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
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
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
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
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
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
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
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
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)
10
Q
Classification of insulin containing items according to:
A
- Origin:
- Natural: bovine or porcine
- bio-synthetic: gene transfer
- Purity: purification eg. by column-chromatography
- 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
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
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
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
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
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
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
17
Q
Preparations for Hypothyroidism
A
- Crude thyroid products (past)
- 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
18
Q
Preparations for Hyperthyroidism
A
- Iodine: before surgery, to block release of T3 and T4
- 131I Isotope: highly radioactive, very short half-life (8 days)
- 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.
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
Non-pituitary gonadotrophins
- hCG: indications, preparations
*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
Oestrogens
- indications, side-effects:
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
Oestrogens
- preparations
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
Anti-oestrogenic compounds:
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
Progestogens
- Progesterone indication
- Types of synthetic preparations
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
Progestogens
- classification
* MAP, FGA, Norgestomet,
* Proligestone and Megestrol acetate
* Altrenogest (allyl-trenbolone)
* Melengestrol acetate (MGA)
* Antiprogestogens: Aglepristone, dopamin receptor agonists.
31
Progestogens
- Medroxy progesterone (MAP): indications, preparations, side effects
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
Progestogens
- Flurogestone acetate (FGA) and Norgestomet
_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
Progestogens:
- Proligestone and Megestrol acetate: indications, preparations
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
Progestogens:
- Altrenogest, Melengestrol acetate (MGA): indications, preparations
_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
Antiprogestogens:
--\> 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
Androgens
- indications, preparations
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
Anabolic steroids
- indications, preparations, side effects
--\> 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
Anti-androgens
- preparations
**Ciproterone**
**Delmadinon**
39
Prostaglandins
- synthetic analogues, indication, side effects
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
Uterine stimulating agents and indications:
* Oxytocin
* prostaglandins
* ergot alkaloids
* cholinergic - parasympathetic drugs
Indications:
* during prolonged parturition
* to promote involution (flaccid uterus)
* for post-parturient heamorrhage
41
Oxytocin
- indications, preparations, side-effects
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
Ergot alkaloids
- indication, preparations
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
Prostaglandins
- preparations, side effects
Preparations:
* **Etiproston:** Cow. IM
* **Luprostiol:** Mare, sow, cow. IM
* **Dinoporst:** mare, cow, sow,. IM
Side effects:
* colic disorders
* nausea, vomitting, diarrhea
* bronchoconstriction
44
Uterine relaxing agents
- groups, indications
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
Beta2-adrenoceptor agonists
- indications, preparations
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
Uterine relaxing agents:
- the other preparations except beta2-adrenoceptor...
**- 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
