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PTP |
8806411006608 |
8806411006615 |
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297900ATB
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Estradiol valerate
Brand Names/Synonyms
- Aerodiol
- Agofollin
- Alora
- Altrad
- Amnestrogen
- Aquadiol
- Bardiol
- Beta-Estradiol
- Cis-Estradiol
- Cis-Oestradiol
- Climaderm
- Climara
- Combipatch
- Compudose
- Compudose 200
- Compudose 365
- Corpagen
- D-Estradiol
- D-Oestradiol
- Delestrogen
- Depo-Estradiol
- Dermestril
- Dihydrofollicular Hormone
- Dihydrofolliculin
- Dihydromenformon
- Dihydrotheelin
- Dihydroxyesterin
- Dihydroxyestrin
- Dihydroxyoestrin
- Dimenformon
- Dimenformon Prolongatum
- Diogyn
- Diogynets
- Divigel
- Encore
- Esclim
- Estinyl
- Estrace
- Estraderm
- Estraderm Tts
- Estradiol Cypionate
- Estradiol Valerate
- Estradiol-17beta
- Estradurin
- Estraldine
- Estrasorb
- Estreva
- Estrifam
- Estring
- Estring Vaginal Ring
- Estroclim
- Estroclim 50
- Estrofem 2
- Estrofem Forte
- Estrogel
- Estrogens, Esterified
- Estrol
- Estrovite
- Evex
- Evorel
- Extrasorb
- Femestral
- Femestrol
- Feminone
- Femogen
- Fempatch
- Femring
- Femtrace
- Femtran
- Follicyclin
- Ginedisc
- Ginosedol
- Gynergon
- Gynestrel
- Gynodiol
- Gynoestryl
- Gynpolar
- Innofem
- Lamdiol
- Lynoral
- Macrodiol
- Macrol
- Menest
- Menorest
- Menostar
- Microdiol
- Nordicol
- Oestergon
- Oestradiol
- Oestradiol R
- Oestrogel
- Oestroglandol
- Oestrogynal
- Ovahormon
- Ovasterol
- Ovastevol
- Ovociclina
- Ovocyclin
- Ovocycline
- Ovocylin
- Perlatanol
- Primofol
- Profoliol
- Profoliol B
- Progynon
- Progynon Dh
- Progynon-Dh
- Ricifon
- Ritsifon
- Sandrena Gel
- Sisare Gel
- Sk-Estrogens
- Soldep
- Sotipox
- Syndiol
- Systen
- Theelin, Dihydro-
- Tradelia
- Trial Sat
- Trocosone
- Vagifem
- Vivelle
- Zerella
- Zumenon
Brand Name Mixtures
- Alesse 21 Tablets (Ethinyl Estradiol + Levonorgestrel)
- Alesse 28 Tablets (Ethinyl Estradiol + Levonorgestrel)
- Brevicon 0.5/35 21 Tab (Ethinyl Estradiol + Norethindrone)
- Brevicon 0.5/35 28 Tab (Ethinyl Estradiol + Norethindrone)
- Brevicon 1/35 21 Tab (Ethinyl Estradiol + Norethindrone)
- Brevicon 1/35 28 Tab (Ethinyl Estradiol + Norethindrone)
- Calf-Oid Implant (Estradiol Benzoate + Progesterone)
- Climacteron Injection (Estradiol Benzoate + Estradiol Dienanthate + Testosterone Enanthate Benzilic Acid Hydrazone)
- Demulen 50 (21 Day Pack) (Ethinyl Estradiol + Ethynodiol Diacetate)
- Demulen 50 (28 Day Pack) (Ethinyl Estradiol + Ethynodiol Diacetate)
- Min-Ovral 21 Tab (Ethinyl Estradiol + Levonorgestrel)
- Min-Ovral 28 Tab (Ethinyl Estradiol + Levonorgestrel)
- Neo Mens Tab (Ethinyl Estradiol + Ethisterone)
- Ortho 10/11 Tablets (21 Day) (Ethinyl Estradiol + Norethindrone)
- Ortho 10/11 Tablets (28 Day) (Ethinyl Estradiol + Norethindrone)
- Ovral 21 Tab (Ethinyl Estradiol + Norgestrel (Norgestrel))
- Ovral 28tab (Ethinyl Estradiol + Norgestrel)
- Preven Tablets (Ethinyl Estradiol + Levonorgestrel)
- Synphasic 21 Tablets (Ethinyl Estradiol + Norethindrone)
- Synphasic-28 Tablets (Ethinyl Estradiol + Norethindrone)
- Tri-Cyclen Lo (Ethinyl Estradiol + Norgestimate)
- Triphasil 21 Tab (Ethinyl Estradiol + Levonorgestrel)
- Triphasil 28 Tab (Ethinyl Estradiol + Levonorgestrel)
- Triquilar 21 (Ethinyl Estradiol + Levonorgestrel)
Chemical IUPAC Name13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diolNorgestrel
Brand Names/Synonyms
- Alesse
- Alpha-Norgestrel
- Component of Lo/Ovral
- Component of Ovral
- D-Norgestrel
- DL-Norgestrel
- Follistrel
- Jadelle
- LD Norgestrel
- Ld Norgestrel [French]
- Levlen
- Levlen Ed
- Levonorgestrel
- Levonorgestrel Implants
- Levonorgestrel [Usan:Ban:Inn]
- Levonorgestrelum [Inn-Latin]
- Levonova
- Levora-21
- Levora-28
- Lo/Ovral
- Logynon
- Logynon Ed
- Methylnorethindrone
- Microgest Ed
- Microgyn
- Microgynon
- Microgynon 21
- Microgynon 28
- Microgynon 30 Ed
- Microgynon Cd
- Microlut
- Microlution
- Microval
- Minivlar 30
- Mirena
- Monofeme 28
- Monovar
- NOG
- Neogest
- Neogynon 21
- Nordet
- Nordette
- Nordette 21
- Nordette 28
- Norgeston
- Norgestrel [Progestins]
- Norgestrel [Usan:Ban:Inn:Jan]
- Norgestrelum [Inn-Latin]
- Norplant
- Norplant 2
- Norplant II
- Norplant System in Plastic Container
- Ovral
- Ovral-Lo
- Ovran
- Ovranette
- Ovrette
- Plan B
- Postinor
- Preven
- Rigevidon 21+7
- Stediril
- Stediril 30
- Tetragynon
- Tri-Levlen
- Tri-Levlen 21
- Triagynon
- Triciclor
- Trifeme 28
- Trigoa
- Trinordiol
- Trinordiol 21
- Trinordiol 28
- Triphasil
- Triphasil 21
- Triphasil 28
- Triquilar Ed
- Trivora
Brand Name Mixtures
- Lo-Femenal 21 Tablets (ethinyl estradiol + norgestrel)
- Ovral 21 Tablets (ethinyl estradiol + norgestrel)
- Ovral 28 Tablets (ethinyl estradiol + norgestrel)
