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Pharmacology Month 1 Week 2 Day 5 Sympathomics
Pharmacology Month 1 Week 2 Day 5 Sympathomics
65
Pharmacology
Graduate
05/18/2018

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Term
Mean arterial pressure is
Definition
cardiac output times SVR
Term
Cardiac output is
Definition
heart, beta 1 and 2. agonizing beta causes an inc in cardiac output
Term
SVR is
Definition
alpha 1, alpha 2, beta 2. agonize alpha 1 and SVR goes up, opposite with beta 2 and central alpha 2 agonists
Term
drugs that mainly affect B1
Definition
metoprolol (met a pro. lol), acebutolol (ace butter lol), alprenolol (alfredo lol), atenolol (attend lol), betaxolol (better tax lol), celiprolol (sell a pro lol), esmolol (is small lol), nebivolol (never bowl lol) (selectivity can be lost w increased dose)
Term
drugs that affect B1 and B2 evenly
Definition
propanolol, cartelol (cart all), nadolol (neighbor all), penbutolol (pen button all), pindolol (pin doll all), timolol (timber all)
Term
drugs that mainly affect B2
Definition
butoxamine (botox mine)
Term
a1 selective blockers
Definition
prazosin, terazosin, doxazosin, phenoxybenzamine (fend off ben)
Term
a1a selective blockers
Definition
tamulosin
Term
non-selective a1+2 blocker
Definition
phentolamine (fend off amy)
Term
a2 selective blocker
Definition
yohimbine (yo him) (improves male sexual function and promotes sympathetic outflow, not clinically proven)
Term
phenoxybenzamine
Definition
not commonly used because duration of action is too long, can last up to 48 hrs
Term
B1 blockers
Definition
MEN2A2B, Metoprolol (met a pro. lol), esmolol (is small lol), nebivolol (never bowl lol), atenolol (attend lol), acebutolol (ace butter lol), bisoprolol (biz pro lol), betaxolol (better tax lol), may be safer to use in asthmatics than non selective beta blockers (bc blocking B2 can cause bronchial smooth muscle contraction which would be bad in asthmatics)
Term
non-selective B1+2 and a1 antagonists
Definition
carvedilol, labetalol (label it all) (for greater lowering of BP)
Term
non-selective B1+2
Definition
all the other "-lol"s, ex propanolol, sotalol (sortof all)
Term
beta blockers half lives
Definition
most 10 hrs w exception of esmolol (IV) which is shorter (10 min) (good for emergent situations)
Term
beta blocker lipid solubility
Definition
higher lipid solubility, more it will penetrate CNS (GAD, stage fright)
Term
partial agonist activity beta blockers
Definition
acebutolol (ace butter lol), cartelol (cart all), celiprolol (sell a pro lol), pindolol (pin doll all), penbutolol (pen button all) (partially activate beta receptor and inhibit at same time, keep HR and BP stable, not commonly used in practice)
Term
beta blocker local anesthetic aciton
Definition
experimentally been shown to block calcium channels, not used this way clinically
Term
BPH treatment
Definition
a1 blockers- zosins (can cause dec in systemic svr and bp) or a1 tamulosin (better, prostate and bladder smooth muscle will relax)
Term
alpha 1 blockers for hypertension
Definition
zosins (dec svr, located in baroreceptors of carotid arteries)
Term
treatment for hypertension
Definition
any beta blocker, (also a1 blocker). beta blockers dec cardiac output by decreasing heart's ability to pump out volume, dec volume to surplus circulation -> dec BP. they also suppress the RAS system- renin-angiotensin-aldosterone system, beta blockers in the kidneys where RAS is activated so dec SVR by decreasing amount of sodium in circulation- sodium helps promote the absorption of water)
Term
ischemic heart disease treatment
Definition
any beta blocker, works by decreasing cardiac output by decreasing oxygen demand by the heart, slows it down, also decreased amnt of fluid by suppressing RAS so heart doesn't have to work as hard
Term
heart failure treatment
Definition
any beta blocker, decreased demand, decreased fluids so heart doesn't have to work as hard
Term
cardiac arrhythmia treatment
Definition
any beta blocker, decrease HR (also effective for managing supraventricular arrhythmias/atrial arrhythmias). beta 1+2 antagonists work by increasing atrioventricular nodal refractory period
Term
ventricular arrhythmia treatment
Definition
sotalol- blocks beta receptors in the heart and potassium channels
Term
conduction fibers of heart and electrical functioning and ventricular arrhythmias
Definition
electricity flows down these from SA node (starts HR) to middle of heart AV node (gatekeeper of electrical impulses to ventricles), pass into ventricles and cause contraction (atrial contraction 1st -> AV node -> ventricular contraction). beta receptors are primarily located at AV node. why beta blockers are bad for ventricular arrhythmias bc it bypasses the AV node
Term
sympathetic is
Definition
adrenergic, stressed out, dopamine, norepi, epi neutrotransmitters, receptors are alpha, beta and dopamine
Term
affects beta 3
Definition
mirabegron
Term
agonize beta 1 or 2
Definition
cardiac output goes up
Term
agonize alpha 1
Definition
SVR goes up
Term
agonize beta 2 or central alpha 2
Definition
SVR goes down
Term
receptor selectivity for alphas and betas
Definition
not absolute, dose dependent and drug-drug interactions can affect drug receptor specificity, ex give drug that enhances effects of dopamine. or if you have liver failure get inc lvls of drug and dec receptor specificity
Term
MOA of alpha 1
Definition
agonism of alpha 1 -> conversion of GDP to GTP -> upregulation and inc activity of phospholipase C ->

