Term
|
Definition
|
|
Term
| what kind of drug is epi? |
|
Definition
|
|
Term
| what kind of drug is dopamine? |
|
Definition
| dopamine receptor, B agonist |
|
|
Term
| what kind of drug is tyramine? |
|
Definition
| indirectly acting sympathomimetic |
|
|
Term
| what kind of drug is ephedrine? |
|
Definition
| directly and indirectly acting sympathomimetic |
|
|
Term
| what kind of drug is amphetamine? |
|
Definition
| indirectly acting sympathomimetic |
|
|
Term
| what kind of drug is phenylephrine? |
|
Definition
|
|
Term
| what kind of drug is clonidine? |
|
Definition
|
|
Term
| what kind of drug is isoproterenol? |
|
Definition
|
|
Term
| what kind of drug is dobutamine? |
|
Definition
|
|
Term
| what kind of drug is metaproterenol? |
|
Definition
|
|
Term
| what kind of drug is albuterol? |
|
Definition
|
|
Term
| what kind of drug is terbutaline? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| what drug is used when have a stuffy nose to clear airway? |
|
Definition
| phenylephrine (a1 agonist) |
|
|
Term
| what is a drug that can be used in the ICU to increase peripheral resistance without increasing CO? |
|
Definition
| phenylephrine (a1 agonist) |
|
|
Term
| prototype drug for a2 receptor |
|
Definition
|
|
Term
|
Definition
at the neuroeffector junction - on the nerve terminus itself
feeds back and binds a2 receptor of the neuron releasing NE and inhibits release of more NE
feedback regulator of NE release |
|
|
Term
| prototype drug for B1 receptor |
|
Definition
|
|
Term
| prototype drug for B2 receptor |
|
Definition
|
|
Term
| what are the 3 ways adrenergic agonists can have an effect? |
|
Definition
1. act directly on adrenergic receptors
2. act by promoting release of endogenous NE
3. mixed actions |
|
|
Term
| actions of a1 receptor agonists |
|
Definition
1. vasoconstriction - increases peripheral resistance and BP
2. venoconstriction - decreases capacitance and increases venous pressure and right heart filling pressure
3. contraction of the iris radial (dilator) muscle - induces myddriasis
4. constriction of bladder and intestine sphincters |
|
|
Term
| arteriole effect of a1 receptor agonists |
|
Definition
vasocontriction
increases peripheral resistance and BP |
|
|
Term
| venous effect of a1 receptor agonists |
|
Definition
venoconstriction
decreases capacitance
increases venous pressure and right heart filling pressure |
|
|
Term
| effect of a1 receptor agonists in the eye |
|
Definition
contraction of the iris radial (dilator) muscle
induces mydriasis |
|
|
Term
| effect of a1 receptor agonists on bladder and intestine |
|
Definition
| contraction of sphincters |
|
|
Term
| actions of a2 receptor agonists |
|
Definition
| inhibition of neuronal NE release - decrease BP |
|
|
Term
| prototype a2 receptor agonist |
|
Definition
clonidine
developed to be an anti-HTN drug - decrease BP by inhibiting neuronal release of NE |
|
|
Term
| prototype a1 receptor agonist |
|
Definition
|
|
Term
| effect of phenylephrine infusion? |
|
Definition
BP increase
BV are related to heart via baroreceptors
constrict vessels --> decrease CO --> decrease HR and SV via baroreceptors
reversible |
|
|
Term
| normal response to getting up from laying down (getting up in the morning)? |
|
Definition
BP drops initially - a1 receptors cause constriction to stop from crashing
need more blood - HR and contractility increase - vasoconstrict |
|
|
Term
| side effects of a1 blockage |
|
Definition
orthostatic HTN and syncope - block normal phys that allows for vasoconstriction
problem elderly woman on a1 receptor blocker for HTN - can fall and break a hip |
|
|
Term
| a1 receptor mediates ____ in BV |
|
Definition
|
|
Term
|
Definition
don't constrict - stiffen and decrease compliance
