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Endo-Repro Drugs > Womnen's Health Drugs > Flashcards

Womnen's Health Drugs Flashcards

1
Q

Tamoxifen

A
  • Selective Estrogen Receptor Modulator
  • Competitive partial agonist inhibitor of E2 at the ER in ER2+ breast cancer
  • Oral admin; T1/2 7-13 hrs; predominantly liver excretion
  • Breast CA tx in post-menopausal women and chemo-prevention in high risk women
    Adverse effects:
  • Hot flashes (low estrogen)
  • N/V
  • Partial ER agonist in the endometrium- elevates endometrial cancer risk
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2
Q

Raloxifene

A
  • Selective Estrogen Receptor Modulator
  • Competitive partial agonist inhibitor of E2 at the ER in ER2+ breast cancer
  • Doesn’t have any endometrial ER activity so it can be used as an osteoporosis treatment
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3
Q

Anastrozole & Letrozole

A
  • Aromatase inhibitors- prevent conversion of androstenedione to estrone and conversion of testosterone to estradiol which are both catalyzed by aromatase
  • Suppress plasma estrogen levels in post-menopausal women
  • No partial agonist activity; selective aromatase inhibition
  • Effective on some tamoxifen resistant breast tumors
    Adverse Effects: due to low estrogen
  • hot flashes
  • Vaginal dryness
  • N/V
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4
Q

Methotrexate

A
  • Folic Acid Antagonist
  • Highly effective against rapidly proliferating trophoblasts
  • Can use to cause abortion of ectopic pregnancy if it hasn’t ruptured
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5
Q

Magnesium Sulfate

A
  • Ca2+ antagonist, used for seizure prophylaxis in pre-eclampsia
  • IV admin or IM if seizing
  • Renal excretion (modify for renal damage from pre-eclampsia)
  • Avoid MgSO4 intox: ensure adequate urine output, check patellar/bicep tendon reflexes (Mg causes hyporeflexia while pre-eclampsia causes hyperreflexia), no respiratory depression
  • Reverse with IV Calcium Gluconate
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6
Q

Endometrial Cancer Treatment

A
  • Platinum agents (Cisplatin, carboplatin)
  • Paclitaxel
  • Doxorubicin
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7
Q

OCP Adverse Effects

A

Mild: Headache, nausea, mastalgia, edema
- Breakthrough bleeding
- Migraine exacerbation w/ estrogen withdrawal (contraindicated w/ aura)
- No withdrawal bleeding
Moderate: - Exacerbation of acne, hirsuitism and weight gain with androgenic progestins (L-norgestrel)
- Ureteral dilation and increased bacteruria
- More frequent/difficult to tx vaginal infections
- Amenorrhea after OCP cessation
Severe: - Venous thromboembolic disease (3x risk increase)
- MI risk w/ smoking, obesity, DM, Htn. or hyperlipidemia ESPECIALLY over 35 y.o.
- Increase stroke risk in women over 35 y.o. currently using OCPs
- Cholestatic Jaundice w/ progestin only agents, reversible and genetically based
- Depression

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8
Q

OCP Contraindications + Cautions

A
  • Contraindications: - Htn., migraine w/ aura, liver disease, gallbladder disease
  • Pt. w/ Hx of CVD, cerebrovascular disease or thromboembolic disease
  • Drugs that induce hepatic metabolism can increase estrogen/progestin metab and make them less effective
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9
Q

OCP Benefits

A
  • Reduce risk of ovarian cysts, ovarian and endometrial cancers and benign breast disease
  • Reduce ectopic preg. risk
  • Fe deficiency and RA less common
  • Relief of PMS, dysmenorrhea and endometriosis sx
  • Improvement of acne and hirsuitism (if not androgenic progestin)
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10
Q

Ortho Evra

A
  • Transdermal Patch (28 day cycle)

- Combo ethinyl estradiol + norelgestromin

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11
Q

Nuva Ring

A
  • Vaginal ring (28 day cycle)

