Gestofit

The major progestational steroid that is secreted primarily by the corpus luteum and the placenta. Gestofit acts on the uterus, the mammary glands and the brain. It is required in embryo implantation; pregnancy maintenance, and the development of mammary tissue for milk production. Gestofit, converted from pregnenolone, also serves as an intermediate in the biosynthesis of gonadal steroid hormones and adrenal corticosteroids.

Disorders related to a Gestofit deficit.

By oral route (vaginal route is recommended as an alternative if oral route is not suitable): Menstrual irregularities due to ovulation disorders or anovulation, premenstrual disorders, breast pain or benign breast disorders (mastopathies), bleeding (due to fibroma), therapy of the menopause (adjunctive use with estrogen in postmenopausal women for prevention of endometrial hyperplasia), menace of preterm delivery and can be used up to 36 week of pregnancy, threatened miscarriage or prevention of habitual miscarriage due to luteal phase deficiency up to the 12th week of pregnancy, treatment of subfertility or primary or secondary infertility related to Gestofit insufficiency in particular in In Vitro fertilization (IVF) cycles and/or oocyte donation.

For all other Gestofit indications, the vaginal route represents an alternative to the oral route, in case of adverse events due to Gestofit (somnolence, dizzinesss).

Progestins are hormones. They are used by both men and women for different purposes.

Progestins are prescribed for several reasons:

• To properly regulate the menstrual cycle and treat unusual stopping of the menstrual periods (amenorrhea). Progestins work by causing changes in the uterus. After the amount of progestins in the blood drops, the lining of the uterus begins to come off and vaginal bleeding occurs (menstrual period). Progestins help other hormones start and stop the menstrual cycle..
• To help a pregnancy occur during egg donor or infertility procedures in women who do not produce enough Gestofit. Also, Gestofit is given to help maintain a pregnancy when not enough of it is made by the body.
• To prevent estrogen from thickening the lining of the uterus (endometrial hyperplasia) in women around menopause who are being treated with estrogen for ovarian hormone therapy (OHT). OHT is also called hormone replacement therapy (HRT) and estrogen replacement therapy (ERT).
• To treat pain that is related to endometriosis, a condition where the endometrial tissue which lines the uterus becomes displaced in other female organs.
• To treat a condition called endometriosis, to help prevent endometrial hyperplasia, or to treat unusual and heavy bleeding of the uterus (dysfunctional uterine bleeding) by starting or stopping the menstrual cycle.
• To help treat cancer of the breast, kidney, or uterus. Progestins help change the cancer cell's ability to react to other hormones and proteins that cause tumor growth. In this way, progestins can stop the growth of a tumor.
• To test the body's production of certain hormones such as estrogen.
• To treat loss of appetite and severe weight or muscle loss in patients with acquired immunodeficiency syndrome (AIDS) or cancer by causing certain proteins to be produced that cause increased appetite and weight gain.

Progestins may also be used for other conditions as determined by your doctor.

Depending on how much and which Gestofit you use or take, a Gestofit can have different effects. For instance, high doses of Gestofit are necessary for some women to continue a pregnancy while other progestins in low doses can prevent a pregnancy from occurring. Other effects include causing weight gain, increasing body temperature, developing the milk-producing glands for breast-feeding, and relaxing the uterus to maintain a pregnancy.

Progestins can help other hormones work properly. Progestins may help to prevent anemia (low iron in blood), too much menstrual blood loss, and cancer of the uterus.

Progestins are available only with your doctor's prescription.

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although these uses are not included in product labeling, progestins are used in certain patients with the following medical conditions:

• Carcinoma of the prostate
• Corpus luteum insufficiency
• Hot flashes
• Polycystic ovary syndrome
• Precocious puberty

Assisted Reproductive Technology

Gestofit® 8% is administered vaginally at a dose of 90 mg once daily in women who require Gestofit supplementation. Gestofit® 8% is administered vaginally at a dose of 90 mg twice daily in women with partial or complete ovarian failure who require Gestofit replacement. If pregnancy occurs, treatment may be continued until placental autonomy is achieved, up to 10-12 weeks.

Secondary Amenorrhea

Gestofit® 4% is administered vaginally every other day up to a total of six doses. For women who fail to respond, a trial of Gestofit® 8% every other day up to a total of six doses may be instituted.

It is important to note that a dosage increase from the 4% gel can only be accomplished by using the 8% gel. Increasing the volume of gel administered does not increase the amount of Gestofit absorbed.

Note: The PATIENT INFORMATION SHEET contains special instructions for using the applicator at altitudes above 2500 feet in order to avoid a partial release of Gestofit® before vaginal insertion.

How supplied

Gestofit® is available in the following strengths:

4% gel (45 mg) in a single use, one piece, disposable, white polyethylene vaginal applicator with a twist-off top. Each applicator contains 1.45 g of gel and delivers 1.125 g of gel.

NDC-55056-0406-1 - 6 Single-use prefilled applicators.

