Tìm theo
Medroxyprogesterone Acetate
Các tên gọi khác (18 ) :
  • (6alpha)-17-(Acetyloxy)-6-methylpreg-4-ene-3,20-dione
  • 17-Acetoxy-6alpha-methylprogesterone
  • 17-Acetoxy-6α-methylprogesterone
  • 17alpha-Hydroxy-6alpha-methylprogesterone acetate
  • 17α-hydroxy-6α-methylprogesterone acetate
  • 6-alpha-Methyl-17-alpha-acetoxyprogesterone
  • 6-alpha-Methyl-17-alpha-hydroxyprogesterone acetate
  • 6alpha-Methyl-17-acetoxy progesterone
  • 6alpha-Methyl-17alpha-hydroxyprogesterone acetate
  • 6alpha-Methyl-4-pregnene-3,20-dion-17alpha-ol acetate
  • 6α-Methyl-17-acetoxy progesterone
  • 6α-Methyl-17α-hydroxyprogesterone acetate
  • Medroxyacetate progesterone
  • Medroxyprogesterone 17-acetate
  • Medroxyprogesterone acetate
  • Methylacetoxyprogesterone
  • Metigestrona
  • MPA
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 71-58-9
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C24H34O4
PTK: 386.5244
Medroxyprogesterone acetate (INN, USAN, BAN), also known as 17α-hydroxy-6α-methylprogesterone acetate, and commonly abbreviated as MPA, is a steroidal progestin, a synthetic variant of the human hormone progesterone. It is used as a contraceptive, in hormone replacement therapy and for the treatment of endometriosis as well as several other indications. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate, what is normally being administered is MPA and not MP. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H34O4
Phân tử khối
386.5244
Monoisotopic mass
386.245709576
InChI
InChI=1S/C24H34O4/c1-14-12-18-19(22(4)9-6-17(27)13-21(14)22)7-10-23(5)20(18)8-11-24(23,15(2)25)28-16(3)26/h13-14,18-20H,6-12H2,1-5H3/t14-,18+,19-,20-,22+,23-,24-/m0/s1
InChI Key
InChIKey=PSGAAPLEWMOORI-PEINSRQWSA-N
IUPAC Name
(1S,2R,8S,10R,11S,14R,15S)-14-acetyl-2,8,15-trimethyl-5-oxotetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-en-14-yl acetate
Traditional IUPAC Name
provera
SMILES
[H][C@@]12CC[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])C[C@H](C)C2=CC(=O)CC[C@]12C
Độ tan chảy
214.5 °C
Độ hòa tan
22.2mg/L
logP
3.5
logS
-5.2
pKa (strongest acidic)
17.82
pKa (Strongest Basic)
-4.9
PSA
60.44 Å2
Refractivity
107.81 m3·mol-1
Polarizability
44.05 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Medroxyprogesterone acetate is a synthetic progestin more potent than progesterone.
Cơ Chế Tác Dụng : Medroxyprogesterone acetate (INN, USAN, BAN), also known as 17α-hydroxy-6α-methylprogesterone acetate, and commonly abbreviated as MPA, is a steroidal progestin, a synthetic variant of the human hormone progesterone. It is used as a contraceptive, in hormone replacement therapy and for the treatment of endometriosis as well as several other indications. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate, what is normally being administered is MPA and not MP. [Wikipedia] Progestins diffuse freely into target cells in the female reproductive tract, mammary gland, hypothalamus, and the pituitary and bind to the progesterone receptor. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from GI tract
▧ Protein binding :
90%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Following oral dosing, MPA is extensively metabolized in the liver via hydroxylation, with subsequent conjugation and elimination in the urine. Most MPA metabolites are excreted in the urine as glucuronide conjugates with only minor amounts excreted as sulfates.