causes - blood to be increased back to the heart and increase right heart filling pressure and thus pre-load |
|
|
Term
| actions of B1 receptor agonists |
|
Definition
1. increased cardiac contractility and HR
2. increased lipolysis
3. production of renin from the kidneys |
|
|
Term
| effects of B1 receptor agonist on heart |
|
Definition
| increased contractility and HR |
|
|
Term
| effects of B1 receptor agonist on peripheral fat |
|
Definition
|
|
Term
| effects of B1 receptor agonist on renin production |
|
Definition
increased renin production from kidneys
kidneys are singly innervated by the arterioles that lead to them |
|
|
Term
| action of B2 receptor agonists |
|
Definition
1. relaxation of vascular SM; vasodilation results in decreased peripheral vascular resistance and BP
2. reflexive tachycardia with B2 agonist infusion
3. bronchodilation
4. uterine SM relaxation
5. gluconeogenesis and glycogenolysis in the liver |
|
|
Term
| effects of B2 receptor agonist on vasculature |
|
Definition
relaxation of vascular SM - vasodilation
results in decreased peripheral vascular resistance and BP |
|
|
Term
| effects of B2 receptor agonist on heart |
|
Definition
|
|
Term
| effects of B2 receptor agonist on lungs |
|
Definition
|
|
Term
| effects of B2 receptor agonist on uterus |
|
Definition
|
|
Term
| effects of B2 receptor agonist on liver |
|
Definition
| gluconeogenesis and glycogenolysis |
|
|
Term
| most B1 receptors are located on |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
preload
contractility
afterload |
|
|
Term
| effects of infusing B1 agonist? |
|
Definition
increase HR
increase contractility (force of contraction)
afterload - NOT increased with selective B1 agonist
preload - not increased directly by B1; determined by veins |
|
|
Term
| effect on afterload with selective B1 agonist? |
|
Definition
|
|
Term
| why does preload increase with B1 receptor agonists? |
|
Definition
not directly
determined by veins |
|
|
Term
|
Definition
airway
skeletal muscle BV
BV going to liver
NOT in central BV |
|
|
Term
| which BV do not contain B2 receptors? |
|
Definition
|
|
Term
| effect on HR with infusion of a1 receptor agonist? |
|
Definition
|
|
Term
| effect on HR with infusion of B2 receptor agonist? |
|
Definition
|
|
Term
| NE is an agonist to which receptors? |
|
Definition
| a1, a2, B2 adrenergic receptors |
|
|
Term
| effect of NE in renal BV? |
|
Definition
induces profound constriction of renal BV
dangerously reduces renal blood flow
problem in patient with low GFR |
|
|
Term
| is NE effective in oral admin? |
|
Definition
|
|
Term
| why is NE not effective when administered orally? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| epi is an agonist to which receptors? |
|
Definition
|
|
Term
| what receptor mediates bronchodilator effect of epi? |
|
Definition
|
|
Term
| what complicates the B2 bronchodilator effect of epi? |
|
Definition
cardiac stimulation - B1
and
elevations in systolic BP - a1 |
|
|
Term
|
Definition
emergency management of anaphylactic shock - characterized by severe bronchial constriction and CV collapse
included as a vasoconstrictor agent in most local anesthetic (procaine-like) preparations |
|
|
Term
| why is epi included in most local anesthetic preparations? |
|
Definition
as a vasoconstrictor agent
to limit diffusion of local anesthetic |
|
|
Term
| side effects of epi used parenterally in high doses? |
|
Definition
| can produce cardiac arrhythmia |
|
|
Term
| when can epi produce cardiac arrythmias? |
|
Definition
| when used parenterally in high doses |
|
|
Term
|
Definition
by parenteral injection - as cardiac stimulant in emergencies
inhalation or injection - as bronchodilator |
|
|
Term
| which receptor does NE not target physiologically? |
