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Pharmacology > Hormones > Flashcards

Hormones Flashcards

1
Q

Growth hormone

A
  • Protein (not PO),controlled by GHRH, GH plasma levels and Gherlin polypeptide (GI, hypothalamus)
  • Inc. by sleep, excersice, stress , HYPOglycaemia, dopamine, alpha-agonists. => Giantism/acromegaly
  • Dec. GC, HYPERglycaemia, beta-agonist=> dwarfism
  • Stimulates IGF-1 secretion , anabolic hormone
  • Use: inc. milk production and meat quality, alopecia in dog.
  1. Synthetic analogue: Octreotide, Lanreotide
  2. Dopaminergic agents: Cabergoline
  3. GH receptor antagonist:(IGF-1 inhib.)Pegvisomat (Somavert)
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2
Q

ACTH

A
  • Protein, inc. synthesis of enzyme involved in steroid biosynthesis (cholesterol ->pregnenolone)-. Inc. cortisol and corticosterone levels.
  • indications: dec. GC , cow ketosis, adrenal cortex atrophy, stimulation test, Adrenocortical hypo/hyperplasia.

Addison’s disease:
fludrocortisone. SE:increased blood pressure, inflammation, hypokalemia, hypernateamia

Cushing syndrome:
*Pituitary induced hypercortisolism:
Bromocriptine, Cyproheptadine
* Adrenal gland induced hypercortisolism :
1. Trilostane: selective inhibitor of 3B-hydroxysteroid dehydrogenase. SE: GI, lethargy, acute pancreatitis , addison’s crisis.
2.Ketoconazole weekly increasing dose.
3. Mitotane (must be avoided!)

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3
Q

TSH

A

*glycoprotein, no approved veterinary product in the market
*Effect: inc. iodine uptake by the thyroid gland, production and secretion of thyroid hormones.
*Used to diagnose primary hypothyroidism.
*inc. GH, GnRH, cortisol production + dec. prolactin
Hypothyroidism:
1. Iodine containing agents: iodised salt, Lgol solution
2. levothyroxine-Na
3.liothyronine (Lack of tissue deiodinase) overdose: hyperthyroidism like signs

Hyperthyroidism: mostly Cats!
1.Methimazol/Tiamazol
Side-effects: Liver damage, emesis, immune mediated haemolytic anaemia, facial pruritus

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4
Q

ADH

A

*protein hormome, responsible for water and Na retention , K excretion.
*Binds V1a (endothelium) -vasoconstriction
V2 (renal tubules) - inc. water absorption by aquaporin-2
*Use: diagnosis+ treatment of central diabetes insiphidus. Differential Diagnosis of diabetes mellitus

  1. Natural vasopressin nasal spray: short HL+BA, local irritation
  2. Desmopressin (synth. Analouge) - SC,PO,nasal, longer
  3. Chlorpropamide: PO, antidiabetic
  4. In syndrome of inappropriate ADH (overproduction): Conivaptan (IV, V1+V2 antagonist) , Tolvaptan , Lixivaptan (V2 antagonist)
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5
Q

Insulin

A

Protein, preproinsulin>proinsulin>insulin , stored in secretory granules in a complex with zinc (B-cells), exocytosis (ATP-dep K channels> inc. Ca>Ca-calmodulin protein kinase>fusion of granules with membrane)

  • Inc. IC uptake of glu,AA,FA,K. Anabolic hormome- glycogenesis, lipogenesis, protein synthesis
  • Degraded rapidly by insulinase
  • Indications: DM in cat+dog, fatty liver+ ketosis in Bo

DM I: SC

  1. Caninsulin:Swine origin (lente insulin) - amorphous (intermediate duration) , crystalline (prolonged,12-24h) higher Zn content+acetate buffer
  2. Insuman® Rapid
  3. Human ProZinc®

DM II: PO
1. Acarbrose: alpha-glucosidase inhibitor (latent carbohydrate absorption- after meal) - dogs+cats
2. Sulfonylureas: increased insulin secretion.
Glipizide - cats, gliclazide ,glibenclamide
3.Biguanides decrease of insulin resistance. (metformin, Buformin)
4. Glinides: increased insulin secretion. (nateglinide)
5. Glitazones: activation of nuclear receptors, liver, adipose tissue and muscles increased insulin sensitivity. (pioglitazone)

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6
Q

Insulin: adverse effects and interactions.

