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pharmacology 2 > hormonal contraception > Flashcards

hormonal contraception Flashcards

(45 cards)

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1
Q

hypothalamus producing GnRH

A

produces it in a cyclical manner

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2
Q

GnRH acts on

A

anterior pituitary to make it produce FSH and LH

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3
Q

HPO axis

A

hypothalamo-pituitary-ovarian

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4
Q

FSH acts during

A

first half of the manstual cycle

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5
Q

LH acts during

A

2nd half of the menstrual cycle

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6
Q

FSH causes production of

A

oestrogen from granuloma cells in dominant follicle

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7
Q

LH causes production of

A

porgesterone>oestrogen

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8
Q

3 endogenous oestrogenen

A

E2 - 17b oestradiol, major
E1 - estrone, minor
E3 - oestriol, pregnancy

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9
Q

17b oestradiol E2

A

most abundant and potent

produced by ovarian granulosa cells

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10
Q

oestrone E1

A

produced by ovaries and adrenals

levels increase slightly after menopause

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11
Q

oestriol E3

A

placental - only in pregnancy

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12
Q

endogenous oestrogens are

A

18-carbon steroids
transported by SHBG
bind oestrogen receptors

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13
Q

oestrogen receptors

A

ERa and ERb
expressed redundantly in reproductive system and breast
expressed non-redundantly in CVS, skeleton, CNS and immune system - not reproductive effects of oral contraceptives
ERa/b are ligand activated transcription factors (target genes with EREs) - slow response time

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14
Q

ERa over expressed in

A

breast cancers
not ERb
anti oestrogen blocking ERa are widely used in breast cancer

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15
Q

oestrogen levels modulate

A

FSH and LH release
cyclical changes in uterus and breasts
induction of progesterone receptors

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16
Q

metabolic actions of oestrogen

A

increase bone mass by blocking bone resorption - why women are more susceptible to osteoporosis
improve TG profile - improve HDL:LDL ratio
increase coagulability - venous thrombosis embolism and stroke

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17
Q

progesterone

A

secreted mainly by the corpus luteum and placenta
secreted in the second half of the cycle
levels decrease before mestruation (unless pregnant)
transported by albumin and corticosteroid binding globulin CBG

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18
Q

progesterone receptor

A

ligand activated transcription factor expressed in female reproductive tract, breast and CNS

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19
Q

actions of progesterone

Study These Flashcards
A

prepare for/maintain pregnancy
uterine/cervical effects
- endometrium, decreased proliferation, increase secretory changes
- cervix - thickens and decrease secretions, decrease sperm penetration
- myometrium - decrease uterine excitability
- breasts - glandular development
- hypothalamus - decrease LH surge and GnRH release, block ovulation
- CNS - increase body temperature

20
Q

2 types oral contraceptives

Study These Flashcards
A
  • combined contraceptives (COCs) contain oestrogen and a progestogen
  • progestogen only contraceptives
21
Q

until recently, endogenous hormones were not used orally due to

Study These Flashcards
A

their extensive 1st pass hepatic metabolic - very low bioavailability

22
Q

combined oral contraceptives

Study These Flashcards
A

contain a synthetic oestrogen and a synthetic progestogen

23
Q

oestrogens used in the pilll

Study These Flashcards
A

ethinyloestradiol and mestranol

24
Q

synthetic oestrogens

Study These Flashcards
A

ethinylestradiol EE- derivative of estradiol, addition of ethinyl group to reduce hepatic metabolism and allow it to be taken orally
mestranol - pro-drug of EE - undergoes demethylation, less potent

