Adrenergic Drugs Flashcards
Is epinephrine an agonist or antagonist and what receptor types does it effect?
agonist; a1, a2, B1, B2 (nonselective)
Is norepinephrine an agonist or antagonist and what receptor types does it effect?
agonist; a1, a2, B1 (nonselective)
Is amphetamine indirect or direct acting and what is its mechanism of action?
indirect; increases release of NE
Is Isoproterenol an agonist or antagonist and what receptor types does it effect?
non selective B agonist; B1 and B2
Is Dobutamine an agonist or antagonist and what receptor types does it effect?
Agonist; B1
Is Albuterol an agonist or antagonist and what receptor types does it effect?
Agonist; B2
Is Terbutaline an agonist or antagonist and what receptor types does it effect?
Agonist; B2
Is Phenylephrine an agonist or antagonist and what receptor types does it effect?
Agonist; a1
Is Colnidine an agonist or antagonist and what receptor types does it effect?
Agonist; a2
Is a-methyldopa an agonist or antagonist and what receptor types does it effect?
Agonist; a2
What class of drugs is Fenoldopam in and what is its mechanism?
selective dopamine agonist; vasodilation
Is dopamine and indirect acting, or direct acting drug?
both
Is dopamine an agonist or antagonist and what receptor types does it effect?
agonist; D1, a1, B1
What is NE used to treat?
hypotension
What is Epi used to treat?
Anaphylactic shock (a1 and B2), combined with local anesthetic to control hemorrhage and contain the anasthetic (a1), glaucoma
What is amphetamine used for?
ADHD, narcolepsy and recreational drug
What is Isoproterenol used to treat?
Bronchodilator/asthma, shock (increases CO), heart block (increases HR)
What is Dobutamine used to treat?
cardiac decompensation (increases contractility), shock (increases HR), and heart block
What is Albuterol used to treat?
Prevent or reverse exercise-induced bronchospasm, mild asthma, COPD
What is Terbutaline used to treat?
Prevent or reverse exercise-induced bronchospasm, mild asthma, COPD
What are some side effects of Albuterol and Terbutamine?
masking of progressively severe inflammation, tachycardia, muscle tremors
What is phenyephrine used to treat and how does it work?
Nasal congestion and postural hypotension by vasoconstriction (a1)
Whats is Clonidine used to treat and how does it work?
Hypertension, shock, withdrawal from drug dependence by decreasing sympathetic outflow from CNS (a2 agonist)
What is a-methyldopa used to treat and how does it work?
Hypertension, shock, withdrawal from drug dependence by decreasing synthesis of NE
What is Fenoldopam used for?
to increase blood flow at renal, mesenteric, and cerebral arteries (only 10 min t1/2 though)
What is dopamine used to treat?
shock, renal failure (d1vasodilation) in renal and mesenteric arteries), and hypotension (a1 vasoconstriction)
What can happen at high doses of dopamine? low doses?
high doses- a1 direct activity and NE release indirect activity causing vasoconstriction
low doses- direct action on D1 receptors causing vasodilation
What are some side effects of NE?
hypertension, arrhythmia and headache
What are some side effects of Epi?
palpitations, arrythmia,headache and tremor
What are some side effects of Amphetamines?
hypertension, insomnia, anxiety and arrythmias
What are some side effects of Isoproterenol?
palpitations, tachyarrythmia and headche
What are some side effects of Dobutamine?
tachyarrythmia, and hypertension
What are some side effects of Phenylephrine?
hypertension and reflex bradycardia
Which of the following is a pro-drug and can cross the BBB? Phenylephrine, Clonidine or a-Methyldopa
a-methyldopa
Is phentolamine an agonist or antagonist and what receptor types does it effect?
antagonist; a1 and a2
Is phenoxybenzamine an agonist or antagonist and what receptor types does it effect?
antagonist; a1 and a2 (non competitive blockers)
Is prazosin an agonist or antagonist and what receptor types does it effect?
antagonist; a1
Is terazosin an agonist or antagonist and what receptor types does it effect?
antagonist; a1
What are phentolamine and phenoxybenzamine used to treat?
