Reproductive Pharms Flashcards

1
Q

GnRH/FSH/LH analogues

A
  • Uses
    o Treatment of fertility disorders
    o Increased reprodictive success
  • A single high dose of GnRH will stimulate FSH and LH release from the anterior pituitary
  • Slow continuous release of GnRH causes down-regulation of receptors on the anterior pituitary and inhibition of FSH and LH release
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2
Q

GnRH analogues

A
  • Buserelin
  • Gonadorelin
    o Anoestrus
    o Ovarian dysfunction
    o Cystic ovarian disease
    o Oestrus synchronization
    o Improved conception
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2
Q

Deslorelin

A
  • Chemical castration: suppress reproductive axis in male dogs and ferrets, lionesses, kangaroos (extra-label in wildlife)
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3
Q

Synthetic GnRH analogues (Improvac)

A

o Suppresses boar taint

o Male antelope contraceptive

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3
Q

Chrono-gest)

A
  • Used in ovines/caprines

- Females: induction of ovulation

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4
Q

Testosterone

A
  • Androgenic (male characteristics) and anabolic (protein building)
  • Testosterone is essential for development of the male reproductive tract, muscle and bone and RBC formation
  • Lipid soluble, high first-pass effect
  • Not really effective for increasing libido – tends to cause infertility!
  • No vet products in SA for small animals and horses (Synovex contains testosterone for heifers)
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5
Q
  • Testosterone Uses
A

o In female dogs: treating androgen sensitive carcinomas (mammary)
o In male dogs: urinary incontinence, rare forms of symmetrical alopecia, mammary tumours
o In cattle; for oestrus detectors and growth promotion
o Anabolic effect in chronic debilitating conditions
o Improvement of renal function in chronic interstitial nephritis

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6
Q
  • Testosterone Side Effects
A

o Infertility
o Perianal adenomas
o Prostatic disorders

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7
Q

Anabolic Steroids

A
  • Derivatives of testosterone
  • Androgenic hormonal activity has been reduced relative to the tissue building activity
  • Anabolic actions include
    > Protein anabolism, increased muscle mass, Ca and P retention
    > Increase erythrocyte development in bone marrow
  • No veterinary products currently available in SA for small animals and horses
  • Nandrolone, Boldenone available overseas
  • For cattle there is trenbolone acetate
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8
Q
  • Anabolic steroids Clinical uses:
A

o Growth promoting in feedlot cattle
- Promotes growth, feed efficacy, lean carcass formation
o For geriatrics; recovery of chronic debilitating conditions
o Improvement of post-surgical wound healing
o Counter catabolic action of glucocorticoids
o Improve renal function in chronic interstitial nephritis
o Counter effects of hypoplastic anemia
o Treatment of androgen sensitive carcinomas

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9
Q
  • Anabolic Steroids Side effects
A
o	Heptatotoxicity in humans 
o	Masculinization of females 
o	Electrolyte and water retention 
o	Infertility/impotence 
o	Teratogenicity 
o	Premature closure of growth plates 
o	Prostatic hypertrophy 
	Don’t use if there is pre-existing prostate pathology
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10
Q
  • Oestrogens Sources
A

o Natural oestrogen
 In most species; estradiol-17B, estrone and estriol
 Estradiol-17B secreted by the ovary; converted into estrone and estriol during liver metabolism
 The adrenal cortex and corpus luteum produce some oestrogen
 In late pregnancy large quantities of oestrogen are produced by the placenta
o Plant oestrogens e.g. subterranean clover (Trifolium spp)
o Synthetic oestrogen

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11
Q
  • Oestrogens Disposition
A

o Well absorbed from mucous membranes, GIT and injection sites
o Natural oestrogen has a high first-pass effect
o Very high plasma binding (natural oestrogens; sex-hormone binding globulin)
o Widely distributed, including the CNS
o Metabolized in the liver

