Term
8 yo boy
office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer
treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely
exam - normal except lungs (expiratory wheezing)
diagnosis? |
|
Definition
asthma
diagnose with pulmonary function test - decrease FEV1 that is responsive to bronchodilators
symptoms - typically worse at night |
|
|
Term
8 yo boy
office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer
treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely
exam - normal except lungs (expiratory wheezing)
what do you prescribe? |
|
Definition
**albuterol inhaler
or tiotropium - muscarinic antagonist |
|
|
Term
8 yo boy
office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer
treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely
exam - normal except lungs (expiratory wheezing)
what is the mechanism of action of albuterol? |
|
Definition
B2 receptor agonist
B2 --> Gs --> increased cAMP --> dilation of SM |
|
|
Term
8 yo boy office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely exam - normal except lungs (expiratory wheezing)
what are the effects of albuterol in this type of patient? |
|
Definition
| relaxes bronchial SM inhibits mediator release from mast ecll stimulates mucociliary clearance pathophys of asthma is complex - not just contraction; also inflammation, remodeling, and angiogenesis |
|
|
Term
8 yo boy
office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer
treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely
exam - normal except lungs (expiratory wheezing)
what are the most common side effects of albuterol? |
|
Definition
tolerance - asthmatics with remodeled bronchioles
high CO
high BP - activating B1
*skeletal muscle tremor
*tachycardia
*cough |
|
|
Term
8 yo boy
office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer
treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely
exam - normal except lungs (expiratory wheezing)
what doesn't albuterol have a lot of effect on the heart? |
|
Definition
heart is B1 - shouldn't get high concentrations there is drug is inhaled
not completely specific - some action on heart |
|
|
Term
8 yo boy
office - chronic cough; frequent throughout day; symptoms 2-3 nights/month; off and on for a year; worse in spring and fall; worse when riding bike or playing soccer
treated twice in past year - antibiotics and cough suppressants; doesn't clear up completely
exam - normal except lungs (expiratory wheezing)
what meds can be used to provide long-term control of asthma symptoms? |
|
Definition
combined therapy - inhaled steroids + long acting B2 agonist
advair, tiotropium
chromolyn - membrane stabilizing actions; K channel blocker; some efficacy
2nd line - oral theophylline, leukotriene inhibitors, or systemic steroids |
|
|
Term
| what drug would be best for treatment of an acute attack of asthma? |
|
Definition
inhaled albuterol
fast acting and most localized therapy for an acute attack |
|
|
Term
| what drug would be best for generalized anaphylactic reaction? |
|
Definition
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
start an IV infusion of _____ in an attempt to raise BP? |
|
Definition
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
infusion of dopamine - attempt to increase BP
what effects can be expected with low dose (2-5 mg/kg/min) dopamine? |
|
Definition
reduces arterial resistance
increase blood flow in renal, coronary, and splanchnic systems
positive ionotropic effect |
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
infusion of dopamine - attempt to increase BP
how does dopamine dose affect response? |
|
Definition
| different doses act on different receptors |
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
infusion of dopamine - attempt to increase BP
what effects can be expected with high dose (15-20 mg/kg/min) dopamine? |
|
Definition
a1 receptors response
high dose required to hit a1 receptors |
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
infusion of dopamine - attempt to increase BP
which receptors mediate low dose effects of dopamine? |
|
Definition
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
infusion of dopamine - attempt to increase BP
what effects occur with higher dose dopamine?
