Fertility Drugs/ Gonadotropin Drugs drugs

Gonadotropin drugs


Gonadotropins are fertility medications given by injection that contain follicle-stimulating hormone (FSH) alone or combined with luteinizing hormone (LH).

Gonadotropins are a class of medications used to treat infertility and disorders associated with reproductive functions.


Drugs that affect the female reproductive system typically include hormones and hormonal-like agents.

These drug types include;

  1.  Female Sex Hormones
  2. Estrogen Receptor Modulators
  3. Fertility Drugs/gonadotropins
  4. Drugs used in labor
  5. Abortifacients
gonadotropin sites

Gonadotropin Sites of Action

Female Sex Hormones

The female sex hormones can be used to replace hormones that are missing or to act on the control mechanisms of the endocrine system to decrease the release of endogenous hormones.
Drugs that act like estrogen, particularly at specific estrogen receptors, are also used to stimulate the effects of estrogen in the body with fewer of the adverse effects.

Female sex hormones include;

  • Estrogens 
  • Progestins


This hormone is naturally produced by the ovaries, placenta and adrenal glands. It stimulates the development of female sex characteristics, prepares the body for pregnancy, affects the release of FSH and LH, and is responsible for proliferation of the endometrial lining.

Low estrogen in the body is responsible for the signs and symptoms of menopause, in the uterus, vagina, breast and cervix.

Other Functions of estrogen include;

  1. Breast development.
  2. Increase cholesterol in bile, to prevent damaging effects of bile salts.
  3. Increases fat storage, such as in breast tissue.
  4. Maintains bone mineral density.
  5. Maintains muscle strength.
  6. Prevents atherosclerosis, by increasing HDL concentration and lowering LDL.
  7. Estrogen is responsible for maintaining libido, memory, and mental health. 
  8. It stimulates ovulation, maintains the uterine walls and is important in vaginal lubrication.
Indications of Estrogen Therapy.
  • Estrogens are used for hormone replacement therapy (HRT) when ovarian activity is blocked or absent.
  • Is used to control the signs and symptoms of menopause.
  • They can also be used in therapy for prostate cancer and inoperable breast cancer, also as palliative care.
  • Treatment of female hypogonadism(when the body produces little or no hormones).
  • Treat ovarian failure.
  • Oral contraceptives (estrogen and progestin)
  • Morning after pill (emergency pills)
  • Endometriosis
  • Dysmenorrhea, used with progestin.


This promotes maintenance of pregnancy and it is called a pregnancy hormone.

Its functions include;

  1. Transforms proliferative endometrium into secretory endometrium.
  2. Prevents follicle maturation, ovulation and uterine contractions.
  3. Used in contraceptives. It inhibits release of GnRH, FSH and LH, hence follicle development and ovulation are prevented.
Indications of Progestin.
  • Used as a contraceptive.
  • Maintains pregnancy and development of secondary sex characteristics.
  • Use to treat primary and secondary amenorrhea, and functional uterine bleeding.
  • Treatment of acne and premenstrual dysphoric disorder (PMDD).
  • For the relief of signs and symptoms of menopause .
Contraindications of Female Sex hormones.


  • Known allergies
  • Idiopathic vaginal bleeding.
  • Breast Cancer(Estrogen dependant cancer)
  • CVA since it increases clotting factor prodn.
  • Hepatic dysfunction.
  • Pregnancy.
  • Lactation.


  • PID
  • STD
  • Endometriosis
  • Renal and hepatic disorders.
  • Epilepsy.
  • Asthma.
  • Migraine headaches
  • Cardiac Dysfunction —potential excerbation.
Adverse Effects.
  • Corneal Changes.
  • Photosensitivity.
  • Peripheral edema.
  • Chloasma ( patches on the face)
  • Hepatic adenoma.
  • Nausea
  • Vomiting.
  • Abdominal cramps.
  • Bloating.
  • Withdraw bleeding.
  • Changes in menstrual flow.

Important aspects/issues to remember.

  1.  Women receiving any of these drugs should receive an annual medical examination, including
    breast examination and Pap smear, to monitor for adverse effects and underlying medical
  2. Women taking estrogen should be advised not to smoke because of the increased risk of
    thrombotic events.
  3. Women who are receiving these drugs for fertility programs should receive a great deal of psychological support and comfort measures to cope with the many adverse effects associated
    with these drugs. The risk of multiple births should be explained.
  4. Drugs are used in treatment of specific cancers in males and they should be advised about the
    possibility of estrogenic effects.
  5. Not indicated during pregnancy or lactation because of potential for adverse effects on the fetus
    or neonate.
Examples of female sex hormones and dosages.


  1. Estradiol, 1–2 mg/day orally or  1–5 mg IM every 3–4 weeks or  2–4 g intravaginal cream daily.
  2. Estrogens, conjugated (C.E.S., Premarin), 0.3–1.25 mg/day orally.
  3. Estropipate (Ortho-Est, Ogen), 0.625–5 mg/day orally.


  1. Etonogestrel (Implanon) 68 mg implanted sub dermally for up to 3 yr, replaced or changed when needed.
  2. Medroxyprogesterone (Provera) 5–10 mg/day PO for 5–10 days for amenorrhea or 400–1000 mg/week IM for cancer therapy or 150 mg of deep IM every 3 months (13 weeks) for contraception.
Clinically important Drug Interactions


  •  Barbiturates, rifampin, tetracyclines, phenytoin: decreased serum estrogen levels
  • Corticosteroids: increased therapeutic and toxic effects of corticosteroids.
  • Nicotine: Increased risk of thrombi and emboli
  • Grapefruit juice: inhibition of metabolism of estradiols
  • St. John’s wort: can affect metabolism of estrogens and can make estrogen-containing
    contraceptives less effective.


  •  Barbiturates, carbamazepine, phenytoin, griseofulvin, penicillin, tetracyclines, rifampin: reduced
    effectiveness of progestins
  • St. John’s wort: can affect the metabolism of progestins and can make progestin-containing
    contraceptives less effective..
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