| Drug type | Active ingredient | Examples | Major mechanism | Efficacy | Indications | Comments | ||
| Hirsutism | Menstrual irregularity | Insulin-lowering | ||||||
| First-line treatment for menstrual irregularity and hyperandrogenism: | ||||||||
| Oral contraceptive pills | Ethinyl estradiol 30 mcg + drospirenone | Yasmin Yaz | Suppress ovarian function | + | + | Menstrual irregularity, hirsutism | Contraindicated in patients with venous thrombosis, uncontrolled hypertension | |
| Ethinyl estradiol 35 mcg + norgestimate | Ortho Cyclen | |||||||
| Ethinyl estradiol 50 mcg + ethynodiol diacetate | Demulen 1/50 Zovia 1/50 | |||||||
| Progestin | Micronized progesterone | Prometrium | Normalizes endometrial cycle | + | Menstrual irregularity | Less efficacious than oral contraceptive pills | ||
| Medroxyprogesterone acetate | Provera | |||||||
| Other options occasionally used for selected patients: | ||||||||
| Cell cycle inhibitor | Eflornithine HCl 13.9 percent (topical) | Vaniqa | Irreversible inhibitor of ornithine decarboxylase | + | Focal hirsutism | Contraindicated in pregnancy and lactation | ||
| GnRH agonist* | Leuprolide acetate depot | Depot Lupron | Suppress gonadotropins | + | + | Oral contraceptive alternative | Contraindicated in patients with osteoporosis without add-back estrogen | |
| Glucocorticoid* | Glucocorticoid | Prednisone | Suppress adrenal androgen | + | + | Isolated functional adrenal hyperandrogenism | Poor efficacy. Contraindicated in obese or glucose-intolerant patients. | |
| For patients with hirsutism that is not controlled satisfactorily within six months by the above treatments: | ||||||||
| Antiandrogens | Spironolactone | Spironolactone Aldactone | Competitive inhibitor of androgen binding to the androgen receptor | + | ± | Severe hirsutism | Use only with appropriate contraception because of adverse effects on fetus. Contraindicated in kidney or liver failure. | |
| Cyproterone acetate* | Cyproterone acetate Androcur | Competitive inhibitor of androgen binding to the androgen receptor | + | ± | Severe hirsutism | Use only with appropriate contraception because of adverse effects on fetus | ||
| Flutamide* | Flutamide Apo-flutamide Euflex Eulexin | Nonsteroidal competitive inhibitor of androgen binding to the androgen receptor | + | ± | Severe hirsutism | Use only with appropriate contraception because of adverse effects on fetus. Monitor for liver failure. Contraindicated in liver disease. | ||
| Finasteride* | Proscar | Competitive 5α-reductase inhibitor | + | ± | Severe hirsutism | Use only with appropriate contraception because of adverse effects on fetus | ||
| For patients with obesity and marked insulin resistance: | ||||||||
| Biguanide | Metformin | Glucophage, Glucophage XR, Glumetza | Reduces hepatic glucose production | ± | ± | Obesity and insulin resistance; type 2 diabetes | Efficacy poor unless weight control is achieved | |
| Thiazolidinedione* | Pioglitazone | Actos | Peroxisome proliferator-activated receptor agonist | ± | + | Type 2 diabetes | Contraindicated in patients with hepatic or cardiac disease | |
