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Clinical pharmacology > Reproductive system drugs > Flashcards

Reproductive system drugs Flashcards

1
Q

Female sex hormone Production is regulated by the following: (3)

A

Cerebral cortex
Hypothalamus
Hypophysis

The reproductive function is regulated by the cerebral cortex. Hypothalamus is rated second.

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2
Q

Female sex hormones are considered to be the following hormones: (4)

A

FSH and LH, estrogens and gestagens (ie. progesterone)

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3
Q

The neurosecretory cells in the hypothalamus produce specific hormones that are called

A

hypophysiotropic hormones,
i.e. releasing factors , i.e. liberins.

Their role is to stimulate or inhibit the release of hormones from the adenohypophysis.

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4
Q

Gonadotropins are produced under the control of

A

respective liberins in the adenohypophysis.

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5
Q

Mechanism of action of Hormones that are produced in the adenohypophysis can be either:

A

direct-acting with a direct effect on the tissues of the organism: prolactin, somatotropin.

or indirect-acting stimulate another endocrine organ, causing the release of hormones: e.g. gonadotropic hormones, adrenocorticotropic hormone, thyrotropin-releasing hormone.

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6
Q

Estrus cycle in cattle

A

21 days

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7
Q

review this Estrus cycle in dog-schematic

A
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8
Q

Two main Gonadotropic hormones:

A

Follicle-stimulating hormone (FSH)
Luteinizing hormone (LH)

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9
Q

name a a luteotropic hormone

A

prolactin

participates in the regulation of the milk production process and in some animal species it has a stimulating effect on the corpus luteum (mouse, rat).

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10
Q

what is Gonadorelin

A

is a gonadotropin-releasing hormone agonist (GnRH agonist) which is used in fertility medicine and to treat amenorrhea and hypogonadism.

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11
Q

function of drug Gonadorelin

A

stimulates the release of FSH and LH from the hypophysis, as a result of that the follicle matures, ovulation occurs and the production of progesterone begins (cat and dog). I

t increases the production of testosterone in male dogs and cats.

used for the stimulation of ovulation, for inducing estrus & treatment of follicular cysts in dogs and cats.

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12
Q

what is Buserelin

A

sold under the brand name Suprefact among others, is a medication which is used primarily in the treatment of prostate cancer and endometriosis.

Buserelin is a gonadotropin-releasing hormone agonist (GnRH agonist) and works by preventing the production of sex hormones by the gonads.

(GnRH) – several products for animals

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13
Q

how do FSH and LH work together to produce mature ova

A

FSH stimulates growth of secondary follicles in the ovarian cortex and raises the mitotic activity of the follicular epithelium.

LH ensures the final maturation of follicle and ovulation, thereafter it stimulates the development of the corpus luteum.

LH also causes the production of estrogens and gestagens (progesterone).

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14
Q

When is FSH and LH synthesis and release from the hypophysis during an estrus cycle?

A

occurs continuously throughout the estrus cycle.

The level and proportion of either hormone depends upon the phase of the estrus cycle.

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15
Q

The estrogens circulating in the blood suppress what?
and enhance what?

A

The estrogens circulating in the blood suppress the FSH releasing factor and enhance the production of the LH releasing factor.

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16
Q

Gestagens inhibit the production of

A

LH releasing factor.

If the sex hormone content of the blood is reduced, the secretion of gonadotropins increases as a response to it and vice versa, an increase in the content of sex hormones in the blood (medicinal products) suppresses the secretion of gonadotropins. Feedback.

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17
Q

17beta-estradiol is

A

a natural estrogen. It is comprised of two similar substances: estrone and estriol.

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18
Q

17beta-estradiol is produced by (2)

A

Theca interna cells of Graafian follicles or placenta.

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19
Q

The biological effect of synthetic estrogens is

A

the same as the natural estrogens but the intensity of action is more potent and duration is longer.

They are much more stable than natural estrogens. Most of them have a non-steroidal structure.

