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| Related FDA Approved Drug |
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µå·°ÀÎÆ÷ ÀǾàǰ ¿ä¾à/»ó¼¼Á¤º¸
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°æ±¸ÇÇÀÓÁ¦ (Oral Contraceptives)
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Levonorgestrel and ethinylestradiol / G03AA07
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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.
Levonorgestrel¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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 levonorgestrel 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.
Levonorgestrel¿¡ ´ëÇÑ Pharmacology Á¤º¸ Levonorgestrel 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. Levonorgestrel 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
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| Protein Binding |
Estradiol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ >95%
Levonorgestrel¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 55%
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| Half-life |
Estradiol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 36 hours
Levonorgestrel¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available
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| Absorption |
Estradiol¿¡ ´ëÇÑ Absorption Á¤º¸ 43%
Levonorgestrel¿¡ ´ëÇÑ Absorption Á¤º¸ Levonorgestrel is not subjected to a "first-pass" effect and is virtually 100% bioavailable.
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| Pharmacokinetics |
Ethinyl EstradiolÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : À§Àå°üÀ¸·ÎºÎÅÍ ½Å¼ÓÇÏ°í °ÅÀÇ ¿ÏÀüÈ÷ Èí¼öµÈ´Ù.
- »ýü³»ÀÌ¿ë·ü : ¾à 50%
- ºÐÆ÷ : ü³» Á¶Á÷¿¡ ½Å¼ÓÇÏ°Ô ºÐÆ÷ÇÑ´Ù.
- ´Ü¹é°áÇÕ : 95% ÀÌ»ó
- ´ë»ç : °£¿¡¼ ºÒȰ¼ºÈµÈ´Ù.
- ¹Ý°¨±â : ¾à 8½Ã°£ (¹üÀ§ : 5-16 ½Ã°£)
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : ´ë°³ 1½Ã°£ À̳»
- ¼Ò½Ç : ¾à 60%´Â ´¢¸¦ ÅëÇØ, 40%´Â ´ëº¯À» ÅëÇØ ¹è¼³µÈ´Ù.
LevonorgestrelÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Levonorgestrel Çdz» ÀÌ½Ä :
- ´Ü¹é°áÇÕ : ¼ºÈ£¸£¸ó °áÇÕ ±Û·ÎºÒ¸° (SHBG), ¾ËºÎ¹Î ¹× ¥á1-glycoprotein¿¡ °áÇÕÇÑ´Ù.
- ´ë»ç : °£´ë»ç
- ¹Ý°¨±â : 11-45 ½Ã°£
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : ÀÌ½Ä ÈÄ 24½Ã°£ À̳»
- ¼Ò½Ç : ÁÖ·Î Æ÷ÇÕü·Î¼ ½Å¹è¼³µÈ´Ù.
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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.
Levonorgestrel¿¡ ´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.
Levonorgestrel¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50>5000 mg/kg (orally in rats)
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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
Levonorgestrel¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital Phenobarbital decreases the effect of levonorgestrelAprobarbital Phenobarbital decreases the effect of levonorgestrelButabarbital Phenobarbital decreases the effect of levonorgestrelButalbital Phenobarbital decreases the effect of levonorgestrelButethal Phenobarbital decreases the effect of levonorgestrelCarbamazepine Carbamazepine decreases the contraceptive effectDihydroquinidine barbiturate Phenobarbital decreases the effect of levonorgestrelHeptabarbital Phenobarbital decreases the effect of levonorgestrelHexobarbital Phenobarbital decreases the effect of levonorgestrelMethohexital Phenobarbital decreases the effect of levonorgestrelMethylphenobarbital Phenobarbital decreases the effect of levonorgestrelPentobarbital Phenobarbital decreases the effect of levonorgestrelPhenobarbital Phenobarbital decreases the effect of levonorgestrelPrimidone Phenobarbital decreases the effect of levonorgestrelQuinidine barbiturate Phenobarbital decreases the effect of levonorgestrelSecobarbital Phenobarbital decreases the effect of levonorgestrelTalbutal Phenobarbital decreases the effect of levonorgestrelPhenytoin Phenytoin decreases the contraceptive effectMephenytoin Phenytoin decreases the contraceptive effectFosphenytoin Phenytoin decreases the contraceptive effectEthotoin Phenytoin decreases the contraceptive effect
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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.
Levonorgestrel¿¡ ´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]
Levonorgestrel¿¡ ´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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| Dosage Form |
Estradiol¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Disc TransdermalGel TransdermalLiquid IntramuscularPatch TransdermalRing IntravaginalTablet IntravaginalTablet Oral
Levonorgestrel¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Insert, extended release IntrauterineTablet Oral
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| Drug Category |
Estradiol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-menopausal AgentsAnticholesteremic AgentsEstrogens
Levonorgestrel¿¡ ´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
Levonorgestrel¿¡ ´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
Levonorgestrel¿¡ ´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
Levonorgestrel¿¡ ´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
Levonorgestrel¿¡ ´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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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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