Autonomic Nervous System Drugs

hezikry's version from 2015-08-06 20:33

Sympathetic basics

Question Answer
VasoconstrictAlpha 1
Mydriasis (dilate eyes)Alpha 1
Increase bladder sphincter toneAlpha 1
Increase BP (vasculature)Alpha 1
Increase peripheral vascular resistance (PVR)Alpha 1
decrease RBFalpha 1
decrease sympathetic outflowalpha 2
decrease insulin releasealpha 2
decrease aqueous humor productionalpha 2
Increase heart rateBeta 1
Increase contractilityBeta 1
Increase BP (heart)Beta 1
Increase reninBeta 1
VasodilateBeta 2
BronchodilateBeta 2 **don't give beta 2 blockade to asthmatics
DECREASE uterine toneBeta 2
Increase HR (baroreflex)Beta 2
increase insulin releasebeta 2 and M3
decrease insulin releasealpha 2
HAV1 M and MGq
GSB1, B2, D1, H2, V2

Parasympathetic basics

Question Answer
CNS, enteric nervous systemM1
decreased heart rate and contractility of atriaM2
increased bladder contractionM3

Dopamine, Histamine and Vasopressin receptors

Question Answer
D1relaxes renal vascular smooth muscle
D2modulates neurotransmitter release especially in brain
H1increases nasal and bronchial mucus production
H2increases gastric acid secretion
V1increases vascular smoont muscle contraction
V2increases H20 permeability and reabsorption in collecting tubules of kidney

Cholinergic Agonists

Question Answer
Name thembethanechol, carbachol, methacholine, pilocarpine
Postoperative ileusbethanechol
challenge test for diagnosis of asthmamethacholine
open angle and closed angle glaucomapilocarpine

Indirect Agonists (anticholinesterases) inactivate acetylcholinesterase and increase acetylcholine in the cleft

Question Answer
Name themdonepzil, edrophonium, neostigmine, physostigmine, pyridostigmine
Diagnosis of Myasthenia Gravisedrophonium
MG, urinary retention, postoperative ileus, reversal of neuromuscular junction blockage. NO CNS penetrationneostigmine
use in anticholinergic toxicity (aka atropine overdose). Crosses blood brain barrierphysostigmine
Organophosphate poisoning symptoms. Due to 2 much acetylcholine. Organophosphate irreversibly inhibits acetylcholinesteraseDUMBBELS (Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation CNS, lacrimation, Sweating, Salivation
if just give atropine in organophosphate poisoningdoes not prevent nicotinic effects such as muscle paralysis so give pralidoxime
antidote for organophosphate poisoningatropine and pralidoxime (regenerates acetylcholinesterase)
antidote for nondepolarizing NMJ drugs (aka curoniums)neostigmine and give atropine to prevent bradycardia from overstimulation of parasympathetic
antidote for depolarizing NMJ drugs (aka succinylcholine)anticholinesterases

Muscarinic antagonists

Question Answer
COPD, asthmaipratropium
Reduces bladder spasms and urge urinary incontinenceoxybutynin, solifenacin, tolerodine
motion sicknessscopolamine
Atropine tox symptomsHot as a hare. Dry as a bone. Red as a beet. Blind as a bat. Mad as a hatter. Tachycardia
Parkinson'sBenzotropine (Park my Benz)
Treatment for atropine overdosephysostigmine

Direct sympathomimetics

Question Answer
albuterol effectB1 greater than B2
DobutamineB1 greater than b2, alpha
epinephrineB1, B2, alpha 1, alpha 2
NEalpha 1 greater than alpha 2 greater than Beta 1
Phenylephrinealpha 1 greater than alpha 2
evaluation of tachyarrhthymiasisoproterenol
hypotensionNE, phenylephrine
low dose dopamineD1 and D2
medium doses dopamineB1 and B2
high doses dopaminealpha 1 and alpha 2

Indirect Sympathomimetics

Question Answer
amphetamineindirect general agonist, reuptake inhibitor
Narcolepsy, obesity, ADHDamphetamine
Cocaineindirect general agonist, reuptake inhibitor
Ephredrineindirect general agonists releases stored catecholamines

alpha 2 agonists

Question Answer
hypertensive emergencyclonidine
hypertension in pregnancyalpha-methyldopa

alpha blockers

Question Answer
nonselectivephenoxybenzamine and phentolamine
patients on MAO inhibitors who eat tyramine rich foodsphentolamine
selective alpha 1 blockersprazosin, terazosin, doxazosin
Selective for prostatetamsulosin
selective alpha 2 blockermirtazapine. use for depression

beta blockers

Question Answer
non-selective beta blockersN to Z
beta 1 blockersA to M with exception of C and L which are alpha 1 and beta 1
glaucoma drugstimolol, nadolol
non-selective beta 1, beta 2, alpha antagonistlabetalol and carvedilol
partial beta agonistpindolol, acebuetolol
do not use in anginabeta 1 and beta 2 weak agonists
selective antagonistsA to M
nonselective antagonistsN to Z

