Shared Flashcard Set

Details

Pharmacology Exam 2: adrenergic agonists
adrenergic agonists
102
Anatomy
Graduate
02/01/2011

Additional Anatomy Flashcards

 


 

Cards

Term
Sympathetic agonists are also called ____ or ___ ___.
Definition
- sympathomimetics
- adrenergic agonists
Term
various classifications of adrenergic agonists:
Definition
- catecholamine vs. non-catecholamine
- direct vs. indirect acting
- re-uptake inhibitors
Term
you cannot take catecholamines orally.
Definition
Term
Non-catecholamine adrenergic agonists are ___ lasting and __ be taken by mouth.
Definition
longer
can
Term
non-catecholamine alpha agonist:
Definition
phenylephrine
Term
Beta 2 agonists:
Definition
- Albuterol
- Ritodrine
- Terbutaline

beta 2 agonists = art
Term
Indirect acting sympathomimetics:
Definition
- Amphetamines
- Tyramine
Term
mixed acting sympathomimetics:
Definition
- ephedrine
- pseudoephedrine
Term
Topical vasoconstrictors:
Definition
- Naphazoline
- Oxymetazoline
- Tetrahydrozaline

topical vasoconstrictors= NOT
these are your nasal sprays
Term
NE reuptake blockers:
Definition
- cocaine
- impipramine
Term
epinephrine stimulates ___ alpha and beta receptors.
Definition
all
Term
Isoproterenol acts like a catecholamine is an agonist for __ _, _, and _ receptors.
Definition
- beta 1,2, and 3
Term
Dopamine acts on what receptors:
Definition
alpha 1
beta 1
dopamine
Term
Dobutamine acts like a catecholamine and is only an agonist for the ___ ___ receptors.
Definition
beta 1
Term
amphetamines and tyramine can cause ___ release.
Definition
NE
Term
the prototypic catecholamine is :
Definition
epinephrine
Term
the prototypic noncatecholamine agonist is:
Definition
phenylephrine
Term
prototypic beta 2 agonist is :
Definition
Albuterol
Term
Prototypic indirect acting agonist:
Definition
tyramine
Term
OTC indirect agonist:
Definition
pseudoephedrine
Term
Oxymetazoline reuptake inhibitor:
Definition
cocaine
Term
a direct mode of action means it acts on a ___.
Definition
receptor
Term
An indirect mode of action means that it causes the release of ___ from nerve terminals.
Definition
NE
Term
Mixed action drugs have both ___ and ___ effects.
Definition
direct and indirect
Term
Alpha adrenergic effects:
Definition
1. constriction of blood vessels via alpha 1 (to lesser extend alpha 2)
2. mydriasis via alpha 1
3. contraction of the spleen via alpha 1
4. contraction of the uterus via alpha1
5. inhibited release of insulin via alpha2
6.constriction of bladder sphincter alpha 1
7. Increased glycogenolysis in liver beta2
8. ejaculation, vas deferens alpha 1
9. relaxation of intestinal smooth muscle alpha 2
Term
Beta adrenergic effects:
Definition
1. Heart: positive ionotropic and chronotropic effects beta 1
2. relaxation of bronchioles beta2
3. relaxation of uterus beta 2
4. relaxation of skeletal muscle arterioles beta 2
5. increased liver glycogenolysis, beta2
6. increased adipose tissue lipolysis beta3
7.increased releasae of insulin beta2
8.stimulate release of renin beta1
Term
list the catecholamines:
Definition
- epinephrine
- norepinephrine
- dopamine
- dobutamine
- isoproterenol
Term
Epinephrine is more potent for __ than __ receptors. But clinically, when given at therapeutic doses we see ___ are affected. The concept of __ __ requires knowledge of which receptor response will prevail.
Definition
- beta than alpha
- both
- net effect
Term
epinephrine effects on the heart:
Definition
Via beta 1 receptors:
- positive inotropic effect (contractility)
- positive chronotropic effect (rate)
- increased automaticity (sa node depolarizes more quickly): latent pacemakers become active= increased ectropic beats, arrhythmias may result b/c refractory period is reduced after an ap
- increased conduction rate in the AV node
Term
ultimately epinephrine causes the ___ __ to __ and the __ of ___ to increase, so ___ ___ is ___. Thus ___ consumption ____.