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12
Q
  • Oestrogens Clinical Uses
A

o Treatment of urinary incontinence; oestriol
- Indicated for spayed bitches > 1 year of age
- Improves functioning of urethral sphincter
o Growth stimulant in feedlot animals (anabolic effects)
o Treatment of perianal adenomata, prostatic hypertrophy (including some prostatic tumours), testicular tumours and some mammary tumours
o Treat endometritis; endothelium-protective
o For misalliance; oestrogen prevents implantation and prolongs oestrus
o Treatment of pseudopregnancy (cabergoline or spaying give better and safer results)

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13
Q
  • Oestrogens Side effects
A
o	Bone marrow dyscrasia; lethal if overdosed in dogs 
o	Fatty changes in the liver (dogs) 
o	Iatrogenic pyometra secondary to Cystic Endometrial Hyperplasia (CEH) 
o	Mammary neoplasia 
o	Prolonged oestrus 
o	Vaginal prolapse in ewes 
o	Follicular cysts 
o	Decreased milk release
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14
Q
  • Oestrogens Veterinary Formulations
A

o Oestriol
- Urinary incontinence in female spayed dogs
o Oestradiol
- Growth promoter often together with progesterone or testosterone in ear implants
- Has anabolic effects
o Zeranol
- Oestrogen-like effects used for growth promotion

15
Q

Progesterones and Progestagens

A
  • Progestogens are synthetically produced and have similar actions as progesterones, produced by the CL for the maintenance of pregnancy.
  • Overall, they inhibit the release of gonadotrophin releasing hormone (GnRH). Oestrus prevention!
  • Progesterone is the hormone responsible for maintenance of pregnancy and mostly produced mostly by the corpus luteum, then smaller amounts from the placenta and adrenals.
  • Progesterone increases endometrial gland growth and secretions and causes mammary alveoli development.
  • Progesterone also some anabolic effects and behavioural effects.
16
Q
  • Progesterone and progestagens Clinical Uses
A

o Oestrus synchronization and anoestrous in sheep and cattle
o Physiological concentrations help maintain pregnancy in case of threatening abortion
o High concentrations prevents implantation and decidualisation (cellular changes of endometrium that allows placenta formation)
o Used for treatment of military dermatitis in cats
o Behavioural problems
 Urine spraying (cats)
 Aggression
o Non-specific anabolic effect and appetite stimulant
o Prostatic hyperplasia, vaginal hyperplasia, pseudopregnancy
o Inhibition of oestrus cycle in small animals (AVOID!)

17
Q
  • Progesterone and progestagens Side effects
A

o Local skin/tissue reaction at site of injection
o Weight gain (polyphagia), PU/PD
o Anabolic and renal effects
o Diabetes mellitus (Insulin resistance)
o Atrophy of the adrenal gland  don’t combine with corticosteroids
o Cystic endometrial hyperplasia, possibly leading to pyometra – don’t use to prevent heat in cats and dogs
o Hyperplasia, milk secretion and a probable increase incidence of mammary tumors

18
Q
  • Progesterone and progestagens Veterinary formulations
A
o Progesterone 
- Heifers and cows
o Flugestone 
- Ewes
o Altrenogest 
- Gilts,
- Oral
o Norgestomet and estradiol valerate 
o Proligestone 
- Suppress or postpone oestrus in dogs 
- Can cause prolonged anoestrus 
- Risk of causing pyometra 
- Used to treat miliary dermatitis in cats 
o Melengesterol acetate 
- Growth promoter in cattle
19
Q
  • Progesterone and progestagens Old formulations
A

o Megesterol acetate (Ovarid®)
o Suppress oestrus in bitches
o Treat vaginal hyperplasia and pseudopregnancy in bitches
o To control unacceptable male behavior
o In cats to treat various progestin-responsive dermatological problems
- Medroxyprogesterone acetate

20
Q
  • Medroxyprogesterone acetate
A

o Suppress oestrus in bitches
o treat certain behavioral disorders such as aggression and male cat spraying
o treat dermatological disorders

21
Q

Aglepristone

A
  • Oestrogens historically used for misalliance → swelling of the fallopian tube
  • Aglepristone is a safer, more effective abortifacient in cats, dogs and rabbits
  • Has a higher affinity for uterine receptors than endogenous progesterone
  • Effective for up to 45 days after mating
    o Prevents implantation in early pregnancy
    o Abortogenic in later pregnancy
  • Used extra-labelly for pyometra treatment and inducing parturition (dogs)
  • Two SC injections, 24hrs apart (be precise with timing)
    o Abortion within 4 days after treatment
22
Q

