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Pharma 1 > parasympathetic and sympathetic nervous system > Flashcards

parasympathetic and sympathetic nervous system Flashcards

1
Q

M1 , M2, M3: where do they work?

- side effects

A
  • M 1 ,M 3 stomach and glands, bronchial smooth
    muscle, eye ciliary muscle excitation –, vascular
    endothelium (NO) inhibition
  • M 2 heart inhibition
- Side effects: 
bradycardia
bronchoconstrictio
miosis
salivation
vomiting, diaorrhea
urination
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2
Q

Muscarinic ACh receptors:

- response to ACh binding =

A

G protein cascade is activated

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3
Q

Indirect parasympathomimetics

- how they work

A

ACh esterase enzyme inhibition —> ACh

degradation is reduced

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4
Q

Carbachol

A

non specific to M ACh receptors: several side effects
excellent activity, nowadays: exclusively locally
1. applied in the uterus in the case of metritis (intrauterine)

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5
Q
  1. Bethanechol

2. Methacholine

A

used in human medicine mostly

  1. M- ACh specific
    induction of intestinal peristalsis after operations
    urinary bladder atony ! (veterinary field)

M ACh specific
cardiovascular system —> atrial fibrillation
pronounced peripherial vasodilatation —> ergot toxicosis

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6
Q

Pilocarpine

  • use
  • side effects
A

natural alkaloid ( Pilocarpus jaborandi)
earlier: important role in ophtalmology
1. GLAUCOMA therapy (miosis can be seen after approx. 15 mins)
2. KCS (Keratoconjunctivitis sicca): effect is ambiguous
side effect: mild after local administration

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7
Q

Direct parasympathomimetics

A 
Acetylcholine (ACh)
Carbachol
Bethanechol
Methacholine
Pilocarpine
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8
Q

Receptors for indirect parasympathomimetics:

A

 primarily on nicotinic ACh receptors
 furthermore on muscarinic ACh receptors
 on ACh receptors in the CNS

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9
Q

Physostigmine

  • characteristics
  • use
A
  • contains tertiary nitrogen –> lipophilic –> kinetics!
  • very small therapeutic index systemically (atropine poisoning)
  • eye drop : glaucoma treatment
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10
Q

Neostigmine

  • Characteristics
  • use
A

•quaternary nitrogen —> less lipophilic –> kinetics!
•eye drop : treatment of glaucoma
•given systemically it is safer
- Given IV or IM

  • myasthenia gravis treatment
    suspending the action of non depolarizing muscle relaxants
  • increasing intestinal motility
  • inducing emesis
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11
Q

Pyridostigmine

  • Characteristics
  • admin
  • use
A
  • quaternary nitrogen –> less lipophilic –> kinetics!
    •given systemically it is safer
    •orally this has the best bioavailability (F=3 8% only)

Use:
myasthenia gravis treatment
increasing intestinal motility

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12
Q

Edrophonium

  • Characteristics
  • effect, use
A

•competitive inhibition in the neuromuscular junction —> action is suspended by diffusion
•short effect: 5-15 minutes
- myasthenia gravis diagnosis = Tensilon test

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13
Q

Organophosphates

  • Characteristics
  • use
  • antidote
A
  • irreversible
  • inhibitors of AChE
  • ectoparasiticides (e.g. diazinon)
  • in humans treatment of glaucoma (e.g. echothiophate)
    antidote: atropine, pralidoxime
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14
Q

Indirect parasympathomimetics

A 
Organophosphates
Edrophonium
Pyridostigmine
Neostigmine
Physostigmine
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15
Q

Atropine

Dose (mg/kg) Symptoms

A

Dose (mg/kg) Symptoms
0,5 :Mouth dryness, decreased perspiration
1: tachycardia, mydriasis
2: +accomodation, disturbances
5: +constipation
10: +ataxia, excitation, hallucination, delirium, coma

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16
Q

Drugs used in:

  1. diagnostic examination of the eye
  2. in uveitis the prevention of synechiae
A
  1. tropicamide,homatropine (short acting)

2. atropine (long acting)

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17
Q

atropine was used earlier for

premedication which drug is most used now?

