Table 1.
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:
|
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 |
|
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 |
|
Antiandrogens | ||||
Spironolactone (Aldactone®) [109] | Competitive antagonistic activity against aldosterone receptors causes potassium retention, sodium and water excretion | Hirsutism, acne | Gynecomastia |
|
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 |
|
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 |
|
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 |
|
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.