-> inc activity of DAG -> inc activity of protein kinase C
-> enhanced by IP3 -> inc free calcium -> release of adrenergic neurotransmitter

[image]
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Term
MOA of beta receptors
Definition
agonist activates beta receptor -> GDP -> GTP -> inc ATP -> inc GTP to cyclic AMP -> inc release of calcium -> action potential and inc release of epi, norepi, dopamine

[image]
Term
agonize alpha 2 MOA
Definition
agonize alpha 2 -> GDP -> GTP -> dec conversion of ATP -> cAMP -> dec dopamine, norepi, epi

[image]
Term
first sympathiomimetic drug isolated
Definition
phenylethylamine
Term
catecholamine
Definition
has OH present in 3rd or 4th position, ex dopamine (inc's potency, dec duration of action, dec CNS penetration) (ex dopamine has 15 min half life and phenylethylamine has 1 hr half life) (dopamine not clinically useful for CNS diseases, amphetamine-ADHD- is bc has OH)
Term
structure of sympathiomemetic drugs
Definition
inc size of alkyl size chain or the longer the side chain, the more likely it will agonize beta receptor and the less likely it will agonize alpha receptor, ex isoproterenol has a long side chain and large alkyl subunit so it is more likely to be a beta selective agonist, epinephrine has equal beta and alpha selectivity, norepi is shortest and has more alpha selectivity
Term
add a group to alpha of side chain
Definition
inc duration of action, blocks degredation by MAO (ex CH3 group on methoxamine, ephedrine and amphetamine that increases duration of action)
Term
alpha agonists a1> a2>>>>>>beta
Definition
phenylephrine (finally free dine), methoxamine (a1> a2>>>>>>beta), clonidine (chronic dine), methylnorepinephrine (might i never dine) (a2>a1>>>>>>>Beta)
Term
mixed alpha and beta agonists
Definition
norepinephrine (a1=a2, b1>>b2), epinephrine (a1=a2, b1=b2)
Term
beta agonists
Definition
dobutamine (dobby is mine) (b1>b2>>>>a), isoproterenol (i so pretend it all) (b1=b2>>>>a), albuterol terbutaline (there's a brutal line) metaproterenol (might i pretend it all) ritodrine (right in line) (b2>>b1>>>>a)
Term
dopamine agonists
Definition
dopamine (D1 = D2>>b>>a), Fenoldopam (fend off the pam) (D1>>D2)
Term
phenylephrine (finally free dine)
Definition
inc's SVR, commonly referred to as an IV vasopressor bc of its selective alpha 1 agonism activity
Term
mixed alpha and beta agonists
Definition
dopamine, norepi, epi, have vasopressor effect and inotrope effect
Term
agonism of beta 1 and 2 drug is called
Definition
inotrope (inc CO, SV and HR)
Term
agonism of alpha 1 drug is called
Definition
vasopressor, inc SVR
Term
differences in agonism of betas and alphas
Definition
agonism of beta 1 and 2 causes inc cardiac output, agonism of beta 1 causes inc cardiac output-primaryily affects myocardium, b2 agonism cuases inc cardiac output and causes bronchial smooth muscle to relax (good for asthma/albuterol)
Term
iv inotropes
Definition
dobutamine and isoproterenol
Term
oral vasopressor that agonizes alpha 1 activity
Definition
midodrine (middle of dream)
Term
IV vasopressor drugs
Definition
epinephrine, norepinephrine, dopamine, phenylephrine (finally free dine)
Term
catecholamines
Definition
epinephrine, norepinephrine, dopamine, fenoldopam (fend off the pam) , dopamine agonists, dobutamine (dobby of mine)
Term
Amphetamine derivatives
Definition
amphetamine, modafinil (modify), methylphenidate (mild fend off date)
Term
Special sympathomimetics
Definition
cocaine, ephedrine (weight loss no longer available), tyramine (try me)
Term
Genitourinary B2
Definition
terbutaline inj. (there's a brutal line), ritodrine (riddle dream)
Term
sedative central a2
Definition
dexmedetomidine (dexter of mine)
Term
pulmonary b2 for local application
Definition
albuterol ,terbutaline inj. (inhaler available only
in Canada)
Term
opthalmic a2 for local application
Definition
brimonidine (brim of a dime)
Term
nasal a2a for local application
Definition
Oxymetazoline (ought you get in line)
Term
Shock
Definition
• Complex acute cardiovascular syndrome, low BP
• dec mean arterial pressure, dec ability to deliver oxygen to tissues-> cell death->organ failure
Term
treatment for shock
Definition
IV vasopressors (epinephrine, norepinephrine, dopamine, phenylephrine), exception is cardiogenic shock- use IV inotropes (dobutamine, isoproterenol) then vasopressors
Term
types of shock
Definition
NO CASH, Neurogenic, Obstructive, Cardiogenic, Anaphylactic, Septic, Hypovoluemic
Term
distributive shock
Definition
vasodilation, septic and anaphylactic, immune-mediated
Term
what is tyramine
Definition
found in foods that are highly fermented (cheese, wine, alcohol), inc consumpiton -> inc conversion to norepinephrine. tyramine is broken down by MOA (monamine oxidase). if you take an MOA inhibitor (depression), inc's tyramine indirectly. but if you also consume a lot of tyramine containing foods, inc risk of too much norepinephrine -> inc CO and SVR -> hypertension or hypertensive crisis
Term
most commonly used beta 2 agonist
Definition
albuterol, and terbutaline injectable (for asthma), historically used to treat w epinephrine and isoproterenol (inc SVR and BP)
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