8% gel (90 mg) in a single use, one piece, disposable, white polyethylene vaginal applicator with a twist-off top. Each applicator contains 1.45 g of gel and delivers 1.125 g of gel.

NDC-55056-1601-6 - 6 Single-use prefilled applicators

NDC-55056-1601-5 - 15 Single-use prefilled applicators

NDC-55056-1601-8 - 18 Single-use prefilled applicators

Each applicator is wrapped and sealed in a foil overwrap.

Store at 25°C (77°F); excurs ions permitted to 15-30°C (59-86°F).

Manufactured for: Columbia Laboratories, Inc. Livingston, NJ 07039. Manufactured by: Fleet Laboratories Ltd., Watford, United Kingdom. Revised: May 2009

See also:
What is the most important information I should know about Gestofit?

Do not use Gestofit vaginal without your doctor's consent if you are pregnant, unless you are using the medication as part of your fertility treatment. Tell your doctor if you become pregnant during treatment. If you are not being treated for infertility, use an effective form of birth control while you are using this medication.

Some forms of this medication may contain plant-based oils. Do not use Gestofit vaginal without telling your doctor if you have any type of food allergy.

Using Gestofit vaginal can increase your risk of blood clots, stroke, heart attack, or breast cancer.

You should not use this medication if you have: a history of stroke or blood clot, circulation problems, severe liver disease, a hormone-related cancer such as breast or uterine cancer, abnormal vaginal bleeding, or if you have recently had a tubal pregnancy or an incomplete abortion.

Gestofit vaginal is sometimes given for only 6 to 12 days at a time. When used as part of fertility treatment, Gestofit vaginal may be given for up to 12 weeks into a pregnancy. Following your dosing schedule is very important for this medication to be effective. Try not to miss any doses.

This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

Gestofit vaginal can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Use Gestofit oil as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Gestofit oil. Talk to your pharmacist if you have questions about this information.
• Gestofit oil is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Gestofit oil at home, a health care provider will teach you how to use it. Be sure you understand how to use Gestofit oil. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.
• Do not use Gestofit oil if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.
• Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.
• If you miss a dose of Gestofit oil, contact your doctor as soon as possible.

Ask your health care provider any questions you may have about how to use Gestofit oil.

Use: Labeled Indications

Oral: Prevention of endometrial hyperplasia in nonhysterectomized, postmenopausal women who are receiving conjugated estrogens; treatment of secondary amenorrhea

IM: Treatment of amenorrhea or abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer

Intravaginal gel: Part of assisted reproductive technology (ART) for infertile women with Gestofit deficiency; treatment of secondary amenorrhea

Vaginal insert: To support embryo implantation and early pregnancy by supplementation of corpus luteal function as part of ART for infertile women

Off Label Uses

Reduce the risk of recurrent spontaneous preterm birth

Based on the American College of Obstetricians and Gynecologists (ACOG) practice bulletin for the prediction and prevention of preterm birth, vaginal Gestofit is an effective and recommended treatment option to reduce the risk of recurrent spontaneous preterm birth in appropriately selected women (ie, singleton pregnancy and prior spontaneous preterm singleton birth). Therapy may begin at 16 to 24 weeks (regardless of cervical length) or sooner (ie, <24 weeks) in women who have a cervix <20 mm. Use is not recommended as an intervention for women with multiple gestations.

See also:
What other drugs will affect Gestofit?

Drugs known to induce the hepatic cytochrome-P450-3A4 system [e.g. rifampicin, carbamazepine or St. John's wort (Hypericum perforatum)-containing herbal products] may increase the elimination rate and thereby decrease the bioavailability of Gestofit. In contrast ketoconazole and other inhibitors of cytochrome P450-3A4 may decrease elimination rate and thereby increase the bioavailability of Gestofit.

The effect of concomitant vaginal products on the exposure of Gestofit from Gestofit has not been assessed. However, Gestofit is not recommended for use with other vaginal products (such as antifungal products) as this may alter Gestofit release and absorption from the vaginal tablet.

See also:
What are the possible side effects of Gestofit?

Clinical Studies Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The safety data reflect exposure to Gestofit in 808 infertile women (74.9% White, 10.3% Hispanic, 5.4% Black, 5% Asian, and 4.6% Other) in a single Assisted Reproductive Technology 10 week clinical study conducted in the U.S. Gestofit was studied at doses of 100 mg twice daily and 100 mg three times daily. The adverse reactions that occurred at a rate greater than or equal to 2% in either Gestofit group are summarized in Table 1.

Table 1: Number and Frequency of Reported Adverse Reactions in Women Treated with Gestofit in an Assisted Reproductive Technology Study

Other less common reported adverse reactions included vaginal irritation, itching, burning, discomfort, urticaria, and peripheral edema.

Expected Adverse Reaction Profile Seen with Gestofit

Gestofit is also expected to have adverse reactions similar to other drugs containing Gestofit that may include breast tenderness, bloating, mood swings, irritability, and drowsiness.