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Pharmacology 2 > Hormones, ppt > Flashcards

Hormones, ppt Flashcards

1
Q

Somatotropin

  • Use, drugs
A

Use:

  • growth promoter?, to increase milk production, meat quality
  • replacement therapy
  • growth-hormone responsive alopecia in dog

Drugs:

  • Recombinant biosynthetic human GH, SC 0.1unit/kg 3 times/week
  • Somatrem: synthetic GH + one additionam meth. slow release inj. formulation
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2
Q

Somatotropin

  • GH inhibition
A

Overproduction excess of GH: Acromegaly or giantism

  • Synthetic somatostain analogues: Octreotide, Lanreotide
  • Dopaminergig agents: Cabergoline
  • Pegvisomant (Somavert): GH receptor antagonist, inhibition of IGF-1 synthesis
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3
Q

Corticotropin

  • Use
A
  • To increase glucocorticoid level where its already relatively or absolutely low
  • cow ketosis
  • to restore(recall) the function of adrenal cortex (after prolonged use of glucocorticoids)
  • stimulation test/differential diagnosis of adrenocortical hypo-and/or hyperplasia
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4
Q

Corticotropin

  • drugs
A

Natura ACTH with porcine origin

  • depot preparations are available for IM injections
  • Disadvantages:
  • short half life (15min), immunogenicity, orally ineffective)
  • Synthetic products without antigenic hazard:
  • Tetracosactride, Cosyntropin

CRH: synthetic human and ovine corticotropin-releasing hormone

  • use: CRH stimulation test
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5
Q

Thyrotropin (TSH)

  • Effect, Use
A

Effect: it increases iodine uptake by the thyroid gland and the production and secretion of thyroid hormones

Use:

  • in research
  • treatment of Acanthosis nigricans
  • to diagnose primary hypothyroidism TSH or biosynthetic
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6
Q

ADH, Vasopressin

  • Use, Preparations
A

Use:

  • diagnosis and treatment of total and partial central diabetes insipidus (DI)
  • separation from diabetes mellitus (DM) - differential diagnosis

Preparations:

  • Natural vasopressin nasal spray (short duration of action, local irritation, low PO bioavailability)
  • Synthetic analogue Desmopressin (with longer duration of action) injectible SC, oral and nasal spray dosage available
  • Other possibility: Chlorpropamide (oral sulfonylurea antidiabetics) PO
  • In DI Thiazide diuretics may be used, paradoxical action
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7
Q

Overproduction of ADH = SIADH

  • preparations
A
  • Conivaptan: only IV (less selective, also V1)
  • Tolvaptan and Lixivaptan: V2 receptor selective antagonists. PO

Non-specific drugs:

  • Demeclocycline derivate of Tetracycline
  • Lithium derivate of antidepressants
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8
Q

Lack of insulin results in:

A
  • Glucose intolerance, hyperglyceamia, glucosuria
  • PU/PD, saluresis (Na, K)
  • weight loss
  • incomplete fat metabolism –> increased plasma FFA –> ketoacidosis –> Coma = complicated form of DM
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9
Q

Insulin

  • Use
A
  • to treat DM (dog and cat)
  • ketosis and fatty liver in cattle which are non-responsive to glucose or glucorticoid therapy alone (200-300 IU of Protamine Zinc Insulin)
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10
Q

Classification of insulin containing items according to:

A
  1. Origin:
  • Natural: bovine or porcine
  • bio-synthetic: gene transfer
  1. Purity: purification eg. by column-chromatography
  2. Formulation: rapid-depot, Semilente-lente-ultralente
  • Regular (Crystalline zinc, soluble) insulin: Rapid onset, short duration of action, depends on route of admin: IV (4-8), SC, IM
  • Insulin Zinc Suspension (Lente insulin) Caninsulin: Higher Zn content + acetate buffer, suspension, intermediate duration, crystalline more prolonged (12-24 hr).
  • Protamine Zinc Insulin (PZI): suspension of insulin modified by addition of protamine sulphate and zinz chlroide in buffered water - duration 24-36 hr.
  • Isophane insulin (Neutral Protamine Hagedorn =NPH): suspension of zinc insulin crystals and protamine zinc in buffered water - cloudy milky suspension, duration 12-30 hr. (possible BID application)
  • Surfen insulin: long activity - aminoquinuride surfactant
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11
Q

