Adrenergics-Chen Flashcards
What are the alpha-1 agonists?
Norepinephrine, Phenylephrine, Naphazoline, Oxymetazoline
What is the MOA of Norepinephrine?
Alpha-1 at therapeutic dose, B1 and B2 with increased dose; direct action
What are the effects of Norepinephrine?
Vasoconstriction > heart stimulation; increase BP; increase TRP; reflex bradycardia
When would you use Norepinephrine?
Shock (IV) to increase BP, rapid onset, extremely short action (1-2min); slow drip, not PO
What are the side effects of Norepinephrine?
Increased BP/hypertensive crisis/hemorrhage, reflex bradycardia, excessive nasal dryness, blurred vision, IV infiltration > tissue necrosis
What is the MOA of Phenylephrine?
Selective for alpha-1
What are the effects of Phenylephrine?
Vasoconstriction > heart stimulation; increases BP; Increases TPR; reflex bradycardia
When would you use Phenylephrine?
IV to increase BP, PO or intranasally as nasal decongestant, ophthalmic drops for mydriasis
What are the side effects of Phenylephrine?
CVS: increase in BP, cardiac failure and arrhythmia, reflex bradycardia; infiltration necrosis after parenteral admin; rebound nasal congestion
What is the MOA of Naphazoline?
Selective for alpha-1
What are the effects of Naphazoline?
Vasoconstriction > heart stimulation; increases BP; increases TPR; reflex bradycardia
When would you use Naphazoline?
PO or intranasally as nasal decongestant; ophthalmic drops for mydriasis; relief of redness of eye
What are the side effects of Naphazoline?
CVS: increase in BP, cardiac failure and arrhythmia, reflex bradycardia; infiltration necrosis after parenteral admin; rebound nasal congestion
What is the MOA of Oxymetazoline?
Non-selective alpha agonist
What are the effects of Oxymetazoline?
Vasoconstriction > heart stimulation; increases BP; increases TPR; reflex bradycardia
When would you use Oxymetazoline?
PO or intranasally as nasal decongestant; ophthalmic drops for mydriasis; relief of redness of eye
What are the side effects of Oxymetazoline?
CVS: increase in BP, cardiac failure and arrhythmia, reflex bradycardia; infiltration necrosis after parenteral admin; rebound nasal congestion
What are the alpha-2 Agonists?
Clonidine
What is the MOA of Clonidine?
Stimulates pre-synaptic alpha-2 receptors in CNS
What are the effects of Clonidine?
Decreases sympathetic outflow to the periphery
Whwhen would you use Clonidine?
Hypertension; withdrawal symptoms from opiates, tobacco smoking, and benzodiazepines
What are the side effects of Clonidine?
Lethargy, sedation, constipation, dry mouth; abrupt discontinuance > rebound hypertension
What are the Beta-1 Agonists?
Dobutamine
What is the MOA of Dobutamine?
Selective B1 agonist
What are the effects of Dobutamine?
Increases force > HR at therapeutic concentration
When would you use Dobutamine?
Parentally for acute CHF as an inotropic drug
What are the side effects of Dobutamine?
Develop ventricular arrhythmias; development of tolerance with prolonged use (downregulate receptor)
What are the Beta-2 Agonists?
Albuterol, Terbutaline, Isoproterenol
What is the MOA of Albuterol?
Selective B2 agonist
What are the effects of Albuterol?
Relax smooth muscle, bronchodilation, relax uterus, vasodilation in skeletal muscle blood vessels
When would you use Albuterol?
PO/SC/Inhalation/IV for 3-6 hrs; acute bronchospasm in asthma; use slmeterol/formoterol for long acting and can combine with steroid for asthma
What are the side effects of Albuterol?
Tremor, tachycardia (at higher doses can cause some beta-1 stimulation on heart)
What is the MOA of Terbutaline?
Selective B2 agonist
What are the effects of Terbutaline?
Relax smooth muscle, bronchodilation, relax uterus, vasodilation in skeletal muscle blood vessels
When would you use Terbutaline?