|
Definition
B2
epi does - accounts for difference in CV response between the two |
|
|
Term
| which binds a2 with higher affinity: epi or NE? |
|
Definition
|
|
Term
| what is the physiologically more important location of a2 receptors? |
|
Definition
|
|
Term
| what is the physiologically most important ligand for a2 receptors? why? |
|
Definition
NE
epi is not released at the neuroeffector junction which is the physiologically most important location of a2 receptors
epi can bind a2 - not its primary role |
|
|
Term
|
Definition
| prototype a1 selective agonist |
|
|
Term
|
Definition
applied topically to the nasal mucosa - induces vasoconstriction to improve air flow
works well for stuffy noses and common cold |
|
|
Term
| phenylephrine systemic use |
|
Definition
| increase BP - induces a vagally-mediated reflex of slowing the heart in patients with paroxysmal tachycardia |
|
|
Term
| clonidine and a-methyl-dopa type |
|
Definition
| agonist at presynaptic a2 adrenergic receptors |
|
|
Term
| a-methyl-dopa is converted to ____ and stored in ____ |
|
Definition
a-methylnorepinephrine
sympathetic nerve terminals |
|
|
Term
| what is the classic non-selective B adrenergic agonist? |
|
Definition
|
|
Term
|
Definition
| agonist of B1 and B2 adrenergic receptors |
|
|
Term
|
Definition
| by inhalation as a bronchial dilator |
|
|
Term
| isoproterenol side effects |
|
Definition
| induces tachycardia more frequently than B2 selective agonists (lacks specificity) |
|
|
Term
| dobutamine tends to have ____ action on the _____ than dopamine |
|
Definition
|
|
Term
|
Definition
| agonist for B-adrenergic receptors |
|
|
Term
|
Definition
| used to stimulate the heart in cardiogenic shock |
|
|
Term
| metaproterenol, albuterol, terbutaline, and salmeterol type |
|
Definition
| selective agonist for B2 adrenergic receptors |
|
|
Term
| metaproterenol, albuterol, terbutaline, and salmeterol use |
|
Definition
| used for bronchodilation in management of reversible airway diseases (asthma, COPD) |
|
|
Term
| metaproterenol, albuterol, terbutaline, and salmeterol delivery |
|
Definition
| by inhalers - deliver meds to airway and avoid confounding effects |
|
|
Term
| who typically gets metaproterenol, albuterol, terbutaline, and salmeterol toxicity |
|
Definition
| patients with dyspnea and anxiety about not being able to breath - often take too much of the drugs |
|
|
Term
| effects of taking too much metaproterenol, albuterol, terbutaline, and salmeterol |
|
Definition
| drives Na/K ATPase - can cause hypokalemia and problems that go along with it |
|
|
Term
| effects of dompamine at moderate doses? |
|
Definition
agonist of D1 dopaminergic receptors
relaxes SM in renal BV and improves renal blood flow |
|
|
Term
| effects of dopamine at high doses |
|
Definition
agonist of cardiac B1 (and B2) receptors
increases cardiac contractility |
|
|
Term
| effects of dopamine at VERY high doses |
|
Definition
becomes an agonist of a1 adrenergic receptors
produce vasoconstriction and raise BP |
|
|
Term
|
Definition
| short - rapid inactivation by hepatic MAO and COMT |
|
|
Term
|
Definition
rapid
by hepatic MAO and COMT |
|
|
Term
|
Definition
found in many plants
used in China for >200 years
introduced in West medicine in 1924 as the first orally active sympathomimetic |
|
|
Term
|
Definition
| non-catechol phenylisopropylamine |
|
|
Term
|
Definition
|
|
Term
|
Definition
| direct a1 and B2 adrenergic activity |
|
|
Term
| ephedrine indirect action |
|
Definition
| mainly - indirectly to promote release of endogenous NE |
|
|
Term
| how does ephedrine mostly act? |
|
Definition
indirectly
promote release of endogenous NE |
|
|
Term
|
Definition
|
|
Term
|
Definition
principal use - decongestant
