Reproductive Pharmacology (redue) Flashcards

1
Q

What are the 3 sources of gonadotropins and which gonadotropins comes from which source?

A

Pituitary : FSH and LH

Pregnant women : HCG

Serum of pregnant mares : ECG

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2
Q

GnRH is a secretagogue for ____ and ____ release.

A

FSH and LH

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3
Q

From where is GnRH released?

A

Hypothalamus

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4
Q

What are the 2 uses of GnRH in the female?

A
  1. Increase conception (induces ovulation)

2. Tx follicular cysts

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5
Q

What is 1 use of GnRH in the male?

A

To increase libido

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6
Q

What are 3 GnRH preparations used in vet med?

A
  1. Gonadorelin
  2. Deslorelin
  3. Triptorelin
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7
Q

Which of the following is used in mares: Gonadorelin, Deslorelin, Triptorelin? How is it administered?

A

Deslorelin - SQ

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8
Q

Which of the following can be used in dogs: Gonadorelin, Deslorelin, Triptorelin? In which other species is it used? How is it administered?

A

Gonadorelin - SQ

Used in dogs, cats, and ruminants

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9
Q

Which of the following is used in sows: Gonadorelin, Deslorelin, Triptorelin? How is it administered?

A

Triptorelin - intravaginal

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10
Q

What is the common name of Gonadorelin?

A

Ovacyst

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11
Q

What is the common name of Deslorelin?

A

SucroMate

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12
Q

What is the common name of Triptorelin?

A

OvuGel

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13
Q

For what is Leuprolide acetate used?

A

For the control of adrenocortical disease in ferrets neutered too young

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14
Q

Adrenocortical disease in ferrets is the overproduction of sex steroids by the adrenal gland. What are the clinical signs of this?

A

Males - aggressive sexual behavior

Females - constant estrus

Alopecia

Pruritus

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15
Q

What is the mechanism of action for Leuprolide acetate?

A

(GnRH receptor agonist)

Disrupts pulsatile GnRH secretion, causing a down-regulation of GnRH receptors.

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16
Q

What are GnRH vaccines used for?

A

GnRH vaccines are an excellent way to control population in dogs and wild horses - they serve as a form of chemical sterilization (neuter)

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17
Q

How does FSH stimulate the development of follicles in the female?

A

FSH increases the production of estrogen in granulosa cells, then estrogen increases the FSH receptors in follicles, increasing follicular development.

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18
Q

What is the function of aromatase?

A

Converts testosterone to estradiol

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19
Q

FSH has 2 important actions in the male, what are they?

A
  1. Increase diameter of seminiferous tubules

2. Increase development of spermatozoa

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20
Q

What 5 main effects does LH have on a female?

A
  1. Induce ovulation
  2. Induce luteinization
  3. Increase progesterone production
  4. Increase estrogen production
  5. Increase testosterone production in theca cells
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21
Q

What effect does LH have on a male?

A

Increases testosterone levels by proliferation of leydig cells

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22
Q

Where does testosterone come from in the female?

A

Theca cells

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23
Q

Where does testosterone come from in the male?

A

Leydig cells

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24
Q

What is the mechanism of action of FSH and LH?

A

Activate Gs-adenylyl cyclase system –> increase cAMP –> activate PKA –> activate enzymes of sex steroid synthesis

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25
Q

What does PKA activate in order to increase mRNA for proteins for the proliferation of enzymes for sex steroid synthesis?

A

CREB (cAMP response element binding protein)

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26
Q

Where is HCG synthesized in a pregnant women?

A

Placenta

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27
Q

When are HCG levels the highest in a pregnant women?

A

First 2 months of the pregnancy

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28
Q

What are the 4 clinical uses of LH/HCG?

A
  1. Induce ovulation
  2. Treat follicular cysts
  3. Treat persistent infertility in the female
  4. Treat cryptorchidism
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29
Q

What are the 3 clinical uses of FSH/ECG?

A
  1. Breeding control
  2. Induce superovulation
  3. Treat infertility in the male
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30
Q

Repeated interspecies use of ECG and HCG may cause __?__ in animals.

A

Anaphylaxis

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31
Q

Which of the following has the LONGEST T1/2 in the human: LH, FSH, HCG, or ECG?

A

ECG

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32
Q

In the human, how long are the half lives of the following: LH, FSH, HCG, ECG?

A

LH = 30 minutes

FSH = 60 minutes

HCG = 8 hours

ECG = 24 hours

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33
Q

Why does ECG have the longest half life?

A

ECG has the greatest carbohydrate content

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34
Q

Carbohydrates account for ____% of FSH, LH, TSH, ____% of HCG and ____% of ECG.

A

Carbohydrates account for 13-16% of FSH, LH, TSH, 31% of HCG, and 47% of ECG.

