Autonomic Drugs Flashcards
Sympathetic Nervous System organs innervated by cholinergic fibers?
Sweat glands and Adrenal Medulla
Botulinum Toxin
Prevents release of ACh at all cholinergic terminals
Nicotinic ACh receptors
Description
Location?
Ligand gated Na/K channel
Autonomic ganglia and NMJ
α1 System Kind of receptor? Class Function
Sympathetic
GPCR
q
Vascular SM contraction, Pupillary dilator muscle contraction (mydriasis), Intestinal and Bladder Sphincter muscle contraction
α2 System Kind of receptor? Class Function
Sympathetic
GPCR
i
↓ sympathetic outflow, ↓ insulin release, ↓ lipolysis, ↑ platelet aggregation
β1 System Kind of receptor? Class Function
Sympathetic
GPCR
s
↑ HR, contractility, rennin release, lipolysis
β2 System Kind of receptor? Class Function
Sympathetic
GPCR
s
Vasodilation, Bronchodilation, ↓ Uterine Tone (tocolysis)
↑ HR, contractility, lipolysis, insulin release
Ciliary Muscle Relaxation and ↑ Aqueous Humor production
M1 System Kind of receptor? Class Function
Parasympathetic
GPCR
q
CNS, Enteric Nervous System
M2 System Kind of receptor? Class Function
Parasympathetic
GPCR
i
↓ HR and atrai contractility
M3 System Kind of receptor? Class Function
Parasympathetic
q
GPCR
Exocrine gland secretion, gut peristalsis, bladder contraction, Bronchoconstriction, Pupillary sphincter muscle contraction (Miosis), Ciliary muscle contraction (accommodation)
D1
Kind of receptor?
Class
Function
GPCR
s
Relaxes renal vascular smooth muscle
D2
Kind of receptor?
Class
Function
GPCR
i
Modulates transmitter release, esp in brain
H1
Kind of receptor?
Class
Function
GPCR
q
Nasal and Bronchial mucus production, contraction of bronchioles, pruritus, pain
H2
Kind of receptor?
Class
Function
GPCR
s
Gastric Acid Secretion
V1
Kind of receptor
Class
Function
GPCR
q
Vascular smooth muscle contraction
V2
Kind of receptor
Class
Function
GPCR
s
↑ water permeability and reabsorption in collecting tubule of kidneys
Autonomic Receptor Mnemonic
QISS and QIQ until you're SIQ of SQS α1, α2, β1, β2 M1, M2, M3 D1, D2 H1, H2 V1, V2
Autonomic drugs that use IP3/DAG
“HAVe 1 M&M”
H1, α1, V1, M1, M3
Autonomic drugs that ↓ cAMP
“MAD2”
M2, α2, D2
Autonomic drugs that ↑ cAMP
Gs
“Bill Bob Doesn’t Have Value”
β1, β2, D1, H2, V2
Hemicholinium
Blocks re-uptake of choline at ACh nerve terminal
Vesamicol
Blocks ACh packaging into vesicles
Metyrosine
Inhibits conversion of Tyrosine to DOPA
Reserpine
Inhibits packaging of DA into vesicles
May be turned into NE in vesicle
Guanethidine
Inhibits release of NE
Bretylium
Inhibits release of NE
Cocaine Re NE
Inhibit re-uptake of NE
TCA Re NE
Inhibit re-uptake of NE
Amphetamine Re NE
Inhibit re-uptake of NE
Presynaptic Regulation of Noradrenergic nerve terminals
NE –> α2 –/ NE release
ATII –> NE release
ACh –> M2 –/ NE release
Bethanechol MoA Uses Organs affected Dynamics
Muscarinic agonist
PostOp ileus, Neurogenic ileus, Urinary retention
“Bethany Call me if you want to activate your Bowels or Bladder”
Activates Bowel and Bladder smooth muscle
Resistent to AChE
Carbachol
MoA
Uses
Mnemonic
Muscarinic and Nicotinic Agonists
Glaucoma, Pupillary Contraction, and Relief of Intraocular Pressure
“CARBon copy of AcetylCHOLine”
Pilocarpine MoA Affects Uses Organs affected Dynamics Mnemonic
Muscarinic Agonist
Stimulator of sweat, tear, and salivary glands
Open and closed angle glaucoma
Contracts ciliary muscles of eye (closed angle glaucoma), Pupillary sphincter (closed angle glaucoma)
Resistant to AChE
“You Cry, Drool, and Sweat on your PILOw”
Methacholine
MoA
Use
Muscarinic Agonist
Asthma challenge
Neostigmine
MoA
Distribution
Uses
Reversible AChE inhibitor
“Neo CNS” No CNS penetration
PostOp and neurogenic ileus and urinary retention, MG, Reversal of NMJ blockade PostOp
Pyridostigmine
MoA
Uses
Distribution
Reversible AChE inhibitor
“Rid of MG.” MG (long acting)
Does not penetrate CNS
Edrophonium
MoA
Uses
Reversible AChE inhibitor
Diagnosis of MG (short acting)
Physostigmine
MoA
Distribution
Uses
Reversible AChE inhibitor
Crosses BBB
Anticholinergic toxicity
“PHYso PHYxes atropine poisoning”
Donepezil
Distribution
Uses
Reversible AChE inhibitor
CNS
Alzheimer’s Disease
Risk of all AChE inhibitors
Exacerbation of COPD, Asthma, Peptic Ulcer Disease
Cholinesterase Inhibitor Poisoning What is it? What causes it? Presentation Classic pt Antidote
Irreversible AChE inhibition
Organophosphates like Parathion
“DUMBBELSS”
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation (of skeletal muscle and CNS), Lacrimation, Sweating, Salivation
