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| Related FDA Approved Drug |
±âÁØ ¼ººÐ: ESTRADIOL HEMIHYDRATEESTRASORB (ESTRADIOL HEMIHYDRATE)
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µå·°ÀÎÆ÷ ÀǾàǰ ¿ä¾à/»ó¼¼Á¤º¸
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M088710/¿¡½ºÆ®¶óµð¿Ã1/2¼öȹ° 1.0325¹Ð¸®±×·¥ /
M088710/¿¡½ºÆ®¶óµð¿Ã1/2¼öȹ° 2.065¹Ð¸®±×·¥ /
M040057/ÃÊ»ê³ë¸£¿¡Ä¡½ºÅ×·Ð 1¹Ð¸®±×·¥ /
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8806439013404 |
| BIT ¾àÈ¿ºÐ·ù |
¿©¼ºÈ£¸£¸óÁ¦ (Estrogens & progesterones and related drugs)
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| ATC ÄÚµå |
Norethisterone and estrogen / G03FB05
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247 (³Æ÷È£¸£¸ó ¹× Ȳüȣ¸£¸óÁ¦ )
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±¸¹ÙÄÚµå: 8806038101021/ºñ°í:-
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ÀüüÀӽŠ±â°£º°·Î ¿©·¯µî±ÞÀÌ Á¸ÀçÇÒ ¼ö ÀÖÀ¸¸ç °¡Àå À§Çèµµ°¡ ³ôÀº Á¤º¸¸¸ º¸¿©Áý´Ï´Ù. ´Ü, º¹ÇÕÁ¦ÀÇ °æ¿ì ¸ðµç º¹ÇÕÁ¦¼ººÐ¿¡ ´ëÇÑ ÀÓºÎÅõ¿©µî±ÞÀÌ Ç¥½ÃµÈ°ÍÀº Àý´ë ¾Æ´Ï¸ç Ç¥½ÃµÈ°ÍÁß¿¡ °¡Àå À§Çèµµ°¡ ³ôÀº Á¤º¸¸¸ ³ªÅ¸³³´Ï´Ù.
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(estradiol )
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»ó±â ÀÓºÎÅõ¿©¿¡ ´ëÇÑ Á¤º¸´Â Àü»êó¸® µÇ¸é¼ ÀÔ·Â ¿À·ù °¡´É¼ºÀÌ Á¸ÀçÇÕ´Ï´Ù. ¿À·ù °¡´É¼ºÀ» ÃÖ¼ÒÈÇϱâ À§ÇÏ¿© ¸¹Àº ³ë·ÂÀ» ±â¿ïÀ̰í ÀÖÀ¸³ª, ±× Á¤È®¼º¿¡ ´ëÇÏ¿© È®½ÅÀ» µå¸± ¼ö ¾ø½À´Ï´Ù. ÀÌ¿¡ ´ëÇØ ȸ»ç´Â Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù.
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À¯·áÁ¤º¸ÀÔ´Ï´Ù.
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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|
| µ¶¼ºÁ¤º¸ |
Estradiol¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Estradiol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
|
| Pharmacology |
Estradiol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.
|
| Metabolism |
Estradiol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2A6 (CYP2A6)Glucuronosyltransferase
|
| Protein Binding |
Estradiol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ >95%
|
| Half-life |
Estradiol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 36 hours
|
| Absorption |
Estradiol¿¡ ´ëÇÑ Absorption Á¤º¸ 43%
|
| Pharmacokinetics |
Estradiol hemihydrateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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| Biotransformation |
Estradiol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.
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| Toxicity |
Estradiol¿¡ ´ëÇÑ Toxicity Á¤º¸ Can cause nausea and vomiting, and withdrawal bleeding may occur in females.
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| Drug Interactions |
Estradiol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital The enzyme inducer decreases the effect of hormonesAprobarbital The enzyme inducer decreases the effect of hormonesButabarbital The enzyme inducer decreases the effect of hormonesButalbital The enzyme inducer decreases the effect of hormonesButethal The enzyme inducer decreases the effect of hormonesEthotoin The enzyme inducer decreases the effect of hormonesFosphenytoin The enzyme inducer decreases the effect of hormonesGriseofulvin The enzyme inducer decreases the effect of hormonesHeptabarbital The enzyme inducer decreases the effect of hormonesHexobarbital The enzyme inducer decreases the effect of hormonesMephenytoin The enzyme inducer decreases the effect of hormonesMethohexital The enzyme inducer decreases the effect of hormonesMethylphenobarbital The enzyme inducer decreases the effect of hormonesPentobarbital The enzyme inducer decreases the effect of hormonesPhenobarbital The enzyme inducer decreases the effect of hormonesPhenytoin The enzyme inducer decreases the effect of hormonesPrednisolone The estrogenic agent increases the effect of corticosteroidPrednisone The estrogenic agent increases the effect of corticosteroidPrimidone The enzyme inducer decreases the effect of hormonesSecobarbital The enzyme inducer decreases the effect of hormonesTalbutal The enzyme inducer decreases the effect of hormonesRaloxifene Association not recommendedUrsodeoxycholic acid Estrogens decreases the effect of ursodiol
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Estradiol¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food to decrease nausea.
|
| Drug Target |
[Drug Target]
|
| Description |
Estradiol¿¡ ´ëÇÑ Description Á¤º¸ Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]
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| Drug Category |
Estradiol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-menopausal AgentsAnticholesteremic AgentsEstrogens
|
| Smiles String Canonical |
Estradiol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC12CCC3C(CCC4=C3C=CC(O)=C4)C1CCC2O
Estradiol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC12CCC3C(CCC4=C3C=CC(O)=C4)C1CCC2O
Estradiol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC12CCC3C(CCC4=C3C=CC(O)=C4)C1CCC2O
|
| Smiles String Isomeric |
Estradiol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@]12CC[C@H]3[C@@H](CCC4=C3C=CC(O)=C4)[C@@H]1CC[C@@H]2O
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| InChI Identifier |
Estradiol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1
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| Chemical IUPAC Name |
Estradiol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (8R,9S,13S,14S,17S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
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| Drug-Induced Toxicity Related Proteins |
ESTRADIOL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Myc proto-oncogene protein Drug:estradiol Toxicity:cytotoxic responses . [¹Ù·Î°¡±â] Replated Protein:3-hydroxy-3-methylglutaryl-coenzyme A reductase Drug:estradiol Toxicity:stimulate steroidogenesis. [¹Ù·Î°¡±â] Replated Protein:Stromelysin-2 Drug:estradiol Toxicity:nonbacterial prostatitis. [¹Ù·Î°¡±â] Replated Protein:Transcription factor E2F1 Drug:estradiol Toxicity:cytotoxic responses. [¹Ù·Î°¡±â] Replated Protein:Glucocorticoid receptor Drug:estradiol Toxicity:glucocorticoid resistance. [¹Ù·Î°¡±â]
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. ESTRADIOL[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.5[SGOT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 2.8[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 2.1[LDH Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.2[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.3
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