Adrenergic Pharmacology Flashcards
Vasoconstricts renal blood vessels
Norepinephrine
Inhibits hydroxylation of tyrosine to DOPA
Metyrosine
Inhibits vesicular transport of NE and dopamine
Reserpine
Inhibits release of NE
Guanethidine
Promotes release of NE
Amphetamines
Tyramine
Diffusion and reuptake of NE is inhibited by?
Cocaine
TCAs
Increases stores of NE and dopamine
MAOIs
Non-selective, direct-acting sympathomimetic
Epinephrine
Norepinephrine
Dopamine
Beta-nonselective sympathomimetic
Isoproterenol
Alpha 1-selective sympathomimetics
Phenylephrine
Pseudoephedrine
Alpha 2 selective sympathomimetics
Clonidine
Apraclonidine
Methyldopa
Brimonidine
Beta 1-selective sympathomimetic
Dobutamine
Beta 2-selective sympathomimetic
Albuterol/salbutamol
Ritodrine
Terbutaline
Alpha-nonselective adrenergic antagonist
Phenoxybenzamine
Phentolamine
Alpha 1-selective antagonist
Prazosin Doxazosin Terazosin Tamsulosin Silodosin
Beta-nonselective antagonist
Propranolol Pindolol Timolol Labetalol Carvedilol Nadolol
Beta 1-selective antagonist
Atenolol Betaxolol Esmolol Acebutolol Metoprolol
Used in cardiac arrest, anaphylaxis, asthma, COPD, Hemostasis
Epinephrine
Used in neurogenic shock and cardiogenic shock (last resort)
Norepinephrine
First line drug for shock; used in heart failure
Dopamine
Low dose dopamine (1-5mcg/kg/min) activates what receptors?
D1 receptors
Medium dose dopamine (5-15mcg/kg/min) stimulates what receptors?
B1 receptors
High dose (>15mcg/kg/min) stimulates what receptors?
Alpha receptors
Beta-nonselective sympathomimetic used for asthma; causes tachycardia
Isoproterenol
Decongestant; mydriatic; causes rebound nasal congestion
Phenylephrine
Pseudoephedrine
Causes mydriasis without cycloplegia
Phenylephrine
Pseudoephedrine
Used for hypertension, cancer pain, and opioid withdrawal
Clonidine
Used to treat rebound hypertension caused by clonidine
Phentolamine
Used for pre-eclampsia
Methyldopa
Alpha 2-selective
SE of methyldopa
Sedation Hemolytic anemia (positive Coomb's test)
Alpha 2-selective sympathomimetic used for glaucoma
Apraclonidine
Used for acute heart failure; DOC for cardiogenic shock
Dobutamine
Beta 1-selective sympathomimetic
Used in cardiac testing for amputated patients
Dobutamine
DOC for acute attacks of asthma
Albuterol/salbutamol
Used for tocolysis of preterm labor
Terbutaline
Ritodrine
Beta 2-selective sympathomimetics may precipitate arrhythmias in patient with concurrent?
COPD and heart disease
Sympathomimetic of choice for acute heart failure and septic shock
B1 and D1 agonist
Sympathomimetic of choice for hemostasis, decongestion, and spinal shock
Alpha 1 agonist
Sympathomimetic of choice for bronchospasm and premature labor
B2 agonist
Sympathomimetic of choice for hypertension and glaucoma
Alpha 2 agonist
Irreversible, nonselective, alpha blocker
Phenoxybenzamine
Reversible, nonselective, alpha blocker
Phentolamine
Alpha 1-selective blocker
Prazosin
Terazosin
Tamsulosin
Silodosin
Alpha 2-selective blocker
Yohimbine
Nonselective beta blocker
Propranolol Pindolol Timolol Labetalol Carvedilol Nadolol
Beta 1-selective blocker
Atenolol Betaxolol Esmolol Acebutolol Metoprolol
Beta 2-selective blocker
Butoxamine
Used for pheochromocytoma (pre-surgical)
Phenoxybenzamine
Phentolamine
Most selective for prostatic smooth muscle
Tamsulosin
Used for BPH
Alpha 1-selective blocker
Pharmacologic advantage of alpha 1-selectivity
Reflex tachycardia is less common and less severe
Beta blockers which may be used for pheochromocytoma
Carvedilol
Labetalol
Causes erectile dysfunction
Beta blockers
Beta blocker with the longest half-life
Nadolol
Beta blockers with absent local anesthetic activity; useful in glaucoma (decreases aqueous secretion from the ciliary epithelium)
Timolol
Betaxolol
B1 blocker used for SVT
Esmolol
Beta blocker with the shortest half-life
Esmolol
Vasodilates renal blood vessels
Dopamine
Alpha 1 agonists
Midodrine
Phenylephrine
MOA of alpha-1 agonists
Activates phospholipase C, resulting in increased intracellular calcium and vasoconstriction (increases BP)
Indication for alpha-1 agonists
Orthostatic hypotension
Toxicity of alpha-1 agonists
Supine hypertension; piloerection (goosebumps); urinary retention
Alpha-1 agonist used as a decongestant
Phenylephrine
Alpha-2 agonists
Clonidine Methyldopa Dexmedetomidine Tizanidine Apraclonidine Brimonidine
Mechanism of action of alpha-2 agonists
Inhibits adenylyl cyclase and interacts with other intracellular pathways; vasoconstriction is masked by central sympatholytic effect, which lowers BP
Indication of alpha-2 agonists
Hypertension
Toxicity of alpha-2 agonists
Dry mouth and sedation
Alpha-2 agonists used in glaucoma to reduce intraocular pressure (decreases aqueous secretion)
Apraclonidine
Brimonidine
B1 agonist
Dobutamine
MOA of B1 agonist
Activates adenylyl cyclase, increasing myocardial contractility; positive inotrope
Indication of B1 agonist
Cardiogenic shock; acute heart failure
B2 agonist
Albuterol
MOA of B2 agonist
Activates adenylyl cyclase; bronchodilation
Indication of B2 agonist
Asthma
Toxicities of B2 agonist
Tremor
Tachycardia
D1 agonist
Fenoldopam
MOA of D1 agonist
Activates adenylyl cyclase; vascular smooth muscle relaxation
Indication of D1 agonist
Hypertension
D2 agonist
Bromocriptine
MOA of D2 agonist
Inhibits adenylyl cyclase and interacts with other cellular pathways; restores dopamine actions in the CNS
Indications of D2 agonist
Parkinson’s disease; prolactinemia
Toxicity of D2 agonist
Orthostatic hypotension