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MD1 SF3 - EXAM 1 > Pharmacologie: Partie 2: Pharmacologie du système nerveux autonome, Sympathomimétiques /Sympatholytiques > Flashcards

Pharmacologie: Partie 2: Pharmacologie du système nerveux autonome, Sympathomimétiques /Sympatholytiques Flashcards

1
Q

What does stimulation of alpha-1 post-synaptic receptors do in the SNS?

A

Vasoconstriction, mydriase, contraction of GI and bladder sphincters

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2
Q

What does stimulation of alpha-2 post-synaptic receptors do?

A

SNS: agrégation plaquettaire, inhibit insulin release, stimulate GH release, inhibit ADH release

CNS: analgesia, sedation, depression of CV system

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3
Q

What does stimulation of alpha-2 pre-synaptic receptors do?

A

Sympathetic (AR)

Inhibit noradrenaline release

Parasympathetic (HR)

Inhibit acetylcholine release

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4
Q

What does stimulation of beta-1 post-synaptic receptors do?

A

Sympathetic

Increase HR, increase cardiac automaticity and contractility, lipolysis

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5
Q

What does stimulation of beta-2 post-synaptic receptors do?

A

Sympathetic

vasodilation, bronchodilation, relaxation of GI tract, uterus and bladder, glycogenolysis, secretion of insulin

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6
Q

What does stimulation of beta-2 pre-synaptic receptors do?

A

Sympathetic (AR)

Increase NA secretion

Parasympathetic (HR)

Increase ACh secretion

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7
Q

What is a sympathomimétique?

A

Medication that reproduce the effects of a stimulation from the sympathetic nervous system

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8
Q

What are the two kinds of sympathomimétiques?

A

SYMAD: à action directe

  • directly stimulates the receptor

SYMAID: à action indirecte

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9
Q

What is the effect of a sympathomimétique on alpha-1 receptors? SYMAD

A

NA released by post-ganglionnaire nerve…

Where are these receptors located?

blood vessels, intestines (sphincters), radial iris muscles, sphincter of the prostate

NO ALPHA-1 RECEPTORS ON THE HEART

  1. Blood vessels:
    • increase arterial pressure and vascular resistance (VASOCONSTRICTION)
  2. Eyes:
    • Contraction of muscle dilatateur radial de la pupille —> mydriase (opening of pupil)
  3. Bladder:
    • Contraction of sphincter
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10
Q

What are the clinical uses of sympathomimétiques in terms of alpha-1 agonists?

A

Reduce nasal congestion (vasoconstriction) —> DO NOT USE IN GLAUCOMA PTS

treatment of hypotension but be careful of bradycardia reflex in response to constriction

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11
Q

What is the effect of a sympathomimétique on alpha-2 receptors? SYMAD

A

Périphériques:

  • not as important and not really prescribed for these effects but
  • agrégation plaquettaire, inhibition of insulin/ADH release and stimulation of growth hormone

Central:

  • analgesia, sedation, depression of CV system

Pre-synaptic:

  • decrease in sympathetic tonus (inhibit NA release) and parasympathetic (inhibit ACh release)
  • Auto and heteroreceptors on post-ganglionic nerve endings
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12
Q

What are the main clinical uses of sympathomimétiques in terms of alpha-2 agonists?

A

Clonidine: used often in chronic pain (per os)

Clonidine is an α-2 adrenergic receptor agonist with central and peripheral action. CNS effects are mediated in the ‘anxiety centre’ whilst the peripheral effects in the GI tract are via decreasing acetylcholine release, thereby reducing the strength and frequency of colonic motor contractions.

Dexmedetomidine: sedative w/o respiratory distress (IV)

short-term sedative and analgesic

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13
Q

What is the effect of a sympathomimétique on beta-1 receptors? SYMAD

A

ALL ABOUT THE HEART! —> increases ionotropy and HR and renin secretion (SRAA) but not as important as the heart

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14
Q

What is the effect of a sympathomimétique on beta-2 receptors? SYMAD

A

SNS: Vasodilation, bronchodilation, relaxation of GI/bladder, glycogenolysis, insulin secretion, increase of potassium capture by skeletal muscles, relaxation of cilliary muscle to accommodate for seeing far

pre-synaptic: auto/heteroreceptor… increase ACh and NA release

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15
Q

What is the impact of sympathomimétiques on insulin secretion? SYMAD

A

Alpha-1 —> lower secretion

Beta-2 —> increase secretion

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16
Q

What are the different types of SYMADs most used in clinical settings?

