Combination Contraceptives (with Estrogen and derivatives)

Progestin contraceptives used in combination with estrogen derivatives, usually with Ethinyl Estradiol. Other estrogens include Estradiol derivatives such as estradiol cypionate, estradiol valerate, estradiol undecylate, and estradiol benzoate.
DrugDrug NameDrug Indication
DB04839Cyproterone acetateFor the palliative treatment of patients with advanced prostatic carcinoma.
DB06789Hydroxyprogesterone caproateHydroxyprogesterone caproate is indicated for the prevention of spontaneous preterm births in singleton pregnancies in women who have previously had a spontaneous preterm birth. (1)
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.
DB09123DienogestIndicated for use as the treatment of endometriosis alone and as a contraceptive in combination with ethinylestradiol.
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.
DB06730GestodeneNot Available
DB12474LynestrenolNot Available
DB06713NorelgestrominNorelgestromin is used for contraception and menopausal hormonal therapy. Norelgestromin may potentially be used in breast cancer treatment due to its inhibitory effect on estrone sulfatase . They convert sulfated steroid precursors to estrogen during pregnancy.
DB00957NorgestimateFor the prevention of pregnancy
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.
DB13528ChlormadinoneNot Available
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]
DB01395DrospirenoneDrospirenone, in combination with ethinyl estradiol, is indicated as an oral contraceptive for the prevention of pregnancy. In addition to its use for contraceptive effects, this combination is used to treat moderate acne vulgaris and the symptoms of premenstrual dysphoric disorder.[L7973,L7976] The drug has approved indications for combination with estrogens for the treatment of menopause-associated symptoms, such as vasomotor symptoms and vulvovaginal atrophy. Drospirenone combined with estrogen may also may aid in the prevention of osteoporosis in women who have been post-menopausal for at least a year and are not candidates for other therapies.[L7997,L8075] It can sometimes be found in preparations containing estrogen and folic acid for folic acid replenishment during oral contraception.[L8078] When used for the treatment of acne vulgaris, drospirenone-containing contraceptives should only be used in women ≥14 years of age who have experienced menarche, desire oral contraception, and do not have any contraindications to oral contraceptives.[L7976] Off-label uses for this drug include the treatment of menstrual irregularities, dysmenorrhea, hirsutism, and endometriosis.[A2439,A182576]
DB00823Ethynodiol diacetateFor the prevention of pregnancy in women who elect to use this product as a method of contraception.
DB00367Levonorgestrel**Emergency contraception** Levonorgestrel, in the single-agent emergency contraceptive form, is indicated for the prevention of pregnancy after the confirmed or suspected failure of contraception methods or following unprotected intercourse. It is distributed by prescription for patients under 17, and over the counter for those above this age.[L7760] This levonorgestrel-only form of contraception is not indicated for regular contraception and must be taken as soon as possible within 72 hours after intercourse.[A181976,L7760] It has shown a lower efficacy when it is used off label within 96 hours.[T659] **Long-term contraception or nonemergency contraception** In addition to the above indication in emergency contraception, levonorgestrel is combined with other contraceptives in contraceptive formulations designed for regular use, for example with ethinyl estradiol.[L7766] It is used in various hormone-releasing intrauterine devices for long-term contraception ranging for a duration of 3-5 years.[L7778,L7781,L7787] Product labeling for Mirena specifically mentions that it is recommended in women who have had at least 1 child.[L7778] A subdermal implant is also available for the prevention of pregnancy for up to 5 years.[L7823] **Hormone therapy and off-label uses** Levonorgestrel is prescribed in combination with estradiol as hormone therapy during menopause to manage vasomotor symptoms and to prevent osteoporosis.[L7805]Off-label, levonorgestrel may be used to treat menorrhagia, endometrial hyperplasia, and endometriosis.[T659]
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.
