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Adrenergics Flashcards

1
Q

Sympathomimetics

A

Adrenergic Agonists

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2
Q

Sympatholytics

A

Adrengergic antagonists

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3
Q

a1 in Eye

A

Contraction of the radial muscle of iris (mydriasis)

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4
Q

a1 in Arteries, Vein

A

Vasoconstriction

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5
Q

a1 in urinary tract of male

A

Constriction of sphincter

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6
Q

a1 in vas deferens

A

Ejaculation

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7
Q

a2 in pre-syaptic nerve terminals

A

inhibits NT release

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8
Q

a2 in CNS

A

Sympathetic outflow to vessel inhibition

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9
Q

Classes of Adrenergic Agonists

A 
Direct-acting
-Catecholamines
-Non-catecholamines
Indirect acting
-Indirect only
-Mixed activity
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10
Q

Base structure of agonist

A

Phenylethylamine

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11
Q

Importance of catecholamine structure

A

3,4 hydroxylation of phenyl group (catechol group) improves affinity for maximal alpha, beta receptors

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12
Q

Factors affecting affinity for agonists

A

2 carbons b/w aromatic ring and amino group affords greatest sympathomimetic activity
Substitution of alkyl group on the amino group tends to increase beta activity

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13
Q

Features influence bioavailability/metabolism

A

Absence of one or both -OH on phenyl increases oral effectiveness
Substitution on alpha-carbon makes the compound more resistant to MAO
Substitution of -OH group on beta carbon decreases lipid solubility and decreases CNS actions, increases peripheral activity

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14
Q

Metabolism of catecholamines

A

Metabolized by MAO and catechol-O-methyltransferase
Not effective by oral administration
Must be given parenterally to avoid liver
Short half life (minutes)

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15
Q

Predominant role of catecholamines

A

CV actions

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16
Q

Norepinephrine - Receptor selectivity

A

Alpha1/2,Beta1

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17
Q

Norepinephrine - CV Effects

A

Alpha-1 primarily
Increases peripheral vascular restriction (PVR)
Increases mean BP
Reflex towards bradycardia (Decreased HR)

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18
Q

Norepinephrine - Therapeutic uses

A

Vasoconstrictor in certain acute care situations (shock)

Elevate BP during reduced sympathetic tone (examples: neurological injury, spinal anesthesia)

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19
Q

Epinephrine - Receptor selectivity

A

All major receptors (alpha-1/2,beta-1/2)

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20
Q

Epinephrine - CV Effects

A

Increase HR, contractile force, cardiac output
Increase systolic BP, decrease diastolic BP
Vasoconstriction except in skeletal muscle beds so net PVR decrease (Beta-2)

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21
Q

Epinephrine - Respiratory effects

A

Bronchodilation

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22
Q

Epinephrine - Metabolic effects

A

Hyperglycemia

Increase free fatty acids

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23
Q

Epinephrine - Therapeutic uses

A

Hypersensitivity reaction - Allergies, bronchoconstriction
Increase duration of action of local anesthetics
Bradyarrhythmias
Opthalmic uses - Mydriatic so decreases hemorrhage and conjunctival congestion

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24
Q

Dose dependence of Epi on PVR

A

Low concentration of epi results in B2 vasodilation
High concentration of epi, B2 is saturated so binds to A1 resulting in vasoconstriction
At high concentration CV effects becomes the same as norepi

