Segesterone acetate and ethinyl estradiol vaginal system

What is Segesterone acetate and ethinyl estradiol vaginal system?

It is a toroidal-shaped (ring), nonbiodegradable, flexible, opaque white vaginal system containing two active components, a progestin, segesterone acetate, and an estrogen, ethinyl estradiol. When placed in the vagina, It releases an approximate average 0.15 mg/day of segesterone acetate and 0.013 mg/day of ethinyl estradiol over the 21 days in-use period of each cycle for up to 13 cycles (total of 273 days). Each cycle is 28 days, with 21 days in and 7 days out.

• Segesterone Acetate

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Segesterone

1. Chemical Name: 16-methylene-17α-acetoxy-19-nor-pregn-4-ene-3,20-dione
2. Molecular Formula: C23H30O4
3. Molecular Weight: 370.5
4. Physical Form: White, or yellowish white powder
5. Solubility: Slightly soluble in n-hexane, soluble in ethyl acetate and methanol, freely soluble in acetone (USP classification)
6. Melting Point: 173°C–177°C

• Ethinyl Estradiol

Ethinylestradiol

1. Chemical Name: 19-Nor-17α -pregna-1,3,5(10)-trien-20-yne-3,17-diol
2. Molecular Formula: C20H24O2
3. Molecular Weight: 296.4
4. Physical Form: White to slightly yellowish-white crystalline powder
5. Solubility: Practically insoluble in water, freely soluble in alcohol, it dissolves in alkaline solution
6. Melting Point: 181°C–185°C

What are the uses of this medicine?

It is indicated for use by females of reproductive potential to prevent pregnancy.

How does this medicine work?

Combination hormonal contraceptive (CHC) lower the risk of becoming pregnant primarily by suppressing ovulation.

Who Should Not Use this medicine?

It is contraindicated in females who are known to have the following conditions:

• A high risk of arterial or venous thrombotic diseases. Examples include females who are known to:

1. Smoke, if over age 35.
2. Have current or history of deep vein thrombosis or pulmonary embolism.
3. Have cerebrovascular disease.
4. Have coronary artery disease.
5. Have thrombogenic valvular or thrombogenic rhythm diseases of the heart (for example, subacute bacterial endocarditis with valvular disease, or atrial fibrillation).
6. Have inherited or acquired hypercoagulopathies.
7. Have uncontrolled hypertension or hypertension with vascular disease.
8. Have diabetes mellitus and are over age 35, diabetes mellitus with hypertension or vascular disease, or other end-organ damage, or diabetes mellitus of >20 years duration.
9. Have headaches with focal neurological symptoms, migraine headaches with aura, or are over age 35 with any migraine headaches.

• Current or history of breast cancer or other estrogen- or progestin-sensitive cancer.
• Liver tumors, acute hepatitis, or severe (decompensated) cirrhosis.
• Undiagnosed abnormal uterine bleeding.
• Hypersensitivity to any of the components of ANNOVERA. Hypersensitivity reactions reported include: throat constriction, facial edema, urticaria, hives, and wheezing.
• Use of Hepatitis C drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, due to the potential for alanine transaminase (ALT) elevations.

What are the brand names and dosage forms of this medicine?

• Brand name: Annovera; NDC code: 50261-313-01.
• Each ANNOVERA releases an approximate average 0.15 mg/day of segesterone acetate (SA) and 0.013 mg/day of ethinyl estradiol (EE) when placed in the vagina over a period of 21 days of each cycle for up to 13 cycles (total of 273 days). Each cycle of use is 28 days with 21 days in and 7 days out.
• ANNOVERA (segesterone acetate and ethinyl estradiol vaginal system) is a toroidal-shaped (ring), nonbiodegradable, flexible, opaque white, contraceptive vaginal system containing 103 mg of SA and 17.4 mg EE.
• It is 56 mm in overall diameter and 8.4 mm in cross-sectional diameter. It contains 2 channels of approximately 3.0 mm diameter and 27 mm length into which steroid-containing cores are inserted. The cores are 3 mm in diameter with one releasing SA alone and the other releasing both SA and EE.
• It is designed to be used for up to 13 cycles (1 year).
• It is not made with natural rubber latex.

Is this medicine FDA approved?

It is approved by US FDA on Aug 10, 2018.

What are the active and inactive ingredients in Segesterone acetate and ethinyl estradiol vaginal system?

• Active ingredients:

1. Segesterone acetate
2. Ethinyl estradiol

• Inactive ingredient:

1. Titanium dioxide
2. Dibutyltin dilaurate

How should this medicine be used?

• ANNOVERA is a hormonal birth control method that is used for 3 out of 4 weeks every month. The same vaginal system is reusable for up to 1 full year (1 year includes 13 cycles; each cycle is 28 days).
• After you insert ANNOVERA for the first time, you will remove it at the end of week 3 and leave it out for 7 days. You will reinsert ANNOVERA at the end of week 4 of each 4-week cycle. You will repeat this pattern with ANNOVERA for up to 13 cycles. Scheduled insertions and removals of ANNOVERA should be at about the same time of the day and the same day of the week for each monthly cycle.

What side effects can this medication cause?

• Serious cardiovascular events and stroke
• Vascular events
• Liver disease

What to do in case of emergency/overdose?

There have been no reports of serious ill effects from overdose of CHCs. Overdosage may cause withdrawal bleeding in females and nausea. In case of suspected overdose, all ANNOVERA vaginal systems should be removed and symptomatic treatment given.

Can this medicine be used in pregnancy?

• Epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to CHCs before conception or during early pregnancy.
• Discontinue ANNOVERA if pregnancy occurs, because there is no reason to use CHCs during pregnancy.

Can this medicine be used in children?

Safety and efficacy of ANNOVERA have been established in women of reproductive age. Efficacy is expected to be the same for postpubertal adolescents under the age of 18 as for users 18 years and older. Use of ANNOVERA before menarche is not indicated.

What should I know about storage and disposal of this medication?

• Prior to dispensing ANNOVERA to the user, store ANNOVERA at 20°C to 25°C (68°F to 77°F), excursions permitted to 15°C to 30°C (59°F to 86°F)
• Protect ANNOVERA from direct sunlight.
• Do not refrigerate or freeze and avoid excessive heat.

• Dailymed label info on Segesterone acetate and ethinyl estradiol vaginal system
• FDA Segesterone acetate and ethinyl estradiol vaginal system

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