Insulin

  • side effects, interactions
A

Side effects:

  • acute hypoglycaemia: excessive insulin dose or inadequate food intake
  • Somogyi rebound effect: hypoglycaemia induced hyperglyceamoa due to compensatory release of insulin-antagonistic hormones (glucagon, catecholamines, glucocorticoids, growth hormone)
  • allergic reactions, antibody formation

Interactions:

  • drugs which reduce hypoglycaemic activity: glucocoticoids, dobutamin, oestrogen/progesterone, xylazine, thiazide diuretics
  • Drugs which increase hypoglycaemia activity: anabolic steroids, beta-adrenergic blockers (propranolol), MAO inhibitors, phenylbutazone, salicylates, alcohol
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12
Q

Oral antidiabetics

  • preparations/groups
A

(orally active hypoglycaemic drugs)

Mainly used in “Type” insulin non-dependet diabetes. Warnings: hypoglycaemia, serious liver or kidney insufficiency

Preparations:

  • Sulphonylurea substances
  • Biguanides
  • Thiazolidine diones
  • Acarbos
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13
Q

Oral antidiabetics

Sulphonylurea substances

A
  • Sulphonylurea substances
  • Tolbutamide: short action, cardiovascular side effect
  • Chlorpropamide: long acting (see ADH too)
  • Metahexamide
  • Glibenclamide
  • Glipizide

​Action:

  • release of insulin increase
  • sensitivity of the cells to insulin increase
  • number of receptors increase
  • the binding of insulin to plasma proteins decrease
  • glucagon releases decrease
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14
Q

Oral antidiabetics

  • Biguanides
A

Biguanides:

  • Fenformine
  • Buformine
  • Methformine

Action:

  • Stimulation of the action of insulin (increased utiliztion in cells), decreased oral absorption of glucose
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15
Q

Oral antidiabetics

  • Thiazolidine diones
A

Thiazolidine diones

  • Glitazones
  • Troglitazone, draglitazone

Action:

  • veterinary experoences are not available
  • modulation of insul dependet genes, reduction of blood sugar level
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16
Q

Oral antidiabetics

  • Acarbos
A

Acarbos:

  • in GI inhibition of the alpha-glycosidase (eg. amylase) activity,
  • less rapid elevation of blood sugar level after food consumption
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17
Q

Preparations for Hypothyroidism

A
  1. Crude thyroid products (past)
  2. Synthetic preparations:
  • L-thyroxine/Levothyroxine: Forthyron 200 or 400tabl. Dog, cat, horse, SID, BID. PO
  • L-thyroxine-Na: dog. Injectable IV or SC
  • L-tri-iodothyronine (T3, Liothyronine): Dog, TID. PO. Only indicated when Levothyroxine therapy has failed. T3 has more rapid onset and shorted duration (2 days) of action than T4
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18
Q

Preparations for Hyperthyroidism

A
  1. Iodine: before surgery, to block release of T3 and T4
  2. 131I Isotope: highly radioactive, very short half-life (8 days)
  3. Thiouracils
  • Thiouracil 12 mg/kg: more side effects: emesis, liver, haemolytic aneamia
  • Propylthiouracil: 5mg/cat 3x
  • Thiamazole (Methimazole): 5mg/cat 3x. Its prodrug is the Carbamazole.
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19
Q

Preparations for treatment of Hypoadrenocorticism (Addisons) + side effects

A

Preparations:

  • Aldosterone - available only for reaserch
  • Desoxycorticosterone pivalate (DOCP): a long acting ester of Desoxycorticosterone acetat (DOCA) - available as a sterile suspension for IM inj. + hydrocortisone/glucocorticoid replacement. Dog
  • Fludrocortisone acetate: PO, Dog. Every 12 hours orally. Slight glucocorticoid side effect

Side effects:

  • hypokalaemia
  • hypernatreamia, water retention
  • muscle weakness
  • hypertension
  • increased susceptibility to inflammation
20
Q

Preparations for treatment of Hyperadrenocorticism (Cushings)

A

Pituitary-dependent Cushings (K9=85%):

  • Bromocrptine: dog, horse, daily 2x
  • Cyproheptadine-HCl (PERITOL syrup dog, horse)

