ANS Flashcards
M1
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
- cholinergic
- nerve endings
- Gq
- increased IP2 and DAG
- activate myenteric plexus
M2 cholinergic/adrenergic - location -mechanism -2nd messenger -Action
-cholinergic
-heart, some nerve endings
-Gi
-decreases cAMP, activates K+ channels
Slows SA node
M3
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
- cholinergic
- smooth muscle, glands, endothelium
- Gq
- increased IP3, DAG cascade
- contract detrusor, increase salivation
Nn
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
- cholinergic
- ANS ganglia
- Na-K ion channel
- Na
- Depolarizes postgang fiber, evokes AP
Nm
- cholinergic/adrenergic
- location
- mechanism
- 2nd messenger
- Action
- cholinergic
- neuromuscular plate
- Na-K ion channel
- Na
- depolarizes muscle cell and evokes AP and contraction
A1
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
- adrenergic
- smooth muscle (especially vasculature) , glands
- Gq
- increase IPR, DAG
- increase Ca and causes contraction of vascular SM and/or secretion from glands
A2
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
- adrenergic
- nerve endings and some smooth muscle
- Gi
- decrease cAMP
- decrease transmitter release in the nerve and decrease contraction in smooth muscle
B1
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
- adrenergic
- cardiac muscle and JGA
- Gs
- increase cAmP
- increase HR and contractility and renin release
B2
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
- adrenergic
- smooth muscle, liver,heart
- Gs
- increase cAMP
- relax bronchiolar smooth muscle; increase glycogenolysis; increase HR and contractility
B3
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
- adrenergic
- adipose cells
- Gs
- Increase cAMP
- increase lipolysis
Dopamine
- cholinergic/adrenergic
- location
- G protein
- 2nd messenger
- Action
- adrenergic
- smooth mucle
- Gs
- increased cAMP
- relax vasculature in renal arterioles
Phenylephrine Description
synthetic alpha receptor agonist that is most selective for a1
Phenylephrine Action
vaso and venoconstriction by stimulating contraction of vascular smooth muscle
Phenylephrine Indications (3)
Nasal decongestant
Mydriatic (pupil dilator)
increased BP in vasodilator state
Other facts about phenylephrine (3) -potency compared to Norepi -deactivation -routes
less potent than norepi
not deactivated by COMT
can be given topically and IV
Clonidine short card info
Description
-selective A2 agonist
Clonidine short card Action
stimulate a2 in brianstem, causes down regulation of sympathetic nervous system
Clonidine indications (short card) (2)
treat hypertension
treat migraine
Clonidine other facts
- route
- side effects
- overdose effect
- orally or patch
- sedation/ dry mouth
- if given IV or OD can cause high BP
Phenylephrine brand name
Neosynephrine
Clonidine brand name
Catapres
Isoproterenol brand name
Isuprel
Isoproterenol description
B1/B2 receptor agonist
isoproterenol actions
potent b1/b1 agonist
isoproterenol indications
3
increase cardiac contractility
increase HR
increase cardiac conduction
isoproterenol other facts
- route
- why isn’t it used so much
- what else does it cause
- iv
- no longer used in CCu b/c can cause tachyarrhythmias like V-tach
- also causes vasodilation
Dobutamine trade name
Dobutrex
Dobutamine description
synthetic B1 receptor agonist
dobutamine action
potent b1 agonist in heart (increases contractility more than HR) and blood vessels (dilates renal and mesenteric vessels)
dobutamine indications (2)
- increase cardiac contractility more than HR
- Use for in CCU for patients in cardiogenic shock where you do not want tachycardia (i.e. most MI)
dobuatmine other facts
- route
- side effects (3)
-IV
tachy, hypertension, ectopy
albuterol trade name
ventolin
albuterol description
synthetic b2 selective receptor agonist
albuterol actions
b2 agonist: receptors on smooth muscle cells in airways and uterus and relaxes above tissues
albuterol indications (2)
prompt acting rescue inhaler for asthma, COPD
and inhibits premature labor
albuterol other facts
- most often given as..