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35
Q

Removal of ____ ____ from one of these glycoprotein hormones (FSH, LH, HCG, ECG) greatly decreases the T1/2.

A

Sialic acid

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36
Q

HCG is found in the urine of _____women.

A

Pregnant

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37
Q

FSH is found in the urine of _____ women.

A

Postmenopausal

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38
Q

What are the 4 natural sources of estrogen?

A
  1. Ovary
  2. Testicle
  3. Adrenal gland
  4. Placenta
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39
Q

____% of estrogens are bound to plasma proteins.

A

90%

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40
Q

Concerning estrogens, which of the following has a high affinity and low capacity: albumin OR sex-steroid binding globulin?

A

Sex-steroid binding globulin

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41
Q

What is the plasma T1/2 of estradiol?

A

30 minutes

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42
Q

What is the most potent form of estrogen?

A

Estradiol

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43
Q

What are the roles of estrogen in the body?

A
  1. Increase sexual receptivity
  2. Increase repro tract growth
  3. Increase oxytocin receptor expression
  4. Dilate the cervix
  5. Increase mammary growth
44
Q

What effect does estrogen have in the ruminant?

A

Luteolysis

45
Q

What effect does estrogen have in the pig?

A

CL retention

46
Q

What effects do estrogens have on the bone?

A

Decrease IL-6 and IL-11 –> decreases osteoclastic vitality –> increases bone mass

Ossification of epiphyseal plate –> decreases bone growth

47
Q

Which of the following contain testosterone and which contain progesterone: Synovex-C, -S, -H?

A

Synovex-C = Progesterone

Synovex-S = Progesterone

Synovex-H = Testosterone

48
Q

Other than estradiol benzoate, what does Synovex-Plus contain?

A

Trenbolone acetate

49
Q

In which animals can Synovex-Plus be used?

A

Steers OR heifers

50
Q

What is the name of the only non-steroidal estrogen available in the U.S. for use in beef cattle and sheep as an ear implant?

A

Zeranol

51
Q

True or False: Estradiol preparations require pre-slaughter withdrawal.

A

FALSE

52
Q

True or False: Zeranol requires pre-slaughter withdrawal.

A

FALSE - not in cattle, 40 days in sheep

53
Q

What are the 6 mechanisms of estrogen-induced anabolism?

A
  1. Increased GH secretion
  2. Increased GH receptor expression
  3. Increased IGF-1 secretion
  4. Increased IGF-1 receptor expression
  5. Increased IGF-1 binding proteins
  6. Increased mRNA for muscle protein
54
Q

What is the main (recommended) indication for the use of estrogens clinically?

A
  1. To treat problems associated with spaying: incontinence, vaginitis, dermatitis.
55
Q

What is the name of the drug used to treat urinary incontinence in the spayed dog?

A

Estriol (Incurin)

56
Q

What is the name of the alpha-AR agonist used to contract the bladder sphincter muscle in incontinent dogs?

A

Phenylpropanolamine

57
Q

What are the 2 approved treatment methods for prostatic hyperplasia?

A
  1. Finasteride (Proscar)

2. Castration

58
Q

What is the MOA of Finasteride (Proscar)?

A

Inhibits 5-alpha reductase, the enzyme used to convert testosterone to dihydrotestosterone

59
Q

What are the 6 side effects associated with estrogen use?

A
  1. Abortion
  2. Prolapsed vagina or rectum
  3. Aplastic anemia
  4. Pyometritis
  5. Follicular cysts
  6. Bone fracture
60
Q

What are the 3 natural sources of progestins?

A
  1. Adrenal gland
  2. Ovary
  3. Placenta
61
Q

What is the plasma half life of progestins?

A

30 minutes

62
Q

What are the 5 clinical uses of progestins?

A
  1. Synchronization of estrus
  2. Treatment of implant failure
  3. Contraception in the bitch
  4. Control of aggressiveness
  5. Control of inappropriate urination
63
Q

What are the 2 side effects associated with the use of progestins?

A
  1. Endometrium hyperplasia

2. Glucocorticoid effects (diabetes, inhibition of the adrenal cortex)

64
Q

What is RU 486?

A

Progestin receptor antagonist - very efficient abortifacient and parturition-inducing agent

65
Q

What are the 3 natural sources of androgens?

A
  1. Ovary
  2. Testicle
  3. Adrenal gland
66
Q

____% of circulating testosterone is bound by plasma proteins.

A

90%

67
Q

What is the plasma T1/2 of testosterone?

A

20 minutes

68
Q

What are the 4 actions of androgens?

A
  1. Increase spermatogenesis
  2. Increase growth of accessory organs
  3. Increase bone growth
  4. Increase EPO synthesis
69
Q

What are the 4 clinical uses of androgens?

