Pharm- hormone contraceptives

  1. what is the first oral contraceptive approved for CONTINUOUS use?
    what does this mean?
    and what is the trade-off?
    • Lybrel
    • This means no scheduled periods...and possibly a lower incidence of PMS, headaches, and anemia.     
    • But the tradeoff is possible breakthrough bleeding. 
    • Up to 50% of women have 7 or more days of bleeding or spotting during the first 3 months. This decreases with continued use.
  2. Lybrel contains:
    • Ethinyl estradiol 20 micrograms & Levonorgestrel 90 micrograms·         
    • No placebo  pills·        
    • No pill free period
  3. The first FDA-approved low dose COC taken 365 days a year:
  4. what are other progestin only meds? and what is their main ingredient?
    • Nor-QD, Nora-BE, Camila, Errin, Heather, Jolivette, Micronor
    • Contains norethindrone 0.35 mg
  5. with these drugs, Nor-QD, Nora-BE, Camila, Errin, Heather, Jolivette, Micronor, what is it imp to tell your pt?
    • these are less forgiving
    • XX has to take pill at the same time every day (c/in 2 hrs)
    • If you don’t, you have to use a back-up method or don’t have sex
    • Could be issues with compliance
  6. who are good candidates for these progestin only pills?
    • smokers over 35
    • postpartum
    • breastfeeding
  7. why should you not start an OC after giving birth?
    there's already an increased risk for clots
  8. ingredients and dose for Depro-Provera
    • (medroxyprogesterone acetate)
    • progestin only
    • 150 mg IM q 3 mo
    • also available sub Q
    • given by practitioner
    • have to confirm that pt is not preg before injection

  9. BBW for Depo-Provera
    BMD loss
  10. adverse effects for Depo-Provera
    • wt gain
    • menstrual irregularities
  11. how long does it take fertilization to return after taking Depo-Provera
    10 mo
  12. Progestin only contraceptives that are administered q 3 years and q 3 mo and 5 years
    • Depo-Provera (Medroxyprogesterone acetate 150 mg) IM injection q 3 MONTHS
    • Depo-SubQ Provera (Medroxyprogesterone acetate 104 mg) SQ injection q 3 MONTHS
    • Implanon (Etonogestrel) implantable subdermal rod- good for 3 YEARS
    • Mirena (Levonogestrel 20 mcg/day) IUD good for 5 YEARS
  13. how long can a copper IUD stay in?
    up to 10 years
  14. Loestrin 24 contains:
    • Contains 24 active 20 mcg ethinyl estradiol and 1 mg norethindrone acetate pills plus 4 iron placebo pills 
    • Advantage: shorter periods
  15. Yasmin 28 contains:
    • Contains 30 mcg EE and 3 mg Fourth generation progestin drospirenone
    • monophasic
  16. Yaz contains:
    FDA approved to treat:
    • Contains 20 mcg EE and 3 mg drospirenone
    • 24 active pills and 4 placebo
    • FDA approved to treat PMDD and acne
  17. Transdermal patch
    increased risk of:
    • once a week for three weeks, followed by one week off
    • Increase risk of thrombosis, but not as much as pregnancy risk of thrombosis
    • It may be prudent (do something else 1st choice)  to first consider low-dose oral estrogen contraceptives containing older progestins. This is esp true in XX who are at an increased risk for thrombosis
    • Too much estrogen…. 58 mcg. Over the max of 50
  18. Vaginal ring
    • Ring in three weeks and out for one week (or for four weeks with no ring-free week)
    • 15 mcg/day EE
    • .12 mg/day etonogestrel
  19. what are 2 brands for implantable contraception?
    site of implantation:
    duration of protection:
    • Implanon  and Nexplanon
    • Both are restricted distribution
    • It is a rod
    • A single 4 cm long implant with time-released etonogestrel
    • Implanted in the upper arm
    • Inserted and removed by a clinician
    • Provides up to three years of protection against pregnancy
  20. Adverse effects of hormone contraception:
    • Nausea
    • Bloating
    • Breakthrough bleeding
    • Acne- switch to a less androgenic protestin one
    • Hirsutism
    • Breast tenderness
  21. serious health risks for hormone contraception?
