Peringatan Keamanan

Intraperitoneal LD50 (rat): 327 mg/kg MSDS.

Use in pregnancy

Only forms of progesterone that are indicated on product labeling for pregnancy should be used. Some forms of progesterone should not be used in pregnancy FDA label, F3904. Refer to individual product monographs for information regarding use in pregnancy. Many studies have found no effects on fetal development associated with long-term use of contraceptive doses of oral progestins. Studies of infant growth and development that have been conducted have not demonstrated significant adverse effects, however, these studies are few in number. It is therefore advisable to rule out suspected pregnancy before starting any hormonal contraceptive F3904.

Effects on fertility

Progesterone at high doses is an antifertility drug and high doses would be expected to impair fertility until cessation F3916. The progesterone contraceptive should not be used during pregnancy.

Carcinogenicity

Progesterone has been shown to induce or promote the formation of ovarian, uterine, mammary, and genital tract tumors in animals. The clinical relevance of these findings is unknown F3913. Certain epidemiological studies of patients using oral contraceptives have reported an increased relative risk of developing breast cancer, especially at a younger age and associated with a longer duration of use. These studies have mainly involved combined oral contraceptives, and therefore, it is unknown whether this risk is attributable to progestins, estrogens, or a combination of both. At this time, there is insufficient data to determine whether the use of progestin-only contraceptives increases the risk in a similar way to combined contraceptives. A meta-analysis of 54 studies showed a small increase in the frequency of breast cancer diagnosis for women who were currently using combined oral contraceptives, or had used them within the past 10 years. There was no increase in the frequency of having breast cancer diagnosed ten or more years after cessation of hormone use. Women with breast cancer should not use oral contraceptives, as there is no sufficient data to fully establish or negate the risk of cancer with hormonal contraceptive use F3904.

Use in breastfeeding

Progesterone has been detected in the milk of nursing mothers F3901, F3904. No adverse effects, in general, have been found on breastfeeding ability or on the health, growth, or development of the growing infant. Despite this, isolated post-marketing cases of decreased milk production have been reported F3904.

Progesterone

DB00396

small molecule approved vet_approved

Deskripsi

Progesterone is a hormone that occurs naturally in females, and is essential for endometrial receptivity, embryo implantation, and the successful establishment of pregnancy. A low progesterone concentration or an insufficient response to progesterone can cause infertility and pregnancy loss A175609. Progesterone is used in various contraceptive preparations to prevent ovulation and fertilization T481, A175612 as well as in other formulations to promote and support pregnancy. Please see Medroxyprogesterone acetate, Megestrol acetate, Dydrogesterone and Hydroxyprogesterone entries for information on various other forms of progesterone.

Pharmaceutical progesterone is made from a plant source as a starting material and is chemically identical to progesterone of human ovarian origin FDA label. Progesterone is available in gelatinized capsule form, vaginal gel form, tablet form, vaginal insert form, and injection form, all used for various purposes Label,F3898,F3904,F3901,F3907.

Struktur Molekul 2D

Berat 314.4617
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Absorption half-life is approximately 25-50 hours and an elimination half-life of 5-20 minutes (progesterone gel) [F3898]. Progesterone, administered orally, has a short serum half-life (approximately 5 minutes). It is rapidly metabolized to _17-hydroxyprogesterone_ during its first pass through the liver [A175657].
Volume Distribusi When administered vaginally, progesterone is well absorbed by uterine endometrial tissue, and a small percentage is distributed into the systemic circulation. The amount of progesterone in the systemic circulation appears to be of minimal importance, especially when implantation, pregnancy, and live birth outcomes appear similar for intramuscular and vaginal administration of progesterone [A175657].
Klirens (Clearance) **Apparent clearance** 1367 ± 348 (50mg of progesterone administered by vaginal insert once daily) [A175657]. 106 ± 15 L/h (50mg/mL IM injection once daily) [A175657].