Pituitary-and/or Adrenal-dependent Cushings:

  • Ketoconazole
  • Mitotane (LYSODREN): highly effective but toxic
  • Trilostane (VETORYL capsules/drops): selective inhibition of 3BHSD
21
Q

Hormones affecting reprodution

  • classification:
A

Sex steroids:

  • oestrogens, androgens, gestagens

Other types:

  • Gn-RH analogues
  • pituitary and non-pituitary gonadotrophins
  • prostaglandins
  • oxytocin
  • melatonin
22
Q

Gonadotrophic releasing hormone (GnRH):

  • preparations
A

Synthetic forms and anlouges are available (nonapeptides)

Application: SC, IM, IV (only Eq), SC implants for chemical sterilization

Preparations:

  • Gonadorelin: horse, cow, swine, rabbit
  • Buserelin: horse, cow, rabbit
  • Fertirelin: Cow
  • Lecirelin: Cow
  • Deslorelin: Suprelorin SC implant, male dogs, 6 month duration
23
Q

Gonadotrophic releasing hormone (GnRH):

  • Indications, Side effects
A

Indications: wide range of species

  • to reduce the time interval from calving to first ovulation
  • for treatment of ovarian follicular cysts in dairy cattle
  • to contrl the time of ovulation at the end of prostaglandin or progestogen synchronisation schedule
  • to allow the timing of ovulation and covering to be arranged more prcisely in mares during oestrus –> to maximise the chance of conception and nidation
  • to provoke ovulation in rabbits
  • to increase fertility stripping, reducing egg binding
  • chemical castration

Side effects:

  • hyperthermia, allergic reaction
  • corpus luteum cysts
  • should not be used in pregnant animals (embryo death)
  • should not be used in starved cachectic animals
24
Q

Non-pituitary gonadotrophins

  • PMSG, eCG: indications, preparations
A

Pregnant mare serum gonadotrophin

Indications:

  • Female: to induce follicular growth and ovulation (alone or after pretreatment with progesterone), for superovulation (increase litter size, embryo transfer)
  • Male: to stimulate speratogenesis and libido

Preparations:

  • Werfaser inj.
  • Gonadophyl inj.
  • Suidan inj. + hCG
  • Combination with hCG is effectively used for treatment of post-weaning anoestrus in sows.
25
Q

Non-pituitary gonadotrophins

  • hCG: indications, preparations
A

Human Chorionic Gonadotrophin

Indications:

  • Females: to cause ovulation in the mare at time of breeding, for the treatment of nymphomania due to cystic ovaries, for ovarian stimulation
  • Males: in treatment of cryptorchidism

Preparations:

  • Werfachor inj.
  • P.G 600 inj.
  • Nymfalon inj. + progesterone
  • Suidan inj. + PMSG
  • Prolan S inj. + oestradiol: in sow to provoke ovulation
26
Q

Oestrogens

  • indications, side-effects:
A

Indications:

Females:

  • to control reproduction is limited
  • in the treatment of uterine infections
  • inhibition of nidation - misalliance in the bitch
  • to treat urinary incontinence and dermatitis in old ovariextomised bitches
  • to diminish (or stop) lavttion in bitches and cats
  • to treat cattle having persistent CL due to certain cases

Males:

  • anal adenoma, prostate hypertrophy, benign tumour

Side effects:

  • in cow: postparturient straining with prolapse of vagina, uterus
  • in dog: aneamia, endometritis
  • ovarian suppression and hypoplasia -> ovarian cysts
  • feminisation in the male
  • it should not be given to animals with mammary tumours, during pregnancy
27
Q

Oestrogens

  • preparations
A

Veterinary preparations:

  • Oestradiol benzoate inj.
  • Oestradiol cypionate - ECP inj.
  • Oestradiol valerate

Combinations:

  • Prolan-S inj (hCG), Sesoral tabl. (methyltestosterone)
  • PRID: A Progesterone-releasing intravaginal devide
  • Crestar SC. implant + Norgestomet

Stilbenes: Diethylstilbestrol, Hexoestrol

  • synthetic non-steroidal oestrogens, have high oral activity, are not easily metabolised, are carcinogenc –> PROHIBITED!

