Prescription Therapies Flashcards

(52 cards)

1
Q

Types of contraception

A

-despite decline in fertility during peri meno, pregnancy is still possible until menopause is reached
-hormone contraception helpful for sxs for perimeno and in cont pregnancy prevention
-long-active, reversible contraceptive methods (i.e. copper IUD) one of the four levonorgestrel-releasing intrauterine systems (LNG-IUS), and the etonogestrel subdermal implant provide long-term protection from pregnancy & tx AUB

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2
Q

Types of contraception (cont)

A

-combo estrogen-progestin contraceptives (pills, patch, ring) are only appropriate for healthy, lean, nonsmoking perimeno women; contraindicated in women aged 35yo who smoke, other potential contraindication include HTN, DM, obesity, other comorbidities
-CDC guidelines through US selected practice recs for contraceptive use (SPR) and the US Medical Eligibility Criteria for Contraceptive Use (MEC)

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3
Q

nexplanon

A

-etonogestrel subdermal implant
-a progestin (synthetic progestogen)

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4
Q

LNG-IUS

A

-levonorgestrel-releasing intrauterine system
-a progestogen
-can provide long-term protection from pregnancy & treat AUB
-Skyla 13.5mg - 3 yrs
-Kyleena 19.5mg - 5 yrs
-Liletta & Mirena 52mg - 5-7 yrs

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5
Q

skyla

A

-LNG-IUS contraception
-13.5mg; 3yrs
-may be better options for nulliparous or if smaller cervix/uterus
-AE: irregular spotting+, subsides, no menses 13% @1yr

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6
Q

kyleena

A

-LNG-IUS contraception
-19.5mg; 5yrs
-similar size as 13.5mg device
-AE: irregular spotting+, subsides, no menses 19% @1yr

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7
Q

mirena & liletta

A

-LNG-IUS contraception
-52mg; 5-7yrs
-for heavy menses, endometriosis pain (off label), endometrial hyperplasia/bleeding w ET (off label)
-AE: irregular spotting+, subsides, no menses 19% @1y, 37% @3y

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8
Q

copper T380A

A

-IUD contraception
-10-12yrs
-incr cramping/menses flow

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9
Q

intrauterine contraception

A

-safe, highly effective, convenient long-term contraception, office procedure
-risk for uterine perf is 1:1000 insertions (6x worse if breastfeeding)
-expulsion rates ~10% over 3yrs

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10
Q

progestin-only contraceptives

A

-best for perimeno who cannot have estrogen dose
-safer alternative for smokers +35yo, women w HTN, and hx of VTE
-IUD, subdermal implant

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11
Q

progestin-only contraception injection

A

-depot MPA
-150mg buttock or UE q3 mo
-some wt gain, fertility return 12-18mo delay
-AE: irregular spotting+, no menses by 4th injection, lower BMD
-alternative: Norethindrone (Aygestin) 200mg IM q2mo

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12
Q

progestin-only contraception oral

A

-nortehindrone 0.35mg daily
-good for perimeno; needs to be taken same time daily
-no hormone-free (inactive) pills
-unscheduled bleeding can happen

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13
Q

combo (estrogen-progestin) contraceptives

A

-mostly OCs, transdermal patch, vaginal ring
-safe, effective for midlife women healthy, lean, and do not smoke
-AE: VTE, unscheduled bleeding
-several OC forms based on 24/4 regimen (better ovarian follicular activity suppression) vs traditional 21/7
-ultralow doses available

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14
Q

combo (E-P) contraceptives (cont.)

A

-drospirenone differs from other synthetic progestins (derived from 17A-spironolactone) so has mild antimineralocorticoid effects
–> approved for tx premens dysphoric disorder when combined w ethinyl estradiol (EE)
-most OCs include EE for estrogen
-2 others: estradiol valerate and dienogest - approved for contraception and heavy menses bleeding
-extended OC formulations result in less-than-monthly withdrawal bleeding and are equally as effective and safe –> continuing low-dose EE during inactive pill periods or discontinuing active tablets 3 days can reduce unscheduled bleeding w extended-cycle regimens

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15
Q

emergency contraception

A

-taken after sex to prevent pregnancy, meant for occasional use bc other methods more reliable
-72-120hrs after sexual intercourse
-most effective form is copper IUD (99%), inhibits fertilization & implantation
-progestin-only (POP) uses LNG as two 0.75mg tabs taken 12h apart or as a single 1.5mg dose which reduces pregnancy by 88%
-POP EC available OTC wo rx
-ulipristal acetate can be used up to 5 days after unprotected sex & is rx only; more effective than POP EC

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16
Q

noncontraceptive benefits of OC

A

-restores regular menses
-decreased dysmenorrhea
-reduces heavy menses
-reduces pain a/w endometriosis (continuous use of OC)
-suppression of VMS
-enhanced BMD & possible prevention of osteoporotic fxs
-decreased need for bx for benign breast disease
-prevention of epithelial ovarian & endometrial malignancies
-improves acne that may flare up with perimeno

