progesterone

progesterone

 [pro-jes´tĕ-rōn]

a steroid sex hormone that is the principal progestational agent; it plays a major part in the menstrual cycle. During the maturation of the secondary oocyte (ovum), estrogen, the principal female sex hormone, is produced at a high rate. At ovulation estrogen production is sharply reduced, and the ovary then creates within itself a special endocrine structure called the corpus luteum whose sole function is to produce progesterone. Unless fertilization takes place, the corpus luteum disappears when it has performed its function. The progesterone it has produced is promptly carried by the blood to the uterus, as was the estrogen previously. Both hormones now work to prepare the uterus for possible conception.

In pregnancy progesterone acts in a way that protects the embryo and fosters growth of the placenta. By decreasing the frequency of uterine contractions it helps to prevent expulsion of the implanted zygote. It also promotes secretory changes in the mucosa of the fallopian tubes, thereby helping to provide nutrition for the fertilized ovum as it travels through the tube on its way to the uterus.

Another function of progesterone is promotion of the development of the mammary glands in preparation for lactation. prolactin, from the anterior lobe of the pituitary gland, stimulates production of milk, and progesterone prepares the glands for milk secretion. Progesterone also has an indirect effect on the fluid and electrolyte balance of the body by blocking the effect of aldosterone. Diminished secretion of progesterone can lead to menstrual difficulties in nonpregnant women and spontaneous abortion in pregnant women.

Progesterone is used medically in the treatment of dysfunctional uterine bleeding and abnormalities of the menstrual cycle, as part of postmenopausal hormone replacement therapy, as a test for endogenous estrogen production, and as an adjunct in the treatment of infertility associated with partial or complete ovarian failure; administered orally, intramuscularly, or intravaginally.

progesterone

Crinone, Endometrin, Prometrium

Pharmacologic class: Progestin

Therapeutic class: Hormone

Pregnancy risk category B (oral), D (injection),NR (vaginal)

FDA Box Warning

• Estrogen plus progestin therapy shouldn't be used for prevention of cardiovascular disease or dementia.

• The Women's Health Initiative (WHI) estrogen plus progestin substudy reported increased risk of stroke, deep vein thrombosis, pulmonary embolism, and myocardial infarction in postmenopausal women (ages 50 to 79) during 5.6 years of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo.

• The substudy also demonstrated increased risk of invasive breast cancer.

• The WHI Memory Study estrogen plus progestin ancillary study of the WHI reported increased risk of dementia in postmenopausal women ages 65 and older.

Action

Suppresses ovulation by altering the vaginal epithelium, relaxing uterine smooth muscle, and promoting mammary tissue growth. Also inhibits pituitary activity and causes withdrawal bleeding in presence of estrogen.

Availability

Injection (in sesame or peanut oil with benzyl alcohol): 50 mg/ml in 10-ml vials

Micronized capsules (oral) in peanut oil: 100 mg, 200 mg

Micronized vaginal gel: 4%, 8%

Indications and dosages

➣ Secondary amenorrhea

Adults: 400 mg/day P.O. in evening for 10 days, or 5 to 10 mg/day I.M. for 6 to 8 days, given 8 to 10 days before expected menstrual period. Or 45 mg (one applicatorful of 4% gel) vaginally once every other day for up to six doses; may increase to 90 mg (one applicatorful of 8% gel) once every other day for up to six doses.

➣ Dysfunctional uterine bleeding

Adults: 5 to 10 mg I.M. daily for 6 days

➣ To prevent postmenopausal estrogen-induced endometrial hyperplasia

Adults: 200 mg/day P.O. at bedtime for 14 days on days 8 to 21 of 28-day cycle or on days 12 to 25 of 30-day cycle. If patient currently receives estrogen 1.25 mg/day, 300 mg progesterone in two divided doses (100 mg 2 hours after breakfast and 200 mg at bedtime); further adjustment may be required.

➣ Corpus luteum insufficiency; assisted reproduction technology

Adults: For luteal-phase support, 90 mg (one applicatorful of 8% gel) vaginally once daily. For in vitro fertilization, 90 mg (one applicatorful of 8% gel) vaginally once daily, starting within 24 hours of embryo transfer and continued through day 30 after transfer; if pregnancy occurs, treatment may continue for up to 12 weeks. For partial or complete ovarian failure, 90 mg (one applicatorful of 8% gel) vaginally b.i.d. while patient undergoes donor oocyte transfer; if pregnancy occurs, treatment may last up to 12 weeks.

Contraindications

• Hypersensitivity to drug, peanuts (injection, micronized capsules), or sesame (injection)

• Thromboembolic disease

• Cerebrovascular disease

• Severe hepatic disease

• Porphyria

• Breast or reproductive system cancer

• Missed abortion

• Undiagnosed vaginal bleeding

• Diagnosis of pregnancy

Precautions

Use cautiously in:

• renal or cardiovascular disease, seizure disorders, fluid retention, diabetes mellitus, asthma, migraine, depression

• history of hepatic disease

• breastfeeding patients.