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20
Q

Describe Diethylstilbestrol.

A

Synthetic nonsteroidal estrogen.

It can be used for inducing estrus, to synchronise estrus.

In farm animals, it induces luteolysis through the prostaglandin F2alfa release.

No product in EU, but in use in USA.
Not recommended anymore!

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21
Q

Pharmacokinetics of estrogens

A

Natural estrogens are absorbed well from the GI and broken down quickly.

Biotransformation occurs in the liver, to a lesser degree in the uterus.

Excreted through the kidneys, mainly as esters of glucuronic acid or sulfuric acid.

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22
Q

Use of estrogens in production animals. (3)

A

Estrogens are used for treatment of various reproductive disorders in farm animals.

For inducing estrus in the case of silent estrus and anestrus.

In the case of underactive ovaries.

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23
Q

Side effects of synthetic estrogens. (3)

A

Estrogens may cause endometrial hyperplasia.

If administered to young dogs, they may cause tumors of the ovaries.

In cats they may damage the pancreas, liver and heart.

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24
Q

Synthetic estrogens contraindications. (4)

A

Contraindicated in pregnant animals.

Contraindicated during concurrent progesterone treatment.

If administered to pregnant animals, the fetus develops malformations in the urinary and reproductive organs, usually fatal.

Some estrogens have been proved to have a carcinogenic effect (in lab animals).

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25
Q

Gestagens are Steroid hormones produced by?
Give 3 examples.

A

the corpus luteum, but also to some extent in the adrenal glands and placenta.

Progesterone
Megestrol (synthetic progesterone, progestin)
Medroxyprogesterone (synthetic)

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26
Q

Functions of progesterone. (6)

A

causes growth and development of the uterine glands and increases the intensity of secretion.

Participates in embryo transplantation.

Creates favorable conditions for embryo development.

Suppresses uterine contractions, reduces the sensitivity of the uterus to oxytocin.

Inhibits the production of gonadotropic hormones, prevents estrus, ovulation and a new estrous cycle, maintains gestation.

cause uterine cervix constriction, reduced secretion of mucus, increased viscosity of mucus.

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27
Q

Side effects of gestagens.
In cats?
In dogs?

A

In cats, inhibition of the adrenal glands, even to atrophy. Endometrial hyperplasia, hypertrophy of the mammary glands, increase in body weight.

In dogs, increase in body weight, endometrial hyperplasia, lethargy, behavioral changes, inhibition of the adrenal glands.

28
Q

Contraindications for gestagens/progestins. (4)

A

Diestrus
After the administration of estrogens

Diabetes
Endometrial and mammary gland disease

29
Q

Use of exogenous gestagens/progestins. (5)

A

Estrous synchronization
For preventing or postponing estrus
In case of pseudopregnancy
In case of habitual abortion (multiple miscarriages)
For the treatment of prostatic hyperplasia

30
Q

Describe the product PRID Delta.

A

A medical device containing progesterone.

For intravaginal administration, used in cows. Left for 7 days in vagina.

Administration of PGF2-alfa 24 hours before taking device out.

56 hours after removal -> artificial insemination.

Similar product called CIDR.

31
Q

Synthetic progestins Act on what receptors?

A

progesterone receptors in the hypothalamus/pituitary, and thus decrease FSH and LH output.

The withdrawal of progestin therapy initiates a new estrous cycle and ovulation.

32
Q

The withdrawal of progestin therapy initiates

A

a new estrous cycle and ovulation.

33
Q

Name 2 Synthetic progestins

A

Altrenogest – estrous synchronization in sows.

Proligestone - administered at the start of estrus, inhibited follicular growth as a result of the reduction in concentration of luteinizing hormone and reduced production of estradiol from mature follicles.

Follicular atresia occurs and estrus is interrupted. For postponing and interrupting estrus in dogs, cats and ferrets.