25
synthetic progestogens
multiple - differentiations in potency and spectrum of activity 1st generation - ethisterone - significant androgenic effects: acne, hirsutism, weight gain, no longer used 2nd generation - norethisterone, levonorgestrel - reduced androgenic side effects 3rd generation - desogestrel, gestodene - reduced androgenic and lipid effects but increased thromboembolic effects
26
how does the combined pill work
inhibit ovulation - prevent release of FSH (follicle development) and LH (ovulation synergistic effect of oestrogen (FSH) and progestogen (LH) thickens cervical mucus - forms a barrier to sperm via progestogen effect thin endometrial lining - reduce endometrial receptivity to inhibit implantation
27
3 mechanisms of combined pill
inhibit ovulation thicken cervical mucus thin endometrial lining
28
efficacy of COC
>99% with perfect use effectiveness reduced by - compliance - delayed start of the next pack - decrease HPO suppression - missed pills - vomiting - decreases intestinal absorption - broad spectrum antibiotics (ampicillin) - decreases enterohepatic circulation (probably more a theoretical than a real problem) - CYP3A4 induction - griseofulvin, anti-epileptics (phenytoin, carbamazepine), TB drugs (rifampicin), st john's wort
29
regimens and dose of COC
21 days OC and 7 days placebo 7 days hormone free - withdrawal bleed (not a period) no biological reason for a withdrawal bleed and extended OCP regimens may increase compliance
30
COC formulations
``` monophasic - same daily dose of EE and progestogen phased regimens (biphasic and triphasic) - dose varies to mimic cyclical endogenous hormone secretion biphasic - constant EE, progestogen in 2nd half of cycle triphasic - increase EE in middle to decrease breakthrough bleeding plus stepwise increase in progesterone no contraceptive advantage ```
31
breakthrough bleeding
treat by increasing oestrogen or progesterone
32
nausea
treat by reducing oestrogen dose to take the pill at night with food
33
fluid retention, breast tenderness
treat by decreasing oestrogen dose
34
chloasma
treat by avoiding sun, use sun screen
35
androgenic and antiandrogenic side effects
ance depression, irritability and fatigue reduction in libido
36
enhanced coagulation
dose related risk metabolic side effect of oestrogen older contraceptives had more of a problem with this increases clotting - DVT, pulmonary embolism, MC, stroke increase risk in obesity, long haul travel and underlying genetic clotting abnormalities eg. factor 5 laden MI risk increases >35yo, smoker, hypertensive
37
breast cancer and oestrogen
oestrogen promotes breast cancer - early menarche, nulliparity, late age of 1st pregnancy, lack of breast feeding - all increases risk of breast cancer role of progestogen is more complex increased risk of breast cancer in usage of the pill reduction in risk when pill is stopped
38
cervical cancer risk
causal link not established | may be behavioural in origin - OC users more sexually active, use barrier contraceptive methods less, exposed to HPV
39
protective risk effects of COC
decreased ovarian risk, endometrial, colorectal decreased risk os long term - does not diminish when pill is ceased reduced risk of PID, salpingitis and ectopic pregnancy improvement in acne improvement in menstrual problems: cramps, heavy flow, endometriosis, premenstual syndrome, iron deficiency anaemia
40
contraindications of the COC
- pregnancy - history of VTE or Stroke - CVD - coronary artery disease, valvular disease - major elective surgery - stop 1 month beforehand - oestrogen dependant breast cancer sufferer - migraine with aura - increase stroke risk - hepatic disease - acute hepatitis, severe cirrhosis >35 years old, obese, smoker with HT and DM
41
progestogen only OC
minipill contain no oestrogen useful with COC is contraindicated or not tolerated
42
progestogen only OC mechanism of action
- inhibitor of ovulation due to inhibition of LH surge - thickens and decreases amount of servical mucous, impedes sperm penetration - endometrium thins - decreases implantation rate 30-40% of progestogen only OCs still ovulate, so less effective than combined OCs requires more meticulous compliance
43
minipill
progestogen only OC
44
long acting reversible contraceptives
LARCs IUDs, progestogen implants more effective reversible contraceptive 20x more effective than OC safe for most women, including adolescents, post partum, post abortion menstrual cycle disturbance is common, with irregular bleeding but decreased bleeding over time levonorgestrel IUD often decreases bleeding - used therapeutically
45
antisperm antibodies
some women naturally produce antibodies to sperm immunological infertility topically delivered trap >99.9% of sperm still in clinical trials

pharmacology 2 (19 decks)

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