sympathomimetics and sympatholytics Flashcards
____ is the neurotransmitter that is released at the postganglionic nerve endings of the sympathetic nervous systme.
norepinephrine
Neurons that release norepinephrine are referred to as ____.
adrenergic
Adrenergic receptors where norepinephrine acts are located on _____ and _____ muscle membranes.
cardiac and smooth muscle membranes.
adrenergic drugs can be further broken down into what two classes
Sympathometics (agonists)
Sympatholytic (antagonists)
the adrenergic receptors subdivided into two types which are?
alpha and beta receptors
alpha receptors are subdivided into what?
alpha 1 receptors
Alpha 2 receptors
individual organs generally possess 1 main type of receptor and this allows the utilization of specific drugs that can ______ bind to and stimulate or block the individual adrenergic receptor.
selectively
_________ are adrenergic blocking drugs that antagonize/decrease sympathetic activity
Sympatholytics (agonists for alpha and beta)
________ are adrenergic blocking drugs that antagonize decrease sympathetic activity
Sympatholytics (antagonists for alph and beta)
sympatholytic drugs are also called two other names which are?
antagonists
blockers
sympatholytics = ________
sympathomimetics = _______
antagonists
agonists
the activation of alpha 1 adrenergic receptors stimulate what four systems?
blood vessels
eye
bladder
prostate
Sympathomimetic drugs of the alpha adrenergic class conistst of which 2 drugs
Norepinepherine and Epinephrine
alpha 1 receptor activation causes what signs and symptoms?
vasoconstriction of blood vessels = increased blood pressure and increased contractibility of the heart
pupil dilation
bladder relaxation
contraction of the prostate
what are the disadvantages of norepinepherine administration
must be used Intraveneously/injected and it has a very short duration of action
mydriasis means?
pupil dilation
what is the more important clinical effect that is generated by alpha 1 receptors causing
contraction of smooth muscle
alpha drugs are administered _____(route) in hypotensive states such as after surgery to increase blood pressure and maintain circulation. With the exception for which medication?
intravenously
midodrine (proamatine)
what are the non therapeutic effects of alpha 1 agonists
Contraction of sphincter and GI/GU track
what are the main 2 target organs that alpha 1 act on
cardiovascular and eyes
what alpha adrenergic drugs are used to treat hypotension using.
A LNP
Aramine, Pro Amatine, levophed, neo-synepherine
what type of alpha adrenergic drugs are included in the over the counter cold and allergy preparations for relief of nasal decongestion?
alpha 1 adrenergic agonist
a few of the alpha 1 adrenergic agonist drugs are used in opthalmology for what?
dilate the pupils and ocular decongestant
what is the main effect of the alpha adrenergic drugs used to treat hypotension
increase BP due to vasoconstriction of smooth muscle (A LNP)
alpha 1 adrenergic agonist drug end in what? except for which drug?
“ine”
metarminol (aramine)
what are the major adverse effects of administering alpha adrenergic drugs
excessive vasoconstriction
name the two alpha 1 adrenergic agonist that are used for occular decongestant?
Naphazoline (Naphcon)
Tetrahydrozoline (Visine)
Remember No Tears when putting in eye drops! and that alpha 1 adrenergic agonist end in ine.
Name the alpha adrenergic agonist used fro nasal decongestant?
naphazoline (Privine)
phenylephrine
pseudoephedrine
tetrahydrozoline (Tyzine)
xylometazoline
Alpha adrenergics must be carefully administered to patients with HTN or cardiovascular concerns d/t
increased hemorrage, cardiac arythmias and and cerebral concerns
for patients recieiving alpha adrenergic medications, what need to be frequenly obtained
BP measurements at frequent intervals
The most common side effects from alpha adrenergic medications when used for nasal decongestion include
excessive dryness (d/t vasoconstriction and decreased blood flow)
why can alpha adrenergic medications be administered over the counter
because adminsitration of the drug does not cause as severe of side effects such as death when compared to the IV form
what is the function of alpha adrenergic blocking drugs
the alpha blockers compete with Epi and norepi for the binding to the alpha adrenergic receptors. This prevents norepi and epi from producing an Alpha SYMPATHETIC response
what is the main pharmacological effect that alpha blockers produce
relaxation of smooth muscles
In BPH patients, there is an enlargement of the prostate gland, which interferes with urine flow through the urethra. Alpha blocking drugs help with BPH how?
relax the smooth muscle of the urethra, which improves urinary flow
causes prostate to constrict as well
for pateints with pheochromocytoma, the treatment of which drug can lower and control BP until the tumor is removed
Phenoxybenzamine
what are the drug names for the class of alpha adrenergic “blocking”
“SIN”
Alfuzosin, Doxazosin, Prazosin, Silodosin, Tamsulosin, Terazosin
Phenoxybenzamine (remember this is used for pheochromocytoma)
What is the name of the medication that helps control blood pressure for pheochromocytomas until surgery, what class do they below to? What is the route of administration?
