Autonomic Drugs Flashcards
Adrenal medulla and sweat gland innervation
Sympathetic nervous system innervated by cholinergic fibers
Nicotinic ACh receptors
ligand-gated Na/K channels
Nn in autoniomic ganglia
Nm in NMJ
H1 G-protein
Gq, increase mucus and permability
H2 G-protein
Gs, increases gastric secretion
V1 G-protein
Gq, increase vascular smooth muscle contraction
V2 G-protein
Gs, increase H2O permeability
Gq G protein receptors
H1, alpha1, V1, M1, M3
activates PLC and makes PIP2 into IP3/DAG
IP3 increases Ca
DAG protein kinase C
Gs Protein receptors
Beta-1 &2, D1, H2, V2
activates Adenylyl Cyclase
Gi protein receptors
M2, alpha2, D2
inactivates adenylyl cyclase
MoA Hemichoinium
Inhibits reuptake of choline
MoA Botulinum
inhibits release of ACh from presynaptic
MoA of Vesamicol
Inhibits ACh storage
MoA of Metyrosine
Inhibits Tyrosine becoming DOPA
MoA of Reserpine
Irreversibly inhibits VMAT whichnormally transports NE, Dopamine, and serotonin into intracellular vesicles
MoA of Bretylium and Guanethidine
inhibits NE release
Cocaine, TCAs, amphetamines
inhibits reuptake of NE
Bethanechol
Postoperative ileus, neurogenic ileus, and urinary retention
Carbachol
glaucoma, pupillary constriction, and relief of intraocular pressure
Pilocarpine
potent stimulator of sweat, tears, and saliva
open and closed-angled glaucoma
Methacholine
challenge test for diagnosis of asthma
Direct cholinomimetic agents
bethanechol, carbachol, pilocarpine, methacholine
Anticholinesterases
neostigmines, pyridostigmine, physostigmine, Donepezil, Rivastigmine, galantamine, edrophonium
Neostigmine
postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade postop
AChE for myasthenia gravis (long acting); does not penetrate CNS
Pyridostigmine
AChE for anticholinergic toxicity (crosses BBB)
Physostigmine
Anticholinesterase for Alzheimer’s
Donepezil, rivastigmine, galantamine
Edrophonium
historically used for myasthenia gravis diagnosis
Cholinesterase inhibitor poisoning
DUMBBELSS
diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimatino, sweating and salivation
Antidote for cholinesterase poisoning
Atropine(competitive inhibitor) + Pralidoxime (regenerates AChE)
Produce mydriasis and cycloplegia
Atropine, homatropine, tropicamide
Anti-muscarinic for Parkinson Disease
Benztropine
Muscarinic antagonist for motion sickness
Scopolamine
Anti-muscarinic for COPD and asthma
ipratropium and tiotropium
Reduce urgency in mild cystitis and reduce bladder spasms.
oxybutinin, darifenacin and solifanacin
Anti-muscarinic used post-op to reduce airway secretions
Glycopyrrolate (parenterally)
Anti-muscarinic used to decrease drooling and peptil ulcer
Glycopyrrolate (oral)
Atropine
anti-DUMBBELS
muscarinic antagonist
Atropine toxicity
hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter
can cause acute closed-angled glaucoma in elderly
Anaphylaxis, open angle glaucoma, asthma, hypotension
Epinephrine
Epinephrine receptor effect
beta > alpha
alpha predominate at high doses
hypotension (but decrease renal perfusion)
Norepinephrine
NE receptor effect
alpha1 > alpha2> beta1
Electrophysiological evaluation of tachyarrhythmias. can worsen ischemia
Isoproterenol B1 = B2
unstable bradycardia, HF, shock; inotropic and chronotropic alpha effects predominate at hgh doses
dopamine
DA receptor effect
D1 = D2 >beta > alpha
Heart failure (inotropic > chronotropic), cardiac stress testing
Dobutamine
hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant)
Phenylephrine
For Acute Asthma
Albuterol
B2>B1
For long term asthma of COPD control
Salmeterol
B2>B1
Reduce premature uterine contractions
terbutaline
B2>B1
For narcolepsy, obesity, attention deficit disorder
Amphetamine
nasal decongestion, urinary incontinence, hypotension
Ephedrine
Causes vasoconstriction and local anesthesia
Cocaine
Never give beta-blockers with this intoxication, can lead to unopposed alpha-1 activation and extreme hypertension
Cocaine
Alpha-2 Agonists
Clonidine and alpha-methyldopa
Used for HTN in pregnancy
alpha-methyldopa
Toxicity causes direct Coombs + hemolytic anemia, SLE-like syndrome
Clonidine
Off labeled used for ethanol and opioid withdrawl
Clonidine
Toxicity causes CNS depression, bradycardia, hypotension, respiratory depression and small pupil size
Clonidine
Irreversible alpha blocker
Phenoxybenzamine
Pheochromocytomas (used preoperatively) to prevent catecholamine (hypertensive) crisis
Phenoxybenzamine
Reversible alpha blocker
Phentolamine
Give to patients on MAO inhibitors who eat tyramine-containing foods
Phentolamine
Toxicity of Phenoxybenzamine
orthostatic hypotension and reflex tachycardia
alpha-1 selective blockers
prazosin, terazosin, doxazosin, tamsulosin
Used for urinary symptoms of BPH
-osin ending drugs
alpha-1 blocker for PTSD
prazosin
alpha-2 selective blocker
Mirtazapine used for depression
S/E of Mirtazepine
sedation, increased serum cholesterol, and increased appetite
Epinephrine w/ alpha blockade (phentolamine)
causes reversal of mean blood pressure change from high BP (w/o phentolamine) to low BP (w/ phentolamine)
Phenylephrine w/ alpha blockade (phentolamine)
the alpha blocker will suppress phenylephrine response on BP
SVT
metoprolol and esmolol, decrease AV conduction velocity
May exacerbate asthma or COPD
Beta blocker toxicity
non-selective alpha and beta antagonists
carvedilol and labetalol
non-selectiva antagonists (B1=B2)
nadolol, pindolil (partial agonist), propanolol, timolol
Beta-1 selective antagonists
acebutolol, atenolol, betaxolol, esmolol, metoprolol
ABEAM
What are you going to do with all that junk all that junk inside that trunk?
I’m gunna gunna get you drunk, get get you drunk
