Contraceptives, Oral

Compounds, usually hormonal, taken orally in order to block ovulation and prevent the occurrence of pregnancy. The hormones are generally estrogen or progesterone or both.
DrugDrug NameDrug Indication
DB00304DesogestrelOral desogestrel is used in combination with [ethinylestradiol] as a contraceptive agent for the prevention of pregnancy.[FDA label] Desogestrel is part of the combined oral contraceptives that contain a mix of estrogen and progestin which inhibit ovulation.[L5698]
DB00351Megestrol acetateFor the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
DB00367LevonorgestrelFor the treatment of menopausal and postmenopausal disorders and alone or in combination with other hormones as an oral contraceptive.
DB00603Medroxyprogesterone acetateUsed 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.
DB00717NorethisteroneFor the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer.
DB00823Ethynodiol diacetateFor the prevention of pregnancy in women who elect to use this product as a method of contraception.
DB00834MifepristoneFor the medical termination of intrauterine pregnancy through 49 days' pregnancy. Also indicated to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous Cushing's syndrome who have type 2 diabetes mellitus or glucose intolerance and are not candidates for surgery or have had unsuccessful surgery.
DB00957NorgestimateFor the prevention of pregnancy
DB06730GestodeneNot Available
DB09123DienogestIndicated for use as the treatment of endometriosis alone and as a contraceptive in combination with ethinylestradiol.
DB09371NorethynodrelNot Available
DB09389NorgestrelNorgestrel in combination with ethinyl estradiol is indicated for the prevention of pregnancy in women who elect to use this product as a method of contraception.
DB11619GestrinoneEndometriosis with or without accompanying sterility. Treatment is limited to a single course of 6 months duration per lifetime [L1699, L1700].
DB12474LynestrenolNot Available
DB13528ChlormadinoneNot Available
DB13563NorgestrienoneNot Available
DB13310OrmeloxifeneNot Available
DB04839Cyproterone acetateFor the palliative treatment of patients with advanced prostatic carcinoma.
DB01395DrospirenoneFor the prevention of pregnancy in women who elect an oral contraceptive.
DB13981Nomegestrol acetateNot Available
DB13685QuingestanolNot Available
DB00977EthinylestradiolFor treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
DB00783EstradiolEstradiol is indicated for the treatment of moderate to severe vasomotor symptoms and vulvar and vaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, and for the prevention of post-menopausal osteoarthritis. It is also used for the treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease, and for the treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).
DB13857DemegestoneNot Available
DB14678Norethindrone enanthateNot Available
DrugDrug NameTargetType
DB00304DesogestrelProgesterone receptortarget
DB00304DesogestrelEstrogen receptor alphatarget
DB00304DesogestrelCytochrome P450 3A4enzyme
DB00304DesogestrelSerum albumincarrier
DB00304DesogestrelSex hormone-binding globulincarrier
DB00304DesogestrelCytochrome P450 2C9enzyme
DB00304DesogestrelUDP-glucuronosyltransferase 1-1enzyme
DB00351Megestrol acetateProgesterone receptortarget
DB00351Megestrol acetateGlucocorticoid receptortarget
DB00351Megestrol acetateMultidrug resistance protein 1transporter
DB00351Megestrol acetateCytochrome P450 3A4enzyme