Phenoxybenzamine (Dibenzyline)
Alpha-Adrenergic Blocking Drugs
PO
what are the three drugs used to spetreat BPH with alpha adrenergic drugs
“TSA”
- Tamsulosin (FLOmax)
- Silodosin (RamoFLOW)
- Alfuzosin (UROatral)
blocking one division of the autonomic nervous system usually produces some effects that are similar to stimulating what?
give an example
the other division of the autonomic nervous system
so if you give an alpha blockade, the side effects are simular to an increase in parasympathetic activity in the organs that are blocked.
what is the function of Beta 1 adrenergic receptors
increase HR and force of contraction
The side effects for alpha 1 blockers are?
constriction of pupils
nasal congestion
increase in gastrointestinal activity
increased salivation
bladder contraction
blood vessels dilate
heart rate decrease
lungs- bronchioles constrict and increase in secretions.
Remember these are the same a parasympathetic stimulation
Describe the organs and effects that beta 1 receptors have
HEART and KIDNEY
Heart: increase contractility and HR
Kidney: increase Renin secretion, angiotensin, increase BP
Describe the organs and effects that beta 2 receptors have on the body
SMOOTH MUSCLE, Lungs, Uterus, Liver
Smooth muscle: Gastrointestinal track (decrease GI motility)
Lungs: Bronchodialation
Uterus: relaxation of urerine smooth muscle
Liver: increase blood sugar
what medications are just with Beta 2 receptor agonists
I-SMART
- I: Isoetharine
- S: salmeterol
- M: metaproterenol
- A: Albuterol
- R: NONE
- T: Terbutaline
Beta 2 receptors are important in OB cases why?
because beta 2 receptors are found in the uterine smooth muscle stimulation of the beta 2 receptors within the uterus relaxes the smooth muscle and inhibits urterine contractions which can occur during premature labor
list the beta adrenergic drugs that also stimulate alpha?
dopamine
ephedrine
epinephrine
what are the beta1 drugs
“IDE”
- Isoproterenol
- Dopamine & Dobutamine
- Epinepherine & Ephederine
What receptors does the beta adrenergic drug Isoproterenol work on
Beta 1 & Beta 2
what is the main use for Dopamine and Dobutamine
circulatory shock and acute heart failure
out of the beta 2 agonist what medications can also be give other ways than aersolized? and how?
albuterol- aerolsol inhalant, tablets, syrups
terbutaline -IV, tablets
what is one main disadvantage of using Isoproternol
it has a dual action causing both dialation and increase contraction of heart leading to overstimulation of the heart
list the administration routes for epinephrine?
IV (acute anaphlyaxis profound hypotension and bradycardia)
SC (around a central line insertion site that is bleed)
IM (epipen anaphlyaxis)
Aerosol inhalant (rescue for asthma attack bronchodilator)
what is the use for terabutaline
arrest premature labor
Dopamine functions as a neurotransmiter in the brain forming a precursor for _____
norepinepherine
list the administration routes for ephedrine and the main use for it?
route: capsules and parenteral
use: bronchodilator
out of dopamine or dobutamine, which drug produces a greater beta 1 effect
dobutamine (treats acute HF)
(pumps the heart more compared to dopamine which has alpha and beta efffects used to circulatory shock)
list the uses for terbutaline? list the route of administration?
bronchodilator/preterm labor
systemic route (tablet or IV)
list the indication for dobutamine and the route?
acute heart failure, IV infusion
list the indication for dopamine and route?
circulatory shock, IV infusion
list the indicaition for isoproternol and route?
cardiac stimulant
IV injection not INFUSION
Beta drugs may produce ______ nervous system stimulation, causing what three symptoms.
central nervous system stimulation
restlessness
tremors
anxiety
the main adverse effect of epinephrine is?
overstimulation of the heart causing palpitations or cardiac arrhythmias
use extreme caution given epinephrine in what patient population?
patients with existing heart disease
The use of beta 2 drugs to arrest preterm labor can cause a variety of _______ effects and complications.
cardiovascular
because the use of beta 2 drugs to stop preterm labor can cause cardiovascular complications, what should be implemented?
fetal heart rate and maternal pulse rate and blood pressures should be monitored in patients that have to be administered beta 2 drugs for the cause of preterm labor
Beta blocking drugs bind to _______ adrenergic receptors and antagonize the effects of ______ and _____.
beta
epinephrine and norepinephrine
what is the most important beta organ?
heart
the main effect of beta blockers on the heart is to?
