Adrenergic Drugs Flashcards Preview

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Flashcards in Adrenergic Drugs Deck (23):
1

Prazosin (Minipress)

Alpha-1 Antagonist
Selective alpha-1 blocker
Primary use - antihypertensive
Very little alpha 2 activity means no reflex tachycardia
Induces vasodilation, decreases venous return
Also improves urinary flow
First dose phenomenon - CNS effects the first time its taken

2

Methoxamine

Alpha-1 Agonist
Not a substrate for COMT or MAO — very long half life
Primary use - vasoconstrictor

3

Clonidine

Alpha-2 Agonist
Primary use - Treat Hypertension
Central suppression of BP via action on alpha 2 receptors
Transient spike in BP, followed by prolonged hypotension

4

Reserpine

Sympatholytic
Globally depletes catecholamines
Inhibits amine and dopamine uptake, irreversible
Further blocks NE storage and synthesis
Extremely long acting (weeks)

Side Effects: significant CNS effects (depression, sedation, suicide)

5

Propanalol

Nonselective Beta-1 and Beta-2 antagonist
Primary uses - antihypertensive, heart disease (via decreasing HR)
At rest has little effect on a normal heart
Also treats glaucoma (via decreasing intraocular pressure)
Can reduce peripheral symptoms of hyperthyroidism

Side Effects: bronchoconstriction due to beta 2 antagonist action. Should not be used in patients with underlying lung disease
Also can cause profound hypoglycemia in diabetics
Membrane stabilizing effect, reduces membrane excitability

6

Phentolamine

Alpha Antagonist
Nonselective competitive alpha blocker
Primary use - pheochromocytoma
Poor antihypertensive because it induces reflex tachycardia
Also used in erectile dysfunction

Side Effects: orthostatic hypotension, reflex cardiac stimulation, nasal congestion

7

Phenylephrine

Alpha-1 Agonist
Not a substrate for COMT — long half life
Primary use - VASOCONSTRICTOR
Treat hypotension
Nasal decongestant

8

Phenoxybenzamine

Alpha Antagonist
Covalent, irreversible nonselective alpha blocker
May take days to recover alpha activity
Primary Use - treatment of PHEOCHROMOCYTOMA
Also used in benign prostate hypertrophy

Side Effects: orthostatic hypotension, nasal congestion, ejaculatory dysfunction

9

Ephedrine

Mixed Acting Adrenergic Agonist
Indirectly induces NE release, direct alpha/beta agonist
Primary Use - bronchodilation (mostly displaced by beta 2 selectives), urinary incontinence (promotes retention), appetite suppression

10

Cocaine

Prevents uptake from removing NE from the synaptic cleft, prolonging signaling

11

Terbutaline/Albuterol

Beta-2 Agonist
Not a substrate for COMT or MAO — very long half life
Primary use - BRONCHODILATOR
Better than non-selective beta agonists because they do not cause cardiac stimulation, unless you use too often
Inhibit mast cell secretion
Inhalation limits side effects

12

Methyl Tyrosine

NE Synthesis Inhibitor
Inhibits tyrosine hydroxylase, resulting in global catecholamine decrease
Blocks tyrosine —> L-DOPA conversion
Primary use - pheochromocytoma
Given pre-operatively to reduce risks when excising pheos

Side effects: sympathetic depression

13

Metroprolol

Cardioselective Beta-1 blocker
Primary uses - antihypertensive, ischemic heart disease (via decreasing HR)
At rest has little effect on a normal heart
Does not cause bronchoconstriction

14

Beta-2 Agonists

Bronchodilators

15

Alpha-1 Agonists

Vasoconstrictor
Treat hypotension, stimulate mydriasis, rhinitis (used as a decongestant)

16

Dobutamine

Beta-1 Agonist
Primary use - INOTROPE
Treat Congestive Heart Failure, increase cardiac contractility
Also promotes vasodilation
Side effects - tolerance may develop

17

Beta-3 Agonists

Treat urinary urgency or overactive bladder

18

Amphetamine (Vyvanse, Adderal)

Indirect Adrenergic Agonist
Enhances NE release and acts as a powerful CNS stimulant
Primary use - SCHEDULE I, but reduces fatigue, increases alertness, improves physical performance

Side Effects: appetite suppression, dependency, tolerance

19

Beta-1 Agonists

Vasodilator, treat congestive heart failure
Stimulate cardiac contractility
Dilates renal vasculature

20

Metraminol

Mixed Acting Adrenergic Agonist
Indirectly replaces NE in storage granules, direct alpha 1 agonist
Primary use - treat hypotension

21

Methyldopa

NE Synthesis Inhibitor
False neurotransmitter, displaces NE and binds with much lower affinity
Converted to alpha methyl norepinephrine in the body
Primary use - antihypertensive, probably via action on central alpha 2 receptors (similar to clonidine)

Side effects: CNS effects including sedation, drowsiness
Also sympathetic depression (orthostatic hypotension, nasal congestion, etc)

22

Alpha-2 Agonists

Vasodilator
Anti-hypertensive, treat hypertensive crisis

23

Guanethidine

Sympatholytic
Displaces NE from storage vesicles and exposes them to degradation by MAO. Also interferes with vesicle release
Primary use - strong antihypertensive. Vasodilator
Good oral availability with long half life

Side Effects: orthostatic hypotension, GI upset & diarrhea, male sexual disturbance