    • Blood clots
    • Heart attack
    • Stroke
    • ACHES= Abd pain, Chest pain,HA’s, Eye or visual changes, Severe leg pain or swelling
  22. BBW for hormone contraceptives:
    Smoking and cardiovascular events
  23. CI for COC:
    • Over 35 and smoker – patch and ring as well
    • Clotting disorders
    • History of DVT or PE
    • Migraine with aura or focal neurological deficit
    • Estrogen or progestin dependent cancer or
    • history
    • Strong risk factors for atherosclerosis
    • Active liver disease
    • Unexplained vaginal bleeding
  24. Emergency contraception options:
    • Plan B (levonorgestrel) OTC, 1 tab maximum efficacy w/in 72h, moderate efficacy w/in 120h (5 days)
    • Next Choice (levonorgestrel) OTC, 1 tab PO q12 x2 doses
    • Ella (ulipristal) it’s a Rx, diff mech, works by blocking progesterone receptors. takes asap, works up to 5 days of unprotected sex
  25. what is oxytocin (Pitocin)?
    A naturally occurring neuropeptide produced in the hypothalamus & secreted by the posterior pituitary
  26. where does oxytocin (Pitocin) act?
    Acts primarily on smooth muscle of the breast and uterus
  27. what does oxytocin lead to?
    Leads to let-down reflex to release milk from breast and uterine contraction during & after delivery   (+fb loop; once labor starts, uterine contractions caused by oxytocin cause more oxytocin release) so stronger contractions
  28. Kinetics of oxytocin (Pitocin)- do need to know
    • Administered IV or IM (cannot give po since it’s a peptide)
    • Half-life is 3 minutes
  29. indication of oxytocin:
    • Induction of Labor
    • Augmentation of Labor
    • Prevention & Treatment of Postpartum Bleeding
  30. Adverse effects of oxytocin?
    • Anti-diuretic effect
    • Uterine rupture (rare)
    • Abnormally high uterine tone *
    • Hypotension c/ rapid infusion
  31. CI of oxytocin:
    • Previous uterine rupture
    • hypersens. to drug/class/compon
    • if benefit-to-risk ratio favors surgery
    • if vaginal delivery contraindicated
    • cephalopelvic disproportion, significant
    • unfavorable fetal position or presentation
    • fetal distress w/o imminent delivery
    • total placenta previa
    • vasa previa
    • cord presentation or prolapse
    • uterine hyperactivity or hypertonicity
    • genital HSV infxn, active
    • cervical CA, invasive
    • inadequate progress w/ adequate contractions
  32. BBW for oxytocin:
    not for elective labor induction
  33. DI of oxytocin:
    • if you have 2 drugs that stimulate the uterus, there will be a synergistic effect
    • Sympathomimetics
    •      Increase risk of severe HTN
    • Carboprost tromewthamine
    •      Increase risk of uterine overstimulation
    •      May be given prior to carboprost
    • Dinoprostone vaginal insert
    •      Increase risk of uterine overstimulation
    •      Wait >30 mins after removal b4 using oxytocin
    • Dinoprostone vaginal gel
    •      Increase risk of uterine overstimulation
    •      Wait >6 hrs after last gel b4 using oxytocin
  34. Reproductive prostaglandins drugs:
    (will be given both names)
    • Misoprostol (Cytotec) PGE1
    • Dinoprostone (Cervidil) PGE2
    • Dinoprostone (Prepidil) vaginal gel
    • Carboprost (Hemabate) PGE2 alpha
  35. BBW for Misoprostol (Cytotec)
    • Preg
    • women of child bearing age
  36. BBW for Carboprost (Hemabate)
    and dosage route:
    • Appropriate use
    • IM
  37. Female reproductive effects of PG:
    • cervical softening
    • increased uterine contraction
  38. Indication for PGE1 and PGE2?
    • Labor induction
    • cervical ripening
  39. Indication for PGF 2 alpha?
    Treatment of postpartum hemorrhage (not 1st line)
  40. CI (says not gong to ask)?
    • severe asthma
    • glaucoma
    • MI
    • obstetric: unexplained vaginal bleeding; ruptured membranes; previous C-section
  41. Adverse effects of PGE?
    • Fever
    • Smooth muscle contraction of airways leading to an asthma-type rxn
    • Smooth muscle contraction of vasculature leading to HTN
    • Diarrhea, cramping, & nausea
  42. Analogs for gonadotropin hormone drugs:
    • Lupron
    • Naferelin (Synarel)
    • Danazol
    • RhoGAM
  43. analogs for gonadotropin hormone:
    • interact with the gonadotropin-releasing hormone receptor resulting in the release of FSH and LH from the pituitary
    • Initially there is an increase in FSH and LH secretion.