34
Q

Indications for use of exogenous Chorionic gonadotropin (human).
Cow
Horse
Dog

A

Cattle: Improvement in conception rate,
nymphomania, anestrus, ovarian cysts together with irregular estrous cycle.

Horse: Inducing ovulation, anestrus.

Dog: Inducing ovulation, anestrus, delayed ovulation, extended proestrus, in male dogs cryptorchidism or weak libido.

35
Q

Prostaglandins are what type of molecule.

A

Unsaturated cyclic fatty acids with 20 carbon atoms.

36
Q

Prostaglandins are divided into

A

many groups based upon chemical structure: PGA, PGD, PGE, PGF.

37
Q

Which prostaglandin is important in human reproductive function, and which, in cattle?

A

PGE is important in the human reproductive function,
in cattle PGF is important (PGF2α).

38
Q

Examples of synthetic prostaglandins. (5)

A

Cloprostenol (synthetic PGF2α)
Dinoprost (synthetic PGF2α)

Fenprostalene (synthetic PGF2α)
Luprostiol (synthetic PGF2α)
Tiaprost (synthetic PGF2α)

39
Q

Effects of PGF2-alfa (4)

A

causes myometrial contractions,
cervical relaxation and luteolysis.

Does not have an effect on ovulation.

It stimulates both pregnant and nonpregnant uterus, increases the uterine muscle tone.

40
Q

Side effects of PGF2-alfa.

A

Stomach ache
Vomiting, diarrhea
Urination
Tachycardia
Fever
Hypersalivation
Restlessness

41
Q

Contraindications for PGF2-alfa. (3)

A

Gestation
Liver and kidney disease

Pregnant and asthmatics (can cause bronchoconstriction) must not work with the preparation. And not to be administered intravenously.

42
Q

exogenous prostaglandins uses (4)

A

For inducing abortion
For inhibiting milk synthesis

For inducing estrus, reduction of the interval between two estruses.
In case of pseudopregnancy

43
Q

What hormone inhibits prolactin?

A

Dopamine originating from the hypothalamus inhibits the secretion of prolactin in the pituitary gland, therefore dopamine agonists inhibit the secretion of prolactin.

44
Q

What hormone indirectly inhibits the secretion of prolactin? (not dopamine)

A

Serotonin inhibits the secretion of dopamine in the hypothalamus and thereby indirectly stimulates the secretion of prolactin.

45
Q

Name 2 dopamine agonists that inhibit prolactin through dopamine production.

A

metoclopramide
acepromazine

46
Q

Describe drug Cabergoline

A

Is a specific dopamine agonist and thus inhibits prolactin secretion.

Used in the treatment of pseudopregnancy and suppression of lactation in small animals.

47
Q

Name 3 drugs that inhibit prolactin and thus are used for the treatment of pseudopregnancy.

A

Cabergoline
Bromocriptine
Metergoline

48
Q

Describe drug Bromocriptine mesylate.

A

Is a synthetic ergot alkaloid substance, which directly inhibits prolactin synthesis by acting on the D2 receptors in the pituitary gland.

Bromocriptine is in a class of medications called dopamine receptor agonists.

It treats hyperprolactinemia by decreasing the amount of prolactin in the body.

49
Q

Describe drug Metergoline.

A

Serotonin antagonist.

Metergoline suppresses prolactin release from pituitary cells, used in the treatment of hyperprolactinemia and to suppress lactation.

50
Q

Describe drug Aglepristone.

A

Tradename Alizin

is a synthetic, steroidal antiprogestogen that competes with progesterone on the uterine progesterone receptor level.

Induces abortion within 7 days from the day of administration (or fetal resorption). Used in dogs and also for the treatment of pyometra.

51
Q

Alizin active ingredient

A

Aglepristone

52
Q

Substances increasing the intensity of uterine contractions (4)

A

Prostaglandins
Hormones of the posterior lobe of the pituitary gland (e.g. oxytocin)

Ergot fungus alkaloids (ergot alkaloids cause ergotism (toxicosis))
Glucocorticoids (dexamethasone)

53
Q

There are two hormones in the posterior lobe of the pituitary gland:

A

oxytocin and vasopressin.

