Autonomic Drugs by Class Flashcards
- acetylcholine
- bethanechol
- carbachol
- cevimeline
direct M agonists, choline esters
muscarine
pilocarpine
M agonists, alkaloids
nicotine
varenicline
direct nicotinic agonist
neostigmine physostigmine pyridostigmine rivastigmine ambenonium demecarium carbaryl
cholinesterase inhibitors, carbamates
edrophonium
cholinesterase inhibitor, simple alcohol ester
echothiophate soman sarin parathion malathion isofluorophate DFP
cholinesterase inhibitor, organophosphates
donepezil
tacrine
galantamine
cholinesterase inhibitors
atropine scopolamine homatropine pirenzepine tropicamide tolterodine dicyclomine fesoteridine mepenzolate solifenacin oxybutinin darifenacin
M antagonist - tertiary amine
atropine methyl nitrate methscopolamine ipratropium propantheline glycopyrrolate
M antagonist - quaternary amine
hexamethonium
trimethaphan
mecamylamine
ganglionic blocking drugs
pralidozime (2-PAM)
cholinesterase regenerator
epinephrine (a1, a2, b1, b2) norepinephrine (a1, a2, b1) isoproterenol (b1, b2) dobutamine (b1) dopamine (d1)
catecholamines
ephedrine/pseudoephedrine cocaine tyramine amphetamine methamphetamine methylphenidate
indirect sympathomimetics
phenylephrine
methoxamine
oxymetazoline (afrin)
alpha-1 selective agonists
clonidine
methydopa
guanfacine
guanabenz
alpha-2 selective agonists
dobutamine
prenalterol
beta-1 selective agonists
albuterol
salmeterol
terbutaline
beta-2 selective agonists
- act on peripheral vasculature
- contract smooth muscle, pressor effects
alpha 1 adrenoceptors
- presynaptic autoregulation of neurotransmitter release
- decrease cAMP
alpha 2 adrenoceptors
- activate adenylyl cyclase, increase cAMP
- equal affinity for epi and NE
beta 1 adrenoceptors
- activate adenylyl cyclase, increase cAMP
- higher affinity for epi than NE
beta 2 adrenoceptors
- potent vasoconstrictor (alpha-1) and cardiac stimulant (beta-1)
- positive inotropic and chronotropic actions on the heart (beta-1)
- epinephrine activates beta-2 receptors
- mixed effects on TPR, increases venous capacitance
epinephrine
- alpha-1, beta-1 activator
- little effect on beta-2 receptors
- increases peripheral resistance
- increases diastolic and systolic BP
- compensatory vagal reflexes overcome direct positive chronotropy, at high doses may directly increase HR
norepinephrine
- potent nonselective beta agonist
- positive chronotropic and inotropic actions
- increases cardiac output
- decreases diastolic and MAP
isoproterenol
- activates D1 receptors in renal vasculature
- increases renal blood flow
dopamine
- relatively beta-1 selective synthetic catecholamine
- activates alpha-1 receptors
dobutamine
- alpha-1 agonist
- not inactivated by COMT, longer duration of actions
- mydriatic and decongestant, can raise BP
phenylephrine
alpha-1 selective sympathomimetic
methoxamine
first orally active sympathomimetic drug
ephedrine
- OTC decongestant
- release endogenous NE
pseudoephedrine
- direct alpha-1 agonists
- topical decongestant
oxymetazoline, xylometazoline
used as antihypertensives, diminish SNS outflow
alpha-2 agonists (clonidine, methlydopa, guanfacine, guanabenz)
- increase cardiac output with less reflex tachycardia
- lack of beta-2 stimulated venous dilation
beta-1 agonists
asthma and uterine relaxation in premature labor
beta-2 agonists (albuterol, salmeterol, terbutaline, ritodrine)
- indirect sympathomimetic, stimulant effect on mood and alertness
- drug of abuse
amphetamine
higher ratio of central to peripheral actions than amphetamine
methamphetamine
amphetamine variant used in ADHD
methylphenidate
sympathomimetic due to blockade of uptake 1
cocaine
releases stored catecholamines, found in fermented foods, MAO inhibitors potentiate effects, can produce hypertensive crisis
tyramine
phentolamine
phenoxybenzamine
tolazoline
nonselective alpha antagonists
prazosin terazosin doxazosin tamsulosin alfuzosin silodosin labetalol
alpha-1 selective antagonists
yohimbine
alpha-2 selective antagonists
reserpine
guanadrel
adrenergic neuron blocking drugs
propanolol nadolol timolol pindolol cartelolol penbutolol levobunalol labetalol
nonselective beta antagonists
metoprolol esmolol atenolol acebutolol betaxolol bisoprolol nebivolol
beta-1 selective antagonists
butoxamine
beta-2 selective antagonist
reversible (competitive) alpha antagonist
phentolamine
irreversible alpha antagonist, long duration of action
phenoxybenzamine
lower peripheral vascular resistance, reduce blood pressure
alpha antagonists
can reverse pressor effects of epinephrine, may cause postural hypotension and reflex tachycardia
alpha antagonist
- alpha antagonist, nonselective, competitive
- reduces TPR, MAP
- reflex tachycardia
phentolamine
irreversible alpha antagonist, binds covalently
- treatment of pheochromocytoma
- postural hypotension and tachycardia limit use
phenoxybenzamine
prazosin and terazosin
alpha-1 selective antagonist
alpha-1 antagonist with longer half life, treat HTN and BPH
doxazosin
competitive alpha-1 antagonists, good efficacy in BPH
tamsulosin, alfuzosin
alpha-2 selective antagonist, no clinical role, ED
yohimbine
pindolol, acebutolol, and carteolol
beta-antagonists with intrinsic sympathomimetic effects
ultra short acting beta-1 selective antagonist
esmolol
benazepril captopril enalapril fosinopril lisinopril moexipril perindopril quinapril ramipril trandolapril
ACE inhibitors
candesartan eprosartan irbesartan losartan olmesartan telmisartan valsartan
Angiotensin receptor antagonists
aliskiren
renin inhibitor
bosentan
endothelin receptor antagonist
aprepitant
neurokinin-1 receptor antagonist
desmopressin
vasopressin
vasopressin agonist
conivaptan
vasopressin receptor antagonist
aminophylline
theophylline
dyphylline
methylxanthines
albuterol, bitolterol, pirbuterol, metaproterenol, terbutaline
b-2 agonists
salmeterol and formoterol
long acting beta agonists
epinephrine, ephedrine, isoproterenol
sympathomimetics
ipratropium, tiotropium, atropine
muscarinic antagonists
montelukast, zafirlukast, zileuton
leukotriene antagonists
beclomethasone, budesonide, dexamethasone, flunisolide, fluticasone, mometasone
glucocorticoids
omalizumab
anti-IgE antibody
mepolizumab, reslizumab
anti IL-5 antibody
cromolyn sodium, nedocromil sodium
prophylactic agents