Cholinergic droogz

Question Answer
BethanecolDirect muscarinic agonist: Bladder and Bowel (ileus) (post op.) [Bethany calls on your Bowels and Bladder]
CarbacholDirect muscarinic agonist: Glaucoma
PilocarpineDirect muscarinic agonist: Open angle glaucoma (contracts ciliary), Closed angle glaucoma (contracts pupillary sphincter), Increases saliva (Xerostomia caused by radiation or Sjögren's) [Drool, cry and sweat on your Pillow]
NeostigmineIndirect muscarinic agonist: Myasthenia Gravis, Ileus (post op. and neurogenic), Reverse NMJ blockade (after anesthesia)
**does NOT penetrate CNS**
PyridastigmineIndirect muscarinic agonist: Long term Myasthenia Gravis
**does NOT penetrate CNS**
EdrophoniumIndirect muscarinic agonist: "Tensilon Test" to Dx Myasthenia Gravis treatment -- short-acting
**Does NOT penetrate CNS**
PhysostigimineIndirect muscarinic agonis: Glaucoma; Atropine overdose [Physo Phyxes Atropine]
**Penetrates CNS
DonepezilIndirect muscarinic agonist: Alzheimer's [Galant Donnie forgets his Rivals]
GalantamineIndirect muscarinic agonist: Alzheimer's [Galant Donnie forgets his Rivals]
RivastigmineIndirect muscarinic agonist: Alzheimer's [Galant Donnie forgets his Rivals]
AtropineMuscarinic antagonist: Organophosphate poisoning, Bradycardia, Dilates pupil
HomatropineMuscarinic antagonist: Pupil dilation -- short acting
TropicamideMuscarinic antagonist: Pupil dilation -- short acting
CyclopentolateMuscarinic antagonist: Pupil dilation -- short acting
BenztropineMuscarinic antagonist: Parkinson's, lessens side effects of antipsychotics [Park my Benz]
ScopolamineMuscarinic antagonist: Decrease secretions (on ventilator), Motion sickness [Scope down your throat and on a boat]
IpratropiumMuscarinic antagonist: COPD and asthma [I Pray for Tio jim to breathe]
TiotropiumMuscarinic antagonist: COPD and asthma [I Pray for Tio jim to breathe]
OxybutyninMuscarinic antagonist: Urge incontinence [On The Darn Toilet]
TolterodineMuscarinic antagonist: Urge incontinence [On The Darn Toilet]
DarifenacinMuscarinic antagonist: Urge incontinence [On The Darn Toilet]
SolifenacinMuscarinic antagonist: Urge incontinence [On The Darn Shitter]
TrospiumMuscarinic antagonist: Urge incontinence [On The Darn Toilet]
DiphenylhydramineH1 blocker with anticholinergic side effects.
**NOT a muscarinic antagonist**
DoxylamineH1 blocker with anticholinergic side effects.
**NOT a muscarinic antagonist**
AmantadineStimulates dopamine release and blocks dopamine reuptake with anticholinergic side effects.
**NOT a muscarinic antagonist**
TCAs (ex. amitriptyline)Cholinergic side effects
**NOT a muscarinic antagonist**
EchothiophateIndirect muscarinic agonist: Glaucoma
HemicholiniumCholine uptake inhibitor
*Research only*
VesamicolAntagonizes the packaging of ACh into secretory vesicle
*Research only*
Black widow toxinInduces release of ACh into synapse >> spastic paralysis
Botulinum toxinInhibits ACh release into synapse >> flaccid paralysis
Choline acetylransferaseEnzyme that converts Acetyl CoA+Choline >> ACh from Acetyl CoA and choline. Deficient in Alzheimer's.
PralidoximeIndirect Muscarinic antagonist (Reactivates AchE): Organophosphate poisoning


