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All about: Progesterone

Big Image Pronouncation: (pro-JESS-ter-ohn)
Class: Progestin

Trade Names:
Crinone
- Vaginal gel 4% (45 mg)
- Vaginal gel 8% (90 mg)

Trade Names:
Prochieve
- Vaginal gel 4% (45 mg)
- Vaginal gel 8% (90 mg)

Trade Names:
Prometrium
- Capsules 100 mg (micronized progesterone)
- Capsules 200 mg (micronized progesterone)

Trade Names:
Progesterone in Oil
- Injection 50 mg/mL

Mechanism of Action

Pharmacology

Inhibits secretion of pituitary gonadotropins, thereby preventing follicular maturation and ovulation (contraceptive effect); inhibits spontaneous uterine contraction; transforms proliferative endometrium into secretory endometrium.

Pharmacokinetics

Absorption

Rapidly absorbed from the GI tract (oral); rapidly absorbed (IM). T max is 1 to 2 hr (oral); 6.8 hr (8% gel); and 9.2 hr (90 mg IM). C max is 17.3 to 72.5 ng/mL (100 to 300 mg/day for oral).

Distribution

Protein binding is 96% to 99%, primarily to serum albumin (50% to 54%) and transcortin (43% to 48%). Undergoes enterohepatic recycling and distributes into breast milk.

Metabolism

Metabolized in the liver to pregnanediols and pregnenolones metabolites, which are conjugated to glucuronide and sulfate metabolites.

Elimination

Excreted in the kidney (50% to 60% metabolites), bile/feces (approximately 10% metabolites), and small amount as unchanged in the bile. The t ½ is approximately 2 to 3 hr (after first 6-hr oral ingestion) and approximately 8 to 9 hr thereafter (oral). Absorption t ½ is a few minutes (IM) and 25 to 50 hr (gel). Elimination t ½ is approximately 10 wk (IM) and 5 to 20 min (gel).

Duration

3 to 6 mo (IM, long-acting).

Special Populations

Renal Function Impairment

Use with caution and only with careful monitoring because metabolites are eliminated this way.

Severe liver insufficiency

Contraindicated.

Indications and Usage

Injection

Amenorrhea and abnormal uterine bleeding caused by hormonal imbalance in the absence of organic pathology (eg, uterine cancer).

Gel

Progesterone supplementation or replacement as part of an assisted reproductive technology (ART) treatment for infertile women with progesterone deficiency.

Capsule

Prevention of endometrial hyperplasia in nonhysterectomized postmenopausal women receiving conjugated estrogen tablets.

Capsules and gel

Use in secondary amenorrhea.

Contraindications

Hypersensitivity to progestins; thrombophlebitis, thromboembolic disorders, cerebral hemorrhage (or history of these disorders); impaired liver function; breast or genital organ cancer; undiagnosed vaginal bleeding; missed abortion; diagnostic test for pregnancy; pregnancy or suspected pregnancy.

Dosage and Administration

Amenorrhea
Adults

IM 5 to 10 mg/day for 6 to 8 consecutive days.

ART
Adults (8% gel)

Intravaginal 90 mg once daily for women requiring progesterone supplementation. In women with partial or complete ovarian failure, who require progesterone replacement, 90 mg bid.

Functional Uterine Bleeding
Adults

IM 5 to 10 mg/day for 6 days.

Prevention of Endometrial Hyperplasia
Adults

PO 200 mg in the evening for 12 days, sequentially per 28-day cycle.

Secondary Amenorrhea
Adults

PO Single 400 mg dose in the evening for 10 days. Intravaginal 45 mg of 4% gel every other day for up to 6 doses. Women who fail to respond, 90 mg of 8% gel every other day for up to 6 doses.

General Advice

Capsules
  • Because medication can cause drowsiness, administer prescribed dose in the evening.
  • Administer without regard to meals, but administer with food if GI upset occurs.
Gel
  • For intravaginal administration only. Not for dermal, ophthalmic, or oral administration.
  • Administer gel using prefilled disposable applicator.
  • Discard applicator after delivering dose. Do not save for future use.
  • Do not use concurrently with other intravaginal therapy. If other intravaginal therapy is used, administer at least 6 hr before or after progesterone vaginal gel.
Injection
  • For IM injection only. Not for intradermal, subcutaneous, or intra-arterial administration.
  • Do not administer if particulate matter, cloudiness, or discoloration is noted.
  • Rotate injection sites.

Storage/Stability

Store capsules, vaginal gel, and injection at controlled room temperature (59° to 86°F). Protect capsules from excessive moisture.

Drug Interactions

CYP3A4 inhibitors (eg, ketoconazole)

May inhibit progesterone metabolism, increasing plasma levels and the risk of side effects.

Laboratory Test Interactions

Altered metyrapone test; increased sulfobromophthalein retention and other hepatic function tests; increase in prothrombin factors VII, VIII, IX, and X; altered pregnanediol determination; increase in protein bound iodine and butanol extractable protein bound iodine; decrease in T3 uptake.

Adverse Reactions

Cardiovascular

Hypertension, palpitation, angina pectoris (less than 5%); syncope with and without hypotension.