PO/SC/Inhalation/IV for 3-6 hrs; acute bronchospasm in asthma; inhibit the uterine contractions in premature labor; use salmeterol/formoterol for long acting and can combine with steriod for asthma
What are the side effects of Terbutaline?
Tremor, tachycardia (at higher doses can cause some beta-1 stimulation on heart)
What is the MOA of Isoproterenol?
Non-selective beta agonist; direct action
What are the effects of Isoproterenol?
Relaxation of smooth muscle of bronchioles and intestinal tract; vasodilation within the skeletal muscles > drop in TPR and diastolic pressure; chronotropic actions > rise in systolic pressure; glycogenolysis and hyperlipidemia; myometrial relaxation
When would you use Isoproterenol?
IV metabolized by COMT, not MAO; longer half life than epinephrine; treat heart block, bradycardia, ventricular arrhythmia (torsades de pointes)
What are the side effects of Isoproterenol?
Tachycardia, headache, flushing, ischemia, arrhythmia in coronary artery disease patients; palpitations, increased BP, CNS stimulation/anxiety overdoses; treamors (A HINT)
What is the MOA of Epinephrine?
Works as A1, B1 and B2 agonist; direct action
What are the effects of Epinephrine?
Regional vasoconstriction > increased systolic BP (A1); Increased CO > increased systolic BP (HR/Contractility increase B1); Skeletal muscle vasodilation > decrease diastolic pressure (B2); Broncorelaxation (B2); hyperglycemic effect (B2/A1); lipolysis
When would you use Epinephrine?
IM/IV/SC/Inhalation; rapid onset but brief duration of action; asthma; anaphylactic shock (IM) and angioedema; prolongation of local anesthetics; cardiac arrest, bradycardia, complete heart block in emergency; bleeding ulcers, calrogenic effects/metabolism
What are the side effects of Epinephrine?
Ventricular arrhythmias, headache, restlessness
What is the MOA of Dopamine?
Dose-dependent response on receptors; low= dopaminergic; medium=B1; high=A
What are the effects of Dopamine?
Low= vasodilation; medium= force > rate; High= vasoconstriction
When would you use Dopamine?
Circulatory shock, acute heart failure
What are the side effects of Dopamine?
Tachycardia, anginal pain, arrhythmias, headache
What is the MOA of Fenoldopam?
Peripheral D1 agonist
What are the effects of Fenoldopam?
Rapid vasodilation
When would you use Fenoldopam?
Severe hypertension
What are the side effects of Fenoldopam?
Tachycardia, anginal pain, arrhythmias, headache
What are the alpha antagonists?
Pentolamine, Phenoxybenzamine, Prazosin, Terazosin, Tamsulosin, Alfusozin, Doxazosin, Labetalol, Carvedilol
What is the MOA of Phentolamine?
Nonselective block of A1 and A2
What are the effects of Phentolamine?
Reversible; short acting
When would you use Phentolamine?
For diagnosis and treatment of pheochromocytoma
What are the side effects of Phentolamine?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Phenoxybenzamine?
Nonselective block of A1 and A2
What are the effects of Phenoxybenzamine?
Irreversible; long-acting
When would you use Phenoxybenzamine?
Preoperative management of pheochromocytoma
What are the side effects of Phenoxybenzamine?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Prazosin?
Selective block of A1
What are the effects of Prazosin?
Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle
When would you use Prazosin?
Hypertension
What are the side effects of Prazosin?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Terazosin?
Selective Block of A1
What are the effects of Terazosin?
Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle
When would you use Terazosin?
Hypertension
What are the side effects of Terazosin?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Tamsulosin?
Selective block of A1
What are the effects of Tamsulosin?
Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle
When would you use Tamsulosin?
Benign prostate hyperplasia
What are the side effects of Tamsulosin?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Alfusozin?
Selective block of A1
What are the effects of Alfusozin?
Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle
When would you use Alfusozin?
