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Drugs acting on CV and endocrine system Flashcards

1
Q

Drugs acting on CV system

A
  • ACE inhibitors (angiotensine-convertase enzyme)
  • Pimobendan
  • Digitalis glycosides
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2
Q

ACE inhibitors:

Pharmacological effects

A
  • vasodilatation -> hypotension
  • vena dilation -> decreased preload
  • arteriole dilation -> decreased afterload
  • stroke volume increases -> circulation is improved
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3
Q

ACE inhibitors:

Indications

A
  • Hypertonia (humans, cats)
  • Congestive heart failure (CHF)
  • Proteinuria (chronic kidney disease)
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4
Q

ACE inhibitors:

Pharmacokinetic

A

• well absorbed po., feeding does not affect absorption (except at captopril)
• in the liver enalapril (benazepril, ramipril) ->enalaprilat (benazeprilat, ramiprilat) transformation
->4-6 hs are needed for effect, but last for 12-24 hs
• no activation at captopril, has to be applied more frequently
• lisinoprile: biotransformation is not necessary ->can be given in hepatic failure

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5
Q

ACE inhibitors:

Side effects

A
  • hypotension ->tiredness
  • hyperkalaemia (together e.g. spironolactone) - not characteristic in dogs!
  • vomiting, diarrhoea, anorexia
  • azotaemia
  • dry coughing (especially captopril, humans)
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6
Q

ACE inhibitors:

Active substances

A
  • Captopril: feed affects oral absorption, has to be applied frequently (obsolete drug)
  • Enalapril
  • Ramipril
  • Benazepril
  • Lizinopril: also for patients with hepatic failure
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7
Q

PIMOBENDAN:

Indication

A

• Congestive heart failure

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8
Q

PIMOBENDAN:

Pharmacological effects

A
  • venous dilation ->decreased preload
  • arteriole dilation-> decreased afterload
  • positive inotropic effect
  • stroke volume increases ->circulation is improved
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9
Q

DIGITALIS GLYCOSIDES: Drug name and it´s pharmacological effects, indication, side effects

A

DIGOXINE
• Pharmacological effects: mild positive inotropic effect (negative chronotropic)
• Indication: CHF
• Side effect: several, small therapeutic index
• It is used only in severe cases that are not responding to ACE-inhibitors or pimobendan (with caution!)

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10
Q

Diuretics

A
  • Cardial diuretics
  • Osmotic diuretics
  • Natriuretics
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11
Q

Cardial diuretics

A
  1. ACE inhibitors:
    -inhibition of renin-angiotensin-aldosteron axis
    -limited effect
  2. METHYLXANTINES
    • CAFFEINE, TEOPHYLLINE, TEOBROMINE
    • limited effect
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12
Q

Osmotic diuretics: Drug name and it´s pharmacological effects and indication

A 
MANNIT
Pharmacological effect:
-not reabsorbed in the kidney
-osmotically retains
-water in the tubules
Indication:
• applied when acute renal failure is suspected 
• brain oedema
• pulmonary oedema
• ocular operations (intraocular pressure)
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13
Q

Natriuretics:

Indications

A
  • pulmonary oedema
  • brain oedema
  • other oedemas
  • hydrothorax, hydropericardium
  • maintenance of renal function
  • congestive heart failure
  • hypertonia
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14
Q

Natriuretics:

Loop Diuretics - effect and side effects

A

• Pronounced effect in 1-2 min (when given iv.)
Side effects:
• hypokalaemia (potassium-supplement!), metabolic alkalosis-> less important in dogs
• Ca2+, Mg2+ excretion incr. -> not recommended in case of bladder/kidney stones
• Ototoxic
• Potentiate the ototoxic and nephrotoxic effects of
aminoglycosides

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15
Q

Natriuretics:

Drug names

A
  1. Loop diuretics:
    - FUROSEMIDE (1-5mg/kg bw, po.,im.,iv.!)
  2. Thiazides:
    - HYDROCHLOROTIAZIDE, (CHLOROTIAZIDE) (1-2 mg/kg bw, po., im., iv.)
  3. Potassium-sparing diuretics:
    - SPIRONOLACTONE
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16
Q