Decrease the activity of the heart
Blockade of beta 1 receptors produces affects the heart how?
decrease in heart rate and force of contraction and slows impulse conduction
Beta 1 blocker effects are useful in patients with what conditions?
tachycardia
cardiac arrhythmias
cardiac conditions were excessive sympathetic activity is present
decreasing cardiac function by beta blocker administration can also _____ blood pressure
decrease, beta blockers are commonly used in the treatment of hypertension
is there any specific therapeutic indications for blocking the beta 2 receptors?
no
beta blockers are divided into two groups which are?
nonselective beta blockers
selective beta blockers
Nonselective beta blockers affect which receptors?
beta 1 and beta 2
selective beta blockers affect which receptor?
beta 1 receptors
however at higher doses the selective beta blockers may do what?
begin to block beta 2 receptors in addition to beta 1 receptors.
remember we talked about affinity, they have a much lower affinity for beta 2 receptors, but if there is saturation of beta 1 receptors then they have no other choice and they will start to interact with beta 2 receptors and produce side effects.
how does beta blockers treat migraine?
____ was the first beta blocker used clinically,it blocks both beta 1 and beta 2 receptors.
propranolol
Propranolol and other beta blockers are used in the treatment of what three general conditions?
angina pectoris
hypertension
various cardiac arrhythmias
chronic heart failure
how does beta blockers help gluacoma?
decrease intraocular pressure
How does beta blockers help chronic heart failure?
decreases excessive sympathetic activity and slows the heart rate and appears to decrease the risk of sudden death
name the nonselective beta blockers?
just know O-Z and end in olol
plus nadolol and carvedilol because they have NC not a clue to be cardioselective
name the cardioselective beta blockers?
A-N and end in olol
except for Nadolol and carvedilol because they NC not a clue to be cardioselective.
Common side effects that can occur from administration of beta blockers?
nausea
diarrhea
Serious: reduced heart rate
in general nonselective beta blockers should not be used in which patient population and why?
asthma or other respiratory conditions, because blocking beta 2 receptor sites, nonselective beta blockers may cause bronchoconstriction in individuals with asthma or other respiratory conditions.
So what type of beta blocker should be prescribed to asthma patient and patient with respiratory conditions? special consideration?
cardioselective beta blockers
At higher doses of cardioselective beta blockers theycan also interact with the beta 2 receptors and potentially cause bronchoconstriction.So make sure you stay in the lower range of therapeutic window with cardioselective beta blockers for asthma/respiratory patients.
beta blockers can cause central nervous system effects such as?
drowsiness
mental depression
and other CNS distrubances
alpha adrenergic agonist drug site of action?
alpha 1 receptor
alpha adrenergic drugs agonist main effect?
smooth muscle contraction, vasoconstriction
nonselective beta adrenergic agonist site of action is?
beta 1 and beta 2 receptors
nonselective beta adrenergic agonist main effect?
cardiac stimulation
smooth muscle relaxation
bronchodilation
selective beta 2 adrenergic agonist site of action ?
beta 2 receptors
selective beta 2 adrenegic agonist main effect?
smooth muscle relaxation
bronchodilation
alpha 1 adrenergic blockers site of action?
alpha 1 receptor
alpha 1 adrenergic blocker main effect?
smooth muscle relaxation
vasodilation
nonselective beta 1 and beta 2 adrenergic blockers site of action?
beta 1 and beta 2 receptors
nonselective beta 1 and 2 adrenergic blockers main effect?
cardiac depression
smooth muscle contraction (beta 2 organs)
selective beta 1 adrenergic blockers site of action?
beta 1 receptors
selective beta 1 adrenergic blocker main effect?
cardiac depression (decrease HR/force of contraction)
what are adrenergic drugs that simulate or mimick the sympathetic nervous system?
sympathomimetics