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17
Q

transitioning from hormone contraception to HT

A

-individualization
-may cont contraception until typical age of meno (52yo) or mid-50s, when women will likely reach meno (90% by 55yo)
-can transition from OCs to HT if still symptomatic
-as low-dose OCs have higher hormone levels than HT, hot flashes may reappear transiently

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18
Q

ET HT

A

-unopposed estrogen for postmeno who have undergone hysterectomy or in low doses for women w vaginal sxs regardless of prescence of uterus

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19
Q

EPT HT

A

-for postmeno w uterus
-progestogen reduces risk of endometrial adenocarcinoma bc of unopposed estrogen

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20
Q

estrogen agonist/antagonist therapy HT

A

-SERM
-for postmeno w uterus who prefer a progestogen-free option
-has similar effect to progestogen on the uterine lining

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21
Q

conjugated equine estrogens (CEE)

A

-type of ET
-on the US market >65yrs now
-most used in RCTs
-more is known about efficacy and safety than any other estrogen product
-approved for prevention of osteoporosis

22
Q

synthetic conjugated estrogens (CE)

A

-type of ET
-US govt does not view as a generic equivalent to CEE; approved generic equivalent in Canada
-not approved for prevention of osteoporosis

23
Q

estradiol

A

-type of ET
-mostly widely used estrogen in Europe
-only estrogen available in a govt-approved, bioidentical formulation
-approved for prevention of osteoporosis

24
Q

esterified estrogens

A

-type of ET
-oral products of synthetic estrogen mixtures containing 75-85% sodium estrone sulfate (E1S)
-not indicated for osteoporosis

