Yes

Progestin

Intrauterine contraception in women who have had at least 1 child, are in a stable, mutually monogamous relationship, and have no history of pelvic inflammatory disease; amenorrhea; functional uterine bleeding; replacement therapy

Intravaginal gel: Part of assisted reproductive technology for infertile women with progesterone deficiency; secondary amenorrhea (8% gel is used in those who fail to respond to 4%)

X (manufacturer lists oral capsules as B)

Hypersensitivity to progesterone or any component; pregnancy; thrombophlebitis; undiagnosed vaginal bleeding; carcinoma of the breast; cerebral apoplexy; severe liver dysfunction; capsules contain peanut oil and are contraindicated in patients with allergy to peanuts

Use with caution in patients with impaired liver function, depression, diabetes, and epilepsy. Use of any progestin during the first 4 months of pregnancy is not recommended. Monitor closely for loss of vision, proptosis, diplopia, migraine, and signs or symptoms of embolic disorders. Not a progestin of choice in the elderly for hormonal cycling. Capsules may cause some degree of fluid retention, use with caution in conditions which may be aggravated by this factor, including CHF, renal dysfunction, epilepsy, migraine, or asthma. Patients should be warned that progesterone may cause transient dizziness or drowsiness during initial therapy. Use of progestin treatment may adversely effect carbohydrate and lipid metabolism.

Intrauterine device:

>10%:

Cardiovascular: Edema

Endocrine & metabolic: Breakthrough bleeding, spotting, changes in menstrual flow, amenorrhea

Gastrointestinal: Anorexia

Neuromuscular & skeletal: Weakness

1% to 10%:

Cardiovascular: Embolism, central thrombosis

Central nervous system: Mental depression, fever, insomnia

Dermatologic: Melasma or chloasma, allergic rash with or without pruritus

Endocrine: Changes in cervical erosion and secretions, increased breast tenderness

Gastrointestinal: Weight gain or loss

Hepatic: Cholestatic jaundice

Injection (I.M.):

>10% Local: Pain at injection site

1% to 10%: Local: Thrombophlebitis

Oral capsules:

>10%:

Central nervous system: Dizziness (16%)

Endocrine & metabolic: Breast pain (11%)

5% to 10%:

Central nervous system: Headache (10%), fatigue (7%), emotional lability (6%), irritability (5%)

Gastrointestinal: Abdominal pain (10%), abdominal distention (6%)

Neuromuscular & skeletal: Musculoskeletal pain (6%)

Respiratory: Upper respiratory tract infection (5%)

Miscellaneous: Viral infection (7%)

<5% (limited to important or life-threatening symptoms): Dry mouth, accidental injury, chest pain, fever, hypertension, confusion, somnolence, speech disorder, constipation, dyspepsia, gastroenteritis, hemorrhagic rectum, hiatus hernia, vomiting, earache, palpitation, edema, arthritis, leg cramps, hypertonia, muscle disorder, myalgia, angina pectoris, anxiety, impaired concentration, insomnia, personality disorder, leukorrhea, uterine fibroid, vaginal dryness, fungal vaginitis, vaginitis, abscess, herpes simplex, bronchitis, nasal congestion, pharyngitis, pneumonitis, sinusitis, acne, verruca, urinary tract infection, abnormal vision, lymphadenopathy

Other report adverse effects (incidence unspecified): Hepatitis, elevated transaminases, breakthrough bleeding, change in menstrual flow, amenorrhea, weight change, cervical changes, cholestatic jaundice, anaphylactoid reactions, anaphylaxis, rash, pruritus, melasma, chloasma, pyrexia, insomnia, increased sweating, weakness, tooth disorder, anorexia, increased appetite, nervousness, breast enlargement

Systemic:

>10%:

Cardiovascular: Swelling of face

Central nervous system: Headache, mood changes, nervousness

Endocrine & metabolic: Amenorrhea, irregular menstrual cycles, menorrhagia, spotting, ovarian enlargement, ovarian cyst formation

Gastrointestinal: Abdominal pain

1% to 10%:

Cardiovascular: Hot flashes

Central nervous system: Dizziness, mental depression, insomnia

Dermatologic: Dermatitis, acne, melasma, loss or gain of body, facial, or scalp hair