▧ Half Life :
50 days
▧ Clearance :
* 64110 +/- 42662 mL/min [postmenopausal women under fasting conditions with a single Dose of 2 × 10 mg] * 74123 +/- 35126 mL/min [postmenopausal women under fasting conditions with a single Dose of 8 × 2.5 mg] * 41963 +/- 38402 mL/min [postmenopausal women following daily administration of one PROVERA 10 mg tablet for 7 days]
Độc Tính : Side effects include loss of bone mineral density, BMD changes in adult women, bleeding irregularities, cancer risks, and thromboembolic disorders.
Chỉ Định : Used as a contraceptive and to treat secondary amenorrhea, abnormal uterine bleeding, pain associated with endometriosis, endometrial and renal cell carcinomas, paraphilia in males, GnRH-dependent forms of precocious puberty, as well as to prevent endometrial changes associated with estrogens.
Tương Tác Thuốc :
  • Acenocoumarol Medroxyprogesterone may increase the anticoagulant effect of acenocoumarol.
  • Amobarbital The enzyme inducer, amobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Anisindione Medroxyprogesterone may increase the anticoagulant effect of anisindione.
  • Aprobarbital The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Artemether Artemether may decrease the effectiveness of medroxyprogesterone by increasing its metabolism via CYP3A4. Consider an alternate non-hormonal means of contraception during artemether therapy.
  • Bexarotene Bexarotene may decrease the serum concentration of Contraceptives (Progestins). Since bexarotene is teratogenic and can lower serum concentrations of medroxyprogesterone, it is advised that women of childbearing potential use two forms of contraception (including at least one non-hormonal form).
  • Bosentan Bosentan may decrease the contraceptive effect of medroxyprogesterone. Hormonal contraception should not be relied on alone during concomitant therapy with bosentan.
  • Butabarbital The enzyme inducer, butabarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Butalbital The enzyme inducer, butalbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Butethal The enzyme inducer, butethal, decreases the effect of the hormone agent, medroxyprogesterone.
  • Colesevelam Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Progestins). Administer oral progestin-containing contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider alternatives in order to avoid this combination when possible, due to the risk for impaired contraceptive effectiveness.
  • Dicoumarol Medroxyprogesterone may increase the anticoagulant effect of dicumarol.
  • Ethotoin The enzyme inducer, ethotoin, decreases the effect of the hormone agent, medroxyprogesterone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the hormone, medroxyprogesterone.
  • Griseofulvin The enzyme inducer, griseofulvin, may decrease the effect of the hormone, medroxyprogesterone.
  • Heptabarbital The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Hexobarbital The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Mephenytoin The enzyme inducer, mephenytoin, decreases the effect of the hormone agent, medroxyprogesterone.
  • Methohexital The enzyme inducer, methohexital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Methylphenobarbital The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Phenobarbital The enzyme inducer, phenobarbital, may decrease the effect of the hormone, medroxyprogesterone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of medroxyprogesterone.
  • Primidone The enzyme inducer, primidone, may decrease the effect of the hormone, medroxyprogesterone.
  • Secobarbital The enzyme inducer, secobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Talbutal The enzyme inducer, talbutal, decreases the effect of the hormone agent, medroxyprogesterone.
  • Thiopental Thiopental may decrease the effect of Medroxyprogesterone. Contraceptive failure may occur. Alternative nonhomomonal contraception should be used during concomitant therapy.
  • Warfarin Medroxyprogesterone may alter the anticoagulant effect of warfarin. Concomitant therapy should be avoided. Monitor for changes in coagulation status if medroxyprogesterone is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Suspension - Intramuscular
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Depo-provera
  • Công ty :
    Sản phẩm biệt dược : Depo-subq provera 104
  • Công ty :
    Sản phẩm biệt dược : Makena
  • Công ty :
    Sản phẩm biệt dược : Provera
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00603
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08150
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00951
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0009-0064-06
PharmGKB
http://www.pharmgkb.org/drug/PA450344
Wikipedia
http://en.wikipedia.org/wiki/Medroxyprogesterone
RxList
http://www.rxlist.com/cgi/generic/medrox.htm
Drugs.com
http://www.drugs.com/medroxyprogesterone.html
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