CNS

Headache, depression, dizziness, worry, fatigue, emotional lability, irritability (at least 5%); confusion, somnolence, speech disorder, anxiety, impaired concentration, insomnia, personality disorder (less than 5%); asthenia, anorexia, increased appetite, nervousness (clinical trials); migraine, decreased libido.

Dermatologic

Acne, verruca, wound debridement (less than 5%); pain at injection site, melasma, chloasma, photosensitivity.

EENT

Earache, nasal congestion, pharyngitis, abnormal vision (less than 5%).

GI

Abdominal bloating and pain, nausea, vomiting, diarrhea (at least 5%); constipation (at least 2%); dry mouth, dyspepsia, gastroenteritis, hemorrhagic rectum, hiatus hernia (less than 5%); tooth disorder (clinical trials).

Genitourinary

Breast tenderness, urinary problems, vaginal discharge, breast pain, vaginal dryness (at least 5%); breast carcinoma (at least 2%); leucorrhea, uterine fibroid, vaginal dryness, fungal vaginitis, vaginitis, UTI (less than 5%); breast enlargement (clinical trials); breakthrough bleeding, spotting, change in menstrual flow, amenorrhea, changes in cervical squamo-columnar junction and cervical secretions, vaginal candidiasis, pruritus vulvae, endometriosis, spontaneous abortion, pelvic infection.

Hepatic

Cholecystectomy (at least 2%); hepatitis, elevated transaminases (postmarketing); cholestatic jaundice.

Hematologic-Lymphatic

Lymphadenopathy (less than 5%).

Metabolic-Nutritional

Edema, peripheral edema (less than 5%); increase or decrease in weight.

Musculoskeletal

Joint or musculoskeletal pain, back pain (at least 5%); arthritis, leg cramps, hypertonia, muscle disorder, myalgia (less than 5%).

Respiratory

Upper respiratory tract infection, coughing (at least 5%); bronchitis, pneumonitis, sinusitis (less than 5%).

Miscellaneous

Hot flashes, chest pain, night sweats, swelling of hands and feet, viral infection (at least 5%); accidental injury, chest pain, fever (less than 5%); abscess, herpes simplex (less than 5%); increased sweating (clinical trials); anaphylaxis and anaphylactoid reactions, pyrexia, masculinization of female fetus.

Precautions

Pregnancy

Category X ; Category B ( Prometrium capsule).

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Depression

Carefully observe patients with history of depression.

Fluid retention

Use cautiously when conditions that might be affected by this factor are present (eg, asthma, cardiac or renal dysfunction, epilepsy).

Ophthalmic effects

Discontinue medication if there are any sudden changes in vision or other serious ophthalmic effects.

Peanut oil

Capsule contains peanut oil and should not be used in patients allergic to peanuts.

Thrombotic disorder

Discontinue if these conditions occur or are suspected.

Vaginal bleeding

With irregular vaginal bleeding, including breakthrough bleeding, nonfunctional causes should be considered and adequate diagnostic measures undertaken.

Patient Information

  • Explain name, dose, action, and potential side effects of drug.
  • Advise patient to read Patient Information leaflet before using the first time and with each refill.
  • Instruct diabetic patient taking estrogen and progesterone to monitor blood glucose more frequently when therapy is started and to inform health care provider of significant changes in readings.
  • Teach patient proper method of breast self-examination, and remind patient to perform monthly.
  • Instruct patient to immediately report any of the following symptoms to health care provider: pain in groin or calves; sharp chest pain, coughing blood, or sudden shortness of breath; crushing chest pain or heaviness in chest; abnormal vaginal bleeding; breast lumps; sudden severe headache; dizziness or fainting; tremors or seizure; vision or speech problems; weakness or numbness of arms or legs; severe abdominal pain; depression; yellowing of the skin or eyes; or persistent pain, pus, or bleeding at injection site.
  • Advise patient that drug may cause dizziness and/or drowsiness and to use caution while driving or performing other tasks requiring mental alertness, coordination, or physical dexterity until tolerance is determined.
  • Advise women to notify health care provider if pregnant, planning to become pregnant, or breastfeeding.
  • Advise patient that follow-up visits and examinations, including Pap smear, at least once a year, will be required to monitor therapy and to keep appointments.
  • Capsules
  • Advise patient to take prescribed dose in the evening to minimize problems with medication-induced drowsiness or dizziness.
  • Remind patient using progesterone for prevention of endometrial hyperplasia to take prescribed dose once daily for 12 days per 28-day cycle.
  • Remind patient using progesterone for treating secondary amenorrhea that prescribed dose is taken once daily for 10 days.
  • Advise patient to take each dose without regard to meals but to take with food if stomach upset occurs.
  • Vaginal Gel
  • Review instructions for preparing the applicator and administering the gel.
  • If gel will be used at altitudes above 762 m, review special instructions for preparing the applicator to prevent partial release of gel before vaginal insertion.
  • Instruct patient to discard applicator after use and not to save for future use.
  • Advise patient that gel should not be used at the same time as other intravaginal products. If other intravaginal therapy is being used, instruct patient to administer at least 6 hr before or after the progesterone vaginal gel.
  • Advise patient that small, white globules may appear as a discharge, even several days after using gel, but that this is normal and of no concern.
  • Advise patient to discontinue use and notify health care provider if vaginal irritation develops while using the medication.
  • Injection
  • Advise patient that injection will be prepared and administered by a health care provider in a medical setting.

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