Hormones and Contraceptives Top Drugs

Conjugated estrogens • Estradiol (various forms) • Progesterone • Medroxyprogesterone • Testosterone • Combo OCPs (mono, bi, tri) • Ethinyl estradiol/etonogestrel • Levonorgestrel

Conj. Estrogens class and brand name

estrogen, premarin

Conj. estrogen MOA and Ind

MOA: female development and maintenance (breast tissue, vagina, uterine mucosa proliferation, bones, plate closure), works with LH/FSH cycle

Ind: menopause symptoms, vaginal atrophy, osteoporosis prevention, hypogonadism, affirming care

Conj. estrogen dosing and forms

Tablet

0.3-1.25 mg QD (continuous or cycle)

conj. estrogen kinetics

CYP3A4 and CYP1A2

conj. estrogen Interactions, P/CI

P/CI: caution or avoid with liver disease; no if pregnant; lactation okay, caution with elderly (clot risk); if E or P dependent cancer history; clot history; abnormal bleeding

I: levothyroxine

Conj. Estrogen ADE

Box warning: breast cancer, CV disease, endometrial cancer, dementia risk

Weight change, headache, N/D/V, mood change, increased BP, migraine, breast pain, swelling, hair growth

Conj. estrogen monitoring and counseling

M: T and Z score (bone health), Pap smear/pelvic exam, breast exam, hormone levels if needed

C: smoking increases CV disease risk; take with progesterone if uterus still present.

Levonorgestrel class and brand name

progestin

Oral: Plan B One-Step, New Day, and more

IUD: Kyleena, Litetta, Mirena, Skyla

Levonorgestrel MOA and IND

MOA:

Oral: delay ovulation and decrease chances of implantation

IUD: decrease likelihood of implantation, more localized effects

Ind: emergency contraception, contraception, heavy bleeding

Levonorgestrel forms and dosing

Tablet: 1.5 mg PO ASAP, or within 72 hours IUD: strength and timeframe vary, continuous low dose

Levonorgestrel Kinetics

no kinetics with levo.

Levonorgestrel P/CI

P/CI: not in pregnancy, okay in lactation, not to use with endometrial or cervical cancer, active STI/GU/or infection

levonorgestrel ADE

nausea and headache

levonorgestrel Counseling

C: if vomit within 2 hours, need to redose for effect, won’t work if already pregnant, not as effective if BMI over 30

IUD: if threads not visible, see doctor; may see spotting or breakthrough bleeding; max use 3-8 years depending on product

Ethinyl estradiol/etonogestrel class and brand name

estrogen and progestin

NuvaRing

Ethinyl estradiol/etonogestrel MOA and IND

MOA: same as other hormonal drugs

Ind: contraception

Ethinyl estradiol/etonogestrel Forms and dosing

vaginal ring with different dosing depending of brand

Nuvaring: Use for one cycle and discard on off week

Ethinyl estradiol/etonogestrel Kinetics

CYP3A4

Ethinyl estradiol/etonogestrel P/CI

P/CI: caution with liver disease, not with pregnancy, okay with lactation, avoid older adults because of CV risk; not to use with clotting history, uncontrolled HTN

Ethinyl estradiol/etonogestrel ADE

Box warning: do not use if smoker or migraines over 35 years old

Ethinyl estradiol/etonogestrel Counseling

C: if it comes out, wash with cool water and replace within 3 hours; if out for more than 7 days, need secondary protection

Testosterone class and brand name

Class: Androgen (CS3)
Brand names: AndroGel, Androderm

Testosterone MOA and IND

MOA: Male development and sex characteristics, hair growth, anabolic effects
Ind: Hypogonadism, gender-affirming care

Testosterone Forms and Dosing

Forms: Gel, solution, cream, various injectables
Dosing: Topical: 20-100 mg active ingredient (apply 1-3 pumps to clean, intact skin QD); Injectable: 50-100 mg IM q1-2 weeks

Testosterone P/CI and Interactions

P/CI: Avoid in pregnancy/lactation; caution/restrict in older adults unless hypogonadism; contraindicated in breast or prostate cancer (men)
Interactions: Warfarin (avoid combination)

Testosterone Counseling and Monitoring

Counseling: Do not apply to genitals; keep skin dry for 5-6 hours post-application; prevent skin-to-skin contact with others

Monitoring: LFTs, CBC, lipids, BP, weight, serum testosterone concentrations if needed

Testosterone ADE

Muscle gain, mood change, balding, increased BP, increased H/H, worsening BPH, PSA increase, gonadal atrophy, acne, CV disease, prostate cancer, POME (Aveed brand)