Definition
- heart rate to increase
- force of contraction to increase
- cardiac output is increased
- oxygen consumption is increased
Term
On skeletal muscle arterioles there are ___ _ and ___ __ receptors. At physiological quantities of epinephrine, the ___ receptors are acted on and we see ____. At pharmacologic doses ___ receptors are acted on and we see ____.
Definition
- beta 2 and alpha 1
- physiological> beta 2> vasodilation
- pharmacological> alpha 1> vasoconstriction
Term
Veins have only __ _ receptors so they can only ____ in response to increased sympathetic stimulation.
Definition
- only alpha 1
- constrict
Term
coronary blood vessels ___ in response to epinephrine b/c of ___ _ receptors.
Definition
dilate
beta 2
Term
Kidney, skin, and mucosal blood vessels ___ in response to epineprhine b/c of ___ _ receptors.
Definition
vasoconstrict
alpha 1
Term
cerebral blood vessels remain unchanged in presence of epinephrine
Definition
Term
Net effect of epinephrine on blood pressure and cardiac function depends on:
Definition
- dose
- circulatory status
- compensatory reflexes- baroreceptors are stretch receptors in carotid sinus and aortic arches that sense blood pressure changes and maintain homeostasis
Term
When baroreceptors sense a change in bp, signals are transmitted to the ___ center in the __ ___to alter parasympathetic and sympathetic outflow to the heart and blood vessels.
Definition
- vasomotor
- brain stem
Term
If baroreceptors sense a sudden increase in bp, sympathetic tone will be ___ and ___ tone to the ___ node will be ___.
Definition
- sympathetic tone will decrease
- vagal tone to SA node will increase
Term
If baroreceptors sense a sudden drop in bp, symp tone will ___ and parasymp tone will ___.
Definition
increase
decrease
Term
metabolic effects of epinephrine:
Definition
- calorigenic and tremor effects in skeletal muscle via beta 2
- increased glycogenolysis (beta 2)
- increased lipolysis (beta 3)
Term
Clinical uses of epinephrine:
Definition
1. Bronchial asthma
2. Anaphylactic shock
3. Infiltration with local anesthetics
4. Cardiac resuscitation
5. Topical for hemostasis
Term
how does epinephrine treat bronchial asthma:
Definition
. Administered by inhalation. Bronchodilation (2) and inhibition of antigen-induced histamine release.
Term
How does epinephrine treat anaphylactic shock?
Definition
(give IV or SC) Improves breathing by same mechanisms as in 1 above, plus increases blood pressure and reverses edema (1).
Term
epinephrine reverses edema by __ _ receptors
Definition
alpha 1
Term
Anaphylaxis is an ___ phenomenon. Three things occur all related to the dump of histamine. list these 3 things.
Definition
1. Bronchoconstriction
2. profound vasodilation so bp drops
3. edema

Epinephrine (epi pen) is ideal treatment for this. Epinephrine is a physiolgical antagonist b/c it diates brochioles (beta 2 effect), raises bp (alpha 1 affect), and edema comes out of venules so epinephrine stops any additional edema from forming and allows present edema to be rid by lymphatics.
Term
Lidacane anesthetic injected with epinephrine at dentist, without the epinephrine the lidacaine could be deathly.
Epinephrine constricts the vessels and keeps the lidacaine in the specific area. Epinephrine acts on alpha 1 and beta 2 receptors, but alpha overrides the beta, so as concentration drops beta takes over. So initial constriction with alpha but then after get dilation with beta 2 receptors.
Definition
Term
Adverse effects of epinephrine:
Definition
1. arrhythmias (beta 1 effects)
2. cerebral hemorrhage (alpha 1 effects)
3. necrosis distal to site of injection
4. CNS effects: anxiety, headache
Term
Contraindications for epinephrine:
Definition
1. Hypertension
2. Shock
3. Hyperthyroidism
4. Angina pectoris
5. Degenerative heart disease