DB00367LevonorgestrelProgesterone receptortarget
DB00367LevonorgestrelEstrogen receptor alphatarget
DB00367Levonorgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB00367LevonorgestrelCytochrome P450 3A4enzyme
DB00367LevonorgestrelCytochrome P450 19A1enzyme
DB00367LevonorgestrelAndrogen receptortarget
DB00367LevonorgestrelSex hormone-binding globulintarget
DB00603Medroxyprogesterone acetateProgesterone receptortarget
DB00603Medroxyprogesterone acetateEstrogen receptor alphatarget
DB00603Medroxyprogesterone acetateCytochrome P450 3A4enzyme
DB00603Medroxyprogesterone acetateCytochrome P450 2C8enzyme
DB00603Medroxyprogesterone acetate3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2enzyme
DB00603Medroxyprogesterone acetateCytochrome P450 2C9enzyme
DB00717NorethisteroneProgesterone receptortarget
DB00717NorethisteroneCytochrome P450 3A4enzyme
DB00717NorethisteroneMultidrug resistance protein 1transporter
DB00717NorethisteroneCytochrome P450 2C19enzyme
DB00717NorethisteroneCytochrome P450 3A5enzyme
DB00717NorethisteroneCytochrome P450 3A7enzyme
DB00717NorethisteroneSerum albumincarrier
DB00717NorethisteroneSex hormone-binding globulincarrier
DB00823Ethynodiol diacetateEstrogen receptor alphatarget
DB00823Ethynodiol diacetateProgesterone receptortarget
DB00823Ethynodiol diacetateCytochrome P450 3A4enzyme
DB00834MifepristoneProgesterone receptortarget
DB00834MifepristoneGlucocorticoid receptortarget
DB00834MifepristoneCytochrome P450 3A4enzyme
DB00834MifepristoneCytochrome P450 3A5enzyme
DB00834MifepristoneCytochrome P450 3A7enzyme
DB00834MifepristoneMultidrug resistance protein 1transporter
DB00834MifepristoneMultidrug resistance-associated protein 1transporter
DB00834MifepristoneCytochrome P450 2D6enzyme
DB00834MifepristoneProstate-specific antigentarget
DB00834MifepristoneNuclear receptor subfamily 1 group I member 2target
DB00834MifepristoneBile salt export pumptransporter
DB00834MifepristoneCytochrome P450 2C8enzyme
DB00834MifepristoneCytochrome P450 2C9enzyme
DB00834MifepristoneSolute carrier organic anion transporter family member 1B1transporter
DB00834MifepristoneSolute carrier organic anion transporter family member 1B3transporter
DB00957NorgestimateProgesterone receptortarget
DB00957NorgestimateEstrogen receptor alphatarget
DB00957NorgestimateCanalicular multispecific organic anion transporter 1transporter
DB00957NorgestimateCytochrome P450 3A4enzyme
DB00957NorgestimateAndrogen receptortarget
DB06730GestodeneCytochrome P450 3A5enzyme
DB06730GestodeneCytochrome P450 3A7enzyme
DB06730GestodeneProgesterone receptortarget
DB06730GestodeneCytochrome P450 3A4enzyme
DB09123DienogestCytochrome P450 3A4enzyme
DB09123DienogestProgesterone receptortarget
DB09123DienogestAndrogen receptortarget
DB09371NorethynodrelEstrogen receptor alphatarget
DB09371NorethynodrelAndrogen receptortarget
DB09371NorethynodrelSex hormone-binding globulintarget
DB09371NorethynodrelCytochrome P450 3A4enzyme
DB09389NorgestrelProgesterone receptortarget
DB09389Norgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB09389NorgestrelAndrogen receptortarget
DB09389NorgestrelCytochrome P450 3A4enzyme
DB09389NorgestrelCytochrome P450 19A1enzyme
DB11619GestrinoneSex hormone-binding globulintarget
DB11619GestrinoneProgesterone receptortarget
DB11619GestrinoneGlucocorticoid receptortarget
DB11619GestrinoneAndrogen receptortarget
DB11619GestrinoneGonadotropin-releasing hormone receptortarget
DB11619GestrinoneEstrogen receptor alphatarget
DB11619GestrinoneCytochrome P450 3A4enzyme
