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26 Cards in this Set
- Front
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Epinephrine Receptors: Agonist or Antagonist Cardiovascular Effects: high/low dose Respiratory Effects: Administration and excretion: Therapeutic uses: |
-a1, a2, B1, B2 AGONIST -high dose: potent vasopresso, rapid increase in BP (a1), increase HR, contractile force and CO (B1) -low dose: cause vasodilation, decrease diastolic BP (B1) increase HR and contractility, increase systolic BP (B1) no increase in MAP -Bronchodilation -parenteral admin, short half-life -hypersensitivity reactions, increase duration of action of local anesthetics |
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Norephinephrine Receptors: Agonist or Antagonist Cardiovascular Effects: Administration and excretion: Therapeutic uses: |
-a1, a2, B1 AGONIST -increase peripheral vascular resistance (a1), increase blood pressure (a1), cause reflex bradycardia (overcoming B1 effects) -parenteral admin, short half-life -vasoconstrictor under certain intensive care situations (shock and hypotension due to reduced sympathetic tone) |
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Dopamine Receptors: Agonist or Antagonist Cardiovascular Effects: low/intermediate/high Administration and excretion: Therapeutic uses:
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-D1, B1, a1 AGONIST -low dose: "renal dose"-dilate renal and mesenteric arteries, D1 decreases periph vascular resistance -intermediate dose: "cardiac dose"- increase HR (B1), contractile force (B1), and CO (B1) (D1 +B1) -high dose: "pressor dose"- vasconstriction and increase peripheral vascular resistance (D1+B1+a1) -IV admin, dose titrated, short half life -used for severe decompensated heart failure, shock |
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Isoproterenol Receptors: Agonist or Antagonist Cardiovascular Effects: Respiratory Effects: Administration and excretion: Therapeutic uses: |
nonselective B adrenergic receptor agonist -B1, B2 AGONIST - Decrease PVR (B2), Increase HR, contractile force and CO (B1), Decrease mean BP (systolic goes up (B1) but diastolic comes down (B2)) -Bronchodilation (B2) -brief duration, metabolized by COMT -emergency use to stimulate heart during bradycardia or heart block |
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Dobutamine Receptors: Agonist or Antagonist Cardiovascular Effects: Administration and excretion: Therapeutic uses: |
-racemic mixture, overall B1 AGONIST -increased HR, contractility, and CO (B1) [minimal change in PVR and BP] -metabolized rapidly, short half-life -SHORT-TERM treatment of cardiac compensation, cardiac stress testing |
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Albuterol Receptors: Agonist or Antagonist Administration and excretion: Therapeutic uses: Adverse Effects: |
- Selective B2 adrenergic AGONIST -Cause bronchodilation (B2) (conteracts bronchoconstriction seen in asthma) -Can be given via inhalation or orally -Short acting (3-4 hrs) and rapid onset (~15min) -Adverse effects include tachycardia, anxiety, and tremors (vasodilation gets into periphery and causes increase rebound increase HR) |
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Salmeterol Receptors: Agonist or Antagonist: Administration and excretion: Therapeutic uses:
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-Selective B2 adrenergic AGONIST -Causes bronchodilation (B2) -Used for pts with COPD or severe asthma -Long-lasting (12 hours), slow onset -Must be inhaled |
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Phenylephrine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses:
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-selective a1 adrenergic AGONIST - increases systolic and diastolic BP (a1), reflex decrease in HR due to high BP, decrease flow in most vascular beds (a1) -eyedrops, nasal spray, IV admin -ophthalmic uses: mydriatic, decrease hemorrhage nasal decongestant: oral or nasal spray (vasoconstrict nasal mucosal, decrease swelling) use with local anesthetics to increase duration of action treatment of severe hypotension
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Clonidine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse Effects: |
-selective a2 adrenergic AGONIST -works as an anti-hypertensive (decreases sympathetic outflow by targeting central a2 receptors) - decrease HR, contractility, CO -orally active/administered -dry mouth and sedation common, also sexual dysfunction, bradycardia, edema, rebound hypertension with sudden discontinuation (due to loss of sympathetic outflow) |
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Methyldopa Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: |
-orally active prodrug -metabolized in nerve terminals to a-methyldopamin and a-methylNE, both of which are potent a2 agonists -bind to central a2 and reduce sympathetic outflow -anti-hypertensive -orally administered -dry mouth and sedation common, also sexual dysfunction, bradycardia, edema, rebound hypertension with sudden discontinuation (due to loss of sympathetic outflow) |
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Tyramine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: |
-found within the diet -causes the release of NE, causing sympathomimetic actions -is metabolized by MAO, so pts on MAO inhibitors have a build up of tyramine, causing a release of NE and can have a HTN crisis |