Absorpsi

Oral micronized capsules Following oral administration of progesterone in the micronized soft-gelatin capsule formulation, peak serum concentration was achieved in the first 3 hours. The absolute bioavailability of micronized progesterone is unknown at this time. In postmenopausal women, serum progesterone concentration increased in a dose-proportional and linear fashion after multiple doses of progesterone capsules, ranging from 100 mg/day to 300 mg/day FDA label. IM administration After intramuscular (IM) administration of 10 mg of progesterone in oil, the maximum plasma concentrations were achieved in about 8 hours post-injection and plasma concentrations stayed above baseline for approximately 24 hours post-injection. Injections of 10, 25, and 50 mg lead to geometric mean values for maximum plasma concentration (CMAX) of 7, 28, and 50 ng/mL, respectively F3916. Progesterone administered by the intramuscular (IM) route avoids significant first-pass hepatic metabolism. As a result, endometrial tissue concentrations of progesterone achieved with IM administration are higher when compared with oral administration. Despite this, the highest concentrations of progesterone in endometrial tissue are reached with vaginal administration A175657. Note on oral contraceptive tablet absorption Serum progestin levels peak about 2 hours after oral administration of progesterone-only contraceptive tablets, followed by rapid distribution and elimination. By 24 hours after drug administration, serum levels remain near the baseline, making efficacy dependent upon strict adherence to the dosing schedule. Large variations in serum progesterone levels occur among individuals. Progestin-only administration leads to lower steady-state serum progestin levels and a shorter elimination half-life than concurrent administration with estrogens F3904.

Metabolisme

Progesterone is mainly metabolized by the liver. After oral administration, the major plasma metabolites found are 20 a hydroxy-?4 a-prenolone and 5 a-dihydroprogesterone. Some progesterone metabolites are found excreted in the bile and these metabolites may be deconjugated and subsequently metabolized in the gut by reduction, dehydroxylation, and epimerization FDA label. The major plasma and urinary metabolites are comparable to those found during the physiological progesterone secretion of the corpus luteum F3913.

Rute Eliminasi

Progesterone metabolites are excreted mainly by the kidneys. Urinary elimination is observed for 95% of patients in the form of glycuroconjugated metabolites, primarily 3 a, 5 ß–pregnanediol (pregnandiol) F3913. The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the urine and bile. Progesterone metabolites, excreted in the bile, may undergo enterohepatic recycling or may be found excreted in the feces.

Interaksi Makanan

5 Data
  • 1. Administer vitamin supplements.
  • 2. Avoid alcohol.
  • 3. Limit caffeine intake.
  • 4. Take at the same time every day.
  • 5. Take with food.