Administration

• Before first dose, make sure patient has read package insert regarding adverse effects. Reinforce written information with oral review.

☞ Before first I.M. dose, ask if patient has allergy to peanuts or sesame. Before giving micronized capsules, ask about peanut allergy.

• Inject I.M. dose deep into muscle. Rotate injection sites.

Adverse reactions

CNS: depression, emotional lability, cerebrovascular accident

CV: thrombophlebitis, thromboembolism

EENT: retinal thrombosis

GI: abdominal cramps

GU: amenorrhea, breakthrough bleeding, spotting, cervical erosions, breast tenderness, menstrual flow changes, galactorrhea

Hepatic: hepatitis

Respiratory: pulmonary embolism

Skin: melasma, rash, angioedema

Other: gingival bleeding, weight gain or loss, hypersensitivity reactions including anaphylaxis

Interactions

Drug-drug. Conjugated estrogens: increased levels of both drugs

Drug-diagnostic tests. Alkaline phosphatase, amino acids, low-density lipoproteins: increased levels

Chloride and sodium excretion: reduced (with high doses)

High-density lipoproteins: decreased level

Pregnanediol excretion: reduced

Thyroid function tests: altered results

Drug-herbs. Red clover: interference with drug effects

Drug-behaviors. Smoking: increased risk of thromboembolic effects

Patient monitoring

☞ Watch for evidence of thromboembolic disorders, including cerebrovascular accident, pulmonary embolism, diplopia, proptosis, or sudden partial or complete vision loss (may signal retinal thrombosis). If these occur, discontinue drug and notify prescriber immediately.

☞ Assess for emotional lability and depression.

Patient teaching

☞ Teach patient to recognize and immediately report signs and symptoms of thromboembolic disorders.

☞ Instruct patient and significant other to stay alert for and immediately report depression.

• Advise patient to monitor weight regularly and report significant changes.

• Tell female patient that drug may cause menstrual abnormalities.

• Advise female patient to discuss breastfeeding with prescriber before taking drug.

☞ Instruct patient to immediately report possible pregnancy.

• Tell patient that smoking increases thromboembolism risk. Encourage her to stop smoking if she smokes.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

pro·ges·ter·one

(prō-jes'tĕr-ōn),

An antiestrogenic steroid, believed to be the active principle of the corpus luteum, isolated from the corpus luteum and placenta or synthetically prepared; used to correct abnormalities of the menstrual cycle, as a contraceptive, and to control habitual abortion.

Synonym(s): luteohormone, pregnancy hormone, progestational hormone

progesterone

(prō-jĕs′tə-rōn′)

n.

1. A steroid hormone, C₂₁H₃₀O₂, that is secreted by the corpus luteum of the ovary and by the placenta and that acts to prepare the uterus for implantation of the fertilized ovum and to maintain pregnancy.

2. This compound formulated as a drug, usually prepared synthetically from phytosterols, used in the treatment of infertility, amenorrhea, abnormal uterine bleeding, and certain other conditions.

pro·ges·ter·one

(prŏ-jes'tĕr-ōn)

An antiestrogenic steroid, believed to be the active principle of the corpus luteum, isolated from the corpus luteum and placenta or synthetically prepared; used to correct abnormalities of the menstrual cycle, as a contraceptive, and to control habitual abortion.
Compare: bioregulator
Synonym(s): luteal hormone, luteohormone, progestational hormone.

progesterone

The hormone secreted by the CORPUS LUTEUM of the ovary and by the PLACENTA. Progesterone acts during the menstrual cycle to predispose the lining of the womb (endometrium) to receive and retain the fertilized ovum. During pregnancy, progesterone from the placenta ensures the continued health and growth of the womb and promotes the growth of the milk-secreting cells of the breasts. Progesterone-like substances (progestogens) are widely used in medicine and are common constituents of oral contraceptives. The hormone is used to treat menstrual symptoms and infertility and as an adjunct to oestrogen in post-menopausal hormone replacement therapy (HRT). Brand names are Crinone, Cyclogest and Gestone.

progesterone

a female sex hormone produced by the CORPUS LUTEUM and the PLACENTA which is concerned with preparing the uterus to receive the fertilized OVUM, and in maintaining pregnancy. Progesterone is secreted on the stimulus of the corpus luteum by the pituitary hormones LH and LTH (LUTEOTROPHIC HORMONE).

Progesterone

A hormone naturally secreted by the ovary, or manufactured synthetically, that prepares the uterus for implantation of a fertilized egg.

Mentioned in: Dysfunctional Uterine Bleeding, Dysmenorrhea, Endometrial Cancer, Hormone Replacement Therapy, Menopause, Premenstrual Syndrome, Saw Palmetto

pro·ges·ter·one

(prŏ-jes'tĕr-ōn)

Antiestrogenic steroid, believed to be the active principle of corpus luteum, isolated from corpus luteum and placenta or synthetically prepared; used to correct abnormalities of the menstrual cycle, as a contraceptive, and to control habitual abortion.
Synonym(s): progestational hormone.