Prostaglandins F alpha two Clinical uses

A

oCattle and sheep (latter extra-label)
 Oestrous synchronization
 Abortifacient (C:1 st 5 months, S: duration)
 Induction of parturition (C: last 2 weeks)
 Treat luteal cysts (C)
 Treating pyometra and foetal mummification
 Silent heat or subclinical oestrous (C)

oPigs 
	Induction of parturition
o	
Horses 
	Pyometra 
	Oestrous synchronization; improves breeding efficiency 
	Abortifacient 

oDogs and cats (extra-label)
 Abortifacient
 Cystic endometrial hyperplasia/pyometra complex

23
Q

Prostaglandins F alpha two Side effects and contraindications

A

o Abortifacient or parturition inducer
o Bronchoconstriction – care with asthma or other respiratory diseases
o Contraindicated in cardiopulmonary disease
o Don’t use to treat closed-cervix pyometra otherwise risk uterine rupture
o Drug reaction in some species – animals uncomfortable, restless, ataxic, vomiting etc.

24
Q

Prostaglandins F alpha two Veterinary formulations

A

o Cloprostenol (Estrumate)
- Bovines, pigs
o Dinoprost (Lutalyse, Enzaprost)
- Bovines, equines, pigs

25
Q

Ecbolics and Tocolytics

A
  • Ecbolics induce uterine contractions and causing expulsion of the foetus
  • Tocolytics suppress labour or uterine contractions to delay parturition
26
Q

Oxytocin

A
  • A nonapeptide released from the neurohypophysis by nerve impulses
    o Increased by afferent impulses which originate from the dilating cervix and anterior vagina
  • Synthesized oxytocin is commercially available and is physiologically and chemically like natural oxytocin
  • Administered intramuscularly or intravenously
  • Used in most species to increases strength and frequency of uterine contractions
    o Dependent on conditioning by progesterone (pregnancy), generally best response when oestrogen levels are high and in patients already in labour
    o Caution if cervix not dilated or birth canal obstructed (uterine rupture)
  • Promotes milk let down (contraction of mammary myoepithelial tissue)
  • Adrenaline at physiological levels markedly reduces the effect of oxytocin on the uterus or mammary gland
27
Q
  • Oxytocin Clinical Uses
A
o	Aid expulsion of the placenta, evacuation of uterine debris and aids involution, incl. after caesarian section 
o	To control uterine bleeding 
o	Primary inertia in small animals 
o	Induce parturition in mares 
o	Galactagogue – especially in sows
28
Q
  • Oxytocin Veterinary formulations
A

o Intertocin-S, Fentocin

29
Q

Clenbuterol

A

-Beta 2 agonist
-Stops uterine contractions for 6 – 8 hours
-Used to manage dystocia
o Correct presentation
o Prepare for surgery (caesarean)
o Beta-mediated vasodilation increases foetal perfusion
o Replace prolapsed uterus

29
Q

Bovine Somatotropin

A
  • A naturally occurring growth hormone produced in the pituitary gland
    -rBST is BST produced by recombinant DNA (bacterial) technology
    o Boostin®
    o Supplementation is used to increase milk yield
  • BST upregulates IGF in liver; redirection of nutrients from fat to mammary glands and milk formation (10% increase)
  • Only with food-compensation
  • SC injection
    o Repeat every 14 or 28 days from the 9th week of lactation
  • No milk withdrawal
    o Protein hormone, not a steroid, so activated when taken orally (biologically inactive in humans)
30
Q

Chorulon

A
  • Females: “ovulatory failure” (anoestrous, suboestrous, prolonged oestrous, cysts); assist with fertility
  • Males: temporary increase in testosterone
  • Induce early abortion, stimulate lactation
31
Q

Folligon

A
  • Females: “ovulatory failure” (anoestrous) and superovulation after synchronization (ere embryo transfer)
  • Males: help with spermatogenesis
32
Q

PG 600

A
  • Females: to increase fertility and litter size

- Used in pigs