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Pharmacology > Drugs affecting fertility and reproduction 1 > Flashcards

Drugs affecting fertility and reproduction 1 Flashcards

1
Q

Estrogens - MoA

A

Hypertensive effect by increased angiotensinogen synthesis.
Thromboembolic effect by increased hepatic synthesis of clotting factors.
Gallbladder disease by increased cholesterol excretion in bile.

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2
Q

Estrogens - Clinical use

A

Primary hypogonadism, including cases caused by surgical oophorectomy, menopause

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3
Q

Estrogens - Contraindications and Special consideration

A

CONTRAINDICATED: pregnancy, uterine fibroids.

Use with caution if hepatic diseases, endometriosis, thromboembolic diseases, hypercalcemia

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4
Q

Estrogens - Adverse effects

A

Breast tenderness, headache, edema, nausea, vomiting, anorexia, change in libido
HT, thromboembolic disorders, gallbladder disease

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5
Q

Conjugated equine estrogens - Clinical use

A

HRT in postmenopausal women

Estrone can be adm IM

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6
Q

Conjugated equine estrogens - Special consideration

A

Hydrolyzed to estrone and equilin before absorption from the gut.
Converted in the liver to sulfate and glucuronide conjugates

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7
Q

Ethinyl estradiol and Mestranol - Clinical use

A

Oral estrogen-progestin contraceptives
Acne vulgaris
Dysmenorrhea

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8
Q

Micronized estradiol and Trandermal estradiol - Clinical use

A

HRT in postmenopausal women

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9
Q

Long-lasting ester of estradiol + Route of adm

A

Estradiol cypionate and Estradiol valerate

IM: both Oral: estradiol valerate

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10
Q

Estradiol valerate - Clinical use

A

Contraceptive, Heavy or prolonged menstrual bleeding

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11
Q

Estrogens

A 
Conjugated eqine estrogens
Ethinyl estradiol
Mestranol
Micronized estradiol
Vaginal estradiol tablets
Estradiol cypionate
Estradiol valerate
Transdermal estradiol
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12
Q

Progesterone esters

A

Suppress ovarian function in the treatment of dysmenorrhea, endometriosis, and uterine bleeding.

In HRT, the progesterone esters are used in combination with estrogens to decrease the incidence of estrogen-induced irregular bleeding and to prevent uterine hyperplasia and endometrial cancer.

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13
Q

Progesterone esters - Special consideration

A

Extend oral bioavailability and half-life of progesterone

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14
Q

Esters of progesterone + Route of dam

A

Megestrol - Oral
Hydroxyprogesterone caproate - IM
Medroxyprogesterone acetate - IM + oral

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15
Q

Hydroxyprogesterone caproate - Clinical use

A

Reduce the risk of preterm delivery in women with a history of at least one spontaneous preterm birth.

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16
Q

What is the progestin- only contraceptive?

A

Medroxyprogesterone acetate

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17
Q

Synthetic progestins

A 
Norgestrel
Desogestrel
Norgestimate
Norethindrone
Drospirenone
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18
Q

Which synthetic progestin is a spironolactone derivative?

A

Drospirenone

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19
Q

Synthetic progestins - are mostly derivatives of?

A

nortestosterone

20
Q

Synthetic progestins - MoA

A

Estrogenic, antiestrogenic and androgenic activities

21
Q

Synthetic progestins - Clinical use

A

Oral contraceptives

Dysmenorrhea, endometriosis, uterine bleeding

22
Q

Which synthetic progestin has more androgenic activity than other progestins?

A

Norgestrel

23
Q

Which synthetic progestins has less androgenic and more pro gestational activity?

A

Desogestrel and Norgestimate

24
Q

Which synthetic progestin has an intermediate androgenic potency?

A

Norethindrone

25
Q

Which synthetic progestin is an aldosterone antagonist?

A

Drospirenone

26
Q

Drospirenone - Special considerations

A

Antiandrogenic effect

Less incidence of weight gain, mood changes and acne

27
Q

Norgrestrel - Adverse effects

A

Increased incidence of acne, hirsutism, increased libido, oily skin.