25
estropipate
-type of ET -oral forme of estrone sulfate that has been solubilized and stabilized by piperazine -approved for prevention of osteoporosis
26
ethinyl estradiol
-type of ET -widely used in combination contraceptives
27
oral ET administration
-most widely used form in North America -bc of first-pass uptake & metabolism in the GI & the liver -->incr HDL cholesterol, a/w 25% incr triglycerides; incr hepatic globulins, coagulation factors, & some inflammatory markers; decr E-selectin, which may affect CAD
28
vaginal ET administration
-cream, tablet, insert, rings (low dose for local therapy & two higher doses for systemic therapy) available -small amounts of E administered locally are effective for treating GSM -endometrial protection is not needed w local doses of estrogen -women w uterus using one of the synthetic rings need endometrial protection (add progestogen
29
transdermal/topical ET administration
-patch, gel, spray, emulsion forms available -not subjected to first-pass hepatic metabolism -a/w more stable serum levels -minimal effect on sexual functioning -risk of skin-to-skin transfer of small amounts -some studies have shown incr in VTE & stroke w oral ET but not transdermal -stroke & VTE events were comparable across oral, transdermal, & placebo groups in the Kronos Early Estrogen Prevention Study (KEEPS)
30
micronized progesterone (MP)
-type of PT -compound identical to endogenous progesterone -prometrium is the only FDA-approved bioidentical progestogen -contraindicated in women w peanut allergy -bedtime dosing advised bc of sedating effects
31
progestin
-type of PT -synthetic products w progesterone-like activity -classified into 2 groups based on structure -1) chemical structure similar to progesterone: MPA (medroxyprogesterone acetate) most commonly used & studied in the US for endometrial protection -2) chemical structure similar to testosterone: more potent than those structurally similar to MP or progesterone
32
Continuous-cyclic (sequential) EPT administration
-daily estrogen w progestogen added cyclically for 12-14 d/mo -80% of women will experience bleeding w progestogen withdrawal
33
Continuous-cyclic (sequential) LONG-cycle EPT administration
-daily estrogen w progestogen added 14 d/2-6mo -reduces withdrawal bleeding episodes but results in heavier, longer bleeding -not recommended as standard therapy -requires endometrial monitoring
34
Continuous-combined EPT administration
-daily estrogen and progestogen -low rates of endometrial hyperplasia -higher rates of amenorrhea -decreased breakthrough bleeding after 2yrs
35
Intermittent-combined EPT administration
-daily estrogen w progestogen dose intermittently administered in cycles of 3 d on, 3 d off -1yr clinical trials have shown amenorrhea rates of 80% & favorable safety profiles
36
ET w estrogen agonist/antagonist
-tissue-selective estrogen complex (TSEC) -daily estrogen w daily selective estrogen-receptor modulator (SERM) -approved for tx of VMS and prevention of osteoporosis -amenorrhea rates similar to placebo -safety profile comparable to placebo
37
Alternative progestogen options
-progestin-containing IUD and progesterone vaginal gel -potentially may provide endometrial ca protection -long-term efficacy data is needed
38
Contraindications to HT
-undiagnosed abnormal genital bleeding -known, suspected, or hx of breast ca, except in appropriately selected patients being treated for metastatic disease or w oncology involvement -suspected estrogen-dependent neoplasia -active or history of DVT, PE -active or recent (w/in past year) arterial thromboembolic disease -liver dysfunction or disease -known or suspected pregnancy -known hypersensitivity to ET or EPT -porphyria cutanea tardis
39
Potential AE of HT
-uterine bleeding (starting or returning) -breast tenderness (sometimes enlargement) -nausea -abdominal bloating -fluid retention in extremities -changes to the shape of the cornea (sometimes leading to contact lens intolerance) -headache (sometimes migraine) -dizziness -mood changes w EPT, particularly w progestin -angioedema -gallstones, pancreatitis
40
Timing of HT initiation
-possibly less risk a/w HT use and potential CHD benefit if initiated closer to the time of menopause -in contrast, HT use initiated further from menopause may be harmful -per WHI: absolute risk of CHD was lower in younger, recent postmeno; MI risk incr during first year of EPT in older women, use of HT w/in 10yrs of menopause onset was a/w lower CHD risk than if started >20yrs from LMP; women 50-59yo in the ET arm had more favorable all0cause mortality & fewer MIs -Early Estrogen Prevention Study & the Early Versus Late Intervention Trial With Estradiol also showed safety of HT use initiated early in menopause
41
Monitoring HT
-annual return visits - more frequent visits for new starts or those with AES -annual mammogram -endometrial sampling is not required unless postmeno bleeding develops -clinical goal: use appropriate HT dose, duration, regimen, route of admin; periodic evaluation
42
Stopping systemic HT
-decision should be individualized on the basis of severity of sxs & risk-benefit ration considerations -approximately 50% of women will experience recurrence of sxs w discontinuation -low-dose, local ET may be continued as long as vaginal sxs are present
43
Bioidentical HT
-marketing term not recognized by FDA -hormones that are chemically identical to the hormones produced by the ovaries during the reproductive yrs -term used for custom-compounded HT by compounding pharmacies - these are not FDA approved -several FDA-approved preparations on market (estradiol pills, patches, gels, sprays, vaginal ring) and oral micronized progesterone
44
Pros of custom-compounded HT formations
-allows individualized dosing & combinations of therapy -allows for different modes of administration: subdermal implants, sublingual tablets, rectal suppositories, nasals sprays -products can be prepared so binders, fillers, dyes, preservatives, or adhesives
45
Cons of custom-compounded HT formulations
-do not have to undergo FDA approval -not FDA regulated - doesn’t require proof of claim & are not held to same standard of manufacture -often not covered by 3rd party payers -not found to be safer than FDA-approved formulations in clinical trials; may even have harms a/w unknown pharmacokinetics -lack of evidence of efficacy superior to FDA-approved products -concerns about purity & potency -lack of monitoring AEs
46
Bioidenticals: 2020 NASEM Recs
-July 2020 National Academy of Sciences, Engineering, & Medicine (NASAM) issued report that assessed clinical utility of compounded bioidentical hormone therapy (cBHT); recs: - restrict use of cBHT to certain situations such as ppl w allergies, unavailable doses in FDA-approved products, or testosterone for women w sexual dysfunction - improved education for prescribers & pharmacists who market, prescribe, compound, & dispense cBHT preparations - expending & improving oversight & review of compounding pharmacies - collection & disclosing info on conflicts of interest - the evidence base on safety, effectiveness, & use of cBHT preps should be strengthened & expanded - patient preference is not reason alone to use these products
47
SERM (selective estrogen-receptor modulators)
-aka estrogen receptor agonists/antagonists -exhibits both agonist & antagonist properties, depending on target tissue -lipid soluble properties -like estrogen, bind to hormone receptors ER-a & ER-b -naturally occurring: phytoestrogens - isoflavones, coumestans, prenylflavonoids; food sources: nuts, oil containing seeds, legumes, & soy-containing products
48
Tamoxifen
-SERM -potent antiestrogen in breast tissue -can reduce risk of invasive ER+ breast ca in high-risk women by 49% -estrogen agonist on bone, liver, & uterus
49
Raloxifene
-2nd gen SERM -estrogen agonist on bone -minimal effect on uterine endometrium -antiestrogen if effects on breast -lower risk of uterine ca, VTE, & cataracts compared w tamoxifen
50
Ospemifene
-SERM -estrogen agonist on vaginal tissue -FDA approved for treatment of moderate to severe dyspareunia -modes incr in hot flashes compared w placebo (9.6% vs 3.4%) -estrogenic-type response on endometrium but was not aw incr in hyperplasia or endometrial ca w/in first year -a/w slight incr risk hemorrhagic stroke & VTE (black box warning)
51
Bazedoxifene
-3rd gen SERM -estrogen agonist on bone -estrogen antagonist on breast & endometrial tissue -approved in Europe & Japan for tx of osteoporosis -combined w CEE is available in US for tx of VMS & prevention of osteoporosis
52
Toremifene
-SERM -r/t tamoxifen -FDA approved to treat advanced estrogen-sensitive breast ca & as adjuvant tx of early breast ca -weaker effect on endometrium compared w tamoxifen -may prolong QT interval in the heart (black box warning)