A

They can either be:

  1. selective for a subtype of receptor
  2. non-selective

This selectivity varies according to the molecule used and the dose

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17
Q

What are some examples of selective SYMADs?

A

phenylephrine —> alpha-1

isoproterol —> beta-1 > beta-2… NO ALPHA

clonidine —> alpha-1… VERY little alpha-1 stim

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18
Q

How do SYMAIDs work?

A

MOST NA MOLECULES ARE RECAPTURED (80%)

  1. Block recapture of NA in adrenergic nerve endings —> NA accumulation which decreases the NA reserves
  2. Inhibition of enzyme that degrades NA (inhibiteur de la monoamine oxydase)
  3. Increase NA secretion
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19
Q

Specifics of SYMAIDs… use 1:

A

Block recapture of NA in adrenergic nerve endings —> NA accumulation which decreases the NA reserves

examples?

cocaine and some anti-depressants

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20
Q

Specifics of SYMAIDs… use 2:

A

inhibition of enzyme that degrades NA (inhibiteur de la monoamine oxydase)

examples?

certain anti-depressants

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21
Q

Specifics of SYMAIDs… use 3:

A

increase NA secretion

example?

EPHEDRINE

22
Q

What are the main clinical uses of sympathomimétiques? (SYMADs and SYMAIDs) –> 5

A
  1. Vasopressors
  2. Inotropic agents
  3. Epinephrine/adrenaline
  4. Treatment of bradyarrhythmia
  5. Clonidine
23
Q

What are vasopressors?

A

Molecule used to increase BP via action on alpha-1 receptors

24
Q

What are some examples of vasopressors?

A

phenylephrine (PURE)

  • vasoconstriction but has bradycardia reflex via baroreceptors

norepinephrine/noradrenaline, epinephrine/adrenaline

ephedrine (indirect)

25
Q

What are ionotropic agents?

A

Molecules used to increase force of contraction of the heart via action on beta-1 receptors

26
Q

What are some examples of ionotropic agents?

A

norepinephrine/noradrenaline, epinephrine/adrenaline (wont dim. BP)

ephedrine

dobutamine, isoproterol —> also have beta-2 effect

27
Q

What is epinephrine/adrenaline?

A

molecules used for reanimation and treatment of anaphylactic shock, used to promote hemostasis and increase the duration of action of local anesthetics

28
Q

What SYMADs and SYMAIDs are used in the treatment of bradyarrythmia?

A

Epinepherine, dopamine and isoproterol (not really used cause it also decreases BP)

29
Q

What is clonidine used for?

A

used to treat HTA because its effect on alpha-2 receptors —> dim. sympathetic

30
Q

What conditions are counter indications for using sympathomimétiques?

A

Cardiovascular: insuffisance, arythmie, angor, HTA

Insomnia

Prostatic hyperplasia

31
Q

How does cocaine work?

A

SYMAID

blocks neuronal recapture of NA and dopamine

32
Q

What are alpha blockers?

A

Competitive antagonists for adrenergic alpha receptors

33
Q

What are the different kinds of alpha blockers?

A

non-selective

ex: phentolamine (alpha-1 and alpha-2)

selective

ex: alpha-1 prazosine, alpha-2 yohimbine

34
Q

Do alpha blockers impact beta receptors?

A

Sorta… indirectly by making NT more available

35
Q

What are the principal effects of alpha-1 blockers?

A

relaxation of smooth vascular muscles —> hypotension, tachycardia reflex, postural hypotension

nasal congestion

myosis

relaxation of bladder sphincter —> easier to urinate

relaxation of prostate, vas deferens, seminal vesicles

36
Q

What are the principal effects of alpha-2 blockers?

A

Increase NA liberation by adrenergic nerve endings (autoreceptor)

Increase ACh liberation by cholinergic nerve endings (heteroreceptor)

37
Q

What are some clinical uses of alpha blockers?