DB12474LynestrenolCytochrome P450 3A4enzyme
DB12474LynestrenolCytochrome P450 2C9enzyme
DB12474LynestrenolCytochrome P450 2C19enzyme
DB13528ChlormadinoneCytochrome P450 3A4enzyme
DB04839Cyproterone acetateAndrogen receptortarget
DB04839Cyproterone acetateCytochrome P450 19A1enzyme
DB04839Cyproterone acetateProstate-specific antigentarget
DB04839Cyproterone acetateCytochrome P450 3A4enzyme
DB01395DrospirenoneProgesterone receptortarget
DB01395DrospirenoneMineralocorticoid receptortarget
DB01395DrospirenoneAndrogen receptortarget
DB01395DrospirenoneProstaglandin G/H synthase 2enzyme
DB01395DrospirenoneCholinesteraseenzyme
DB01395DrospirenoneCytochrome P450 3A4enzyme
DB13981Nomegestrol acetateCytochrome P450 3A4enzyme
DB13685QuingestanolCytochrome P450 3A4enzyme
DB00977EthinylestradiolEstrogen receptor alphatarget
DB00977EthinylestradiolNuclear receptor subfamily 1 group I member 2target
DB00977EthinylestradiolCytochrome P450 3A4enzyme
DB00977EthinylestradiolCytochrome P450 2C8enzyme
DB00977EthinylestradiolBile salt export pumptransporter
DB00977EthinylestradiolSodium/bile acid cotransportertransporter
DB00977EthinylestradiolCanalicular multispecific organic anion transporter 1transporter
DB00977EthinylestradiolMultidrug resistance protein 1transporter
DB00977EthinylestradiolSex hormone-binding globulintarget
DB00977EthinylestradiolUDP-glucuronosyltransferase 1-1enzyme
DB00783EstradiolEstrogen receptor alphatarget
DB00783EstradiolNuclear receptor subfamily 1 group I member 2target
DB00783EstradiolSex hormone-binding globulincarrier
DB00783EstradiolEstrogen receptor betatarget
DB00783EstradiolCytochrome P450 1A2enzyme
DB00783EstradiolUDP-glucuronosyltransferase 1-1enzyme
DB00783EstradiolSerum albumincarrier
DB00783EstradiolFatty acid-binding protein, intestinalcarrier
DB00783EstradiolCytochrome P450 3A4enzyme
DB00783EstradiolCytochrome P450 3A5enzyme
DB00783EstradiolCytochrome P450 3A7enzyme
DB00783EstradiolSolute carrier family 22 member 2transporter
DB00783EstradiolSolute carrier family 22 member 1transporter
DB00783EstradiolSolute carrier family 22 member 3transporter
DB00783EstradiolSolute carrier organic anion transporter family member 2B1transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1A2transporter
DB00783EstradiolMultidrug resistance-associated protein 7transporter
DB00783EstradiolSolute carrier family 22 member 11transporter
DB00783EstradiolATP-binding cassette sub-family G member 2transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1B1transporter
DB00783EstradiolMultidrug resistance protein 1transporter
DB00783EstradiolCytochrome P450 1A1enzyme
DB00783EstradiolCytochrome P450 1B1enzyme
DB00783EstradiolCytochrome P450 2C19enzyme
DB00783EstradiolCytochrome P450 2C8enzyme
DB00783EstradiolCytochrome P450 2C9enzyme
DB00783EstradiolSolute carrier family 22 member 8transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1B3transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1C1transporter
DB00783EstradiolSolute carrier organic anion transporter family member 4A1transporter
DB00783EstradiolNeuronal acetylcholine receptor subunit alpha-4target
DB00783EstradiolNuclear receptor coactivator 2target
DB00783EstradiolG-protein coupled estrogen receptor 1target
DB00783EstradiolATP synthase subunit atarget
DB00783EstradiolBeclin-1target
DB00783EstradiolEstradiol 17-beta-dehydrogenase 2target
DB00783EstradiolEstrogen-related receptor gammatarget
DB13857DemegestoneProgesterone receptortarget
DB13857DemegestoneCytochrome P450 3A4enzyme