Chemical IUPAC Name(8R,9S,10R,13S,14S,17S)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15, 16-dodecahydrocyclopenta[a]phenanthren-3-one
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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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.
Norgestrel¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Norgestrel binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Norgestrel will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge.
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| 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.
Norgestrel¿¡ ´ëÇÑ Pharmacology Á¤º¸ Norgestrel is used as a female contraceptive. Norgestrel is a progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Norgestrel tricks the body processes into thinking that ovulation has already occurred, by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries.
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| Metabolism |
Estradiol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2A6 (CYP2A6)Glucuronosyltransferase
Norgestrel¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2C19 (CYP2C19)
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| Protein Binding |
Estradiol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ >95%
Norgestrel¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Norgestrel-binding protein in the plasma appeared to be a protein different from human serum albumin, corticosteroid-binding globulin and sex-steroid-binding protein. High binding (>95%).
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| Half-life |
Estradiol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 36 hours
Norgestrel¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 5-14 hours
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| Absorption |
Estradiol¿¡ ´ëÇÑ Absorption Á¤º¸ 43%
Norgestrel¿¡ ´ëÇÑ Absorption Á¤º¸ 65%
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| Pharmacokinetics |
Estradiol valerateÀÇ 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.
Norgestrel¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
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| Toxicity |
Estradiol¿¡ ´ëÇÑ Toxicity Á¤º¸ Can cause nausea and vomiting, and withdrawal bleeding may occur in females.
Norgestrel¿¡ ´ëÇÑ Toxicity Á¤º¸ Nausea, vomiting, and drowsiness/fatigue; Withdrawal bleeding; LD50=mg/kg (orally in rat)
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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
Norgestrel¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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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.
Norgestrel¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food.Avoid excessive quantities of coffee or tea (Caffeine).Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.Take at the same time everyday.
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| Drug Target |
[Drug Target]
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| 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]
Norgestrel¿¡ ´ëÇÑ Description Á¤º¸ A synthetic progestational hormone with actions similar to those of progesterone and about twice as potent as its racemic or (+-)-isomer (norgestrel). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. [PubChem]
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| Drug Category |
Estradiol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-menopausal AgentsAnticholesteremic AgentsEstrogens
Norgestrel¿¡ ´ëÇÑ Drug_Category Á¤º¸ Contraceptive Agents, FemaleContraceptivesContraceptives, Oral, Synthetic
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| 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
Norgestrel¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCC12CCC3C(CCC4=CC(=O)CCC34)C1CCC2(O)C
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| 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
Norgestrel¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@H]34)[C@@H]1CC[C@@]2(O)C
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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
Norgestrel¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C21H28O2/c1-3-20-11-9-17-16-8-6-15(22)13-14(16)5-7-18(17)19(20)10-12-21(20,23)4-2/h2,13,16-19,23H,3,5-12H2,1H3/t16-,17+,18+,19-,20-,21-/m0/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
Norgestrel¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
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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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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´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) 0.3ESTRADIOL VALERATE[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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