2.02 Medications the female reproductive organs

Contraceptives

Medications that are used to prevent pregnancy are called CONTRACEPTIVES. They can be taken orally are the most effective form of birth control

  • Contraceptive medications are made up of synthetic estrogen and progesterone (progestin)
  • Oral contraceptives come in three different formulations   * Monophasic: The dosage of estrogen and progestin are the same in each pill taken during the person’s menstrual cycle. Ex: norethindrone and ethinyl estradiol.   * Biphasic: Provided in either 21-28 day dosage packages, they contain a consistent dose of estrogen in each pill, but the level progestin changes based on the day of the menstrual cycle. The dose of progestin is lower in the first 10 days of the menstrual cycle and decreases for the remainder of the 21-28 day package. Ex: Norethindrone and ethinyl estradiol   * Triphasic: This type of oral contraceptive is provided in doses that replicate the hormone levels in a menstrual cycle. There are 3 different dosages of estrogen and progestin that are administered over the 21 or 28 day packages. Ex: Norethindrone and ethinyl estradiol.
  • Contraceptives also come in other forms.   * There are preparations that administered via injection in regular intervals. (Preferable for people who forget to take medication and people who need to avoid menstrual bleeding)
  • Contraceptives can be administered transdermally and intravaginally   * when this medications are stopped in the 3rd week, menstruation begins.

Mechanism of Action

Function the same way that the naturally occurring hormones estrogen and progesterone do.

  • The main functin of these hormones is to suppress the activation of the hypothalamic-pituitary system, and as a result ovulation is inhibited.
  • Contraceptives also increase the thickness of mucous in the uterus, slowing down the sperm so that they cannot reach any follicle that does develop. The medications also prevent any fertilized follicle from implanting into the lining of the uterus.

Uses

Not only used to prevent pregnancy but also to treat those who have illnesses like endometriosis.

  • Endometriosis: A disorder that causes those affected to experience pain in their pelvis and abdomen, the pain results from abnormal growth of the endometrium.
  • Contraceptives can also make the menstrual cycle timing more predictable.
  • Contraceptives also decrease the amount of blood loss during menstruation and as a result can be of benefit for those who have low levels of hemoglobin already or when menstrual bleeding is excessive.
  • EMERGENCY contraceptives: Used when contraceptive failures occur. (they come orally.)

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Contraindications

Patients with a history of allergy to any of the components of oral contraceptives that are administered.

  • pregnancy
  • those who have a high risk of myocardial infarction (heart attack)
  • blood cloths in the veins (venous thrombosis)
  • blood clots in the lungs (pulmonary embolism)
  • stroke
  • don’t take smoking tobacco, it will increase the risk of developing blood clots.

Adverse effects

  • Central Nervous System: stroke, migraine headaches, dizziness, headaches, depression, mood changes, vision changes
  • Cardiovascular system: hypertension, heart attack, thromboembolism, pulmonary embolism, swelling
  • GI tract: diarrhea, loss of appetite, constipation, weight gain, nausea, vomiting.
  • amenhorrhea, erosion of tissues of the cervix, bleeding during menstrual cycles, breast tenderness and enlargement.

Ex: Medroxyprogesterone (Depo-Provera)

Medications used to Enhance Fertility

When women experience hormone imbalances from impaired hypothalamus, pituitary, and/or ovarian dysfunction, exogenous hormones may be administered

  • If this is not adequate, medications that simulate secretion of GnRH from the hypothalamus may be prescribed.
  • Commonly prescribed ovulation stimulant called clomiphene

Mechanism of Action

Clomiphene blocks the estrogen receptors in both the brain and the uterus. When the regions of the hypothalamus sense the low level of estrogen, they increase the secretion of GnRH, FSH, and LH

  • this results in the stimulation and maturation of the ovarian follicles causing ovulation and, when timed appropriately with intercourse, conception.

Uses

These medications are used for the promotion of ovulation for women have primary infertility.