A
  • Adverse effects: acute hypoglycemia, Somogyi rebound effect (hypoglycemia->hyperglycaemia due to compensation by anti-insulin hormomes), allergy,Ab
  • Interaction: hyperglycaemic (GC,dobutamin, oestrogen, progesterone,xylazine, thiazides diuretic)+hypoglycaemic drugs (,B-blockers,MAO inhibore, phenylbutazone, anabolic steroids, salicylates
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7
Q

Oral anti-diabetics warnings

A
  • Mainly type-2 diabetes (NIDD, Insulin resistancy)

* Warnings: Hypoglycaemia, serious liver/kidney insufficiency

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8
Q

Oral antidiabetics: Sulphonylurea substances:

A

*Inc. insulin release, sensitivity in cells, receotors, binding, glucagon release.
*5 drugs:
Tolbutamide (short, CV SE)
Chloropropamide (long acting , also for Diabetes insiphidus)
Metahexamide, Glibenclamide, Glizipine

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9
Q

Oral antidiabetics: Biguqnides

A
  • inc. utilization in cells, dec. Glu oral absorption
    1. Fenformine (phenyl-ethyl)
    2. Buformine (Butyl): ADEBIT
    3. Methformine (Dimethyl)
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10
Q

Oral antidiabetics:

  1. Thiazolidine diones
  2. Acarbos
A
  1. Modulation of insulin dependent genes , reduction of blood sugar level
    * No experience in veterinary (glitazones, troglitazones, draglitazone)
  2. Inhibition of alpha-glycosidase (e.g alpha-amylase) activity; less rapid elevation of glu blood level after meal
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11
Q

Mineralocorticoids: Addison’s disease (hypoandrenocorticism)

A
  1. Aldosterone: in research
  2. Desoxycorticosterone pivalate: long acting, IM + hydrocortisone/GC replacement
  3. Fludrocortisone acetate: PO, slight GC effect

*SE: Hypokalemia (>muscle weakness), hypernatraemia, water retention (hypertension) , inflammation susp.

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12
Q

Mineralocorticoids: Cushing’s disease

Hyperadrenocorticism

A

K 9-85%
*Pitutary dependant:
Bromocriptine , Cyproheptadine-HCl (PERITOL)

*Pitutary/adrenal dependent:
Ketoconazole , Mitotane , Trilostane (selective inhibition of 3BHSD)

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13
Q

Thyroid hormones: hypothyroidism

A

More common, may arise from iodine def. , Feeding cabbage (ru), thyroid malfunction (primary), TSH def. (Secondary)

  1. L-thyroxine/Levothyroxine: PO
  2. L-thyroxine-Na : IV,SC
  3. L-tri-iodothyronine (T3): PO, only imducated when Levothyroxine had failed. Rapid onset , short durations
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14
Q

Calcitonin

A

Control hyperglycaemia (Paget’s disease, ergocalciferol , vit. D2 poisoning)

Salcatonin (from salmon)

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15
Q

Calcitonin

A

Control hyperglycaemia (Paget’s disease, ergocalciferol , vit. D2 poisoning)

Salcatonin (from salmon)

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16
Q

Thyroid hormones: hyperthyroidism

A
  1. Iodine (I131 isotope): before surgery, to block T3+4 release, highly radioactive, short HL
  2. Tiouracil: SE: Emesis, liver, liver, haemolytic anemia
  3. Propylthiouracil
  4. Thiamazole (methimazole): its prodrug is carbamazole which also used in therapy
17
Q