which receptors mediate these effects? |
|
Definition
vasoconstriction
mediated by a1-adrenoreceptors |
|
|
Term
65 yo woman
admitted to ICU - sepsis caused by UTI
hypotensive (80/40); elevated HR; decreased urine output
institution of antibiotic therapy and IV fluid
infusion of dopamine - attempt to increase BP
why use dopamine over NE? |
|
Definition
NE - worry about constricting afferent arterioles in kidney
already oligouric
NE - would compound reduced GFR |
|
|
Term
25 yo man in septic shock
low dose dopamine is admin
most likely result? |
|
Definition
increase renal blood flow
DA - binds to specific receptors in kidney vasculature - increases renal blood flow
CO - increased by DA action on B1 receptors |
|
|
Term
| in contrast to NE, metaraminol and methoxamine are metabolized by what? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| used to prevent hypotension due to spinal anesthesia |
|
|
Term
|
Definition
|
|
Term
|
Definition
| used to support, restore, or maintain BP during anesthesia |
|
|
Term
| metaraminol and methoxamine vs. NE |
|
Definition
not substrates for COMT or MAO
longer duration of action |
|
|
Term
| what are used to reduce mucous membrane congestion? |
|
Definition
a-adrenoreceptor sympathomimetic
cause vasoconstriction --> reduce mucous membrane congestions
phenylephrine |
|
|
Term
| how does phenylephrine act in reducing mucous membrane congestion? |
|
Definition
|
|
Term
| what is the prototype a-adrenergic agonist? |
|
Definition
|
|
Term
| what type of drug is prazosin? |
|
Definition
|
|
Term
| what type of drug is yohimbine? |
|
Definition
|
|
Term
| what type of drug is phenoxybenzamine? |
|
Definition
| a1 and a2 irreversible antagonist |
|
|
Term
| what type of drug is phentolamine? |
|
Definition
| a1 and a2 irreversible antagonist |
|
|
Term
| what type of drug is propranolol? |
|
Definition
|
|
Term
| what type of drug is timolol? |
|
Definition
|
|
Term
| what type of drug is pindolol? |
|
Definition
|
|
Term
| what type of drug is nadolol? |
|
Definition
|
|
Term
| what type of drug is metoprolol? |
|
Definition
|
|
Term
| what type of drug is atenolol? |
|
Definition
|
|
Term
| what type of drug is esmolol? |
|
Definition
|
|
Term
| what type of drug is acebutolol? |
|
Definition
|
|
Term
| what type of drug is reserpine? |
|
Definition
|
|
Term
| what type of drug is guanethidine? |
|
Definition
|
|
Term
| what type of drug is 6-hydroxydopamine? |
|
Definition
|
|
Term
| what type of drug is labetalol? |
|
Definition
|
|
Term
| what type of drug is carvedalol? |
|
Definition
|
|
Term
| a adrenergic antagonists specificity |
|
Definition
may be specific for a1 or a2
or may block both types |
|
|
Term
|
Definition
|
|
Term
| prototype a1 receptor antagonist |
|
Definition
|
|
Term
|
Definition
| used in management of HTN |
|
|
Term
|
Definition
postural hypotension (orthostatic)- block a1 vasoconstiction response
nasal stuffiness
problems with ejaculation |
|
|
Term
|
Definition
|
|
Term
|
Definition
| enhances neuronal release of NE by blocking negative feedback inhibition (most important action of a2 on pre-synaptic terminal of neuroeffector junction) |
|
|
Term
| most important physiological action of a2? |
|
Definition
located at pre-synaptic terminal of neuroeffector junction
NE is released - binds to a2 receptor - blocks more release of NE |
|
|
Term
|
Definition
| competitive antagonist at both a1 and a2 |
|
|
Term
| effect of phentolamine on NE release |
|
Definition
can cause excess NE release from sympathetic terminals
mimic cocaine |
|
|
Term
| what drugs cause increase NE release from nerve terminal? |
|
Definition
|
|
Term
| why do phentolamine and yohimbine cause increaed NE release? |
|
Definition
| block a2 receptors - block feedback inhibition to NE release |
|
|
Term
|
Definition
| irreversible antagonist at both a1 and a2 receptors |
|
|
Term
|
Definition
| no longer used in clinical medicine |
|
|
Term
| specificity of B adrenergic antagonists |
|
Definition
| if therapeutically useful - competitive antagonists at B1 or both B1 and B2 subtypes |
|
|
Term
| use of B adrenergic antagonists? |
|
Definition
management of HTN
cardiac arrhythmia
angina pectoris
other disorders |
|
|
Term
|
Definition
competitive antagonist at both B1 and B2 receptor
doesn't discriminate between actions on heart and lungs |
|
|
Term
|
Definition
HTN
cardiac dysrhythmias
angina pectoris
decrease oxygen demand and workload |
|
|
Term
| propranolol actions on cardiostimulatory effects? |
|
Definition
blocks effects of neuronally secreted NE and circulating epi
B2 - discriminates between NE and epi |
|
|
Term
| propranolol effect on renin secretion? |
|
Definition
| blocks renal B adrenergic receptors responsible for renin secretion |
|
|
Term
| propranolol effect on cardiac contractility |
|
Definition
|
|
Term
| who should avoid propranolol? |
|
Definition
| patients in heart failure because it depresses cardiac contractility |
|
|
Term
patient with heart failure
being treated with low dose B blockers
comes in with angina and CHF
what is concern about adding another B blocker?
