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PHRM 825 Steroids Exam 2 > Progestins > Flashcards

Progestins Flashcards

1
Q

what are the physiological effects of progesterone?

A
  1. menstruation cycle
  2. metabolic effects
  3. interference with adolescence
  4. depressant and hypnotic effects
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2
Q

what does the menstrual cycle do in terms of physiological effects?

A

causes maturation and secretory changes in the endometrium following ovulation

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3
Q

what are the metabolic effects associated with physiological effects?

A
  1. inc. basal insulin levels and insulin response to glucose
  2. promotes glycogen storage in the liver
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4
Q

what are the interferences with aldosterone in the physiological effects?

A
  1. competes with aldosterone for mineralocorticoid receptor
  2. cause decrease in Na+ reabsorption –> inc. aldosterone secretion in adrenal cortex
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5
Q

what are the clinical uses for progestins?

A
  1. hormonal contraception
  2. hormone replacement therapy in combo with estrogens
  3. endometriosis (excess growth)
  4. dysmenorrhea
  5. bleeding disorders
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6
Q

what are the structural characteristics responsible for changes in drug properties?

A
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7
Q

what is the mechanism of action/physiological effects of hormonal contraceptives?

A
  1. mostly oral administration
    – adherence then is more critical for progestin-only therapies
  2. inhibition in ovulation
  3. suppression of ovary function
  4. change in cervical mucous in endometrium
  5. suppression of lactation and leads to enlargement of breasts
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8
Q

what is the metabolism of progestins like?

A
  1. rapidly absorbed followed by any route of admin
  2. almost completely metabolized in one passage through the liver
  3. excreted in the urine
  4. half-life in plasma is about 5 min.
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9
Q

what are the generic types of contraceptives?

A

IUD, Implant, Oral (monophasic, biphasic, triphasic), Injection, ring

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10
Q

what is levonorgestrel?

A
  1. 2nd gen
  2. only levo form is active
  3. high bioavailability
  4. used in IUD
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10
Q

what makes the drug a first line progestin?

A
  1. replacement at 19-methyl with H –> enhances activity
  2. replacement at 17-acetyl with OH –> inc. oral bioavailability
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10
Q

what is norgestimate?

A
  1. 2nd gen
  2. prodrug
  3. converted to levonorgestrel oxime and then levonogestrel in vivo
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10
Q

what is deogestrel?

A
  1. 3rd gen
  2. prodrug
  3. rapidly metabolized to etonogestrel
  4. high oral bioavailability
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10
Q

what is etonogestrel?

A
  1. strucure analogous to levonorgestrel
  2. active form of desogestrel
  3. 3rd gen
  4. used in implant and vaginal ring
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10
Q

what is drosperinone?

A
  1. 4th gen
  2. weak progestogenic activity
  3. antimineralocorticoid activity
  4. negates side effects of theynyl estrdiol in combo therapy
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10
Q

what is medroxyprogesterone acetate?

A
  1. 1st gen progestin
  2. used for depot inj.
  3. acts as long-acting progesterone-only contraceptive
10
Q

what are the mild adverse effects of oral contraceptives?

A
  1. nausea, HTN, edema, breast fullness –> estrogens
  2. inc. appetite, fatique, breast regression –> progestin
10
Q

what are the moderate adverse effects of oral contraceptives?

A

1, irregular periods –> more common in progesteron-only
2. weight gain, acne, hirsutism –> more common in combos
3. amenorrhea

10
Q

what are the severe adverse effects of oral contraceptives?

A
  1. venous thromboembolic disease –> estrogens
  2. myocardial infarction –> progestins
  3. dangerous in women over age 35 who smoke
10
Q

what are the emergency contraceptives?

A
  1. morgning after pill
  2. 99% effective if taken in 72 hours
  3. combo (yuzpe regimen)
  4. progestin only (plan B)
  5. side effects
    –> nausea, vomiting –> more common in combo
10
Q

what is ulipristal acetate?

A
  1. selective progesterone receptor modulator (SPRM)
  2. emergency contraceptive
  3. effective up to 5 days after
  4. side effects
    –> nausea, abdominal pain
11
Q

what does ulipristal acetate look like?

A
12
Q

what is mifepristone?

A
  1. RU-486
  2. progesterone antagonist
  3. abortifacient
    –> combo with misoprostol up to 70 days
  4. side effects
    –> nausea, vomiting, bleeding
  5. banned in indiana
13
Q

what does mifepristone look like?

A
14
Q

what is danazol?

A
  1. weak androgen, progestin, and antiestrogen
  2. effective for endometriosis
    –>. inhibits surge of LH and FSH to suppress ovary function and causes atophy in endometrium
  3. adverse effects
    –> weight gain, dec. breast size, acne, oily skin, hirsutism
  4. contraindications
    –> hepatic dysfunction, pregnancy or breast feeding
15
Q

what does danazol look like?

A

PHRM 825 Steroids Exam 2 (8 decks)

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