A

Hypertensive emergencies:

  • phentolamine (alpha-1 and 2)

Treat accidental sub-cutaneous infiltration for a sympathomimétique

  • phenoxybenzamine (alpha-1 and 2) —> non-competitive antagonist
  • MUST USE FAST OTHERWISE POSSIBLE NECROSIS OF TISSUE

Raynaud’s

  • Phenoxybenzamine (alpha-1 and 2), prazosine (alpha-1)

Increase NA release —> pre-synaptic effects:

  • Yohimbine (alpha-2)
    • Treatment of idiopathic orthostatic hypotension
    • Erectile dysfunction

Benign hypertrophy of the prostate:

  • Tamsulosin (alpha-1a) VERY LOCAL AND SPECIFIC EFFECT BECAUSE OF TARGETED RECEPTOR
38
Q

What conditions are counter indications for using alpha blockers?

A

Orthostatic hypotension (alpha-1) —> dim. of sympathetic vasoconstriction reflexes

Arrhythmia (tachycardia reflex)

Nasal congestion

Headaches

39
Q

What are beta blockers?

A

Competitive antagonists for beta adrenergic receptors

40
Q

What are the different kinds of beta blockers?

A

non selective

propranolol

selective

beta-1: metoprolol (cardioselective)

beta-2: butoxamine NO REAL CLINICAL USES

41
Q

Do beta blockers impact alpha receptors?

A

No DIRECT effect BUT alpha effects are amplified due to a increased availability of NT

42
Q

What are the principal effects of beta-1 blockers? (5)

A

dim. HR and contractility of heart
dim. speed of AV conduction
dim. débit cardiaque (short term)
dim. vascular resistance (long term)
dim. renin secretion and BP

43
Q

What are the principal effects of beta-2 blockers?

A

Increase vascular resistance (short term)

Bronchoconstriction —> asthma = counterindication

dim. glycogenolysis and insulin secretion
dim. entry of potassium into muscle cells
dim. NA and ACh release (auto/heteroreceptors)

44
Q

What are the main effects of alpha and beta blockers on the heart and blood vessels?

A

BLOQ beta-1: dim. HR, contractility, and débit –> dim. BP

BLOQ beta-2: constriction –> increases vascular resistance

BLOQ alpha-1: dilation –> dim. BP

45
Q

What are some clinical uses of beta blockers? (beta-1 = lol)

A

HTA:

  • propranolol (1 and 2), metoprolol (1), esmolol

Ischemia, arrhythmia, I.C:

  • bisoprolol (1), metoprolol

Glaucoma:

  • diminish the production of aqueous humour: timolol (1 and 2) —> drops

Other:

  • Migraines and idiopathic tremors
46
Q

What conditions are counter-indications for using beta blockers?

A

asthma, bradycardia and they can mask signs of hypoglycemia (shaking… so be careful if diabetic)

47
Q

What are the important cholinomimétiques to know?

A

methacholine: used to induce bronchoconstriction

neostigmine: used to treat myasthenia gravis

organophosphates: sarin gaz

48
Q

What are the important anticholinergiques to know?

A

atropine: used to treat the symptoms of low heart rate

glycopyrrolate: helps to control conditions such as peptic ulcers that involve excessive stomach acid production.

49
Q

What are the important sympathomimétiques to know?

A

noradrenaline: used to treat people with very low blood pressure

  • nonselective agonist of all adrenergic receptors

adrenaline: EpiPens

  • alpha-1 receptors

phenylephrine: decongestant

  • post-synaptic alpha-adrenergic receptor

​isoproterenol: used for the treatment of bradycardia

  • non-selective β adrenoceptor agonist

ephedrine:

  • direct and indirect sympathomimetic. It binds directly to both alpha and beta receptors

clonidine:

  • α-2 adrenergic receptor agonist

salbutamol: Ventolin (used to relieve symptoms of asthma and chronic obstructive pulmonary disease)

  • selective beta-2 adrenergic receptor agonist
50
Q

What are the important sympatholytiques to know?

A

phentolamine: alpha-adrenergic antagonist activity
metoprolol: beta1-selective (cardioselective) adrenergic receptor blocking agent

MD1 SF3 - EXAM 1 (11 decks)

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