also recommended for stress incontinence in women |
|
|
Term
| what drug would cause slight decrease in HR, increase in systolic, diastolic, and mean BP, and a large increase in peripheral resistance? |
|
Definition
| NE - get reflexive bradycardia from peripheral vasoconstriction despite B1 activation (from baroreceptor reflex) could be phenylephrine - same BP response (maybe larger); HR reduced more because no B1 action |
|
|
Term
| what drug would cause slight increase in HR, increase in systolic BP, decrease in diastolic BP, very minimal increase in mean BP, and a slight decrease in peripheral resistance? |
|
Definition
epi - acts on B2
eliminates rise in BP seen with NE
don't get reflexive bradycardia seen with NE
binds B1 - increases HR
B2 actions on BV - primarily in liver and skeletal muscle |
|
|
Term
| what drug would cause significant increase in HR, slight increase in systolic BP, decrease in diastolic BP, slight decrease in mean BP, and a large decrease in peripheral resistance? |
|
Definition
isoproterenol - B1 and B2 only; no a
big increase in HR
no vascoconstrictor response
enormous change in peripheral resistance |
|
|
Term
| peripheral resistance is the relationship between? |
|
Definition
|
|
Term
| pressure from inflow (aortic flow) - resistance to pressure (outflow) = |
|
Definition
|
|
Term
|
Definition
|
|
Term
| what is tocolytic therapy? |
|
Definition
use of B adrenergic agents to attenuate premature labor, delay delivery, allow fetal maturation
thereby - reducing neonatal morbidity and mortality |
|
|
Term
| what is a common side effect of B-adrenergic tocolytic therapy for treatment of preterm labor? |
|
Definition
|
|
Term
| what drug is often used for tocolytic therapy? |
|
Definition
| terbutaline (B-adrenergic agonist) |
|
|
Term
| how do B-adrenergic agonists control serum K? |
|
Definition
| activate Na/K ATPase by increasing cAMP - take K out of blood and store in cell --> hypokalemia |
|
|
Term
| what can happen with abrupt withdrawal of a B adrenergic agonist? |
|
Definition
| can get rebound hyperkalemia |
|
|
Term
| what are the major side effects of B agonists? |
|
Definition
cardiac arrhythmias
hypokalemia
can precipitate angina
insomnia
anxiety
tremor |
|
|
Term
| what are the major side effects of a agonists? |
|
Definition
headache
**reflexive bradycardia
excitability
restlessness
can precipitate angina |
|
|
Term
|
Definition
| direct and indirect agonist |
|
|
Term
|
Definition
| indirect acting sympathomimetics |
|
|
Term
|
Definition
| normal byproduct of tyrosine metabolism |
|
|
Term
| where is tyramine found in high concentrations? |
|
Definition
|
|
Term
|
Definition
| enters NE nerve terminal via the amine transporter and causes NE release |
|
|
Term
| tyramine in converted to ____ by ______ |
|
Definition
octopamine
dopamine-B-hydroxylase |
|
|
Term
|
Definition
| readily metabolized by MAO |
|
|
Term
| in what patients are the effects of tyramine intensified? |
|
Definition
| patients treated with MAO inhibitors |
|
|
Term
| how does drug tolerance to tyramine develop? |
|
Definition
| develops as NE is completely replaced by octopamine |
|
|
Term
|
Definition
| indirect acting sympathomimetic |
|
|
Term
|
Definition
|
|
Term
| do amphetamines have direct effect on adrenergic receptors? |
|
Definition
|
|
Term
| effect of amphetamines on CNS? |
|
Definition
|
|
Term
|
Definition
| indirect acting sympathomimetic |
|
|
Term
|
Definition
blocks neuronal uptake1 pathway for NE
extends half life of NE at synaptic cleft |
|
|
Term
| what is important to know about cocaine toxicity? |
|
Definition
negative impact can be played out over 72-98 hours after ingested
toxicity is potentially several days after use because of long half life |
|
|
