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DERS (endo/repro pharm) > L43- Contraceptives (general + oral) > Flashcards

L43- Contraceptives (general + oral) Flashcards

1
Q

(1) = most common goal of contraception

(2) are the other goals

A

-*prevention of pregnancy

  • menstrual cycle regulation
  • reduction of premenstrual symptoms
  • Acne Tx
  • Hirsutism (excess androgens)
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2
Q

(1) types of OCPs

(2) and (3) are the major general approaches

A

1- combined OR progestin-only

2- preventing ovulation
3- impairing implantation

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3
Q

describe mechanism of preventing ovulation

A

1) give estrogen
2) stabilize (prevent fluctuations) of estrogen levels
3) suppress FSH, LH release

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4
Q

describe mechanism of impairing implantation

A

give progestin –> maintains elevate progesterone levels:

  • thickens cervical mucus –> prevents sperm penetration
  • induces changes in endometrium –> impairs implantation
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5
Q

list estrogen oral contraceptives

A
  • ethinyl estradiol

- mestranol (prodrug –> ethinyl estradiol)

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6
Q

list progestins

A 
norethindrone
norgestrel
levonorgestrel
desogestrel
norgestimate
drospirenone
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7
Q

describe the non-progesterone activity of progestin

A

variable Androgenic activity:

  • levonorgestrel, norgestrel: highest
  • norethindrone: 2nd
  • desogestrel, norgestimate: 3rd gen.
  • drospirenone: antiandrogenic
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8
Q

describe oral contraceptive preparations

A

Monophasic: fixed dose estrogen and progestin in each active pill

Biphasic, Triphasic: variable proportions one or both hormones

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9
Q

Biphasic and Triphasic OCP preparations have the following advantages over Monophasic:

  • (T/F) more efficacious
  • (T/F) less amount and monthly dosing
  • (T/F) less AEs
  • (T/F) hormone levels more closely related to changes in menstrual cycle
A

1- F
2- T, reduced progestins
3- T, related to dec amount / dose
4- T

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10
Q

name most common combined OCP and discuss most common dosing

A

35 µg ethinyl estradiol (or less, aka ‘low dose’) + progestin

One mo: 21 hormonal pills, 7 pill placebo (consecutive- allows withdrawal from bleeding)

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11
Q

describe the type of combined OCP dosing regimens

A

Common: 21 hormonal days, 7 placebos

Extended Cycle: 84 hormonal days, 7 placebo –> only 4 menstrual cycles per year

Continuous: 21 hormonal days, then 4-7 reduced dose days

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12
Q

list the many benefits of combined OCPs

A
  • reduced risk endometrial, ovarian cancer
  • improve menstruation regulation
  • breast disease relief
  • ovarian cyst prevention
  • reduced risk of symptomatic PID
  • acne control
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13
Q

OCPs have many AEs, (1) are the main concern limiting long-term use. (2) is an adjustment that have greatly reduced AEs.

A

1- CVS toxicity

2- reduced dosage

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14
Q

________ OCP AEs can improve spontaneously by the third cycle

A
  • nausea
  • bloating
  • breakthrough bleeding
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15
Q

________ most common OCP AE

A

breakthrough bleeding (vaginal spotting)- more w/ low estrogen doses –> stabilizes endometrium

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16
Q

describe HAs as an OCP AE

A

-usually mild, transient

  • migraine maybe associated with CVA
  • -> indication to stop OCP
17
Q

OCP AEs:

  • (1) positive hormone effects
  • (2) negative hormone effects
  • inc (3) production
  • (4), an over effect of hormones administered
  • decreases the incidences of (5)
  • a few patients with (6) disease may need to stop
A

1- Androgenic progestins –> acne, oily skin, hirsutism –> switch to less or non-androgenic progestin

2- progestins –> insulin resistance (competes for receptor) –> therefore low progestin content to avoid hyperglycemia

3- estrogen –> melanocyte production–> melasma

4- amenorrhea

5- endometrial and ovarian cancer

6- depression

18
Q

OCP cardiac AEs:

  • increases (1) production –> increasing risk of (2) events in general
  • (3) name the (2) events
  • (4) are the precipitating risk factors
A

1- Estrogen –> inc factor VII, factor X, fibrinogen

2- thromboembolic events

3- thromboembolism, thrombophlebitis, HTN, MI, cerebral thrombosis

4- obesity, smoking, HTN, DM, >35 y/o

19
Q

OCP AEs: Liver Enzyme (induction/inhibition) is the main concern, explain

A

drugs that induce CYP450:

  • *inc estrogen metabolism
  • rifampin mainly (+ the others you known)
20
Q

OCP AEs effect on Antibacterials

A

Ethinyl estradiol –> undergoes bile excretion –> hydrolyzed by intestinal bacteria –> active drug reabsorption

  • if given Antibiotic –> dec estrogen levels may occur
  • some antibiotics dec OCP efficacy
21
Q

list the ABSOLUTE OCP contraindications

A
  • pregnancy
  • > 35 + smoking (15 cigs)
  • surgery or immobilization injury
  • thrombophlebitis, thromboembolic disorders
  • stroke, CAD

-breast CA, estrogen dependent CA, benign/malignant liver tumor

  • vaginal bleeding, uncontrolled HTN, DM + vascular disease
  • migrains w/ aura
  • active hepatitis
22
Q

list the RELATIVE OCP contraindications

A
  • migraine w/o aura
  • lactation
  • HTN, DM
  • Heart and Kidney disease
  • gallbladder disease, cholestasis during pregnancy
  • SCD
23
Q

Progestin Only Pills:

  • (1) formulation
  • (2) efficacy compared to combined OCP
  • (3) benefits
  • (4) disadvantages
A

(impairs implantation)
1- norethindrone, norgestrel (not used in US)

2- less –> only blocks 60-80% of cycles

3- NO thromboembolic events + dec dysmenorrhea, des blood in menstruation, dec PMS Sxs

4- bleeding / spotting

DERS (endo/repro pharm) (13 decks)

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