    • Prolonged activation of GnRH receptors thought to lead to receptor down-regulation & a decrease in FSH and LH
    • Initially an increase then a decrease. Thought to be due to a down regulation of receptors
  44. Indication for analogs for gonadotropin hormone:
    • Endometrosis
    • Central Precocious Puberty
    • Premature ovulation prevention (off-label)
    • Palliative treatment of advanced prostate cancer
  45. How does Lupron work?
    • Stops signals from pituitary gland to the ovary
    • There is first an increase in symptoms but then it starts to work
    • Less LH and FSH, so there is less estrogen produced
    • Initially, increase in GnRH --> increase LH & FSH --> increase estrogen, THEN YOU DECREASE IT, down regulation of receptors
  46. Facts about GnRH:
    _____  oral activity
    exhibit ___    ____ clearance
    available as _____ and _____ formulations (slow release)
    side effects:         due to:
    Preg Category:
    • poor oral activity
    • exhibit rapid metabolic clearance
    • available as injection and depot formulations (slow release)
    • side effects are menopausal like (due to the low levels of estrogen) ; also thinning of bones
    • Category X
  47. Leuprolide (Lupron Depot)
    route of administration:
  48. what can happen when Lupron Depot is used alone?
    • Bone thinning
    • Hot flashes
  49. what type of therapy can help with SE?
    • add-back therapy
    • Therapy given that is enough to prevent the SE, but not so much that we’re back to where we started. Minimize SE and maximize treatment
  50. Lupron Depot 4 month and 6 month indication:
    Advanced prostate CA, palliative
  51. Lupron Depot-Ped indication:
    Central precocious puberty
  52. Lupron Depot-Ped 3 month indication:
    CA, pallative
  53. Eligard (SC) dose & indication
    • 7.5 mg SC q mo
    • advanced prostate CA
  54. Naferelin (Synarel) indication:
    • Endometriosis - 1 spray in one nostril bid for 6 mo
    • Central precocious puberty- 2 sprays in each nostril (IEN) bid
  55. SE of Naferelin (Synarel)
    menopause like
  56. MOA of Naferelin (Synarel)
    inhibits gonadotropin (FSH & LH) release, suppressing steroidgenesis
  57. CI of Naferelin (Synarel)
    • Preg
    • undiagnosed vaginal bleeding
  58. Danazol (Danocrine)
    a synthetic androgen
  59. Danazol (Danocrine) indications:
    • endometriosis
    • fibrocystic breast dz
  60. MOA of Danazol (Danocrine):
    suppresses LH and FSH
  61. CI of Danazol (Danocrine):
    • pregnancy
    • breastfeeding
    • undiagnosed vaginal bleeding
    • significant renal & hepatic impairment
  62. BBW for Danazol (Danocrine):
    • can cause contraceptive failure;
    • use non-hormonal contraception during treatment
  63. Rho D immune globulin (RhoGAM) indication:
    Rh-incompatible preg; Rh-incompatible transfusion
  64. CI for RhoGAM:
    Rh-positive pts
  65. MOA of RhoGAM:
    • exact mechanism unknown. 
    • Suppresses the immune response of Rh-negative patients to Rh-positive RBCS
  66. What does it mean to be Rh-negative?
    • you don't have a certain protein ("D antigen" or the Rh factor) on the surface of your red blood cells
    • If you do have it, you're Rh-positive.
  67. When is being Rh-negative a problem? and why?
    • usually not a problem during 1st preg
    • prob= if 2nd preg with Rh-positive man or during transfusions
    • In pregnancy, if the mother is carrying an Rh-positive baby (from the father) & she is Rh-negative, the mother’s immune system will produce antibodies against the baby’s foreign Rh-positive blood. 
    • The mothers immune system attacks the baby's RBC's leading to potential hemolytic dz of the baby
  68. How does RhoGAM work?
    • RhoGAM  contains antibodies to the Rh factor
    • RhoGAM is injected into the muscle of an Rh-negative mother
    • This results in antibodies that circulate in the mother’s bloodstream which protect against Rh-positive red blood cells from the fetus.
    • The mother’s immune system does not need  to respond further.
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Pharm- hormone contraceptives
Pharm- hormone contraceptives- part 2