54
Q

Oxytocin is produced in the

A

neurosecretory cells of the nuclei of the hypothalamus. From there, it moves to the posterior lobe of the pituitary gland from whence its secreted.

The release into the bloodstream occurs due to the effect of cholinergic impulses originating from the hypothalamus.

55
Q

physiological role of oxytocin is (4)

A

the enhancement of the movement of spermatozoa and zygote, and participation in the mechanism of giving birth.

Oxytocin also causes contractions of the myoepithelium of the udder, promoting the ejection of milk in lactating animals.

56
Q

Clinical use of oxytocin (5)

A

Stimulation of birthing
In case of uterine atony after giving birth
In case of retained placenta
Treatment of inflammatory conditions of the uterus
For the ejection of milk (milking)

57
Q

Ergot alkaloids effect on uterine muscle.

A

They increase the tone of the uterine muscle, strengthen contractions, especially during gestation and after giving birth.

They have historically been used in case of uterine bleeding, for removal of placenta, in case of uterine atony after giving birth.

Not to be used for stimulation of giving birth. Contractions are very powerful, fetal suffocation and uterine rupture may occur!

However, some product utilizing ergot alkloids may be available for sows.

58
Q

Substances inhibiting uterine contractions (4)

A

beta-adrenomimetics
Local anesthetics

Denaverine hydrochloride (anticholinergic/spasmolytic; regulation of uterine contractions during parturition).

Potentially Narcotic analgesics

59
Q

clinical Use of Substances inhibiting uterine contractions (3)

A

Alleviation of obstructed labor
Improvement of wrong delivery position and posture
Fetotomy & caesarean section

60
Q

Phenylpropanolamine is an

A

adrenergic agent that assists in the tightening of the muscles of the bladder sphincter, effectively controlling bladder leakage and other symptoms of urinary incontinence.

Tradename Propalin.

It stimulates the α-adrenergic receptors of bladder sphincter. Efficacy is demonstrated only in female dogs after hysterectomy.

61
Q

Estriol is a?
Used in?

A

Short-acting natural estrogen used in dogs for the treatment of hormone-responsive urinary incontinence caused by urethral sphincter incompetence occurring after ovariohysterectomy.

Not to be used in unspayed female dogs, efficacy has only been proven in dogs that have undergone ovariohysterectomy.

Large doses of estrogen may promote tumors in organs that have estrogen receptors e.g. mammary glands.

62
Q

Two meds that can be used to treat urinary incontinence in spayed dogs.

A

propalin/phenylpropanolamine
estriol

63
Q

Describe drug Deslorelin and its use.

A

Tradename Suprelorin.
A GnRH agonist, administered by implant.

Administration as a low continuous dose causes suppression of the function of the pituitary-gonadal axis. Treated animals then fail to synthesize and/or release FSH and LH.

Used for the induction of temporary infertility in healthy uncastrated male dogs and in ferrets. The restoration of fertility has not been studied.

64
Q

Describe the GnRH analogue protein conjugate (preparation Improvac) and its use.

A

Is an Immunological preparation for boars, solution for injection.

Induces immune response to endogenous gonadotropin-releasing factor that controls the testicular function through gonadotropic hormones FSH and LH.

The immunization effect arises from the reduction of testicular function caused by reduced GnRH activity.

This causes a reduction in the production and concentration of testosterone and other testicular steroids, including one of the primary substances that cause “boar off-flavor”, androsterone.

65
Q

Describe drug Osaterone and its use.

A

Steroidal antiandrogen, inhibits the side effects of the production of excess testosterone.

Prevents the binding of androgens to prostatic receptors through competing and blocking the transport of testosterone to the prostate.

No changes in the quality of semen have been observed.

Used for the treatment of benign prostatic hypertrophy in male dogs.

Clinical pharmacology (21 decks)

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