Autonomic Nervous system and drugs Flashcards
What is the action of Botulinum toxin? What bacteria is it associated with?
Action: Protease that cleaves SNARE proteins –> Inhibits release of ACH –> FLACCID paralysis
Bacteria: Clostridium (other clostridia are C. Diff, Tetanus, and C. Perfringens)
Note: Carried on a phage (Shiga, Botulinum, Cholera, Diptheria, strep pyogenes)
What are the pre and post ganglionic receptors for parasympathetic innervation?
Pre: Ach-Nictoninc-(N)
Post: Ach-Muscarinic-(1-5)
How do nicotinic acetylcholine receptors work? Where are they found?
Ach-Nicotinic(n) AND Ach-Nicotinic(m) receptors = Na/K channels
Found in:
- Parasympathetic preganglionic (N-n)
- Sympathetic preganglionic (N-n)
- Adrenal medulla (N-n)
- Skeletal muscle (N-m)
How do muscarinic acetylcholine receptors work? Where are they found?
muscarinic receptors = GPCR
Found in:
- Parasympathetic postganglionic
- Sympathetic postganglionic (sweat)
All preganglionics act on what kind of receptors?
Nicotinic-N acetylcholine
Where are Nicotinic-M acetylcholine receptors found?
ONLY in skeletal muscle
Where are Muscarinic acetylcholine receptors found?
Postganglionic parasympathetics (all) and sympathetics (sweat)
What are the pre and post ganglionic receptors of the sympathetic nervous system?
Pre: Acetylcholine Nicotinic-N (like all preganglionics)
Post:
- Norepinephrine Alpha and Beta (most places)
- Acetylcholine Muscarinic (sweat glands)
- D (renal vessels and renal smooth muscle)
- nothing postganglionic for adrenal medulla
Where are norepinephrine alpha and beta receptors found?
On sympathetically innervated:
- cardiac cells
- smooth muscl
- glands
- nerve terminals
NOT on sweat glands and adrenal medulla (which are also sympathetic). Those have Ach-M (sweat) and Ach-Nn (adrenal medulla)
What are the pre and post ganglionic receptors of the adrenal medulla?
Trick question! There is no pre/post. Just one neuron synapsing onto Acetylcholine-Nicotonic-N receptors
What are the pre and post ganglionic receptors of the parasympathetic nervous system?
Pre: Acetylcholine-Nictoninic-N
Post: Acetylcholine-Muscarinic
What are the pre and post ganglionic receptors of skeletal muscle?
Trick question: There is no pre/post! Just one neuron synapsing onto Acetylcholine-Nicotinic-M receptor (the ONLY place we see nicotinic-M!)
What 4 broad categories does the sympathetic nervous system innervate?
- Sweat glands (use Ach-M receptor)
- Adrenal medulla (uses Ach-Nn receptor)
- Renal vasculature, renal SM (uses D receptor)
- Cardiac, SM, glands (use NE-alpha or NE-beta receptors)
First generation antihistaminics (H1 histamine receptor blocks) have what undesirable side effects?
- Antimuscarinic (Pupillary dilation, dry mouth, urinary retention, constipation)
- Anti-alpha-adrenergic (hypotension, dizziness)
- Anti-serotonergic (apetite stim, weight gain)
What do alpha 1 receptors do?
- Vasoconstriction (smooth muscle in the vessels contracts)
- Intestinal/bladder sphincter contraction
- Pupillary dilation
*memory: Picture making an alpha with string. You pull it TIGHTER to do vasoconstriction and bladder sphincter constriction, You LOOSEN it to make an eye (pupillary dilation)
What do alpha 2 receptors do?
- Decrease sympathetic outflow - STOP RUNNING
- Decrease insulin release - STOP TAKING UP SUGARY FOR ENERGY
- Decrease lipolysis - STOP USING FAT FOR ENERGY
- Decrease aqueous humor production - DONT WORRY ABOUT GETTING WIND IN YOUR EYES
- Increase platelet aggregation - NOW THAT YOU ARE DONE RUNNING, HEAL UP
*memory: Everything you would want to do to relax. Time 2 acclimate.
