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Autonomic Nervous System


Pharmacology
Shan Nanji

ANS Parasympathetic &


Sympathetic Basics
!Parasympathetic

- CHOLinergic

Uses ACh Pre & Post Synaptically.

!Craniosacral,

cGMP
!MUSCARINIC - Most
!NICOTINIC: Located at NMJ and
Ganglia

! Sympathetic

adreNErgic

Uses ACh Pre Synaptically and NE Post-Synaptically


!

Thoracolumbar, cAMP
!
!

Shan Nanji - NanjiMD@gmail.com

NICOTINIC Most
MUSCARINIC Sweat Glands & Adrenal Medulla

Parasympathetic System
- Cholinergic
!M1

CNS/ENS

!M2

Heart

!M3

EG MP AC BB

Increases Exocrine Gland Secretion


! Increases Gut Motility
!

! Miosis via Pupillary sphincter

!Accommodation via Ciliary


! Bronchoconstriction
! Bladder constriction
Shan Nanji - NanjiMD@gmail.com

+ Anti-ACh-Esterases
MOA:
Prevent degradation of ACh increasing endogenous AcH
- More ACh (acetylCHOLine) so more CHOLinergic!
! Edrophonium Dx Myasthenia Gravis, used to differentiate it
from cholinergic crisis

!NeOstigmine/PyridoSTIGmine Rx Myasthenia
Gravis (No BBB)
!

Rx Myasthenia Gravis, Ileus, Urinary Retention, Reversal of NMJ


Blockage

! PhysoSTIGmine Rx for Atropine Overdose (Will cross BBB),


also for glaucoma

! Ecothiophate For Glaucoma

Ecoth-EYE-ophate

! Donepezil For Alzheimers disease - Lipid Soluble


DONT-epezil - DONT remember anything - Alzheimers. Buddy of DONTepezil is Tacrine.

! Tacrine Lipid Soluble Rx Alzheimer's


Shan Nanji - NanjiMD@gmail.com

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Anti-ACh Anti-Cholinergics
MOA:
So, if cholinergics agonize M3
an Anti-ACh will ANTAGONIZE M3.

Antagonizing M3 will cause:


! Decrease

Exocrine Gland Secretions


! Decrease Gut Motility
! No Miosis so Mydriasis
! No Accommodation so loss of accommodation
! Bronchodilation
! Bladder relaxation

Shan Nanji - NanjiMD@gmail.com

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Anti-ACh Anti-Cholinergics
MOA:
So, if cholinergics agonize M3
an Anti-ACh will ANTAGONIZE M3.

Antagonizing M3 will cause:


! Decrease

Exocrine Gland Secretions


! Decrease Gut Motility
! No Miosis so Mydriasis
! No Accommodation so loss of accommodation
! Bronchodilation
! Bladder relaxation
Shan Nanji - NanjiMD@gmail.com

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Anti-ACh
Trops

! Atropine Mydriasis w/Cyclopegia, Management of


Anti-AChE poisoning homaTROPine or TROPicamide can also be used
! Benztropine/Trihexyphenidyl Lipid Soluble
Parkinsons Disease and EPS Symptoms
(CNS Entry) for __________________,
due to antipsychotics
ASTHMA
COPD
! Ipratropium Safe to use in ________and
__________
I Pray I Breathe

! Glycopryrrulate, Oxybutinin Reduce urgency


in mild cystitis and reduce bladder spasms
! Scopolamine Motion Sickness
Shan Nanji - NanjiMD@gmail.com

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Alpha 1 Receptor
Vasoconstriction
! __________________
Sphincter - causes Urinary Retention. so used in incontinance
! Constricts
__________________

Mydriasis via radial (dilator muscle)

Shan Nanji - NanjiMD@gmail.com

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Alpha 1 Receptor Pharmacology


Alpha 1 Agonists
! EpinephRINE/NorepinephRINE

EphedRINE
PseudoephedRINE
__________________
/ __________________

Incontinence in the elderly

If u see R.Kelly on street peeing on ppl then give EphedRINE or PseudoephedRINE

PhenylephRINE
__________________
Neurogenic shock,
pupillary dilation, vasoconstriction, nasal
decongestion

Shan Nanji - NanjiMD@gmail.com

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Alpha 1 Receptor Pharmacology


Alpha 1 Agonists
!EpinephRINE
! Causes Decreased Production of Aqueous Humor
! Vasoconstriction
! Clinical

Use:

! Hypotension
! Asthma
! Anaphylaxis
! Open

Shan Nanji - NanjiMD@gmail.com

Angle Glaucoma

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Alpha 1 Receptor Pharmacology


Alpha 1 Agonists
!NorepinephRINE
! Clinical

Use:

! Hypotension

Shan Nanji - NanjiMD@gmail.com

(Decreased Renal Blood Flow)

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Alpha 1 Receptor Pharmacology


