel.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Desogestrel.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Desogestrel.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Desogestrel.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Desogestrel.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Desogestrel.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Desogestrel.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Desogestrel.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Desogestrel.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Desogestrel.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Desogestrel.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Desogestrel.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Desogestrel.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Desogestrel.

Target Protein

Progesterone receptor PGR
Estrogen receptor ESR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28344968
    Park MJ, Jeon GH: Pulmonary embolism in a healthy woman using the oral contraceptives containing desogestrel. Obstet Gynecol Sci. 2017 Mar;60(2):232-235. doi: 10.5468/ogs.2017.60.2.232. Epub 2017 Mar 16.
  • PMID: 21287884
    Schrager S, Paddock E, Dalby J, Knudsen L: Contraception in Wisconsin: a review. WMJ. 2010 Dec;109(6):326-31.
  • PMID: 18854070
    Shimoni N, Westhoff C: Review of the vaginal contraceptive ring (NuvaRing). J Fam Plann Reprod Health Care. 2008 Oct;34(4):247-50. doi: 10.1783/147118908786000370.
  • PMID: 8924815
    Laurendeau L: Desogestrel contraceptives: the perfect pill for lipids?. Can Fam Physician. 1996 Jan;42:62-71.
  • PMID: 30000422
    Authors unspecified: Desogestrel .
  • PMID: 15006321
    Guillebaud J: CEU New Product Review of the desogestrel-only pill. J Fam Plann Reprod Health Care. 2004 Jan;30(1):64; author reply 64-5.
  • PMID: 8447355
    McClamrock HD, Adashi EY: Pharmacokinetics of desogestrel. Am J Obstet Gynecol. 1993 Mar;168(3 Pt 2):1021-8.
Textbook
  • ISBN: 978-0-7817-6879-5
    Lemke T., Williams D., Roche V. and Zito W. (2008). Foye's Principles of Medicinal Chemistry (6th) (6th ed.). Lippincott Williams & Wilkins.
  • ISBN: 978-1-4377-0310-8
    Bardal S, Waechter J, Martin D. (2011). Applied Pharmacology. Elsevier Health Sciences.
  • ISBN: 978-3-642-73792-3
    Runnebaum B., Rabe K. and Kiesel L. (1988). Female contraception. Springer-Verlag.

Contoh Produk & Brand

Produk: 113 • International brands: 2
Produk
  • Apri
    Kit • - • Oral • US • Generic • Approved
  • Apri 21
    Tablet • - • Oral • Canada • Approved
  • Apri 28
    Tablet • - • Oral • Canada • Approved
  • Apri 28 Day
    Kit • - • Oral • US • Generic • Approved
  • Apri 28 Day
    Kit • - • Oral • US • Generic • Approved
  • Azurette
    Kit • - • Oral • US • Generic • Approved
  • Azurette
    Kit • - • Oral • US • Generic • Approved
  • Azurette
    Kit • - • Oral • US • Generic • Approved
Menampilkan 8 dari 113 produk.
International Brands
  • Cerazette — Organon
  • Marvelon — Adcock Ingram Pharmaceuticals

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