Interaksi Obat

1182 Data
Glycochenodeoxycholic Acid Progesterone may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Pravastatin Progesterone may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Diethylstilbestrol Progesterone may decrease the excretion rate of Diethylstilbestrol which could result in a higher serum level.
Isradipine Progesterone may decrease the excretion rate of Isradipine which could result in a higher serum level.
Flucloxacillin Progesterone may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Indomethacin Progesterone may decrease the excretion rate of Indomethacin which could result in a higher serum level.
Atenolol Progesterone may decrease the excretion rate of Atenolol which could result in a higher serum level.
Rosiglitazone Progesterone may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Cerivastatin Progesterone may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Loratadine Progesterone may decrease the excretion rate of Loratadine which could result in a higher serum level.
Atropine Progesterone may decrease the excretion rate of Atropine which could result in a higher serum level.
Diclofenac Progesterone may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Losartan The metabolism of Losartan can be decreased when combined with Progesterone.
Fluorescein Progesterone may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Progesterone may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Naproxen Progesterone may decrease the excretion rate of Naproxen which could result in a higher serum level.
Disulfiram Progesterone may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Cefaclor Progesterone may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Tinidazole Progesterone may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Repaglinide Progesterone may decrease the excretion rate of Repaglinide which could result in a higher serum level.
Telmisartan Progesterone may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ezetimibe Progesterone may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Sulfamethoxazole Progesterone may decrease the excretion rate of Sulfamethoxazole which could result in a higher serum level.
Fenofibrate Progesterone may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Nitrendipine Progesterone may decrease the excretion rate of Nitrendipine which could result in a higher serum level.
Rosuvastatin Progesterone may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Nifedipine Progesterone may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Sulfinpyrazone Progesterone may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Ofloxacin Progesterone may decrease the excretion rate of Ofloxacin which could result in a higher serum level.
Taurocholic acid Progesterone may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Prasterone sulfate Progesterone may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Indocyanine green acid form Progesterone may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Progesterone may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide Progesterone may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Dihydroergocristine Progesterone may decrease the excretion rate of Dihydroergocristine which could result in a higher serum level.
Glycyrrhizic acid Progesterone may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Atorvastatin Progesterone may decrease the excretion rate of Atorvastatin which could result in a higher serum level.
Belantamab mafodotin Progesterone may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Progesterone.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Progesterone.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Progesterone.
Dabrafenib The serum concentration of Progesterone can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Progesterone can be increased when it is combined with Luliconazole.
Exenatide Exenatide can cause a decrease in the absorption of Progesterone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Thalidomide Progesterone may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Progesterone can be decreased when used in combination with Ulipristal.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Progesterone.
Perampanel The metabolism of Perampanel can be increased when combined with Progesterone.
Warfarin The metabolism of Warfarin can be increased when combined with Progesterone.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Progesterone.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Progesterone.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Progesterone.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Progesterone.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Progesterone.
Mirabegron The serum concentration of Progesterone can be increased when it is combined with Mirabegron.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Progesterone.
Lumacaftor The serum concentration of Progesterone can be decreased when it is combined with Lumacaftor.
Tranexamic acid Progesterone may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Progesterone can be decreased when it is combined with Clobazam.
Griseofulvin The metabolism of Progesterone can be increased when combined with Griseofulvin.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Progesterone.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Progesterone.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Progesterone.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Progesterone.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Progesterone.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Progesterone.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Progesterone.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Progesterone.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Progesterone.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Progesterone.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Progesterone.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Progesterone.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Progesterone.
Hydrocortisone acetate The serum concentration of Hydrocortisone acetate can be increased when it is combined with Progesterone.
Hydrocortisone succinate The serum concentration of Hydrocortisone succinate can be increased when it is combined with Progesterone.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Progesterone.
Prednisolone hemisuccinate The serum concentration of Prednisolone hemisuccinate can be increased when it is combined with Progesterone.
Methylprednisolone hemisuccinate The serum concentration of Methylprednisolone hemisuccinate can be increased when it is combined with Progesterone.
Prednisone acetate The serum concentration of Prednisone acetate can be increased when it is combined with Progesterone.
Clocortolone acetate The serum concentration of Clocortolone acetate can be increased when it is combined with Progesterone.
Melengestrol acetate The serum concentration of Melengestrol acetate can be increased when it is combined with Progesterone.
Betamethasone phosphate The serum concentration of Betamethasone phosphate can be increased when it is combined with Progesterone.
Cortisone The serum concentration of Cortisone can be increased when it is combined with Progesterone.
Budesonide The serum concentration of Budesonide can be increased when it is combined with Progesterone.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Progesterone.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Progesterone.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Progesterone.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Progesterone.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Progesterone.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Progesterone.
Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Progesterone.
Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Progesterone.
Fluticasone The serum concentration of Fluticasone can be increased when it is combined with Progesterone.
Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Progesterone.
Paramethasone The serum concentration of Paramethasone can be increased when it is combined with Progesterone.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Progesterone.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Progesterone.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Progesterone.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Progesterone.
Mometasone furoate The serum concentration of Mometasone furoate can be increased when it is combined with Progesterone.

