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. 2022 Jan 6;23(2):583. doi: 10.3390/ijms23020583

Table 1.

Commonly prescribed medications in PCOS.

Generic Name (Brand)/Ref Mechanism of Action Purpose of Therapy Common Side Effects Contraindications
COCs (estrogen and progestin)
Levonorgestrel/Ethinyl estradiol—LD and HD [100] Inhibition of ovulation via negative feedback on the hypothalamus
alters the regular pattern of gonadotropin secretion of FSH and LH from the anterior pituitary gland
Menstrual cyclicity, hirsutism, acne Nausea and vomiting (especially at first), breast tenderness, breakthrough bleeding, weight gain, acne or darkening of facial skin, etc. Oral contraceptives should not be used in women who currently have the following conditions:
  • Thrombophlebitis or thromboembolic disorders

  • A history of deep vein thrombophlebitis or thromboembolic disorders

  • Cerebral vascular or coronary artery disease

  • Known or suspected carcinoma of the breast

  • Carcinoma of the endometrium or other known or suspected estrogen-dependent neoplasia

  • Undiagnosed abnormal genital bleeding

  • Cholestatic jaundice of pregnancy or jaundice with prior pill use

  • Hepatic adenomas or carcinomas

  • Known or suspected pregnancy

Desogestrel/Ethinyl estradiol (Marvelon®, Mircette®) [101] Menstrual cyclicity Depression, headache, migraine, mood changes, skin rash, urticaria, decreased or increased libido, weight gain or loss, abdominal pain, diarrhea, nausea and vomiting, breast hypertrophy and tenderness, vaginal discharge, hypersensitivity reactions, etc.
Cyproterone acetate/Ethinyl estradiol (Diane 35®) [102] Menstrual cyclicity Dysmenorrhea, breast tenderness, change in libido, headache, depression, nervousness, chloasma, varicosity, edema, dizziness
Drospirenone/Ethinyl estradiol (Yasmin®) [103] Menstrual cyclicity, hirsutism, acne PMS, headache or migraine, breast pain/tenderness/discomfort, nausea and vomiting, abdominal pain/tenderness/discomfort, mood changes
Drospirenone/Ethinyl estradiol (Yaz®) [104] Menstrual cyclicity, hirsutism, acne Headache or migraine, menstrual irregularities, nausea and vomiting, breast pain or tenderness, mood changes, fatigue, irritability, decreased libido, increased weight
Dienogest/estradiol valerate (Natazia®) [105] Menstrual cyclicity, hirsutism, acne Headaches, irregular uterine bleeding, breast tenderness, nausea and vomiting, acne, and increased weight
Chlormadinone acetate/Ethinyl estradiol (Belara®) [106] Menstrual cyclicity, hirsutism, acne Breast pain or tension, depressed state, loss of libido, migraine or headache
Progestins
Medroxyprogesterone acetate (Provera®) [107] Inhibition of secretion of pituitary gonadotropins,
Prevention of follicular maturation and ovulation
Menstrual cyclicity, Amenorrhea, change in menstrual flow, hot flash, weight gain or weight loss, menstrual disease, abdominal pain, headache, nervousness
  • Undiagnosed abnormal genital bleeding

  • Known, suspected, or history of cancer of the breast

  • Known or suspected estrogen, progesterone dependent neoplasia

  • Active deep vein thrombosis, pulmonary embolism, or a history of these conditions

  • Active or recent arterial thromboembolic disease (e.g., stroke and myocardial infarction)

  • Known liver dysfunction or disease

  • Missed abortion

  • As a diagnostic test for pregnancy

  • Known hypersensitivity to the tablets

  • Known or suspected pregnancy

Biguanides
Metformin (Glucophage®) [108] ↓hepatic glucose production ↓intestinal absorption,
↑insulin sensitivity
Impaired glucose tolerance,
type II diabetes
Diarrhea, nausea and vomiting, flatulence, asthenia, indigestion, abdominal discomfort, headache
  • Severe renal impairment

  • Known hypersensitivity to metformin hydrochloride

  • Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma

Antiandrogens
Spironolactone (Aldactone®) [109] Competitive antagonistic activity against aldosterone receptors causes potassium retention, sodium and water excretion Hirsutism, acne Gynecomastia
  • Hyperkalemia

  • Addison’s disease

  • Concomitant use of eplerenone

Finasteride
(Propecia®) [110]
A competitive and specific inhibitor of Type II 5-alpha-reductase, an enzyme that converts the androgen testosterone into DHT Hirsutism, acne Decreased libido, erectile dysfunction, and ejaculation disorder
  • Pregnancy

  • Hypersensitivity to any components of this product

Antiestrogens
Clomiphene citrate (Clomid®) [111] Occupying ERs for a longer duration than estrogen, inhibiting normal estrogen negative feedback, which results in increased pulsatile GnRH secretion from the hypothalamus and pituitary gonadotropin release Ovulation induction Ovarian enlargement, vasomotor flushes, abdominal-pelvic discomfort/distention/bloating, nausea and vomiting, breast discomfort, blurred vision, lights/ floaters/waves/unspecified visual complaints, photophobia, diplopia, scotomata, phosphenes, headache, abnormal uterine bleeding, intermenstrual spotting, menorrhagia
  • Hypersensitivity to any components of this product

  • Pregnancy

  • Liver disease or a history of liver dysfunction

  • Abnormal uterine bleeding of undetermined origin

  • Ovarian cysts or enlargement not due to PCOS

  • Uncontrolled thyroid or adrenal dysfunction

  • In the presence of an organic intracranial lesion such as pituitary tumor

Aromatase inhibitors
Letrozole
(Femara®) [112]
Nonsteroidal competitive inhibitor of the aromatase enzyme which catalyzes the conversion of androgens to estrogens Ovulation induction Hot flashes, arthralgia, flushing, asthenia, edema, arthralgia, headache, dizziness, hypercholesterolemia, sweating increased, bone pain
  • Women of premenopausal endocrine status, including pregnant women

Abbreviations: COC: Combined oral contraceptives; DHT: Dihydrotestosterone; ER: Estrogen receptor; FSH: Follicle-stimulating hormone; GnRH: Gonadotropin-releasing hormone; HD: High dose; IM: Intramuscular; LD: Low dose; LH: Luteinizing hormone; PCOS: Polycystic ovary syndrome; PMS: Premenstrual syndrome; Ref: Reference; XR: Extended-release.