don't have to memorize these, its just used in emergency situations
Term
Contraindications for epinephrine:
Definition
1. Hypertension
2. Shock
3. Hyperthyroidism
4. Angina pectoris
5. Degenerative heart disease

don't have to memorize these, its just used in emergency situations
Term
Norepinephrine or ____ is selective for __ _, __ _, and __ _ receptors. What are its pharmacological effects?
Definition
- Levophed
- alpha 1
- alpha 2
- beta 1
pharmocologic effects:
1. Heart beta 1 direct effects (iontropic and choriontropic effects)
2. Vasculature: alpha 1 > vasoconstriction which activates the baroreceptors
Term
NE has no beta 2 affects so not used for anaphylactic shock. NE is much shorter acting than epinephrine, so not used to control blood pressure.
Definition
Term
Net effect of NE:
Definition
- positive inotropic effects but reflex bradycardia with increased systolic and diastolic blood pressures
Term
E widens the pulse pressure because it stimulates 2 receptor on arterioles, causing vasodilation
Because E at this dose does not raise mean blood pressure, no vagal reflexes are activated
Contrast these effects of those of NE, which essentially has no stimulant 2 effect
Definition
Term
with a low dose of epinephrine you would see the diastolic pressure ___ b/c of __ __ receptors causing ___ ___. You would see the systolic pressure would be ___ b/c of the increased contractility and ejection fraction via ___ _ recptor effects. Thus with epinephrine you see a ___ pulse pressure but has __ effect on mean blood pressure.
Definition
- decreasing
- beta 2
- arteriole dilation
- increasing
- beta 1
- widened pulse pressure
- no change in mean arterial pressure
Term
Isoproterenol has pure ___ effects so it would ___ diastolic pressure even more than epi did, and it would increase contractility even more than epi did so systolic is more increased. So ultimately mean bp ___ a little bit and ___ __ is increased.
Definition
- beta
- decrease
- decrease
- heart rate
Term
w/o parasympathetic input the heart rate would be around:
Definition
90bpm
Term
NE increases pulse pressure via the ___ _ receptor b/c diastolic did not decrease b/c NE does not have ___ action, so you see ___ _ effect of ___. This increased bp is sensed by the barorecptors which in turn causes heart rate to ____. So NE is telling the heart to beat faster but the vagus is telling it so slow down, and when they both are having input, we know the ___ is more powerful.
Definition
alpha 1
beta 2
alpha 1 effect of vasoconstriction
decrease
parasympathetics
Term
inject NE hos is pulse rate, blood pressure, and peripheral resistance affected?
Definition
- peripheral resistance increases
- blood pressure increases
- pulse rate decreases
Term
inject epi, how is peripheral resistance, blood pressure, and heart rate affected?
Definition
- peripheral resistance decreases (at low doses)
- blood pressure stays same
- heart rate increases
Term
inject isoproterenol how is peripherial resistance, blood pressure, and heart rate affected?
Definition
- peripheral resistance decreases
- blood pressure decreases a little
- heart rate increases
Term
LOW DOSES OF EPINEPHRINE> FILL BETA 2 RECEPTORS (DECREASED BP), HIGH DOSES FILL ALPHA RECEPTORS (INCREASED BP)
Definition
Term
Isoproterenol (Isuprel)
Definition
1 and 2 stimulant. (no alpha effects).
Pharmacological effects:
1. Heart: Positive inotropic and chronotropic effect.
2. Vasculature: Vasodilatation of skeletal muscle arterioles (2 receptors on arterioles).
Term
Isoproterenol: Clinical Uses
Definition
Relatively limited because of intense cardiac effects.
1. Bronchial asthma (Aerosol)
2. Heart block. (give by IV. catheter.)
Side effects
Common: tachycardia, flushing, headache, rapid pounding heart.
Serious: arrhythmias, angina
Term
notice that isoproterenol, a pure beta1/beta2 agonist, has a greater ____ effect than E. This is because E is both a beta2 agonist and also an alpha 1 agonist. For E, The alpha 1 effects partly offset the beta2 effects at this dose. Indeed, if the dose of E is raised, only alpha1 agonist effects will be seen because E has more efficacy at alpha1 than beta2 receptors.
Definition
- vasodilation
Term
Epi is more potent for __ _ receptors but more efficacious at __ _ receptors.
Definition
- more potent at beta 2s
- more efficacious at alpha 1s
Term
Dopamine aka ___ is an agonist at __ receptors and cause ___ in the kidneys. This is also a ___ _ agonist which leads to ___ ___ __. It is also an __ _ agonist which can lead to ___ (less potent here than others though).
Definition
- Intropin
- D1
- vasodilation
- beta 1
- increased cardiac output
- alpha 1
- vasoconstriction
Term
Intropin is :
Definition
dopamine
Term
Levophed is :
Definition
norepinephrine
Term
adrenalline is:
Definition
epinephrine
Term
dopamine is a precursor to ___ in all ___ neurons.
Definition
norepinephrine
norepinephrine
Term
Shock basically means you have inadequate ___ __, the cardinal sign of shock is ___ ___ __.
Definition
inadequate cardiac output
low blood pressure
Term
If we lose a lot of blood, flow to many organs will stop except for these three:
Definition
- heart
- brain
- kidney