DB13981Nomegestrol acetateNot Available
DB13685QuingestanolNot Available
DB00294EtonogestrelEtonogestrel is administered in subdermal implants as long-acting reversible contraception. It is known to be effective in postpartum insertion including breastfeeding women.[A175990] Etonogestrel is part of the long-acting contraceptive implants that prevent pregnancy. The implant's effect can remain for 5 years.[L5698]
DB09371NorethynodrelNot Available
DB13563NorgestrienoneNot Available
DrugDrug NameTargetType
DB04839Cyproterone acetateAndrogen receptortarget
DB04839Cyproterone acetateProstate-specific antigentarget
DB04839Cyproterone acetateCytochrome P450 3A4enzyme
DB04839Cyproterone acetateCytochrome P450 19A1enzyme
DB06789Hydroxyprogesterone caproateProgesterone receptortarget
DB06789Hydroxyprogesterone caproateCytochrome P450 3A4enzyme
DB06789Hydroxyprogesterone caproateCytochrome P450 3A5enzyme
DB06789Hydroxyprogesterone caproateCytochrome P450 2C19enzyme
DB00717NorethisteroneProgesterone receptortarget
DB00717NorethisteroneMultidrug resistance protein 1transporter
DB00717NorethisteroneCytochrome P450 2C19enzyme
DB00717NorethisteroneSerum albumincarrier
DB00717NorethisteroneSex hormone-binding globulincarrier
DB00717NorethisteroneCYP3Aenzyme
DB09123DienogestCytochrome P450 3A4enzyme
DB09123DienogestProgesterone receptortarget
DB09123DienogestAndrogen receptortarget
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
DB06730GestodeneCytochrome P450 3A5enzyme
DB06730GestodeneCytochrome P450 3A7enzyme
DB06730GestodeneProgesterone receptortarget
DB06730GestodeneCytochrome P450 3A4enzyme
DB06730GestodeneCytochrome P450 2C19enzyme
DB12474LynestrenolCytochrome P450 3A4enzyme
DB12474LynestrenolCytochrome P450 2C9enzyme
DB12474LynestrenolCytochrome P450 2C19enzyme
DB06713NorelgestrominSteryl-sulfataseenzyme
DB06713NorelgestrominProgesterone receptortarget
DB06713NorelgestrominSerum albumintarget
DB06713NorelgestrominAndrogen receptortarget
DB06713NorelgestrominCytochrome P450 3A4enzyme
DB00957NorgestimateProgesterone receptortarget
DB00957NorgestimateEstrogen receptor alphatarget
DB00957NorgestimateCanalicular multispecific organic anion transporter 1transporter
DB00957NorgestimateCytochrome P450 3A4enzyme
DB00957NorgestimateAndrogen receptortarget
DB09389NorgestrelProgesterone receptortarget
DB09389Norgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB09389NorgestrelAndrogen receptortarget
DB09389NorgestrelCytochrome P450 3A4enzyme
DB09389NorgestrelCytochrome P450 19A1enzyme
DB13528ChlormadinoneCytochrome P450 3A4enzyme
DB00304DesogestrelProgesterone receptortarget
DB00304DesogestrelEstrogen receptor alphatarget
DB00304DesogestrelCytochrome P450 3A4enzyme
DB00304DesogestrelSerum albumincarrier
DB00304DesogestrelSex hormone-binding globulincarrier
DB00304DesogestrelCytochrome P450 2C9enzyme
DB00304DesogestrelUDP-glucuronosyltransferase 1-1enzyme
DB01395DrospirenoneProgesterone receptortarget
DB01395DrospirenoneMineralocorticoid receptortarget
DB01395DrospirenoneAndrogen receptortarget
DB01395DrospirenoneProstaglandin G/H synthase 2enzyme
DB01395DrospirenoneSerum paraoxonase/arylesterase 1enzyme
DB01395DrospirenoneGlucocorticoid receptortarget
DB01395DrospirenoneCytochrome P450 3A4enzyme
DB00823Ethynodiol diacetateEstrogen receptor alphatarget
DB00823Ethynodiol diacetateProgesterone receptortarget
DB00823Ethynodiol diacetateCytochrome P450 3A4enzyme
DB00367LevonorgestrelProgesterone receptortarget
DB00367LevonorgestrelEstrogen receptor alphatarget
DB00367Levonorgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB00367LevonorgestrelCytochrome P450 3A4enzyme
DB00367LevonorgestrelAndrogen receptortarget
DB00367LevonorgestrelSex hormone-binding globulintarget
DB00367LevonorgestrelGlucocorticoid receptortarget
DB00367LevonorgestrelCytochrome P450 3A5enzyme
DB00351Megestrol acetateProgesterone receptortarget
DB00351Megestrol acetateGlucocorticoid receptortarget
DB00351Megestrol acetateMultidrug resistance protein 1transporter
DB00351Megestrol acetateCytochrome P450 3A4enzyme
DB13981Nomegestrol acetateCytochrome P450 3A4enzyme
DB13685QuingestanolCytochrome P450 3A4enzyme
DB00294EtonogestrelEstrogen receptor alphatarget
DB00294EtonogestrelProgesterone receptortarget
DB00294EtonogestrelCytochrome P450 3A4enzyme
DB00294EtonogestrelSerum albumincarrier
DB00294EtonogestrelSex hormone-binding globulincarrier
DB09371NorethynodrelEstrogen receptor alphatarget
DB09371NorethynodrelAndrogen receptortarget
DB09371NorethynodrelSex hormone-binding globulintarget
DB09371NorethynodrelCytochrome P450 3A4enzyme