28
Q

Drospirenone - Adverse effects

A 
Decreased BP (decreased salt and water retention).
In contraceptive: 2-3X increased risk of VTE compared to levonorgestrel (but still low risk)
29
Q

Estrogen - Progestin contraceptives - MoA

A

Synergistic suppression of ovulation, by feedback inhibition of GnRH secretion.
Estrogen component: Decreased FSH secretion (no maturation of follicle).
Progestin component: inhibit LH surge (no ovulation).
Delayed maturation of endometrium, development of viscous cervical mucus

30
Q

Estrogen - Progestin contraceptives - Clinical use

A

Contraceptives
Acne vulgaris
Dysmenorrhea

31
Q

Estrogen - Progestin contraceptives - Special consideration and Contraindication

A

For dysmenorrhea: treatment is started some days before menstruation. NSAIDs are alternative treatment for dysmenorrhea.
Smokers over 35 years should use other contraceptive methods.
Caution if gall bladder disease.
CONTRAIND: thromboembolic disease, history of MI, CAD, active liver disease, breast cancer, carcinoma of reproductive tract

Reduce incidence of endometrial and ovarian cancer. Does not increase the risk of breast cancer. Low risk of hepatic adenoma

32
Q

Estrogen - Progestin contraceptives - Adverse effects

A

Hypertension, thromboembolic disorders, gallstones
High dose: breast cancer
Increases Risk of stroke, MI, DVT
Increased Estrogen: breast enlargement, dizziness, dysmenorrhea, edema, headache, irritability, nausea, vomiting, weight gain (cyclic)
Decreased Estrogen: Atrophic vaginitis, continuous bleeding, early bleeding, hypomenorrhea, vasomotor symptoms
Increased Progestin: Acne, depression, fatigue, hirsutism, libido change, oily skin, weight gain (noncyclic)
Decreased Progestin: Dysmenorrhea, hypermenorrhea, late-cycle bleeding

33
Q

Estrogen - Progestin contraceptives - Interactions

A

Carbemazepine, phenytoin: increased hepatic metabolism of oral contraceptives (may cause contraceptive failure).
Antibiotics (penicillins, tetracyclines): Decreased enterohepatic cycling of contraceptives and decreased contraceptive effect.
Estrogen cause increased potency of cyclosporine, antidepressants, glucocorticoids + increase antagonize warfarin effect + increased hepatotoxicity of dantrolene

34
Q

Difference between Monophasic and Triphasic estrogen- progestin contraceptives

A

Monophasic: Same amount of progestin throughout cycle.

Triphasic: Increased amount of progestin after 7-14 days

35
Q

Monophasic estrogen-progestin contraceptives + Special considerations

A

Ethinyl estradiol + levonorgestrel: 84 days continuous use, then 7 inactive tablets.
Drospirenone + ethinylestradiol: Available for 21-day and 24-day regimens (latter less rates of contraceptive failure)

36
Q

Ethinyl estradiol + levonorgestrel - Clinical use

A

Menstrual suppression

37
Q

Extended-cycle preparations contain

A

Ethinyl estradiol + levonorgestrel

38
Q

Norelgestromin/ethinylestradiol (ortho evra) - Special considerations and Adverse effects

A

4 week adm cycl. New patch same day each week for 3 weeks, week 4 is patch-free.
Less effective in women weighting >198 pounds.

Greater incidence of venous thromboembolism than oral contraceptives

39
Q

Progestin-only contraceptives - MoA

A

Decrease Frequency of GnRH pulse (Decrease LH surge).
Thicken & decrease cervical mucus, create a thin, atrophic endometrium that is hostile to implantation of the blastocyst
IUD: produces localized effects on the endometrium

40
Q

Progestin-only contraceptives - Clinical use

A

Suited as contraceptive for smokers, older women, or with contraindication for estrogen

41
Q

Progestin-only contraceptives - Special consideration

A

Increased Contraceptive failure risk compared to estrogen-progestin contraceptives.
Must be taken daily without interruption

42
Q

Progestin-only contraceptives - Adverse effects

A

Frequent spotting, amenorrhea, increased risk of ectopic pregnancy.
Irregular and unpredictable menstrual cycle

43
Q

Progestin-only contraceptives

A

Norethindrone
Medroxyprogesterone
Levonorgestrel
Ulipristal acetate

44
Q

Medroxyprogesterone acetate - Clinical use

A

Castration agent in men convicted of pedophilia, serial rape, sex crimes.

45
Q

Emergency contraceptives

A

Levonorgestrel and Ulipristal acetate

46
Q

Levonorgestrel - Adverse effects

A

Usually nausea and vomiting (reduced by eg promethazine).

Headache, dizziness, leg cramps, abdominal cramps

Pharmacology (55 decks)

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