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QuickView for Levonorgestrel (compound)


PubChem
Name: Levonorgestrel
PubChem Compound ID: 10335940
Description: 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.
Molecular formula: C21H28O2
Molecular weight: 316.462 g/mol
DrugBank
Identification
Name: Levonorgestrel
Name (isomeric): DB00367
Drug Type: small molecule
Description: 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.
Synonyms:
SOH-075; Levonorgestrelum [INN-Latin]
Brand: Tri-Levlen 21, Nordette 21, Levonelle, Trinordiol 21, Microgynon Cd, Ovral-Lo, Microgynon 30 Ed, Trinordiol 28, Norplant 2, Levora-28, Trifeme 28, Microgest Ed, Stediril 30, Malloside, Neogynon 21, Trigoa, Levora-21, Triciclor, Norplant II, Postinor-2, NorLevo, Logynon Ed, Ovrette, Microgynon 21, Triagynon, Nordette 28, Jadelle, Microlution, Minivlar 30, Microgynon 28, Levonova, Microval, Mirena, Nordet, Plan B, Follistrel, Levlen Ed, Monofeme 28, Rigevidon 21+7, Ovranette, Norplant, Levlen, Trivora, Tri-Levlen, 72-HOURS, Nordette, Microgyn
Brand name mixture:
Triquilar 21 Tab(Ethinyl Estradiol + Levonorgestrel), Triphasil 28 Tab(Ethinyl Estradiol + Levonorgestrel), Alesse 21 Tablets(Ethinyl Estradiol + Levonorgestrel), Alesse 28 Tablets(Ethinyl Estradiol + Levonorgestrel), Min-Ovral 21 Tab(Ethinyl Estradiol + Levonorgestrel), Min-Ovral 21(Ethinyl Estradiol + Levonorgestrel), Min-Ovral 28 Tab(Ethinyl ...
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Category: Contraceptive Agents, Female, Contraceptives, Oral, Synthetic, Contraceptives
CAS number: 797-63-7
Pharmacology
Indication: For the treatment of menopausal and postmenopausal disorders and alone or in combination with other hormones as an oral contraceptive.
Pharmacology:
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 ...
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Mechanism of Action:
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 (lut...
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Absorption: Levonorgestrel is not subjected to a "first-pass" effect and is virtually 100% bioavailable.
Protein binding: 55%
Biotransformation: Hepatic
Route of elimination: About 45% of levonorgestrel and its metabolites are excreted in the urine and about 32% are excreted in feces, mostly as glucuronide conjugates.
Clearance: 7.7 +/- 2.7 L/h [Healthy Female Volunteers under Fasting Conditions]
Toxicity: LD50>5000 mg/kg (orally in rats)
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
Avoid excessive quantities of coffee or tea (Caffeine).
Take with food.
Take at the same time everyday.
Drug interaction:
EthotoinPhenytoin decreases the contraceptive effect
TalbutalPhenobarbital decreases the effect of levonorgestrel
PhenytoinPhenytoin decreases the contraceptive effect
MethohexitalPhenobarbital decreases the effect of levonorgestrel
WarfarinLevonorgestrel may alter the anticoagulant effect of warfarin. Concomitant therapy should be avoided. Monitor for changes in coagulation status if levonorgestrel is initiated, discontinued or dose changed.
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Targets


Enzymes