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25
Isoproterenol - Receptor selectivity
B1/2
26
Isoproternol - CV Effects
Decrease PVR Increase HR, contractile force, CO Decrease mean BP
27
Isoproternol - Respratory effects
Bronchodilation
28
Isoproternol - Therapeutic uses
Emergency use for treatment of bradycardia or heart block
29
Dopamine - CV effects
``` Low dose (0.5 ug/kg/min) Renal dose - Dilation of renal and mesenteric arteries, decreasing PVR, increase renal flow (D1 receptor) Intermediate dose (5-10 ug/kg/min) Cardiac dose - Increases HR, contractile force, CO (D1 + B1) High dose (10-20 ug/kg/min) Pressor dose - Vasoconstriction and increased PVR (D1 + B1 + A1)Used in coronary care settings ```
30
Dobutamine racemic effects
(-) : A1 agonist, B agonist (+) : A1 antagonist, B agonist Net result: B1 agonist
31
Dobutamine CV effects
Increased HR, contractility, CO | Minimal change in PVR and BP
32
Dobutamine Therapeutic uses
Short-term treatment of cardiac decompensation (cardiac surgery, heart failure, MI) Cardiac stress testing
33
B1 - Heart response
Increased HR, contractile force, AV nodal conduction velocity
34
B1 - Kidney response
Renin release
35
B2 - Artery (Skeletal, cardiac muscle) response
Dilation
36
B2 - Bronchi response
Dilation
37
B2 - Skeletal muscle response
Glycogenolysis
38
B2 - Liver response
Glycogenolysis, gluconeogenesis
39
D1 Receptor response
Arteries (kidney, mesentery) - Dlation
40
Methyldopa - Metabolism and receptors
Orally active pro-durg (Catecholamine Agonist) Metabolized in nerve terminals to alpha-methyldopamine, alpha-methylnorepi, which are stored and released with nerve stimulation A2 receptor agonists, and stimulate central A2 receptors to reduce sympathetic outflow
41
Methyldopa - Major therapeutic use
HTN | Especially gestational HTN, has no effect on fetus
42
Methyldopa - Side effects
From CNS penetration | Sedation, dry mouth, edema, rebound HTN if discontinued
43
Where does methyldopa target for decreased sympathetic outflow?
CNS | PNS would not have the CV effects
44
Phenylephrine - Target and CV effects
A1 adrenergic recepetor agonist Increase systolic and diastolic BP, PVR Reflex decrease in HR Decrease flow in most vascular beds
45
Phenylephrine - Therapeutic uses
Opthalmic: Mydriatic Nasal decongestant: Oral or nasal spray Adminster with local anesthetics to increase duration of action Treatment of HTN
46
Similar drug to phenylephrine
Midodrine
47
Clonidine - Target
A2 adrenergic receptor Orally active
48
Clonide - Therapeutic Use, CV effect
Anti-HTN by CNS: Activates central A2 receptors decreasing sympathetic outflow (Hypothalamus and medulla) Prolonged BP lowering Decreases PVR, HR, CO
49
Clonide - Adverse effects
Dry mouth, sedation (50% of patients), edema, rebound HTN
50
Albuterol - Therapeutic use
Bronchodilator - Asthma
51
Albuterol - Adverse effects
Tremor, anxiety, tachycardia
52
Salmeterol - Target and kinetics
B2 adrenergic receptor agonist Long duration of action: 12h Aryl alkyl (11 carbons) substitution makes the compound lipophilic
53
Salmetrol - Therapeutic use
COPD, nocturnal or persistent asthma | Too slow for acute bronchospasm (asthma attack)
54
Tyramine - Function
Indirect only agonist in presence of MAO inhibitors - Metabolized in liver, no effect In presence of MAO inhibitors - Reaches axon synapse and encourages monoamine release (dopamine, norepi, epi), can lead to HTN
55
Example of mixed acting sympathomimetics
Amphetamine Methamphetamine Ephedrine/Pseudoephdrine
56
Amphetamine - Target and effects
CNS stimulant in addition to peripheral alpha/beta action Depresses appetite Effective after oral administration (long half-life) Releases NE from adrenergic nerves, weak direct alpha/beta agonist, competes with NET
57
Amphetamine - Therapeutic uses
Narcolepsy | ADD
58
Ephedrine - Targets and metabolism
Direct agonist of alpha/beta receptors, release NE Orally active CNS stimulation
59
Ephedrine - Usage
Previously for asthma | Found in some herbal supplements but now banned by FDA
60
Pseudoephedrine - Targets
Direct A1 agonist, minor B2 activity | Less CNS stimulation
61
Pseudoephedrine - Therapeutic use
OTC Nasal Decongestant (Oral, Spray) | Sale is now limited due to illegal use in synthesis of methamphetamine
62
General Side Effects/Toxicity of Sympathomimetics and Receptor cause
Throbbing headache - Alpha (vasoconstriction) Increased heart rate, palpitations - Beta Pericardial pain - Beta (Angina due to increased HR) Cardiac arrhythmias - Beta Cerebral hemorrhage - Alpha (Increased BP) Restlessness, anxiety - Both
63
Definition of Adrenergic Neuron Blockers
Agents that block the synthesis, storage or release of norepinephrine
64
Guanethidine and Guanadrel - Target and Kinetics