Pheochromocytoma, Raynaud’s, frostbite (cause vasodilation)
What are Prazosin and Terazosin used to treat?
primary hypertension and benign prostatic hypertrophy (causes vasodilation)
What are some side effects of phentolamine and phenoxybenzamine?
Postural hypotension and inhibition of ejaculation
What are some side effects of Prazosin and Terazosin?
Postural hypotension (usually only with 1st dose b/c it is selective)
Name the 1st generation B antagonist drugs and whether they are nonselective or selective.
propanolol and timolol; non selective B1 and B2
Name the 2nd generation B antagonist drugs and whether they are selective or non selective.
metoprolol, bisoprolol and atenolol; B1 selective
Name the 3rd generation B antagonist drugs and whether they are selective or non selective.
carvedilol and labetalol; non selective B1 and B2
betaxolol; selective B1
What are some of the side effects of the non selective, 1st generation B antagonist drugs, Propanolol and timolol?
Bradycardia, bronchoconstriction and sexual dysfunction
What are the non selective, 1st generation B antagonist drugs, Propanolol and timolol used to treat?
Angina, hypertension, and Arrythmias
Which B antagonist is the one that all other are compared to?
Propanolol
What are the selective, 2nd generation B antagonist drugs, metoprolol, bisoprolol and atenolol, used to treat?
hypertension, angina, arrythmias and CHF
What are some side effects of the selective, 2nd generation B antagonist drugs, metoprolol, bisoprolol and atenolol?
Bradycardia and sexual dysfunction
What are the nonselective/selective 3rd generation B antagonist drugs, carvediol (NS), labetalol (NS), and betaxolol (S) used to treat?
CHF and hypertension
What are some side effects of the non selective 3rd generation B antagonist drugs, carvediol and labetalol?
Bradycardia and fatigue
What are some side effects of the selective 3rd generation B antagonist drug, betaxolol?
bradycardia
What is the mechanism of action of cocaine?
prevents NE reuptake (main process for terminating NE signal)
What is the mechanism of action of tyramine?
Increases cytoplasmic NE release via an exchange transporter-tyramine goes in, NE goes out
What is the mechnism of action of Guanethidine and what is it used to treat?
False NT-vesicles fill with guanethidine instead of NE; used to treat hypertension
doesn’t cross BBB*
What is the mechanism of action of reserpine and what is it used to treat?
It binds to the uptake transporter and inhibits it causing the vesicles that normally contain NT to be empty; used to be used an antihypertensive but not used in US anymore
What is the mechanism of action of a-me-tyrosine and what is it used to treat?
inhibits tyrosine hydroxylase causing a decrease in NE synthesis; used to treat pheochromocytoma
What is Ephedrine used to treat?
nasal congestion, is also an anorexic
Which of the following drugs has depression and suicide as a possible side effect? Guanethidine, reserpine or a-me-tyrosine
Reserpine
Name the 3 mechanisms for removal of NE from the synaptic cleft.
Uptake1-into neuron, Uptake2-into extraneuronal cells, and diffusion into bloodstream
What is the difference in release between norepinephrine and epinephrine?
norepi- released locally into synapse (neurotransmitter)
epi- released into blood stream from adrenal medulla (neurohormone)
What are the 2 main enzymes that metabolize adrenergic drugs?
monoamine oxidase and catechol-O-methyltransferase
What medications/therapies should be considered to treat shock?
volume NE Isoproterenol Dopamine-vasodilation to save kidneys a-blockers-vasodilation
What are the 3 main cautions to think about when treating with a-agonists?
localized ischemia at infusion site, avoid extravasation and gradually decrease infusion
Why are beta blockers better at treating hypertension than alpha blockers?
not sure but most likely possibilities include: blocks renin release from JGA, and blocking of presynaptic receptors that enhance NE release
Why are Beta blockers the first line therapy in CHF?
slows the system down to save the heart muscle from going downhill faster