Benign prostate hyperplasia
What are the side effects of Alfusozin?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Doxazosin?
Selective block of A1
What are the effects of Doxazosin?
Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle
When would you use Doxazosin?
Hypertension and benign prostate hyperplasia
What are the side effects of Doxazosin?
Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal
What is the MOA of Labetalol?
A1 and NS beta blocker
What are the effects of Lebetalol?
Decreases PR and CO, more balanced approach to inhibiting the SNS
When would you use Lebetalol?
IV for hypertension and hypertensive emergencies, pheochromocytoma
What are the side effects of Labetalol?
Combination of alpha/beta blockade, hepatic injury
What is the MOA of Carvedilol?
A1 and NS Beta blocker
What are the effects of Carvedilol?
Decreases PR and CO, more balanced approach to inhibiting the SNS
When would you use Carvedilol?
Heart failure
What are the side effects of Carvedilol?
Combination of alpha/beta blockade, hepatic injury
What are the beta antagonists?
Propranolol, Timolol, Nadolol, Metoprolol, Atenolol, Acebutolol, Esmolol, Nebivolol, Pindolol
What is the MOA of Propranolol?
Nonselective B antagonist
What are the effects of Propranolol?
Prototype; most lipid soluble beta blocker; highest membrane stabilizing effect
What are the side effects of Propranolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Timolol?
Nonselective B antagonist
When would you use Timolol?
Chronic open-angle glaucoma (topical); hypertension and migraine prophylaxis
What are the side effects of Timolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Nadolol?
Nonselective B antagonist
What are the effects of Nadolol?
More potent than Propranolol; long duration of action (HL= 20-24 hrs)
When would you use Nadolol?
Hypertension, angina, migraine prophylaxis
What are the side effects of Nadolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Metoprolol?
Selective B1 blocker
What are the effects of Metoprolol?
Cardioselective
When would you use Metoprolol?
Safer than non-selective for COPD and asthma; hypertension, angina, acute MI, heart failure, tachycardia
What are the side effects of Metoprolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Atenolol?
Selective B1 blocker
What are the effects of Atenolol?
Reduces CO
When would you use Atenolol?
Safer than non-selective for COPD and asthma; hypertension, angina, acute MI, heart failure, tachycardia
What are the side effects of Atenolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Acebutolol?
Selective B1 blocker
What are the effects of Acebutolol?
Half life= 3hrs; active metabolite (diacetolol) half life= 8-12hrs; membrane stabilization and ISA
When would you use Acebutolol?
Ventricular arrhythmias
What are the side effects of Acebutolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Esmolol?
Selective B1 blocker
What are the effects of Esmolol?
Short half-life (8-9min)
When would you use Esmolol?
Safer than non-selective for COPD and asthma; IV for hypertensive crisis and acute SVT
What are the side effect of Esmolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Nebivolol?
Selective block of B1; Release of NO > vasodilation
What are the effects of Nebivolol?
Vasodilation
When would you use Nebivolol?
Safer than non-selective for COPD and asthma; hypertension
What are the side effects of Nebivolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Pindolol?
Nonselective Beta antagonist
What are the effects of Pindolol?
IS and membrane stabilization
When would you use Pindolol?
Antihypertensive drug when people have diminished cardiac reserve
What are the side effects of Pindolol?
Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation
What is the MOA of Reserpine?
Blocks ventricular amine transporter
What are the effects of Reserpine?
Reduces SNS activity (storage/release); depletes serotonin and dopamine in CNS
When would you use Reserpine?
Hypertension, used to be used as antipsychotic
What are the side effects of Reserpine?
Hypotension, reflex tachycardia; increase GI/CNS depression; sedation
What is the MOA of Guanethidine?
Displaces NE from storage vesicles; acts as false NT
What are the effects of Guanethidine?
Reduces SNS activity (storage/release)
When would you use Guanethidine?
Hypertension
What are the side effects of Guanethidine?
Hypotension, reflex tachycardia; increase GI/CNS depression; sedation