- other route
- what’s the deal w/ IV
- side effects (3)
- metered dose inhaler
- nebulizer
- rarely given as iv infusion
- anxiety, tachy, tremor
Mirabegron trade name
Myrbetriq
Mirabegron Description
selective B3 agonist
Mirabgeron action
stimulates b3 receptors in smooth muscle of bladder, reduces detrusor muscle tone
Mirabegron indications
- treatment of patients w/ overactive bladder with features of urinary urgency/frequency
- inreases bladder capacity
- does not produce bothersome anticholinergic symptoms like tolteridine
other facts about mirabegron
2
approved in June 2012
administered orally as extended release tablets
Methoxamine description
alpha 1 and 2 agonist
Epinephrine tradename/ and one other name
EpiPen
Adrenaline
Epinephrine Drug class
- pharmacologic
- therapeutic
- pharm: direct acting adrenergic agonist
- Therapeutic: vasopressor, cardiac stimulant, bronchodilator, adjunct to local anesthetics, treatment for anaphylaxis
Epinephrine Pharmacodynamics
major action is to stimulate a1 adrenoreceptors to cause vasoconstriction and venoconstriction; stimulate b1 receptors for tachycardia and increased contractility ; b2 for bronchodilation–these actions are helpful in severe allergic runs by stabilizing mast cells (b1/b2)
Epi Pharmacokinetics
- route(4)
- metabolism
can be given IV (immediate), IM variable , SC (5-15 min), via inhalation (1-5 min onset) , opthalmic topical
- metabolized by COMT and then renally excreted
Epi Toxicity (5)
excessive vasoconstriction HTN hemorrhagic stroke angina arrhythmias
Epi Interactions
risk of excessive hypertension in patents taking propranolol
Epi special considerations (2)
utility w/ local anesthetics
drug of choice in severe anaphylactic runs (along w/ others)
Epi indications and dose/route
3
for anaphylaxis: 0.1-0.5 mg SC or IM
for cardiac arrest: 1-5 mg IV push
for infusion 1-4 mcg/min
Epi : things to monitor (5)
BP HR rhythm infusion site evidence of extravasation
Norepinephrine trade name/ one other name
Levophed
noradrenaline
norepi drug class
- pharm
- therapeutic
pharm- direct acting adrenergic agonist
therapeutic- vasopressor, vasoconstrictor
Norepi pharmacodynamic
major action is to stimulate a1 adrenorecpetors to increase vasoconstriction and venoconstriction. This increases CO, SVR, and MAP, but decrease blood flow to vulnerable tissues like skin, muscle, and kidney
also stimulates b1 in heart, increasing HR and contractility. Main effects are vasoconstriction and cardiac stimulation
Norepi Toxicity
2
excessive vasoconstriction in mesenteric vessels, peripheral arterioles causing ischemia, infraction, gangrene, reflex brady
Norepi interactions
use cautiously in peeps takin MAO inhibitors like phenlzine;
risk of excessive hypertension in peeps taking propranolol
Norepi special considerations
3
correct volume depletion before giving NE
select infusion site carefully-extravasation is a major problem; monitor patent and BP continuously in ICu; use cautiously in ped and geriatric patients
Norepi Indications and dose/route
for adults with acute hypotension and shock related to low SVR
infuse 2-12 mcg/min
norepi things to monitor (4)
BP
HR
infusion site
extravasation
Dopamine trade name
intropin
dopamine descrption
agonist at DA, B1, and a1 receptors
dopamine actions
relative potency depends on dose being delivered; DA agonist at low dose, B1 agonist at medium dose; a1 agonist at high dose
Dopamine indications (2)
shock of various etiologies in ICu
can produce increased contractility (B1)
vasoconstriction (a1) and improve mesenteric and renal perfusion (DA)
Dopamine Other facts
-route
given IV , preferably for a short period of time
Norepi pharmacokinetics
F~ 100% Given IV only metabolized by comt and mao in liver metabolites excreted in urine half life is 1-2 minutes can cross placenta, but not BBB
Ephedrine description
Alkaloid obtained from plants
Ephedrine action
acts inertly to release NE from adrenergic nerve endings, also some direct agonism at receptors
Ephedrine Indications (2)
Mild to moderate hypotension during surgery (very fast acting)
Nasal decongestion
other facts about ephedrine
- duration of action
- potent stimulant of what
- side effects (2)
- FDA status
- somewhat prolonged action
- potent CNS stimulant
- side effects = hypertension and insomnia
- OtC banned by FDA
Pseudoephedrine description
synthetic derivative of ephedrine
actions of pseudoephedrine
acts indirectly to release NE from adrenergic nerve endings, and some direct agonism at alpha and beta adrenergic receptors
pseudoephedrine indications
- nasal and sinus decongestant
- less ability to dilate bronchioles than ephedrine
other fact about pseudo ephedrine
- when approved
- what year were bulk sales reported