what would be best option? |
|
Definition
could throw into low output failure because decreases contractility
best option - B1 specific blocker |
|
|
Term
| propranolol effect in lungs |
|
Definition
blocks bronchial B2 receptors
can seriously exacerbate asthma |
|
|
Term
| what 2 types of patients should you be wary about giving propranolol to? |
|
Definition
|
|
Term
| propranolol action on membrane? |
|
Definition
| membrane stabilizing activity - less susceptible to evoke AP or depolarizing event that will constrict |
|
|
Term
|
Definition
B1 and B2 receptor antagonist
non-specific |
|
|
Term
| how do timolol and nadolol differ compared to propranolol? |
|
Definition
| **low membrane stabilizing effect |
|
|
Term
|
Definition
used topically in the eye - management of glaucoma
management of HTN |
|
|
Term
|
Definition
B1 and B2 receptor antagonist
**intrinsic sympathomimetic activity |
|
|
Term
| how is pindolol's intrinsic sympathomimetic activity different than other drugs? |
|
Definition
it's a partial agonist
doesn't negate all signals - just diminishes response; lower % inhibition |
|
|
Term
| pindolol membrane stabilizing activity? |
|
Definition
|
|
Term
| metoprolol, atenolol, acebutolol, and esmolol type |
|
Definition
| B1 selective receptor antagonist |
|
|
Term
| metoprolol, atenolol, acebutolol, and esmolol use |
|
Definition
| primarily for treatment of HTN |
|
|
Term
| metoprolol, atenolol, acebutolol, and esmolol side effects |
|
Definition
| may produce cardiac decompensation in patient with borderline heart failure |
|
|
Term
| what could metoprolol, atenolol, acebutolol, and esmolol produce in patients with borderline heart failure? |
|
Definition
|
|
Term
| why are metoprolol, atenolol, acebutolol, and esmolol better suited to treat HTN in asthmatics? |
|
Definition
| they are less prone than pan-B blockers to induce bronchial constriction |
|
|
Term
| labetolol and carvedilol type |
|
Definition
| reversible a1, B1, and B2 selective receptor antagonist |
|
|
Term
| labetolol and carvedilol hemodynamic effects |
|
Definition
similar to propranolol and pazosin
B1 - decrease CO
a1 - decrease peripheral resistance |
|
|
Term
| labetolol and carvedilol use |
|
Definition
potent anti-HTN agent
malignant HTN or HTN that is unresponsive to typical medications |
|
|
Term
| labetolol and carvedilol side effects |
|
Definition
postural hypotension
bronchospasm
nasal congestion |
|
|
Term
| what drug would be used to treat an 83 yo post-menopausal woman with unresponsive HTN? |
|
Definition
|
|
Term
83 yo post-menopausal woman with unresponsive HTN who is treated with labetolol or carvedilol
what is a potential side effect?