Target Protein

Progesterone receptor PGR
Mineralocorticoid receptor NR3C2
Estrogen receptor ESR1
Steroid 17-alpha-hydroxylase/17,20 lyase CYP17A1
Kappa-type opioid receptor OPRK1
Alpha-1-acid glycoprotein 1 ORM1
Glucocorticoid receptor NR3C1
Androgen receptor AR
Sex hormone-binding globulin SHBG
Estrogen receptor beta ESR2

Referensi & Sumber

Synthesis reference: Nejib M. Nasraoui, Alain Piasco, "Derivatives of 19-nor progesterone; process for producing them and the pharmaceutical compositions incorporating them." U.S. Patent US5223492, issued May, 1971.
Artikel (PubMed)
  • PMID: 17747122
    Allen WM: THE ISOLATION OF CRYSTALLINE PROGESTIN. Science. 1935 Aug 2;82(2118):89-93.
  • PMID: 4922128
    Allen WM: Progesterone: how did the name originate? South Med J. 1970 Oct;63(10):1151-5.
  • PMID: 15135772
    Schumacher M, Guennoun R, Robert F, Carelli C, Gago N, Ghoumari A, Gonzalez Deniselle MC, Gonzalez SL, Ibanez C, Labombarda F, Coirini H, Baulieu EE, De Nicola AF: Local synthesis and dual actions of progesterone in the nervous system: neuroprotection and myelination. Growth Horm IGF Res. 2004 Jun;14 Suppl A:S18-33.
  • PMID: 3184927
    Hould FS, Fried GM, Fazekas AG, Tremblay S, Mersereau WA: Progesterone receptors regulate gallbladder motility. J Surg Res. 1988 Dec;45(6):505-12.
  • PMID: 10584066
    Payne VA, Chang YT, Loew GH: Homology modeling and substrate binding study of human CYP2C18 and CYP2C19 enzymes. Proteins. 1999 Nov 1;37(2):204-17.
  • PMID: 9328296
    Yamazaki H, Shimada T: Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9. doi: 10.1006/abbi.1997.0302.
  • PMID: 20104424
    Young SL, Lessey BA: Progesterone function in human endometrium: clinical perspectives. Semin Reprod Med. 2010 Jan;28(1):5-16. doi: 10.1055/s-0029-1242988. Epub 2010 Jan 26.
  • PMID: 27567593
    Lopez LM, Ramesh S, Chen M, Edelman A, Otterness C, Trussell J, Helmerhorst FM: Progestin-only contraceptives: effects on weight. Cochrane Database Syst Rev. 2016 Aug 28;(8):CD008815. doi: 10.1002/14651858.CD008815.pub4.
Menampilkan 8 dari 14 artikel.
Textbook
  • Danielle B. Cooper; Rotimi Adigun (2018). Oral contraceptives. StatPearls Publishing.
  • Dhanalakshmi K. Thiyagarajan; Rebecca Jeanmonod (2019). Physiology, Menstrual Cycle. StatPearls publishing.

Contoh Produk & Brand

Produk: 180 • International brands: 12
Produk
  • Ach-progesterone
    Capsule • 100 mg • Oral • Canada • Generic • Approved
  • Act Progesterone Injection
    Solution • 50 mg / mL • Intramuscular • Canada • Approved
  • Advanced Formula Progesto-Life
    Cream • 16.9 mg/1mL • Topical • US • OTC
  • Auro-progesterone
    Capsule • 100 mg • Oral • Canada • Generic • Approved
  • Bijuva
    Capsule • - • Oral • US • Approved
  • Bijuva
    Capsule • - • Oral • Canada • Approved
  • Bijuva
    Capsule • - • Oral • Canada • Approved
  • Bijuva
    Capsule • - • Oral • US • Approved
Menampilkan 8 dari 180 produk.
International Brands
  • Agolutin — Biotika
  • Cyclogest — Actavis
  • Gesterol
  • Gestone — Nordic Pharma
  • Progestasert
  • Progestogel — Besins
  • Qi Ning — Aisheng Pharmaceutical
  • Relantan — Aversi
  • Susten — Sun Pharma
  • Utrogestran — Faran Laboratories

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