A

glycopyrrolate

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18
Q

Drug used in treatment of horse RAO, COPD and human

(feline) asthma :

A

ipratropium

19
Q

decreases secretion and motility (used

in ruminants)

A

benzethimide

20
Q

decreases smooth muscle function –> antispasmodic

effect in the intestine –> very effective in horse colic

A

esp. butyl scopolamine

21
Q

Which animal is relatively resistant to atropine! (liver atropinase)

A

Rabbit

22
Q

Atropine toxicosis symptoms:

A

Symptoms: dry mouth, tachycardia, mydriasis, constipation, convulsions, coma, death

23
Q

α1 receptor effects:

A

smooth muscle contraction
*increased sphincter constriction
vasoconstriction
mydriasis

24
Q

α2 receptor effects:

A

inhibition of neurotransmitter release (NA!)
GI relaxation
inhibition of insulin release

25
Q

β receptors effects:

A 
- β1 receptor
cardiac effects (positive inotropic, chronotropic)
  • β2 receptor
    vasodilatation
    bronchodilatation
    uterus relaxation
  • (β 3 receptor
    lipolysis in fat tissue)
26
Q

Nonspecific sympathomimetics

A

Adrenalin
Noradrenalin
Dopamine

27
Q

Adrenaline

  • receptors
  • effects
  • indications
A
  • noncspecific: mainly β 1 and β 2 receptors
    * α-receptors in higher dosage

cardiac effect
arrhytmogenic!
blood pressure increases

indications:

  • cardiac stop
  • severe bronchoconstriction
  • anaphylaxia
  • local vasoconstriction (haemorrhages)
  • increase in duration of local anaesthetics
28
Q

Noradrenaline

  • receptors
  • effects
  • indications
A
  • nonspecific (mainly β 1 and α 1 receptors)

cardiac effect
blood pressure is significantly increased!

indications (rare):
-hypotension

29
Q

Dopamine

- receptors

A
  • low dose D 1 receptors (kidney!)
  • medium dose β 1 receptors (heart!)
  • high dose α 1 receptors (pressor)
30
Q

Specific sympathomimetics

A

Dobutamine
Isoproterenol

Beta agonists: (mainly B2, higher doses B1)
clenbuterole
salbutamole
 terbutaline
 salmeterole
isoxsuprine
31
Q

Dobutamine

  • receptors
  • effects
  • indication
A
  • mainly β 1 receptors
    cardiac effect
    indications:
    -cardiogenic shock (IV. infusion)
32
Q

Isoproterenol

A

only β receptors ( β 1 and β 2)

- heart+bronchi+muscle vessels

33
Q

Which Beta 2 agonist is leaat lightly to cause cardiac effect?

A

clenbuterole 4:1
salbutamole 650:1
salmeterole 50000:1

34
Q

β2 agonists indications:

A 
horse RAO
feline asthma
bronchitis, bronchopneumonia
tracheal hypoplasia
tracheal collapse
35
Q

Phenylephrine

  • receptors
  • uses
A 
α adrenoceptor agonists 
mainly α 1 receptors -->  vasoconstriction
- use:
rarely
local and systemic usage
Allergy, cold
\+ Hypotension, shock (?)?)
36
Q

Xylometazoline, oxymetazoline, naphazoline, tetryzoline are:

A

mainly α 1 receptors –> vasoconstriction

local usage

37
Q

Phenylpropanolamine

A

mainly α 1 receptors —> urinary bladder sphincter
constriction!
per os usage (empty stomach)
side effects

38
Q

α adrenoceptor agonists: 8stk

α2 agonists: 4stk

A 
Phenylephrine
Xylometazoline,
 oxymetazoline,
 naphazoline,
 tetryzoline
Phenylpropanolamine
Ephedrine
Amphetamine

α 2 agonists (sedato hypnotics)
xylazine, detomidine, medetomidine, romifidine

39
Q

Ephedrine

  • receptors
  • use
A 
nonspecific, direct and indirect effects
- uses: 
tachyphylaxis
CNS
allergy, incontinence (p.o.)
40
Q

Nonspecific α antagonists

- drugs

A
  • Phenoxybenzamine (urethra sphincter relaxation)
    long duration of action
  • Phentolamine
  • Tolazoline
41
Q

α1 antagonists

A

prazosine, doxasozine (urethra sphincter relaxation)

42
Q

α2 antagonists

A

atipamezole, yohimbine

43
Q

Nonspecific β antagonists

A

Propranolole
Timolole
SIDE EFFECTS

44
Q

Specific β 1 antagonists

A

Metoprolole

Atenolole

Pharma 1 (15 decks)

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