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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
What are ionotropic agents?
Molecules used to increase force of contraction of the heart via action on beta-1 receptors
26
What are some examples of ionotropic agents?
norepinephrine/noradrenaline, epinephrine/adrenaline (wont dim. BP) ephedrine dobutamine, isoproterol —\> also have beta-2 effect
27
What is epinephrine/adrenaline?
molecules used for reanimation and treatment of anaphylactic shock, used to promote hemostasis and increase the duration of action of local anesthetics
28
What SYMADs and SYMAIDs are used in the treatment of bradyarrythmia?
Epinepherine, dopamine and isoproterol (not really used cause it also decreases BP)
29
What is clonidine used for?
used to treat HTA because its effect on alpha-2 receptors —\> dim. sympathetic
30
What conditions are counter indications for using sympathomimétiques?
**Cardiovascular**: insuffisance, arythmie, angor, HTA Insomnia Prostatic hyperplasia
31
How does cocaine work?
SYMAID blocks neuronal recapture of NA and dopamine
32
What are alpha blockers?
Competitive antagonists for adrenergic alpha receptors
33
What are the different kinds of alpha blockers?
**non-selective** ex: phentolamine (alpha-1 and alpha-2) **selective** ex: alpha-1 prazosine, alpha-2 yohimbine
34
Do alpha blockers impact beta receptors?
Sorta... indirectly by making NT more available
35
What are the principal effects of alpha-1 blockers?
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
What are the principal effects of alpha-2 blockers?
Increase NA liberation by adrenergic nerve endings (**autoreceptor**) Increase ACh liberation by cholinergic nerve endings (**heteroreceptor**)
37
What are some clinical uses of alpha blockers?
**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
What conditions are counter indications for using alpha blockers?
Orthostatic hypotension (alpha-1) —\> dim. of sympathetic vasoconstriction reflexes Arrhythmia (tachycardia reflex) Nasal congestion Headaches
39
What are beta blockers?
Competitive antagonists for beta adrenergic receptors
40
What are the different kinds of beta blockers?
**non selective** propranolol **selective** beta-1: metoprolol (cardioselective) beta-2: butoxamine NO REAL CLINICAL USES
41
Do beta blockers impact alpha receptors?
No DIRECT effect BUT alpha effects are amplified due to a increased availability of NT
42
What are the principal effects of beta-1 blockers? (5)
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
What are the principal effects of beta-2 blockers?
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
What are the main effects of alpha and beta blockers on the heart and blood vessels?
**BLOQ beta-1:** dim. HR, contractility, and débit --\> dim. BP **BLOQ beta-2:** constriction --\> increases vascular resistance **BLOQ alpha-1:** dilation --\> dim. BP
45
What are some clinical uses of beta blockers? (beta-1 = lol)
**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
What conditions are counter-indications for using beta blockers?
asthma, bradycardia and they can mask signs of hypoglycemia (shaking... so be careful if diabetic)
47
What are the important cholinomimétiques to know?
**methacholine:** used to induce bronchoconstriction **neostigmine:** used to treat myasthenia gravis **organophosphates:** sarin gaz
48
What are the important anticholinergiques to know?
**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
What are the important sympathomimétiques to know?
**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
What are the important sympatholytiques to know?
phentolamine: alpha-adrenergic antagonist activity metoprolol: beta1-selective (cardioselective) adrenergic receptor blocking agent

MD1 SF3 - EXAM 1 (11 decks)

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