Adrenergic Agonists/antagonists Flashcards
Norepinephrine
Mech
Tx
Side Eff
Non-selective Agonist: α1, α2, β1
Tx: Acute Hypotension
Hypertension; arrythmias; headache
Epinephrine
Mech
Tx
Side Eff
Non-selective Agonist: α1, (α2), β1, β2
Tx: Anaphylactic shock; combined with local anesthetics; glaucoma
Palpitation; arrhythmias; headache
Amphetamine
Mech
Tx
Side Eff
Increases NorEpi Release
Tx: ADHD, narcolepsy, recreation
Hypertension, insomnia, anxiety, arrhythmias
Isoproterenol
Mech
Tx
Side Eff
Non-selective β agonist
Agonist: β1, β2
Tx: shock; heart block
Palpitation; tachyarrhythmia; headache
Dobutamine
Mech
Tx
Side Eff
β1-selective β agonist
Agonist: β1
Tx: Cardiac decompensation; shock; heart block
Tachyarrythmias; hypertension
Albuterol
Mech
Tx
Side Eff
β2-selective β agonist
Agonist: β2
Tx: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD
Can mask progressively severe inflammation
Tachycardia, muscle tremor
Terbutaline
Mech
Tx
Side Eff
β2-selective β agonist
Agonist: β2
Tx: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD
Can mask progressively severe inflammation
Tachycardia, muscle tremor
Phenylephrine
Mech
Tx
Side Eff
α1-selective α agonist
Agonist: α1
Tx: Nasal congestion; postural Hypotension
Hypertension; reflex bradycardia
Clonidine
Mech
Tx
Side Eff
α2-selective α agonist
Agonist: CNS α2
Tx: Hypertension; shock; withdrawal from drug dependence
Sedation
α-methyldopa
Mech
Tx
Side Eff
α2-selective agonist
Crosses BBB- activates CNS a2 receptors
Tx: Hypertension
Sedation
Fenoldopam
Mech
Tx
Side Eff
Selective dopamine agonist
Agonist: D1 only
Tx: Increase blood flow at renal, mesenteric, and cerebral arteries
Dopamine
Mech
Tx
Side Eff
Mixed acting (direct/indirect) Agonist: D1, α1, β1
Low dose = Direct @ D1 Receptors
Medium dose = Direct @ Beta 1, some Indirect
High dose = Direct @ Alpha 1, some Indirect
Vasoconstriction (@ high doses)
Phentolamine
Mech
Tx
Side Eff
Non-selective α-antagonist
Antagonist: α1, α2
Tx: Pheochromocytoma, Raynaud’s, frostbite
Postural hypotension; inhibit ejaculation
Phenoxybenzamine
Mech
Tx
Side Eff
Non-selective α-antagonist
Antagonist: α1, α2;
non-competitive blocker
Tx: Pheochromocytoma, Raynaud’s, frostbite
Postural hypotension; inhibit ejaculation
Prazosin
Mech
Tx
Side Eff
α1-selective antagonist
Antagonist: α1
Tx: Primary HTN, BPH
Postural hypotension (usually 1st dose)
Terazosin
Mech
Tx
Side Eff
α1-selective antagonist
Antagonist: α1
Tx: Primary HTN, BPH
Postural hypotension (usually 1st dose)
Propranolol
Mech
Tx
Side Eff
Non-selective β-antagonist (1st generation)
Antagonist: β1, β2
Tx: Angina, Hypertension, Arrythmias
Bradycardia, Bronchoconstriction, Sexual Dysfunction
Timolol
Mech
Tx
Side Eff
antagonist (1st generation)
Antagonist: β1, β2
Tx: Glaucoma
Bradycardia, Bronchoconstriction, Sexual Dysfunction
Metropolol
Mech
Tx
Side Eff
β1-selective antagonist (2nd generation)
Antagonist: β1
Tx: HTN, Angina, Arrythmias, CHF
Bradycardia, Sexual Dysfunction
Atenolol
Mech
Tx
Side Eff
β1-selective antagonist (2nd generation)
Antagonist: β1
Tx: HTN, Angina, Arrythmias, CHF
Bradycardia, Sexual Dysfunction
Bisoprolol
Mech
Tx
Side Eff
β1-selective antagonist (2nd generation)
Antagonist: β1
Tx: HTN, Angina, Arrythmias, CHF
Bradycardia, Sexual Dysfunction
Carvedilol
Mech
Tx
Side Eff
Non-selective β-antagonist
Antagonist: β1, β2
3rd gen
Tx: CHF, HTN
Bradycardia, Fatigue
Labetalol
Mech
Tx
Side Eff
Non-selective β-antagonist
Antagonist: β1, β2
3rd gen
Tx: CHF, HTN
Bradycardia, Fatigue
Betoxolol
Mech
Tx
Side Eff
β1-selective antagonist Antagonist: β1
3rd gen
Tx: CHF, HTN
Bradycardia
Tyramine
Mech
Tx
Side Eff
Indirect acting agonist
Increases cytoplasmic NE release
No Tx
Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out
Cocaine
Mech
Tx
Side Eff
Prevents NE reuptake
Tx: Local anesthetic, vasoconstrictor
Insomnia, anxiety, arrhythmias
Guanethidine
Mech
Tx
Side Eff
Nerve ending blocker False neurotransmitter (vesicles become full of guanethidine rather than NE)
Tx: Antihypertensive
Many and serious
Don’t really use this in US; doesn’t cross BBB
Reserpine
Mech
Tx
Side Eff
Nerve ending blocker
Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it)
Tx: Older antihypertensive
Many and serious (depression and suicide are major ones)
Cheap! (used abroad)
α-me-tyrosine
Mech
Tx
Side Eff
Nerve ending blocker
Inhibit tyrosine hydroxylase (decreases NE synthesis)
Tx: Pheochromocytoma
Many and serious
Ephedrine
Mech
Tx
Side Eff
Mixed, direct (β2)/indirect agonist
Nasal decongestion, anorexic
