Peringatan Keamanan

The oral LD50 in rats is >6400mg/kg and in mice is >16g/kg.L8738 The intraperitoneal LD50 in rats is >900mg/kg and in mice is >1500mg/kg.L8738 The subcutaneous LD50 in rats is >900mg/kg and in mice is>1500mg/kg.L8738

Patients experiencing and overdose or oral medroxyprogesterone acetate (MPA) may present with nausea, vomiting, breast tenderness, dizziness, abdominal pain, drowsiness, fatigue, and withdrawal bleeding.L8657,L8660 Treat patients by stopping MPA and beginning symptomatic treatment.L8657,L8660 Patients who have been given too much of a MPA depo injection should contact a healthcare professional, hospital emergency department, or local poison control immediately.L8696

Medroxyprogesterone acetate

DB00603

small molecule approved investigational

Deskripsi

Medroxyprogesterone acetate (MPA) is a progesterone derivative that is more resistant to metabolism for improved pharmacokinetic properties.A14848 MPA can be use to treat secondary amenorrhea, endometrial hyperplasia, abnormal uterine bleeding, osteoporosis, vasomotor symptoms in menopause, vulvar and vaginal atrophy, prevent pregnancy, manage pain in endometriosis, prevent pregnancy, and is also used in palliative care for endometrial and renal carcinoma.L8657,L8660,L8663,L8666,L8669

Medroxyprogesterone acetate was granted FDA approval on 18 June 1959.L8657

Struktur Molekul 2D

Berat 386.5244
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Oral medroxyprogesterone acetate (MPA) has an absorption half life of 15-30min and a biological half life of 40-60 hours.[A186086] Intramuscular MPA has an absorption half life of 0.86±0.30 days and an elimination half life of 24.03±21.74 days.[A186095] Subcutaneous MPA has an absorption half life of 1.05±0.56 days and an elimination half life of 30.90±15.11 days.[A186095]
Volume Distribusi The volume of distribution of medroxyprogesterone acetate is 20±3L.[L8696]
Klirens (Clearance) The mean clearance of medroxyprogesterone acetate (MPA) is 1668±146L/day or 21.9±4.3L/kg/day.[A186113] Due to the high inter patient variability in MPA pharmacokinetics, clearance has been reported to be 1600-4000L/day.[L8696]

Absorpsi

Absorption of oral medroxyprogesterone acetate (MPA) varies considerably between formulations.A186086 A 1000mg oral dose reaches an average Cmax of 145-315nmol/L while a 500mg oral dose reaches an average Cmax of 33-178nmol/L with a Tmax of 1-3 hours and a lag time of half an hour.A186086 The AUC of a 500mg oral dose of MPA was 543.4-1981.1nmol\*L/h depending on formulation.A186086 Intramuscular MPA reaches a Cmax of 4.69±1.52nmol/L with a Tmax of 4.75±2.09 days and an AUC of 81.58±27.64days\*nmol/L.A186095 Subcutaneous MPA reaches a Cmax of 3.83±1.56nmol/L with a T±max of 6.52±2.07 days and an AUC of 72.26±38.73days\*nmol/L.A186095 However, the pharmacokinetics of MPA may also vary depending on injection site.A186098

Metabolisme

Medroxyprogesterone acetate undergoes beta hydroxylation to form the metabolites 6-beta (M-2), 2-beta (M-4), and 1-beta-hydroxymedroxyprogesterone acetate (M-3).A14848 M-2 and M-4 are further metabolized to 2-beta,6-beta-dihydroxymedroxyprogesterone (M-1).A14848 M-3 is further metabolized to 1,2-dehydromedroxyprogesterone acetate (M-5).A14848

Rute Eliminasi

The majority of medroxyprogesterone acetate (MPA) is eliminated in the urine as glucuronide conjugates and a minority of sulphate conjugates.L8657,L8660,L8663,L8666 Glucuronide conjugates are also detected in the feces.L8696 Determining the exact ratio of metabolites and parent compound eliminated in the urine and feces is difficult as the metabolite profile in the urine is not significantly differentA186137 and radio labelling studies are not readily available.L8657,L8660,L8663,L8666,L8669

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. St. John's Wort may decrease the effectiveness of medroxyprogesterone acetate.
  • 2. Take with food. Food increases the bioavailability of medroxyprogesterone acetate.