- what year increased security
- what year labeled as risk of injury/death or no cold products for kids
- 1959
- 1996
- 2005
- 2008
Amphetamine description
synthetic compound similar to ephedrine
amphetamine actions
acts indirectly to release NE from adrenergic nerve endings
amphetamine indications
- none are FDA approved
- obesity
- narcolepsy
- ADHD
amphetamine other facts
- approval
- risk of dependence
- side effects
- 1939
- high risk of dependence
- insomnia, restlessness, tremor
Tyramine description
naturally occurring byproduct of tyrosine metabolism; present in fermented food
tyramine actions
indirectly releases NE from adrenergic nerve endigns
tyramine indications
none are FDA approved
- obesity
- narcolepsy
- ADHD
tyramine other facts
- metabolized by what enzyme
- what kind of patients should be watched out for
- what is a common interations
- MAO
- patients on MAOIs
- food/drug
- MAOI+ food= hypertensive crisis
Cocaine description
purifed alkaloid extract from coca plant
cocaine actions
indirectly blocks reuptake of NE, Epi, and DA, and can stimulate release of Ne, Epi, and DA
can also sat as local anesthetic and CNS stimulant
indications (2)
- nose bleeds (anesthesia plus vasoconstriction)
- anesthesia for corneal surgery
other facts about cocaine
- effects compared to amphetamine
- routes
- side effects (5)
more intense, longer lasting
smoked, snorted, injected
HTN, tachy, arrhythmias, seizures, MI
Prazosin Trade name
Minipress
Prazosin Drug class
- pharmacologic
- therapeutic
- selective alpha 1 adrenoreceptor blocker
- antihypertensive, treatment of BPH
Prazosin pharmacodynamics
blocks alpha 1 receptors on arterioles and veins, thereby inhibiting NE-mediated faso and venoconstriction
Prazosin pharmacokinetics
- route
- bioavailability
- onset
- duration
- where is it metabolized
available po or transdermal
variable oral bioavailability (~60%) , onset 2h, duration 12-24h; extensively metabolized in liver
Prazosin Toxicity
excessive hypotension with syncope, especially orthostatic, especially in patients on diuretics
Prazosin Interactions
additive effects w/ most other antihypertensives, especially diuretics
Prazosin special considerations
2
start gradually, and at bedtime, to avoid first time passing out; male patients w/ BPH?
Prazosin indications and dose/route
as mono therapy begin with 1 mg tid, advance to 20mg per day divided tie
Prazosin monitor
BP, weight, edema
Tamsulosin tradename
Flomax
Tamsulosin cost
5-70 $ per month
Tamsulosin drug class
- phram
- therapeutic
selective a1blocker
treatment of obstructive symptoms of BPH
Tamsulosin pharmacodynamics
selectively blocks a1 receptors, but preferentially in the prostate, leading to relaxation of smooth muscles in the bladder neck and prostate, improving urine flow, and reducing obstructive symptoms of BPH venoconstricton
Tamsulosin Pharmacokinetics
- how much is absorbed
- what % metabolized by CYP 450 enzymes
- half life
- duration of action
completely absorbed after oral ingestion; >90% metabolized by CYP 450 enzymes
half life about 6 hrs, but duration of action up to 15 hours due to slow absorption
Tamsulosin Toxicity (3)
excessive hypotension with syncope, especially orthostatic, especially in patients on diuretics,allergic rxns, decreased libido
Tamsulosin Interactions
additive effects w/ most antihypertensives, especially diuretics
Tamsulosin special considerations (3)
- rule out carcinoma of prostate before beginning treatment
- do not crush or chew tablets, as that wills speed up absorption;
- can ask be used to treat spasm of ureter in patients with kidney stones
Tamsulosin Indications and dose/route
for symptoms of BPH, 0.4 mg po qd or bid; similar doses for renal colic
Tamsulosin monitor
BP
Prazosin cost
4-20 $ per month
Phentolamine trade name
Regitine
Phentolsamine Drug class
- pharm
- therapeutic
- non-selective competitive alpha adrenergic receptor blocker
- antihypertensive drug for patents w/ pheochromocytoma
phentolamine pharmacodynamics
blocks a1/a2 adrenergic receptors and presynaptic and post synaptic alpha receptors , decreasing preload and after load
phentolamine/regitine pharmacokinetics - route -F - plasma half-life
only comes in IV formulations, so F=100%; plasma half-life about 20 min after IV dose
phentolamine/regitine toxicity (3)
- excessive hypotension w/ syncope especially orthostatic, especially in patients on diuretics;
- allergic rxns;
- decrease libido
phentolamine interactions
additive effects w/ most other antihypertensives, especially diuretics
phentolamine special considerations
3
- rule out carcinoma of prostate before beginning treatment
- do not crush or chew tablets, as that wills speed up absorption;
- can ask be used to treat spasm of ureter in patients with kidney stones