Farmer working with insecticides
Atropine + Pralidoxime (regenerates active AChE)
Homatropine MoA Molecule like it? Organs affected? Uses
Muscarinic Antagonist
Atropine, Tropicamide
Eye
Produces mydriasis and cycloplegia
Benztropine
MoA
Organs involved
Use
Muscarinic Antagonist
CNS
“PARK my BENZ”
Parkinson’s Disease
Scopolamine
MoA
Organs involved
Uses
Muscarinic Antagonist
CNS
Motion sickness
Ipratropium MoA Molecules like it Organis involved Use
Muscarinic Antagonist Tiotropium Respiratory COPD and Asthma "I PRAY i can breath again"
Oxybutynin
MoA
Organs involved
Use
Muscarinic Antagonist
GU
Reduce urgency in mild cystitis and reduce bladder spasms
Glycopyrrolate
MoA
Organs involved
Use
Muscarinic Antagonist
GU and Respiratory
Parenteral: PreOp use to reduce airway secretions
Oral: Drooling, Peptic Ulcers
Atropine
MoA
Eye, Airway, Stomach, Gut, Bladder
Presentation
Muscarinic Antagonist
↑ pupil dilation, cycloplegia (acute angle glaucoma in elderly)
↓ airway secretions, ↓ stomach acids, ↓ gut motility (constipation), ↓ bladder urgency
Blocks DUMBBeLSS (excitation mediated by nicotinic receptors)
Atropine Poisoning
Hot as a Hare Dry as a Bone Red as a Beat Blind as a Bat Mad as a Hatter
What receptors does Epi affect?
What are its uses?
α1, α2, β1, β2 (β more)
Anaphylaxis, Open Angle Glaucoma, Asthma, Hypotension
What receptors does NE affect?
What are its uses?
α1, α2, β1 (α more)
Hypotension (but ↓ Renal Perfusion)
What receptors does Isoproterenol affect?
What are its uses?
β1, β2
Torsade de pointes, Bradyarrhythmias (but can worsen ischemia)
What receptors does DA affect?
What are its uses?
α1, α2, β1, β2, D1
Shock (renal perfusion) and heart failure
What receptors does Dobutamine affect?
What are its uses?
α1, α2, β1, β2 (β1 way more so!)
Heart failure, Cardiac stress test
What receptors does Phenylephrine affect?
What are its uses?
α1 and α2 (α1 more)
Hypotension, Ocular procedures (mydriatic), Rhinitis (decongestant)
What receptors does Albuterol affect?
Similar drugs?
What are its uses?
β1, β2 (β2 more so) Salmeterol, Terbutaline A: acute Asthma S: long term Asthma, COPD T: reduce premature uterine contractions
Ritodrine
What receptors does it affect?
Uses
β2
Reduce premature uterine contractions
Amphetamine
MoA
Uses
Release of stored Catecholamines
Narcolepsy, Obesity, ADD
Ephedrine
MoA
Uses
Release of stored Catecholamines
Nasal decongestion, Urinary incontinence, Hypotension
Cocaine
MoA
What does it lead to?
Contraindications
Inhibits reuptake of catecholamines
Vasoconstriction and local anesthesia
β blockers contraindicated because can lead to unopposed α activation and HTN
NE vs Isoproterenol
NE –> ↑ in systolic and diastolic BP
α mediated vasoconstriction –> ↑ MAP –> Bradycardia
Isoproterenol –> β2 mediated vasodilation –> ↓ MAP and ↑ HR through β1 and reflex activity
Clonidine
MoA
Molecules similar to it?
Uses
α2 agonist –> ↓ central sympathetic outflow
α methyldopa
HTN esp with Renal Disease
Phenoxybenzamine MoA Reversibility Uses Tox
α blocker
Irreversible
Pheochromocytoma (PreOp)
Orthostatic Hypotension and reflex Tachycardia
Phentolamine
MoA
Reversibility
Uses
α blocker
Reversible
Give to pts on MAO inhibitors who eat tyramine-containing foods
α1 blockers
Names
Uses
Tox
Prazosin, Terazosin, Doxazosin, Tamsulosin
HTN, Urinary retention in BPH
Orthostatic Hypotension, Dizziness, Headache
α2 blockers
Names
Uses
Tox
Mirtazapine
Depression
Sedation, ↑ Cholesterol, ↑ Appetite
Phenylephrine vs Epi on α blockade
Epi will cause net decrease in BP because of actions on β
PE will cause a reversal to baseline because it is pure α
β blockers
Names
Applications
Acebutolol, Betaxolol, Esmolol, Atenolol, Metolol, Propanolol, Timolol, Pindolol, Labetalol
Angina Pectoris, MI, SVT (M and E ↓ conduction velocity), HTN (renin), CHF, Glaucoma (T ↓ secretion of aqueous humor)
β blockers Tox
Use with caution in…
Bradycardia (AV block and CHF), Bronchoconstriction, Claudication, Lipids, Vivid dreams (seizures, sedation), Impotence, Masks hypoglycemia
Use with caution in diabetics, ↓ insulin release
Use with caution in diabetics
β1 blockers
“A BEAM” Before M in the alphabet
Acebutolol, Betaxolol, Esmolol, Atenolol, Metoprolol
Non selective β blockers
“Please Try Not βeing Picky” After M in the alphabet
Propanolol, Timolol,Nadolol, Pindolol
α and β non selective blockers
Carvedilol, Labetalol
Partial β Agonists
Pindolol, Acebutolol