Natriuretics - Thiazides: use and side effects

A

• Mainly used in human practice as combined preparations (e.g. with ACE-inhibitors) to decrease blood pressure
Side effects:
• Hypokalaemia-> potassium-supplement
• Metabolic alkalosis

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17
Q

Natriuretics:

Potassium-sparing diuretics and its effects and side effects

A

SPIRONOLACTONE
• Antagonism of aldosterone -> heart remodelling delayed! -> Na+ excreted, K+ retained
• Very slow effect! 2-3 days
• Minimal diuretic effect!
Side effects:
• rarely hyperkalaemia (incidence increased when applied together with ACE-inhibitors) -> not true in animals

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18
Q

Drugs acting on the endocrine system

A
  • GnRH analogues
  • Gonadotrop hormones
  • Progestagens
  • Progesteron antagonists
  • Estrogens
  • Prostaglandins
  • Other hormones
  • Dopamine agonists
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19
Q

GnRH analogues

A
  • Receptal inj. (buserelin)
  • Depherelin inj. (gonadorelin)
  • Fertagyl inj. (gonadorelin)
  • Suprelorin implantatum (deslorelin)
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20
Q

Gonadotrop hormones

A
  • Pregnyl inj. (hCG) – human

- P.G.600 inj. (hCG and PMSG)

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21
Q

Progestagens

A
  • Chronogest intravaginal sponge (flurogestone)
  • Crestar impl.+inj. (norgestomet+estradiol)
  • Regumate oral sol. (altrenogest)
  • Covinan inj. (proligestone)
  • Depo-Promone inj. (medroxyprogesteron-acetate)
  • Ovarid tabl. (megestrol acetate)
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22
Q

Progesteron antagonists

A

-Alizin inj. (aglepriston)

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23
Q

Estrogens

A
  • Mesalin inj. (estradiol benzoate)
  • Incurin tabl. (estriol)
  • Sesoral tabl. (ethinyl oestradiol + methyl testosterone)
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24
Q