Interaksi Obat

1496 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Medroxyprogesterone acetate.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Medroxyprogesterone acetate.
Acitretin The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Acitretin.
Aprepitant The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Aprepitant.
Atazanavir The serum concentration of Medroxyprogesterone acetate can be increased when it is combined with Atazanavir.
Boceprevir The serum concentration of Medroxyprogesterone acetate can be increased when it is combined with Boceprevir.
Prucalopride The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Prucalopride.
Sugammadex The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Sugammadex.
Thalidomide Medroxyprogesterone acetate may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Ulipristal.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Medroxyprogesterone acetate.
Perampanel The metabolism of Perampanel can be increased when combined with Medroxyprogesterone acetate.
Warfarin The metabolism of Warfarin can be increased when combined with Medroxyprogesterone acetate.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Medroxyprogesterone acetate.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Medroxyprogesterone acetate.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Medroxyprogesterone acetate.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Medroxyprogesterone acetate.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Medroxyprogesterone acetate.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Medroxyprogesterone acetate.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Medroxyprogesterone acetate.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Medroxyprogesterone acetate.
cis-Diamminechlorocholylglycinateplatinum(II) The therapeutic efficacy of cis-Diamminechlorocholylglycinateplatinum(II) can be decreased when used in combination with Medroxyprogesterone acetate.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Medroxyprogesterone acetate.
Aramchol The therapeutic efficacy of Aramchol can be decreased when used in combination with Medroxyprogesterone acetate.
Ox bile extract The therapeutic efficacy of Ox bile extract can be decreased when used in combination with Medroxyprogesterone acetate.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Medroxyprogesterone acetate.
Tranexamic acid Medroxyprogesterone acetate may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Clobazam.
Colestipol Colestipol can cause a decrease in the absorption of Medroxyprogesterone acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Medroxyprogesterone acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Medroxyprogesterone acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Medroxyprogesterone acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Griseofulvin The metabolism of Medroxyprogesterone acetate can be increased when combined with Griseofulvin.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Medroxyprogesterone acetate.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Medroxyprogesterone acetate.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Medroxyprogesterone acetate.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Medroxyprogesterone acetate.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Medroxyprogesterone acetate.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Medroxyprogesterone acetate.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Medroxyprogesterone acetate.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Medroxyprogesterone acetate.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Medroxyprogesterone acetate.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Medroxyprogesterone acetate.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Medroxyprogesterone acetate.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Medroxyprogesterone acetate.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Medroxyprogesterone acetate.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Medroxyprogesterone acetate.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Medroxyprogesterone acetate.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Medroxyprogesterone acetate.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Medroxyprogesterone acetate.
Hydrocortisone acetate The serum concentration of Hydrocortisone acetate can be increased when it is combined with Medroxyprogesterone acetate.
Hydrocortisone succinate The serum concentration of Hydrocortisone succinate can be increased when it is combined with Medroxyprogesterone acetate.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Medroxyprogesterone acetate.
Prednisolone hemisuccinate The serum concentration of Prednisolone hemisuccinate can be increased when it is combined with Medroxyprogesterone acetate.
Methylprednisolone hemisuccinate The serum concentration of Methylprednisolone hemisuccinate can be increased when it is combined with Medroxyprogesterone acetate.
Prednisone acetate The serum concentration of Prednisone acetate can be increased when it is combined with Medroxyprogesterone acetate.
Clocortolone acetate The serum concentration of Clocortolone acetate can be increased when it is combined with Medroxyprogesterone acetate.
Melengestrol acetate The serum concentration of Melengestrol acetate can be increased when it is combined with Medroxyprogesterone acetate.
Betamethasone phosphate The serum concentration of Betamethasone phosphate can be increased when it is combined with Medroxyprogesterone acetate.
Cortisone The serum concentration of Cortisone can be increased when it is combined with Medroxyprogesterone acetate.
Budesonide The serum concentration of Budesonide can be increased when it is combined with Medroxyprogesterone acetate.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Medroxyprogesterone acetate.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Medroxyprogesterone acetate.
Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Medroxyprogesterone acetate.
Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Medroxyprogesterone acetate.
Fluticasone The serum concentration of Fluticasone can be increased when it is combined with Medroxyprogesterone acetate.
Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Medroxyprogesterone acetate.
Fludrocortisone The serum concentration of Fludrocortisone can be increased when it is combined with Medroxyprogesterone acetate.
Trilostane The serum concentration of Trilostane can be increased when it is combined with Medroxyprogesterone acetate.
Paramethasone The serum concentration of Paramethasone can be increased when it is combined with Medroxyprogesterone acetate.
Ciclesonide The serum concentration of Ciclesonide can be increased when it is combined with Medroxyprogesterone acetate.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Medroxyprogesterone acetate.
Fluprednisolone The serum concentration of Fluprednisolone can be increased when it is combined with Medroxyprogesterone acetate.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Medroxyprogesterone acetate.
Melengestrol The serum concentration of Melengestrol can be increased when it is combined with Medroxyprogesterone acetate.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Medroxyprogesterone acetate.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Medroxyprogesterone acetate.
Mometasone furoate The serum concentration of Mometasone furoate can be increased when it is combined with Medroxyprogesterone acetate.
Hydrocortisone cypionate The serum concentration of Hydrocortisone cypionate can be increased when it is combined with Medroxyprogesterone acetate.
Clobetasol propionate The serum concentration of Clobetasol propionate can be increased when it is combined with Medroxyprogesterone acetate.
Fluocinonide The serum concentration of Fluocinonide can be increased when it is combined with Medroxyprogesterone acetate.
Hydrocortisone butyrate The serum concentration of Hydrocortisone butyrate can be increased when it is combined with Medroxyprogesterone acetate.
Desoximetasone The serum concentration of Desoximetasone can be increased when it is combined with Medroxyprogesterone acetate.
Mometasone The serum concentration of Mometasone can be increased when it is combined with Medroxyprogesterone acetate.
Fluocortolone The serum concentration of Fluocortolone can be increased when it is combined with Medroxyprogesterone acetate.
Prednisolone acetate The serum concentration of Prednisolone acetate can be increased when it is combined with Medroxyprogesterone acetate.
Fluorometholone The serum concentration of Fluorometholone can be increased when it is combined with Medroxyprogesterone acetate.
Difluocortolone The serum concentration of Difluocortolone can be increased when it is combined with Medroxyprogesterone acetate.
Flumethasone The serum concentration of Flumethasone can be increased when it is combined with Medroxyprogesterone acetate.
Methylprednisolone aceponate The serum concentration of Methylprednisolone aceponate can be increased when it is combined with Medroxyprogesterone acetate.
Vitamin A The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Vitamin A.
Bexarotene The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Bexarotene.

