Adrenergic Receptor Agonists/Antagonists Flashcards
What are the 2 non-selective adrenergic receptor agonists?
Norepinephrine
Epinephrine
What is norepinephrine an agonist for?
a1
a2
B1
What is epinephrine an agonist for?
a1
a2
B1
B2
Name the indirect acting adrenergic receptor agonist…
Amphetamine
What is the mechanism of action for amphetamine?
Increases release of NE
What class does isoproterenol fall in?
Non-selective B agonist
What is isoproterenol an agonist for?
B1
B2
What class does dobutamine fall in?
B1-selective B agonist
What is dobutamine an agonist for?
B1
What class does albuterol fall in?
B2-selective B agonist
What is albuterol an agonist for?
B2
What class does terbutaline fall in?
B2-selctive B agonist
What is terbutaline an agonist for?
B2
Non-selective agonist used for acute hypotension
NE
Non-selective agonist used for anaphylactic shock; also combined with local anesthetics and used to treat glaucoma…
Epi
Indirect acting adrenergic receptor agonist used for the treatment of ADHD, narcolepsy, recreation
Amphetamine
What are the side effects of NE?
HTN
arrhythmia
headache
What are the side effects of EPI?
Palpitation
arrhythmias
headache
What are the side effects of amphetamine?
HTN
insomnia
anxiety
arrhythmias
Non-selective B agonist used for the treatment of shock, and heart block…
Isoproterenol
B1-selective B agonist used for the treatment of cardiac decompensation, shock, and heart block…
Dobutamine
B2-selective B agonist used to prevent or reverse exercise-induced bronchospasm; mild asthma; COPD…
Albuterol
B2-selective B agonist used to prevent or reverse exercise-induced bronchospasm; mild asthma; COPD and early labor…
Terbutaline
What are the side effects of isoproterenol?
Palpitation
Tachyarrhythmia
headache
What are the side effects of dobutamine?
Tachyarrythmias
HTN
Albuterol and terbutaline can potentially mask what?
Progressively severe inflammation
What are the side effects of albuterol and terbutaline?
Tachycardia
Muscle tremor
a1-selective a agonist..
Phenylephrine
What is phenylephrine an agonist for?
a1
What are the 2 a2-selective a agonists?
Clonidine
a-methyldopa
What is the mechanism of action for clonidine?
CNA a2 agonist
What is the mechanism of action for a-methyldopa?
Metabolite (a-methylnorepinephrine) activates CNS a2 receptors
What is phenylephrine used for?
Nasal congestion
postural hypotension
What is clonidine used for?
HTN
Shock
Drug withdrawal
What is a-methyldopa used for?
HTN
What are the side effects of phenylephrine?
HTN
Reflex bradycardia
What are the side effects of clonidine and a-methyldopa?
Sedation
a2-selective a agonist that can cross the BBB and is a prodrug…
a-methyldopa
Selective dopamine agonist…
Fenoldopam
What is fenoldopam an agonist for?
D1 only
Mixed acting (direct/indirect) adrenergic receptor agonist…
Dopamine
What is dopamine and agonist for?
D1–low dose (direct)
a1–high dose (direct with some indirect (NE))
B1–med dose (direct with some indirect (NE))
What is Fenoldopam used for?
Increase blood flow at renal, mesenteric and cerebral arteries
What is dopamine used for?
Shock
Renal failure
Hypotension
What is the side effect of dopamine?
Vasoconstriction at high doses
Name the 2 non-selective a-antagonists…
Phentolamine
Phenoxybenzamine
What is phentolamine an antagonist for?
a1
a2
What is phenoxybenzamine an antagonist for?
a1
a2
non-competitive blocker–covalently bind receptor
What are the non-selective a-antagonist drugs, phentolamine and phenoxybenzamine, used for?
Pheochromocytoma
Raynaud’s
Frostbite
What are the side effects of all the a-antagonists?
Postural hypotension
What are the side effects of the non-selective a-antagonists?
Postural hypotension
Inhibit ejaculation
Name the 2 a1-selective antagonist…
Prazosin
Terazosin
What are the uses of Prazosin and Terazosin?
Primary HTN
BPH
Name the 2 non-selective B antagonist (1st generation)
Propranolol
Timolol
What are propranolol and timolol antagonist for?
B1
B2
What non-selective B antagonist is used to treat angina, HTN, and arrhythmias?
Propranolol
What are the side effects of propranolol and timolol?
Bradycardia
Bronchoconstriction
Sexual dysfunction
Non-selective B antagonist used to treat glaucoma…
Timolol
Name the 3 2nd generation B1-selective antagonists…
Metoprolol
Atenolol
Bisoprolol
What are all 3 2nd generation B1-selective antagonists used to treat? (Metoprolol, Atenolol, Bisoprolol)
HTN
Angina
Arrhythmias
CHF
What are the side effects of all 3 2nd generation B1-selective antagonists? (Metoprolol, Atenolol, Bisoprolol)
Bradycardia
sexual dysfunction
What are the 2 3rd generation “A” non-selective B antagonists?
Carvedilol
Labetalol
What are all the 3rd generation B antagonists used for?
CHF
HTN
What are the side effects of the 2 3rd generation “A” non-selective B antagonists? (Carvedilol and Labetalol)
Bradycardia
Fatigue
Name the 3rd generation “B” B1 selective antagonist…
Betaxolol
What is betaxolol used for?
CHF
HTN
What are the side effects of Betaxolol?
Bradycardia
What is the indirect acting adrenergic receptor agonist, which works through increasing cytoplasmic NE release?
Tyramine
A drug that prevents NE re-uptake and is used as a local anesthetic and vasoconstrictor?
Cocaine
What are the side effects of cocaine?
Insomnia
Anxiety
Arrhythmias
Name the 3 nerve ending blockers…
Guanethidine
Reserpine
a-me-tyrosine
What is the mechanism for guanethidine?
False NT–causing vesicles to become full of guanethidine rather than NE
What is guanethidine used for?
antihypertensive
What isn’t Guanethidine used?
Many and serious side effects
unable to cross BBB
Nerve ending blocker that causes release of empty vesicles by it binds the re-uptake transporter and stops NE from reentry…
Reserpine
What is reserpine used for?
it is an old antiHTN
What is the mechanism for a-me-tyrosine, a nerve ending blocker?
Inhibits tyrosine hydroxylase–decreasing NE synthesis
What is a-me-tyrosine used for?
treatment of pheochromocytoma
Mixed, direct B2/indirect agonist used for nasal decongestion and anorexia?
Ephedrine