Question Answer
Atropine and Jimson Weed poisoningHot as hare. Dry as a bone. Red as a beet. Blind as a bat. Mad as a hatter. The bowl and bladder loose their tone and heart runs alone.
Atropine has what effects on the eyemydriasis, cycloplegia (paralysis of accomodation)
Anticholinergics are contraindicated in eye conditionglaucoma!!
What drug classes can have side effects similar to atropineTCA (amitriptyline), H1 receptor antagonist, neuroleptics and antiparkinsonian drugs

Urge Incontinence and Urinary Retention Drugs

Question Answer
Drugs used for urge incontinenceoxybutynin
Drugs used for urinary retentionbethanechol

Sympathetic Droogz

Question Answer
Epinephrinea1, a2, ß1, ß2 agonist: Anaphylaxis, Croup, Hypotension
Norepinephrinea1>a2, ß1 agonist: Hypotension, Septic shock
DopamineAgonist. Low: DA, Medium: ß1+ß2, High: a1+a2: HF, Unstable bradycardia, Shock
Dobutamineß1 > ß2 agonist; use for heart stress test, cardiogenic shock
Isoproterenolß1, ß2 agonist: Evaluate tachyarrhythimas. Not used clinically.
Phenylephrinea1 > a2 agonist: Dilates pupils, Rhinitis, Hypotension
Albuterolß2 > ß1 agonist: Asthma
Levalbuterolß2 > ß1 agonist: Asthma
Salmeterolß2 > ß1 agonist: Asthma longterm or COPD
Terbutalineß2 > ß1 agonist: Stops premature uterine contractions, Treats bronchospasm
Clonidinea2 agonist (which inhibits NE): Malignant HTN
*Beware of rebound HTN*
Alpha-methyldopaa2 agonist, inhibits DOPA decarboxylase: HTN in pregnancy (Pre-eclampsia)
PrazosinSelective a1 blocker: BPH [-azosin = a1 blockers]
*can cause hypotension + reflex tachycardia*
DoxazosinSelective a1 blocker: BPH [-azosin = a1 blockers]
*can cause hypotension + reflex tachycardia*
TerazosinSelective a1 blocker: BPH [-azosin = a1 blockade]
*can cause hypotension + reflex tachycardia*
TamsulosinVery selective a1 blocker in prostate: BPH
* does NOT cause hypotension/reflex tachycardia *
PhenoxybenzamineNonselective a-blocker: Pheochromocytoma
PhentolamineNonselective a-blocker: Pheochromocytoma
PropanololNonselective ß-blocker: HTN
TimololNonselective ß-blocker: Glaucoma
NadololNonselective ß-blocker: Glaucoma
MetoprololSelective ß1-blocker: HTN
AtenololSelective ß1-blocker: HTN
EsmololSelective ß1-blocker: Arrhythmia
PindololWeak ß1 and ß2 partial agonist, Competitively inhibits epi+NE: HTN with bradycardia [PACEs epi]
AcebutololWeak ß1 and ß2 partial agonist, Competitively inhibits epi+NE: HTN with bradycardia [PACEs epi]
AmphetamineIndirect sympathomimetic (Stimulates release of stored catecholamines): Narcolepsy, ADHD, Obesity
EphedrineIndirect sympathetic agonist (Stimulates release of stored catecholamines): Urinary incontinence, Nasal decongestant
CocaineIndirect sympathomimetic (Inhibits re-uptake of NE): Nasal decongestant, Anesthesia
ReserpineBlocks VMAT, inhibiting NE release
TyramineStimulates release of NE: nonpyschoactive sympathomimetic effects
**Does NOT cross the BBB**
BretyliumBlocks NE release from presynaptic cell: Anti-arrhythmic
TCAsBlock NE reuptake
Catechol-O-methyl transferase (COMT)Methylates catecholamines rendering them inactive
Monoamine oxidase (MAO)Oxidizes monoamines such as catecholamines, rendering them inactive
MetyrosineInhibits NE synthesis via Tyrosine hydroxylase (Tyrosine >> DOPA)
Angiotensin IIStimulates VMAT, stimulating release of NE
GuanethidineInhibits release of NE
How do M2 receptors regulate NE?Inhibit NE release (makes sense... don't want redundant signals)

Effect of Drugs on ACH

Question Answer
botulinum toxininhibits Ach release
black widow toxinstimulates Ach release
vesamicolinhibits Ach packaging
hemocholinuminhibits choline transport

Effects of drugs on NE

Question Answer
amitriptylineinhibits NE reuptake
amphetaminestimulates NE release
cocaineinhibits NE reuptake
guanethidineinhibits NE release
resperidinesinhibit NE packaging