GnRH

A

*Hypothalamus (Optic+suprachiasmatic areas), small amount in uterus+ovaries
*Pulsative release, same Composition in all mammals
*Action: stimulates the production of LH and FSH
1. Deslorelin: SUPRELORIN SC implant , make dogs for 6 months
2. Gonadorelin: cow+eq+su+rabbit
3.Buserelin: eq
4. Fertirelin: cow
5. Lencirelin: cow
SC,IM

*indications: reduce time interval btw calving to ovulation, treat ovarian follicilar cyst, control ovulation time+synchronization, induce ovulation in rabbit, inc. fertility in su, chemical castration in Hu+K9

  • SE: hyperthermia, allergy, corpus luteum cyst.
  • Don’t use in pregnant/starved animals
18
Q

FSH

A
  • inc. growth of follicles by granulosa cells (ovaries) *spermatogenesis by Seretoli cells (testis)
  • Indications: super-ovulation in donor cows used for embryo transfer.
19
Q

LH

A
  • final maturation of the follicle and estrogen secretion
  • Inc. testosterone secretion by Leydig cells
  • Indications: to induce ovulation, lueinize follicilar cyst
20
Q

PMSG, eCG

pregnant mare serum gonandotropin

A
  • glycoprotein, secreted by endometrial cups of pregnant mares in early pregnancy in order to maintain the corpus luteum (which maintains high progesterone levels to sustain the pregnancy)
  • Indications: follicular growth and ovulation, to induce super-ovulation. Males: inc. spermatogenesis+libido
  1. WERFASER inj.
  2. GONADOPHYL inj.
  3. SUIDAN inj.
    * Combination with hCG to treat post weaning anoestrus in su
21
Q

hCG

Human chronic gonandotropin

A

Glycoprotein, secreted from the chorionic portion of placenta , HL 12-24h
*Used as LH: female: ovulation (eq), nymphomania dye to cystic ovaries. Male: treating cryptorchidism

  1. WERFACHOR inj. , NYMFALON inj. (+Progesterone)
  2. P.G 600 inj.n, SUIDAN inj. (+PMSG)
  3. PROLAN inj. (+ oestradiol) - su, ovulatio
22
Q

Sex hormone steroid pathway

A

Cholesterol=> Pregnenolone=> Progesterone=> Testosterone=> Estrogen
*Fat soluble , short HL, protein bound in blood

23
Q

Natural estrogen: oestrone , oestradiol-17-B , oestriol

A
  • produced by granulosa cells , corpus luteum, adrenal cortex,testis, placenta
  • Effects: female sex organs development, 2ndary sex character, inc. cervical mucosa , Na +H2O retention, ossification, epiphyseal closure, GnRH release (dose dep)
  • Pharmacokinetics: skin, mucous membranes, GI,SC,IM

*Use: female: dog-treatment for uterine infections, inhibition of nidation, urinary incontinence, dermatitis , stop lactation, presidtant CL in bo.
Male: anal adenoma , prostate hypertrophy/benign tumor

*SE: cow: prolapse vagina,uterus. Dog: anaemia, endometritis , ovarian supression and hypoplasia- ovarian cyst , feminisation in male.
NOT used in pregnancy or mammary tumours

  1. OESTRADIOL BENZOATE inj
  2. Estradiol bcypionate - ECP inj.
  3. Estradiol valerate
    * Combinations: PROLA-s inj. (HCG) , SEROSAL tab. (Methyltestosterone) , CRESTAR sc implant
24
Q

Anti-estrogen compounds

A
  1. Aromatase inhibitor of estrogen synthesis (anastrozole, letrozole)
  2. Estrigen receptor modulators:
    i. Tamoxifen - treats estrogen-dep. Mammary tumors
    ii. Raloxifene- antagonist in mammary gland and uterus, agonist in bones
    iii. Clomiphene- only cebtrak (hypothalamic-pitutary)
25
Q

Progesterone

A

Two effects:

  1. Nidation and maintanance of pregnancy
  2. Supression of oestrus and blocking ovulation
    * Transforms proliferative endometrium to secretory endimetrium in pregnant animals, inhibits uterine contractions
    * Main source: corpus luteum. But also produced in adrenal cortex, placenta.
26
Q

Androgens:

Testosterone , Dihydrotestosterone, Androstenedione

A
  • stimulate spermatogenesis , 2ndary make characteristics, muscle development
  • Use: treatment for infertility, hypogonadism, aspermia , dec. Libido. Hormonal alopecia
  1. Andriol caps, Retandrol oil inj., Serosal tab.
27
Q

i. Anabolic steroid

ii. Anti-andriogen

A

i. Stanozolol, Nandrolone, Methandienone

  • Use: chronic disease accompanying with weight loss , erythropoietin stimulation, bone regeneration
  • SE: vasoconstriction, heart faliure, impotence sperm

ii. Ciproterone , Delmadinon

28
Q

Prostaglandins

A

Released in the endometrium, late in diestrus, near term pregnant animal
* Function: reproduction (PGF,PGE) and inflammation + membrane protection (PGE)

  1. Alfaprostol, PGF2alfa- Dinoprost
  2. Cloprostenol
  3. Luprostiol
  • Use: oestrus synchronization, to induce parturition , abortion, pyometra
  • SE: colic, nausea, vomiting , diarrhrea, bronchoconstriction, abortion
29
Q

Oestrus synchronization: Progestogens/Progestagens

A

Type 1- strong gastagens (1st, MAP)
Type 2- weak gastagens (2nd Proligeston)

  1. Medroxy progesterone (MAP): control oestrus and ovulation, intravaginal sponge (VERAMIX) inhibits Oestrus in bitches (NEVER give in pro-oestrus).
    SE: cystic endometrial hyperplasia, mammary tumours
  2. Fluorogesterone (FGA): synchronization in ewe (CHRONOGEST intravaginal sponge)
  3. Norgestomet: string gestation, induce+sync ovulation in cow (CRESTAL imp)
  4. Proligestone and Megestol acetate: weak + antigonandotrophic effect , prevent or suppress ovulation (COVINAN inj. , OVARID inj.) Males: anal adenoma, …
  5. Anti-progestogens: abortion. Aglepristone (ALIZINE) , Dopamine receptot agonists: bromocriptine - prolactin inhibition- less prog. Secretion from corpus luteum
30
Q

Oestrus synchronization: Prostaglandins

A
  1. Cloprostenol
  2. Dinoprost PGF-2Alpha
  3. Etiproston
  4. Luprostiol

Other uses: pyometra, endometritis Abortion, induction of parturition. Eosterus synchronisation
SE: vomiting, diarrhrea, colic disorders, nausea

31
Q

Abortion induction

A
  1. Prostaglandins
  2. Antiprogesterone -Aglepriston, SC
    Side-effects: swelling, skin enlargement at injection site, pyometra/metritis
  3. Ergolines: cabergoline, bromocriptine Major indication pseudopregnancy in bitch Anti-prolactin effect Dopamine receptor modulators Emesis
32
Q

Myometrial stimulants

A
  1. Prostaglandins
  2. oxytocin: dystocia, milk let down , uterine bleeding, retention of foetal membrane and eggs (reptiles too) Side-effects: GI and cardiovascular system! Oxytocin inj., Oxitocinainj., Oxytocineinj., Dila-Part inj., Perlactonnasal spray
  3. carbetocinDepotocininj. synthetic analogue, long duration of activity
  4. Ergometrine, methylergometrine Postpartum + vasoconstriction
33
Q

Myometrial relaxants

A
  1. Beta2 adrenoreceptor agonists: clenbuterol, terbutaline
  2. Antispasmodics • papaverine, drotaverine ,denaverine

indications:
inhibition premature labour,difficult parturition ,intrauterine foetal procedures, reposition of uterus, -procurement of embryos from donors and implantation into the recipients

Pharmacology (25 decks)

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