- Combo ethinyl estradiol + estrongestrel

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12
Q

Implanon, Nexplanon

A
  • Progestin only subdermal implant- estrongestrel
  • Suppresses ovulation for 3 years, remove after 3 years
  • Peak serum concs. in first few weeks
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13
Q

Depo Provera

A
  • Progestin only injection w/ medroxyprogesterone
  • IM every 3 mo.
  • Long acting, shorter menses
    Adverse Effects:
  • Decreased bone density (contraindicated in osteoporosis)
  • Weight gain
  • Can’t self admin
  • Menstrual irregularities (50% of women stop)
  • Slow return of menses after stopping (18 mo. -2 yrs)
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14
Q

Mifepristone

A
  • Progesterone Rec. Antagonist (morning after pill)
  • Luteolytic effect
  • 99% effective w/in 72 hrs
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15
Q

Levongestrel (Plan B)

A

Progestin only, 0.75 mg BID for 1 day

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16
Q

Clomiphene

A
  • Selective ER modulator (SERM)- partial agonist at ERs
  • Selectively inhibits actions of stronger estrogens which reduces neg. feedback to increase FSH/LH and increase estrogen secretion
  • Stimulates ovarian function in women w/ amenorrhea
  • Single course induces single ovulation– 5 day course induces an initial rise in plasma LH/FSH after several days which is then followed by a 2nd rise in gonadotropin levels just prior to ovulation
    Adverse Effects: - hot flashes
  • N/V, anxiety, depression, fatigue
  • breast soreness, weight gain, heavy menses
  • ~10% incidence of multiple pregnancies
17
Q

Leuprolide

A
  • GnRH agonist
  • Controlled ovarian stimulation in IVF– shut down GnRH pulses then give exogenous hormones
  • Reserved for anovulatory women who don’t respond to less complicated tx
18
Q

Ceftriaxone

A
  • 3rd generation Cephalosporin
  • beta-lactam: bacteriocidal, inhibits bacterial cell wall synth
  • Only parenteral tx for gonorrhea
  • Always tx for chlamydia at same time w/ azithromycin or doxycycline
19
Q

Azithromycin

A
  • Macrloide, chlamydia tx

- Bacteriostatic, inhibits translocation (50S inhibitor)

20
Q

Doxycycline

A
  • Tetracycline analog, chlamydia tx

- Bacteriostatic, inhibits elongation (30S inhibitor)

21
Q

Metronidazole

Flagyl

A
  • Kills anaerobic bacteria and some protozoans
  • Pro-drug– activation requires pyruvate ferrodoxin oxidoreductase in susceptible microbes which reduces the NO2 group to form a toxic radical causing oxidative damage to DNA leading to fragmentation and cell death
  • Single oral dose of 2 g– more compliance, fewer GI side effects
  • > 95% cure rate when both partners are treated
  • If first does doesn’t work initiate 7 day course 500 mg BID; vaginal cream less effective
    Adverse Effects:
    Common- nausea, headache, dry mouth
    Infrequent- vomiting, diarrhea, vertigo, dysuria
    Rare- neutropenia, pancreatitis, CNS tox (ataxia, encephalopathy, seizures)
    Contraindications: - Alcohol (worsened N/V)
  • Caution w/ CNS disease b/c of CNS tox
  • Contraindicated in 1st trimester (preg category B)
  • Secreted in breast milk
22
Q

Acyclovir, Valacyclovir, Famiclovir, Peniclovir

A
  • Acyclovir + peniclovir: acyclic guanosine analogs that require a viral kinase for activation s/t they are selectively activated in infected cells
  • Valacyclovir: acyclovir pro-drug
  • Famiclovir: peniclovir pro-drug
  • Competitively inhibit viral DNA polymerase and cause chain termination after incorporation into viral DNA
  • Inhibit viral synthesis
  • Tx first episode w/ 7-10 day course, chronic suppressive therapy for recurrent infections
    Adverse Effects:
  • N/V, headache, diarrhea
  • Rare confusion, hallucinations and seizures w/ high dose valacyclovir

Endo-Repro Drugs (5 decks)

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