Prostaglandins

A
  • Estrumate inj. (cloprostenol)
  • Dinolytic and Enzaprost inj. (dinoprost)
  • Prosolvin inj., Prostapar inj. (luprostiol)
  • Prostavet inj. (etiproston)
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25
Other hormones acting on the endocrine system
- Caninsulin inj. (insulin) - Vetoryl tabl. (trilostane) - Felimazole tabl. (methimazole) - Forthyron tabl. (L-thyroxine)
26
Dopamine agonists
-Galastop oral sol. (cabergoline)
27
Gonadotropin releasing hormones: effects
Stimulation of the production and release of FSH and LH
28
Gonadotropin releasing hormones: Indications
- Reduction of the time interval from calving to first ovulation. - Treatment of ovarian follicular cysts in dairy cattle. - Control the time of ovulation at the end of prostaglandin or progestogen synchronisation schedule. - Allowing the timing of ovulation and covering to be arranged more precisely in mares during oestrus → to maximise the chance of conception and nidation. - Provocation of ovulation in rabbits. - Increasing fertility rate in sows and fur-farming. - Rainbow trout: facilitate stripping, reducing egg binding. - Chemical castration (human, K9)
29
Gonadotropin releasing hormones: Side-effects, contraindications
- Hyperthermia, allergic reaction - Luteal body (CL) cysts - Should not be used in pregnant animals (embryo death) - Should not be used in starved, cahectic animals
30
Gonadotropin releasing hormones: Application
SC, IM (preferred), IV
31
Gonadotropins - HCG: | Effects
- LH- and some FSH-like activity. - It is used to supplement or replace luteinising hormone in cases of ovulation failure or delay, or to help control the timing of ovulation.
32
Gonadotropins - HCG Indications
- Ovulation in the mare at time of breeding. - Treatment of nymphomania due to cystic ovaries (by inducing luteinisation and possibly ovulation). - Ovarian stimulation. - Treatment of cryptorchidism (when no anatomical abnormality is present; genetical → exclusion from breeding).
33
Gonadotropins - HCG: Side-effects, contraindications:
- Anaphylactic reaction | - Pregnancy
34
Gonadotropins - HCG: Application
IM (preferred), IV
35
Gonadotropins - HCG: drug names
- PROLAN - S oily susp. - P. G. 600 inj. - SUIDAN inj. - WERFACHOR inj.
36
Gonadotropins - PMSG (eCG): Effects
-FSH- and some LH-like activity. -Advances the onset of follicular grow and ovulation.
37
Gonadotropins - PMSG (eCG): Indications
- Induction of follicular growth and ovulation (alone or after pre-treatment w. progesterone, progestagens - cow, goat ewe, or in combination with HCG, oestrogen in sow and anoestric bitches) - Superovulation (↑ litter size, embryo transfer) - Stimulate spermatogenesis and libido
38
Gonadotropins - PMSG (eCG): | Side-effects, contraindications
- Anaphylactic reaction | - Pregnancy
39
Gonadotropins - PMSG (eCG): | Application
SC, IM (preferred)
40
Gonadotropins - PMSG (eCG): | Drug names
- FOLLIGON inj. - GONADOPHYL inj. - P. G. 600 inj. - SUIDAN inj. - WERFASER inj.
41
Progesterones: effects
- They prepare and maintain the female reproductive tract for implantation and pregnancy. - They cause development of the mammary glands. - They exert a negative feedback effect on the hypothalamus-pituitary axis, inhibiting the GnRh – gonadotrophins production and release. - It leads to inhibition of ovulation in females and reduced testosterone production in males.
42
Progesterones: Indications
- Oestrus synchronisation - Control oestrus and ovulation - Induction of oestrus in anoestrus cows, ewes - Inhibition of the onset of the next oestrus in bitches and queens with mid-oestrus, suppression of oestrus in pro-oestrus
43
Progesterones: Side-effects, contraindications
- Cystic endometrial hyperplasia - Cystic ovaries - Mammary hyperplasia or nodules - Thinning and discoloration of skin (injectable preparations) - Operator safety, handling with care, particularly by women of child-bearing age
44
Progesterones: Application
Injection (SC, IM), PO, intravaginal devices, SC implant
45
``` Anti-progesterone: and its: 1. Indication 2. Side-effects 3. Application ```
- Aglepristone - Alizin inj. 1. Indication: Abortion, mammary gland cancer 2. Side-effects, contraindications: tissue irritation, excitement, depression, chronic kidney, liver failure, diabetes m. 3. Application: SC dogs (cats)
46
Prostaglandins: Effects
- Regression of CL - Increase activity of smooth muscle in uterus - Relaxation of cervix
47
Prostaglandins: Indications
- Oestrus synchronisation (two inj´s mares 14-18, cows 10-12, ewes and goats 11 days apart) - Induction parturition (sows, mares, cows with glucocorticoids) - Abortion - Treatment of pyometra
48
Prostaglandins: | Side-effects, contraindications