  • Primary infertility refers to women who do not become pregnant after a year of having unprotected intercourse without using contraceptives

\ Contraindications

  • GnRH stimulants shouldn’t be prescribed to women who have an allergy to any of the compounds.
  • Ovarian failure
  • Uncontrolled adrenal or thyroid dysfunction
  • A pituitary tumor
  • liver disease
  • or sex-hormone driven cancer.

Adverse Effects

  • Hot flashes
  • dizziness
  • headache
  • anxiety
  • fatigue
  • bloating
  • vomiting
  • constipation
  • blurred vision
  • breast tenderness

SEVERE AE: Ovarian hyperstimulation is a syndrome that causes the ovaries to swell and become very painful.

\ Hormones

When deficiencies of naturally occurring hormones take place, they can be balanced using synthetic and natural hormone preparations.

  • Hormone levels decline naturally as a women ages and the ovaries cease to function.
  • When FSH and LH are no longer available to perform their normal functions, testosterone, progesterone, and estrogen are not produced in adequate level.   * when these level being to decline they are said to be experiencing Perimenopause: The period time that occurs before menopause   * menopause: the mark of the end of a woman’s reproductive years.   * many symptoms can affect a woman’s daily life, their healthcare provider may choose to prescribe synthetic or naturally occurring preparations.

\ Estrogen

Estrogen is responsible for processes other than regulation of the menstrual cycle. It stimulates the development of secondary female sex characteristics (breasts, skin, bone development, and the distribution of body fat and hair).

Types of estrogens

  • Estradiol
  • estrone
  • estriol   * estrogen connects to estrogen receptors to stimulate the female sex characters.
  • When women develop cancer of these various organs (tissues of the breasts, female genitals, the hypo and the pituitary) and either have surgeries or chemo as treatment, the estrogen receptors can be diminished or removed entirely.   * this is when estrogen replacement may be required.   * Synthetic estrogens are administered.
  • Conjugated estrogen (most common preparation): A mixture of both natural estrogen and compounds with synthetic compounds.   * the natural portion of the med comes from urine of pregnant horses.

Mechanism of Action

Estrogen binds to the intracellular estrogen receptors to stimulate their action.

Uses

Estrogen is used to treat or prevent symptoms that result from estrogen insufficiency.

  • Ovarian Failure
  • uterine bleeding
  • perimenopause
  • menopause
  • osteoporosis

Contraindications

Women who have a history of cancers that are estrogen-dependent, those with undiagnosed abnormal vaginal bleeding, history of stroke or thromboembolism should not be prescribed estrogen or estrogen derivatives. Pregnancy and history of allergy are absolute contra.

Adverse effects

May experience dermatologic issues like chloasma.

  • Chloasma is a condition that causes dark brown patches on the skin.
  • Growth of hair as well as thinning and loss of hair on the scalp.
  • Estrogen has the potential to decrease the effect of anticoagulant medications, increase the potential for toxicity of antidepressants, and be less effective when taken with antibiotic called rifampin.

Progestins

Progesterone is a sex hormone. When progesterone levels rise during the menstrual cycle; they are doing so to prepare the uterus for possible implantation of a fertilized follicle. If this implantation does not occur, progesterone levels drop, and the endometrial lining of the uterus is shed in the form of menstrual blood. Progesterone also causes an increase in body temperature, an increase in the thickness of the mucous in the vagina, relaxation of the muscles of the uterus, and prevention of the release of FSH and LH from the pituitary gland

  • synthetic and natural forms of progesterone that are administered in the form of medication are progestins.   * most often administered in synthetic form.

Mechanism of Action

Progestins bind with progesterone receptors in target tissues to generate the same physiological response as progesterone.

Uses

Used to treat abnormal uterine bleeding that is caused by hormone imbalances ( in perimenopause or menopause), uterine cancer, or fibroids.

  • Fibroids are non-cancerous abnormal growths that may develop in the uterus.
  • Also administered to women who have had previous miscarriages when it is expected that the integrity of the uterine wall has been a factor in preventing successful pregnancy.

Contraindications

Same as estrogen

Adverse effects

  • nausea
  • vomiting
  • amenorrhea
  • bleeding between menstruation
  • swelling
  • alterations in weight
  • high temps
  • sleep disturbances
  • mood changes.

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