Exam #02 - Adrenergic Agonists and Antagonists and Anti-hypertensive Agents Flashcards
Phenylephrine
Type: Direct-acting Adrenergic agonist
Selectivity: Alpha-1 selective
MOA:
powerful post-synaptic alpha-receptor agonist producing vasoconstriction
Major Therapeutic Use:
nasal decongestant
ophthalmic solutions for mydriasis
AE:
high doses can cause hypertensive HA and heart irregularities
Clonidine
Brand Name: Catapres
Type: Direct-acting Adrenergic agonist
Selectivity: Alpha-2 selective
Major Therapeutic Use:
hypertension
MOA: stimulates alpha-2 adrenergic receptors in the brain resulting in reduced sympathetic outflow from the CNS and decreased peripheral resistance, renal vascular resistance, HR, and BP
Notes:
2 similar drugs: Guanabenz & Guanfacine
Dobutamine
Type: Direct-acting Adrenergic agonist
Selectivity: Beta-1 selective
MOA:
stimulates beta-1 receptors in heart
Major Therapeutic Use:
increase CO and cardiac contractility to treat CHF
Terbutaline
Type: Direct-acting Adrenergic agonist
Selectivity: Beta-2 selective
Isoproterenol
Type: Direct-acting Adrenergic agonist
Selectivity: Non-selective Beta agonist
Epinephrine
Type: Direct-acting Adrenergic agonist
Selectivity: Non-selective agonist
MOA:
activates both alpha and beta receptors
Major Therapeutic Use:
anaphylaxis, asthma, cardiac arrest, glaucoma,
cardiac stimulant (inotropic & chronotropic), potent vasoconstrictor, increase duration of LA for nerve block (give LA with epi constricts adjacent vessels and forms pocket), control of local bleeding (esp for facial surgery)
NE
Type: Direct-acting Adrenergic agonist
Selectivity: Non-selective agonist (hits all but beta-2)
MOA:
a sympathomimetic amine alpha activity results in peripheral vasoconstriction and beta activity leading to inotropic stimulation of the heart and coronary artery vasodilation
Major Therapeutic Use:
hypotension
cardiac arrest
Ephedrine
Type: Indirect/Mixed adrenergic agonist
Selectivity: Non-selective agonist
MOA: releases stored catecholamines (namely NE) increasing activity on adrenergic receptors
Major Therapeutic Use:
nasal decongestant, weight loss products
Notes:
found in Ma Huang plant
can cross BBB
Amphetamine
Type: Indirect Adrenergic agonist
MOA: stimulates release of NE, DA, and serotonin by impairing VMAT - more DA gets released into cytosol and gets pushed out into the synapse (some gets metabolized in cytoplasm before it’s released)
appetite suppressant and CNS stimulant
Major Therapeutic Use:
derivatives of amphetamine are used to treat ADHD and narcolepsy
AE:
toxicity due to excess beta receptor stimulation of the heart
Tyramine
Type: Indirect Adrenergic agonist
MOA:
stimulates the release of catecholamine (namely NE)
AE:
Tyramine is found in fermented foods (cheese, sausage, pickled fish, wine). If patient ingests these foods and is also taking a MAO inhibitor, there will be an increase in [NE] which can lead to a hypertensive crisis
Cocaine
Type: Indirect-acting Adrenergic agonist
Therapeutic Use: LA, vasoconstriction, peripheral sympathomimetic actions
MOA: inhibits reuptake of NE, DA, and serotonin by working at the DAT and NET
AE:
toxicity due to beta-receptor stimulation of heart
abuse mainly related to inhibition of DA reuptake
Reserpine
MOA: Irreversibly binds to VMAT stopping the packing of NE and DA into vesicles. Reduces sympathetic output, decreases HR and arterial BP
Major Therapeutic Use:
hypertension
psychotic disorder
Would direct acting adrenergic agonists be impacted by prior treatment with reserpine?
No, responses may actually be potentiated by reserpine (and cocaine)
Would mixed acting adrenergic agonists be impacted by prior treatment with reserpine?
Yes, b/c ephedrine is still acting on post-synaptic receptors, the response would be reduced
Would indirect acting adrenergic agonists be impacted by prior treatment with reserpine?
Yes, responses are abolished b/c stores of NE and DA have been depleted