of these 3, the kidneys give up blood flow first
Term
With shock, the sympathetic is so activated that blood is not getting to the kidneys.
Definition
Term
main use for dopamine:
Definition
- shock, especially hypovolemic shock
- beta 1 effects benefit cardiac output
- alpha 1 effects increase blood pressure
- D1 effects vasodilate the kidney arterioles, leading to better maintenance of blood flow
Term
Duration of catecholamines is not very long, it has to be given via IV infusion or it will me metabolized very quickly.
Definition
Term
Direct acting non-catecholamines are ___ ___, lacking the ___ moeity. They are analogues for NE and Epi.
Definition
synthetic agents
catechol
Term
Non-catecholamines are longer acting and are metabolized more slowly, why?
Definition
- they are not acted upon as readily by MAO as catecholamines are
- they are not stored in vesicles
Term
some direct acting non-catecholamines are effective p.o.
Definition
Term
An alpha adrenergic agonist is ___ aka _____. It acts on the __ _ receptors and causes ___ and __ ___ __. But you can expect ___ ___.
Definition
- Phenylephrine aka Neosynephrine
- alpha 1
- vasconstriction
- increased blood pressure
- reflex bradycardia
Term
___ is used in decongestant cold meds orally and topically.
Definition
Phenylephrine aka Neosynephrine
Term
Phenylephrine uses:
Definition
1. Nasal decongestant
2. Infiltration with local anesthetics (more likely is the use of metaraminol).
3. Pressor agent to maintain bp
4. Ocular examination. Mydriasis without affecting accommodation.
Term
Beta-2 Selective Adrenergic Agonists are __ to __ times more potent at beta 2 than at beta 1, thus they are more selective for ___ muscle over __ muscle. This is longer acting than ____. Tolerance may develop.
Definition
- 5 to 10 so its affinity is 100 times greater
- smooth over cardiac
- longer acting than catecholamines
Term
primary use of beta 2 selective antagonists:
Definition
obstructive lung disease: asthma and COPD
Term
Tolerance develops with beta 2 selective agonists b/c the beta receptor is a __ __ coupled receptor. When these are over activated, they ___ which is a form of ___ ___. this is a problem when asthmatics overuse their inhalers.
Definition
- g-coupled
- internalize
- down regulate
Term
Tolerance develops with beta 2 selective agonists b/c the beta receptor is a __ __ coupled receptor. When these are over activated, they ___ which is a form of ___ ___. this is a problem when asthmatics overuse their inhalers.
Definition
- g-coupled
- internalize
- down regulate
Term
Beta 2 adrenergic agonists used to treat bronchial asthma:
Definition
1. Albuterol (Proventil); Levo-albuterol (Xopinex)
2. Metaproterenol (Metaprel, Alupent)
3. Terbutaline(Brethine)
(aerosol and sc; sc for emergency tx of astma; only 2 agent available sc )
iv.and p.o. to delay delivery.
4. Isoetherine (Bronkosol)
5. Salmeterol (Serevent). Once a day agent for chronic but not acute treatment of asthma. Has slow onset of action