Estradiol brand name and class

estrogen

Estrace (oral)Alora, Climara, Minivelle, Vivelle-DOT,

Menostar (dermal)

Estradiol MOA and IND

MOA: most potent naturally occurring estrogen, major form in reproductive years, same effects on body as all estrogens Ind: osteoporosis prevention (not first line), hormone replacement, menopause, contraception

Estradiol forms and dosing

Tablet, patch, injectable

Oral: 0.5-2 mg QD (continuously in menopause, cycle if not)

Breast or prostate cancer, affirmative care: 1- 10 mg TID

Dermal: 0.014-0.0375mg/day QW or BW

Estradiol kinetics

patch is better absorbed

Estradiol P/CI and interactions

P/CI: caution or avoid with liver disease; no if pregnant; lactation okay, caution with elderly (clot risk); if E or P dependent cancer history; clot history; abnormal bleeding

I: levothyroxine

Estradiol ADE

Box warning: endometrial cancer risk if not progesterone-opposed (with uterus)

Estradiol Counseling and Monitoring

M: T and Z score (bone health), Pap smear/pelvic exam, breast exam, hormone levels if needed

C: smoking increases CV disease risk; take with progesterone if uterus still present.

Dermal: not on genitalia, keep below waistline, remove before MRI, clean/dry skin

Progesterone brand name and class

progestin and Pronetrium

Progesterone MOA and IND

MOA: makes endometrium secretory, stops gonadotropin production, stops follicle maturation and ovulation

Ind: prevent estrogen-caused cancer, secondary amenorrhea, help with infertility

Progesterone forms and dosing

Capsule, vaginal gel/insert

Cap: 200-400 HS 10-12 days each cycle

Gel: 45- 90 mg insert every other day x6 doses

100mg 2-3x/day after egg retrieval, and then continuous for 10-12 weeks

Progesterone kinetics

CYP3A4

Progesterone P/CI and Interactions

P/CI: caution if liver disease, caution in pregnancy and lactating, no use if abnormal bleeding, hormone-dependent cancer history, or clotting history

I: warfarin (monitor)

Progesterone ADE

Weight changes, breast pain, swelling, mood changes, amenorrhea, headache, N/V/D, drowsiness, breakthrough bleeding

Rare: cancer, clotting issues

Progesterone Counseling and Monitoring

C: bleeding should occur 3-7 days after last dose; if not, see dr; if vaginal dose: separate from other vaginal drugs 6 hours, take as prescribed

Medroxyprogesterone brand names and class

progestin

provera and depo-provera

Medroxyprogesterone MOA and IND

MOA: Same as progestin PLUS , some androgenic and anabolic effects noted (not estrogen activity)

Ind: abnormal bleeding, prevent estrogen-caused cancer, secondary amenorrhea, breast/endometrial cancer

Medroxyprogesterone forms and dosing

Tablet, injectable (depo)

5- 10 mg QD (certain days of cycle)

Medroxyprogesterone kinetics

CYP3A4 depo

Medroxyprogesterone P/CI and Interactions

P/CI: caution if liver disease, no use if pregnant, okay if lactating, do not use if hormone cancer history, clotting history, cerebrovascular disease

I: corticosteroids, warfarin (monitor)

Medroxyprogesterone ADE

Box warning: CV disorders, breast cancer, dementia risk, bone mineral density loss

Medroxyprogesterone Counseling and Monitoring

C: bleeding should occur 3-7 days after last dose; if not, see dr; if vaginal dose: separate from other vaginal drugs 6 hours, take as prescribed

Combo OCP (mono,bi,tri) brand name and class

estrogen and progestin, many brand names

Combo OCP (mono, bi, tri) MOA and IND

MOA: estrogen suppresses FSH and LH to stop the process; progestin suppresses LH to stop the process

Ind: contraception, some products approved for acne in females

Combo OCP (mono, bi, tri) forms and dosing

Big dose ranges, mono/bi/triphasic

1 tablet QD, or package directions

Combo OCP (mono, bi, tri) Kinetics

CYP3A4 (competitive inhibitor)

Inhibit: CYP1A2, CYP2C8,

Combo OCP (mono, bi, tri) P/CI and Interactions

P/CI: caution with liver disease

I: corticosteroids, antibiotics, warfarin

Combo OCP (mono, bi, tri) ADE

Box warning: smoking of 35+ yrs increases CV risk

Combo OCP (mono, bi, tri) Counseling and Monitoring

C: same day each day for best effect; if missing 2 doses in a row, no guarantee of effects