Reproductive Pharmacology Flashcards by Trenni Jefferson

______________ regulates overall reproduction

Hypothalamus

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What 2 hormones come from the hypothalamus

Gonadotropin releasing hormone (GnRH)
Dopamine: prolactin- inhibitor hormone
They stimulate/ inhibit the release of anterior pit hormones

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Anterior pituitary glands

Gonadotropins: FSH and LH (act on ovaries + negative feedback on pituitary)
Prolactin

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GnRH

Targets anterior pit. to release LH and FSH
Pulsatile release

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Increased and decreased GnRH

↑= secretion of LH
↓= greater FSH release

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Continuous administration of GnRH

Desensitization and down regulation of GnRH receptors on pituitary gonadotropes
Medical castration

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Follitropin

FSH
Superovulation in cattle

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Folluttein and Chrorulon

hCG
Horses: infertility, male impotence
Cow: cystic ovaries
Pig: induce estrus
Cats: pseudopregnancy
Dog: cryptorchidism

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Ovagen and Pg600 combo

In anestrus for sheep and goat: stimulates ovarian follicular growth
Pig: induces estrus

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Mentropins

Mostly FSH like effect
Cattle: superovulation

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Gonadorelin

Causes surge like release of FSH and LH
Ovulation induction, infertility treatment

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Extralabel use of gonadorelin

GnRH stimulation test to differentiate castration from cryptorchidism
Cystic ovarian disease in bitches
Detect ovarian remains in queens after OVH

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Superelorin use in mares

GnRH analog
Estrual mares to induce ovulation by ↑ LH and inducing ovulation within 48 hrs

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Superelorin use in other animals

Adrenal disease in ferrets (restricted in major species)
Birds with chronic egg-laying/ behavioral
Contraceptive
Aggression in males

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Gonadotropins MOA

LH and hCG act on LH receptor
FSH on FSH receptor
eCG on both receptors ^
G-protein coupled receptors ↑ cAMP levels

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eCG

FSH like activity
Except in horses LH like activity
Super ovulation

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Leuprolide (LH agonist)

Negative feedback: Initially ↑ FSH and LH, then inhibits them
Estrogen and androgen levels ↓ in serum

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Leuprolide uses

Chronic egg laying in birds
Ovarian cysts in GPs

Legal note about GnRH products

Illegal to use products in combination with another drug for estrous synchrony unless approved combos

Prolactin

Major regulator is dopamine (agonist= inhibit)
Stimulates lactation in postpartum period
No analog

Metoclopramide

↑ prolactin: dopamine antagonist
Antiemetic in small animal, ↑ GI motility in small and large animals

Domperidone

↑ prolactin: dopamine antagonist
Stimulates ↑ in lactation through prolactin stimulation
Treatment for fescue toxicosis causing agalactia

Oxytocin in the uterus

Stimulates frequency and force of uterine contraction
Effects dependent on estrogen
Progesterone antagonizes stimulant effect of oxytocin

Oxytocin in the mammary gland

Induces contraction of smooth muscle, resulting in milk ejection

Oxytocin MOA

G-protein coupled membrane receptors Activation lead to generation of IP3 (metabolizes Ca2+) Depolarization-contraction of smooth muscle tissue with oxytocin contractions

Clinical uses of oxytocin

Labor induction (make sure there's no obstruction, can cause uterine rupture) Milk let down Persistent endometritis (mare)

Dinoprost (PGF2a analog)

Luteolytic agent produced by the endometrium Activates GPCR linked to IP3 Ca2+ protein kinase pathway (↓ steroidogenesis and luteolysis)

Dinoprost function

↓ progesterone via luteolysis of the CL ↓ placental progesterone production

Dinoprost clinical uses

Estrus synchronization Abortion and parturition in dogs Uterine contractions in cows Mating-induced endometritis in mare Uterine infections in bitches Inducing parturition in sow

Dinoporost adverse reactions

↑ smooth muscle tones→ diarrhea, abdominal discomfort, bronchoconstriction, ↑ BP Inducement of abortion leading to retained placenta

Dinoprost should not be handled by ___________

Pregnant women *can be absorbed through the skin*

MOA of estrogen and progesterone

Binds to intracellular steroid hormones Hormone-receptor complex interacts with DNA at hormone response elements (transcription factor)

Clinical use for estradiol

Neg feedback of LH and FSH Estrus synchronization Urinary incontinence and perianal gland adenoma in dogs

Progestins

Long lasting ovarian suppression and synchornization of estrous cycle ↑ feedback and ↓ LH and FSH output

Altrenogest (progestin)

Controls estrus cycle in mare and pig High doses: fetal abnormalities in horses

Melengstrol Acetate (progestin)

Approved: medicated feed to suppress estrus in heifers Not: synchronizing estrous cycle/ advancing estrus in heifers

Parturition in cattle

Glucorticoids (dexamethasone, flumethasone) PGF2a, cloprostenol

Parturition in other animals

Farrowing (pigs): PGF2a Mare: oxytocin

Cryptorchidism

Serial injections of hCG

Anabolic steroids (Test.)

Equine: ↑ athletic performance Dogs and cats: aplastic anemia and myeloproliferative disease Ex: stanozolol, nandrolone, boldenone undecylenate

Stanozolol (BANNED)

↑ erythropoiesis, arouse appetite, promote weight gain in equine

Nandrolone (BANNED)

Improve weight gain and appetite in equine

Finasteride

Irreversible 5a reductase inhibitor Blocks conversion of Testosterone to 5a dihydrotest. Treats benign prostatic hyperplasia (apoptosis)