what receptor mediates this response? |
|
Definition
prone to orthostatic hypotension and syncope; get out of bed in the morning, fall, and break hip
blocking a1 receptors causes this |
|
|
Term
| major side effects of a antagonists? |
|
Definition
orthostatic hypotension
dizziness - could result in syncope
headache
nausea
pounding heart beart
weight gain |
|
|
Term
| major side effects of B antagonists |
|
Definition
heart failure - low output failure
negative chronotropic effects
**increased airway resistance - exacerbate serious asthma attack
exacerbation of peripheral arterial disease
**hyperkalemmia
**facilitated hypoglycemia - masking of hypoglycemic crisis in diabetics**
depression
faitgue
sexual dysfunction
weight gain |
|
|
Term
| how do B-agonists and B-antagonists differ in their effects on K concentration in the blood? |
|
Definition
B agonist - hypokalemia; or rebound hyperkalemia with withdrawal
B antagonist - hyperkalemia |
|
|
Term
|
Definition
|
|
Term
|
Definition
taken up by NE transporter
stored in synaptic vesicles
releases as 'false transmitter' |
|
|
Term
| does guanethidine cross the BBB? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| guanethidine side effects |
|
Definition
postural hypotension
nasal stuffiness |
|
|
Term
|
Definition
|
|
Term
|
Definition
| blocks noradrenergic neuronal vesicle amine transport mechanism that maintains the high concentration of NE inside the vesicle |
|
|
Term
|
Definition
| adrenergic nerves are depleted of their NE content |
|
|
Term
|
Definition
|
|
Term
|
Definition
| sometimes useful in management of HTN |
|
|
Term
|
Definition
neuromuscular blocking agent
neurotoxin |
|
|
Term
|
Definition
taken up by adrenergic nerve terminals
converted to reactive quinone |
|
|
Term
|
Definition
|
|
Term
| what drug might be given to a politician who is nervous when talking to people to avoid sweaty palms? |
|
Definition
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital, he was started on oral? |
|
Definition
| metoprolol - B1 blocker; one of the most commonly used anti-HTN meds |
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital - started on oral metoprolol
what are the 2 major side effects of B blockers? |
|
Definition
masking hypoglycemia - not a diabetic
provoking constriction of airways - outgrown asthma |
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital - started on oral metoprolol
metoprolol is selective of which adrenoreceptor? |
|
Definition
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital - started on oral metoprolol
what effects do agents such as metoprolol have on CV system? |
|
Definition
| B blocker - decrease contractility --> decrease HR --> therefore decrease CO |
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital - started on oral metoprolol
in which organ is metoprolol metabolized? |
|
Definition
liver first
some in kidney |
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital - started on oral metoprolol
why must B adrenergic antagonists be used with caution is asthmatics? |
|
Definition
| may provoke hyper reactive airways |
|
|
Term
70 yo man
seen in follow up after hospitalization for MI - underwent angioplasty and is asymptomatic
prior to MI - on no meds, not a smoker, not diabetic
during hospitalization - persistently elevated BP readings
asthma as child - no recent wheezing episode
while in the hospital - started on oral metoprolol
why must B adrenergic antagonists be used with caution is diabetics? |
|
Definition
| may mask symptoms of hypoglycemia |
|
|
Term
which of the following actions of epi are blocked by prazosin?
bronchial dilation
increase cardiac SV
increased HR
mydriasis |
|
Definition
mydriasis
target of prazosin - a1 - blocks epi mediated contraction of radial SM that will result in mydriasis |
|
|
Term
| what are the target receptors of epi? |
|
Definition
|
|
Term
| what receptor is responsible for epi induced bronchial dilation? |
|
Definition
|
|
Term
| what receptor is responsible for epi induced increase in cardiac SV? |
|
Definition
|
|
Term
| what receptor is responsible for epi induced increased HR? |
|
Definition
|
|
Term
34 yo man
prescribed labetalol for HTN
effect on CV system is a result of its action as an antagonist at which receptors? |
|
Definition
| both a and B adrenoreceptors |
|
|
Term
| what other drug besides labetalol blocks both a and B adrenoreceptors? |
|
Definition
|
|
Term
which of the following is the least likely clinical use for B-adrenoreceptor antagonists?
benign prostatic hypertrophy
arrhythmia
HTN
ischemic heart disease |
|
Definition
BPH - a1 mediated problem
other 3 treated with B-blockers |
|
|