Zeranol: synthetic analouge of mould toxin Zearalenone with oestrogenic, anabolic activity

28
Q

Anti-oestrogenic compounds:

A
  1. Aromatase inhibitors of estrogen synhtesis: Anastrozole, letrozole
  2. Oestrogen Receptor Modulators, mixed agonists/antagonists.
  • Tamoxifen: treatment of oestrogen-dependent mammary tumour
  • Raloxifen: antagonist in mammary gland and uterus, agonist in bones
  • Clomiphene: only central (hypothalmic-pituitary) effect
29
Q

Progestogens

  • Progesterone indication
  • Types of synthetic preparations
A

Progesterone indication:

  • synchronisation
  • to prevent embryonic death: not satisfactory
  • to delay parturition: not effective

Synthetic preparations:

  • Type 1 - 1st generation: MAP, Norgestomet
  • Type 2 - 2nd generation: Proligeston
30
Q

Progestogens

  • classification
A
  • MAP, FGA, Norgestomet,
  • Proligestone and Megestrol acetate
  • Altrenogest (allyl-trenbolone)
  • Melengestrol acetate (MGA)
  • Antiprogestogens: Aglepristone, dopamin receptor agonists.
31
Q

Progestogens

  • Medroxy progesterone (MAP): indications, preparations, side effects
A

Indications:

  • to control oestrus and ovulation in cyclic ewes
  • to induce oestrus in anoestrus ewes adminstration as intravaginal sponge : VERAMIX
  • To inhibit onset of the next oestrus i bitches with mid-oestrus (should not be given in pro-oestrus!): Depo-promone inj. , provera tabl.

Side effects: cystic endometrial hyperplasia, mammary tumours

32
Q

Progestogens

  • Flurogestone acetate (FGA) and Norgestomet
A

Fluorogestone acetate (FGA)

  • oestrus synchronisation in wew
  • Chronogest intravaginal sponge

Norgestomet:

  • strong gestagen
  • to induce and synchronise ovulation in heifers and cows
  • Crestal implant
33
Q

Progestogens:

  • Proligestone and Megestrol acetate: indications, preparations
A

Indications:

- Females:

  • to prevent or suppress oestrus and ovulation in companion animals
  • Covinan inj., Ovarid tabl.

- in males:

  • anal adenoma, prostate hyperthrophy, beign tumour
  • increased sexual activity, strange behaviour
34
Q

Progestogens:

  • Altrenogest, Melengestrol acetate (MGA): indications, preparations
A

Altrenogest (allyl trenbolone)

  • oestrus synchronisation, is used in mares and sows. PO
  • it is absorbed from skin - use with care

Melengestrol acetate (MGA):

  • to suppress oestrus in heifers and increase growth (oral) –> banned in EU
  • side effects: forms cysts –> elevated oestrogen level
35
Q

Antiprogestogens:

A

–> to terminate pregnancy - abortion

  • Aglepristone (Alizine): SC, 10mg/kg, a second dose after 24hr + PGF
  • Dopamin receptor agonists: Bromocriptine, Cabergoline - Prolactin inhibition –> less progesterone secretion by CL.
36
Q

Androgens

  • indications, preparations
A

Indications:

  • treatment of infertility, hypogonadism, aspermia, decreased libido. response is rater unsatisfactory
  • hormonal alopecia, certain mammary tumours
  • to treat androgen deficiency in old castrated dogs
  • androgenised cows for detection of oestrus in cattle and sheep

Preparations:

  • Andriol caps. : testosterone undecanoate
  • Retandrol mg oil inj.: testosterone phenylpropionate
  • Sesoral tabl: methyltestosterone and etinyl-oestradiol
37
Q

Anabolic steroids

  • indications, preparations, side effects
A

–> Stanozole, Nandrolone, Metandienone

Indiations:

  • in ageing animal or patient with chronic diseases, polytrauma, etc. suffering from weight loss
  • to promote recovery from debilitatind disease
  • stimulation of erythropoietin, bone regeneration
  • not for growth performance –> influence performance

Preparations:

  • Stromba tabl: stanozolole
  • Nerobol tabl: Metandienone
  • Nerobolil and Retabolil inj.: Nandrolone

Side effects:

  • vasoconstriction, heart failure, impotence, sperm deformity
38
Q

Anti-androgens

  • preparations
A

Ciproterone

Delmadinon

39
Q

Prostaglandins

  • synthetic analogues, indication, side effects
A

synthetic analouges:

  • Alfaprostol
  • PGF2alfa - Dinoprost: Dinolytic
  • Cloprostenol: Remophan, Estrumate, Planate
  • Luprostiol: Prosolvin
  • Etiproston: Prostavet-C

Indications:

  • oestrus synchronisation (mares, cows, ewes, goats)
  • to induce parturition (sows, mares, cows with glucocorticoids)
  • for abortion
  • for treatment of pyometra

Side-effects:

  • colic disorders, nausea, vomitting, diarrhea
  • bronchoconstriction
  • abortion
40
Q

Uterine stimulating agents and indications:

A
  • Oxytocin
  • prostaglandins
  • ergot alkaloids
  • cholinergic - parasympathetic drugs

Indications:

  • during prolonged parturition
  • to promote involution (flaccid uterus)
  • for post-parturient heamorrhage
41
Q

Oxytocin

  • indications, preparations, side-effects
A

Indications:

  • uterine interia: during delivery in all species
  • retention of eggs (birds and reptiles)
  • after parturition
  • milk let down (mastitis)
  • with special care: after c-section, after reposition of prolapsed uterine

Preparations:

  • Synthetic oxytocin: IV (slowly or 1:10 dilution), IM, SC.
  • sow: intra nasal spray
  • mare, cow, botch, quenn: injection
  • Fast metabolism: T1/2el = 1-6 min
  • PO inactive, F=0
  • Carbetocin (Depotocin inj.)
  • synthetic analouge of oxytocin
  • much longer half-life (less frequent inj. once daily)
42
Q

Ergot alkaloids

  • indication, preparations
A

Indications:

  • Ergotoxin: not used, tetany-like spasmodic effect
  • Ergotamine: only after parturition
  • Ergometrine:
  • potent uterine stimulant
  • rarely used during parturution
  • post-partum (haemorrhage, retained placenta) promotes the expulsion of the contents of the uterus

Preparations:

  • Methyl-ergometrine: without strong vascoconstrictor activity. Mare, cow, bitch. IM
43
Q

Prostaglandins

  • preparations, side effects
A

Preparations:

  • Etiproston: Cow. IM
  • Luprostiol: Mare, sow, cow. IM
  • Dinoporst: mare, cow, sow,. IM

Side effects:

  • colic disorders
  • nausea, vomitting, diarrhea
  • bronchoconstriction
44
Q

Uterine relaxing agents

  • groups, indications
A

Groups:

  • Beta2-adrenoceptr agonist (most significant)
  • Antispasmodics
  • Phenotiazines
  • Anticholinergics, eg atropine

Indications:

  • to prevent abortion?
  • to suppress contractions during
  • correction of mapresentation, during embryotomy, obstetrical manouevers
45
Q

Beta2-adrenoceptor agonists

  • indications, preparations
A

Indications:

  • facilitating of obstetrical manouevers,
  • replacement of prolapsed uterus,
  • recovery of embryo from donors,
  • handling of uterus during c-section

Preparations:

  • Isoxuprine
  • side effects: tachycardia, vasodilation, tremor, sweating
    • alpha1-adrenoceptor antagonist
  • IM
  • Clenbuterol: (PLANIPART inj.)
  • cow, once IM or slowly IV
  • Terbutaline: (BRICANYL)
  • same side ffects, but more transient
46
Q

Uterine relaxing agents:

  • the other preparations except beta2-adrenoceptor…
A

- Vetrabutin: (MONZALDON inj.) IM

  • papaverine-like drug
  • interrupts contractions caused by oxytocin
  • not as effective as Clenbuterol
  • contra-indicated in cats!
  • Denaverine: (SENSIBLEX inj.) SC, IM
  • toco-spasmolytic effect: elimination of intensive contractions of uterus, relaxing of cervix
  • Proquamezine, aminopromazine: (MYSPAMOL, Jenotone, inj. tabl.)
  • phenothiazine dericate
  • relaxes myometrium and cervix
  • indications: reposition of prolapsed uterine, spasms of urinary tract or esophagus
  • sheep, cow, horse

Pharmacology 2 (13 decks)

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