Alpha 1 Antagonists

NON
Selective

Pts have HTN

Phentolamine
__________________
Dx Pheochromocytoma, also

for patients on MAOi that ate tyramine

! Phenoxybenzamine
__________________ Rx Pheochromocytoma
! Yohimbine

Impotence Non selective but A2 antagonist then A1

! Prazocin Rx HTN but assoc. with first dose SYNCOPE


A1
selective __________________
! Terazocin/Doxazocin

First line for BPH, also for HTN

Alpha 1 agonist constricts the urinary sphincter so antagonist will relax it so peeing will be easy.
! Tamsulosin Rx BPH. it has LEAST side effects. its Kinna FLOWMAX

i.e. it increases the FLOW so used in BPH and also in Kidney stones cz there also we
want Pt to urinate more so stone may pass.
Shan Nanji - NanjiMD@gmail.com

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Alpha 2 Receptor
NE Release
!Decrease __________________
(makes you less
adrenergic AKA less SYMPATHETIC and MORE
Parasympathetic) so its vasodilatory and is used in HTN.
!Decreases
!Promotes

Shan Nanji - NanjiMD@gmail.com

Insulin Release
__________________

platelet aggregation

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Alpha 2 Receptor Pharmacology


Alpha 2 Agonists
! Clonidine

HTN & Physchosis associated


Rx
__________________,
with rebound HTN

This BIG Methyl group cant cross Placenta so we can give it, same as Propyl grp
on PTH used for Hyperthyroid in pregnancy

! Alpha-Methyl

Dopa Rx HTN, safe in


(+) Hemolytic anemia
pregnancy but can cause Coombs
__________________.
! Guanabenz

Shan Nanji - NanjiMD@gmail.com

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Alpha 2 Receptor Pharmacology


Alpha 2 Antagonists
! Mirtazapine

Depression
Rx __________________,
S/E
Increased appetite, Increased serum
cholesterol, increased sedation
! mirSADzapine

Shan Nanji - NanjiMD@gmail.com

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Beta 1 Receptor
! Increases

Heart Rate

! Increases

Contractility

! Promotes

Glucagon
__________________
Release

! Increases

Ren1n
__________________
Release

! Increases

Shan Nanji - NanjiMD@gmail.com

Lipolysis

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Beta 2 Receptor
! Increases

Contractility

Vasodilation DECREASES: TPR,


__________________
Diastolic Pressure, and Afterload
Relaxation of the Uterus
__________________

! Broncho

dilation
__________________
Insulin Secretion
! Increases __________________.

Shan Nanji - NanjiMD@gmail.com

+
Trouble Remembering Receptors?
! So,

#1 comes BEFORE #2 and

! Letter

G comes BEFORE letter I Alphabetically

!1 = Increase Glucagon
!2 = Increase Insulin
!Get

it! Got it! Good!

!1 BEFORE 2 and G BEFORE

Shan Nanji - NanjiMD@gmail.com

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Beta Receptor Pharmacology


Beta 1 Agonists

Dobutamine
B1 B2
__________________
(__>
__) Congestive Heart
Failure
! Isoproterenol (B1=B2) Bronchospasm, Heart
block and Bradyarrhythmias
!S/E Flushing, Angina, Arrhythmias
!

Beta 2 Agonists
! Albuterol

Asthma short half life


Terbutaline
! __________________
Asthma short half life,
is contracting in premature labor
Premature labor treatment czanduterus
B2 Relaxes uterus
! Ritodrine Premature labor treatment
! Salmeterol Asthma Long term treatment

Shan Nanji - NanjiMD@gmail.com

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Beta Receptor Pharmacology


Beta Receptor Antagonists
! Propanolol

Long half life, used in TH storm


prevents peripheral T4-T3 conversion

T3 is the active form & it increases BMR and so more energy is wasted.

! Esmolol

Short half life

Propanolol is a PRO so works long hours


His buddy ESmolol says Take it EaSY

! Acebutolol,

Atenolol, Pindolol Intrinsic Sympathetic


action i.e. Partial Beta Agonist so they Block B receptors and
__________________
Partially stimulate them too.

! Labetalol

Alpha 1 Antagonistic
& Carvedilol = Has ______
Activity, used in HTN emergency

Shan Nanji - NanjiMD@gmail.com

1-selective antagonists (1 > 2)acebutolol (partial agonist),


atenolol, betaxolol, esmolol, metoprolol

Selective antagonists mostly go


from A to M (1 with 1st half of alphabet)

Nonselective antagonists (1 = 2)nadolol,


pindolol (partial agonist), propranolol, timolol

Nonselective antagonists mostly go


from N to Z (2 with 2nd half of alphabet)

Nonselective - and -antagonistscarvedilol, labetalol

Nonselectives - and -antagonists


have modified suffixes (instead of -olol)

Nebivolol combines cardiac-selective 1-adrenergic blockade


with stimulation of 3-receptors, which activate
nitric oxide synthase in the vasculature

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Beta Receptor Pharmacology


Beta Receptor Antagonists
! Nadalol

In liver failure; decrease variceal


bleeding

! Timolol/Butexalol

Open Angle Glaucoma


__________________
Decreases secretion of Aqueous humor

! Carvedilol

mortality

! Sotolol

& Metoprolol Decrease post MI


Sorry sir i gave u SOTOLOL so now u have to stay in
hospital. Cz K+ has to be monitored closely in Hosp.

Partial K+ Blocker
__________________
Channel Activity, will
increase the QT Interval

Shan Nanji - NanjiMD@gmail.com