A Manly Tone Is Sexy.
Term
Salmeterol lasts longer and was used for quite some time, but last spring it was in advair inhalers (beta 2 long acting affects and the other was topical corticosteroid to slow down inflammation) but FDA said not good for kids>unexpeced cardiac effects (beta 1 effects).
Definition
Term
beta 2 agonists used to treat bronchial asthma:
Definition
A Manly Tale Is Sexy.

Albuterol
Metaproterenol
Terbutaline
Isotherine
Salmeterol
Term
Albuterol beta 2 agonist should be in __ form for acute treatment and ___ for chronic treatment of bronchial asthma.
Definition
- aerosol
- p.o.
Term
side effects caused by the oral route of albuterol:
Definition
hypotension (beta 2) , muscle tremors (beta 2), tachycardia (beta 1), hypokalemia. Effects on blood glucose are variable.
Term
Ritodrine is a ___ __ __ agonist used to ___ ___.
Definition
alpha 2 adrenergic agonist
delay labor
Term
beta 2 adrenergic agonist side effects:
Definition
- skeletal muscle tremors b/c beta 2 receptors on muscle increase energy productin
Term
Indirect Acting Sympathomimetics:
Definition
Tyramine
Amphetamine
many others
Term
Tyramine has the potential to cause a hypertensive crisis in pts on ___ inhibitors.
Definition
MAO inhibitors
Term
Tyramine is found in many foods (red wine, aged cheeses, peanuts). It normally has huge first pass effect by ___ by the gut and liver that it never enters circulation. But if person on ___, then can cause ___ __.
Definition
- monoamine oxidase
- MAOI
- hypertensive crisis
Term
tyramine is a ___ __. if it gets into nerve terminals it causes release of ___ .
Definition
decarboxylated tyrosine
norepinephrine
Term
Pseudoephedrine:
Definition
Naturally occurring in genus Ephedra
There are four isomers; two of these, ephedrine and psuedoephedrine are clinically effective.
Mechanism: indirect (releases NE).
Relatively insensitive to degradation by MAO and COMT. Effective p.o.
Term
pseudoephedrine used to be used orally as decongestant but much less now.
Definition
Term
clincial uses of pseudoephedrine:
Definition
nasal & eustachian tube decongestant
Releases NE – decongestant because of reduced pooling of blood in the venous circulation
Orally active
Does not penetrate CNS significantly – much less dependence potential than ephedrine. Nonetheless, access is now greatly restricted (easy to synthesize methamphetamine from this starting chemical).
Term
pseudoephedrine works as a nasal decongestant b/c it causes release of ___ which reduces ____ ___ in __ circulation.
Definition
- NE
- reduces blood pooling
- venous
Term
pseudephedrine not used much now, b/c easy to make meth from it.
Definition
Term
common OTC products with direct and indirect alpha 1 effects:
Definition
Naphazoline (Privine)
Tetrahyrolazine (Tyzine, Visine)- reduces eye redness
Xylometrazoline (Otrivin)
Oxymetazoline(Afrin)
Supporting users have an ad free experience!