What are the options for delivery of estrogen therapy?

Updated: Oct 16, 2018
  • Author: Janice L Bacon, MD; Chief Editor: Richard Scott Lucidi, MD, FACOG  more...
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Answer

Answer

Preparations for estrogen therapy and EPT include oral, transdermal, injectable, and vaginal formulations. Transdermal delivery systems include patches, gels, sprays, and lotions, while vaginal products include suppositories, creams, and rings.

Because of the potential risks and existing controversies regarding high-dose oral regimens, the popularity of low-dose preparations and different delivery systems (eg, transdermal patches, gels, and lotions) is increasing. One vaginal preparation, the estradiol acetate ring, delivers a systemic dose of estradiol lasting for 3 months per ring.

Non-oral preparations avoid a first-pass hepatic effect. Therefore, they may produce fewer changes in lipids, clotting factors, and inflammatory markers. Data have indicated that transdermal preparations, when compared with oral estrogen, are associated with less risk of venous thromboembolism. [19]

EPT may be continuous (ie, daily administration of estrogen and progestogen) or continuous sequential (ie, daily administration of estrogen, with progestogen added on certain days).

See Tables 2-4 for summaries of the available preparations in the United States (adapted from The Endocrine Society). [113] In addition to the preparations listed in the tables, an oral estrogen-testosterone product (Estratest, Estratest HS; Solvay Pharmaceuticals, Inc, Marietta, GA) is available.

Table 2. Products for Estrogen Therapy (Open Table in a new window)

Oral Products

Composition

Product Name

Available

Doses, mg

Conjugated estrogens

Premarin

0.3, 0.45, 0.625,

0.9, 1.25

Synthetic conjugated estrogens

Cenestin

0.3, 0.45, 0.625,

0.9, 1.25

Enjuvia

0.3, 0.45, 0.625,

1.25

Esterified estrogens

Menest

0.3, 0.625, 1.25,

2.5

17β-estradiol

Estrace

0.5, 1.0, 2.0

Various generics

0.5, 1.0, 2.0

Estradiol

acetate

Femtrace

0.45, 0.9, 1.8

Estropipate (formerly piperazine

estrone sulfate)

Ortho-Est

0.625, 1.25, 2.5

Ogen

0.625, 1.25, 2.5

(0.75 mg estropipate =

0.625 mg estrone)

Transdermal and Topical Products

17β-Estradiol

Formulation

Product

Name

Estradiol

Delivery

Rate,

mg/day

Frequency

Matrix patch

Alora

0.025, 0.05,

0.075, 0.1

Twice

weekly

Climara

0.025, 0.0375,

0.05, 0.075, 0.1

Once

weekly

Esclim

0.025, 0.0375,

0.05, 0.075, 0.1

Twice

weekly

Menostar

0.014

Once

weekly

Vivelle

0.025, 0.0375,

0.05, 0.075, 0.1

Twice

weekly

Vivelle-Dot

0.025, 0.0375,

0.05, 0.075, 0.1

Twice

weekly

Reservoir

patch

Estraderm

0.05, 0.1

Twice weekly

Transdermal

gel

EstroGel

0.06%

0.035

Daily,

metered pump

Elestrin

0.06%

0.0125

Daily,

metered pump

Divigel 0.1%

0.003, 0.009, 0.027

(available dose packets

0.25, 0.5, or 1.0g)

Daily

Topical

emulsion

Estrasorb

0.05 (3.48g/day)

Daily

Transdermal

spray

Evamist (1.7%, metered dose)

1.53mg/spray

Initial:

1 spray/day

Maintenance:

1-3

spray/day

Vaginal Products

Formulation

Composition

Product Name

Dosing

Cream

17β-estradiol

Estrace

Initial:

2-4g/day for 1-2 wks

Maintenance:

1g 1-3 times/wk (1g = 0.1mg estradiol)

Conjugated estrogens

Premarin

Initial:

0.5–2g/day for 1-2 wk

Maintenance:

1-3 times/wk

(1g = 0.625mg estrogen)

Vaginal ring

17β-estradiol

Estring

Releases 7.5µg/day; 90 days

Estradiol acetate

Femring

(systemic)

Releases 0.05mg/day or

0.10mg/day; 90 days

Vaginal tablet

Estradiol hemihydrate

Vagifem

Tab containing 10.3 mcg estradiol hemihydrate = 10 mcg estradiol

Initial: 10 mcg tab intravaginally once daily for 2wk

Maintenance: 10 mcg tab intravaginally twice/wk (eg, Tues and Fri)

Table 3. Oral SERM/Estrogen Combination Products (Open Table in a new window)

Oral SERM/Estrogen Combination Products

Composition

Product Name

Available

Doses, mg

Bazedoxifene/conjugated estrogens

Duavee

20/0.45

Table 4. Progestogens Used for Hormone Therapy (Open Table in a new window)

Route

Drug, Formulation

Composition

Product Name

Available

Doses,

mg

Oral

Progestin, tablet

Medroxyprogesterone acetate

Provera, generics

2.5, 5, 10

Norethindrone

Micronor, Nor-QD, generics

0.35

Norethindrone acetate

Aygestin, generics

5

Norgestrel

Ovrette

0.075

Megestrol acetate

Megace, generics

20, 40

Progesterone, capsule

Progesterone

in peanut oil,

micronized

Prometrium

100, 200

Intrauterine

Progestin, system

Levonorgestrel

Mirena

20μg/day,

5y use

Vaginal

Progesterone, gel

Progesterone

Prochieve 4%

45mg/ applicator

Crinone 4%, 8%

45 or 90mg/ applicator

Table 5. Estrogen–Progestogen Combination Products (Open Table in a new window)

Regimen

Composition*

Product Name

Available

Doses &

Dosing*

Oral continuous cyclic

Conjugated estrogens (E) + medroxyprogesterone acetate (P)

Premphase

0.625mg E + 2.5 or 5.0mg P,

0.3 or 0.45mg E + 1.5mg P

Oral continuous combined

Conjugated estrogens (E) + medroxyprogesterone acetate (P)

Prempro

0.625mg E + 2.5 or 5.0mg P,

0.3 or 0.45mg E + 1.5mg P

Ethinyl estradiol (E) +

norethindrone acetate (P)

Femhrt

5µg E + 1mg P,

2.5µg E + 0.5mg P

17β-estradiol (E) +

norethindrone acetate (P)

Activella

1mg E + 0.5mg P,

0.5mg E + 0.1mg P

17β-estradiol (E) +

drospirenone (P)

Angeliq

1mg E + 0.5mg P

Oral intermittent combined

17β-estradiol (E) +

norgestimate (P)

Prefest

1mg E + 0.09mg P;

E alone for 3 days,

E + P for 3 days, repeat

Transdermal continuous combined

17β-estradiol (E) +

norethindrone acetate (P)

Combi-Patch

0.05mg E + 0.14mg P,

0.05mg E + 0.25mg P

Twice

weekly

17β-estradiol (E) +

levonorgestrel (P)

Climara Pro

0.045mg E + 0.015mg P

Once

weekly

* E = estrogen component; P = progesterone component


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