Endocrine & metabolic: Hyperglycemia, galactorrhea, breast pain, libido decrease

Gastrointestinal: Nausea, change in appetite, weight gain

Genitourinary: Vaginitis, leukorrhea

Neuromuscular & skeletal: Myalgia

<1% (Limited to important or life-threatening symptoms): Thromboembolism, allergic reaction, hot flashes, migraine, tremor, aggressive reactions, forgetfulness, asthma

Toxicity is unlikely following single exposures of excessive doses

Supportive treatment is adequate in most cases

CYP3A3/4 enzyme substrate; CYP3A3/4 enzyme inducer

Increase effect: Ketoconazole may increase the bioavailability of progesterone. Progesterone may increase concentrations of estrogenic compounds during concurrent therapy with conjugated estrogens.

Refrigerate suppositories

Natural steroid hormone that induces secretory changes in the endometrium, promotes mammary gland development, relaxes uterine smooth muscle, blocks follicular maturation and ovulation, and maintains pregnancy

Time to peak concentrations: Oral: 1.5-2.3 hours

Duration of action: 24 hours

Protein binding: 96% to 99%

Metabolism: Liver

Half-life: 5 minutes

Elimination: 50% to 60% renal; ~10% bile and feces

Adults:

Functional uterine bleeding: I.M.: 5-10 mg/day for 6 doses

Contraception: Female: Intrauterine device: Insert a single system into the uterine cavity; contraceptive effectiveness is retained for 1 year and system must be replaced 1 year after insertion

Replacement therapy: Gel: Administer 90 mg once daily in women who require progesterone supplementation

Oral:

Prevention of endometrial hyperplasia (in postmenopausal women with a uterus who are receiving daily conjugated estrogen tablets): 200 mg as a single daily dose every evening for 12 days sequentially per 28 day cycle.

Amenorrhea: 400 mg every evening for 10 days.

Intravaginal gel:

Partial or complete ovarian failure (assisted reproductive technology): 90 mg (8% gel) intravaginally once daily; if pregnancy is achieved, may continue up to 10-12 weeks

Secondary amenorrhea: 45 mg (4% gel) intravaginally every other day for up to 6 doses; women who fail to respond may be increased to 90 mg (8% gel) every other day for up to 6 doses

Administer deep I.M. only

Before starting therapy, a physical exam including the breasts and pelvis are recommended, also a PAP smear; signs or symptoms of depression, glucose in diabetics

Thyroid function, metyrapone, liver function, coagulation tests, endocrine function tests

May cause insomnia or depression

None reported

No information available to require special precautions

Progestins may predispose the patient to gingival bleeding

This drug can only be given I.M. on a daily basis for a specific number of days (or inserted vaginally to remain for 1 year as a contraceptive). It is important that you you have an annual physical assessment, Pap smear, and vision assessment while taking this medication. You may experience increased facial hair or loss of head hair (reversible); photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight); loss of appetite (small frequent meals will help); constipation (increased fluids, exercise, dietary fiber, or stool softeners may help). Diabetics should use accurate serum glucose testing to identify any changes in glucose tolerance. Report immediately pain or muscle soreness; swelling, heat, or redness in calves; shortness of breath; sudden loss of vision; unresolved leg or foot swelling; change in menstrual pattern (unusual bleeding, amenorrhea, breakthrough spotting); breast tenderness that does not go away; acute abdominal cramping; signs of vaginal infection (drainage, pain, itching); or changes in CNS (eg, blurred vision, confusion, acute anxiety, or unresolved depression). Pregnancy/breast-feeding precautions: This drug may cause severe fetal complication. If you suspect you may be pregnant contact prescriber immediately. Consult prescriber if breast-feeding.

Patients should receive a copy of the patient labeling for the drug; administer deep I.M. only; monitor patient closely for loss of vision, sudden onset of proptosis, diplopia, migraine, and signs and symptoms of embolic disorders

Capsule: 100 mg

Gel: 4% (45 mg), 8% (90 mg)

Injection, in oil: 50 mg/mL (10 mL)

Intrauterine system, reservoir: 38 mg in silicone fluid

Jeffrey LP, Chairman, National Study Commission on Cytotoxic Exposure. Position Statement. "The Handling of Cytotoxic Agents by Women Who Are Pregnant, Attempting to Conceive, or Breast-Feeding," January 12, 1987.