- Colic disorders - Nausea, vomiting - Diarrhoea - Bronchoconstriction - Abortion - Operator safety, handling with care, particularly by women of child-bearing age, asthmatics
49
Prostaglandins: Application
IM
50
Oestrogens: Effects
- Initiating behavioural signs of oestrus - Preparing female reproductive tracts for fertilisation - Developing of secretory tissue of mammary gland.
51
Oestrogens: Indications
- Misalliance (inhibition of nidation) - Urinary incontinence, alopecia (replacement) - Male: excess libido, anal adenoma, prostate hyperplasia
52
Oestrogens: Side-effects, contraindications
- Prolapse of vagina, uterus - Anaemia - Cystic endometrial hyperplasia → Pyometra - Ovarian suppression and hypoplasia → ovarian cysts - Feminisation of the male - Should not be given to animals with mammary tumours, during the pregnancy
53
Oestrogens: Application
SC, IM, PO
54
Other endocrine drugs - Levothyroxine - Forthyron tabl., Soloxine tabl. 1. Effects 2. Indication 3. Side-effects 4. Application
1. Effects: Effects of T3-T4 2. Indications: Hypothyroidism 3. Side-effects: Thyrotoxicosis, weight loss, nervousness, tachycardia, PU/PD etc. 4. Application: PO
55
``` Other endocrine drugs - Caninsulin inj. - Insulin 1. Effects 2. Indication 3. Side-effects 4. Application ```
1. Effects: Regulation of carbohydrate (protein, fat) metabolism 2. Indications: Diabetes mellitus 3. Side-effects: hypoglycaemia, (Somogyi-rebound effect), (Allergy) 4. Application: SC
56
``` Other endocrine drugs - Vetoryl capsules - Trilostane 1. Effects 2. Indication 3. Side-effects 4. Application ```
1. Effects: Competitive inhibitor of the enzyme 3-beta hydroxysteroid dehydrogenase. Works at the level of adrenal gland to block the normal steroidogenisis pathway of pregnenolone to progesterone to cortisol, aldosterone and androstenedione. 2. Indications: treatment hyperadrenocorticism (Cushing’s syndrome) 3. Side-effects: lethargy, weakness, vomiting, anorexia and diarrhoea, possibility of iatrogenic Addison's disease 4. Application: PO (dogs, cats /horses/)
57
``` Other endocrine drugs - Prolactin antagonists - Ergolides (Dopaminergic ergot amines) 1. Effects 2. Indication 3. Side-effects 4. Application 5. Drug names ```
1. Effects: Stimulation of dopamine receptors of prolactin-releasing cells in the anterior pituitary, which inhibit the prolactin release. As a consequence, the corpora lute regress. 2. Indications: Pseudopregnancy in bitches (synchronisation – abortion) 3. Side-effects: -Transient hypotension, drowsiness -Vomiting -Anorexia -Pregnancy – lactation (unless their termination is required) 4. Applicaion: PO 5. Drug names: - Bromocriptine BRK tabl. - Cabergoline GALASTOP sol.
58
``` Other endocrine drugs - Decomoton inj. (Carbetocin) 1. Effects 2. Indication 3. Side-effects ```
1. Effects: Contraction of myometrum and myoepithelial cells in mammary gland 2. Indications: -Ecbolic -Uterine inertia; during delivery in all species -Retention of eggs (birds, reptiles) -After parturition -Milk let down (mastitis) 3. Side-effects: -GI – Cardio-vascular systems, swelling at injection site -Dystocia due to obstruction, closed or partly open cervix
59
``` Other endocrine drugs - Ergotin-N inj., Oxymetrin inj. (Ergot alkaloids) 1. Effects 2. Indication 3. Side-effects 4. Application ```
1. Effects: - Abortive - Arithmetic (continuous) contraction of myometrum constriction of peripheral vessels 2. Indications: After parturition, to eliminate retained placenta, stop uterine haemorrhage 3. Side-effects: vasoconstrictor activity 4. Application: PO, IM
60
``` Other endocrine drugs - Sensiblex inj. (Denaverin) - Myometrial relaxants 1. Effects 2. Indication 3. Side-effects 4. Application ```
1. Effects: Toco-spasmolytic, physiological “antidote” of oxytocin (incomplete) 2. Indications: Decreases the magnitude of uterus constrictions, relaxation of cervix 3. Side effects: Closed or partly open cervix 4. Application: SC, IM
61
``` Other endocrine drugs - BETA-2-adrenoreceptor agonists 1. Effects 2. Indication 3. Side-effects 4. Application 5. Drug names ```
1. Effects: Relaxation of uterus and bronchial musculature 2. Indications: - Delay the parturition - Obstetrical manoeuvres, manipulation of foetus - Facilitate replacement of prolapsed uterus - Facilitate handling of uterus during caesarean section - Facilitate recovery the embryos from donors 3. Side-effects: - Transient vasodilatation, tachycardia - Sweating, muscle tremors (with higher doses) 4. Application: IM, IV (slowly) 5. Drug names: - Clenbuterol - PLANIPART inj. - Terbutaline - Isoxsuprine lactate

Pharmacology 1+2 (25 decks)

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