Contraceptives Flashcards

1
Q

Contraceptives work by

A
  1. Supressing
    1. Ovulation
    2. Gametogenesis
  2. Interfering with gestation
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2
Q

Major classes of contraceptives

A
  • Combined oral contraceptives
  • Progestin only
    • less commonly used
  • Transdermal patch
  • Vaginal ring
  • Dermal implants
  • Intrauterine device
  • Postcoital
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3
Q

Major Estrogen analogues

A
  • Ethinyl estradiol
  • Mestranol
    • Pro-drug
    • 50% metabolized into ethinyl estradiol
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4
Q

Progestins

A
  • Medroxyprogesterone
  • Northindrone
  • Etonogestrel
  • Levonogestrel
  • Norelgestromin
  • Norgestral
  • Norgestimate
    • the only one without ANDROGENIC activity
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5
Q

Combined oral contraceptive

Monobasic

A

Constant dose estrogen and progestin

  • adminstered daily for 21 days strating from day 5 of cycle
  • During the last 7 days, this drug is substituted for a placebo and the drug can be withdrawn
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6
Q

Combined oral contraceptives

Tribasic

A
  • Constant estrogen
    • Ethinyl estradiol- 30µg
    • Used to momic the menstrual cycle
  • Variable Progestins
    • Norgestrel
      • 1-6 days (50µg)
      • 7-11 days (75µg)
      • 12-21 days (125µg)
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7
Q

Progestin only pills

Composed of

A

Norethindrone or norgestrel

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8
Q

Progestin only pills

Effectiveness

A

Less than combied oral contraceptives

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9
Q

Progestin only pills

Associated with

A
  • Iregular menstrual bleeding
  • Limited patients acceptance
    • anxiety of getting since its less effective
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10
Q

Progestin only pills

Preferential use

A
  • Breast feeding
    • Progestin does NOT prevent milk production
    • Estrogen does
  • Intolerable to estrogen
  • Smokers with existing cardiovascular complications
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11
Q

Transdermal patch composed of

A

Ethinyl estradiol and Norelgestromin

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12
Q

Transdermal patch applied to

A

The abdomen for 3 weeks. Stop for a week (bleed) and then again

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13
Q

Transdermal patch

Total estrogen exposure

A

60%> than oral contraceptives (combined)

  • Because there is no first pass metabolism
  • Less effective in obese females because there is more fat
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14
Q

Vaginal rings are composed of

A

Ethinyl Estradiol and Etonogestrel

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15
Q

Vaginal rings application

A

Taken for 3 weeks. Stopped for a week

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16
Q

Vaginal rings

Cons

17
Q

Progestin implants composed of

A

Etonogestrel

18
Q

Progestin implants adminstered

A
  • 4cm capsule
  • Placed in the SubQ tissue of upper arm
  • Releases progestin for 3 years
  • If removed, effects are reversed within a month
19
Q

Progestin itrauterine device composed off

A

Levonor gestrel-releasing intrauterine system

  • maintains contraception for 5 years
20
Q

Progesrtin intrauterine device contraindicated in

A
  • Pelvic inflammatory disease
  • Ectopic pregnancy
21
Q

Levonor-gestrel (0.75mg)

A
  • Post coital
  • Adminstered 48-72 hours post coitus
  • 2 doses 12 hours apart
22
Q

Ethinyl estradiol (100ug) and 0.5mg L gestrel

A
  • Combination
  • 2 doses 12 hours apart
  • within 48-72 hours
23
Q

Mifepristone and Misoprostol

A

Mifepristone (RU 486)

  • Progestin receptor blocker
  • may induce abortion

48 hrs later…

Misoprostol

  • prostaglandin receptor analogue
24
Q

MOA

A
  • Supress ovulation
    • Estrogen inhibits LH,FSH therefore no LH surge
    • Estrogen decreases pituitary response to GnRH
  • Progestin analogue
    • Increases thickness of cervical mucose
      • Less permeable to sperm
    • Endometrium less receptive to ovum
    • Inhibits tubular peristalsis
25
Side effects
* CV * Thromboembolism * Thrombophlebitis * MI * Metabolic * Glucose intolerance * Predisposes to DM * conjugated estrogen as replacement decreases risk of T2DM * Weight gain * Serum lipids * E (analogue) decreases LDH and increases HDL * Progesterone increased LDH and decreases HDL * Gallblader * Primarily with estrogen * Increases cholesterol in acid causing stones
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CI
* CV * Thromboembolic disease * Estrogen dependent neoplasm * Liver disease * Preganncy * Over 35 and heavy smoker
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Health benefits
* Uterine fibroids * Functional ovarian cysts * Iron deficiency anemia * Decreases * Ovarian cancer * Endometrial cancer * Acne
28
Drugs that decrease effectiveness of contraceptives
* Rifampicin * Phenytoin * Carbamazepine * Chronic alcohol Because they induce cyp450
29
Drugs that increase effectiveness and SE of contraceptives
* Decrrease Clearance * Warfarin * Theophyline * Inhibit cyp450 * Ketoconazole * Acetominephen
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Gossypol
* Male * decreases spermatigenesis by destroying the cells that produce them * Serious SE * Hypokalemia * severe muscle weakness
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Testosterone enanthate and oral levenogetrel
* (TE)Adminstered IM * Decrease spermatogenesis by 60% * SE * acne * weight gain * prostate size * Polycythemia
32