A
  1. Treat cryptorchidism
  2. Treat mammary gland tumors
  3. Treat infertility
  4. Induction of teaser cows
  5. Growth promotion (as well as reversal of tissue depletion)
  6. Treat anemia
70
Q

DHEA does NOT increase plasma _____ levels, but increases _____ level and decreases _____.

A

DHEA does NOT increase plasma TESTOSTERONE levels, but increases ESTRADIOL levels and decreases HDL.

71
Q

What are the 4 side effects associated with androgen use?

A
  1. Infertility
  2. Water retention
  3. Masculinization of females
  4. Liver disorders
72
Q

What are the 4 anti-androgens available?

A
  1. Finasteride
  2. Cimetidine
  3. Ketoconazole
  4. Trilostane
73
Q

What is the main use for anti-androgens in vet med?

A

Prostatic hyperplasia

74
Q

What are the 5 indications for inducing uterine contractions?

A
  1. Induce labor
  2. Abortion
  3. Expel uterine contents
  4. Post-partum hemorrhage
  5. Treat uterine inertia
75
Q

Which substances have oxytocic activity?

A
  1. Muscle stimulants
  2. Poisons (lead)
  3. PGE2, PGF2-alpha
  4. Glucocorticoids
  5. Ergot alkaloid
  6. Oxytocin, vasopressin
76
Q

What is Domperidone?

A

D2 receptor antagonist

77
Q

What effect does Domperidone have on prolactin?

A

Increases prolactin secretion

78
Q

What effect does Domperidone have on milk production?

A

Increases milk production

79
Q

Does Domperidone cross the BBB?

A

NO

80
Q

Use Domperidone to treat ____ ____ in prepartum mares.

A

Fescue toxicosis

81
Q

The primary source of PGF2alpha is _____ in species other than primates and rodents.

A

Endometrium

82
Q

Vasopressin increases the contractions of what 3 structures?

A
  1. Blood vessels
  2. Uterus
  3. GI
83
Q

_____ enhance the effects of oxytocin.

A

Estrogen

84
Q

_____ reduce the effects of oxytocin.

A

Progesterone

85
Q

What are the 4 clinical uses for oxytocin?

A
  1. Induce labor (only in mares and humans)
  2. Treat placental retention
  3. Milk letdown
  4. Treat dystocia
86
Q

What are the 2 main uses of ergot alkaloids?

A
  1. Post-partum hemorrhage

2. Uterine involution

87
Q

What is the MOA of ergot alkaloids?

A

Activate alpha-1 adrenergic receptors and 5-HT2 receptors, increasing smooth muscle contraction

88
Q

What are the 3 effects of ergot alkaloid overdose?

A
  1. Vomiting
  2. Gangrene
  3. Excitation
89
Q

What are carbachol and bethanechol?

A

Potent uterine contractors

90
Q

Which is more specific, carbachol or bethanechol?

A

Bethanechol is specific to muscarinic receptors, whereas carbachol is non-specific, for muscarinic and nicotinic receptors

91
Q

When should Carbachol or Bethanechol be used?

A

As a last resort - only in large animals that are refractory to other oxytocic agents

92
Q

What are the following: Dinoprost tromethamine and Cloprostenol?

A

PGF2-alpha analogs

93
Q

Which is more potent, Dinoprost tromethamine or Cloprostenol?

A

Cloprstenol

94
Q

PGF2-alpha analogs cause potent ______.

A

Vasoconstriction

95
Q

What effect does PGF2-alpha have on the corpus luteum?

A

Cuts off its blood supply, leading to luteolysis (apoptosis of the CL)

96
Q

What effect does PGF2-alpha have on progesterone levels?

A

Decrease

97
Q

PGF2alpha analogs can be used in estrus synchronization, except in which species?

A

Swine

98
Q

How long after PGF2-alpha induction will a cow or sow go into labor?

A

1 - 8 days (mean 3 days)

99
Q

How long after PGF2-alpha induction with a mare go into labor?

A

1 - 2 days (unless milk is present - labor can then occur within 30 minutes of induction)

100
Q

What would you use to treat pyometra in the dog?

A

PGF2-alpha analog

101
Q

What would you use to induce expulsion of mummified fetuses?

A

PGF-2 alpha analog

102
Q

What would you use instead to synchronize estrous cycle in the pig?

A

Matrix

103
Q

How would you administer PGF2-alpha to induce luteolysis?

A

IM - small repeated doses

104
Q

What is the mechanism of action of long-acting glucocorticoids in induction of labor?

A

Increase PGF2-alpha secretion from the endometrium

105
Q

Why is Dexamethasone (long-acting corticosteroid) not recommended for pregnancy termination in the dog?

A

Have to give large doses, 2x/day for 10 days