What do beta 1 receptors do?
- Increase HR
- Increase contractility
- Increase renin release (vasoconstriction, water retention)
- Increase lipolysis
*memory: There is 1 Bear behind you
What do beta 2 receptors do?
- Vasodilation - BLOOD FLOW
- Bronchodilation *“easier 2 Breathe” - BREATHE
- Decrease uterine tone (tocolysis) - DONT HAVE A BABY
- Ciliary muscle relaxaiton (increase long range focal distance) - LOOK FAR AWAY
- Increase lipolysis - BREAK DOWN FAT FOR ENERGY
- Increase insulin release - TAKE UP GLUCOSE FOR ENERGY
- Increase aqueous humor production - GET STUFF OUT OF YOUR EYES
*memory: Everything you would want to do if you were running away from something. Time 2 book it.
What receptor increases aqueous humor production? Decreases it?
Increase: Beta 2 (memory: Time 2 Book it. Increase production when need to get stuff out of your eyes so you can run)
Decrease: Alpha 2 (memory: Time 2 Accomodate. No need to waster energy worrying about things getting in your eyes).
What receptor causes pupillary dilation?
Alpha 1
*memory: loosen an alpha string to make an eye
What receptor causes lipolysis?
Beta 1 and Beta 2
*memory: 1 bear behind you, time 2 Book it
What receptor decreases lipolysis and insulin release?
Alpha 2 *memory: Time 2 Accomodate; chill out
What receptor causes vasodilation? vasocontriction?
Vasodilation: Beta 2 *memory: Time 2 Book it
Vasoconstriction: Alpha 1 *memory: Tighten an alpha string for vasoconstriction and sphincter constriction
What do dopamine D1 receptors do?
Relax renal vascular smooth muscle
What do dopamine D2 receptors do?
Modulate dopamine NT release, especially in the brain
What do histamine H1 receptors do?
- Increase nasal and bronchial mucus production
- Increase vascular permeability
- Contract bronchioles
- Pruritus
- Pain
*memory: Basically everything allergic. Thats why we block them to treat respiratory allergies (ex: diphenhydramine)
Why are second generation antihistamines less sedation than first generation?
Don’t enter the CNS as well, so don’t interfere with histamine NT release
What do histamine H2 receptors do?
Increase gastric acid secretion
That’s why we use them for peptic ulcer, gastritis, and GERD (ex: cimetidine)
What do vasopressin V1 receptors do?
Increase vascular smooth muscle contraction
*Thats why pitressin, a vasopressin analog that acts on V1 and V2, is used for ICU patients hypotensive crisis
What do vasopressin V2 receptors do?
Act on collecting tubules of the kidney to increase water permeability so water can be absorbed (they are ADH receptors… vasopressin = ADH)
*Thats why desmopressin is used for central diabetes insipidus
Desmopressin acts on V2 receptors so it is used to treat central diabetes insipidus (its basically exogenous ADH). What other completely unrelated disease does it treat, and why?
Von Willebrand’s disease because it also increases Factor 8 and vWF release from endothelial cells
What GPCR class are alpha 1, alpha 2, beta 1, and beta 2 receptors?
*memory: QISS (kiss) the sympathetic nervous system Alpha 1 = Gq Alpha 2 = Gi Beta 1 = Gs Beta 2 = Gs
What does the M1 parasympathetic postganglionic receptor do?
CNS and enteric nervous system stimulation
What does the M2 parasympathetic postganglionic receptor do?
- Decrease HR
2. Decrease contractility of ATRIA
What does the M3 parasympathetic postganglionic receptor do?
- Increase exocrine gland secretion (lacrimal, salivary, gastric)
- Increase gut peristalsis
- Increase bladder contraction
- Bronchoconstriction
- Miosis
- Ciliary muscle contraction (accomodaiton – short range focus)