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Amphetamine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: |
-powerful CNS stimulant -effective with oral administration, long half-life -causes the release of NE and Dopamine from nerve terminals -CNS stimulant, depresses appetite, stimulates respiratory center -phycological dependence can develop -therapeutically used from narcolepsy and ADHD |
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Psuedoephedrine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: |
-strong a1 agonist, some B2 agonist activity -orally effective (minimal CNS stimulation) -used as an oral decongestant (a1 causes vasoconstriction to reduced swelling of nasal mucosa)
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Adrenergic Neuron Blockers |
drugs that disrupt adrenergic neuron function by inhibiting the storage, synthesis, or release of NE |
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Guanethidine and Guanadrel Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
Adrenergic neuron blocker -inhibit NE release and deplete neuronal amine stores -orally administered -long acting -taken up via NET, deplete stores of NE -inhibited by tricyclics that inhibit NET -treats severe hypertension -side effects: orthostatic hypotension, male sexual dysfunction, diarrhea, muscle weakness, edema (all due to decrease NE) |
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Reserpine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
Adrenergic neuron blocker -diffuses into adrenergic neurons -inhibits VMAT (can't gets dopamine into vesicles) -treats hypertension -can enter the CNS--> can cause depression and sedation -side effects: diarrhea, orthostatic hypotension, increased gastric acid secretion |
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Phenoxybenzamine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
-nonselective a adrenergic ANTAGONIST -blocks a1 and a2 receptors -IRREVERSIBLE ANTAGONIST -orally active, long duration of action -used for catecholamine secreting tumors (pheochromocytoma) -adverse effect: hypotension (block a1), reflex cardiostimulation (a2 is blocks, can't down regulate NE release, so more NE release, more B1 stimulation) |
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Phentolamine Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
-nonselective a adrenergic ANTAGONIST -blocks a1 and a2 receptors -competitive, reversible antagonist -orally active, shorter duration (2-4hrs) -used for catecholamine secreting tumors (pheochromocytoma) -adverse effect: hypotension (block a1), reflex cardiostimulation
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Prazonsin Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
-selective a1 ANTAGONIST -decreases vascular tone in arteries and veins (lower BP) -produces favorable effect on lipid profile (decrease LDL, increase HDL) -orally active -treats HTN, short-term treatment of CHF, difficulty urinating -adverse effects: "first-dose" phenomenon (syncope upon first dose) and orthostatic hypotension |
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Tamsulosin Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
-selective a1 ANTAGONIST -favors blockade of a1A receptors in prostate -treats benign prostatic hyperplasia (BPH) (relaxes the sphincters to increase flow) with little effects on BP -orally active
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Propranolol Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
"first-generation" -non-selective B adrenergic ANTAGONIST -antagonist of both B1 and B2 receptors -orally available, large first pass effect, short half-life -used for hypertension, angina, certain cardiac arrhythmias, MI, migraine prophylaxis |
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Timolol Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
"first generation" -non-selective B adrenergic ANTAGONIST -B1 and B1 antagonist -used for hypertension, angina, certain cardiac arrhythmias, MI, migraine prophylaxis, also for wide angle glaucoma (reduce aqueous humor) |
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Metoprolol Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
"seconds-generation" -bioavailable B1-selective ANTAGONIST -used for hypertension, angina, certain cardiac arrhythmias, MI, migraine prophylaxis -also used to treat heart failure -less bronchoconstriction at lower doses |
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Atenolol Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
"second generation" -orally bioavailable B1 ANTAGONIST -longer duration of action (1x day dose) -does not penetrate CNS (less side effects) -used for hypertension, angina, certain cardiac arrhythmias, MI, migraine prophylaxis -less bronchoconstriction at lower doses |
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Labetalol Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
"third-generation" -a1, B1, B2 ANTAGONIST -treats essential hypertension (oral) and hypertensive emergencies (IV)
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Carvedilol Receptors: Agonist or Antagonist: Effects: Administration and excretion: Therapeutic uses: Adverse effects: |
"third-generation" -a1, B1, B2 ANTAGONIST -anti-oxidant properties and anti-inflammatory effects -blocks L-type Ca2+ channels at higher doses -used for hypertension, heart failure, MI |