Target Protein

Progesterone receptor PGR
Estrogen receptor ESR1
ATP-dependent translocase ABCB1 ABCB1
GABA(A) Receptor GABRA1

Referensi & Sumber

Synthesis reference: Klaus ANNEN, Thomas Linz, Karl-Heinz Neff, Rolf Bohlmann, Henry Laurent, "PROCESS FOR PREPARING 17ALPHA-ACETOXY-6-METHYLENEPREGN-4-ENE-3,20-DIONE, MEDROXYPROGESTERONE ACETATE AND MEGESTROL ACETATE." U.S. Patent US20090012321, issued January 08, 2009.
Artikel (PubMed)
  • PMID: 6457935
    Akpoviroro JO, Mangalam M, Jenkins N, Fotherby K: Binding of the contraceptive steroids medroxyprogesterone acetate and ethynyloestradiol in blood of various species. J Steroid Biochem. 1981 May;14(5):493-8. doi: 10.1016/0022-4731(81)90362-9.
  • PMID: 2943134
    Johansson ED, Johansen PB, Rasmussen SN: Medroxyprogesterone acetate pharmacokinetics following oral high-dose administration in humans: a bioavailability evaluation of a new MPA tablet formulation. Acta Pharmacol Toxicol (Copenh). 1986 May;58(5):311-7. doi: 10.1111/j.1600-0773.1986.tb00115.x.
  • PMID: 22078184
    Sierra-Ramirez JA, Lara-Ricalde R, Lujan M, Velazquez-Ramirez N, Godinez-Victoria M, Hernadez-Munguia IA, Padilla A, Garza-Flores J: Comparative pharmacokinetics and pharmacodynamics after subcutaneous and intramuscular administration of medroxyprogesterone acetate (25 mg) and estradiol cypionate (5 mg). Contraception. 2011 Dec;84(6):565-70. doi: 10.1016/j.contraception.2011.03.014. Epub 2011 May 11.
  • PMID: 23993431
    Halpern V, Combes SL, Dorflinger LJ, Weiner DH, Archer DF: Pharmacokinetics of subcutaneous depot medroxyprogesterone acetate injected in the upper arm. Contraception. 2014 Jan;89(1):31-5. doi: 10.1016/j.contraception.2013.07.002. Epub 2013 Jul 12.
  • PMID: 429526
    Gupta C, Osterman J, Santen R, Bardin CW: In vivo metabolism of progestins. V. The effect of protocol design on the estimated metabolic clearance rate and volume of distribution of medroxyprogesterone acetate in women. J Clin Endocrinol Metab. 1979 May;48(5):816-20. doi: 10.1210/jcem-48-5-816.
  • PMID: 11600316
    Altinoz MA, Bilir A, Ozar E, Onar FD, Sav A: Medroxyprogesterone acetate alone or synergistic with chemotherapy suppresses colony formation and DNA synthesis in C6 glioma in vitro. Int J Dev Neurosci. 2001 Oct;19(6):541-7. doi: 10.1016/s0736-5748(01)00045-4.
  • PMID: 3156203
    Yovich JL, Willcox DL, Wilkinson SP, Poletti VM, Hahnel R: Medroxyprogesterone acetate does not perturb the profile of steroid metabolites in urine during pregnancy. J Endocrinol. 1985 Mar;104(3):453-9. doi: 10.1677/joe.0.1040453.
  • PMID: 21562760
    Braden BB, Garcia AN, Mennenga SE, Prokai L, Villa SR, Acosta JI, Lefort N, Simard AR, Bimonte-Nelson HA: Cognitive-impairing effects of medroxyprogesterone acetate in the rat: independent and interactive effects across time. Psychopharmacology (Berl). 2011 Nov;218(2):405-18. doi: 10.1007/s00213-011-2322-4. Epub 2011 May 12.
Menampilkan 8 dari 9 artikel.

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