Orally active, long acting Taken up into adrenergic nerves via NET Inhibit NE relase and deplete neuronal amine stores
65
Guanethidine and Guanadrel - Therapeutic use and side effects
Therapeutic for severe HTN | Can cause orthostatic hypotension, male sexual dysfunction, diarrhea, muscle weakness, edema
66
Reserpine - Target and Kinetics
Diffuses into adrenergic neurons and depletes NE stores by inhibiting VMAT2
67
Reserpine - Therapeutic use and side effects
Therapeutic: essential HTN Can cause sedation, depression (suicidal tendencies), Diarrhea, Orthostatic hypotension, Increased gastric acid secretion
68
Definition of Adrenergic Receptor Antagoinists
Agents whose effects are produced by inhibiting either alpha and/or beta receptors Blocks both endogenous and exogenous catecholamines Targets specific receptor response May affect NE release from adrenergic neurons
69
Non-selective Alpha Adrenergic Receptor Antagonist
Both alpha receptors
70
Overview of phenoxybenzamine
Irreversible non-selective alpha antagonist Orally active, long duration Produces vasodilation proportional to degree of sympathetic tone
71
Overview of phentolamine
Competitive, reversible non-selective alpha agonist Orally active, shorter duration (2-4 h) Block can be overcome (competitive kinetics)
72
Therapeutic use of non-selective alpha antagonist
HTN (phentolamine only) - Cases refractory to other treatments, an only in combination with other agents HTN with pheochromocytoma (Both) Reverse or shorten duration of anesthesia produced by a combination of local anesthetic and sympathomimetic (phentolamine)
73
Side effects of non-selective alpha antagonist
Tachycardia Edema Orthostatic hypotension
74
Prazosin - Overview
A1 Competitive Adrenergic Antagonist Orally active Little blockade of pre-synaptic A2 receptors so minimal tachycardia, CO increase Decrease vascular tone in resistance (aa.) and capacitance (vv.) beds Produces favorable effects on lipid profile
75
Prazosin - Therapeutic uses
HTN Short-term treatment of CHF Urination problems with benign prostatic hyperplasia (BPH)
76
Prazosin - Side effects
First dose phenomenon - hypotension and syncope 30-90 mins after 1st dose Orthostatic hypotension Edema
77
Tamsulosin - Overview
Orally active A1 adrenergic receptor antagonist (favors A1A in prostate over A1B in blood vessels)
78
Tamsulosin - Therapeutic use
Urination problems with BPH | Little effect on BP or HTN
79
Overview of beta-blockers
Beta-blocking selectivity Minor actions: Partial agonists, local anesthetic or quinidine-like activity, some A1 selective as well, can be vasodilating
80
Location of clinically relevant beta receptors
``` Heart Bronchial Smooth Muscles Kidney (renin) Skeletal muscle Blood vessels supplying skeletal muscle Liver ```
81
Propranolol - Overview
Non-selective beta competitive, reversible antagonist | Orally active - substantial first-pass metabolism
82
Propranolol - Therapeutic uses
``` HTN Angina pectoris Cardiac arrhythmias Acute MI Pheochromocytoma Migraine prophylaxis ```
83
Propranolol - Side effects
Cardiac depression, bradycardia/heart block Bronchoconstriction Sedation, impotence, nightmares Mask hypoglycemia
84
Propranolol - Careful in patients with
``` Asthma CHF Bradyarrhythmias, AV block Insulin-dependent diabetes: hypoglycemic episodes Hypotension Vasospastic angina ```
85
Timolol - Overview
Non-selective beta adrenergic receptor antagonist | Orally active
86
Timolol - Therapeutic uses
Similar to propranolol Also widely used in the treatment of wide-angle glaucoma Decreases aqueous humor formation by the ciliary epithelium, leading to decreased intraocular pressure Does not affect pupil size or accomodation Administered as eye drops Small amounts can be absorbed into sytemic circulation
87
Metoprolol - Overview
B1-selective competitive, reversible antagonist 10-fold selectivity for B1 at low doses Cardioselective, 2nd generation beta-blocker
88
Metoprolol - Therapeutic usesH
Similar to propranolol | Also used for CHF
89
Metoprolol - Side effects
Similar to propranolol | Less bronchoconstriction
90
Atenolol - Overview
B1-selective, orally active, once per day dosing Does not penetrate into CNS, less side effects Therapeutic similar to propranolol except for migraine prophylaxis
91
3rd Generation Beta Blockers
Antagonists with additional CV effects due to A1 selectivity
92
Labetolol
Competitive, reversible antagonist of a1, beta | Therapeutic use for essential HTN (orally) and HTN crisis (IV)
93
Carvedilol
Competitive, reversible antagonist of a1, beta | Therapeutic use for CHF, acute MI
94
Albuterol - Target and Kinetics
B2 adrenergic receptor agonist Short acting: 3-6 h after inhalation Primarily taken as inhalant, but also available as oral tablet

PDA Block 1 (13 decks)

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