phentolamine indications and dose/route
-indications (4
- Aid Dx of pheo
- treatment of intraop HTN during pheo removal surgery
- prevention of dermal slugging after extravasation of NE infusion
- hypertensive crisis from sympathomimetic amines
- Dose 5 mg IV, then titrate
phentolamine/regitine monitor
BP
Atenolol brand name
Tenormin
Atenolol similar drugs (2)
metroprolol
Toprol XL
atenolol class price range
4/52 to $100 for Toprol XL
Atenolol/Tenormin
- pharm
- therapeutic (4)
- specific b1 blocker
- antihypertensive, anti arrhythmic, primary and secondary prevention of MI, anti anginal
Atenolol/Tenormin pharmacodynamics
binds directly to B1 receptors w/ preference for beta-1 –leads to lower bP via several potential mechanisms; recent evidence suggests less effective in preventing strokes than other drugs
Atenolol/ Tenormin pharmacokinetics
- route
- F
- onset
- duration
- how many times/ day
- how excreted
- metroprolol metabolism
- po/iv
- variable
- onset 1-2 hrs
- durations 12-24h
- can be given once per day
- renally excreted (so has longer half life)
- metoprolol has hepatic metabolism so has shorter half life
Atenolol/ Tenormin Toxicity
5
- excessive hypotension
- bradycardia
- heart block
- can worsen severe cHF (but indicated for mild/moderate/stable CHF)
- worsen bronchospasm in severe asthmatics
Atenolol/Tenormin Interactions
- additive effects w/ most other anti-hypertensives
- additive AV block with CEBs (calcium entry blockers)
Atenolol/Tenormin Special Considerations
may be especially useful in HTN patients w/ exertional angina, MI, A fib
watch out for abrupt withdrawal
metoprolol has more data for use in patents s/p MI
Atenolol/Tenormin Inidcations and dose/route
for HTN patients
25-100 mg per day in one or two doses
Atenolol/Tenormin monitor (3)
BP HR exercise
Propranolol trade name
Inderal
Propranolol/Inderal drug class
- pharm
- therapeutic (4)
-non specific B blocker
-antihypertensive, antiarrhythmic, primary and secondary prevention of MI
; anti-anginal
Propranolol/Inderal cost
4$ up to $180
Propronalol/Inderal pharmacodynamics
binds to B1/B2 receptors leading to lower BP via several potential mechanisms; recent evidence suggests less effective in preventing strokes than other drugs
Propranolol/Inderal Pharmacokinetcs
- route
- F
- onset
- duration
- how often given / day
- how cleared/metabolized
availabel po or iv variable F onset 1-2 hrs duration: 12-24h can be given once per day cleared by hepatic metabolism
Propranolol/Inderal Toxicity
-4
excessive hypotension; brady; heart block can worse severe CHF (but indicated for mild/moderate/stable CHF; worsen bronchospasm in severe asthmatics
Propranolol/Inderal Interactions
- additive effects w/ most other anti-hypertensives
- additive AV block with CEBs (calcium entry blockers)
Propranolol/Inderal Special considerations
may be especially useful in HTN patients w/ exertional angina, MI, A fib
watch out for abrupt withdrawal
metoprolol has more data for use in patents s/p MI
Propranolol/Inderal indications and dose/route
for HTN patients
25-100 mg per day in one or two doses
Propranolol/Inderal
Monitoring
BP, HR, exercise tolerance
Labetalol brand name
Trandate
Labetalol/Trandate similar drugs
carvedilol/Coreg (brand name)
Labetalol class cost
$4 (carvedilol) to $24 per month
Labetalol/Trandate drug class
- pharm
- therapeutic
mixed a/b blocker
therapeutic- antihypertensive, treatment of stable CHF (corey)
Labetalol/Trandate Pharmacodynamics
reduce BP by blocking b/a receptors and thereby lowering BP by several different mechanisms; patents differ in degree of beta and alpha blockade
Labetalol/Trandate Pharmacokinetics
- absorption
- F
- onset
- metabolism: where/which enzyme
-excellent absorption but high first pass effect leading to F~25%
onset 1-2 hours after po
2-5 minutes when given IV
- extensively metabolized by liver 2D6
Labetalol/Trandate Toxicity
- avoid in ( 5)
- cautious use (3)
avoid in patients with brady, heart block, cHF, asthma, shock -use cautiously in patients with cardiomyopathy, pheochromocytoma, or pregnancy class D
Labetalol/Trandate Interactions
additive effect with most antihypertensives
Labetalol/Trandate Special considerations
- liver fxn
- most troubling side effect
- most often used in which situation
- use reduced doses w/ reduced liver fxn
- dizziness is most troubling side effect
- most often used for HTN crisis
Labetalol/Trandate Indications and dose/route
- most common
- chronic treatment
most commonly given IV with small initial boluses of 20 mg, followed by continuous infusion at 2 mg/min
not usually given po for chronic treatment
80 mg thrice daily, or 240 mg SR (sustained release) once daily
Labetalol/Trandate Monitor (2)
BP, HR